Download Running head: PERSONAL DRUGS PERSONAL DRUGS Personal

Document related concepts

Discovery and development of direct Xa inhibitors wikipedia , lookup

Discovery and development of proton pump inhibitors wikipedia , lookup

Drug design wikipedia , lookup

Discovery and development of cyclooxygenase 2 inhibitors wikipedia , lookup

Plateau principle wikipedia , lookup

Pharmacognosy wikipedia , lookup

Bad Pharma wikipedia , lookup

Medication wikipedia , lookup

Pharmaceutical industry wikipedia , lookup

Discovery and development of direct thrombin inhibitors wikipedia , lookup

Neuropsychopharmacology wikipedia , lookup

Prescription costs wikipedia , lookup

Psychopharmacology wikipedia , lookup

Ofloxacin wikipedia , lookup

Bilastine wikipedia , lookup

Pharmacokinetics wikipedia , lookup

Neuropharmacology wikipedia , lookup

Pharmacogenomics wikipedia , lookup

Dydrogesterone wikipedia , lookup

Drug interaction wikipedia , lookup

Transcript
Running head: PERSONAL DRUGS
1
Personal Drugs
Leah Fite
Wright State University
PERSONAL DRUGS
2
Personal Drugs
First Diagnosis: Community Acquired Pneumonia in the patient with Chronic Obstructive
Lung Disease (COLD)
78 year old male reports to emergency department with complaints of sudden onset of
dyspnea, chills, cough with rust-colored sputum production, fever, fatigue and weakness. Vital
signs are HR: 128bpm, BP 102/78, RR: 30bpm, O2 saturation: 89% on room air. Significant
past medical history includes hypertension, hyperlipidemia, COLD, and smoking with reported 1
pack per day (ppd). Chest radiography reveals pleural effusions and right lower lobe patchy
infiltrates. Physical exam reveals inspiratory crackles with increased tactile fremitus. Patient
reports allergy to penicillin, causing a rash. Sputum culture and blood cultures are obtained and
sent.
I.
Definition of Diagnosis
Pneumonia is a lower respiratory tract infection that involves aspiration of secretions or
inhalation of microorganisms released from other infected individuals, which then activates the
immune response causing vascular edema and alveolar filling, impairing gas exchange (Brashers,
2010). Different microorganisms are responsible for community-acquired pneumonia than those
acquired in the hospital, and tend to be less severe in nature, depending on the presence of
immunosuppression and comorbidities (Brashers, 2010). Diagnosis is based on the presence of
cough with sputum production, fever, and pleuritic chest pain, and supported by chest
radiography which aids in differentiating pneumonia from other causes of similar symptoms such
as bronchitis (Mandell et al., 2007).
II. Therapeutic Objective
The goal of therapy is to resolve the disease by eliminating the infecting organism
through appropriate antimicrobial treatment (Mandell et al., 2007). Current recommendations
suggest initiating antibiotic therapy while still in the emergency department. Due to the length of
time for cultures to result, empiric antibiotic therapy is the mainstay for treatment. Knowledge
of susceptibility and prediction of the most likely pathogen based on patient history and current
symptoms assists in selection of the appropriate empirical therapy (Mandell et al., 2007). Once
cultures are resulted, antibiotic therapy can be narrowed to the most appropriate antibiotic
specific to the microorganism. Antibiotic therapy should be continued for five to ten days, and
the patient should remain afebrile for 48-72 hours before antibiotics are discontinued (Mandell et
al., 2007).
III. Effective Drug Groups
Drug Classification
Macrolides
Efficacy
Pharmacodynamics:
Safety
Side Effects:
Suitability
Contraindications:
PERSONAL DRUGS
(Azithromycin,
Clarithromycin,
Erythromycin,
Fidaxomicin,
Spiramycin)
Azithromycin
(Azithromycin,
Intravenous)
500mg (1): $8.92
Erythromycin
(Erythrocin
Lactobionate,
Intravenous)
500mg (1): $34.66
100mg (1): $45.06
(Lexicomp, 2014)
3
Inhibits RNAdependent protein
synthesis at the
chain-elongation
step; blockage of
transpeptidation by
binding to 50S
ribosomal subunit.
Bactericidal. Grampositive coverage.
Pharmacokinetics:
Distribution:
extensive tissue,
skin, lungs, sputum,
tonsils, and cervix;
decreased to relative
diffusion from blood
into CSF (25% in
inflamed meninges)
Protein binding:
concentration
dependent 7-70%
Metabolism:
demethylation via
hepatic CYP3A4
Half-life
elimination: 1.5-2
hours. End-Stage
Renal Disease: 5-6
hours
Excretion: primarily
urine; Azithromycin:
biliary
(Lexicomp, 2014)
Common: Diarrhea,
pruritus, rash, abdominal
pain, cramping,
vomiting, vaginitis
Rare: Acute renal
failure, arrhythmia,
arthralgia,
bronchospasm, chest
pain, facial edema,
hearing loss, hepatitis,
interstitial nephritis,
pancreatitis, neutropenia
(mild), QTc
prolongation, StevensJohnson syndrome,
thrombocytopenia,
torsade de pointes,
vertigo
Monitor: Liver function
tests, CBC with
differential
(Lexicomp, 2014)
Hypersensitivity to any
macrolide antibiotics,
history of cholestatic
jaundice/hepatic
dysfunction associated
with prior use; history of
QT prolongation or
arrhythmia; concomitant
use with cisapride,
pimozide, ergotamine,
dihydroergotamine,
HMG-CoA reductase
inhibitors, terfenadine;
concomitant use with
colchicines in patients
with renal or hepatic
impairment
Disease-related
precautions: Use with
caution in patients with
pre-existing liver disease
or hepatic impairment.
Use with caution in
patients with
Myasthenia Gravis,
exacerbation may occur.
Dosage adjustment with
severe renal impairment
Drug-drug interactions:
Avoid alcohol and St.
John’s Wort. Avoid
concomitant use with
BCG; Bosutinib;
Cisapride; Conivaptan;
Disopyramide; Fusidic
Acid; Highest Risk
QTc-prolonging agents;
Ibrutinib; Ivabradine;
Lincosamide antibiotics;
Lomitapide; Lovastatin;
Mifepristone; Pimozide;
Pomalidomide;
Quinidine; Quinine;
Silodosin; Simeprevir;
Sivmastatin;
Terfenadine; Tolvaptan;
PERSONAL DRUGS
4
Topotecan; Ulipristal
(Lexicomp, 2014)
Respiratory
Fluoroquinolone
(gemifloxacin,
levofloxacin,
moxifloxacin)
Levofloxacin
(Levaquin,
intravenous)
250mg/50 mL
(50mL): $11.64
500mg/100 mL
(100mL): $22.97
750mg/150mL
(150mL): $30.53
Moxifloxacin
(Avelox, intravenous)
400mg/250mL
(250mL): $46.16
(Lexicomp, 2014)
Cephalosporin
(Third Generation)
(Cefotaxime,
Pharmacodynamics:
DNA gyrase
inhibitor and
inhibitor of
topoisomerase IV,
preventing DNA
replication, repair
and transcription.
Bactericidal. Grampositive and gramnegative coverage.
Pharmacokinetics:
Distribution:
Levofloxacin
Vd 74-112L, high
concentrations in
prostate, lung,
gynecologic tissues,
sinus and saliva.
Moxifloxacin Vd
1.7-2.7L/kg, tissue
concentration
exceeds plasma
concentration is
respiratory tissues,
alveolar
macrophages,
abdominal tissues,
uterine tissues and
sinues
Metabolism:
hepatic
Protein binding:
24%-38%
Half-life
elimination: 6-8
hours
Excretion: primarily
urine
(Lexicomp, 2014)
Pharmacodynamics:
Inhibits cell wall
biosynthesis. Lysis
Side Effects:
Common: Headache,
dizziness, rash, diarrhea,
nausea, abdominal pain,
vomiting,
neutropenia/neutrophilia,
thrombocythemia,
transaminases increased,
GGT increased,
increased CPK, pruritus,
vaginitis
Rare: Agranulocytosis,
anaphylactic reaction,
angioedema,
Clostridium difficile
infection, ECG
abnormalities, hemolytic
anemia, hepatic failure,
INR decreased,
interstitial nephritis,
pancytopenia,
pneumonitis, renal
dysfunction, seizure,
Stevens-Johnson
syndrome, thrombotic
thrombocytopenic
purpura, ventricular
tachyarrhythmias
Monitor: CBC, renal
function, liver function,
WBC and signs of
infection
(Lexicomp, 2014)
Contraindications:
Hypersensitivity
reactions to any
formulation of
fluoroquinolones.
Disease-related
precautions: Use with
caution in patients with
significant bradycardia
or acute myocardial
ischemia; May
exacerbate muscle
weakness in Myasthenia
Gravis; Use with caution
in renal impairment; Use
with caution in patients
with rheumatoid
arthritis, may increase
the risk of tendon
rupture; Use with
caution in patients at
risk of seizures
Drug-drug interactions:
Avoid concomitant use
with BCG; Highest risk
QTc-prolonging agents;
Ivabradine;
Mifepristone; Strontium
ranelate; Avoid dong
quai, St John’s Wort
(Lexicomp, 2014)
Side Effects:
Common: Pruritus,
rash, colitis, diarrhea,
Contraindications:
Hypersensitivity to any
cephalosporin
PERSONAL DRUGS
ceftriaxone, cefdinir,
cefditoren)
Cefotaxime
(Claforan, in D5W
intravenous)
1gm/50mL (50mL):
$12.76
2gm/50mL (50mL):
$21.43
Ceftriaxone
(Ceftriaxone Sodium
in Dextrose
intravenous)
20mg/mL (50mL):
$17.03
40mg/mL (50mL):
$40.33
(Rocephin injection)
1g (1): $75.44
500mg (1): $44.88
(Lexicomp, 2014)
Penicillins
(amoxicillin,
ampicillin, cloxacillin,
nafcillin, oxacillin,
penicillin G,
piperacillin,
ticarcillin)
Ampicillin
(Ampicillin Sodium,
Intravenous)
1g (1): $17.91
2g (1): $34.75
10g (1): $84.00
Nafcillin (Nafcillin
Sodium Intravenous)
5
of bacteria.
Extended gramnegative coverage.
Pharmacokinetics:
Distribution:
Widely to body
tissues and fluids
including aqueous
humor, ascitic and
prostatic fluids,
bone; penetrates
CSF when meninges
inflamed
Metabolism:
partially hepatic
Protein binding:
60%-70%
Half-life
elimination: 1.5
hours-9 hours,
increased with renal
or hepatic
impairment
Excretion: primarily
urine (as unchanged
drug and
metabolites)
(Lexicomp, 2014)
Pharmacodynamics:
Inhibits bacterial
cell wall
biosynthesis,
causing cell wall
destruction.
Bactericidal. Grampositive and gramnegative coverage.
Pharmacokinetics:
Distribution: widely
distributed to bile,
blister, and tissue
fluids; poor CSF
penetration
Protein binding:
15%-90%,
depending on agent
nausea, vomiting, pain at
injection site,
eosinophilia,
thrombocytosis,
leukopenia,
transaminase increase
Rare: agranulocytosis,
anaphylaxis, anemia,
basophilia, increased
BUN/creatinine,
gallbladder sludge and
gallstones, hematuria,
lymphocytosis,
monocytosis,
pancreatitis, vaginitis
Monitor: Prothrombin
time. Monitor for signs
of anaphylaxis. CBC
with differential and
renal function with long
course therapy
(Lexicomp, 2014)
formulation
Disease-related
precautions: Use with
caution in patients with
renal and hepatic
impairment, dosage
adjustment may be
required; Use with
caution in patients with
a history of seizure
disorder; Use with
caution in patients with
a history of GI
disease/colitis
Drug-drug interactions:
Avoid concomitant use
with BCG; levels of
ceftriaxone may be
increased by Lactated
Ringers and calcium
salts; May increase
levels of Vitamin K
antagonists
(Lexicomp, 2014)
Side Effects:
Common: nausea,
diarrhea, abdominal
pain, fever, rash,
Stevens-Johnson
syndrome,
Rare: agranulocytosis,
hemolytic anemia,
hepatotoxicity,
interstitial nephritis,
renal tubular damage,
leukopenia, neutropenia,
seizure,
thrombocytopenia
Monitor: Renal, hepatic,
and hematologic
function with long term
use
Contraindications:
Hypersensitivity to any
penicillin formulation
Disease-related
precautions: Use with
caution in patients with
renal impairment,
dosage adjustment may
be required. Avoid use
with infectious
mononucleosis (high
risk for developing
rash).
Drug-drug interactions:
Avoid concomitant use
with BCG. Allopurinol
may increase effects.
PERSONAL DRUGS
1g (1): $17.52
2g (1): $33.99
(Lexicomp, 2014)
Metabolism:
primarily hepatic
Half-life
elimination: 0.6-1.8
hours
Excretion: depends
on agent; feces,
urine
(Lexicomp, 2014)
Pharmacodynamics:
Carbapenems
(doripenem,
Inhibits bacterial
ertapenem, imipenem, cell wall
meropenem)
biosynthesis by
inhibiting the final
Doripenem (Doribax, transpeptidation step
Intravenous)
of peptidoglycan
250mg (1): $25.30
synthesis in bacterial
500mg (1): $46.00
cell walls. Grampositive, gramErtapenem (Invanz,
negative, and
Intravenous)
anaerobic coverage.
1g (1): $84.89
Pharmacokinetics:
Distribution:
Meropenem
penetrates well into
(Intravenous)
most body fluids and
1g (1): $18.48
tissues, including
500mg (1): $9.24
peritoneal and
retroperitoneal
(Lexicomp, 2014)
fluids, gallbladder,
bile, and urine
Metabolism:
hepatic
Protein binding:
85% (depending on
agent)
Half-life
elimination: 1-1.5
hours
Excretion: urine
(~80% as unchanged
drug and metabolite)
(Lexicomp, 2014)
Pharmacodynamics:
Aminoglycosides
(amikacin, gentamicin, Causes defective
kanamycin,
bacterial cell
streptomycin)
membrane by
6
(Lexicomp, 2014)
(Lexicomp, 2014)
Side Effects:
Common: headache,
diarrhea, nausea,
vomiting, abdominal
pain, constipation,
increased hepatic
enzymes, phlebitis, rash,
pruritus, anemia
Rare: anaphylaxis,
arrhythmia, bradycardia,
bronchoconstriction,
Clostridium-difficile
associated diarrhea,
delirium, heart failure,
ileus, leukopenia,
oliguria, neutropenia,
pancreatitis, pneumonia,
renal insufficiency,
seizure, Stevens-Johnson
syndrome,
thrombocytopenia, toxic
epidermal necrolysis,
ventricular tachycardia
Monitor: renal function,
liver function, CBC with
prolonged therapy
Contraindications:
Hypersensitivity to
carbapenem
formulation;
anaphylactic reaction to
beta-lactam antibiotics
Disease-related
precautions: Use with
caution in patients with
renal impairment
(dosage adjustment may
be required)
Drug-drug interactions:
Avoid concomitant use
with BCG and
prebenecid
(Lexicomp, 2014)
(Lexicomp, 2014)
Side Effects:
Common: ataxia,
dizziness, drowsiness,
headache, seizures,
Contraindications:
Hypersensitivity to
aminoglycosides
Disease-related
PERSONAL DRUGS
Gentamicin Sulfate,
Intraveous
10mg/mL (8mL):
$1.79
(Lexicomp, 2014)
Cephalosporins-First
Generation
(cefazolin)
Cefazolin Sodium,
Intravenous
1g (1): $2.64
(Lexicomp, 2014)
7
interfering with
bacterial protein
synthesis. Gramnegative coverage;
gram-positive
coverage in
combination with
vancomycin
Pharmacokinetics:
Distribution:
primarily into
extracellular fluid.
Vd increased by
edema, ascites, fluid
overload; decreased
in dehydration
Protein binding:
30%
Half-life
elimination: 1.5-3
hours; 36-70 in end
stage renal disease
Excretion: urine
(Lexicomp, 2014)
vertigo, erythema,
itching, pruritus,
anorexia, nausea,
splenomegaly, vomiting,
weight loss,
hypocalcemia,
agranulocytosis, anemia,
hepatomegaly, visual
disturbances, hearing
impairment, hearing
loss, tinnitus, increased
BUN/creatinine, distal
tubular dysfunction,
oliguria, renal failure,
dyspnea
Rare: anaphylaxis,
allergic reaction,
laryngeal edema,
respiratory depression,
paresthesia, myasthenia
gravis-like syndrome,
eosinophilia, leukopenia,
thrombocytopenia
Monitor: urinalysis,
urine output, renal
function, plasma drug
levels. Assess for
ototoxicity
(Lexicomp, 2014)
Pharmacodynamics: Side Effects:
Lysis of bacteria due Common: pruritus, skin
to inhibition of
rash, abdominal cramps,
bacterial cell wall
nausea, vomiting,
synthesis. Gramdiarrhea, oral
positive coverage
candidiasis, hepatitis,
Pharmacokinetics:
increased serum
Distribution: widely transaminase, increased
into most tissues and BUN/creatinine, renal
fluids including
failure
gallbladder, liver,
Rare: anaphylaxis,
kidneys, bone,
eosinophilia, leukopenia,
sputum, bile, pleura, neutropenia, seizure,
and synovial. Poor
Stevens-Johnson
CNS penetration
syndrome,
Protein binding:
thrombocytopenia
74%-86%
Monitor: renal function,
precautions: Use with
caution in patients with
pre-existing renal
impairment (dosage
adjustment may be
required); Use with
caution in patients with
pre-existing vertigo,
tinnitus, or hearing loss;
in patients with
hypocalcemia; in
patients with
neuromuscular disorders
Drug-drug interactions:
Avoid concomitant use
with agalsidase alfa,
agalsidase beta, BCG,
gallium nitrate
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to any
cephalosporin
formulation
Disease-related
precautions: Use with
caution in patients with
renal impairment
(dosage adjustment may
be required); use with
caution in patients with
a history of seizure
disorder
Drug-drug interactions:
Avoid concomitant use
with BCG
PERSONAL DRUGS
CephalosporinsSecond Generation
(cefotetan, cefoxitin)
Cefotetan (Cefotetan
Disodium-Dextrose,
Intravenous)
1g 3.58% (1): $17.58
2g 2.08% (1): $25.14
Cefoxetin (Mefoxin,
Intravenous)
1-2 gm/50mL (50mL):
$10.20
2-1.1gm/50mL
(50mL): $19.37
(Lexicomp, 2014)
CephalosporinsFourth Generation
(cefepime)
Cefepime HCl,
Intravenous
1gm/50mL (50mL):
$31.87
2gm/100mL (100mL):
$51.10
(Lexicomp, 2014)
8
Metabolism:
minimally hepatic
Excretion: urine
hepatic function, CBC
periodically through
treatment
(Lexicomp, 2014)
Pharmacodynamics:
Bacterial lysis by
inhibiting bacterial
cell wall synthesis.
Activity against
anaerobes.
Extended gramnegative coverage.
Pharmacokinetics:
Distribution: widely
to body tissues and
fluids such as bile,
sputum, prostatic,
and peritoneal fluid.
Poor CSF
penetration.
Protein binding:
65%-90%
Half-life
elimination: 45
minutes-5 hours
Excretion: primarily
urine
(Lexicomp, 2014)
Pharmacodynamics:
Inhibits bacterial
cell wall
biosynthesis.
Resistant to
hydrolysis of betalactamases. Grampositive and gramnegative coverage.
Pharmacokinetics:
Absorption: rapid
and complete
Distribution: Vd:
16-20L; penetrates
into bronchial
mucosa at levels of
60% of those
(Lexicomp, 2014)
Side Effects:
Common: diarrhea,
increased transaminases,
hypersensitivity reaction
Rare: anaphylaxis,
urticaria, rash, nausea,
vomiting, eosinophilia,
thrombocytosis,
agranulocytosis,
leukopenia,
thrombocytopenia,
prolonged bleeding
times, increased
BUN/creatinine,
neprotoxicity
Monitor: renal, hepatic,
and hematologic
function with prolonged
therapy. Assess
prothrombin time.
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to any
cephalosporin
formulation
Disease-related
precautions: Use with
caution in patients with
renal impairment
Drug-drug interactions:
Avoid concomitant use
with BCG
(Lexicomp, 2014)
(Lexicomp, 2014)
Side Effects:
Common: diarrhea,
nausea, increased serum
ALT & AST, abnormal
PT/PTT, headache,
fever, rash,
hypophosphatemia
Rare: agranulocytosis,
anaphylaxis, colitis,
coma, decreased
hematocrit, electrolyte
disturbances, increased
BUN/creatinine,
leukopenia, neutropenia,
oral candidiasis,
thrombocytopenia
Monitor: monitor renal
Contraindications:
Hypersensitivity to
penicillins,
cephalosporins, or other
beta-lactam antibiotics
Disease-related
precautions: Use with
caution in patients with
gastrointestinal disease
(colitis), renal
impairment, and seizure
disorder (may increase
the risk of seizure).
Drug-drug interactions:
Avoid concomitant use
with BCG
PERSONAL DRUGS
Glyclycycline
(tigecycline)
Tygacil, Intravenous
50mg (1): $104.39
(Lexicomp, 2014)
Lincosamides
(clindamycin,
lincomycin)
Clindamycin
(Clindamycin
Phosphate in D5W,
intravenous)
300mg/50mL (50mL):
$5.50
600mg/50mL (50mL):
9
reached in the
plasma
Metabolism:
minimally hepatic
Excretion: urine
(Katzung, Masters,
& Trevor, 2010)
(Lexicomp, 2014)
Pharmacodynamics:
Bacteriostatic with
some bactericidal
activity. Inhibits
bacterial protein
synthesis by binding
to 30S ribosomal
subunit. Grampositive and gramnegative coverage
Pharmacokinetics:
Distribution: Vd:
7-9 L/kg with
extensive tissue
distribution
Protein binding:
71%-89%
Metabolism:
hepatic
Half-life
elimination: 27
hours with single
dose
Excretion: primarily
feces; urine
(Lexicomp, 2014)
Pharmacodynamics:
Bacteriostatic or
bactericidal
depending on
concentration,
infection site, and
organism. Inhibits
bacterial protein
synthesis by binding
to 50S ribosomal
subunit, preventing
function and serum
electrolytes.
(Lexicomp, 2014)
(Lexicomp, 2014)
Side Effects:
Common: nausea,
vomiting, diarrhea,
headache, dizziness,
rash, hyponatremia,
abdominal pain,
dyspepsia, anemia,
hypoproteinemia,
increased liver enzymes,
infection, abcess,
weakness, increased
BUN, pneumonia,
abnormal healing
Rare: anaphylaxis, acute
pancreatitis, anorexia,
Clostridium difficile
associated diarrhea,
hepatic failure, increased
bleeding times,
increased creatinine,
Stevens-Johnson
syndrome,
thrombocytopenia
Monitor: frequent
monitoring of hepatic
function
(Lexicomp, 2014)
Side Effects:
Common: pruritus, rash,
urticaria, abdominal
pain, diarrhea, nausea,
vomiting,
agranulocytosis,
abnormal liver function
tests, thrombocytopenia
Rare: anaphylaxis, renal
dysfunction,
polyarthritis,
Contraindications:
Hypersensitivity to
tigecycline
Disease-related
precautions: Use with
caution in patients with
hepatic impairment
(dosage adjustment may
be required). Do not use
for healthcare-acquired
or ventilator-associated
pneumonia.
Drug-drug interactions:
No known interactions
where concomitant use
should be avoided. May
increase levels/effects of
warfarin
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to any
lincosamide formulation
Disease-related
precautions: Use with
caution in patients with
hepatic impairment
(dosage adjustment may
be required)
Drug-drug interactions:
Avoid concomitant use
PERSONAL DRUGS
$8.25
(Lexicomp, 2014)
Glycopeptides
(telavancin,
vancomycin)
Vancomycin HCl,
Intravenous
500mg (1): $3.28
1000mg (1): $5.04
5000mg (1): $36.12
(Lexicomp, 2014)
10
peptide bond
formation. Grampositive and gramnegative anaerobic
coverage.
Pharmacokinetics:
Distribution: Vd
2L/kg. High
concentrations in
bone and urine with
no significant levels
in CSF
Metabolism:
hepatic
Half-life
elimination: 2-3
hours
Excretion: primarily
urine; feces
(Lexicomp, 2014)
Pharmacodynamics:
Bactericidal.
Inhibits bacterial
cell wall synthesis
by blocking
glycopeptide
polymerization
through binding to
D-alanyl-Dalanine
portion of cell wall.
Gram-positive
coverage
Pharmacokinetics:
Distribution: Vd:
0.4-1L/kg. Widely
distributed to body
fluids and tissues.
Relative diffusion
into CSF.
Protein binding:
50%
Half-life
elimination: 5-11
hours; prolonged
with renal
impairment
eosinophilia,
neutropenia, erythema
multiforme, exfoliative
dermatitis, StevensJohnson syndrome,
cardiac arrest,
hypotension
Monitor: With
prolonged therapy,
monitor CBC, liver
function, renal function.
Observe for changes in
bowel frequency.
with BCG, erythromycin
(Lexicomp, 2014)
(Lexicomp, 2014)
Side Effects:
Common: hypotension
with flushing,
erythematous rash (red
man syndrome), chills,
eosinophilia,
neutropenia
Rare: drug rash with
eosinophilia and
systemic symptoms
(DRESS), ototoxicity,
renal failure, StevensJohnson syndrome,
thrombocytopenia
Monitor: periodic renal
function tests, urinalysis,
CBC, serum trough
vancomycin levels.
Monitor for hypotension,
rash, neutropenia,
nausea, vomiting, and
auditory changes
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to
vancomycin
Disease-related
precautions: Use with
caution in patients with
renal impairment
(dosage adjustment may
be required)
Drug-drug interactions:
Avoid concomitant use
with BCG, gallium
nitrate. Levels of
vancomycin may be
increased by
nonsteroidal antiinflammatory agents
(NSAIDs)
(Lexicomp, 2014)
PERSONAL DRUGS
Oxazolidinone
(linezolid)
Zyvox, Intravenous
2mg/mL (100mL):
$72.18
(Lexicomp, 2014)
11
Excretion: urine
(Lexicomp, 2014)
Pharmacodynamics:
Bacteriostatic and
bactericidal
depending on
organism. Inhibits
bacterial protein
synthesis by binding
to 23S ribosomal
RNA of the 50S
subunit, preventing
bacterial translation.
Gram-positive
coverage
Pharmacokinetics:
Distribution: Vd:
40-50L
Metabolism:
hepatic, minimally
metabolized, may be
mediated by
cytochrome P450
Half-life
elimination: 4-5
hours
Excretion: primarily
urine; feces
(Lexicomp, 2014)
Side Effects:
Common: headache,
diarrhea, decreased
hemoglobin,
thrombocytopenia,
insomnia, nausea,
vomiting, increased liver
enzymes, constipation,
abdominal pain,
increased
BUN/creatinine, fever
Rare: anaphylaxis,
angioedema,
Clostridium difficile
associated diarrhea,
dental discoloration,
dyspepsia, hypertension,
hypoglycemia, lactic
acidosis, peripheral
neuropathy,
rhabdomyolysis,
seizures, serotonin
syndrome, StevensJohnson syndrome,
vision loss
Monitor: CBC weekly,
especially in patients at
risk for bleeding. With
extended therapy
monitor visual function
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to
linezolid; concurrent use
or within 2 weeks of
MAO inhibitors
Disease-related
precautions: Use with
caution and closely
monitor those with
uncontrolled
hypertension and
untreated hypothyroid.
Use with caution and
closely monitor blood
pressure in those with
pheochromocytoma; use
with caution in patients
with a history of
seizures. Closely
monitor blood glucose
in diabetic patients
(hypoglycemic episodes
have been reported)
Drug-drug interactions:
Avoid concomitant use
with anilidopiperidine
opiods, apraclonidine,
atomoxetine,
bezafibrate,
buprenorphine,
bupropion, buspirone,
barbamazepine,
clozapine,
cyclobenzaprine,
dexmethylphenidate,
dextromethorphan,
diethylpropion,
hydrocodone,
hydromorphone,
isometheptene,
levonordefrin, MAO
inhibitors, maprotiline,
meperidine, methyldopa,
methylene blue,
PERSONAL DRUGS
Tetracycline
Derivative
Antibiotics
(doxycycline,
tetracycline)
Doxycycline
(Doxycycline Hyclate,
intravenous)
100mg (1): $14.52
(Doxy 100,
intravenous)
100mg (1): $16.80
(Lexicomp, 2014)
12
Pharmacodynamics:
Bacteriostatic.
Inhibits bacterial
protein synthesis by
binding with 30S
ribosomal subunit.
Gram-positive and
gram-negative
coverage.
Pharmacokinetics:
Distribution: Vd:
53-134 L.
Distributes widely
into body tissues and
fluids including
synovial, pleural,
prostatic, seminal
fluids, and bronchial
fluids. Poor CSF
penetration
Protein binding:
90%
Metabolism:
partially inactivated
by GI tract
Half-life
elimination: 12-15
hours in single dose
Excretion: primarily
feces; urine
(Lexicomp, 2014)
Side Effects:
Common: headache,
nausea, vomiting,
diarrhea, abdominal
pain, vaginitis,
hypoglycemia,
erythematous rash,
urticaria, increased BUN
Rare: anaphylaxis,
eosinophilia,
neutropenia, dysphagia,
esophagitis, StevensJohnson syndrome, toxic
epidermal necrolysis,
hepatoxicity
Monitor: CBC, renal
and liver function
periodically with
prolonged therapy
methylphenidate,
mirtazipine, morphine,
nefazodone,
oxymorphone, pizotifen,
SSRIs, serotonin 5HT1D receptor agonists,
SNRIs, tapentadol,
tetrabenazine,
trazodone, tricyclic
antidepressants,
tryptophan
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to any
tetracycline formulation
Disease-related
precautions: Use with
caution in patients with
renal failure (dosage
adjustment may be
required); hepatotoxicity
is rare, but risk may be
increased in patients
with underlying hepatic
impairment
Drug-drug interactions:
Avoid concomitant use
with BCG, pimozide,
retinoic acid derivatives,
strontium ranelate
(Lexicomp, 2014)
(Lexicomp, 2014)
IV. Effective Drug Classification: Respiratory Fluoroquinolone
PERSONAL DRUGS
13
Drug Name
Efficacy
Safety
Suitability
Gemifloxacin
(Factive)
Pharmacodynamics:
Bactericidal.
Inhibition of DNA
gyrase, which is
required to maintain
the DNA structure,
as well as DNA
replication and
transcription, DNA
repair,
recombination, and
transposition.
Gram-positive and
gram-negative
coverage.
Pharmacokinetics:
Absorption: well
absorbed from GI
tract
Protein binding:
60%-70%
Metabolism:
Hepatic (no
involvement of
CYP system)
Half-life
elimination: 7
hours
Excretion:
primarily feces;
urine
Drug
Interaction:
Avoid
concomitant use
with BCG,
highest risk
QTc-prolonging
agents,
ivabradine,
mifepristone,
strontium
ranelate
Levels/effects of
Gemifloxacin
may be
increased by:
insulin,
ivabradine,
mifepristone,
NSAIDs,
probenecid,
QTc-prolonging
agents.
Gemifloxacin
may decrease
the levels/effects
of : BCG,
didanosine,
mycophenolate,
sodium
picosulfate,
sulfonylureas,
typhyoid
vaccine
Levels/effects of
Gemifloxacin
may be
decreased by:
antacids,
calcium salts,
didanosine, iron
salts,
magnesium
salts,
Patient
Education: May
be taken with or
without food,
milk, or calcium
supplements, but
should be taken 3
hours before or 2
hours after
supplements
containing iron,
zinc, or
magnesium.
Report to
prescriber
tachycardia,
severe dizziness,
ankle pain,
arthralgia, edema,
paresthesia, or
rash.
(Lexicomp,
2014)
(Lexicomp, 2014)
Monitor:WBC,
Signs/symptoms
of infection, renal
function
Contraindications:
Hypersensitivity
to gemifloxacin or
and component of
the formulation.
Use with caution
in patients with
renal impairment
(dosage
adjustment may be
required)
(Lexicomp,
2014)
Cost
Factive, oral
320mg (5):
$239.20
(Lexicomp,
2014)
PERSONAL DRUGS
Levofloxacin
(Levaquin)
(Lexicomp,
2014)
multivitamins
with ADEK and
iron, quinapril,
sevelamer,
strontium
ranelate,
sucralfate, zinc
salts
(Lexicomp,
2014)
Pharmacodynamics: Drug
Inhibits bacterial
Interaction:
DNA gyrase which See
is responsible for
Gemifloxacin
DNA replication,
drug
transcription, repair, interactions.
combination, and
transposition.
Promotes breakage
of bacterial DNA
strands. Gramnegative, grampositive, and
atypical bacterial
coverage.
Pharmacokinetics:
Absorption: rapid
and complete
Distribution: Vd:
74-112L. High
concentrations
achieved in lung,
sinus, and saliva
Protein binding:
24%-38%
Metabolism:
Minimal hepatic
Half-life
elimination: 6-8
hours
Excretion:
primarily urine;
feces
(Lexicomp, 2014)
14
Patient
Education:
Tablets may be
taken without
regard to meals,
however, liquid
solution should be
taken 1 hour
before or 2 hours
after meals.
I.V. solution
should be infused
over 60 minutes
and separate from
solutions
containing
magnesium or
calcium. Maintain
adequate
hydration to
prevent
crystalluria.
Immediately
report to provider
with
signs/symptoms of
significant
reaction such as
wheezing, fever,
seizures, swelling
of face, tongue,
lips.
Monitor: Montitor
CBC, renal, and
hepatic function
Levaquin, oral
solution
25mg/mL
(480mL):
$813.37
Levaquin, oral
tablets
250mg (50):
$1184.60
500mg (50):
$1357.66
750mg (50):
$1016.90
Levofloxacin,
oral tablets
250mg (50):
$840.55
500mg (50):
$964.40
750mg (50):
$721.56
Levaquin,
intravenous
250mg/50mL
(50mL): $11.64
500mg/100mL
(100mL):$22.97
750mg/150mL
(150mL):$30.53
Levofloxacin in
D5W,
intravenous
250mg/50mL
(50mL): $8.40
750mg/150mL
(150mL):$12.60
PERSONAL DRUGS
15
periodically
throughout
therapy. Monitor
for signs of
hypersensitivity
reactions.
Moxifloxacin
(Avelox)
(Lexicomp,
2014)
Pharmacodynamics:
Inhibition of
bacterial replication
by inhibiting DNA
gyrase. Grampositive and gramnegative coverage.
Pharmacokinetics:
Absorption: Well
absorbed
Distribution: Vd:
1.7-2.7 L/kg. In
respiratory tissues,
alveolar
macrophages, and
sinus tissues, tissue
concentrations
exceed plasma
concentration
Protein binding:
30%-50%
Metabolism:
Hepatic
Half-life
elimination: 12-16
hours, single oral
dose; 8-15 hours
I.V.
Excretion:
primarily urine;
feces
Drug
Interaction:
See
Gemifloxacin
for drug
interactions
Contraindications:
Hypersensitivity
to levofloxacin or
and component of
quinolone
formulation.
(Lexicomp,
2014)
Patient
Education: May
take oral
formulation
without regard to
meals. Infuse I.V.
over 60 minutes.
Immediately
report
signs/symptoms of
reaction such as
wheezing,
seizures, swelling
of face, lips,
tongue
Monitor: CBC and
signs of infection.
Monitor for
hypersensitivity
reactions.
Contraindications:
Hypersensitivity
to moxifloxacin or
any quinolone
formulation
(Lexicomp,
2014)
(Lexicomp,
2014)
Avelox, oral
400mg (30):
$825.76
Avelox, ABC
pack oral
400mg (5):
$137.63
Avelox,
intravenous
400mg/250mL
(250mL):
$46.16
(Lexicomp,
2014)
PERSONAL DRUGS
16
(Lexicomp, 2014)
V. Drug of Choice: Levofloxacin
This patient will require admission to a non-ICU floor for stabilization and monitoring of
oxygen status, and intravenous antibiotic administration. According to the Infectious Disease
Society of America and the American Thoracic Society, a respiratory fluoroquinolone is the
monotherapy treatment of choice in that environment and is a level I recommendation (Mandell
et al., 2007). Achievement of high antibacterial concentration in the blood and lung tissue early
in treatment is essential for positive prognosis, which is why empiric antibiotic therapy is
initiated, then narrowed down once the pathogen has been identified (Lee, Kim, Kim, Ryu, &
Chang, 2012). In the older adult population with COLD, Streptococcus pneumonia is the most
frequently identified organism. Due to the widespread activity against atypical bacteria,
including gram-positive and gram-negative organisms, levofloxacin is beneficial for treatment of
community-acquired pneumonia in this patient (Lee et al., 2012).
Levofloxacin 750mg intravenous daily will be started on this patient. High-dose
levofloxacin is associated with increased bactericidal effects, due to its concentration-killing
effect (Lee et al., 2012). Once the patient begins to improve clinically, is hemodynamically
stable and able to tolerate oral intake, oral therapy should be started (Mandell et al., 2007). The
change from intravenous to oral remains at 750mg daily, for a maximum of ten days, and
maintains a high pulmonary bioavailability to facilitate early discharge from the hospital (Lee et
al., 2012).
PERSONAL DRUGS
17
Discharge teaching should include educating the patient to complete the entire
prescription of antibiotic and maintain adequate hydration to prevent crystalluria (Lexicomp,
2014). Respiratory hygiene methods such as hand hygiene and covering cough with masks or
tissues should be encouraged to reduce transmission (Mandell et al., 2007). Vaccination status
should be assessed upon admission, with delivery of pneumonia and influenza vaccine prior to
discharge if indicated (Mandell et al., 2007). Materials regarding smoking cessation should be
reviewed and discussed, with strong encouragement for quitting. Follow-up appointment should
be made within 1-2 weeks after discharge to ensure adequate treatment. In Ohio, the advanced
practice nurse (APN) with a current certificate to prescribe (CTP) has the authority to prescribe
levofloxacin (Ohio Board of Nursing, 2014).
Second Diagnosis: Hypertension (HTN) in the African-American
38 year old African-American female in to the office for wellness check-up. Blood
pressure on assessment is 162/93 mmHg, HR: 100bpm, RR: 20pbm, BMI: 31.6. No significant
past medical history. Denies smoking and drinks alcohol socially. Family history positive for
hypertension in father and grandmother.
I. Definition of Diagnosis
The American Society of Hypertension defines hypertension (HTN) in adults age 18 to
80 years of age as a systolic blood pressure (SBP) greater than or equal to 140 mmHg or diastolic
blood pressure (DBP) greater than or equal to 90 mmHg, or both (Weber et al., 2013).
Confirmation of the diagnosis of HTN should be made at a follow-up appointment within one to
four weeks of the first measurement (Weber et al., 2013). Blood pressure measurements should
be performed using an arm cuff with an electronic device to decrease the incidence of inaccurate
readings and observer bias with auscultatory methods, and measurements should be performed in
both arms (Weber et al., 2013). Evaluation of additional history regarding comorbidities
including stroke, coronary artery disease, heart failure, kidney disease, peripheral artery disease,
and diabetes should be assessed to assist in proper pharmacologic treatment. Laboratory testing
such as renal function, liver function, lipid panel, fasting glucose, and urine for albuminuria,
proteinuria, and red blood cells can also help guide treatment. Electrocardiography (ECG) is
important to evaluate the presence of left atrial or ventricular hypertrophy, previous myocardial
infarction, and arrhythmias which can also help guide treatment (Weber et al., 2013).
PERSONAL DRUGS
18
II. Therapeutic Objective
The goal of treatment in the adult less 60 years of age is to lower SBP to less than
140mmHg and DBP to less than 90 mmHg, while also addressing issues often associated with
hypertension such as obesity, lipid disorders, and glucose intolerance (James et al., 2014).
Pharmacologic treatment should be initiated immediately upon diagnosis with monotherapy,
although most patients will require more than one drug to reach adequate blood pressure control
(Weber et al., 2013). Nonpharmacologic measures such as exercise and weight loss, salt
reduction, limited alcohol consumption, and smoking cessation should be implemented to
complement drug therapy for the management of HTN.
III. Effective Drug Groups
Drug Classification
Thiazide Diuretics
(chlorothiazide,
chlorthalidone,
hydrochlorothiazide,
methyclothiazide)
Efficacy
Pharmacodynamics:
Inhibits sodium and
chloride reabsorption
in the distal tubules
causing increased
excretion of sodium
Chlorothiazide (oral) and water, as well as
250mg (100): $21.63 potassium and
500mg (100): $25.25 hydrogen ions
Pharmacokinetics:
Chlorthalidone (oral) Absorption: well
25mg (100): $55.17
absorbed when
50mg (100): $68.04
administered with
100mg
(100): food. Reduced in pts
$101.25
with congestive heart
failure. 65%-75%
Hydrochlorothiazide
bioavailability
(oral tablets)
(reduced by 10%
12.5mg
(100): when administered
$82.43
with food)
25mg (100): $8.48
Distribution: 3.6-7.8
50mg (100): $16.45
L/kg
Protein binding: 40%Methyclothiazide
68%
(oral)
Metobolism: not
5mg (100): $184.23
metabolized
Half-life elimination:
(Lexicomp, 2014)
6-15 hours
Excretion: primarily
in the urine (as
unchanged drug)
Safety
Side Effects:
Common:
Hypotension,
orthostatic
hypotension, dizziness,
vertigo, headache,
alopecia, rash,
hyperglycemia,
hypokalemia,
hyperuricemia,
anorexia, constipation,
cramping, diarrhea,
nausea, gastric
irritation, vomiting,
glycosuria, impotence,
agranulocytosis,
hemolytic anemia,
thrombocytopenia,
muscle spasm,
restlessness, weakness,
renal failure,
respiratory distress,
pneumonitis,
pulmonary edema
Rare: allergic
myocarditis,
eosinophilic
pneumonitis, hepatic
function impairment,
hypercalcemia
Monitor: serum
electrolytes, BUN,
Suitability
Contraindications:
Hypersensitivity to
any formulation of
thiazide diuretics;
anuria
Pregnancy Category:
B
Disease-related
precautions: Use
with caution in
patients with diabetes
or prediabetes,
hepatic impairment,
renal impairment, and
those with moderate
or high cholesterol.
May decrease renal
calcium excretion so
avoid in
hypercalcemia and
parathyroid disease.
Use with caution in
patients with
hypokalemia. May
exacerbate Systemic
Lupus Erythematosus
Drug-drug
interactions: Avoid
concomitant use with
Dofetilide. May
decrease the effects
of antidiabetic agents.
PERSONAL DRUGS
19
(Lexicomp, 2014)
Angiotensin
converting enzymeInhibitors
(benazepril, captopril,
cilazapril, enalapril,
enalaprilat, fosinopril,
lisinopril, moexipril,
quinapril, ramipril,
trandolapril)
Captopril (oral)
12.5mg (100):
$77.18
25mg (100): $83.44
50mg (100): $143.08
100mg (100):
$190.54
Enalapril (oral)
2.5mg (100): $88.33
5mg (100): $106.37
10mg (100): $117.81
20mg (100): $167.64
Enalapril (Vasotec,
oral)
2.5mg (30): $90.52
5mg (30): $113.92
10mg (30): $375.84
20mg (30): $164.28
Lisinopril (oral)
2.5mg (100): $64.25
5mg (100): $96.23
10mg (100): $99.40
20mg (100): 106.40
Lisinopril (Prinivil,
oral)
5mg (90): $132.94
10mg (90): $137.27
20mg (90): $146.93
Pharmacodynamics:
Inhibits conversion of
angiotensin I to
angiotensin II
resulting in increased
plasma rennin activity
and reduction in
aldosterone secretion
Pharmacokinetics:
Absorption: 60-75%,
reduced to 40% with
food. Decreased
bioavailability with
Class II-IV heart
failure
Metabolism: 50%.
hepatic
Half-life elimination:
(renal and cardiac
dependent): 2-10
hours
Excretion: Urine
within 24hrs (50% as
unchanged drug)
(Lexicomp, 2014)
creatinine, blood
pressure. Assess
weight, I&O daily to
determine fluid loss
(Lexicomp, 2014)
Side Effects:
Common:
hypotension, chest
pain, headache,
dizziness, fatigue, rash,
abnormal taste,
abdominal pain,
nausea, vomiting,
diarrhea, weakness,
increased serum
creatinine, cough
Rare: agranulocytosis,
anaphylactoid reaction,
atrial fibrillation, atrial
tachycardia, bone
marrow suppression,
bradycardia, cardiac
arrest, hallucinations,
hepatitis, ileus,
interstitial nephritis,
neutropenia, pulmonary
embolism, StevensJohnson syndrome,
thrombocytopenia,
ventricular tachycardia
Monitor: blood
pressure, BUN, serum
creatinine and
potassium, CBC with
differential in patients
with renal impairment
or collagen vascular
disease
(Lexicomp, 2014)
Drug levels may be
decreased by bile
acid sequestrants,
NSAIDs
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to
any formulation of
ACE inhibitors;
angioedema related to
previous treatment
with ACE inhibitors;
in patients with
diabetes mellitus,
concomitant use of
aliskiren
Pregnancy Category:
D
Disease-related
precautions: Use
with caution in
patients with preexisting renal
insufficiency or renal
artery stenosis. Use
with caution in
patients with
hypertrophic
cardiomyopathy with
outflow tract
obstruction. Use
with caution in severe
aortic stenosis. Close
observation with
initiation in patients
with ischemic heart
disease
Drug-drug
interactions: No
known interactions
with concomitant use
should be avoided.
Levels/effects may be
increased by
Angiotensin II
PERSONAL DRUGS
20
Irbesartan (oral)
75mg (90): $262.63
150mg (30): $92.12
300mg (30): $123.10
receptor blockers,
heparin, loop
diuretics, potassiumsparing diuretics,
thiazide diuretics
(Lexicomp, 2014)
Side Effects:
Contraindications:
Common: chest pain,
Hypersensitivity to
fatigue, hypoglycemia, any formulation of
diarrhea, urinary tract
angiotensin II
infection, anemia,
receptor-blockers; in
weakness, back pain,
diabetes mellitus,
intermittent
concomitant use of
claudication, cough,
aliskiren
hypotension, fever,
Pregnancy Category:
insomnia,
D
hyperkalemia, gastritis, Disease-related
infection
precautions: Use
Rare: acute psychosis
with caution in
with paranoid
patients with renal
delusions, allergic
artery stenosis, renal
reaction, arrhythmia,
impairment, hepatic
bradycardia, BUN
impairment, heart
elevation, AV block,
failure, and
CHF, dyspnea,
aortic/mitral stenosis.
decreased
Dosage adjustment
hemoglobin/hematocrit, may be required.
myocardial infarction,
Drug-drug
syncope,
interactions: Avoid
thrombocytopenia
concomitant use with
Monitor: renal
pimozide. Avoid St.
function tests including John’s Wort.
electrolytes, creatinine, Levels/effects of
and BUN; CBC, blood ARBs affected by
pressure monitoring
CYP system
including CYP2C8,
(Lexicomp, 2014)
CYP2C0, and
CYP3A4 substrates.
(Lexicomp, 2014)
Calcium Channel
Blockers
(amlodipine,
clevidipine, diltiazem,
felodipine,
isradipine,
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to
any calcium channel
blocker formulation.
Pregnancy Category:
C
(Lexicomp, 2014)
Angiotensin II
Receptor-Blockers
(azilsartan, losartan,
valsartan,
candesartan,
eprosartan, irbesartan,
telmisartan,
olmesartan)
Losartan (Cozaar,
oral)
25mg (1000):
$2557.19
50mg (90): $309.48
100mg (90): $421.55
(Losartan Potassium,
oral)
25mg (90): $151.43
50mg (30): $67.88
100mg (90): $277.36
Valsartan (Diovan,
oral)
40mg (30): $118.07
80mg (90): $423.44
160mg (90): $455.33
320mg (90): $576.01
Pharmacodynamics:
Blocks the
vasoconstrictor and
aldosterone-secreting
effects of angiotensin
II. May induce a
more complete
inhibition of renninangiotensin system
than ACE-inhibitors
Pharmacokinetics:
Absorption: 15%33%
Distribution: Vd: 1234L. Does not cross
blood brain barrier
Metabolism: Hepatic
via CYP2C9 and 3A4
Half-life elimination:
6-12 hours
Excretion: urine;
feces
(Lexicomp, 2014)
Pharmacodynamics:
Inhibits calcium
influx into arterial
smooth muscle cells,
producing peripheral
arterial vasodilation,
Side Effects:
Common: peripheral
edema (dose related),
pulmonary edema, AV
block, bradycardia,
palpitations, flushing,
PERSONAL DRUGS
21
nicardipine,
nifedipine,
nisoldipine,
verapamil)
causing a decrease in
peripheral resistance
and blood pressure
Pharmacokinetics:
Absorption: well
Amlodipine
absorbed orally; 64%(amlodipine besylate
90% bioavailability
oral)
Distribution: Vd:
2.5mg (90): $155.68 21L/kg
5mg (90): $155.69
Metabolism: Hepatic.
10mg (90): $213.65
CYP3A4 substrate.
Amlodipine (Norvasc, Extensive first pass
oral)
effect.
2.5mg (90): $318.67 Half-life elimination:
5mg (100): $354.07
10-50 hours,
10mg (90): $436.91
dependent on
medication (increased
Diltiazem (diltiazem
with hepatic
HCl, oral)
dysfunction)
30mg (100): $44.94
Excretion: primarily
60mg (100): $72.36
urine; feces
90mg (100): $112.75
120mg (100):
(Lexicomp, 2014)
$151.81
Diltiazem HCl ER,
oral (12-hour)
60mg (100): $131.42
90mg (100): $150.16
120mg (100):
$195.75
Nimodipine (oral)
30mg (30): $287.43
(Lexicomp, 2014)
Beta-1 Adrenergic
Blockers
(atenolol, bisoprolol,
esmolol, metoprolol,
nebivolol)
Atenolol (oral)
25mg (100): $81.75
50mg (1000):
$798.72
100mg (100):
$125.15
fatigue, dizziness,
pruritus, nausea,
abdominal pain, muscle
cramps, constipation,
weakness, dyspnea
Rare: acute interstitial
nephritis, allergic
reaction, inverted T
wave, ST segment
depression,
thrombocytopenia,
hepatitis,
hypersensitivity
reaction, orthostatic
hypotension,
leukopenia,
pancreatitis, StevensJohnson syndrome,
ventricular tachycardia
Monitor: blood
pressure, heart rate,
peripheral edema
(Lexicomp, 2014)
Disease-related
precautions: Use
with caution in renal
and hepatic
impairment (consider
starting low dose and
monitor closely).
Use with caution in
patients with aortic
stenosis as decreased
coronary perfusion
may occur. Use with
caution in patients
with heart failure and
hypertrophic
cardiomyopathy, as
symptoms may
worsen.
Drug-drug
interactions:
Substrate of
CYP34A; Avoid
concomitant use with
bosutinib,
conivaptan,
dantrolene, fusidic
acid, ibrutinib,
ivabradine,
lomitapide, pimozide,
simeprevir, tolvaptan,
ulipristal
(Lexicomp, 2014)
Pharmacodynamics:
Selectively inhibits
beta-1 adrenergic
receptors, which
blocks the effects of
norepinephrine and
epinephrine, causing
vasodilation and
decreased blood
pressure. Little to no
effect on beta-2
receptors.
Side Effects:
Common: persistent
bradycardia,
hypotension, chest
pain, edema, heart
failure, second or third
degree AV block,
Raynaud’s
phenomenon, dizziness,
fatigue, insomnia,
lethargy, confusion,
depression, headache,
Contraindications:
Hypersensitivity to
any beta-blocker
formulation.
Contraindicated in
severe bradycardia,
significant firstdegree AV block,
sick sinus syndrome,
cardiogenic shock,
decompensated heart
failure.
PERSONAL DRUGS
Metoprolol
(Metoprolol
Succinate, ER oral)
25mg (100): $105.38
50mg (100): $105.38
100mg (100):
$158.35
200mg (100):
$251.98
(Metoprolol Tartrate,
oral)
25mg (100): $24.25
50mg (100): $55.50
100mg (100): $80.10
(Lexicomp, 2014)
22
Pharmacokinetics:
Absorption: rapid
and complete.
Bioavailability 50%70%
Distribution: Vd:
3.2-5.6 L/kg
Metabolism:
Extensively hepatic
via CYP2D6 with
significant first pass
effect
Half-life elimination:
3-6hours (longer in
poor CYP2D6
metabolizers and in
renal impairment)
Excretion: primarily
urine; feces
(Lexicomp, 2014)
Nonselective BetaBlockers
(nadolol, propranolol,
sotalol, timolol)
Nadolol (Corgard,
oral)
20mg (100): $403.24
40mg (100): $471.78
Pharmacodynamics:
Competitively blocks
response to beta-1
and beta-2 adrenergic
stimulation resulting
in decreased blood
pressure, heart rate,
and myocardial
demand
nightmares,
constipation, nausea,
diarrhea, may
aggravate allergic
reactions,
bronchospasm
Rare: dyspnea (in large
doses), hallucinations,
increased liver
enzymes, psychosis,
thrombocytopenia,
wheezing
Monitor: ECG and
blood pressure. Assess
fluid balance, heart
failure symptoms, and
for postural
hypotension. Monitor
glucose levels closely
(may alter glucose
tolerance)
Pregnancy Category:
C
Disease-related
precautions:
Bronchospastic
disease (use
cautiously with close
monitoring);
Conduction
abnormalities
(consider pre-existing
conditions before
initiating); Diabetes
(may mask symptoms
of hypoglycemia);
Heart failure (may
worsen symptoms);
Hepatic impairment;
Myasthenia Gravis;
Peripheral vascular
disease (may
aggravate symptoms
(Lexicomp, 2014)
of arterial
insufficiency);
Psoriais; Psychiatric
disease (may
exacerbate); Thyroid
disease (may mask
tachycardia
associated with
hyperthyroidism)
Drug-drug
interactions: Avoid
concomitant use with
floctafenine,
methacoline
(Lexicomp, 2014)
Side Effects:
Contraindications:
Common: drowsiness, Hypersensitivity to
insomnia,
any formulation of
atrioventricular block,
beta-blockers;
bradycardia, cardiac
uncompensated
conduction disturbance, congestive heart
cardiac failure, cold
failure, cardiogenic
extremities, edema,
shock; severe
hypotension,
bradycardia, sick
PERSONAL DRUGS
80mg (100): $648.16
Propranolol
(Propranolol HCl,
oral)
10mg (100): $33.53
20mg (100): $36.29
40mg (100): $69.11
60mg (100): $121.83
Sotalol (Betapace
oral)
80mg (100): $473.45
120mg (100):
$631.76
160mg (100):
$789.65
23
Pharmacokinetics:
Absorption: rapid
and complete
absorption orally.
Increased
bioavailability to 50%
with protein-rich
foods.
Distribution: 4 L/kg
Metabolism: Hepatic
via CYP2D6 with
extensive first pass
effect.
Half-life elimination:
3-12 hours
Excretion: urine
palpitations, Raynaud’s
phenomenon,
depression, dizziness,
fatigue
Rare: bronchospasm,
cardiac arrhythmia,
confusion,
hallucination,
headache, sedation,
thrombocytopenia,
lupus-like syndrome,
interstitial nephritis,
oliguria, proteinuria
Monitor: heart rate and
blood pressure
(Lexicomp, 2014)
(Lexicomp, 2014)
(Lexicomp, 2014)
Alpha 1 Blocker
(doxazosin,
phenoxybenzamine,
phentolamine,
prazosin, terazosin)
Doxazosin (Cardura,
Pharmacodynamics:
Vasodilation of veins
and arterioles by
inhibition of
postsynaptic alpha1adrenergic receptors
causing a decrease in
Side Effects:
Common: dizziness,
malaise, fatigue,
headache, edema,
vertigo, sexual
dysfunction, polyuria,
weakness, respiratory
sinus syndrome, or
second- or thirddegree AV block;
severe hyperactive
airway disease
Pregnancy Category:
C
Disease-related
precautions:
bronchospastic
disease; conduction
abnormality; diabetes
(may mask signs of
hypoglycemia); heart
failure (may worsen
symptoms); hepatic
and renal
impairment;
myasthenia gravis;
peripheral vascular
disease (may
aggravate
symptoms); psoriasis;
psychiatric disease;
thyroid disease (may
mask tachycardia
associated with
hyperthyroid)
Drug-drug
interactions: Avoid
concomitant use with
beta2-agonists;
bosutinib;
floctafenine;
methacholine;
pazopanib;
pomalidomide;
topotecan; vincristine
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to
any alpha 1 blocker
formulation. Avoid
use in elderly due to
high risk of
orthostatic
PERSONAL DRUGS
oral)
1mg (100):
2mg (100):
4mg (100):
8mg (100):
$245.41
$245.41
$257.57
$270.48
Prazosin (Minipress,
oral capsule)
1mg (250): $313.81
2mg (250): $436.80
5mg (250): $744.68
Terazosin (Terazosin
HCl, oral)
1mg (100): $160.38
10mg (100): $160.50
24
blood pressure and
total peripheral
resistance
Pharmacokinetics:
Absorption: varies by
medication.
Bioavailability 20%82%
Distribution: Vd: 0.5
L/kg
Metabolism:
primarily hepatic via
CYP3A4; secondary
pathways CYP2D6
and 2C19
Excretion: primarily
feces; urine
(Lexicomp, 2014)
tract infection, rhinitis
Rare: abnormal
thinking, allergic
reaction, angina,
bradycardia,
bronchospasm,
cerebrovascular
accident, fever,
hallucinations,
leukopenia, liver
function abnormalities,
pancreatitis, pruritus,
tachycardia
Monitor: blood
pressure with
orthostatics
(Lexicomp, 2014)
(Lexicomp, 2014)
Alpha2-Adrenergic
Agonist
(clonidine,
guanfacine,
methyldopa)
Clonidine (CatapresTTS-1 Transdermal)
0.1mg/24 hrs (4):
$196.15
(Catapres, oral)
0.1mg (100): $202.32
0.2mg (100): $309.53
0.3mg (100): $388.42
Methyldopa
(Methyldopa, oral)
250mg (100): $38.40
500mg (100): $68.49
Pharmacodynamics:
Decreased peripheral
resistance and blood
pressure by
stimulation of alpha2adrenoreceptors in the
brain stem which
activates inhibitory
neurons causing
decreased
sympathetic outflow
from the CNS.
Pharmacokinetics:
Absorption:
Dependent on drug
and route of
administration.
Bioavailability (oral)
580%-90%;
(transdermal) 60%
Distribution: Highly
lipid soluble; Vd:
Side Effects:
Incidence of adverse
events may be lower
with transdermal
compared to oral
Common: orthostatic
hypotension,
drowsiness, headache,
fatigue, sedation,
lethargy, agitation,
hallucinations,
xerostomia,
constipation, erectile
dysfunction,
thrombocytopenia,
weakness; with
transdermal use:
pruritus and erythema,
contact dermatitis,
hyperpigmentation,
burning, edema,
excoriation
hypotension
Pregnancy Category:
C
Disease-related
precautions: Use
with caution in
patients with mild-tomoderate hepatic
impairment. Not
recommended with
severe dysfunction.
Rule out prostate
carcinoma prior to
starting therapy.
Drug-drug
interactions: Avoid
concomitant use with
other alpha 1
blockers, conivaptan,
fusidic acid. Use
with caution in
CYP34A inhibitors
and inducers.
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to
any formulation of
alpha2-adrenergic
agonists.
Pregnancy Category:
C
Disease-related
precautions: Use
with caution in
patients with recent
myocardial infarction
and conduction
disturbances, patients
with cerebrovascular
disease, and those
with renal
impairment.
Drug-drug
interactions: Avoid
concomitant use with
azelastine (nasal),
PERSONAL DRUGS
25
2.9L/kg
Metabolism: Hepatic
by CYP3A4
Excretion: primarily
urine
(Lexicomp, 2014)
Loop Diuretics
(bumetanide,
furosemide,
torsemide)
Bumetanide
(Bumetanide, oral)
0.5mg (100): $30.20
1mg (100): $44.52
2mg (100): $75.18
Furosemide
(Furosemide, oral)
20mg (100): $14.30
40mg (100): $16.30
(Lasix, oral)
20mg (100): $53.76
40mg (100): $75.34
(Lexicomp, 2014)
Pharmacodynamics:
Interferes with
chloride-binding
cotransport system,
inhibits reabsorption
of sodium and
chloride in the
ascending Loop of
Henle which causes
increased water and
sodium excretion
Pharmacokinetics:
Absorption:
Bioavailability 47%64%
Distribution: Vd: 1215L; doubled with
cirrhosis
Metabolism: Hepatic
Half-life elimination:
1 hour
Excretion: Primarily
urine; feces
(Lexicomp, 2014)
Rare: hepatitis, liver
function test
abnormalities, leg
cramps, weight gain,
atrioventricular block,
heart failure
Monitor: blood
pressure (with
orthostatics), heart rate,
mental status
(Lexicomp, 2014)
Side Effects:
Common: electrolyte
disturbances, excessive
urination, hypotension,
dizziness, fever,
headache, increased
cholesterol and
triglycerides, metabolic
alkalosis, nausea,
cramping, constipation,
thrombocytopenia,
increased liver
enzymes, muscle
spasms
Rare: agranulocytosis,
angioedema, aplastic
anemia, anaphylaxis,
atrial fibrillation,
Stevens-Johnson
syndrome, ventricular
tachycardia
Monitor: serum
electrolytes and renal
function, blood
pressure, weight and
intake and output
(Lexicomp, 2014)
Potassium-sparing
Pharmacodynamics:
Side Effects:
lobenguane I 123,
paraldehyde
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to
any formulation of
loop diuretic; anuria
Pregnancy Category:
B/C
Disease-related
precautions: Use
with caution in
patients with
cirrhosis (electrolyte
imbalances may lead
to hepatic
encephalopathy); in
patients with
prediabetes or
diabetes mellitus;
prostatic
hyperplasia/urinary
stricture; systemic
lupus erythematosus
Drug-drug
interactions: Avoid
concomitant use with
other
antihypertensive
agents (may increase
risk of hypotension);
chloral hydrate;
ethacrynic acid. Use
with caution with
CYP2C9 inhibitors
and inducers
(Lexicomp, 2014)
Contraindications:
PERSONAL DRUGS
Diuretics
(amiloride,
eplerenone,
spironolactone,
triamterene)
Amiloride
(Amiloride, oral)
5mg (100): $128.97
Eplerenone
(Eplerenone, oral)
25mg (30): $123.07
Spironolactone
(Aldactone, oral)
25mg (100): $145.40
50mg (100): $255.36
(Lexicomp, 2014)
26
Competes with
aldosterone for
receptor sites in distal
tubules causing
increased water and
sodium chloride
excretion with
potassium and
hydrogen
conservation.
Pharmacokinetics:
Absorption: 15%25%. Bioavailability
69%
Distribution: Vd: 4390 L
Metabolism: Hepatic
via CYP3A4
Half-life elimination:
1-12 hours
(depending on drug)
Excretion: primarily
urine; feces
Common:
hyperkalemia,
hyponatremia,
hypertriglyceridemia,
dizziness, fatigue,
increased creatinine,
cough
Rare: bladder spasm,
cardiac arrhythmia,
chest pain, dysuria,
gastrointestinal
hemorrhage, increased
intraocular pressure,
jaundice, orthostatic
hypotension,
palpitations
Monitor: serum
electrolytes (potassium
and sodium), renal
function, blood
pressure, intake and
output, daily weight
(Lexicomp, 2014)
(Lexicomp, 2014)
Vasodilators
(minoxidil,
hydralazine)
Minoxidil (Minoxidil,
oral)
2.5mg (100): $58.78
10mg (100): $129.14
Hydralazine
(Hydralazine HCl,
oral)
10mg (100): $41.15
25mg (100): $50.83
100mg (100):$101.30
(Lexicomp, 2014)
Pharmacodynamics:
Decreases systemic
vascular resistance by
relaxing smooth
muscle of arterioles;
little to no effect on
veins
Pharmacokinetics:
Absorption: 30%90% bioavailability
(increased with food)
Distribution: protein
binding 85%-90%
Metabolism: Hepatic
with extensive firstpass effect
Half-life elimination:
3.5-4 hours
Excretion: urine
Side Effects:
Common: T-wave
changes, orthostatic
hypotension, peripheral
edema, sodium and
water retention,
tachycardia, anxiety,
chills, nausea, diarrhea,
paralytic ileus, muscle
cramps, hypertrichosis,
increased alkaline
phosphatase,
pulmonary edema
Rare: bullous eruption,
Stevens-Johnson
syndrome, breast
tenderness, leukopenia,
thrombocytopenia,
Monitor: blood
pressure with
Anuria; acute renal
insufficiency;
hyperkalemia;
Addison’s disease or
other symptoms
associated with
hyperkalemia
Pregnancy Category:
B/C
Disease-related
precautions: Avoid
electrolyte imbalance
with hepatic
insufficiency (may
cause hepatic
encephalopathy),
discontinue use prior
to adrenal vein
catheterization
Drug-drug
interactions: Avoid
concomitant use with
cyclosporine,
tacrolimus,
triamterene
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to
minoxidil or
hydralazine;
pheochromocytoma;
mitral valve
rheumatic heart
disease
Pregnancy Category:
C
Disease-related
concerns: Use
caution in patients
with renal
impairment,
cardiovascular
disease, pulmonary
hypertension and
heart failure; Avoid
use for 1 month after
PERSONAL DRUGS
27
(Lexicomp, 2014)
Renin Inhibitor
(aliskiren)
Aliskiren (Tekturna,
oral)
150mg (30): $124.76
300mg (30): $157.39
orthostatics, heart rate.
Renal function tests,
ECG, echocardiogram
every 1-3 months with
initiation, then every 612 months
(Lexicomp, 2014)
Pharmacodynamics:
Side Effects:
Blocks the conversion Common: headache,
of angiotensinogen to fatigue, dizziness,
angiotensin I,
dyspnea,
suppressing the
nasopharyngitis,
negative feedback
diarrhea, cough
loop of the reninRare: anaphylaxis,
angiontensinangina, hepatic
aldosterone system,
insufficiency, increased
decreasing
uric acid,
vasoconstriction and
rhabdomyolysis,
blood pressure
seizure, StevensPharmacokinetics:
Johnson syndrome
Absorption: poor
Monitor: serum
absorption (decreased potassium, serum
by high-fat meal).
creatinine, BUN; blood
3% bioavailability
pressure
Metabolism:
unknown, but studies (Lexicomp, 2014)
indicate via CYP3A4
Half-life elimination:
24 hours
Excretion: primarily
urine; feces
(Lexicomp, 2014)
acute myocardial
infarction
Drug-drug
interactions: Avoid
concomitant use with
pimozide
(Lexicomp, 2014)
Contraindications:
Avoid concomitant
use with ACE
inhibitor or ARB in
patients with diabetes
mellitus
Pregnancy Category:
D
Disease-related
concerns: Increased
incidence of renal
impairment in
patients with diabetes
mellitus; use caution
in patients with renal
impairment
Drug-drug
interactions: Avoid
concomitant use with
cyclosporine and
itraconazole
(Lexicomp, 2014)
IV. Effective Drug Classification: Thiazide Diuretics
Drug Name
Chlorothiazide
(Diuril, Sodium
Diuril)
(Lexicomp, 2014)
Efficacy
Pharmacodynamics:
Diureses by
inhibition of sodium
and chloride
reabsorption in the
distal tubules causing
increased excretion of
sodium, chloride, and
water
Safety
Drug Interaction:
Avoid dofetilide
Increased
effect/toxicity of
chlorothiazide by:
alcohol, alfuzosin,
opiod analgesics,
anticholinergics,
barbiturates, beta2-
Suitability
Patient Education:
Take on an empty
stomach. Take
early in the day
(no later than 6
p.m.) to avoid
nocturia, unless
instructed
otherwise.
Cost
Chlorothiazide
Tablets:
250mg (100): $21.63
500mg (100): $25.25
Diuril
Suspension:
250mg/5mL (237
mL): $63.36
PERSONAL DRUGS
Pharmakokinetics:
Onset of Action:
diuresis within 2
hours
Duration: 6-12 hours
Absorption: poor
Metabolism: not
metabolized
Half-life elimination:
45-120 minutes
Excretion: urine
(Lexicomp)
28
agonists,
corticosteroids
(inhaled and
systemic), MAO
inhibitors,
multivitamins (with
ADE),
pentoxifylline,
phosphodiesterase 5
inhibitors,
prostacyclin
analogues, SSRIs,
bayberry, blue
cohosh, cayenne,
ephedra, ginger,
ginseng, kola
Chlorothiazide may
decrease effect of:
antidiabetic agents
Levels/effects of
Chlorothiazide may
be decreased by:
bile acid
sequestrians,
methylphenidate,
NSAIDs,
yohimbine, black
cohosh, California
poppy, coleus,
golden seal,
hawthorn,
mistletoe,
periwinkle, quinine
(Lexicomp, 2014)
Alcohol may
potentiate
(Lexicomp, 2014)
hypotensive
effects. Teach
orthostatic
precautions, and
blood pressure
monitoring.
Notify provider of
urinary retention
and signs of
reaction including
wheezing, chest
tightness, fever,
cough, itching,
seizures. Common
side effects include
weakness, fatigue,
parasthesia,
abdominal
cramping, GI
irritation.
Pregnancy
category C.
Crosses the
placenta, but may
be continued in
patients who
required thiazide
prior to pregnancy
Monitor: blood
pressure, intake
and output for
excessive water
loss, blood glucose
(monitor closely,
hyperglycemia
may occur), lipid
levels (increased
triglycerides and
cholesterol may
occur), electrolytes
(hypokalemia,
hyponatremia,
hypochloremia,
PERSONAL DRUGS
29
hypomagnesemia,
hypercalcemia
may occur)
Chlorthalidone
(Chlorthalidone)
(Lexicomp, 2014)
Pharmacodynamics:
Inhibits reabsorption
of sodium and
chloride in the
cortical-diluting
segment of the
ascending loop of
Henle
Pharmacokinetics:
Onset of action: Peak
effect 2-6 hours
Duration: 24-72
hours
Absorption: 65%
Protein binding: 75%
Metabolism: hepatic
Half-life elimination:
40-60 hours
(prolonged with renal
impairment)
Excretion: urine
Drug Interaction:
Avoid dofetilide
See above for
additional drugdrug interactions
Contraindications:
Hypersensitivity to
chlorothiazide or
sulfonamidederived drugs;
anuria
(Lexicomp, 2014)
Patient Education:
May take with
food. Take early
in the day (no later
than 6 p.m.) to
avoid nocturia,
unless instructed
otherwise.
Alcohol may
potentiate
hypotensive
effects. May cause
hypokalemia and
photosensitivity.
Pregnancy
category B,
crosses the
placenta, but may
be continued in
patients who
required thiazide
prior to pregnancy.
(Lexicomp, 2014)
Monitor: serum
electrolytes and
renal function,
blood glucose
(monitor closely,
may cause
hyperglycemia),
blood pressure,
and intake and
output to
determine daily
fluid loss
Chlorthalidone
Tablets:
25mg (100)
$55.17
50mg (100):
$68.04
100mg (100):
$101.25
(Lexicomp, 2014)
PERSONAL DRUGS
Hydrochlorothiazide
(Microzide)
(Lexicomp, 2014)
Pharmacodynamics:
Increased excretion
of sodium, water,
potassium, and
hydrogen by
inhibiting sodium
reabsorption in the
distal tubules
Pharmacokinetics:
Onset of action:
diuresis 2 hours
Duration: 6-12 hours
Absorption: well
absorbed when
administered with
food.
Protein binding:
40%-68%
Metabolism: not
metabolized
Half-life elimination:
6-15 hours
Excretion: urine
(Lexicomp, 2014)
30
Contraindications:
Do not give to
patients with
hypersensitivity to
sulfonamidederived drugs;
anuria.
(Lexicomp, 2014)
Drug Interaction:
Patient Education:
Avoid dofetilide
May be taken with
Increased
or without food.
effect/toxicity of
Take early in the
chlorothiazide by:
day (no later than
alcohol, alfuzosin,
6 p.m.) to avoid
opiod analgesics,
nocturia, unless
anticholinergics,
instructed
barbiturates, beta2- otherwise.
agonists,
Alcohol may
corticosteroids
potentiate
(inhaled and
antihypertensive
systemic), MAO
effects. Monitor
inhibitors,
glucose levels
multivitamins (with closely (may cause
ADE),
hyperglycemia).
pentoxifylline,
Teach blood
phosphodiesterase 5 pressure
inhibitors,
monitoring and
prostacyclin
orthostatic
analogues, SSRIs,
precautions.
bayberry, blue
Notify provider of
cohosh, cayenne,
urinary retention,
ephedra, ginger,
sudden vision
ginseng, kola
changes, eye pain
Hydroor irritation, rash.
chlorothiazide
Pregnancy
may decrease effect category B.
of: antidiabetic
Crosses the
agents.
placenta, but may
Levels/effects of
be continued in
Hydropatients who
chlorothiazide may required thiazide
be decreased by:
prior to pregnancy.
benazepril, bile acid
sequestrians,
Monitor: serum
methylphenidate,
electrolytes, blood
Hydrochlorothiazide
Capsules:
12.5mg (100):
$42.45
Microzide Capsules:
12.5mg (100):
$132.06
Hydrochlorothiazide
Tablets:
12.5mg (100):
$82.43
25mg (100): $8.48
50mg (100): $16.45
(Lexicomp, 2014)
PERSONAL DRUGS
31
NSAIDs,
yohimbine, black
cohosh, California
poppy, coleus,
golden seal,
hawthorn,
mistletoe,
periwinkle, quinine
(Lexicomp, 2014)
Methyclothiazide
(Methyclothiazide)
(Lexicomp, 2014)
Pharmacodynamics:
Inhibition of sodium
reabsorption in the
distal tubules causing
increased excretion of
sodium, water,
potassium, and
hydrogen
Pharmacokinetics:
Onset of action:
diuresis 2 hours
Duration: 1 day
Excretion: urine
(Lexicomp, 2014)
Drug Interactions:
Avoid use with
dofetilide
See interactions
with chlorothiazide
for additional drug
interactions.
glucose, renal
function, blood
pressure, intake
and output to
determine fluid
loss
Contraindications:
Hypersensitivity to
sulfonamidederived agents;
anuria
(Lexicomp, 2014)
Patient Education:
May take with
food or milk.
Take early in the
day (no later than
6 p.m.) to avoid
nocturia, unless
instructed
otherwise. Alcohol
may potentiate
hypotensive
effects. Teach
blood pressure
monitoring and
orthostatic
precautions.
Monitor glucose
levels closely (may
cause
hyperglycemia).
Monitor: serum
electrolytes and
renal function,
blood pressure,
intake and output
to determine daily
fluid loss
Contraindications:
Hypersensitivity
to sulfonamide-
Methyclothiazide
Tablets
5mg (100): $184.23
(Lexicomp, 2014)
PERSONAL DRUGS
32
derived agents;
anuria
(Lexicomp, 2014)
V. Drug of Choice: Hydrochlorothiazide
According to the American Society of Hypertension (ASH) and International Society of
Hypertension (ISH), the first-line treatment of HTN in the adult patient is either antiotensin II
receptor-blocker (ARB) or angiotensin converting enzyme-inhibitor (ACE inhibitor), however,
in the African-American population, it is acceptable to start with a thiazide diuretic or calcium
channel blocker (CCB) (Weber et al., 2013). Thiazide diuretics are useful for monotherapy in
the treatment of HTN because they lower blood pressure as effectively as other drug groups with
a greater likelihood of managing goal blood pressure (Flack et al., 2010). The most widely used
diuretic in HTN is hydrochlorothiazide (HCTZ), however, the use of chlorthalidone is preferred
in most situations due to the potency and longer duration of action that continues through the
night (The Medical Letter, 2012), and has been shown beneficial in improving the reduction of
cardiovascular events such as stroke and myocardial infarction (Weber et al, 2013).
Initial dosing of chlorthalidone should be 25mg once daily, and may be titrated up to
100mg/day depending on patient response (Lexicomp, 2014). Renal function and electrolyte
status should be assessed prior to starting therapy, and on a regular basis throughout, since
electrolyte disturbance is a common adverse effect. Discharge teaching should include how to
monitor fluid status and blood pressure on a regular basis (Lexicomp, 2014). Lifestyle
modifications of weight loss, exercise, and low sodium diet should also be encouraged. Instruct
the patient to immediately report urinary retention, rash, or signs of significant reaction
(Lexicomp, 2014). Follow-up after discharge will be necessary within 2-3 weeks to ensure
PERSONAL DRUGS
33
adequate dosage for blood pressure management (Weber et al., 2013). The APN with a current
CTP has the authority to prescribe thiazide diuretics in the state of Ohio (Ohio Board of Nursing,
2014).
Third Diagnosis: Pain with Spinal Cord Injury
26 year old male admitted to trauma ICU after sustaining spinal cord injury at cervical-6
location secondary to a diving accident. No significant past medical history or allergies noted.
After the initial phases of spinal shock suffered by this patient, he begins to experience moderate
intensity burning and tingling from the chest down and is anxious.
I. Definition of Diagnosis
Pain as a result of lesion or disease within the somatosensory nervous system is what
defines neuropathic pain associated with spinal cord injury, and is classified according to the
location of the pain, generally at-level or below-level of injury (Finnerup & Baastrup, 2012).
The pain descriptors in this population are typically verbalized early in the post-injury period as
tingling, burning, pins and needles, shooting, sharp, or shock-like, and are not related to
inflammation, movement, or local tissue damage (Finnerup & Baastrup, 2012). These sensations
are a result of the neuronal hyperexcitability secondary to changes in sodium and voltage-gated
calcium channels within the spinal cord (Finnerup & Baastrup, 2012).
II. Therapeutic Objective
The goal of therapy in the treatment of neuropathic pain in the patient with spinal cord
injury is to balance successful pain reduction with manageable adverse reactions (Dalal, Felix, &
Cardenas, 2013). Effective pain control within this population supports positive perceptions of
PERSONAL DRUGS
34
personal health, and contributes to increased function in daily activities. Improvement in mood,
anxiety, and sleep interference is also a goal of treatment that can be obtained with
pharmacotherapy, as well as cognitive-behavioral principles such as hypnosis (Finnerup &
Baastrup, 2012).
III. Effective Drug Groups
Opiod AnalgesicsFull Agonists
(morphine, fentanyl,
oxycodone,
hydrocodone,
hydromorphone,
meperidine, codeine,
methadone,
oxymorphone,
levorphanol)
Morphine (Morphine
Sulfate, oral)
15mg (100): $22.17
30mg (100): $37.77
Oxycodone
(Oxycodone HCl,
oral)
5mg (100): $48.10
10mg (100): $62.50
15mg (100): $189.48
20mg (100): $110.30
Hydromorphone
(Dilaudid, oral)
2mg (100): $129.83
4mg (100): $211.93
8mg (100): $385.72
Methadone
(Methadone HCl,
oral)
5mg (100): $8.87
10mg (100): $19.20
Pharmacodynamics:
Alters the perception
and response to pain
by binding to opiod
receptors in the CNS,
inhibiting the
ascending pain
pathway
Pharmacokinetics:
Absorption: Varying
rates of
bioavailability (35%100%).
Distribution:
Distributed to skeletal
mucle, liver, intestinal
tract, lungs, spleen,
brain. Varying levels
of distribution and
plasma binding (10%95%)
Metabolism: Hepatic
via CYP3A4 and
CYP2D6
Half-life elimination:
dependent on agent;
2-4 hours; prolonged
with extended release
Excretion: primarily
in urine; feces
Side Effects:
Common:
Somnolence, dizziness,
pruritus, constipation,
nausea, vomiting,
orthostatic
hypotension, headache,
confusion, dysphoria,
euphoria, nervousness,
rash, abdominal pain,
gastritis, weakness,
dyspnea, diaphoresis
Rare: Amenorrhea,
anaphylaxis, apnea,
bronchospasm, cardiac
arrest, decreased cough
reflex, dehydration,
intestinal obstruction,
laryngospasm,
myoclonus, respiratory
arrest, toxic psychoses
Monitor: Efficacy of
pain control, mental
status, vital signs; signs
of addiction, drug
abuse, and diversion
(Lexicomp, 2014)
Contraindications:
Hypersensitivity,
significant respiratory
depression, paralytic
ileus
Disease-related
precautions: Use
with caution in
adrenal insufficiency,
biliary tract
dysfunction, CNS
depression,
depression, or
suicidal tendencies,
history of drug abuse.
Contraindicated in
patients with
suspected or known
paralytic ileus.
Drug-drug
interactions: Avoid
concomitant use with
alcohol, azelastine,
fusidic acid, MAO
inhibitors,
paraldehyde. Use
with caution in
amphetemines,
CYP3A4 inhibitors,
and other CNS
depressants.
(Lexicomp, 2014)
(Lexicomp, 2014)
PERSONAL DRUGS
(Lexicomp, 2014)
Opiod AnalgesicsFull
Agonist/Reuptake
Inhibitors
(tapentadol,
tramadol)
Tramadol (Tramadol
HCl, oral)
50mg (100): $83.40
Tapentadol (Nucynta,
oral)
50mg (100): $287.45
75mg (100): $336.49
100mg (100):
$448.07
(Lexicomp, 2014)
Non-Steroidal AntiInflammatory
Agents (NSAIDS)
(diclofenac, etodolac,
fenoprofen,
floctafenine,
ibuprofen, ketorolac,
meclofenamate,
nabumetone,
naproxen, tolmetin)
Diclofenac
(Cataflam, oral)
35
Pharmacodynamics:
Binds to mu-opiate
receptors causing
inhibition of
ascending pain
pathways, and
inhibition of reuptake
of norepinephrine and
serotonin. Alters the
perception and
response to pain.
Pharmacokinetics:
Absorption: rapid
and complete.
Bioavailability 32%90% (depending on
formulation)
Distribution: protein
binding 20%.
Metabolism:
Extensively hepatic
via CYP2C9,
CYP2C19, and
CYP2D6 with first
pass effect.
Half-life elimination:
6-9 hours; prolonged
in elderly, hepatic, or
renal impairment
Excretion: urine
Side Effects:
Common: flushing,
dizziness, headache,
somnolence, insomnia,
constipation, nausea,
vomiting, dyspepsia,
weakness, orthostatic
hypotension, chest
pain, anxiety,
depression, euphoria,
hot flashes, xerostomia,
diaphoresis
Rare: allergic reaction,
anaphylactic reaction,
angioedema, abnormal
liver function tests,
bradycardia,
bronchospasm,
increased BUN and
creatinine, ECG
abnormalities, night
sweats, palpitations,
pulmonary edema,
tachycardia, seizure,
syncope
Monitor: pain relief,
blood pressure,
respiratory rate; signs
of abuse, tolerance,
addiction or suicidal
ideation
(Lexicomp, 2014)
(Lexicomp, 2014)
Pharmacodynamics:
Side Effects:
Inhibition of
Common: edema,
cyclooxygenase-1 and dizziness, headache,
2 enzymes, causing
pruritus, rash, fluid
decrease in
retention, abdominal
prostaglandin.
pain and distention,
Antipyretic,
constipation, diarrhea,
analgesic, and antiflatulence, heartburn,
inflammatory
peptic ulcer/GI bleed,
Pharmacokinetics:
anemia, increased
Absorption: 80%
bleeding time,
55%-100%
abnormal liver
bioavailability
enzymes, diaphoresis,
Contraindications:
Hypersensitivity;
acute intoxication
with alcohol or other
CNS depressants
Disease-related
precautions: Use
with caution in
patients with renal or
hepatic impairment;
abdominal
conditions; drug or
alcohol abuse
(potential for drug
dependency); head
trauma (exaggerated
increase in ICP may
occur); respiratory
disease (may be at
greater risk of
respiratory
depression)
Drug-drug
interactions:
azelastine (nasal),
carbamazepine,
conivaptan, fusidic
acid, MAO inhibitors,
paraldehyde
(Lexicomp, 2014)
Contraindications:
Hypersensitivity;
patients with allergic,
asthmatic, or
urticarial reaction
after taking NSAIDS
or aspirin.
Disease-related
precautions: May
compromise renal
function; use with
caution in
hypertension (may
PERSONAL DRUGS
50mg (100): $583.70
Etodolac (Etodolac,
oral)
400mg (100):
$146.25
500mg (100):
$148.00
Ibuprofen (Ibuprofen,
oral)
200mg (100): $4.67
400mg (100): $21.22
800mg (100): $38.10
(Lexicomp, 2014)
Non-Steroidal AntiInflammatory
Agents COX-2
Selective
(celecoxib)
Celecoxib (Celebrex,
oral)
50mg (60): $117.49
100mg (100):
$418.99
200mg (100):
$687.24
400mg (60): $618.53
(Lexicomp, 2014)
36
(depending on agent)
Distribution: Vd:
6.35L
Protein binding:
90%-99%
Metabolism: Hepatic;
some agents undergo
first-pass metabolism
Half-life elimination:
2-4 hours
Excretion: primarily
urine; feces
tinnitus
Rare: acute renal
failure,
agranulocytosis,
anaphylaxis, bone
marrow suppression,
decreased creatinine
clearance, duodenal
ulcer, hallucinations,
decreased
hemoglobin/hematocrit,
hypertension,
leukopenia,
hypertension,
pancreatitis, StevensJohnson syndrome,
thrombocytopenia,
Monitor: CBC, renal
function, liver function
(periodic), occult blood
loss, blood pressure
worsen existing
hypertension); use
with caution in
patients with
decreased hepatic
function; do not
administer to patients
with aspirin-sensitive
asthma; may increase
risk of aseptic
meningitis; increased
risk of MI and stroke
following CABG
(Lexicomp, 2014)
Drug-drug
interactions: Avoid
concomitant use with
floctafenine;
ketorolac (nasal &
systemic); COX-2
inhibitor;
omacetaxine;
pimozide
(Lexicomp, 2014)
(Lexicomp, 2014)
Pharmacodynamics:
Side Effects:
Contraindications:
Decreased formation
Common: peripheral
Hypersensitivity to
of prostaglandin
edema, dizziness, fever, celecoxib,
precursors by
headache, rash,
sulfonamides, aspirin,
inhibition of
abdominal pain,
or other NSAIDS.
prostaglandin
nausea, vomiting,
Disease-related
synthesis due to
diarrhea, flatulence,
precautions: Do not
decreasing the
arthralgia, cough,
administer to patients
activity of
pharyngitis, sinusitis
with aspirin-sensitive
cyclooxygenase-2.
Rare: acute renal
asthma; Risk of MI
Pharmacokinetics:
failure,
and stroke may be
Absorption: Absolute agranulocytosis,
increased with use
bioavailability
anaphylactic reaction,
following CABG;
Distribution: 97%
angioedema,
Should not be
protein binding.
cerebrovascular
replacement
Metabolism: Hepatic accident, heart failure,
treatment for
via CYP2C9 with
deep vein thrombosis,
corticosteroidformation of inactive esophageal perforation, dependent diseases;
metabolites
gangrene, hepatic
Use with caution in
Half-life elimination: failure and necrosis,
patients with CYP
11 hours
hypoglycemia, ileus,
isoenzyme
Excretion: primarily interstitial nephritis,
deficiency; Use with
feces; urine
intracranial
caution in renal or
PERSONAL DRUGS
Acetaminophen
(Tylenol)
Tylenol
(Acetaminophen,
oral)
325mg (100): $4.57
500mg (100): $2.61
(Lexicomp, 2014)
Salicylates
(Aspirin, Salsalate)
Aspirin (Aspirin,
oral)
37
hemorrhage,
(Lexicomp, 2014)
leukopenia,
pancytopenia, renal
papillary necrosis,
sudden death, suicide,
thrombocytopenia,
ventricular fibrillation
Monitor: CBC, renal
and liver function tests,
occult blood loss, pain
response, blood
pressure, observe for
weight gain and edema
(Lexicomp, 2014)
Pharmacodynamics:
Side Effects:
Inhibition of the
Common: rash,
synthesis of
decreased serum
prostaglandins
bicarbonate,
resulting in blockade hypocalcemia,
of peripheral pain
hyponatremia,
impulse
hyperglycemia, anemia,
Pharmacokinetics:
leukopenia,
Absorption: rate of
neutropenia,
absorption dependent pancytopenia,
on gastric emptying,
hyperammonia
and varies by dosage
Rare: hypersensitivity
form
reaction, nephrotoxicity
Distribution: 1L/kg
(with overdose),
Protein binding:
anaphylaxis
10%-25%
Monitor: with longMetabolism:
term use, monitor
primarily hepatic with APAP levels; serum
small amounts via
APAP level; monitor
CYP2E1
response to pain/fever
Half-life elimination:
2-3 hours; prolonged (Lexicomp, 2014)
in severe renal
insufficiency
Excretion: primarily
urine
(Lexicomp, 2014)
Pharmacodynamics:
Side Effects:
Irreversibly inhibits
Common:
formation of
gastrointestinal
thromboxane A2.
ulceration, duodenal
Inhibits COX-1 and 2 ulcers, rash, fatigue,
hepatic impairment
Drug-drug
interactions: Avoid
concomitant use with
floctafenine,
ketorolac, NSAIDS,
omacetaxine,
thioridazine
(Lexicomp, 2014)
Contraindications:
severe hepatic
impairment;
hypersensitivity to
any Tylenol
Disease-related
precautions: Use
with caution in
patients with
alcoholic liver
disease; in patients
with known G6PD
deficiency; in patients
with hepatic
impairment; in
patients with renal
impairment
Drug-drug
interactions: Avoid
concomitant use with
pimozide
(Lexicomp, 2014)
Contraindications:
Hypersensitivity;
asthma; rhinitis; nasal
polyps; inherited or
acquired bleeding
PERSONAL DRUGS
325mg (100): $2.47
(Lexicomp, 2014)
38
resulting in decreased
prostaglandin
production
Pharmacokinetics:
Absorption: rapid
absorption with 50%75% bioavailability
Distribution: Vd:
10L; readily
distributed to most
body fluids and
tissues
Metabolism:
Primarily hepatic
Half-life elimination:
3-10 hours depending
on dose
Excretion: urine
(Lexicomp, 2014)
insomnia, nervousness,
metabolic acidosis,
hyperkalemia,
hepatotoxicity,
increased
transaminases, anemia,
prolonged bleeding
times, increased
BUN/creatinine,
Rare: anaphylaxis,
laryngeal edema,
bronchospasm, renal
failure,
rhabdomyolysis,
hearing loss,
angioedema,
dysrhythmias
Monitor: With
prolonged therapy,
monitor CBC.
(Lexicomp, 2014)
Tricyclic
Antidepressants
(amitriptyline,
nortryptyline,
imipramine)
Amitriptyline
(Amitriptyline HCl,
oral)
10mg (100): $18.03
25mg (100): $36.10
50mg (100): $64.15
100mg (100):
$111.10
Imipramine
(Imipramine HCl,
oral)
10mg (100): $42.96
Pharmacodynamics:
Increases synaptic
concentration of
serotonin and
norepinephrine in
CNS.
Pharmacokinetics:
Metabolism: Hepatic
Half-life elimination:
9-27 hours
Excretion: Primarily
urine, feces
(Lexicomp, 2014)
Side Effects:
Common: orthostatic
hypotension,
anticholinergic effects
(constipation, blurred
vision, xerostomia,
urinary retention),
dizziness, sedation,
fatigue, impaired
coordination, weight
gain, nausea, vomiting,
numbness, tremor,
weakness, diaphoresis,
withdrawal reactions
Rare: cardiomyopathy,
paresthesia, allergic
rash, heart block,
seizure, coma
Monitor: Monitor
disorders; viral
infections
Disease-related
precautions: Use
with caution in
patients with platelet
and bleeding
disorders; patients
with dehydration;
patients with heavy
alcohol use; patients
with erosive gastritis
or peptic ulcer
disease; patients with
renal impairment.
Avoid use in severe
hepatic failure
Drug-drug
interactions: Avoid
concomitant use with
floctafenine,
influenze virus
vaccine
(live/attenuated),
ketorolac,
omacetaxine
(Lexicomp, 2014)
Contraindications:
Disease-related
precautions: Use
with caution in
patients with a history
of cardiovascular
disease; patients with
diabetes mellitus,
hepatic impairment,
renal impairment;
those at risk of
seizures
Drug-drug
interactions: Avoid
concomitant use with
aclidinium, cisapride,
iobenguane I 123,
ipratropium,
linezolid, MAO
PERSONAL DRUGS
25mg (100): $71.75
50mg (100): $121.85
(Lexicomp, 2014)
Seratonin and
Norepinephrine
Reuptake Inhibitors
(venlafaxine,
duloxetine,
milnacipran)
Venlafaxine (Effexor
XR, oral)
37.5mg (30):
$203.22
150mg (30): $248.06
Duloxetine
(Cymbalta, oral)
20mg (60): $466.56
60mg (30): $261.72
(Lexicomp, 2014)
39
blood pressure and
pulse rate prior to and
during initial therapy;
ECG in patients with
cardiac disease and
older adults
(Lexicomp, 2014)
Pharmacodynamics:
Side Effects:
Inhibits serotonin,
Common: headache,
norepinephrine, and
somnolence, dizziness,
dopamine reuptake in insomnia, nervousness,
the neurons
anxiety, nausea,
Pharmacokinetics:
xerostomia, anorexia,
Absorption: 92%
constipation, weakness,
with 45%
diaphoresis,
bioavailability
vasodilation,
Metabolism: Hepatic tachycardia,
via CYP2D6
palpitation, yawning,
Half-life elimination: abnormal dreams,
5-10 hours; prolonged chills, agitation,
in cirrhosis and renal confusion, rash,
impairment
pruritus, decreased
Excretion: urine
libido,
hypercholesterolemia,
(Lexicomp, 2014)
abdominal pain,
diarrhea, vomiting,
dyspnea, urinary
frequency, tremor,
seizure, abnormal
accomidation,
pharyngitis, infection
Rare: anaphylaxis,
angioedema,
appendicitis,
arrhythmia, increased
bleeding time,
catatonia, dehydration,
fatty liver, hepatic
failure, abnormal
kidney function,
Stevens-Johnson
syndrome, suicidal
ideation,
thrombocytopenia,
withdrawal syndrome
Monitor: blood
inhibitors, methylene
blue, moxonidine,
tiotropium,
umeclidinium
(Lexicomp, 2014
Contraindications:
Hypersensitivity to
SNRIs; use of MAO
inhibitors intended to
treat psychosis
disorders; in patients
receiving linezolid or
I.V. methylene blue
Disease-related
precautions: Use
with caution in
patients with recent
MI, unstable heart
disease, or
hyperthyroidism;
with hepatic
impairment; in
narrow-angle
glaucoma; with renal
impairment; seizure
disorders
Drug-drug
interactions: Avoid
concomitant use with
conivaptan, fusidic
acid, iobenguane I
123, linezolid, MAO
inhibitors, methylene
blue
(Lexicomp, 2014)
PERSONAL DRUGS
Anti-Epileptics
(carbamazepine,
gabapentin,
pregabalin)
Carbamazepine
(Tegretol, oral)
200mg (100):
$157.19
(Tegretol-XR, oral)
100mg (100): $80.14
200mg (100):$159.94
400mg (100):$319.65
Gabapentin
(Gabapentin, oral)
100mg (100): $53.24
300mg (100):$133.11
400mg (100):$159.71
(Neurontin, oral)
100mg (100):$117.78
300mg (50): $161.04
400mg (50): $186.98
40
Pharmacodynamics:
Anti-nociceptive
activity. Inhibits
excitatory
neurotransmitter
release.
Pharmacokinetics:
Distribution: Vd:
0.5L/kg
Metabolism:
(carbamazepine:
hepatic via CYP3A4)
Half-life elimination:
6 hours; extended
with carbamazepine
Excretion: primarily
urine; feces
(Lexicomp, 2014)
Pregabalin (Lyrica,
oral)
25mg (90): $395.59
300mg (90):$395.59
(Lexicomp, 2014)
pressure, cholesterol,
mental status for
depression, signs of
serotonin syndrome
(Lexicomp, 2014)
Side Effects:
Common: dizziness,
drowsiness, fatigue,
peripheral edema,
hostility, tremor,
headache, depression,
nervousness, pruritus,
weight gain, diarrhea,
nausea, vomiting,
constipation,
impotence, leukopenia,
weakness, myalgia,
blurred vision, rhinitis,
fever, neuroleptic
malignant syndrome
Rare: anaphylaxis,
apnea, cholecystitis,
delirium, dystonia,
extrapyramidal
syndrome, dermatitis,
pancreatitis,
photosensitivity, rash,
Stevens-Johnson
syndrome, syncope,
urinary retention
Monitor: CBC, lipid
panel, liver and renal
function tests, thyroid
function tests; weight;
for multi-organ
hypersensitivity
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to
carbamazepine,
tricyclic
antidepressants or
any component of
formulations; within
14 days of MAO
inhibitor use
Disease-related
precautions: Use
with caution in
patients with renal
failure; severe
cardiovascular
disease; history of
seizure disorder
Drug-drug
interactions: Avoid
concomitant usew
with azelastine,
paraldehyde; With
carbamazepine, use
caution with drugs
having CYP
metabolism
(Lexicomp, 2014)
IV. Effective Drug Classification: Anti-epileptics
Drug Name
Efficacy
Carbamazepine
(Carbatrol,
Pharmacodynamics:
Limits the influx of
Safety
Drug
Interaction:
Suitability
Cost
Patient Education:
Avoid alcohol.
Tablets
Carbamazepine,
PERSONAL DRUGS
Epitol, Equetro,
Tegretol,
Tegretol XR)
(Lexicomp,
2014)
sodium ions across
cell membranes
causing a decrease in
temporal stimulation
causing neural
discharge.
Antineuralgic
effects.
Pharmacokinetics:
Absorption: slow.
85% bioavailability
Distribution: Vd:
0.59-2 L/kg
Protein binding:
75%-90%
Metabolism:
Hepatic via
CYP3A4
Half-life
elimination: variable
depending on
dosing; initial 25-65
hours
Excretion: primarily
urine; feces
(Lexicomp, 2014)
41
Avoid
concomitant use
with abiraterone
acetate,
apixaban,
artemether,
axitinib,
bedaquiline,
boceprevir,
bortezomib,
bosutinib,
cabozantinib,
clozapine,
conivaptan,
crizotinib,
dabigatran
etexilate,
dienogest,
dolutegravir,
dronedarone,
enzalutamide,
everolimus,
fusidic acid,
ibrutinib,
itraconazole,
ivacaftor,
lapatinib,
lumefantrine,
lurasidone,
macitentan,
MAO inhibitors,
mifepristone,
nefazodone,
nifedipine,
nilotinib,
nisoldipine,
paraldehyde,
pazopanib,
pirfenidone,
pomalidomide,
ponatinib,
praziquantel,
ranolazine,
regorafenib,
reverse
transcriptase
May open capsules
and sprinkle over
food. Do not take
with grapefruit
juice. Do not
crush or chew
capsules or
extended release
tablets. Take XR
tablets with meals.
Do not abruptly
stop taking
medication; may
cause seizures.
oral
200mg (100):
$40.65
Tegretol, oral
200mg (100):
$157.19
Epitol, oral
200mg (100):
$30.17
Carbamazepine
ER, oral
200mg (100):
$139.94
400mg (100):
$279.69
Tegretol XR,
oral
100mg (100):
$80.14
200mg (100):
$159.94
400mg (100):
$319.64
Capsules
Monitor: CBC
with differential,
serum iron, lipid
panel, liver
function tests,
renal function.
Observe for excess
sedation. Watch
for rash with
initiating therapy.
Baseline and
periodic eye exams (Lexicomp,
are recommended. 2014)
Contraindications:
Hyper-sensitivity
to carbamazepine
or tricyclic antidepressants; bone
marrow
depression; with or
within 14 days of
MAO inhibitors;
concomitant use
with reverse
transcriptase
inhibitors.
(Lexicomp, 2014)
PERSONAL DRUGS
42
inhibitors,
rivaroxaban,
roflumilast,
romidepsin,
simeprevir,
sofosbuvir,
sorafenib,
telaprevir,
ticagrelor,
tofacitinib,
tolvaptan,
tormifene,
tramadol,
ulipristal,
vandetanib,
vemurafenib,
vincristine,
voriconazole
Carbemazepine
may increase the
levels of:
adenosine,
alcohol,
buprenorphine,
clarithromycin,
clomipramine,
clozapine, CNS
depressants,
desmopressin,
eslicarbazepine,
fosphenytoin,
hydrocodone,
ifosfamide,
lithium, MAO
inhibitors,
methotrimeprazi
ne, metyrosine,
mirtazepine,
paraldehyde,
phenytoin,
pramipexole,
ropinirole,
rotigotine.
Carbamazepine
may be
increased by:
PERSONAL DRUGS
43
allopurinol,
calcium channel
blockers,
carbonic
anhydrase
inhibitors,
cimetidine,
clarithromycin,
conivaptan,
CYP3A4
inhibitors,
danazol,
darunavir,
doxylamine,
droperidol,
fluconazole,
fusidic acid,
grapefruit juice,
hydroxizine,
isoniazid,
lamotrigine,
macrolide
antibiotics,
magnesium
sulfate, protease
inhibitors,
quinine, SSRIs,
tapentadol,
telaprevir,
thiazide
diuretics,
tramadol,
zolpidem
Carbemazepine
may be
decreased by:
bosentan,
CYP3A4
inducers,
dabrafenib,
deferasirox,
felbamate,
fosphenytoin,
ketorolac,
mefloquine,
methylfolate,
PERSONAL DRUGS
Pregabalin
(Lyrica)
mitotane,
orlistat,
phenytoin,
reverse
transcriptase
inhibitors,
rufinamide,
theophylline,
tramadol,
valproic acid
(Lexicomp,
2014)
Pharmacodynamics: Drug
Inhibits excitatory
Interaction:
neuronal release by
Avoid
binding to alpha2concomitant use
delta subunits of
with paraldehyde
calcium channels
Pregabalin may
within CNS.
increase the
Pharmacokinetics:
effects of:
Onset of action:
alcohol,
Pain relief noted as
antidiabetic
early as first week of agents,
therapy
buprenorphine,
Absorption:
CNS
Bioavailability
depressants,
>90%
hydrocodone,
Protein binding: 0% methotrimeprazi
Half-life
ne, metyrosine,
elimination: 6.3
mirazapine,
hours
paraldehyde,
Excretion: urine
pramipexole,
ropinirole,
(Lexicomp, 2014)
rotigotine,
SSRIs, zolpidem
Levels of
Pregabalin may
be increased by:
doxylamine,
droperidol,
hydroxyzine,
magnesium
sulfate,
methotrimeprazi
ne, perampanel,
sodium oxybate,
44
Patient Education:
Avoid alcohol.
May take without
regard to food.
Avoid valerian, St.
John’s wort, kava
kava. Monitor
weight and check
for fluid retention.
Do not stop taking
abruptly.
Monitor: efficacy
of pain control;
sedation; weight
gain/edema;
symptoms of
myopathy or
ocular disturbance.
Contraindications:
Hypersensitivity to
pregabalin or any
component of the
formulation
(Lexicomp, 2014)
Capsules
Lyrica, oral
25mg (90):
$395.59
100mg (90):
$395.59
300mg (90):
$395.59
Solution
Lyrica, oral
20mg/mL (473
mL): $553.82
(Lexicomp,
2014)
PERSONAL DRUGS
45
tapentadol
Levels of
Pregabalin may
be decreased by:
ketorolac,
mefloquine,
orlistat
Gabapentin
(Gralise,
Neurontin)
(Lexicomp,
2014)
(Lexicomp,
2014)
Pharmacodynamics: Drug
Modulation of the
Interaction:
release of excitatory Avoid
neurotransmitters by concomitant use
binding to sites of
with azelastine,
voltage-gated
paraldehyde
calcium channels.
Gabapentin may
Pharmacokinetics:
increase the
Absorption:
effects of:
Variable, with
alcohol,
variable
buprenorphine,
bioavailability
CNS
depending on dose
depressants,
and formula
hydrocodone,
(immediate-release
methotrimeprazi
vs. extended-release) ne, metyrosine,
Distribution: Vd:
mirtazapine,
58L
paraldehyde,
Protein binding: 3% pramipexole,
Half-life
ropinirole,
elimination: 5-7
rotigotine,
hours (prolonged
SSRIs, zolpidem
with anuria)
Effects of
Excretion: urine
Gabapentin may
be increased by:
(Lexicomp, 2014)
doxylamine,
droperidol,
hydroxyzine,
methotrimeprazi
ne, perampanel,
Sodium oxybate,
tapentadol
Effects of
Gabapentin may
be decreased by:
Antacids,
Patient Education:
Avoid alcohol.
With immediate
release, take first
dose in evening to
avoid dizziness
and somnolence.
With extended
release, take with
evening meal. Do
no crush, chew, or
split. Do not
abruptly stop
taking medication.
Monitor: For CNS
depression.
Monitor for
multiorgan
hypersensitivity.
Contraindications:
Hypersenisitivity
to gabapentin or
any component of
the formulation
Use caution with
renal impairment
(dosage
adjustment may be
required)
(Lexicomp, 2014)
Capsules
Gabapentin, oral
100mg (100):
$53.24
300mg (100):
$133.11
400mg (100):
$159.71
Neurontin, oral
100mg (100):
$117.78
300mg (50):
$161.04
400mg (50):
$186.98
Tablets
Gabapentin, oral
600mg (100):
$252.65
800mg (100):
$303.15
Neurontin, oral
600mg (100):
$559.45
800mg (100):
$671.24
(Lexicomp,
2014)
PERSONAL DRUGS
46
ketorolac,
magnesium salts,
mefloquine,
orlistat
(Lexicomp,
2014)
V. Drug of Choice: Pregabalin
Currently, the only FDA-approved medication for treatment of neuropathic pain
associated with spinal cord injury is pregabalin, which is considered class I evidence for
treatment of pain in spinal cord injury in two published studies on spinal cord injury (Dalal et al.,
2013). By binding the alpha2-delta subunits in the CNS, pregabalin reduces neuronal
hyperexcitability passing through pain pathways, and is favorable in this patient population due
to its potency, greater rate of absorption, and decreased possibility for drug interactions due to its
lack of activity at the CYP450 enzyme (Dalal et al., 2013).
Pregabalin is also considered the
drug of choice for patients additionally experiencing anxiety (Finnerup & Baastrup, 2012).
Initial dosing is recommended at 150 mg/day, and may be titrated up to 600 mg/day
based on tolerability and efficacy (Dalal et al., 2013). For patients experiencing neuropathic pain
associated with spinal cord injury, twice daily dosing is recommended for better pain relief. Due
to the chronic issue of neuropathic pain with spinal cord injury, patients may take pregabalin for
life, but should be tapered gradually over one week prior to discontinuation, if the patient no
longer obtains relief (Dalal et al., 2013). Discuss common adverse events with the patient, which
include dizziness, somnolence, and peripheral edema, and immediately report signs of
depression, thoughts of suicide, edema of legs or abdomen, changes in vision, or significant skin
rash. Educate the patient to monitor weight for fluid retention and to not abruptly stop taking the
PERSONAL DRUGS
47
medication if he feels it is not working (Lexicomp, 2014). Additional teaching from an
interdisciplinary standpoint includes strengthening and conditioning excercises, optimal
movement techniques, and physical therapy to also help with pain reduction (Finnerup &
Baastrup, 2012). A follow-up appointment should be scheduled for a week following discharge
to ensure efficacy of dosing, and to increase dosing if necessary. The APN with a valid CTP has
the authority to prescribe pregabalin in the state of Ohio (Ohio Board of Nursing, 2014).
Fourth Diagnosis: Dyslipidemia in the Human Immunodeficiency Virus (HIV)-infected
Patient Status Post Myocardial Infarction
A 52 year old male with history of HIV is admitted to the coronary care intensive care
unit status post myocardial infarction (MI). Vital signs: BP 136/76; HR 82bpm; RR 20bpm; O2
sat 95% on 2L nasal cannula. His lipid profile shows high density lipoprotein (HDL) of
32mg/dL, low-density lipoprotein of 168mg/dL, and triglyceride (TG) level of 230mg/dL. The
patient is currently at an acceptable viral suppression with antiretroviral treatment of indinavir
800mg BID and ritonavir 200mg BID. He smokes 1 ppd, but has no other significant past
medical history. The only significant family history includes his father who has a history of MI
at the age of 50 and coronary heart disease.
I. Definition of Diagnosis
Cholesterol, comprised of very-low-density lipoproteins (VLDLs), low-density
lipoproteins (LDLs), and high-density lipoproteins (HDLs), along with inflammation and
endothelial dysfunction, are all conditions present for atherosclerotic plaque formation in
cardiovascular disease (CVD). (Blaha, Ketlowgetswe, Nudmele, Gluckman, & Blumenthal,
2011). The delivery of cholesterol to the tissues is from LDL, and increased serum
PERSONAL DRUGS
48
concentrations of LDLs along with low levels of HDLs are strong indicators for increased
coronary risk (Brashers, 2010). Secondary to systemic immune activation that stimulate
inflammation and atherosclerosis, and antiretroviral therapy (ART)-related metabolic changes,
patients with HIV are at an increased risk for CVD, especially with patients taking firstgeneration protease inhibitors, which have been shown to increase LDL, triglycerides, and
cholesterol (Hemkens & Bucher, 2013). Diagnosis of dyslipidemia occurs with high LDL-C
(>100mg/dL), high TG (>150mg/dL), and low HDL (<40mg/dL) (Brashers, 2010).
II. Therapeutic Objective
The goal of treatment is to reduce the risk of further atherosclerotic cardiovascular
disease (ASCVD) through secondary prevention by lowering LDL-C and TG (Stone et al.,
2013). There has been no evidence to suggest treatment targets for LDL-C and non-HDL-C,
however, appropriate intensity statin therapy should be initiated and maintained as secondary
prevention to further reduce ASCVD risk for those most likely to benefit (Stone et al., 2013).
Due to potential drug interactions with ART in HIV patients, appropriate statin therapy must be
considered (Hemkens & Bucher, 2013). Treatment goals for HIV patients with ASCVD risk
remain the same for the non-HIV population in that achievement of LDL-C with statin therapy
and diet is the first priority in the management of dyslipidemia (Hemkens & Bucher, 2013).
III. Effective Drug Groups
Drug Classification
HMG-CoA
Reductase
Inhibitors (Statins)
(atorvastatin,
fluvastatin, lovastatin,
pitavastatin,
Efficacy
Pharmacodynamics:
Inhibits cholesterol
biosynthesis by
inhibiting 3hydroxyl3methylglutaryl-
Safety
Side Effects:
Common: headache,
fatigue, insomnia,
dyspepsia, diarrhea,
abdominal pain,
myalgia, arthralgia,
Suitability
Contraindications:
Hypersensitivity to any
statin formulation; active
liver disease;
unexplained persistent
elevation of serum
PERSONAL DRUGS
pravastatin,
rosuvastatin,
simvastatin)
Atorvastatin (Lipitor,
oral)
10mg (100): $589.08
20mg (100): $840.34
80mg (90): $720.28
Rosuvastatin
(Crestor, oral)
5mg (90): $616.80
20mg (90): $616.80
Simvastatin (Zocor,
oral)
5mg (30): $95.87
20mg (30): $224.18
(Lexicomp, 2014)
Bile-Acid
Sequestrants
(colesevelam,
colestipol,
cholestyramine)
Colestevelam
(Welchol, oral)
625mg (180):
$390.96
Colestipol (Colestid,
oral)
1g (120): $144.77
49
coenzyme A
reductase. Increases
HDL, decreases
LDL, cholesterol,
and plasma
triglycerides
Pharmacokinetics:
Absorption: Rapid,
with 30%
bioavailability.
First pass effect
through liver
Metabolism:
Primarily through
inactive and active
metabolites via
CYP2C9, 2C8, and
3A4.
Half-life
Elimination: 14-19
hours
Excretion:
primarily feces;
urine, bile
sinusitis
Rare: increased
alkaline phospatase,
anaphylaxis, anemia,
angioedema,
cognitive
impairment,
depression, diabetes
mellitus, dyspnea,
fever, flushing,
increased HbA1c,
hemolytic anemia,
hepatic failure,
hypersensitivity
reaction, muscle
cramps, StevensJohnson syndrome,
thrombocytopenia,
vomiting
Monitor: Lipid levels
prior to initiation,
then fasting lipid
levels 4 weeks after
initiation; CPK levels
prior to initiation and
(Lexicomp, 2014)
recheck with
symptoms of
myopathy; liver
function tests, repeat
as needed
(Lexicomp, 2014)
Pharmacodynamics: Side Effects:
Increases the fecal
Common:
loss of low density
constipation,
lipoprotein (LDL)
diarrhea, nausea,
cholesterol by
myocardial
binding with bile
infarction, aortic
acids and
stenosis, bradycardia,
eliminating in the
hypertension,
feces
headache, fatigue,
Pharmacokinetics:
hypoglycemia,
Absorption: none
hyperglycemia,
Excretion:
dyspepsia, increased
primarily feces;
C-reactive protein,
urine
back pain, weakness,
upper respiratory
transaminases;
pregnancy; breastfeeding
Disease-related
precautions: Use with
caution in patients who
consume large amounts
of alcohol, or with
history of liver disease;
use with caution in
patients with severe renal
impairment
Drug-drug interactions:
Substrate of CYP3A4, Pglycoprotein. Avoid
concomitant use with
bosutinib, conivaptan,
cyclosporine, fusidic
acid, gemfibrozil,
pimozide, pomalidomide,
posaconazole, red yeast
rice, silodosin, telaprevir,
tipranavir, topotecan,
vincristine
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to any
bile-acid sequestrant
formulation. Should not
be used in patients with
baseline fasting
triglyceride levels
>300mg/dL
Disease-related
precautions: Avoid use
in patients with
gastroparesis or other
severe GI motility
disorders. Use with
caution in patients
PERSONAL DRUGS
(Lexicomp, 2014)
Cholesterol
Absorption
Inhibitor
(ezetimibe)
Ezetimibe (Zetia,
oral)
10mg (90): $589.14
(Lexicomp, 2014)
50
(Lexicomp, 2014)
tract infection,
myalgia
Rare: dysphagia,
esophageal
obstruction, fecal
impaction,
hemorrhoids,
increased serum
transaminases,
infection, intestinal
obstruction,
pancreatitis, unstable
angina
Monitor: Fasting
lipid profile prior to
initiating, 3 months
after initiation, and
every 6-12 months
thereafter; monitor
bowel function.
(Lexicomp, 2014)
Pharmacodynamics: Side Effects:
Decreases delivery
Common: fatigue,
of cholesterol to
diarrhea, increased
liver and increases
transaminase,
cholesterol
arthralgia, extremety
clearance from the
pain, upper
blood by inhibiting
respiratory tract
absorption of
infection, sinusitis
cholesterol at brush Rare: anaphylaxis,
border in small
angioedema,
intestines.
autoimmune
Decreases total
hepatitis,
LDL, ApoB, and
cholecystitis,
triglycerides (TG).
increased CPK,
Increases HDL
dizziness, headache,
Pharmacokinetics:
pancreatitis,
Absorption:
parasthesia,
Variable
rhabdomyolysis,
bioavailability
thrombocytopenia
Metabolism:
Monitor: Assess lipid
undergoes
profile prior to
glucuronide
initiation of therapy
conjugation in small and at regular
intestines and liver; intervals. Monitor
forms active
LFTs and for signs of
susceptible to fat-soluble
vitamin deficiencies
Drug-drug interactions:
Avoid concomitant use
with deferasirox
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to
ezetimibe or any
formulation; concomitant
use with HMG-CoA
reductase inhibitor in
patients with active
hepatic disease;
pregnancy; breastfeeding
Disease-related
precautions:
Use with caution in
patients with mild
hepatic impairment or
severe renal impairment
Drug-drug interactions:
No known interactions
where avoidance of
concomitant use is
recommended
(Lexicomp, 2014)
PERSONAL DRUGS
Fibrates
(bezafibrate,
fenofibrate,
gemfibrozil)
Fenofibrate (Tricor,
oral)
48mg (90): $209.87
145mg (90): $629.59
(Fibricor, oral)
35mg (30): $41.18
105mg (30): $123.56
Gemfibrozil (Lopid,
oral)
600mg (60): $230.88
(Lexicomp, 2014)
Niacin
(niacin, niacor,
niaspan)
51
metabolites
Half-life
Elimination: 22
hours
Excretion:
primarily feces;
urine
(Lexicomp, 2014)
Pharmacodynamics:
Increases VLDLl
catabolism, fatty
acid oxidation, and
elimination of
triglyceride-rich
particles by
downregulating
apoprotein C-III
(inhibitor of
lipoprotein lipase),
and upregulates the
synthesis of
apolipoprotien A-I.
Decreases VLDL,
and total plasma
triglyceride.
Moderate increase
in HDL
Pharmacokinetics:
Absorption:
increased when
taken with food.
80% bioavailability
Metabolism: hepatic
metabolism with
enterohepatic
recycling
Half-life
Elimination: 20
hours
Excretion:
primarily urine;
feces
(Lexicomp, 2014)
Pharmacodynamics:
Partial inhibition of
free fatty acids from
cholelithiasis
(Lexicomp, 2014)
Side Effects:
Common: dyspepsia,
fatigue, vertigo,
eczema, rash,
abdominal pain,
nausea/vomiting,
atrial fibrillation
Rare: increased
alkaline phosphatase,
anemia, angioedema,
arthralgia,
cholelithiasis,
cholecystitis,
increased creatine
phosphokinase,
dermatitis, headache,
hypokalemia,
laryngeal edema,
myalgia, myopathy,
nephrotoxicity,
paresthesia,
Raynaud’s
phenomenon,
rhabdomyolysis,
somnolence
Monitor: Assess
serum cholesterol,
and periodical LFTs
and CBCs for first
year. Monitor for GI
disturbances
Contraindications:
Hypersensitivity to any
fibrate formulation;
hepatic or severe renal
impairment; primary
biliary cirrhosis; preexisting gallbladder
disease
Disease-related
precautions: Use with
caution in patients with
mild-to-moderate renal
impairment
Drug-drug interactions:
Substrate of CYP3A4.
Inhibits CYP1A2,
CYP2C19, CYP2C8, and
CYP2C9. With
gemfibrozil, avoid
concomitant use with
atorvastatin, bexarotene,
enzalutamide, fluvastatin,
lovastatin, pirfenidone,
pitavastatin, pravastatin,
repaglinide, rosuvastatin,
simvastatin
(Lexicomp, 2014)
(Lexicomp, 2014)
Side Effects:
Common:
arrhythmias, edema,
Contraindications:
Hypersensitivity to any
niacin formulation;
PERSONAL DRUGS
Niacin (Niacin, oral)
50mg (100): $2.10
500mg (100): $4.30
Niacin (Niacor, oral)
500mg (100): $38.03
Omega-3 Acids
(lovaza, vascepa)
Lovaza, oral
1g (120): $252.94
Vascepa, oral
1g (120): $220.80
(Lexicomp, 2014)
52
adipose tissue and
increased
liopoprotein lipase
activity, which
increases the rate of
chylomicron
triglyceride removal
from plasma.
Decreases total
cholesterol,
apoliprotein B,
triglycerides,
VLDL, LDL, and
increases HDL.
Pharmacokinetics:
Absorption: rapid
and extensive
Metabolism:
extensive first pass
metabolism
Half-life
Elimination: 20-45
minutes
Excretion: urine
palpitation,
tachycardia, chills,
flushing, pruritus,
gastrointestinal
distress, blurred
vision, fatigue,
glucose intolerance,
hyperuricemia,
hepatic toxicity,
peptic ulcer
exacerbation, dry
eyes
Rare: syncope,
hepatic necrosis,
myalgia, myopathy,
rhabdomyolysis (with
HMG-CoA
reductasee inhibitor
concurrency),
hypersensitivity
reaction
Monitor: Baseline
hepatic
transaminases,
fasting blood glucose
(Lexicomp, 2014)
and uric acid prior to
initiation and every 6
months
(Lexicomp, 2014)
Pharmacodynamics: Side Effects:
Not completely
Common: eructation,
defined. Possible
taste perversion,
inhibition of acyl
dyspepsia, increased
CoA:1, 2
AST/ALT, pruritus,
diacylglycerol
rash
acyltransferase,
Rare: anaphylactic
increased hepaticreaction, asthma,
beta-oxidation,
prolonged bleeding
decrease in hepatic
time, cardiac arrest,
synthesis of
gastritis,
triglycerides,
hyperlipidemia,
increase in plasma
hypertension,
lipoprotein lipase
vasodilation
acitivity
Monitor: Assess lipid
panel at baseline and
(Lexicomp, 2014)
periodically. Monitor
active hepatic disease;
active peptic ulcer;
arterial hemorrhage
Disease-related
precautions: Use with
caution in patients with
unstable angina or MI;
diabetes mellitus; active
gallbladder disease;
hepatic impairment or
heavy alcohol users;
renal impairment
Drug-drug interactions:
No known interactions in
which to avoid
concomitant use. May
increase the effects of
HMG-CoA reductase
inhibitors, and decrease
the levels of bile-acid
sequestrants
(Lexicomp, 2014)
Contraindications:
Hypersensitivity to
omega-3 acids or any
component of
formulation
Disease-related
precautions: Use with
caution in patients with
fish or shellfish allergy;
Not indicated for the
treatment of atrial
fibrillation
Drug-drug interactions:
No known interactions
where concomitant use
should be avoided. May
increase the effects of
PERSONAL DRUGS
53
hepatic transaminase
levels periodically.
(Lexicomp, 2014)
antiplatelet agents and
anticoagulants
(Lexicomp, 2014)
IV. Effective Drug Classification: HMG-CoA Reductase Inhibitors (Statins)
Drug Name
Efficacy
Safety
Suitability
Cost
Atorvastatin
(Lipitor)
Pharmacodynamics:
Inhibits the enzyme
that catalyzes the
rate-limiting step in
cholesterol
synthesis.
Reduction in hepatic
cholesterol results in
increased
expression of LDL
receptors, which
increases uptake and
clearance of LDL
from the blood.
Pharmacokinetics:
Onset of Action: 35 days with
maximal decrease in
plasma cholesterol
and triglycerides of
2 weeks
Absorption: rapid.
30% bioavailability
Distribution: Vd:
~381 L
Protein Binding:
98%
Metabolism:
hepatic
Half-life
Elimination: 20-30
hours
Time to serum peak
concentration: 1-2
hours
Excretion: bile;
Drug Interactions:
Avoid concomitant
use with bosutinib,
conivaptan,
cyclosporine, fusidic
acid, gemfibrozil,
pimozide,
pmalidomide,
posaconazole, red
yeast rice, silodosin,
telaprevir, tipranavir,
topotecan,
vincristine
May increase levels
of: afatinib,
aliskiren,
arepiprazole,
bosutinib,
cimetidine,
daptomycin, digoxin,
diltiazem, dofetilide,
everolimus,
ketoconazole,
lopitapide,
midazolam,
pazopanib, Pglycoprotein/ABCB1
substrates, pimozide,
pomalidomide,
prucalopride,
rivaroxaban,
silodosin,
spironolactone,
topotecan,
trabectedin,
verapamil,
Patient Education:
Avoid excessive
alcohol
consumption. Do
not take with
grapefruit juice.
Do not take with
St. Johns Wort.
May be taken with
food and without
regard to time of
day. Teach
importance of
proper diet and
exercise.
Atorvastatin
Calcium
10mg (90):
$346.94
20mg (90):
$494.80
40mg(90):
$494.89
80mg (90):
$494.89
(Lexicomp,
2014)
Monitor: baseline
fasting lipid panel,
within 4-12 weeks
after initiation or
dose adjustment,
and every 3-12
months. Baseline
measurement of
hepatic function.
Measure CPK in
any patient with
symptoms of
myopathy
Contraindications:
Hypersensitivity to
atorvastatin; active
liver disease;
unexplained
persistent
Lipitor
10mg (100):
$589.08
20mg (100):
$840.34
40mg(100):
$840.34
80mg (90):
$720.28
(Lexicomp,
2014)
PERSONAL DRUGS
urine
(Lexicomp, 2014)
Fluvastatin
(Lescol,
Lescol XL)
(Lexicomp,
2014)
vincristine
Atorvastatin may be
increased by:
amiodarone,
azithromycin,
clarithromycin,
cyclosporine,
CYP3A4 Inhibitors,
diltiazem,
erythromycin,
fenofibrates,
fluconazole,
gemfibrozil,
grapefruit juice,
niacin, protease
inhibitors, quinine,
red yeast rice,
sildenafil, verapamil
Drugs that may
decrease
Atorvastatin:
antacids, bile-acid
sequestrants,
CYP3A4 Inducers,
fosphenytoin,
phenytoin, St. Johns
Wort
(Lexicomp, 2014)
Pharmacodynamics: Drug Interactions:
Increases HDL, and Avoid concomitant
decreases total
use with fusidic acid,
LDL, VLDL,
gemfibrozil,
cholesterols, and
pimozide, red yeast
plasma triglycerides rice
by inhibiting HMG- May increase levels
CoA reductase,
of: aripiprazole,
which is responsible bosentan, carvedilol,
for cholesterol
CYP2C9 substrates,
biosynthesis
daptomycin,
Pharmacokinetics:
dofetilide,
Onset of Action:
lomitapide,
maximal LDL
razopanib, pimozide,
reductions achieved trabectedin, vitamin
within 4 weeks
K antagonists
Absorption:
Fluvastatin may be
Bioavailability
increased by:
54
elevations of serum
transaminases;
pregnancy; breastfeeding
(Lexicomp, 2014)
Patient Education:
Avoid excessive
alcohol intake.
May be taken
without regard to
meals. Do not
break, crush, or
chew extendedrelease tablets; do
not open capsules.
Teach importance
of proper diet and
exercise.
Monitor: baseline
fasting lipid panel,
with repeat 4-12
Fluvastatin
Sodium
20mg (30):
$113.40
40mg (30):
$113.40
Lescol
20mg (30):
$152.02
40mg (30):
$152.02
Lescol XL
80mg (30):
$194.69
(Lexicomp,
PERSONAL DRUGS
Lovastatin
(Altoprev,
Mevacor)
(Lexicomp,
2014)
55
24%-29%
Distribution: Vd:
0.35 L/kg
Protein Binding:
98%
Metabolism:
oxidative
metabolism via
CYP2C9, 2C8, and
3A4. First-pass
hepatic extraction
Half-life
Elimination: 3
hours, 9 hours with
extended release
Time to serum peak
concentration: 1
hour, 9 hours with
extended release
Excretion:
primarily feces;
urine
(Lexicomp, 2014)
amiodarone,
bezafibrate,
boceprevire,
colchicines,
cyclosporine,
cyproterone,
fenofibrates,
fluconazole,
gemfibrozil, niacin,
red yeast rice,
telaprevir
Drugs that may
decrease
Fluvastatin:
antacids,
cholestyramine resin,
fosphenytoin,
phenytoin, rifamycin
derivatives
(Lexicomp, 2014)
Pharmacodynamics:
Completely inhibits
HMG-CoA
reductase, the
ezyme that catalyzes
the rate-limiting
step in cholesterol
biosynthesis
Pharmacokinetics:
Onset of Action:
LDL cholesterol
reduction within 3
days
Absorption: 30%,
increased with
extended release
tablets when taken
in the fasting state.
Increased
bioavailability
Drug Interactions:
See above meds for
concomitant use
May increase levels
of: daptomycin,
diltiazem, dofetilide,
pazopanib,
pimozide,
trabectedin, vitamin
K antagonists
Lovastatin may be
increased by:
amiodarone,
azithromycin,
clarithromycin,
colchicine,
cyclosporine,
CYP3A4 inhibitors,
diltiazem,
erythromycin,
weeks after
initiation or dose
adjustment, and
every 3-12 months
thereafter.
Baseline hepatic
function, with
repeat if symptoms
suggest
hepatotoxicity.
Measure CPK with
symptoms
suggestive of
myopathy
Contraindications:
Hypersensitivity to
fluvastatin; active
liver disease;
unexplained
persistent
elevations of serum
transaminases;
pregnancy; breastfeeding
(Lexicomp, 2014)
Patient Education:
Avoid excessive
alcohol
consumption. Do
not take with
grapefruit juice.
Avoid St. Johns
Wort. Administer
immediate release
with the evening
meal. Administer
extended release at
bedtime; do not
crush or chew.
Teach importance
of proper diet and
exercise.
Monitor: baseline
fasting lipid panel,
2014)
Altoprev,
24hr
20mg,
40mg,
60mg (30):
$555.98
(each)
Lovastatin
10mg (60):
$80.73
20mg (60):
$142.37
40mg (60):
$256.28
Mevacor
20mg (60):
$188.93
40mg (60):
PERSONAL DRUGS
Protein Binding:
95%
Metabolism:
hepatic. Extensive
first-pass effect
Half-life
Elimination: 1-1.7
hours
Time to serum peak
concentration: 2-4
hours immediate
release; 12-14 hours
extended release
Excretion: feces;
urine
(Lexicomp, 2014)
Pitavastatin
(Livalo)
(Lexicomp,
2014)
Pharmacodynamics:
Increase in
expression of LDL
receptors on
hepatocyte
membranes and
stimulation of LDL
catabolism by
inhibiting HMGCoA reductase.
Pharmacokinetics:
Absorption:
bioavailability 51%
Distribution: Vd:
148 L
Protein Binding:
56
fenofibrates,
fluconazole,
gemfibrozil,
grapefruit juice,
niacin, protease
inhibitors,
raltegravir, quinine,
ranolazine, red yeast
rice, sildenafil,
telaprevir, verapamil
Drugs that may
decrease Lovastatin:
CYP3A4 inducers,
dabrafenib,
deferasirox,
efavirenz, etravirine,
fosphenytoin,
phenytoin, St. Johns
Wort
(Lexicomp, 2014)
Drug Interactions:
Avoid concomitant
use with
cyclosporine, fusidic
acid, gemfibrozil,
red yeast rice
May increase levels
of: daptomycin,
pazopanib,
trabectedin, vitamin
K antagonists
Pitavastatin may be
increased by:
atazanavir,
bezafibrate,
clarithromycin,
with repeat 4-12
weeks after
initiation or dose
adjustment, and
every 3-12 months
thereafter.
Baseline hepatic
function, with
repeat if symptoms
suggest
hepatotoxicity.
Measure CPK with
symptoms
suggestive of
myopathy
Contraindications:
Hypersensitivity to
lovastatin; active
liver disease;
unexplained
persistent
elevations of serum
transaminases;
concomitant use of
strong CYP3A4
inhibitors;
pregnancy; breastfeeding
(Lexicomp, 2014)
Patient Education:
Avoid excessive
alcohol
consumption. May
be administered
with or without
food, without
regard to time of
day. Teach
importance of
proper diet and
exercise.
Monitor: baseline
fasting lipid panel,
with repeat 4-12
$340.12
(Lexicomp,
2014)
Livalo
1mg, 2mg,
4mg (90):
$540.00
(each)
(Lexicomp,
2014)
PERSONAL DRUGS
99%
Metabolism:
hepatic. Minimal
CYP2C9 and
CYP2C8
metabolism
Half-life
Elimination: 12
hours
Time to serum peak
concentration: 1
hour
Excretion: feces;
urine
(Lexicomp, 2014)
Pravastatin
(Pravachol)
(Lexicomp,
2014)
57
colchicines,
cyclosporine,
danazol,
erythromycin,
fenofibrates, fusidic
acid, gemfibrozil,
niacin, red yeast rice,
rifamycin, sildenafil,
simeprevir,
telaprevir
Drugs that may
decrease
Pitavastatin:
antacids, bosentan
(Lexicomp, 2014)
weeks after
initiation or dose
adjustment, and
every 3-12 months
thereafter.
Baseline hepatic
function, with
repeat if symptoms
suggest
hepatotoxicity.
Measure CPK with
symptoms
suggestive of
myopathy
Contraindicatioins:
Hypersensitivity to
pitavastatin; active
liver disease;
concurrent use with
cyclosporine;
pregnancy; breastfeeding
(Lexicomp, 2014)
Pharmacodynamics: Drug Interactions:
Patient Education:
Inhibits HMG-CoA Avoid concomitant
Avoid excessive
reductase, the rateuse with fusidic acid, alcohol use. Avoid
limiting enzyme
gemfibrozil,
St. Johns Wort.
involved in
pimozide, red yeast
May take without
cholesterol
rice
regard to meal or
synthesis resulting
May increase levels
time of day. Teach
in decreased LDL
of: ariprazole,
importance of
and increased HDL cyclosporine,
proper diet and
Pharmacokinetics:
daptomycin,
exercise.
Onset of Action:
dofetilide,
several days. Peak
lomitapide,
Monitor: baseline
effect 4 weeks
parozetine,
fasting lipid panel,
Absorption: rapidly pazopanib,
with repeat 4-12
absorbed.
pimozide,
weeks after
Bioavailability 17% trabectedin, vitamin initiation or dose
Protein Binding:
K antagonists
adjustment, and
50%
Pravastatin may be
every 3-12 months
Metabolism:
increased by:
thereafter.
Hepatic
bezafibrate,
Baseline hepatic
Half-life
boceprevire,
function, with
Elimination: 77
clarithromycin,
repeat if symptoms
Pravachol
20mg (90):
$392.80
40mg (90):
$576.41
80mg (90):
$576.41
Pravastatin
Sodium
10mg (90):
$289.36
20mg (90):
$294.04
40mg (90):
$431.50
80mg (90):
$431.50
(Lexicomp,
2014)
PERSONAL DRUGS
hours
Time to serum peak
concentration: 11.5 hours
Excretion: feces,
urine
(Lexicomp, 2014)
Rosuvastatin Pharmacodynamics:
(Crestor)
Inhibits the enzyme
that catalyzes the
(Lexicomp,
rate-limiting step in
2014)
cholesterol
synthesis.
Reduction in hepatic
cholesterol results in
increased
expression of LDL
receptors, which
increases uptake and
clearance of LDL
from the blood.
Pharmacokinetics:
Onset of Action:
within 1 week.
Maximal effect at 4
weeks
Absorption: 20%
bioavailability.
Distribution: Vd:
134 L
58
colchicine,
cyclosporine,
daranavir,
erythromycin,
fenofibrates, fusidic
acid, gemfibrozil,
itraconazole, niacin,
P-glycoprotein/
ABCB1 inhibitors,
raltegravir, red yeast
rice, simeprevir,
telaprevir
Drugs that may
decrease
Pravastatin:
antacids, bile-acid
sequestrants,
efavirenz,
fosphenytoin,
nelfinavir,
phenytoin,
rifamycin, saquinavir
(Lexicomp, 2014)
Drug Interactions:
Avoid concomitant
use with fusidic acid,
gemfibrozil, red
yeast rice
May increase levels
of: daptomycin,
pazopanib,
trabectedin, vitamin
K antagonists
Rosuvastatin may be
increased by:
amiodarone,
bezafibrate,
colchicine,
cyclosporine,
dronedarone,
fenofibrates, fusidic
acid, gemfibrozil,
itraconazole, niacin,
protease inhibitors,
raltegravir, red yeast
rice, simeprevir,
suggest
hepatotoxicity.
Measure CPK with
symptoms
suggestive of
myopathy
Contraindications:
Hypersensitivity to
pravastatin; active
liver disease;
pregnancy; breastfeeding
(Lexicomp, 2014)
Patient Education:
Avoid excessive
alcohol use. May
be taken with or
without food, at
any time of the
day. Teach
importance of
proper diet and
exercise.
Monitor: baseline
fasting lipid panel,
with repeat 4-12
weeks after
initiation or dose
adjustment, and
every 3-12 months
thereafter.
Baseline hepatic
function, with
repeat if symptoms
suggest
Crestor
5mg, 10mg,
20mg (90):
$616.80
(each)
40mg (30):
$205.61
(Lexicomp,
2014)
PERSONAL DRUGS
Simvastatin
(Zocor)
(Lexicomp,
2014)
Protein Binding:
88%
Metabolism:
hepatic via
CYP2C9. High first
pass extraction by
the liver
Half-life
Elimination: 19
hours
Time to serum peak
concentration: 3-5
hours
Excretion: feces
(Lexicomp, 2014)
Pharmacodynamics:
Inhibits HMG-CoA
reductase, the ratelimiting enzyme
involved in
cholesterol
synthesis resulting
in decreased LDL
and increased HDL
Pharmacokinetics:
Onset of Action: 3
days. Peak effect
within 2 weeks
Absorption: 85%;
less than 5%
bioavailability
Protein Binding:
95%
Metabolism:
Hepatic via
CYP3A4.
Extensive first-pass
effect
Half-life
Elimination:
unknown
Time to serum peak
concentration: 1.32.4 hours
Excretion: feces,
urine
59
telaprevir
Drugs that may
decrease
Rosuvastatin:
antacids,
eslicarbazepine
(Lexicomp, 2014)
Drug Interactions:
Avoid concomitant
use with boceprevir,
clarithromycin,
cyclosporine,
CYP3A4 inhibitors,
erythromycin,
fusidic acid,
gemfibrozil,
mifepristone,
protease inhibitors,
red yeast rice,
telaprevir,
telithromycin
May increase levels
of: aripiprazole,
daptomycin,
diltiazem,
pazopanib,
trabectedin, vitamin
K antagonists
Simvastatin may be
increased by:
amiodarone,
amlodipine,
azithromycin,
bezafibrate,
boceprevir,
clarithromycin,
colchicine,
cyclosporine,
hepatotoxicity.
Measure CPK with
symptoms
suggestive of
myopathy.
Contraindications:
Known
hypersensitivity to
rosuvastatin; active
liver disease;
pregnancy; breastfeeding
(Lexicomp, 2014)
Patient Education:
Avoid excessive
alcohol
consumption.
Avoid St. Johns
Wort. Do not take
with grapefruit
juice. May be
administered
without regard to
meals. Take in the
evening for
maximum effect.
Teach the
importance of
proper diet and
exercise
Monitor: baseline
fasting lipid panel,
with repeat 4-12
weeks after
initiation or dose
adjustment, and
every 3-12 months
thereafter.
Baseline hepatic
function, with
repeat if symptoms
suggest
hepatotoxicity.
Simvastatin
5mg (90):
$189.37
10mg (90):
$253.39
20mg,
40mg,
80mg (90):
$442.11
(each)
Zocor
5mg (30):
$95.87
10mg (30):
$128.47
20mg,
40mg,
80mg (30):
$224.18
(each)
(Lexicomp,
2014)
PERSONAL DRUGS
(Lexicomp, 2014)
60
CYP3A4 inhibitors,
cyproterone,
danazol, dasatinib,
diltiazem,
dronedarone,
erythromycin,
fenofibrates,
fluconazole, fusidic
acid, gemfibrozil,
grapefruit juice,
green tea, imatinib,
ivacaftor, limitapide,
luliconazole, niacin,
protease inhibitors,
quinine, raltegravir,
ranolazine, red yeast
rice, sildenafil,
simeprevir,
telaprevir, ticagrelor,
verapamil
Drugs that may
decrease
Simvastatin:
antacids, bosentan,
CYP3A4 inducers,
dabrafenib,
efavirenz, etravirine,
fosphenytoin,
mitotane, phenytoin,
rifamycin, St. Johns
Wort, tocilizumab
(Lexicomp, 2014)
Measure CPK with
symptoms
suggestive of
myopathy
Contraindications:
Hypersensitivity to
simvastatin; active
liver disease;
concomitant use of
strong CYP3A4
inhibitors
(clarithromycin,
erythromycin,
itraconazole,
ketoconazole,
nefazodone,
posaconazole,
voriconazole,
protease inhibitors,
telithromycin),
cyclosporine,
danazol,
gemfibrozil;
pregnancy; breastfeeding
(Lexicomp, 2014)
V. Drug of Choice: Pravastatin
Studies have shown atorvastatin as the drug of choice for the patient who has suffered
MI, and recent studies have demonstrated a reduction in recurrent cardiovascular events and
mortality (Blaha, Ketlogetswe, Nudmele, Gluckman, & Blumenthal, 2011). Patients with HIV
being maintained on ART are at an increased risk of drug interactions secondary to the CYP
system, therefore the majority of statin drugs should not be used in this population. Pravastatin
PERSONAL DRUGS
61
is the drug of choice in this population due to the minimal metabolism via CYP system, resulting
in less drug interactions with ART therapy (Hemkens & Bucher, 2013). Alternative lipidlowering agents such as fibrates, niacin, and fish-oil have been shown to reduce triglycerides
related to ART, however, these drugs cannot be recommended due to evidence-based outcomes
on non-HIV individuals (Hemkens & Bucher, 2013).
The ACC/AHA guidelines recommend moderate-intensity statin therapy for this patient
since he is not a candidate for the recommended high-intensity therapy, with the initial dosing at
40mg daily (Stone et al., 2013). Baseline fasting lipid panel and hepatic panel should be
performed prior to initiation of therapy, and a fasting lipid panel should be performed every 4-12
weeks to evaluate the efficacy of the dose, patient adherence, and monitor for adverse effects
(Stone et al., 2013), therefore instruct the patient on scheduling a follow-up appointment for 2-4
weeks after discharge. Discharge teaching should include non-pharmacologic measures such as
eating a heart healthy diet, increasing physical activity, smoking cessation, and weight reduction
to assist with achieving appropriate LDL-C and TG levels (Stone et al., 2013). The patient must
also be informed to notify the provider of any adverse effects such as unusual muscle cramping
or stiffness, fatigue, jaundice, or other signs of significant reaction such as wheezing, chest
tightness, cough, or swelling of the face (Lexicomp, 2014). The APN with a valid CTP has the
authority to prescribe HMG-CoA reductase inhibitors in the state of Ohio (Ohio Board of
Nursing, 2014).
PERSONAL DRUGS
62
References
Brashers, V. (2010). Chapter 30. Alterations of Cardiovascular Function. In McCance, K.,
Huether, S., Brashers, V., & Rote, N. (Eds), Pathophysiology: The Biologic Basics for
Disease in Adults and Children, 6e. (1142-1208). Maryland Heights, MO: Mosby
Elsevier
Brashers, V. (2010). Chapter 33. Alterations in Pulmonary Function. In McCance, K.,
Huether, S., Brashers, V., & Rote, N. (Eds), Pathophysiology: The Biologic Basics for
Disease in Adults and Children, 6e. (1266-1309). Maryland Heights, MO: Mosby
Elsevier
Blaha, M., Ketlogetswe, K., Ndumele, C., Gluckman, T., Blumenthal, R. (2011). Chapter 51.
Preventive Strategies for Coronary Heart Disease. In Fuster V, Walsh, R., Harrington, R.
(Eds), Hurst's The Heart, 13e. Retrieved April 03, 2014 from
http://accessmedicine.mhmedical.com.ezproxy.libraries.wright.edu:2048/content.aspx?bo
okid=376&Sectionid=40279782
Dalal, K., Felix, E., & Cardenas, D. (2013). Pregabalin for the management of neuropathic pain
in spinal cord injury. Pain Management, 3(5), 359-367.
Finnerup, N., & Baastrup, C. (2012). Spinal cord injury pain: Mechanisms and management.
Current Pain and Headache Reports, 16, 207-216.
Flack, J., Sica, D., Bakris, G., Brown, A., Ferdinand, K., Nesbitt, S., …Jamerson, K. (2010).
Management of high blood pressure in blacks: An update of the International Society in
PERSONAL DRUGS
63
Hypertension in blacks consensus statement. Hypertension, 56, 780-800.
doi: 10.1161/HYPERTENSIONAHA.110.152892
Hemkens, L., & Bucher, H. (2013). HIV infection and cardiovascular disease. European Heart
Journal, 1-11. doi: 10.1093/eurheartj/eht528
Lee, J., Kim, S., Kim, J., Ryu, J., & Chang, J. (2012). High-dose levofloxacin in communityacquired pneumonia: A randomized, open-label study. Clinical Drug Investigation,
32(9), 569-576.
Lexicomp, Inc. (2014). Lexi-Drugs. Retrieved from http://webstore.lexi.com/PDA-Softwarefor- Nurses
Mandell, L., Wunderink, R., Anzueto, A., Bartlett, J., Campbell, D., Dean, N., …Whitney, C.
(2007). Infectious Diseases Society of America/American Thoracic Society consensus
guidelines on the management of community-acquired pneumonia in adults. Clinical
Infectious Diseases, 44(2), S27-S72. doi: 10.1086/5111159
Ohio Board of Nursing (2014). The formulary developed by the Committee on Prescriptive
Governance. Retrieved from http://www.nursing .ohio.gov/practice/jan-62014_Formulary.pdf
Stone, N., Robinson, J., Lichtenstein, A., Bairey Merz, C., Lloyd-Jones, D., Blum, C., …Wilson,
P. (2013). ACC/AHA Guideline on the Treatment of Blood Cholesterol to Reduce
Atherosclerotic Cardiovascular Risk in Adults, Journal of the American College of
Cardiology (2013), doi: 10.1016/j.jacc.2013.11.002.
PERSONAL DRUGS
64
The Medical Letter (2013). Treatment guidelines: Drugs for bacterial infection. The Medical
Letter, 131, 65-78. Retrieved from www.medicalletter.org
The Medical Letter (2012). Treatment guidelines: Drugs for hypertension. The Medical Letter,
113, 1-9. Retrieved from www.medicalletter.org
The Medical Letter (2014). Treatment guidelines: Drugs for lipids. The Medical Letter, 137, 16. Retrieved from www.medicalletter.org
The Medical Letter (2013). Treatment guidelines: Drugs for pain. The Medical Letter, 128,
31-38. Retrieved from www.medicalletter.org
Weber, M., Schiffrin, E., White, W., Mann, S., Lindholm, L., Kenerson, J., …Harrap, S. (2013).
Clinical practice guidelines for the management of hypertension in the community: A
statement by the American Society of Hypertension and the International Society of
Hypertension. The Journal of Clinical Hypertension, 1-13. doi: 10.1111/jch.12237