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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