Download 3) Antihypertensive Drugs (Cont`d)

1
2
Classification of
Ischemic Heart Disease
Ischemic Heart Disease
Chronic coronary
artery disease
(stable angina)
Acute coronary
syndromes
-Unstable Angina
-Myocardial infarction
3
1) Drugs that Affect Blood Coagulation

Used in the prevention and management
of thrombotic and thromboembolic
disorders
4
Intrinsic System
XII
=Factor affected by oral anticoagulatants
(Vitamin K-dependent clotting factor)
XIIa
XI
=Factor affected by heparin
(factor that can be inactivated by antithrombin)
Extrinsic System (thromboplastin)
XIa
IX
VIIa
IXa
X
Xa
PROTHROMBIN
X
THROMBIN
FIBRINOGEN
THE COAGULATION CASCADE
VII
FIBRIN (monomer)
FIBRIN (polymer)
5
1) Drugs that Affect Blood Coagulation (Cont’d)

(i) Anticoagulant drugs
– Drugs that disrupt the coagulation cascade, &
thereby suppress production of fibrin
– Prevention of thrombosis in veins
– Heparin


Suppresses coagulation by helping antithrombin III
inactivate thrombin, factor Xa and other clotting factors
Used in:
– Prevention and treatment of pulmonary embolism, stroke,
deep vein thrombosis (DVT)
– Prevent coagulation in devices in open heart surgery and
renal dialysis
– Treatment of disseminated intravascular coagulation
– Adjunct to thrombolytic therapy of acute myocardial
infarction
6
1) Drugs that Affect Blood Coagulation (Cont’d)

Dosage
– Based on body weights of the patients & their
indications

Adverse effects
– Hemorrhage
– Thrombocytopenia
 Decrease platelet count
– Hypersensitivity reactions
 Since commercial heparin is extracted from
animal tissue
7
1) Drugs that Affect Blood Coagulation (Cont’d)
– Warfarin
 Suppress coagulation by acting as an
antagonist of vitamin K
 4 clotting factors (VII, IX, X & prothrombin)
require vitamin K for their synthesis
 Indications:
– Prevention of venous thrombosis & associated
pulmonary embolism
– prevention of thromboembolism in patients with
prosthetic heart valves
– Prevention of thrombosis during atrial fibrillation
– Reduce risk of recurrent transient ischemic
attacks (TIAs) & recurrent MI
8
1) Drugs that Affect Blood Coagulation (Cont’d)

Daily dose
– usually 3 to 9 mg but it should be based on the INR
values.
– INR targeted values are different in different
indications, usually within 2 to 3.5

Adverse effects:
– Hemorrhage
– Teratogenic
9
1) Drugs that Affect Blood Coagulation (Cont’d)

(ii) Antiplatelet drugs
– Suppress platelet aggregation
– Indicated for prevention of thrombosis
in arteries
10
11) Drugs that Affect Blood Coagulation (Cont’d)

Clopidogrel (Plavix)
– Adenosine diphosphate receptor (ADP) antagonist
– Irreversible blocking of ADP receptors on the
platelet surface
– Prevent ADP-stimulated aggregation
– Indicated for prevention of stroke, vascular death
& MI
– The combination of aspirin and clopidogrel appears
to be the most effective and safest therapy for
secondary prevention of stroke.
11
11) Drugs that Affect Blood Coagulation (Cont’d)

Clopidogrel (Plavix)
– Dose
 75 mg po daily with or without food
– Adverse effects:
 Hemorrhage (GI & Intracranial)
 GI side effects
12
1) Drugs that Affect Blood Coagulation (Cont’d)

Aspirin
– Suppress platelet aggregation by causing
irreversible inhibition of cyclooxygenase, an
enzyme required by platelets to synthesize
thromboxane A2 (TXA2)
13
1) Drugs that Affect Blood Coagulation (Cont’d)

Aspirin
– Indicated in :
 Primary prophylaxsis of MI
 Prevention of reinfarction patients who have
experienced an acute MI
 Prevention of stroke in patients with a history
of TIAs
– Dose
 Maintenance treatment 75-150 mg daily po
– Adverse effects
 GI hemorrhage & also other hemorrhage
 Bronchospasm
14
1) Drugs that Affect Blood Coagulation (Cont’d)

(iii) Thrombolytic drugs
– Promote lysis of fibrin, thereby cause
dissolution of thrombi

Streptokinase
– First bind to plasminogen to form an active
complex
– The streptokinase-plasminogen complex then
catalyzes the conversion of other plasminogen
molecules into plasmin, an enzyme that digests
the fibrin meshwork of clots
15
1) Drugs that Affect Blood Coagulation (Cont’d)

Alteplase (tPA)
– Also known as tissue plasminogen activator (tPA)
– Is produced commercially by recombinant DNA
technology
– Human tPA is an enzyme that promotes
conversion of plasminogen to plasmin, an enzyme
that digests the fibrin matrix of clots

Adverse effects:
– Nausea & vomiting
– Bleeding
16
1) Drugs that Affect Blood Coagulation (Cont’d)

Nursing Alerts:
– Monitor signs of hemorrhage

Lowering of blood pressure, elevation of
heart rate, discoloration of urine or stools,
bruises, petechiae, etc.
– Monitor INR, APTT, PT regularly
– Warfarin is contraindicated in
pregnancy & breast-feeding
17
2) Cardiotonics & other
Inotropic Drugs

The cardiotonics are drugs used to
increase the efficiency & improve
the contraction of the heart muscle,
which leads to improved blood flow
to all tissues of the body
18
2) Cardiotonics & other
Inotropic Drugs (Cont’d)

Digoxin
– Inhibits the enzyme Na, K-adenosine
triphosphatase (Na, K-ATPase), increases the
movement of Na out of myocardial cells after
contraction
– As a result, Ca enters the cell in exchange for
Na, causing additional Ca to be released from
intracellular binding sites
– With the increase in intracellular
concentration of free Ca ions, more Ca is
available to activate the contractile proteins,
actin & myosin, & increase myocardial
19
contractility
2) Cardiotonics & other
Inotropic Drugs (Cont’d)

Side effects:
– Usually associated with excessive dose
– Digoxin toxicity:


anorexia, nausea, vomiting, diarrhoea, visual
disturbance, confusion & mental
disturbance, arrthythmia, heart block
Dosage:
– Maintenance: 62.5-500 mcg daily
20
2) Cardiotonics & other
Inotropic Drugs (Cont’d)

Milrinone (Primacor)
– Increase levels of cyclic adenosine
monophosphate (cAMP) in myocardial cells by
inhibiting phosphodiesterase (PDE)
– Relax vascular smooth muscle to produce
vasodilation & decrease preload & afterload
– Used in short term management of acute
severe heart failure that is not controlled by
digoxin, diuretics & vasodilators
21
2) Cardiotonics & other
Inotropic Drugs (Cont’d)

Side effects:
– Arrhythmias, headache, hypotension

Dosage:
– Maximum dose: 1.13mg/kg daily
22
2) Cardiotonics & other
Inotropic Drugs (Cont’d)

Nursing Alerts:
– Withhold the drug & contact the physician if
there are any signs of digoxin toxicity or
marked changes in the pulse rate/rhythm
– Monitor digoxin levels closely: should be
smaller than 2 ng/ml
– Older adults are particularly prone to digoxin
toxicity
– Hypokalemia makes the heart muscle more
sensitive to digoxin, thereby increasing the
possibility of developing digoxin toxicity
23
3) Antihypertensive
Drugs
– (i) Diuretics
Diuretics are drugs that increase renal
excretion of water, sodium & other
electrolytes, thereby increasing urine
formation & output
 Used in the management of heart failure,
renal & hepatic disease, hypertension,
ophthalmic surgery

24
25
3) Antihypertensive Drugs (Cont’d)
– Thiazide diuretics:
Decrease reabsorption of Na, water, Cl &
bicarbonate in the distal convoluted tubule
 Hydrocholorothiazide

– 25-100 mg daily or BD po

Indapamide (Natrilix)
– 2.5 mg/1.5mg(S.R.) daily po
26
3) Antihypertensive Drugs (Cont’d)
– Loop Diuretics:
Inhibit Na & Cl reabsorption in the
ascending loop of Henle
 Frusemide

– 20-80 mg daily po

Bumetanide (Burinex)
– 0.5-2 mg daily po
27
3) Antihypertensive Drugs (Cont’d)
– Potassium-Sparing Diuretics:

Act directly on the distal tubule to
decrease the exchange of Na for K
– Amiloride : 5-20 mg daily po
– Triamterene: 100-300 mg daily in divided
dose po

Spironolactone
– Block the Na-retaining effects of aldosterone in
the distal tubule
– 25-200 mg daily po
28
3) Antihypertensive Drugs (Cont’d)
– Combination Products

Thiazide & related diuretics are available in
numerous fixed-dose combination with nondiuretic antihypertensive agents & with Ksparing diuretics. This can increase patient
compliance & prevent K imbalances:
– Dyazide (Hydrochlorothiazide 25mg+Triamterene
50mg)
– Moduretic (Hydrochlorothiazide 50mg+Amiloride 5mg)
– Hyzaar (Losartan 50mg+Hydrochlorothiazide 12.5mg)
29
3) Antihypertensive Drugs (Cont’d)
Side effects
Nursing actions
Rationale
Increase urine
output
Give in the early morning if ordered
daily
Peak action will occur during waking
hours & not interrupt with sleep
Keep a bedpan within reach. Assist to
the bathroom anyone who is elderly,
weak, dizzy, or unsteady in walking
Mainly to avoid fall
Postural
hypotension
Assist the patient to get up slowly
Avoid falling
Possibility of
dehydration
Record fluid intake & output regularly
Avoid fluid volume depletion due to
excessive diuresis
Hypo/Hyperkalemia
Monitor serum potassium level (within
3.5- 5 mEq)
Avoid K depletion due to thiazide &
loop diuretics or avoid K
accumulation in patient taking Ksparing diuretics
Electrolytes
imbalance
Monitor K, Na, Cl, Mg & bicarbonate
levels
Avoid electrolyte imbalance
30
3) Antihypertensive Drugs (Cont’d)

(ii) Beta Blockers
– Block beta-1 receptors in the heart
– Hence:
Reduce heart rate
 Reduce force of contraction
 Reduced velocity impulse conduction
through the AV node

31
3) Antihypertensive Drugs (Cont’d)
– Used in:
Hypertension
 Angina pectoris
 Arrhythmias
 Myocardial Infarction
 Heart Failure

32
3) Antihypertensive Drugs
(Cont’d)
– Differ in:




Receptor selectivity
Intrinsic sympathomimetic activity (partial agonist
activity), e.g. Oxprenolol. Pindolol, acebutolol
Lipid solubility
(Atenolol, nadolol, Sotalol are the most watersoluble)
Duration of action, e.g. Esmolol
33
3) Antihypertensive Drugs (Cont’d)
Drug
Receptors
Blocked
Maintenence Dosage in Hypertension
Atenolol
Beta1
50mg daily po
Metoprolol
Beta1
100-200mg daily in one to two doses po
200-400mg daily po (Slow release)
Carvedilol
Beta1 and 2
12.5-50mg bd po
Labetolol
Beta1 and 2
100-200mg bd po with food
Propranolol
Beta1 and 2
160-320mg daily po
34
3) Antihypertensive Drugs
(Cont’d)
Receptor Subtype
Tissue
Effects
Alpha 1,2
Vascular smooth
muscle
Contraction
Beta 1
Heart
Inc. Heart Rate
Inc. Force of
Contraction
Beta 2
Smooth muscle
Relaxation
35
3) Antihypertensive Drugs
(Cont’d)
– Adverse Effects






Bradycardia
Hypotension
Brochospasms
GI disturbances
Heart failure
Fatigue

Nursing Alert
– Check blood
pressure & pulse
frequently,
especially when
dosage is being
increased
36
3) Antihypertensive Drugs (Cont’d)

(iii) Calcium Channel Blockers (CCB)
– Drugs that prevent calcium ions from
entering cells.
– Have the greatest effect on the heart
and blood vessels.
– Widely used to treat hypertension,
angina pectoris and cardiac
dysrhythmias
37
3) Antihypertensive Drugs (Cont’d)
Classification Sites of Dosage
action
Indications
Hypertension
Angina
Y
Arrhythmias
Others
Dihydropyridine
Amlodipine
Arterioles
5-10 mg daily po
Y
Felodipine S.R.
Arterioles
2.5-10 mg daily po
Y
Nifedipine
Arterioles
10-30 mg tid po
10 mg bd po
(Adalat Retard)
30-60 mg daily po
(Adalat GITS)
Y
Nimodipine
Arterioles
60 mg q4h for 21
days
Key: Y-Yes; IND-Ischaemic neurological deficits
Y
IND
38
3) Antihypertensive Drugs (Cont’d)
Classification
Sites of
action
Normal
dosage
Indications
Arrhythmias
Hypertension
Angina
Y
Y
Y
30 mg tid;
Y
90 mg bd (SR)
100-200mg daily
(SR)
Y
Y
Phenylakylamines
Verapamil
Arterioles/
heart
40-480 mg daily
in 2-3 divided
dose, depending
on indications
Benzothiazepines
Diltiazem
Arterioles/
heart
39
3) Antihypertensive Drugs (Cont’d)
– Side effects:
Hypotension, dizziness, weakness,
peripheral edema, headache, heart failure,
pulmonary edema, nausea, constipation
 Bradycardia (Verpamil, Diltiazem)
 Tachycardia (Nifedipdine & other
dihydropyridines)

40
3) Antihypertensive Drugs (Cont’d)

Nursing Alerts:
– The older may have a greater hypotensive
effect after taking CCB’s than younger adults.
The nurse must monitor them closely during
dosage adjustments
– Make position changes slowly to minimize
hypotensive effects
– Some patients may experience dizziness and
light-headedness, especially during early
therapy. The nurse should assist the patient
with all ambulatory activities and instructs
the patients to ask for help when getting out
of bed or ambulating
41
3) Antihypertensive Drugs (Cont’d)

(iv) Drug Acting on Renin-Angiotensin
System
– There are 2 families of drugs:

Angiotensin-converting enzyme (ACE)
inhibitors
– Block the enzyme (ACE) that normally converts
angiotensin I to the potent vasoconstrictor
angiotensin II
– Decrease vasoconstriction & decrease aldosterone
production, reducing retention of Na and water
42
*A-II is the major stimulator of aldosterone secretion
43
3) Antihypertensive Drugs (Cont’d)

(iv) Drug Acting on Renin-Angiotensin
System
– There are 2 families of drugs:

Angiotensin-converting enzyme (ACE)
inhibitors
– Block the enzyme (ACE) that normally converts
angiotensin I to the potent vasoconstrictor
angiotensin II
– Decrease vasoconstriction & decrease aldosterone
production, reducing retention of Na and water
44
3) Antihypertensive Drugs (Cont’d)

Used to treat hypertension, heart failure,
myocardial infarction, and nephropathy
–
–
–
–

Enalapril 10-40mg/day in 1 or 2 doses
Lisinopril 10-40mg once daily
Perindopril 2-8mg daily
Ramipril 1.25-10mg once daily
Side Effects:
– Can produce serious first-dose hypotension
– Cough, due to accumulation of bradykinin
– Hyperkalaemia, due to inhibition of aldosterone release
45
3) Antihypertensive Drugs (Cont’d)

Angiotensin II receptor blockers (ARBs)
– Compete with angiotensin II for tissue binding
sites & prevent angiotensin II from combining with
its receptors in body tissues
– Used for hypertension, may be used as an
alternative to ACE inhibitors in the management
of heart failure and diabetic nephropathy.



Irbesartan 150-300mg once daily
Losartan 25-100mg once daily
Valsartan 80-160mg once daily
46
3) Antihypertensive Drugs
(Cont’d)

Side-effects
– Hypotension
– Less likely to cause cough and hyperkalaemia
than ACE inhibitors
47
3) Antihypertensive Drugs (Cont’d)

Nursing Alerts
Potential Adverse
Effects
Nursing Actions
ACE inhbitors and
Angiotensin II receptor
antagonists may cause first
dose hypotension
Instruct the patient to lie
down if hypotension develops
ACE inhibitors may produce
cough
Warn patients about the
possibility of cough. Consult
the doctor if the cough is
bothersome to the patient
48
3) Antihypertensive Drugs (Cont’d)

Nursing Alerts (cont’d)
Potential Adverse Effects Nursing Actions
ACE inhibitors may cause
hyperkalaemia
Avoid potassium supplements,
potassium containing salt
substitutes and potassiumsparing diuretics
ACE inhibitors and Angiotensin
II receptor antagonists are
contra-indicated in pregnancy
Avoid these dugs in pregnancy
49
4) Antianginal Drugs

Organic Nitrates
– Used to treat or prevent angina
– Mechanism:
 Nitrates
are converted to NO in vascular
smooth muscle
 NO activates guanylate cyclase
 Increase formation of cGMP so that the
intracellular calcium levels decrease
 Vasodilation
50
4) Antianginal Drugs(Cont’d)
– Relieves anginal pain by relaxing smooth
muscles in the blood vessels (vasodilation)
by several mechanisms
Dilate veins
 Dilate coronary arteries
 Dilate arterioles

51
4) Antianginal Drugs (Cont’d)
– Most widely used nitrate is nitroglycerin
(Glyceryl trinitrate)

Since it is highly lipid soluble, it can be
administered by sublingual and transdermal
route, as well as oral and intravenous routes
52
4) Antianginal Drugs (Cont’d)

Nitrate preparations and dosage
Drug and dosage
form
Route
Dosage
Glyceryl Trinitrate
Sublingual tablet
500mcg
Sublingual
1 tablet under the
tongue immediately
as required
Spray 0.4mg/dose
Sublingual
Spray 1-2 doses
under tongue
Capsule 2.5mg
(Retard)
Oral
1-2 capsules 2-3
times a day
53
4) Antianginal Drugs (Cont’d)
Drug and dosage
form
Route
Dosage
Glyceryl Trinitrate (Cont’d)
Transdermal
patches 5mg / 10mg
Transdermal
1 patch every 24
hours
Isosorbide Mononitrate
Tablet 20mg
Oral
20mg bd to tid /
40mg bd
Tablet 60mg
(controlled release)
Oral
30-120mg in the
morning
Capsule 50mg
(sustained release)
Oral
1-2 capsules in the
54
morning
4) Antianginal Drugs (Cont’d)
Drug and dosage
form
Route
Dosage
Isosorbide Dinitrate
Tablet 10mg
Oral
30-240mg in divided
doses
Tablet 40mg
(sustained release)
Oral
20-40mg every 12
hours
Capsule 20mg
(sustained release)
Oral
1 capsule bd or tid
55
4) Antianginal Drugs (Cont’d)
– Tolerance
Tolerance to nitrate induced vasodilation
can develop rapidly
 This may be due to depletion of sulfhydryl
(S-H) groups in the vascular smooth muscle.
These groups are needed to convert nitrate
to NO

56
4) Antianginal Drugs (Cont’d)
– Adverse Effects



Headache
Orthostatic hypotension
– Symptoms include light headedness and
dizziness
Reflex tachycardia
57
4) Antianginal Drugs (Cont’d)

Nursing Alerts:
Potential Adverse Effects Nursing Actions
Headache
Inform patients that headache will
diminish with continued drug use. Can
be relieved by mild analgesics
Orthostatic hypotension
Slowly change from a sitting or lying
position to an upright position. Advise
the patient to lie or sit down if
symptoms of hypotension (eg.
dizziness, lightheadedness) occur
Tolerance
To prevent tolerance, use the
minimum effective dose. For longacting preparations, they should be
used on an intermittent schedule58to
allow at least 8 drug-free hours
5) Antiarrhythmic Drugs


Antiarrhythmic drugs are primary
used to treat cardiac arrhythmias,
which is a disturbance or
irregularity in the heart rate,
rhythm, or both
Antiarrhythmic drugs are divided
into 4 classes
59
5) Antiarrhythmic Drugs (Cont’d)

(i) Class I
– Sodium channel blockers
– Have a membrance-stablizing or anaesthetic
effect on the cell of the myocardium
– Are subdivided into I-A, I-B, I-C
I-A:
 Quinidine

– 200-400 mg tid or qid po

Procainamide
– 25-50 mg/min slow iv injection; max:1g daily
60
5) Antiarrhythmic Drugs (Cont’d)
I-B:
 Lidocaine

– 50- 100 mg single bolus injection; followed by 14 mg/min infusion
I-C:
 Flecainide

– 100 mg bd po; max: 400 mg daily

Propafenone
– 150-300 mg tid po
61
5) Antiarrhythmic Drugs (Cont’d)
– Side effects of Class I:
 Nausea,
vomiting
 Dizziness
 Visual disturbances
 Pro-arrhythmic effect
 Heart block
62
5) Antiarrhythmic Drugs (Cont’d)

(II) Class II
– Beta Blockers
– Block sympathetic stimulation of beta
receptors in the heart & decrease the
heart rate

Propranolol
– 10-40 mg tid or qid po

Acebutolol
– 400-1200 mg daily po in 2 to 3 divided dose

Esmolol
– 50-200 mcg/kg/min IV infusion
63
5) Antiarrhythmic Drugs (Cont’d)
– Side effects of Class II:
 Nausea
 Headache
 Hypotension
 Dizziness
64
5) Antiarrhythmic Drugs (Cont’d)

(III) Class III
– Potassium channel blocker
– Prolong duration of action potential, slow
repolarization, and prolong the
refractory period in both atria and
ventricles

Amiodarone
– 200 mg one to three times daily po

Bretylium
– 5-10 mg/kg IV infusion over 15-30 min q6-8h
65
5) Antiarrhythmic Drugs (Cont’d)

Sotalol
– Has combined Class II & Class III effects
– A beta blocker that also delays repolarization
– 160-320 mg po daily in 2 divided dose
– Side effects of Class III:
Proarrhythmias (Amiodarone & Sotalol)
 Hypotension (Bretylium & Sotalol)
 Malaise, fatigue & tremor (Amiodarone)

66
5) Antiarrhythmic Drugs (Cont’d)

Class IV:
– Calcium Channel Blockers (CCB)
– Block the movement of Ca into conductile
& contractile myocardial cells
– Verapamil & Diltiazem are the only
approved CCB in arrhythmias

Verapamil
– 40-120 mg tid po
67
5) Antiarrhythmic Drugs (Cont’d)

Diltiazem
– 0.25 mg/kg IV injection over 2 min, second bolus of
0.35 mg/kg if needed; followed by 5-15 mg/hr
continuous IV infusion if necessary
– Side effects of Class IV:
Proarrhythmias (Verapamil)
 Heart block
 Hypotension, headache, dizziness, constipation

68
5) Antiarrhythmic Drugs (Cont’d)

Nursing Alerts
– Antiarrhythmic drugs are capable of causing new
arrhythmias, as well as an exacerbation of existing
arrhythmias
– Older adults taking antiarrhythmic drugs are at
greater risk for adverse reactions such as
development of additional arrhythmias or
aggravating of existing arrhythmias, hypotension,
and congestive heart failure. Careful monitoring is
necessary for early identification and management
of adverse effects
69
6) Drugs used for Dyslipidemia

Used in the management of elevated
blood lipids, which is a major risk factor
for atherosclerosis and vascular
disorders such as coronary artery
disease and strokes
70
6) Drugs used for Dyslipidemia (Cont’d)

(i) HMG CoA reductase inhibitors
(Statins)
– Inhibits HMG CoA reductase, the ratelimiting enzyme in cholesterol synthesis
– Increase LDL receptors in hepatocytes

This enables hepatocytes to remove more
LDLs from the blood
– Also decrease VLDL levels and increase
HDL levels
71
6) Drugs used for Dyslipidemia (Cont’d)
Drug
Usual Dosage
Atorvastatin 10-80mg taken at anytime
Comments
Take with or without
food
Fluvastatin
20-40mg daily in the evening, Take with or without
up to 40mg twice daily
food
Pravastatin
10-40mg at night
Take with food to
reduce dyspepsia
Simvastatin
5-80mg at night
Take with food to
reduce dyspepsia
72
6) Drugs used for Dyslipidemia (Cont’d)
– Adverse Effects
Headache, GI side effects (e.g. abdominal
pain, flatulence, diarrhoea, nausea and
vomiting)
 Hepatoxicity
 Myopathy

73
6) Drugs used for Dyslipidemia (Cont’d)

(ii) Fibric acid derivatives (Fibrates)
– Increase oxidation of fatty acids in
liver and muscle tissue, decrease
hepatic production of triglycerides,
decrease VLDL cholesterol and
increase HDL cholesterol
– Main indication is hypertriglceridemia
(high plasma triglycerides)
74
6) Drugs used for Dyslipidemia (Cont’d)
Drug and dosage form
Usual Dosage
Clofibrate
capsule 500mg
2g daily in 2-4 divided doses
Fenofibrate
Capsule 100mg
3 capsules daily in the course
of main meals
Capsule (Micronized
fenofibrate) 200mg
1 capsule daily
75
6) Drugs used for Dyslipidemia (Cont’d)
Drug and dosage form
Usual Dosage
Gemfibrozil
Capsule 300mg
1.2g daily in 2 divided doses
Usual range 0.9-1.5g daily
Tablet 600mg
76
6) Drugs used for Dyslipidemia (Cont’d)
– Adverse Effects
Nausea, vomiting and GI upset
 Cholelithiasis (stones in the gall bladder)
and cholecystitis (inflammation of the
gallbladder)
 Myopathy

77
6) Drugs used for Dyslipidemia (Cont’d)

(iii) Bile acid sequestrants
– Bind bile acids in the intestinal lumen.
This causes the bile acids to be
excreted in faeces and prevents them
being re-circulated to the liver
– Mainly used as an adjunct to Statins to
decrease LDL cholesterol levels
78
6) Drugs used for Dyslipidemia (Cont’d)
– Cholestyramine

Usual dosage
– 12-24g daily in water in one to four divided
doses; Max: 36g daily

Adverse effects
– Constipation, diarrhoea, nausea, vomiting,
gastro-intestinal discomfort
– Decreased absorption of fat-soluble vitamins
79
6) Drugs used for Dyslipidemia (Cont’d)

(iv) Nicotinic acid
– Inhibits mobilization of free fatty
acids from peripheral tissues, thereby
reducing hepatic synthesis of
triglycerides and secretion of VLDL,
which leads to decreased production of
of LDL cholesterol
– Besides reducing LDL and VLDL levels,
also effective in increasing HDL levels
80
6) Drugs used for Dyslipidemia (Cont’d)
– Normal dose

1-2g three times daily
– Adverse effects
Flushing, itching, nausea, vomiting,
diarrhoea
 Hepatotoxic
 Hyperglycaemia and hyperuricaemia

81
6) Drugs used for Dyslipidemia (Cont’d)

Nursing alerts:
Potential Adverse
Effects
Nursing Actions
Statins
Hepatotoxicity
Liver function should be
monitored during therapy
Myopathy
Inform patient about the risk
of myopathy. Instruct them to
notify physician if unexplained
muscle pain or tenderness
occurs
82
6) Drugs used for Dyslipidemia (Cont’d)
Potential Adverse Effects
Nursing Actions
Fibrates
Gallstones
Inform patients about symptoms of
gallbladder disease (e.g. upper
abdominal discomfort, intolerance
of fried foods, bloating) and
instruct them to notify the
physician if these develop
Myopathy
Warn patient to report any signs of
muscle injury, such as tenderness,
weakness, or unusual muscle pain
Liver Disease
Obtain periodic tests of liver
function
83
6) Drugs used for Dyslipidemia (Cont’d)
Potential Adverse
Effects
Nursing Actions
Bile acid sequestrants
Constipation
Inform patients that
constipation can be minimized by
increasing dietary fiber and
fluids. A mild laxative may be
used if needed.
Vitamin deficiency
Absorption of fat-soluble
vitamins (A, D, E, K) may be
impaired. Vitamin supplements
may be required
84
6) Drugs used for Dyslipidemia (Cont’d)
Potential Adverse Effects
Nursing Actions
Nicotinic acid
Flushing
Contact physician if the patient
experiences flushing (face, neck,
ears)
Hepatotoxicity
Monitor liver function during
treatment
Hyperglycaemia
Blood glucose should be monitored
frequently
Hyperuricaemia
Exercise caution in patients with
gout
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87