Drugs that affect the Cardiovascular System

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Drugs that affect the Cardiovascular System
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Classification of Ischemic Heart Disease
Ischemic Heart Disease
Chronic coronary artery disease (stable angina)

• Acute coronary syndromes

-Unstable Angina -Myocardial infarction
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1) Drugs that Affect Blood Coagulation

• Used in the prevention and management of
  thrombotic and thromboembolic disorders

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Intrinsic System
Factor affected by oral anticoagulatants (Vitamin
K-dependent clotting factor)
XII
XIIa
Factor affected by heparin (factor that can be
inactivated by antithrombin)
XI
XIa
Extrinsic System (thromboplastin)
IX
VII
IXa
VIIa
Xa
X
X
THROMBIN
PROTHROMBIN
FIBRINOGEN
FIBRIN (monomer)
FIBRIN (polymer)
THE COAGULATION CASCADE
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1) Drugs that Affect Blood Coagulation (Contd)

• (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

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1) Drugs that Affect Blood Coagulation (Contd)

• 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

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1) Drugs that Affect Blood Coagulation (Contd)

• 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

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1) Drugs that Affect Blood Coagulation (Contd)

• 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

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1) Drugs that Affect Blood Coagulation (Contd)

• (ii) Antiplatelet drugs
• Suppress platelet aggregation
• Indicated for prevention of thrombosis in
  arteries

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11) Drugs that Affect Blood Coagulation (Contd)

• 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.

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11) Drugs that Affect Blood Coagulation (Contd)

• Clopidogrel (Plavix)
• Dose
• 75 mg po daily with or without food
• Adverse effects
• Hemorrhage (GI Intracranial)
• GI side effects

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1) Drugs that Affect Blood Coagulation (Contd)

• Aspirin
• Suppress platelet aggregation by causing
  irreversible inhibition of cyclooxygenase, an
  enzyme required by platelets to synthesize
  thromboxane A2 (TXA2)

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1) Drugs that Affect Blood Coagulation (Contd)

• 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

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1) Drugs that Affect Blood Coagulation (Contd)

• (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

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1) Drugs that Affect Blood Coagulation (Contd)

• 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

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1) Drugs that Affect Blood Coagulation (Contd)

• 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

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2) Cardiotonics otherInotropic 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

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2) Cardiotonics otherInotropic Drugs (Contd)

• 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 contractility

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2) Cardiotonics otherInotropic Drugs (Contd)

• 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

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2) Cardiotonics otherInotropic Drugs (Contd)

• 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

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2) Cardiotonics other Inotropic Drugs (Contd)

• Side effects
• Arrhythmias, headache, hypotension
• Dosage
• Maximum dose 1.13mg/kg daily

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2) Cardiotonics other Inotropic Drugs (Contd)

• 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

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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

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3) Antihypertensive Drugs (Contd)

• 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

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3) Antihypertensive Drugs (Contd)

• 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

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3) Antihypertensive Drugs (Contd)

• 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

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3) Antihypertensive Drugs (Contd)

• Combination Products
• Thiazide related diuretics are available in
  numerous fixed-dose combination with non-diuretic
  antihypertensive agents with K-sparing
  diuretics. This can increase patient compliance
  prevent K imbalances
• Dyazide (Hydrochlorothiazide 25mgTriamterene
  50mg)
• Moduretic (Hydrochlorothiazide 50mgAmiloride
  5mg)
• Hyzaar (Losartan 50mgHydrochlorothiazide 12.5mg)

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3) Antihypertensive Drugs (Contd)
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/Hyper-kalemia Monitor serum potassium level (within 3.5- 5 mEq) Avoid K depletion due to thiazide loop diuretics or avoid K accumulation in patient taking K-sparing diuretics
Electrolytes imbalance Monitor K, Na, Cl, Mg bicarbonate levels Avoid electrolyte imbalance
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3) Antihypertensive Drugs (Contd)

• (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

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3) Antihypertensive Drugs (Contd)

• Used in
• Hypertension
• Angina pectoris
• Arrhythmias
• Myocardial Infarction
• Heart Failure

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3) Antihypertensive Drugs (Contd)

• Differ in
• Receptor selectivity
• Intrinsic sympathomimetic activity (partial
  agonist
• activity), e.g. Oxprenolol. Pindolol, acebutolol
• Lipid solubility
• (Atenolol, nadolol, Sotalol are the most
  water-soluble)
• Duration of action, e.g. Esmolol

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3) Antihypertensive Drugs (Contd)
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
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3) Antihypertensive Drugs (Contd)

• Receptor Subtype Tissue Effects
• Alpha 1,2 Vascular smooth Contraction
• muscle
• Beta 1 Heart Inc. Heart Rate
• Inc. Force of Contraction
• Beta 2 Smooth muscle Relaxation

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3) Antihypertensive Drugs (Contd)

• Adverse Effects
• Bradycardia
• Hypotension
• Brochospasms
• GI disturbances
• Heart failure
• Fatigue

• Nursing Alert
• Check blood pressure pulse frequently,
  especially when dosage is being increased

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3) Antihypertensive Drugs (Contd)

• (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

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3) Antihypertensive Drugs (Contd)
Classification Sites of action Dosage Indications Indications Indications Indications
Hypertension Angina Arrhythmias Others
Dihydropyridine Dihydropyridine Dihydropyridine
Amlodipine Arterioles 5-10 mg daily po Y 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 Y
Nimodipine Arterioles 60 mg q4h for 21 days IND
Key Y-Yes IND-Ischaemic neurological deficits
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3) Antihypertensive Drugs (Contd)
Classification Sites of action Normal dosage Indications Indications Indications
Hypertension Angina Arrhythmias
Phenylakylamines Phenylakylamines Phenylakylamines
Verapamil Arterioles/heart 40-480 mg daily in 2-3 divided dose, depending on indications Y Y Y
Benzothiazepines Benzothiazepines Benzothiazepines
Diltiazem Arterioles/heart 30 mg tid 90 mg bd (SR) 100-200mg daily (SR) Y Y Y
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3) Antihypertensive Drugs (Contd)

• Side effects
• Hypotension, dizziness, weakness, peripheral
  edema, headache, heart failure, pulmonary edema,
  nausea, constipation
• Bradycardia (Verpamil, Diltiazem)
• Tachycardia (Nifedipdine other dihydropyridines)

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3) Antihypertensive Drugs (Contd)

• Nursing Alerts
• The older may have a greater hypotensive effect
  after taking CCBs 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

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3) Antihypertensive Drugs (Contd)

• (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

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A-II is the major stimulator of aldosterone
secretion
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3) Antihypertensive Drugs (Contd)

• (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

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3) Antihypertensive Drugs (Contd)

• 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

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3) Antihypertensive Drugs (Contd)

• 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

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3) Antihypertensive Drugs (Contd)

• Side-effects
• Hypotension
• Less likely to cause cough and hyperkalaemia
  than ACE inhibitors

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3) Antihypertensive Drugs (Contd)

• 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
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3) Antihypertensive Drugs (Contd)

• Nursing Alerts (contd)

Potential Adverse Effects Nursing Actions
ACE inhibitors may cause hyperkalaemia Avoid potassium supplements, potassium containing salt substitutes and potassium-sparing diuretics
ACE inhibitors and Angiotensin II receptor antagonists are contra-indicated in pregnancy Avoid these dugs in pregnancy
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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

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4) Antianginal Drugs(Contd)

• Relieves anginal pain by relaxing smooth muscles
  in the blood vessels (vasodilation) by several
  mechanisms
• Dilate veins
• Dilate coronary arteries
• Dilate arterioles

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4) Antianginal Drugs (Contd)

• 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

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4) Antianginal Drugs (Contd)

• Nitrate preparations and dosage

Drug and dosage form Route Dosage
Glyceryl Trinitrate Glyceryl Trinitrate 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
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4) Antianginal Drugs (Contd)
Drug and dosage form Route Dosage
Glyceryl Trinitrate (Contd) Glyceryl Trinitrate (Contd) Glyceryl Trinitrate (Contd)
Transdermal patches 5mg / 10mg Transdermal 1 patch every 24 hours
Isosorbide Mononitrate Isosorbide Mononitrate 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 morning
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4) Antianginal Drugs (Contd)
Drug and dosage form Route Dosage
Isosorbide Dinitrate Isosorbide Dinitrate 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
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4) Antianginal Drugs (Contd)

• 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

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4) Antianginal Drugs (Contd)

• Adverse Effects
• Headache
• Orthostatic hypotension
• Symptoms include light headedness and dizziness
• Reflex tachycardia

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4) Antianginal Drugs (Contd)

• 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 long-acting preparations, they should be used on an intermittent schedule to allow at least 8 drug-free hours
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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

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5) Antiarrhythmic Drugs (Contd)

• (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 max1g daily

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5) Antiarrhythmic Drugs (Contd)

• I-B
• Lidocaine
• 50- 100 mg single bolus injection followed by
  1-4 mg/min infusion
• I-C
• Flecainide
• 100 mg bd po max 400 mg daily
• Propafenone
• 150-300 mg tid po

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5) Antiarrhythmic Drugs (Contd)

• Side effects of Class I
• Nausea, vomiting
• Dizziness
• Visual disturbances
• Pro-arrhythmic effect
• Heart block

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5) Antiarrhythmic Drugs (Contd)

• (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

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5) Antiarrhythmic Drugs (Contd)

• Side effects of Class II
• Nausea
• Headache
• Hypotension
• Dizziness

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5) Antiarrhythmic Drugs (Contd)

• (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

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5) Antiarrhythmic Drugs (Contd)

• 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)

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5) Antiarrhythmic Drugs (Contd)

• 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

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5) Antiarrhythmic Drugs (Contd)

• 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

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5) Antiarrhythmic Drugs (Contd)

• 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

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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

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6) Drugs used for Dyslipidemia (Contd)

• (i) HMG CoA reductase inhibitors (Statins)
• Inhibits HMG CoA reductase, the rate-limiting
  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

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6) Drugs used for Dyslipidemia (Contd)
Drug Usual Dosage Comments
Atorvastatin 10-80mg taken at anytime Take with or without food
Fluvastatin 20-40mg daily in the evening, up to 40mg twice daily Take with or without food
Pravastatin 10-40mg at night Take with food to reduce dyspepsia
Simvastatin 5-80mg at night Take with food to reduce dyspepsia
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6) Drugs used for Dyslipidemia (Contd)

• Adverse Effects
• Headache, GI side effects (e.g. abdominal pain,
  flatulence, diarrhoea, nausea and
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  
  vomiting)
• Hepatoxicity
• Myopathy

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6) Drugs used for Dyslipidemia (Contd)

• (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)

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6) Drugs used for Dyslipidemia (Contd)
Drug and dosage form Usual Dosage
Clofibrate Clofibrate
capsule 500mg 2g daily in 2-4 divided doses
Fenofibrate Fenofibrate
Capsule 100mg 3 capsules daily in the course of main meals
Capsule (Micronized fenofibrate) 200mg 1 capsule daily
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6) Drugs used for Dyslipidemia (Contd)
Drug and dosage form Usual Dosage
Gemfibrozil Gemfibrozil
Capsule 300mg 1.2g daily in 2 divided doses Usual range 0.9-1.5g daily
Tablet 600mg 1.2g daily in 2 divided doses Usual range 0.9-1.5g daily
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6) Drugs used for Dyslipidemia (Contd)

• Adverse Effects
• Nausea, vomiting and GI upset
• Cholelithiasis (stones in the gall bladder) and
  cholecystitis (inflammation of the gallbladder)
• Myopathy

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6) Drugs used for Dyslipidemia (Contd)

• (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

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6) Drugs used for Dyslipidemia (Contd)

• 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

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6) Drugs used for Dyslipidemia (Contd)

• (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

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6) Drugs used for Dyslipidemia (Contd)

• Normal dose
• 1-2g three times daily
• Adverse effects
• Flushing, itching, nausea, vomiting, diarrhoea
• Hepatotoxic
• Hyperglycaemia and hyperuricaemia

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6) Drugs used for Dyslipidemia (Contd)

• Nursing alerts

Potential Adverse Effects Nursing Actions
Statins 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
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6) Drugs used for Dyslipidemia (Contd)
Potential Adverse Effects Nursing Actions
Fibrates 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
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6) Drugs used for Dyslipidemia (Contd)
Potential Adverse Effects Nursing Actions
Bile acid sequestrants 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
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6) Drugs used for Dyslipidemia (Contd)
Potential Adverse Effects Nursing Actions
Nicotinic acid 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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