Cardiovascular Products

 

9.1 Diuretics

9.2 Anti Anginal/Coronary Vasodilators

9.3 Vasoconstrictor

9.4 Anti Arrhytmic Agents

9.5 Vascular Sclerosants

9.6 Cerebro-Vascular Agents

9.7 Antihypertensive Agents

9.8 Inotropic Agents

9.9 Hypolipidaemic Products

9.10 Haematological Products

 

9.1 Diuretics

ACETAZOLAMIDE

Dosage Form: Tablet 250 mg; Injection 500 mg/vial (II)

 

Recommended Dose: 250-375 mg ORALLY once daily in morning for 1 or 2 days, alternating with day of rest. By IM/IV injection: 250-500 mg. Drug induced oedema: 250-375 mg daily, 1 to 2 days.

 

Indications: CHF induced oedema, oedema due to adverse drug reaction

 

Contra-Indications: Arenal gland failure,cirrhosis, hyponatremia/hypokalemia, hyperchloremic acidosis, hypersensitivity to acetazolamide, severe hepatic or renal disease.

 

Special Precautions: Avoid in renal impairment, first trimester of pregnancy, chronic closed-angle glaucoma, care in acidosis, diabetes mellitus.

AMILORIDE HCL + HYDROCHLOROTHIAZIDE (MODURETIC)

Dosage Form: Tablet 5 mg + 50 mg (I)

 

Recommended Dose: Hpertension, initially ½ tablet daily, increased if necessary to max. 1 tablet daily. Congestive heart failure, initially ½ tablet daily, increased if necessary to max. 2 tablets daily. Oedema and ascites in cirrhosis of the liver, initially 1 tablet daily, increased if necessary to max. 2 tablets daily; reduce for maintenance if possible.

 

Indications: Hypertension, congestive heart failure, oedema and ascites in cirrhosis of the liver.

 

Contra-Indications: Hyperkalaemia, renal failure

 

Special Precautions: Pregnancy and breast feeding, renal impairment (avoid if moderate to severe), diabetes mellitus, elderly

CHLOROTHIAZIDE

Dosage Form: Tablet 500 mg (II)

 

Recommended Dose: Oedema, Associated with congestive heart failure, hepatic cirrhosis, renal dysfunction, corticosteroid and estrogen therapy; Adjunct: 0.5-1 g ORALLY once or twice daily, may give every other day or 3-5 days each week. Hypertension: 0.5-1 g ORALLY divided once or twice-daily.

 

Indications: Oedema, Oedema Associated with congestive heart failure, hepatic cirrhosis, renal dysfunction, corticosteroid and estrogen therapy; Adjunct, Hypertension.

 

Contra-Indications: Anuria, hypersensitivity to chlorothiazide or sulfonamides.

 

Special Precautions: Avoid lithium, diabetes mellitus, electrolyte imbalance, geriatric patients, hyperuricemia or gout, hypotension, liver disease, may aggravate digitalis toxicity, post-sympathectomy patients, renal disease, sensitivity reactions may occur with or without a history of allergy or asthma,systemic lupus erythematosus.

FRUSEMIDE

Dosage Form: Tablet 40 mg; Injection 20 mg/2 ml (II)

 

Recommended Dose: By mouth, oedema, initially 40 mg in the morning; maintenance 20–40 mg daily, increased in resistant oedema to 80 mg daily or more; child 1–3 mg/kg daily, max. 40 mg daily. Oliguria, initially 250 mg daily; if necessary larger doses, increasing in steps of 250 mg, may be given every 4–6 hours to a max. of a single dose of 2 g (rarely used). By intramuscular injection or slow intravenous injection , initially 20–50 mg; child 0.5–1.5 mg/kg to a max. daily dose of 20 mg. By intravenous infusion (by syringe pump if necessary), in oliguria, initially 250 mg over 1 hour (rate not exceeding 4 mg/minute), if satisfactory urine output not obtained in the subsequent hour further 500 mg over 2 hours, then if no satisfactory response within subsequent hour, further 1 g over 4 hours, if no response obtained dialysis probably required; effective dose (up to 1 g) can be repeated every 24 hours.

 

Indications: Oedema, oliguria due to renal failure.

 

Contra-Indications: Precomatose states associated with liver cirrhosis; renal failure with anuria.

 

Special Precautions: Hypotension; correct hypovolaemia before using in oliguria; prostatic enlargement; although manufacturer advises that rate of intravenous administration should not exceed 4 mg/minute, single doses of up to 80 mg may be administered more rapidly; hepatic impairment, renal impairment, pregnancy.

INDAPAMIDE, INDAPAMIDE SR

Dosage Form: Tablet 2.5 mg, SR 1.5 mg (II)

 

Recommended Dose: Tablet 2.5 mg: 2.5 mg in the morning. Tablet 1.5 mg (sustained-release): 1.5 mg daily

 

Indications: Essential hypertension

 

Contra-Indications: Severe hepatic impairment

 

Special Precautions: Monitor plasma potassium and urate concentrations in elderly, hyperaldosteronism, gout, or with concomitant cardiac glycosides; hyperparathyroidism (discontinue if hypercalcaemia); porphyria; hepatic impairment); renal impairment—stop if deterioration); pregnancy); breast-feeding).

MANNITOL

Dosage Form: Injection 10% (10 gm/100 ml) (500 ml), 20% (20 gm/100 ml) (500 ml) (II)

 

Recommended Dose: Acute renal failure; Prophylaxis - Oliguria: (during cardiac and other surgeries) 50-100 grams IV as a 5%-15% solution (concentration dependent on patient's fluid requirements); Acute renal failure - Oliguria: use test dose; 300-400 mg/kg (21-28 grams for a 70-kg patient) or up to 100 grams of solution, given as a single dose (often in addition to furosemide); Cerebral edema - Raised intracranial pressure: 0.25-1 gram/kg IV over 20 to 30 minutes every 6-8 hr; MAX 6 grams/kg/24 hr;Cerebral edema - Raised intracranial pressure: (to reduce brain mass before/after neurosurgery) 1.5-2 grams/kg IV over 30-60 min; Raised intraocular pressure: 1.5-2 grams/kg IV infused over 30-60 min as a 15%-20% solution; MAX 6 grams/kg/24 hr; Toxicity of drug: continuous IV infusion as a 5%-20% solution (concentration dependent on patient's fluid requirements and urinary output); discontinue if no benefit is shown after infusion of 200 grams.

 

Indications: Acute renal failure; Prophylaxis – Oliguria, Acute renal failure – Oliguria, Cerebral edema - Raised intracranial pressure, Raised intraocular pressure, Toxicity of drug.

 

Contra-Indications: Anuria, dehydration (severe), heart failure or pulmonary congestion (after initiation of mannitol), hypersensitivity to mannitol, intracranial bleeding (except during craniotomy), pulmonary edema/congestion,renal damage/dysfunction (after initiation of mannitol).

 

Special Precautions: Cardiopulmonary dysfunction, electrolyte imbalance, renal impairment

SPIRONOLACTONE

Dosage Form: Tablet 25 mg (II)

 

Recommended Dose: 100–200 mg daily, increased to 400 mg if required; child initially 3 mg/kg daily in divided doses

 

Indications: Oedema and ascites in cirrhosis of the liver, malignant ascites, nephrotic syndrome, congestive heart failure, primary hyperaldosteronism

 

Contra-Indications: Hyperkalaemia, hyponatraemia; Addison's disease

 

Special Precautions: Potential metabolic products carcinogenic in rodents; elderly; monitor electrolytes (discontinue if hyperkalaemia); porphyria; hepatic impairment; renal impairment; pregnancy; breast-feeding.

 

9.2 Anti Anginal/Coronary Vasodilators

9.2.1 Nitrates

GLYCERYL TRINITRATE

Dosage Form: Tablet 0.5 mg (II)

 

Recommended Dose: Sublingually 0.3–1 mg, repeated as required

 

Indications: Prophylaxis and treatment of angina and left ventricular failure.

 

Contra-Indications: Hypersensitivity to nitrates; hypotensive conditions and hypovolaemia; hypertrophic obstructive cardiomyopathy, aortic stenosis, cardiac tamponade, constrictive pericarditis, mitral stenosis; marked anaemia, closed-angle glaucoma.

 

Special Precautions: Severe hepatic or renal impairment; hypothyroidism, malnutrition, or hypothermia; head trauma, cerebral haemorrhage; recent history of myocardial infarction; metal-containing transdermal systems should be removed before cardioversion or diathermy; tolerance.

ISOSORBIDE DINITRATE

Dosage Form: Tablet 10 mg; Injection 10 mg/10 ml (II)

 

Recommended Dose: By mouth, daily in divided doses, angina 30–120 mg, left ventricular failure 40–160 mg, up to 240 mg if required. By intravenous infusion, 2–10 mg/hour; higher doses up to 20 mg/hour may be required

 

Indications: Prophylaxis and treatment of angina and left ventricular failure.

 

Contra-Indications: Hypersensitivity to nitrates; hypotensive conditions and hypovolaemia; hypertrophic obstructive cardiomyopathy, aortic stenosis, cardiac tamponade, constrictive pericarditis, mitral stenosis; marked anaemia, closed-angle glaucoma.

 

Special Precautions: Severe hepatic or renal impairment; hypothyroidism, malnutrition, or hypothermia; head trauma, cerebral haemorrhage; recent history of myocardial infarction; metal-containing transdermal systems should be removed before cardioversion or diathermy; tolerance.

NITROGLYCERIN

Dosage Form: Transdermal Disc (TDD) 5 mg, 10 mg; Injection 10 mg/10 ml (l)

 

Recommended Dose: 5mg daily applied to healthy, non-hairy, clean and dry skin of chest or on inner side of upper arm. If well tolerated, dose can be increased (stepwise) to 10-20 mg daily.

 

Indications: Treatment of angina pectoris and congestive heart failure

 

Contra-indications: Known intolerance of organic nitrate drugs and marked anaemia.

 

Special Precautions: Not intended for immediate relief of acute attacks. If these occur, other preparation should be used. Apply new disc every 24 hours to different site.

9.2.2 Calcium Channel Blocker

AMLODIPINE BESYLATE

Dosage Form: Tablets 5 mg, 10 mg (II)

 

Recommended Dose: Hypertension or angina, initially 5 mg once daily; max. 10 mg once daily.

 

Indications: Hypertension, prophylaxis of angina.

 

Contra-Indications: Cardiogenic shock, unstable angina,significant aortic stenosis; pregancy and breastfeeding

 

Special Precautions: Hepatic impairment.

AMLODIPINE BESYLATE + ATORVASTATIN

Dosage Form: Tablet 5 mg +10 mg, 10 mg + 10 mg, 5 mg + 20 mg (II)

 

Recommended Dose: 5 mg/10 mg to a max dose of 10 mg/80 mg once daily.

 

Indications: For hypertension in patients stabilized on the individual components in the same proportions.

 

Contra-Indications: Active liver disease or unexplained persistent elevations of serum transaminases >3x the upper limit of normal. Pregnancy, lactation or women of childbearing potential who are not using adequate contraceptive measures.

 

Special Precautions: Heart failure. Co-administration with drugs that may decrease the levels or activity of endogenous steroid hormones (eg ketoconazole, spironolactone & cimetidine). History of liver disease or heavy alcohol consumption. Perform liver fucntion tests before treatment & periodically thereafter. Should an increase in ALT or AST of >3x the upper limit of normal persist, reduce dose or withdraw drug. Patients should be advised to report promptly any unexplained muscle pain, muscle tenderness or weakness especially if accompanied by malaise or fever. Discontinue if markedly elevated CPK levels occur or myopathy is diagnosed or suspected. Women of childbearing potential. Rarely, patients (esp those w/ severe obstructive coronary artery disease) have developed increased frequency, duration &/or severity of angina or acute MI on starting Ca-channel blocker therapy or at the time of dosage increase.

AMLODIPINE BESYLATE + VALSARTAN

Dosage Form: Tablet 5 mg + 80 mg, 5 mg + 160 mg, 10 mg + 160 mg (I)

 

Recommended Dose: 1 tab/day

 

Indications: Essential hypertension where BP is not adequately controlled on antihypertensive monotherapy

 

Contra-Indications: Pregnancy

 

Special Precautions: Risk of hypotension in Na- &/or vol-depleted patients. ß-blocker w/drawal should be gradual. Severe renal impairment (CrCl <10 mL/min), dialysis. Unilateral/bilateral renal artery stenosis, stenosis to a solitary kidney, after recent kidney transplantation, hepatic impairment, biliary obstructive disorders. Aortic or mitral stenosis, obstructive hypertrophic cardiomyopathy. May impair ability to drive or operate machinery. Avoid in women planning a pregnancy, lactation. Childn <18 yr

DILTIAZEM HYDROCHLORIDE

Dosage Form: Tablet 30 mg; Injection 10 mg (II)

 

Recommended Dose: Angina, 60 mg 3 times daily (elderly initially twice daily); increased if necessary to 360 mg daily

 

Indications: Prophylaxis and treatment of angina; hypertension

 

Contra-Indications: Severe bradycardia, left ventricular failure with pulmonary congestion, second- or third-degree AV block (unless pacemaker fitted), sick sinus syndrome; pregnancy; breast-feeding.

 

Special Precautions: Reduce dose in hepatic and renal impairment; heart failure or significantly impaired left ventricular function, bradycardia (avoid if severe), first degree AV block, or prolonged PR interval.

FELODIPINE

Dosage Form: Tablet 2.5 mg, 5 mg, 10 mg (I)

 

Recommended Dose: Hypertension, initially 5 mg (elderly 2.5 mg) daily in the morning; usual maintenance 5–10 mg once daily; doses above 20 mg daily rarely needed. Angina, initially 5 mg daily in the morning, increased if necessary to 10 mg once daily.

 

Indications: Hypertension, prophylaxis of angina

 

Contra-Indications: Unstable angina, uncontrolled heart failure; significant aortic stenosis; within 1 month of myocardial infarction; pregnancy, including the early stages, hypertensitivity to felodipine

 

Special Precautions: Withdraw if ischaemic pain occurs or existing pain worsens shortly after initiating treatment or if cardiogenic shock develops; severe left ventricular dysfunction; avoid grapefruit juice (may affect metabolism); reduce dose in hepatic impairment; breast-feeding.

NIFEDIPINE

Dosage Form: Tablet 10 mg (II)

 

Recommended Dose: 10 mg tds up to 20 mg tds if necessary with or after food. Elderly: 5 mg tds. For immediate effect, bite the capsule and retain liquid in mouth (in angina): 10-20 mg. Maximum dose: 180 mg/day regular release preparation. Children: 0.25-0.5 mg/kg SL.

 

Indications: Prophylaxis of angina; hypertension; Raynaud's phenomenon

 

Contra-Indications: Cardiogenic shock; advanced aortic stenosis; within 1 month of myocardial infarction; unstable or acute attacks of angina; porphyria.

 

Special Precautions: Withdraw if ischaemic pain occurs or existing pain worsens shortly after initiating treatment; poor cardiac reserve; heart failure or significantly impaired left ventricular function (heart failure deterioration observed); severe hypotension; reduce dose in hepatic impairment; diabetes mellitus; may inhibit labour; pregnancy; breast-feeding; avoid grapefruit juice (may affect metabolism).

NIMODIPINE

Dosage Form: Tablet 30 mg; Injection 10 mg /50 ml (I)

 

Recommended Dose: Adult: PO Prophylaxis of neurological deficit following subarachnoid haemorrhage 60 mg 4 hrly for 21 days beginning w/in 4 days of onset of haemorrhage. IV Ischaemic neurological deficits following subarachnoid haemorrhage Initial: 1 mg/hr for 2 hr, up to 2 mg/hr if no severe decrease in BP is observed. Start treatment at once and continue for 5-14 days. Total duration should not exceed 21 days if patient has received oral treatment. Treatment, by intravenous infusion via central catheter, initially 1 mg/hour (up to 500 micrograms/hour if body-weight less than 70 kg or if blood pressure unstable), increased after 2 hours to 2 mg/hour if no severe fall in blood pressure; continue for at least 5 days (max. 14 days); if surgical intervention during treatment, continue for at least 5 days after surgery; max. total duration of nimodipine use 21 days

 

Indications: Prevention and treatment of ischaemic neurological deficits following aneurysmal subarachnoid haemorrhage.

 

Contra-Indications: Within 1 month of myocardial infarction; unstable angina.

 

Special Precautions: Cerebral oedema or severely raised intracranial pressure; hypotension; avoid concomitant administration of nimodipine tablets and infusion, other calcium-channel blockers, or beta-blockers; concomitant nephrotoxic drugs; avoid grapefruit juice (may affect metabolism); hepatic impairment; renal impairment & pregnancy.

9.2.3 Other

PAPAVERINE HCL

 

Dosage Form: Injection 60 mg/2 ml (I)

 

Recommended Dose: Papaverine hydrochloride may be administered intravenously or intramuscularly. The intravenous route is recommended when an immediate effect is desired, but the drug must be injected slowly over the course of 1 or 2 minutes to avoid uncomfortable or alarming side effects. Parenteral administration of papaverine hydrochloride in doses of 1 to 4 mL is repeated every 3 hours as indicated. In the treatment of cardiac extrasystoles, 2 doses may be given 10 minutes apart.

 

Indications: Papaverine is recommended in various conditions accompanied by spasm of smooth muscle, such as vascular spasm associated with acute myocardial infarction (coronary occlusion), angina pectoris, peripheral and pulmonary embolism, peripheral vascular disease in which there is a vasospastic element, or certain cerebral angiospastic states; and visceral spasm, as in ureteral, biliary, or gastrointestinal colic.

 

Contraindications: Intravenous injection of papaverine is contraindicated in the presence of complete atrioventricular heart block. When conduction is depressed, the drug may produce transient ectopic rhythms of ventricular origin, either premature beats or paroxysmal tachycardia.

Papaverine hydrochloride is not indicated for the treatment of impotence by intracorporeal injection. The intracorporeal injection of papaverine hydrochloride has been reported to have resulted in persistent priapism requiring medical and surgical intervention.

 

Special Precautions: Should not be added to Lactated Ringer's Injection, because precipitation would result.

Papaverine hydrochloride should be used with caution in patients with glaucoma. The medication should be discontinued if hepatic hypersensitivity with gastrointestinal symptoms, jaundice or eosinophilia becomes evident or if liver function test values become altered.

 

TRIMETAZIDINE DIHYDROCHLORIDE (Metabolic Agent)

Dosage Form: MR tablet 35 mg (I* - Medical)

 

Recommended Dose: 1 tab morning & evening. Should be taken with food.

 

Indications: Prophylactic treatment of episodes of angina pectoris. Adjuvant symptomatic treatment of vertigo & tinnitus. Adjuvant treatment of the decline in visual acuity & visual field disturbances presumably of vascular origin.

 

Contra-Indications: Pregnancy & lactation.

 

Special Precautions: Not indicated for treatment of acute angina attacks, unstable angina or MI.

 

9.3 Vasoconstrictor

DOBUTAMINE HYDROCHLORIDE

Dosage Form: Injection 250 mg/20 ml (vial) (I)

 

Recommended Dose: 2.5-10 mcg/kg/min.

 

Indications: Short-term treatment of cardiac failure secondary to acute MI or cardiac surgery.

 

Contra-Indications: Idiopathic hypertropic subaortic stenosis.

 

Special Precautions: Monitor ECG & BP continuously. Correct hypovolaemia before treatment. Atrial fibrillation w/ rapid ventricular response, pre-existing hypertension.

EPHEDRINE

Dosage Form: Injection 30 mg/ml (II)

 

Recommended Dose: IM, SC or IV Severe, acute bronchospasm 12.5-25 mg. When used as a pressor agent Adult 25-50 mg SC/IM. If necessary, a 2nd IM dose of 50 mg or an IV dose of 25 mg may be given. Direct IV inj, 10-25 mg may be given slowly. Max parenteral adult dose: 150 mg in 24 hr. Childn 3 mg/kg or 100 mg/m2 SC or IV daily, in 4-6 divided doses.

 

Indications: Treatment of bronchial spasm in asthma & to produce cardiac stimulation & vasoconstriction in the treatment of shock. Adjunct to correct haemodynamic imbalances which persist after adequate fluid vol replacement. Treat hypotension during spinal anaesth.

 

Contra-Indications: Closed-angle glaucoma. Patients being treated w/ MAOIs or w/in 10 days of ceasing such treatment. Coronary thrombosis, HTN & hyperthyroidism.

 

Special Precautions: Geriatric males (esp those w/ an enlarged prostate), diabetics, & patients w/ CV disease. Patients receiving chloroform, cyclopropane, halothane or other halogenated anaesth.

NORADRENALINE (NOREPINEPHRINE) BITARTRATE

Dosage Form: Injection 4 mg/4 ml amp (I)

 

Recommended Dose: Acute hypotension, by intravenous infusion, via central venous catheter, of a solution containing noradrenaline acid tartrate 80 micrograms/mL (equivalent to noradrenaline base 40 micrograms/mL) at an initial rate of 0.16–0.33 mL/minute, adjusted according to response. Cardiac arrest, by rapid intravenous or intracardiac injection, 0.5–0.75 mL of a solution containing noradrenaline acid tartrate 200 micrograms/mL (equivalent to noradrenaline base 100 micrograms/mL)

 

Indications: Acute hypotension, Cardiac arrest

 

Contra-Indications: Hypertension (monitor blood pressure and rate of flow frequently); pregnancy.

 

Special Precautions: Coronary, mesenteric, or peripheral vascular thrombosis; following myocardial infarction, Prinzmetal's variant angina, hyperthyroidism, diabetes mellitus; hypoxia or hypercapnia; uncorrected hypovolaemia; elderly; extravasation at injection site may cause necrosis

HAEMACCEL (MODIFIED POLYPEPTIDES- POLYGELINE)

Dosage Form: Injection 3.5% (II)

 

Recommended Dose: The usual dose is 500 to 1000 milliliters (mL), with total dosage not to exceed 2500 mL daily (or approximately 20 mL/kg/day). Patients losing volumes of blood greater 1500 mL will require blood transfusion other than polygeline and crystalloid solutions.  

 

Indications: Volume expander

 

Contra-Indications: Hypersensitivity to polygeline, Asthma, Histamine release predisposition,  Hemostatic defects, Cardiac failure, Hypercalcemia

Special Precautions Patients with impaired renal function, patients at risk of developing pulmonary edema and/or congestive heart failure

PHENYLEPHRINE HCL

Dosage Form: Injection 1% (10 mg/ml) (I* - ICL & OT Cardiology)

 

Recommended Dose: SUBCUTANEOUSLY OR INTRAMUSCULAR: Usual dose, from 2mg to 5 mg. Range, from 1mg to 10mg. Initial dose should not exceed 5mg. INTRAVENOUSLY: Usual dose, 0.2mg. Range, from 0.1mg to 0.5mg. Initial dose should not exceed 0.5 mg. Injections should not be repeated more often than every 10 to 15 minutes. A 5 mg intramuscular dose should raise blood pressure for one to two hours. A 0.5 mg intravenously dose should elevate the blood pressure for about 15 minutes.

 

Indications: For the maintenance of an adequate level of blood pressure during spinal and inhalation anesthesia. For the treatment of vascular failure in shock, shock–like states and drug induced hypertension or hypersensitivity. To overcome paroxysmal supraventricular tachycardia, to prolong spinal anesthesia and as a vasoconstrictor in regional analgesia.

 

Contra-Indications: Should not be used in patients with severe hypertension, ventricular tachycardia or in patients who are hypersensitivity to it or to any of the components.

 

Special Precautions: Phenylephrine hydrochloride should be employed only with extreme caution in elderly patients or in patients with hyperthyroidism, bradycardia, partial heart block, myocardial disease or severe arteriosclerosis.

 

9.4 Anti Arrhythmic Agents

ADENOSINE

Dosage Form: Injection 3 mg/ ml (2 ml vial) (I)

 

Recommended Dose: By rapid intravenous injection into central or large peripheral vein, 3 mg over 2 seconds with cardiac monitoring; if necessary followed by 6 mg after 1–2 minutes, and then by 12 mg after a further 1–2 minutes; increments should not be given if high level AV block develops at any particular dose

 

Indications: Rapid conversion to a normal sinus rhythm of paroxysmal supraventricular tachycardias, including those associated w/ accessory by-pass tract (Wolff-Parkinson-White syndrome). Aid to diagnosis of broad or narrow complex supraventricular tachycardias.

 

Contra-Indications: second- or third-degree AV block and sick sinus syndrome (unless pacemaker fitted); asthma

 

Special Precautions: atrial fibrillation or flutter with accessory pathway (conduction down anomalous pathway may increase); heart transplant

AMIODARONE HCL

Dosage Form: Tablet 200 mg; Injection 150 mg/3 ml (II)

 

Recommended Dose: By mouth, 200 mg 3 times daily for 1 week reduced to 200 mg twice daily for a further week; maintenance, usually 200 mg daily or the minimum required to control the arrhythmia.By intravenous infusion via central venous catheter, initially 5 mg/kg over 20–120 minutes with ECG monitoring; subsequent infusion given if necessary according to response up to max. 1.2 g in 24 hours.Ventricular fibrillation or pulseless ventricular tachycardia, by intravenous injection over at least 3 minutes, 300 mg.

 

Indications: Treatment of tachyarrythmias associated with Wolff-Parkinson-White syndrome, control of ventricular and supraventricular arrythmias, in management of angina pectoris. Reserve for treatment of life-threatening arrythmias or which are unresponsive to other drugs. Ventricular extra systoles, atrial or ventricular tachyarrythmias, flutter, atrial fibrillation and ventricular fibrillation.

 

Contra-Indications: Sinus bradycardia, sino-atrial heart block; unless pacemaker fitted avoid in severe conduction disturbances or sinus node disease; thyroid dysfunction; iodine sensitivity; avoid intravenous use in severe respiratory failure, circulatory collapse (except in cardiac arrest), severe arterial hypotension; avoid bolus injection in congestive heart failure or cardiomyopathy; pregnancy; breast-feeding.

 

Special Precautions: Liver-function and thyroid-function tests required before treatment and then every 6 months (see notes above for tests of thyroid function); serum potassium concentration and chest x-ray required before treatment; heart failure; elderly; severe bradycardia and conduction disturbances in excessive dosage; intravenous use may cause moderate and transient fall in blood pressure (circulatory collapse precipitated by rapid administration or overdosage) or severe hepatocellular toxicity (monitor transaminases closely); porphyria.

b-ADRENORECEPTOR BLOCKING AGENTS

Refer 9.7 Antihypertensive Agents.

LIGNOCAINE HYDROCHLORIDE

Dosage Form: Injection 100 mg/5 ml, 500 mg/5 ml (I)

 

Recommended Dose: By intravenous injection, in patients without gross circulatory impairment, 100 mg as a bolus over a few minutes (50 mg in lighter patients or those whose circulation is severely impaired), followed immediately by infusion of 4 mg/minute for 30 minutes, 2 mg/minute for 2 hours, then 1 mg/minute; reduce concentration further if infusion continued beyond 24 hours (ECG monitoring and specialist advice for infusion.

 

Indications: Ventricular arrhythmias, especially after myocardial infarction

 

Contra-Indications: Sino-atrial disorders, all grades of atrioventricular block, severe myocardial depression; porphyria.

 

Special Precautions: Lower doses in congestive cardiac failure, and following cardiac surgery; elderly; hepatic impairment; renal impairment; pregnancy.

PHENYTOIN SODIUM

Dosage Form: Capsule 30 mg, 100 mg; Suspension 30 mg/5 ml, 125 mg/5 ml; Injection 50 mg, 100 mg/2 ml, 250 mg/5 ml (II)

 

Recommended Dose: By slow IV inj: 3.5-5 mg/kg repeated if necessary at a rate not exceeding 50 mg/min. Maintenance: orally 100-200 mg tds with or after food. ECG monitoring recommended. For maximum benefit, dosage should be individualized.

 

Indications: Treatment of digitalis induced arrythmias of both the ventricular and supraventricular types.

 

Contra-Indications: IV administration to patients with heart block, bradycardia, Stokes-Adams syndrome.

 

Special Precautions: Elderly, children, diabetes mellitus, impaired renal and hepatic function, severe respiratory depression, hypotension, severe myocardial insufficiency. Avoid extravasation, abrupt withdrawal, pregnancy. Discontinue if skin rash occurs.

VERAPAMIL HYDROCHLORIDE

Dosage Form: Tablet 40 mg; Injection 5 mg/2 ml (I)

 

Recommended Dose: By mouth, supraventricular arrhythmias (but see also Contra-indications), 40–120 mg 3 times daily, Angina, 80–120 mg 3 times daily. Hypertension, 240–480 mg daily in 2–3 divided doses. By slow intravenous injection over 2 minutes (3 minutes in elderly), 5–10 mg (preferably with ECG monitoring); in paroxysmal tachyarrhythmias a further 5 mg after 5–10 minutes if required.

 

Indications: Angina pectoris, hypertension, treatment of supraventricular arrythmias (PSVT), atrial fibrillation, atrial flutter.

 

Contra-Indications: Hypotension, bradycardia, second- and third-degree AV block, sick sinus syndrome, cardiogenic shock, sino-atrial block; history of heart failure or significantly impaired left ventricular function, even if controlled by therapy; atrial flutter or fibrillation complicating Wolff-Parkinson-White syndrome; porphyria.

 

Special Precautions: First-degree AV block; acute phase of myocardial infarction (avoid if bradycardia, hypotension, left ventricular failure); patients taking beta-blockers; hepatic impairment; children, specialist advice only; pregnancy and breast-feeding; avoid grapefruit juice (may affect metabolism).

 

9.5 Vascular Sclerosants

SODIUM TETRADECYL SULPHATE

Dosage Form: Injection 3%  in 1 ml ampule (I)

 

Recommended Dose: Slow injection into empty isolated segment of veins, 0.1-1ml according to site and condition being treated

 

Indications: Sclerotherapy of vericose vein

 

Contra-Indications: Inability to walk, acute phlebitis, oral contraceptive use, obese legs

 

Special Precautions: Extravasation may cause necrosis of tissues.

 

9.6 Cerebro-Vascular Agents

9.6.1 Peripheral Vasodilator

CINNARIZINE

Dosage Form: Tablet 25 mg (II)

 

Recommended Dose: Initially: 75 mg tds. Maintenance: 75 mg bd-tds.

 

Indications: Peripheral vascular disease, Raynaud's disease.

 

Special Precautions: In patients with hypotension, extra pyramidal symptoms, epilepsy, prostatic hypertrophy, urinary retention, glaucoma and pyloroduodenal obstruction. Hepatic disease and renal impairment.

 

PAPAVERINE HCL

Dosage Form: Injection 60 mg/2 ml (I)

 

Recommended Dose: Papaverine hydrochloride may be administered intravenously or intramuscularly. The intravenous route is recommended when an immediate effect is desired, but the drug must be injected slowly over the course of 1 or 2 minutes to avoid uncomfortable or alarming side effects. Parenteral administration of papaverine hydrochloride in doses of 1 to 4 mL is repeated every 3 hours as indicated. In the treatment of cardiac extrasystoles, 2 doses may be given 10 minutes apart.

 

Indications: Papaverine is recommended in various conditions accompanied by spasm of smooth muscle, such as vascular spasm associated with acute myocardial infarction (coronary occlusion), angina pectoris, peripheral and pulmonary embolism, peripheral vascular disease in which there is a vasospastic element, or certain cerebral angiospastic states; and visceral spasm, as in ureteral, biliary, or gastrointestinal colic.

 

Contraindications: Intravenous injection of papaverine is contraindicated in the presence of complete atrioventricular heart block. When conduction is depressed, the drug may produce transient ectopic rhythms of ventricular origin, either premature beats or paroxysmal tachycardia.

Papaverine hydrochloride is not indicated for the treatment of impotence by intracorporeal injection. The intracorporeal injection of papaverine hydrochloride has been reported to have resulted in persistent priapism requiring medical and surgical intervention.

 

Special Precautions: Should not be added to Lactated Ringer's Injection, because precipitation would result.

Papaverine hydrochloride should be used with caution in patients with glaucoma. The medication should be discontinued if hepatic hypersensitivity with gastrointestinal symptoms, jaundice or eosinophilia becomes evident or if liver function test values become altered.

 

PENTOXIFYLLINE

Dosage Form: Tablet 400 mg (I)

 

Recommended Dose: 400 mg 2–3 times daily

Indications: Peripheral vascular disease.

 

Contra-Indications: Cerebral haemorrhage, extensive retinal haemorrhage, acute myocardial infarction; pregnancy and breast-feeding.

 

Special Precautions: Hypotension, coronary artery disease; renal impairment, severe hepatic impairment; avoid in porphyria.

 

9.7 Antihypertensive Agents

9.7.1 Centrally Acting Agents

METHYLDOPA

Dosage Form: Tablet 250 mg (II)

 

Recommended Dose: Initially 250 mg 2–3 times daily, increased gradually at intervals of 2 or more days, max. 3 g daily; elderly initially 125 mg twice daily, increased gradually, max. 2 g daily.

 

Indications: Hypertension.

 

Contra-Indications: Depression, active liver disease, phaeochromocytoma; porphyria

 

Special Precautions: History of liver impairment ; renal impairment; blood counts and liver-function tests advised; history of depression; positive direct Coombs' test in up to 20% of patients (may affect blood cross-matching); interference with laboratory tests.

9.7.2 Vasodilating Agents

HYDRALLAZINE HCL (@ Dihydrallazine)

Dosage Form: Injection 20 mg (II)

 

Recommended Dose: Hypertensive crisis; Adult: 5-10 mg via slow IV inj, repeated if necessary after 20-30 min. Alternatively, as continuous IV, initial dose is 200-300 mcg/min. Maintenance: 50-150 mcg/min.

 

Indications: Hypertensive crisis

 

Contra-Indications: Severe tachycardia, dissecting aortic aneurysm, heart failure with high cardiac output, cor pulmonale, myocardial insufficiency due to mechanical obstruction, coronary artery disease, idiopathic SLE. Patients with recent MI.

 

Special Precautions: Cerebrovascular disorders. Ischaemic heart disease. Hepatic or renal impairment. May deplete pyridoxine in the body. May impair ability to drive or operate machinery. Monitor for postural hypotension if given to patients with heart failure. Withdraw gradually. CBC and antinuclear antibody tests should be carried out every 6 mth during long-term therapy. Urine analysis is also recommended. Pregnancy and lactation. Daily doses >100 mg may increase the risk of SLE especially in women and slow acetylators.

SILDENAFIL

Dosage Form: Tablet 50 mg (II)

 

Criteria of use: For Pulmonary arterial hypertension only

 

Recommended Dose: Pulmonary arterial hypertension, Adult: 50-100 mg OD. 50 mg QID, if developed nausea, headache, decreased dose; 12.5 mg QID for 1-2 week, then up to 12.5 mg 4 hourly. Peadiatric: 0.3–2 mg/kg/dose every 3-6 hour. Erectile Dysfunction: Adult: 50 mg OD taken approximately 1 hour before sexual activity. The dose may be increased to 100 mg/decreased to 25 mg. Max 100 mg OD. Elderly > 65 years old: initially 25 mg may increase to 50-100 mg based on efficacy & toleration.

 

Indications: Pulmonary arterial hypertension &. Erectile Dysfunction

 

Contra-Indications: Patients receiving nitrates (in any form)/patients in whom vasodilation/sexual activity are inadvisable (patients with severe cardiovascular disorders e.g. unstable angina/ severe cardiac failure), severe hepatic impairment, hypotension (< 90/50mmHg), recent history of stroke/myocardial infarction, known hereditary degenerative retinal disorders such as retinitis pigmentosa. Hypersensitivity to sildenafil.

 

Special Precautions: Anatomical deformation of the penis (angulation, cavernal fibrosis, Peyronie's disease), Conditions predisposing patients to priapism (sickle cell anemia, multiple myeloma, or leukemia), Bleeding disorders or active peptic ulceration/untreated proliferative diabetic retinopathy, Retinitis pigmentosa or other retinal abnormality, Coronary ischemia or congestive heart failure, Multi-drug antihypertensive regimens, Concurrent use of erythromycin, cimetidine, or other drugs that could prolong the half-life of sildenafil, coadministarion with ritonavir not advised,if necessary, max dose of sildenafil is 25mg/48 hours.

SODIUM NITROPRUSSIDE

Dosage Form: Injection 50 mg/ 5 ml ampule (I)

 

Recommended Dose: Adult Commence infusion at 0.5 mcg/kg/min & adjust in increments of 0.5 mcg/kg/min every 5 mins until desired BP reduction is obtained. Patient not receiving antihypertensive drugs 3 mcg/kg/min (range: 0.5-10 mcg/kg/min).

 

Indications: Immediate reduction of BP of patients in hypertensive crises. To produce controlled hypotension during anesth to reduce bleeding.

 

Contra-Indications: Compensatory hypertension; physically poor-risk patients or w/ uncorrected anaemia or hypovolemia or those w/ known inadequate cerebral circulation. Avoid sildenafil, tadalafil, vardenafil.

 

Special Precautions: Renal, hepatic or cerebrovascular impairment; low plasma-cobalamin conc; Leber's optic atrophy; hypothyroidism, impaired cyanide metabolism, hypothermia, stress.

9.7.3 a-b-Adrenoceptor Blocking Agent

ESMOLOL HCL

Dosage Form: Injection 100 mg/10ml (I)

 

Recommended Dose: SUPRAVENTRICULAR TACHYCARDIA

Dosage needs to be titrated, using ventricular rate as the guide. An initial loading dose of 0.5 milligrams/kg (500 micrograms/kg) infused over a minute duration followed by a maintenance infusion of 0.05 milligrams/kg/min (50 micrograms/kg/min) for the next 4 minutes is recommended. This should give a rough guide with respect to the responsiveness of ventricular rate. After the 4 minutes of initial maintenance infusion (total treatment duration being 5 minutes), depending upon the desired ventricular response, the maintenance infusion may be continued at 0.05 mg/kg/min or increased step-wise (e.g. 0.1 mg/kg/min, 0.15 mg/kg/min to a maximum of 0.2 mg/kg/min) with each step being maintained for 4 or more minutes.

 INTRAOPERATIVE AND POSTOPERATIVE TACHYCARDIA AND/OR HYPERTENSION

In the intraoperative and postoperative settings it is not always advisable to slowly titrate the dose of BREVIBLOC (Esmolol Hydrochloride) to a therapeutic effect. Therefore, two dosing options are presented: immediate control dosing and a gradual control when the physician has time to titrate.

Immediate Control

For intraoperative treatment of tachycardia and/or hypertension give an 80 mg (approximately 1 mg/kg) bolus dose over 30 seconds followed by a 150 mcg/kg/min infusion, if necessary. Adjust the infusion rate as required up to 300 mcg/kg/min to maintain desired heart rate and/or blood pressure.

Gradual Control

For postoperative tachycardia and hypertension, the dosing schedule is the same as that used in supraventricular tachycardia. To initiate treatment, administer a loading dosage infusion of 500 mcg/kg/min of BREVIBLOC for one minute followed by a four-minute maintenance infusion of 50 mcg/kg/min. If an adequate therapeutic effect is not observed within five minutes, repeat the same loading dosage and follow with a maintenance infusion increased to 100 mcg/kg/min.

 

Indications: Supraventricular tachycardia, Intraoperative and postoperative tachycardia and/or hypertension.

 

Contraindications: In patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock or overt heart failure.

 

Special Precautions: Because the acid metabolite of esmolol is primarily excreted unchanged by the kidney, it should be administered with caution to patients with impaired renal function. The elimination half-life of the acid metabolite was prolonged ten-fold and the plasma level was considerably elevated in patients with end-stage renal disease.

LABETALOL HCL

Dosage form : Tablet 100 mg,  Injection  25 mg/ 5 ml (II)

 

Recommended dose: By mouth, initially 100 mg (50 mg in elderly) twice daily with food, increased at intervals of 14 days to usual dose of 200 mg twice daily; up to 800 mg daily in 2 divided doses (3–4 divided doses if higher); max. 2.4 g daily

By intravenous injection, 50 mg over at least 1 minute, repeated after 5 minutes if necessary; max. total dose 200 mg

 

Indications: hypertension (including hypertension in pregnancy, hypertension with angina, and hypertension following acute myocardial infarction); hypertensive crisis, controlled hypotension in anaesthesia

 

Contra-Indications: asthma, uncontrolled heart failure, Prinzmetal's angina, marked bradycardia, hypotension, sick sinus syndrome, second- or third- degree AV block, cardiogenic shock, metabolic acidosis, severe peripheral arterial disease; phaeochromocytoma (apart from specific use with alpha-blockers, see also notes above

 

Special Precautions: Severe hepatocellular damage reported after both short-term and long-term treatment. Appropriate laboratory testing needed at first symptom of liver dysfunction and if laboratory evidence of damage (or if jaundice) labetalol should be stopped and not restarted

9.7.4 b-Adrenoceptor Blocking Agents

ATENOLOL

Dosage Form: Tablet 50 mg, 100 mg (II)

 

Recommended Dose: For hypertension, 50 mg daily increase every week up to max of 200 mg. Maintenance: 100 mg daily. Angina: 100 mg daily. Arrythmias: 50-100 mg daily.

 

Indications: Hypertension, Angina, Arrhythmias

 

Contra-Indications: Asthma (important: see Bronchospasm below), uncontrolled heart failure, Prinzmetal's angina, marked bradycardia, hypotension, sick sinus syndrome, second- or third- degree AV block, cardiogenic shock, metabolic acidosis, severe peripheral arterial disease; phaeochromocytoma (apart from specific use with alpha-blockers, see also notes above)

 

Special Precautions: Avoid abrupt withdrawal especially in ischaemic heart disease; first-degree AV block; portal hypertension (risk of deterioration in liver function); diabetes; history of obstructive airways disease (introduce cautiously and monitor lung function—see also Bronchospasm below); myasthenia gravis; history of hypersensitivity—may increase sensitivity to allergens and result in more serious hypersensitivity response, also may reduce response to adrenaline (epinephrine) see also notes above; reduce dose of oral propranolol in hepatic impairment; renal impairment, pregnancy, breast-feeding.

BISOPROLOL FUMARATE

Dosage Form: Tablet 2.5 mg, 5 mg (I)

 

Recommended Dose: For hypertension, 2.5 mg – 20 mg. Usual dose: 5 mg daily, increase gradually to achieved an optimum effect by a few days for a several weeks. Angina: 5-20 mg daily.

 

Indications: Hypertension and angina

 

Contra-Indications:  Cardiogenic shock, Hypersensitivity to bisoprolol, Overt cardiac failure, Second and third degree AV block, Severe sinus bradycardia

 

Special Precautions: Anaesthesia / surgery (myocardial depression), Avoid abrupt withdrawal, gradual withdrawal over a period of 1-2 weeks is recommended ( when discontinued: decrease gradually to avoid  rebound hypertension / angina and other severe cardiovascular problem (myocardial infarction, arrhytemias, sudden death), Bronchospastic disease, Congestive heart failure,Diabetes mellitus, Hepatic disease, Hyperthyroidism / thyrotoxicosis, Peripheral vascular disease, Renal disease

 

CARVEDILOL

 

Dosage Form: Tablet 6.25 mg, 25 mg (I)

 

Recommended Dose: Hypertension, initially 12.5 mg once daily, increased after 2 days to usual dose of 25 mg once daily; if necessary may be further increased at intervals of at least 2 weeks to max. 50 mg daily in single or divided doses; elderly initial dose of 12.5 mg daily may provide satisfactory control. Angina, initially 12.5 mg twice daily, increased after 2 days to 25 mg twice daily

Adjunct in heart failure (section 2.5.5) initially 3.125 mg twice daily (with food), dose increased at intervals of at least 2 weeks to 6.25 mg twice daily, then to 12.5 mg twice daily, then to 25 mg twice daily; increase to highest dose tolerated, max. 25 mg twice daily in patients with severe heart failure or body-weight less than 85 kg and 50 mg twice daily in patients over 85 kg

 

Indications: Hypertension; angina; adjunct to diuretics, digoxin, or ACE inhibitors in symptomatic chronic heart failure

 

Contra-Indications: Asthma, uncontrolled heart failure, Prinzmetal’s angina, marked bradycardia, hypotension, sick sinus syndrome, 2nd or 3rd degree AV block, cardiogenic shock, metabolic acidosis, severe peripheral arterial disease, phaeochromocytoma, hepatic impairment.

 

Special Precautions: Before increasing dose, ensure renal function and heart failure not deteriorating. Avoid in acute or decompensated heart failure requiring intravenous inotropes.

METOPROLOL TARTRATE

Dosage Form: Tablet 100 mg (II)

 

Recommended Dose: Oral: For hypertension: Initially 50-100 mg bd for 1 week. Maintenance: 100-200 mg bd. Angina: 50-100 mg bd-tds. Hyperthyroidism: 50 mg qid. Arrythmias: 50 mg bd-tds up to 300 mg daily if necessary, in divided doses. Injection: up to 5 mg at rate 1-2 mg/min, repeated after 5 min if necessary, toatal dose of 10-15 mg. Surgery: 2-4 mg by slow IV inj. at induction or to control arrythmias developing during anaesthesias; 2 mg doses may be repeated to a max of 10 mg. Early intervention within 12 hrs of infarction, 5 mg by IV inj. every 2 min to a max of 15 mg followed after 15 min by 15 mg p.o q 6 hourly for 48 hrs.

 

Indications: Hypertension, as monotherapy or in combination with diuretic. In angina pectoris. Adjunct treatment of hyperthyroidism and arrythmias. Migraine prophylaxis.

 

Contra-Indications: AV block, severe bradycardia, cardiogenic shock, heart failure, acute MI.

 

Special Precautions: Withdrawal of drug should be gradual, pregnancy, sinus bradycardia, surgery, diabetes, thyrotoxicosis, CHF.

PROPRANOLOL HYDROCHLORIDE

Dosage Form: Tablet 10 mg, 40 mg; Injection 1 mg/ml (1 ml amp) (II)

 

Recommended Dose: For hypertension: initially 40 mg bd increase at weekly intervals, when necessary; maintenance 160-320 mg daily. Angina: initially 10 mg bd-qid; maintenance 120-240 mg daily. Migraine: tremor initially 40 mg bd-tds; maintenance 80-160 g daily. Cardiac arrythmias: 10-40 mg tds-qid. Pheochromocytoma (concurrent with alpha-adrenoceptor blockade): 60 mg daily for 3 days; maintenance 30 mg daily. For emergency treatment of cardiac arrythmias: slow IV 1mg over 1 min, repeated if necessary every 2 min up to max of 10 mg (5 mg in anaesthesia). Atropine IV 1-2 mg should be given before injecting propranolol.

 

Indications: Hypertension, angina pectoris, cardiac arrythmias, prevention of migraine, essential tremor, pheochromocytoma, SVT, hyperthyroidism, anxiety or stage fright.

 

Contra-Indications: AV block, bronchospasm, metabolic acidosis, concomitant administration of verapamil, sinus bradycardia, in anaesthesia with agents that produce myocardial depression. Hypoglycemia. IV administration in hypertension. Bronchial asthma, diabetes, allergic rhinitis, Raynaud's disease, peripheral vascular disease, venom-sensitive patients.

 

Special Precautions: In patients undergoing anaesthesia: either gradual withdrawal of drug 24 hrs before or protect patient against bradycardia by IV atropine of 1-2mg and avoid agents causing myocardial depression. Reduce dosage in renal failure. Withdrawal of drug should be gradual. Propranolol is not suitable for emergency treatment of hypertension. Reduce oral dose in liver disease, late pregnancy and during breast-feeding. Given to congestive heart failure only when patient is fully digitalised and with great caution.

SOTALOL HYDROCHLORIDE

Dosage Form: Tablet 80 mg (I* - Physician)

 

Recommended Dose: By mouth with ECG monitoring and measurement of corrected QT interval, arrhythmias, initially 80 mg daily in 1–2 divided doses increased gradually at intervals of 2–3 days to usual dose of 160–320 mg daily in 2 divided doses; higher doses of 480–640 mg daily for life-threatening ventricular arrhythmias under specialist supervision

 

Indications: Hypertension, angina pectoris, thyrotoxicosis, arrhythmia, MI.

 

Contra-Indications: Bronchial asthma, COPD, cardiogenic shock, right ventricular failure secondary to hypertension, severe sinus bradycardia, > 1st degree heart block, uncontrolled CHF, renal failure.

 

Special Precautions: Prolonged fasting, diabetic ketoacidosis, metabolic acidosis, heart rate at rest < 50 beats/min, surgery, anaesth that cause myocardial depression, history of bronchial asthma, bronchospasm, abrupt w/drawal; IDDM. Monitor electrolyte balance.

9.7.5 a-Adrenoreceptor Blocking Agents

ALFUZOSIN

Dosage Form: Tablet XL 10 mg (I* - Urologist)

 

Recommended Dose: Adults: 10mg once daily

 

Indications: Treatment of functional symptoms of benign prostatic hypertrophy. Adjuvant treatment to a catheter in acute urinary retention related to benign prostatic hypertrophy.

 

Contra-Indications: Alpha-blockers should be avoided in patients with a history of postural hypotension and micturition syncope.

 

Special Precautions: Since selective alpha-blockers reduce blood pressure, patients receiving antihypertensive treatment may require reduced dosage and specialist supervision. Caution may be required in the elderly and in patients with hepatic impairment and severe renal impairment.

DOXAZOSIN

Dosage Form: Tablet XL 4 mg (as mesylate) (I* - Urologist)

 

Recommended Dose: BPH 4 mg once daily. HTN 4 mg once daily, may increase to 8 mg after 4 wk.

 

Indications: Urinary outflow obstruction & symptoms associated w/ benign prostatic hyperplasia (BPH). Hypertension (HTN).

 

Contra-Indications: Hypersensitivity to quinazolines. History of GI obstruction, oesophageal obstruction, pregnancy & lactation.

 

Special Precautions: Pregnancy, lactation. Impaired liver function, postural hypotension. GI disorders.

PRAZOSIN HYDROCHLORIDE

Dosage form : Tablet 1mg, 2mg (II)

 

Recommended dose: Hypertension, 500 micrograms 2–3 times daily for 3–7 days, the initial dose on retiring to bed at night (to avoid collapse, see Cautions); increased to 1 mg 2–3 times daily for a further 3–7 days; further increased if necessary to max. 20 mg daily in divided doses. Congestive heart failure, 500 micrograms 2–4 times daily (initial dose at bedtime, see above), increasing to 4 mg daily in divided doses; maintenance 4–20 mg daily in divided doses (but rarely used). Raynaud's syndrome (but efficacy not established ) initially 500 micrograms twice daily (initial dose at bedtime, see above) increased, if necessary, after 3–7 days to usual maintenance 1–2 mg twice daily

 

Indications: See under Dose

 

Contra-Indications: Not recommended for congestive heart failure due to mechanical obstruction (e.g. aortic stenosis)

 

Special Precautions: First dose may cause collapse due to hypotension (therefore should be taken on retiring to bed); elderly; hepatic impairment, renal impairment, pregnancy, breast-feeding.

TERAZOSIN HYDROCHLORIDE

Dosage Form: Tablet 1 mg, 2 mg, 5 mg (I*)

 

Recommended Dose: Benign prostatic hyperplasia (BPH) Initially 1 mg at bedtime, increase in a stepwise fashion to 2 mg, 5 mg or 10 mg once daily. Hypertension Initially 1 mg at bedtime. Dose range 1-5 mg once daily.

 

Indications: Symptomatic benign prostatic hyperplasia (BPH). Hypertension.

 

Contra-Indications: Pregnancy.

 

Special Precautions: May impair ability to drive or operate machinery. Lactation.

9.7.6 Angiotensin-Converting Enzyme Inhibitors

CAPTOPRIL

Dosage Form: Tablet 25 mg (II)

 

Recommended Dose: Hypertension: initially 12.5 mg twice daily. With diuretic, elderly, renal impairment: initially 6.25 mg bd (first dose at bedtime). Maintenance: 25 mg twice daily. Max: 450 mg/day. Heart failure: initially 6.25-12.5 mg with a diuretic. Maintenance: 25 mg tds.

 

Indications: Treatment of hypertension and CHF where other therapy has failed.

 

Contra-Indications: Bilateral or unilateral renal artery stenosis. Hereditary or idiopathic angioedema associated w/ previous treatment w/ ACE inhibitor. Hemodialysis. Pregnancy & lactation.

 

Special Precautions: May get a severe fall in blood pressure in sodium-depleted patients, on diuretics or under-going dialysis. Reduce dose or avoid in renal impairment. Serious autoimmune disease including SLE. Patients on immunosurpressants. Hyperkalaemia. Renal artery stenosis. Surgery/anaesthesia. Withraw if angioedema or laryngeal stridor occurs.

ENALAPRIL MALEATE

Dosage Form: Tablet 5 mg, 20 mg (I)

 

Recommended Dose: Initially: 5 mg daily. Maintenance: 10-30 mg daily. Max of 40 mg daily.

 

Indications: Treatment of hypertension and CHF.

 

Contra-Indications: Hypersensitivity.

 

Special Precautions: Reduce dose in patients with renal impairment, symptomatic hypotension, pregnancy and lactation. Febrile illness.

PERINDOPRIL ERBUMINE

Dosage Form: Tablet 4mg, 8mg (II)

 

Recommended Dose: Hypertension: 2mg daily. Usual maintenance dose 4mg once daily; maximum 8mg daily. CHF (adjunct): Initial dose 2mg in the morning under close medical supervision; maintenance 4 mg daily

 

Indications: Treatment of essential and renovascular hypertension and CHF (adjunct)

 

Contra-Indications: Bilateral or unilateral renal artery stenosis. Hereditary or idiopathic angioedema associated with precious treatment with ACE inhibitor. Hemodialysis. Pregnancy & lactation.

 

Special Precaution: Renal & hepatic impairment, collagen vascular disease, diabetic, surgery & anaesthetic. Children. Elderly.

PERINDOPRIL ERBUMINE + INDAPAMIDE

Dosage Form: Tablet 4 mg + 1.25 mg (II)

 

Recommended Dose: 1 tablet daily.

 

Indications: Treatment of essential hypertension.

 

Contra-Indications: Bilateral renal artery stenosis or single functioning kidney, severe renal failure (CrCl <30 mL/min), dialysis patients, hepatic encephalopathy, severe hepatic impairment, hyperkalaemia or hypokalaemia, untreated decompensated cardiac insufficiency. Avoid combinations w/ K-sparing diuretics, K salts, lithium & non-antiarrhythmic drugs causing torsades de pointes. Previous history of angioneurotic oedema linked to treatment w/ ACE inhibitor; hereditary or idiopathic angioneurotic oedema. Pregnancy & lactation.

 

Special Precautions: Renal insufficiency esp when associated w/ systemic autoimmune collagen vascular diseases eg SLE or scleroderma. Concomitant treatment w/ immunosuppressants or treatment causing leukopenia. Marked Na & water depletion, hypotension, CHF, cirrhosis w/ oedema & ascites, ischaemic heart disease, cerebral circulatory insufficiency, severe cardiac insufficiency (grade IV) or IDDM patients. Monitor serum K regularly. Surgery. Elderly. May impair ability to drive or operate machinery.

RAMIPRIL

Dosage Tablet 2.5 mg, 5 mg (I)

 

Recommended Dose: It is recommended Ramipril is taken ones daily, starting with dose of 2.5 mg and then the dose be doubled at intervals of 2-3 weeks if necessary, and depending on the patient’s responses. The usual maintenance dose is 2.5-5 mg daily where the maximum permitted daily dose is 10 mg. In patients with impaired renal function, ie a creatinine clearance between 50 and 20 ml/min/1.73 body surface area, the initial dose is generally reduced to 1.25 mg. The maximum permitted daily dose is 5mg in such cases.  

 

Indications: Hypertension

 

Contra-Indications: Hypersensitivity to Ramipril or any of recipients, allergy to starch, patients with a history of angioneuratic oedema, flow reducing narrowing of the renal artery, bilateral or unilateral in the single kidney. Ramipril must not be taken during pregnancy  

 

Special Precautions: Requires regular medical supervision. It is recommended that dehydration ,reduced blood volume or salt deficiency be corrected before initiating treatment ( in patients with concomitant heart failure however, this must be carefully weighed against the risk of volume overload )

9.7.7 Angiotensin II Receeptor Antagonists

AMLODIPINE BESYLATE + VALSARTAN

Dosage Form: Tablet 5 mg + 80 mg, 5 mg + 160 mg, 10 mg + 160 mg (I)

 

Recommended Dose: 1 tab/day

 

Indications: Essential hypertension where BP is not adequately controlled on antihypertensive monotherapy

 

Contra-Indications: Pregnancy

 

Special Precautions: Risk of hypotension in Na- &/or vol-depleted patients. ß-blocker w/drawal should be gradual. Severe renal impairment (CrCl <10 mL/min), dialysis. Unilateral/bilateral renal artery stenosis, stenosis to a solitary kidney, after recent kidney transplantation, hepatic impairment, biliary obstructive disorders. Aortic or mitral stenosis, obstructive hypertrophic cardiomyopathy. May impair ability to drive or operate machinery. Avoid in women planning a pregnancy, lactation. Childn <18 yr

IRBESARTAN

Dosage Form: Tablet 150 mg, 300 mg (II)

 

Recommended Dose: Initial and recommended dose: 150 mg once daily. Maybe increased to 300 mg or other antihypertensive agents may be added. In volume depleted patients, correct prior to administration. Elderly >75 yrs and hemodialysis patients, consider initiating with 75 mg.

 

Indications: Essential hypertension.

 

Contra-Indications: Pregnancy and lactation

 

Special Precautions: Increased risk of severe hypotension in patients with renal artery stenosis. Monitoring of plasma-potassium concentration and serum creatinine in the elderly and patients with renal impairment (lower initial doses may be more appropriate); Monitoring of serum-potassium in heart failure patients.

IRBESARTAN + HYDROCHLOROTHIAZIDE

Dosage Form: Tablet 150 mg + 12.5 mg, 300 mg +12.5 mg, 300 mg + 25 mg (II)

 

Criteria of use: Restricted for patients who not responding to Irbesartan monotherapy

 

Recommended dose: 1 tab once daily

 

Indications:  Treatment of essential HTN in patients whose BP is inadequately controlled on irbesartan or hydrochlorothiazide alone

 

Contra-Indications: Pregnancy, anuria and prior hypersensitivity to irbersartan or other Angiotensin II receptor blocking agents or thiazide diuretics

 

Special Precautions: Patients with history of hypersensitivity to sulphonamide and derived medication, sodium or volume depleted patients, electrolyte abnormalities

LOSARTAN

Dosage Form: Tablet 50 mg, 100 mg (II)

 

Recommended Dose: Initially 50 mg once daily. May increase to 100 mg once daily. Intravascular volume depletion: Starting dose 25 mg. History of hepatic impairment: lower doses.

 

Indications: Hypertension

 

Contra-Indications: Pregnancy

 

Special Precautions: Increased risk of severe hypotension in patients with renal artery stenosis. Monitoring of plasma-potassium concentration and serum creatinine in the elderly and patients with renal impairment (lower initial doses may be more appropriate); cirrhosis and hepatic impairment, changes in renal function, lactation and children.

LOSARTAN + HYDROCHLOROTHIAZIDE

Dosage Form: Tablet 50 mg + 12.5 mg, 100 mg + 25 mg (II)

 

Recommended Dose: Fixed-dose combination is not indicated for initial therapy. A patient not adequately controlled with losartan monotherapy or hydrochlorothiazide (HCTZ) 25 mg daily may be switched to losartan/HCTZ 50/12.5 mg once daily. If after 3 weeks blood pressure remains elevated, then dose may be increase to 100/25 mg. Maximal antihypertensive effects are attained after approximately 3 weeks. More than 100/25 mg daily is not recommended. Losartan/HCTZ may be administered with or without food.

 

Indication: Treatment of hypertension where combination therapy is appropriate.

 

Contra-Indications: Intravascularly volume depleted, severe renal impairment, hepatic impairment, anuria, hypersensitivity to other sulfonamide-derived drugs, pregnancy.

 

Special Precautions: Bilateral renal artery stenosis or stenosis of the artery to a solitary kidney, hypotension and electrolyte or fluid inbalance. Dosage adjustments in antidiabetic agents including insulins may be required. Hyperparathyroidism, SLE, lactation, children.

 

TELMISARTAN

 

Dosage Form: Tablet 40 mg, 80 mg (I)

 

Recommended Dose: Treatment of essential HTN Adult 20-40 mg once daily. Max: 80 mg once daily w/ or w/o diuretic. Severe HTN 160 mg alone or in combination w/ 12.5-25 mg hydrochlorothiazide. CV risk reduction Recommended dose: 80 mg once daily. Dose may be adjusted depending on patient's BP.

 

Indication: Treatment of essential HTN. Reduction of the risk of MI, stroke or death in patients ≥55 yr at high risk of CV events (history of coronary/peripheral arterial disease, stroke, transient ischemic attack, diabetes). May be used as additonal treatment to antihypertensive, antiplatelet or lipid-lowering therapy.

 

Contra-Indications: Biliary obstructive disorders, severe hepatic impairment. Pregnancy (2nd & 3rd trimesters), lactation.

 

Special Precautions: Bilateral renal artery stenosis or stenosis of the artery to a single functioning kidney, vol &/or Na depletion, severe CHF, aortic or mitral valve stenosis, obstructive hypertrophic cardiomyopathy, hepatic insufficiency. Monitor serum K & creatinine in renally impaired patients. Rare hereditary condition of fructose intolerance.

VALSARTAN

Dosage Form: Tablet 80 mg, 160 mg (II)

 

Recommended Dose: Hypertension, usually 80 mg once daily (elderly over 75 years, mild to moderate hepatic impairment, moderate to severe renal impairment, intravascular volume depletion, initially 40 mg once daily); if necessary increased after at least 4 weeks to 160 mg daily. Myocardial infarction, initially 20 mg twice daily increased over several weeks to 160 mg twice daily if tolerated (consider lower dose in mild to moderate hepatic impairment)

 

Indication: Hypertension; myocardial infarction with left ventricular failure or left ventricular systolic dysfunction

 

Contra-Indications: Severe hepatic impairment, cirrhosis, biliary obstruction, breast-feeding

 

Special Precautions: Severely sodium- or volume-depleted patients. No adjustment is required for patients with renal impairment. However, in severe cases (creatinine clearance < 10ml/min) no data are available and therefore caution is advised. Hepatic insufficiency, Valsartan is mostly eliminated unchanged in the bile and patients with biliary obstructive disorders showed lower Valsartan clearance, caution when driving or operating machinery, children, lactation.

 

VALSARTAN + HYDROCHLOROTHIAZIDE

 

Dosage Form: Tablet 80 mg + 12.5 mg, 160 mg + 12.5 mg, 160 mg + 25 mg (II)

 

Recommended Dose: 1 tablet daily. May be taken with or without food.

 

Indications: Treatment of Hypertension.

 

Contra-Indications: Pregnancy, severe hepatic impairment, biliary cirrhosis & cholestasis. Anuria, severe renal impairment. Refractory hypokalaemia, hyponatraemia, hypercalcaemia & symptomatic hyperuricaemia.

 

Special Precautions: Risk of hypotension in Na &/or vol depleted patients, renal artery stenosis, renal & liver disease; disturbance of serum electrolyte balance. Caution when driving or operating machinery. Lactation (avoid).

 

9.8 Inotropic Agents

9.8.1 Cardiac Glycosides (positive inotropic)

DIGOXIN

Dosage Form: Tablet 0.0625 mg, 0.25 mg; Elixir 50 mcg/ml; Injection 500 mcg/2 ml (II)

 

Recommended Dose: Adults and children over 10 yrs: Rapid digitalisation of 1-1.5 mg followed by 0.25 mg every 6 hrs until desired therapeutic effect. Slow oral digitalisation: 0.5-1 mg daily over 1-3 weeks. Emergency parenteral digitalisation: slow IV inj. 0.5-1 mg followed by 0.5 mg after few hours and repeated if necessary. Maintenance (all routes): 0.25-0.75 mg daily in divided doses. Infants and children under 10 yrs: Digitalisation (all routes) 0.020 mg/kg repeated every 6 hrs until desired therapeutic effect. Maintenance 0.010-0.020 mg/kg is given daily foe few days. Geriatrics: Rapid oral digitalisation: 0.5-0.75 mg every 4-6 hrs, maintenance 0.125-0.5 mg daily. OR initial oral/IV loading doses of 10 mcg/kg of LBW followed with maintenance oral doses of 0.125-0.5 mg/day as a single daily dose and adjusted according to desired serum concentrations. Paediatrics: individualised and age-dependent ranging from loading doses of 8-12 mcg/kg/dose to 35-60mcg/kg/dose with maintenance doses calculated as 25% to 35% of the oral loading dose.

 

Indications: Congestive heart failure. Cardiac arrythmias especiallly atrial fibrillation or flutter.

 

Contra-Indications: Toxicity due to cardiac glycosides. In ventricular arrythmias. In patients with Wolff-Parkinson-White Syndrome with atrial fibrillation.

 

Special Precautions: In heart block, severe pulmonary disease, advanced heart failure, acute myocarditis. Patients on cardiac glycosides previously, reduce dosage in impaired renal function, in elderly and in premature infants. Enhance effects in hypokalaemia, hypercalcaemia, hypoxia, hypothyroidism and hypomagnesaemia. Bioavailability of the various dosage forms must be considered when switching to a different preparation. Cardioversion. Amiloid cardiomyopathy.

9.8.2 Sympathomimetics

9.8.2.1 Inotropics

DOBUTAMINE HYDROCHLORIDE

Dosage Form: Injection 250 mg/20 ml (vial) (I)

 

Recommended Dose: By IV infusion: 1.0-10.0 mcg/kg/min adjusted according to response. On rare occasions, infusion rates up to 40 mcg/kg/min have been required.

 

Indications: For inotropic support in the short-term treatment of adults with cardiac decompensation due to depressed contractility resulting from organic heart disease (chronic low-output cardiac failure or acute myocardial failure) or cardiac surgical procedures.

 

Contra-Indications: Idiopathic Hypertropic Subaortic Stenosis (IHSS).

 

Special Precautions: Continuous monitoring of ECG & BP required. Patients with hypertension, myocardial infarction, arteriosclerosis, inotropic effect reversed by concomitant administration of beta-blockers. Patients with atrial fibrillation should be digitalised prior to adminstration of dobutamine. Hypovolaemia should be corrected with suitable volume expanders prior treatment.

DOPAMINE HYDROCHLORIDE

Dosage Form: Injection 40 mg/ml (5 ml ampoule) (II)

 

Recommended Dose: By IV infusion: initially 1-5 mcg/kg/min, gradually increased by 1-4 mcg/kg/min at 10-30 min intervals, up to 20-50 mcg/kg/min. In advanced states of circulatory decompensation, infusion rates of > 50 mcg/kg/min have been used. Paediatric: 0.3-25 mcg/kg/min as a continuous infusion to a maximum of 50 mcg/kg/min.

 

Indications: For correction of haemodynamic imbalances present in the shock syndrome due to myocardial infarction, traumas, endotoxic septicaemia, open heart surgery, renal failure and chronic cardiac decompensation, when patients do not respond to plasma volume expansion.

 

Contra-Indications: Pheochromocytoma or uncorrected tachyarrythmias or ventricular fibrillation.

 

Special Precautions: Hypovolaemia should be corrected prior to treatment. Use with caution in patients with ischemic heart disease. Low dose in shock due to acute myocardial infarction. When dose > 50 mg/kg/min are employed, urine output should be measured frequently. Avoid extravasation of drug. MAO inhibitors. Angina. Peripheral vascular disorders (dopamine can produce peripheral gangrene).

Vasoconstrictor

EPHEDRINE

Dosage Form: Injection 30 mg/ml (II)

 

Recommended Dose: IM, SC or IV Severe, acute bronchospasm 12.5-25 mg. When used as a pressor agent Adult 25-50 mg SC/IM. If necessary, a 2nd IM dose of 50 mg or an IV dose of 25 mg may be given. Direct IV inj, 10-25 mg may be given slowly. Max parenteral adult dose: 150 mg in 24 hr. Childn 3 mg/kg or 100 mg/m2 SC or IV daily, in 4-6 divided doses.

 

Indications: Treatment of bronchial spasm in asthma & to produce cardiac stimulation & vasoconstriction in the treatment of shock. Adjunct to correct haemodynamic imbalances which persist after adequate fluid vol replacement. Treat hypotension during spinal anaesth.

 

Contra-Indications: Closed-angle glaucoma. Patients being treated w/ MAOIs or w/in 10 days of ceasing such treatment. Coronary thrombosis, HTN & hyperthyroidism.

 

Special Precautions: Geriatric males (esp those w/ an enlarged prostate), diabetics, & patients w/ CV disease. Patients receiving chloroform, cyclopropane, halothane or other halogenated anaesth.

NORADRENALINE (NOREPINEPHRINE) BITARTRATE

Dosage Form: Injection 4 mg/4 ml amp (I)

 

Recommended Dose: Acute hypotension, by IV infusion, via central venous catheter, of a solution containing norepinephrine acid tartrate 80mcg/ml (equivalent to norepinephrine base 40 mcg/ml) at a intial rate of 0.16-0.33ml/minute, adjusted according to response.

 

Indications: Acute hypotension

 

Contra-Indications: Pregnancy, hypertension

Special Precautions: Coronary, mesenteric, or peripheral vascular thrombosis; following myocardial infarction, Prinzmetal’s variant angina, thyroid disease, diabetes mellitus; hypoxia or hypercapnia; appropriate blood volume replacement required; elderly; extravasation at injection site may cause necrosis.

PHENYLEPHRINE HCL

Dosage Form: Injection 1% (10 mg/ml) (I*- ICL & OT Cardiology)

 

Recommended Dose: SUBCUTANEOUSLY OR INTRAMUSCULAR: Usual dose, from 2mg to 5 mg. Range, from 1mg to 10mg. Initial dose should not exceed 5mg. INTRAVENOUSLY: Usual dose, 0.2mg. Range, from 0.1mg to 0.5mg. Initial dose should not exceed 0.5 mg. Injections should not be repeated more often than every 10 to 15 minutes. A 5 mg intramuscular dose should raise blood pressure for one to two hours. A 0.5 mg intravenously dose should elevate the blood pressure for about 15 minutes.

 

Indications: For the maintenance of an adequate level of blood pressure during spinal and inhalation anesthesia. For the treatment of vascular failure in shock, shock–like states and drug induced hypertension or hypersensitivity. To overcome paroxysmal supraventricular tachycardia, to prolong spinal anesthesia and as a vasoconstrictor in regional analgesia.

 

Contra-Indications: Should not be used in patients with severe hypertension, ventricular tachycardia or in patients who are hypersensitivity to it or to any of the components.

 

Special Precautions: Phenylephrine hydrochloride should be employed only with extreme caution in elderly patients or in patients with hyperthyroidism, bradycardia, partial heart block, myocardial disease or severe arteriosclerosis.

9.8.2.3 Cardiopulmonary Resuscitation

ADRENALINE ACID (EPINEPHRINE) TARTRATE

Dosage Form: Injection 1 mg/ml (1 ml ampoule) (II)

 

Recommended Dose: By SC, IM: 0.5-1 ml of 1 in 1000 solution diluted to 10 ml or 5-10 ml of 1 in 10000 solution every 5 min. By intracardiac 1-2 mg per 10 ml. By IV, 0.1-0.25 mg given slowly and repeat 5-15 min if necessary.

 

Indications: In cardiac resuscitation procedures.

 

Contra-Indications: In narrow angle glaucoma. Shock (other than anaphylactic shock), organic heart disease, organic brain damage or cerebral arterio sclerosis.

 

Special Precautions: Diabetes, cardiovascular disease, geriatric patients, hyperthyroidism. Avoid IV use with tricyclic antidepressant digoxin or quinidine because of the risk of arrythmia.

ISOPRENALINE HYDROCHLORIDE

Dosage Form: Injection 1 mg/5 ml ampoule (I)

 

Recommended Dose: For shock: By IV infusion: 0.5-5 mcg/min (0.25-2.5 ml diluted solution 1:500000) up to 30 mcg/min if necessary. For management of broncospasm during anaesthesia by IV inj. 0.01-0.02 mg (0.5-1 ml diluted solution 1:50000) repeated when necessary. For cardiac standstill/arrythmias: By IV inj: 0.02-0.06 mg (1-3 ml of diluted solution 1:50000) IV infusion 5 mcg/min (1.25 ml) of diluted solution 1:250000. By IM: 0.02-1 mg, SC: 0.15-0.2 mg.

 

Indications: Adjunct in management of shock treatment of cardiac standstill or arrest, carotid sinus-stokes, ventricular tachycardia and arrythmias. Management of bronchospasm, cardiac arrythmias.

 

Contra-Indications: Preexisting cardiac arrythmias and tachycardia caused by digitalis intoxication. Concurrent administration with halogenated anaesthesia.

 

Special Precautions: Never give simultaneously with adrenaline, but may be used alternately. Correct hypovolaemia prior to or during treatment. Monitor carefully patients in shock. Use with caution in el inhibitors. Angina. Peripheral vascular disorders (dopamine can produce peripheral gangrene).

 

9.9 Hypolipidaemic Products

ATORVASTATIN

Dosage Form: Tablet 10 mg, 20 mg (I)

 

Recommended Dose: Initially 10 mg once daily. Dose range: 10-80 mg once daily.

 

Indications: Reduction of elevated total & LDL cholesterol, apolipoprotein B & triglycerides in patients with primary hypercholesterolaemia, mixed hyperlipidaemia, heterozygous & homozygous familial hypercholesterolaemia.

 

Contra-Indications: Active liver disease or elevated serum transaminases > 3 times the upper limit of normal. Pregnancy & lactation.

 

Special Precautions: Monitor of creatine phosphokinase  & transaminase elevations. Avoid alcohol consumption.Patients should be advised to report unexplained muscle pain.

CHOLESTYRAMINE

osage Form: Anhydrous powder 4g/sachet (I)

 

Recommended Dose: 4g tds-qid, to be mixed with 2-6 ounces of water or other fluids, up to 36 g daily in some cases. Child over 6 yrs: 80 mg/kg tds.

 

Indications: Hypercholesterolaemia, pruritus associated with partial biliary obstruction, intractable infantile diarrhoeas and those that are due to bile acid malabsorption.

 

Contra-Indications: Complete biliary obstruction, pregnancy, hyperlipoproteinaemia types III, IV or V

 

Special Precautions: Other drugs should be taken one hour before or 4 hrs after administration of cholestyramine. Give Vit. A, D and K supplements on prolonged therapy. Should not be taken in its dry form.

EZETIMIBE

Dosage Form: Tablet 10 mg (II)

 

Criteria of use: Follow malaysian lipid clinical practice guidelines and previously on maximum dose of statins

 

Recommended Dose: 10 mg once daily, used alone or w/ a statin. When co-administered w/ a statin, the dosage instructions for that particular statin should be consulted.

 

Indications: Administered alone or w/ an HMG-CoA reductase inhibitor (statin) indicated as adjunctive therapy to diet in patients w/ primary (heterozygous familial & non-familial) hypercholesterolemia. Administered w/ a statin for patients w/ homozygous familial hypercholesterolemia. Patients may also receive adjunctive treatments (eg, LDL apheresis). Reduction of elevated sitosterol & campesterol levels in patients w/ homozygous familial sitosterolemia.

 

Contra-Indications: Hypersensitivity. Combination w/ an HMG-CoA reductase inhibitor is contraindicated in patients w/ active liver disease or unexplained persistent elevations in serum transaminases.

 

Special Precautions: When co-administered w/ a statin, perform liver function tests at baseline & according to the recommendations of the statin. Not recommended for moderate  or severe liver dys

function. Co-administration w/ fibrates not recommended. Caution when initiating Ezetrol in the setting of cyclosporine. Monitor cyclosporine conc. Pregnancy, lactation. Not recommended for childn <10 yr.

FENOFIBRATE

Dosage Form: Capsule Supra 160 mg (I* - Medical)

 

Recommended Dose: 1 capsule once daily.

 

Indications: Hyperlipidaemia types IIa, IIb, III and IV.

 

Contra-Indications: Impaired renal and hepatic function, pre-existing gall bladder disease, pregnant and lactating women.

 

Special Precautions: Reduce the dosage of any concurrent administered anti-coagulants approximately 1/3 and the prothrombin time should be monitored closely.

GEMFIBROZIL

Dosage Form: Capsule 300 mg (I)

 

Recommended Dose: 0.8-1.2 g daily in two divided doses, before morning and evening meals.

 

Indications: Hyperlipidaemia types II and IV.

 

Contra-Indications: Impaired renal and hepatic function, biliary cirrhosis, pre-existing gall bladder disease.

 

Special Precautions: Reduce the dosage of any concurrent administered anti-coagulants, diabetes, hypothyroidism.

LOVASTATIN

Dosage Form: Tablet 20 mg, 40 mg (I)

 

Recommended Dose: Initially 20 mg once daily. Adjust at 4-wk intervals up to 80 mg daily.

 

Indications: Reduction of total & LDL cholesterol in patients w/ primary hypercholesterolaemia (type IIa & IIb) when response to diet alone has been inadequate.

 

Contra-Indications: Active liver disease or unexplained persistent elevation or serum transaminases. Pregnancy & lactation.

 

Special Precautions: Persistent elevation of serum transaminases up to 3 times the normal values (discontinue). Perform baseline & periodic liver function tests; & baseline serum creatine kinase levels. Chronic or substantial alcohol consumption or history of liver disease. Women of childbearing potential.

PRAVASTATIN

Dosage Form: Tablet 20 mg (I)

 

Recommended Dose: 10-40 mg administered once a day at bedtime.

 

Indications: Patients with primary hypercholesterolaemia, intolerant or non-responsive to other forms of therapy.

 

Special Precautions: Pregnancy, not recommended for patients < 18 years old.

SIMVASTATIN

Dosage Form: Tablet 10 mg, 20 mg, 40 mg (I*- Physician)

 

Recommended Dose: Hypercholesterolemia; starting dose 10 mg/day in the evening. Max 40 mg/day. Adjust at 4 week intervals as required. Mild to moderate hypercholesterolemia; initiate with 5mg/day. CHD; start 20 mg/day in the evening. Adjust at 4 week intervals as required. Max: 40 mg/day.Patient taking immunosuppressives and in severe renal insufficiency (CrCl<30mL/mins) Max: 10 mg/day.

Indication: Hypercholesterolemia, CHD.

 

Contra-Indications: Active liver disease or unexplained persistent elevation of serum transaminase, pregnancy,lactation and hypersensitivity.

 

Special Precautions: Elevations of serum transaminase.If the transaminase level rise persistently to 3 times the upper limit of normal, discontinue drug. Recommed that liver function tests be performed before treatment begins and periodically thereafter. Caution in patients who consume substantial quantities of alcohol and/or have a history of liver disease. If muscle symptoms and/or marked elevation of CPK level occur, discontinue drug. Women of childbearing age.  

 

9.10 Haematological Products

9.10.1 Anticoagulants, Anti Thrombotic And Clotting Agents

ACETYLSALICYLIC ACID

Dosage Form: Tablet 300 mg (II); Low Dose Preparation 100 mg,100 mg + 45 mg glycine (I)

 

Recommended Dose: A single dose of 150-300 mg given as soon as possible after an ischaemic event. Maintenance dose 75 mg daily. Adult 1 tab daily.

 

Indications: Prophylaxis of cerebrovascular disease or myocardial infarction.

 

Contra-Indications: Haemophiliac, intolerance to aspirin, peptic ulcer or dyspepsia. Concomitant use with Probenecid or other uricosuric agent, bleeding ulcers, haemorrhage state, anaemia, compromised cardiac funtion, hypoprothrombinaemia or Vitamin K deficiency.

 

Special Precautions: In patients prone to dyspepsia, impaired renal or hepatic function, dehydration, bronchial asthma, patients on anticoagulants or hypoglycaemic agents. Not recommended for infants under one year of age. Pregnancy, lactation, allergis diseases, G6PD deficiency.

CLOPIDOGREL

Dosage Form: Tablet 75 mg (I)

 

Recommended Dose: 75 mg once daily with or without food. No adjustment is necessary for elderly patients or patients with renal disease.

 

Indications: Reduction of atherosclerotic events (myocardial infarction, stroke and vascular death)

 

Contra-Indications: Hypersensitivity to clopidogrel or any components of it’s. Active pathological bleeding eg: peptic ulcer or hemorrhage

 

Special Precautions: Should be use in precaution in patients who may be at risk of increased bleeding from trauma, surgery or other pathological conditions.  

DIPYRIDAMOLE

Dosage Form: Tablet 25 mg, 75 mg (II)

 

Recommended Dose: For thromboembolism: 100 mg tds-qid before food, increased to 600 mg daily if required. For angina, 50 mg tds. Prevention of stroke: 75 mg tds combined with aspirin.

 

Indications: Thromboembolism, angina, prevention of stroke (combined with aspirin).

 

Contra-Indications: In hypotension following myocardial infarction. Hypersensitivity.

 

Special Precautions: In patients with hypotension. Use during percutaneous transluminal coronary

DROTRECOGIN ALFA (ACTIVATED)

Dosage Form: Injection 5 mg/vial (activated) (I)

 

Criteria of use: Restricted to ICU patients for severe sepsis

 

Recommended Dose: Severe sepsis: 24 mcg/kg/hr IV for 96 hours.

 

Indications: Adjunctive treatment of Severe sepsis with multiple organ failure.

 

Contra-Indications: Internal bleeding, haemorrhagic stroke (recent 3 months), intracranial or intraspinal surgery or severe head trauma (recent 2 months), intracranial neoplasma/lesion/cerebral herniation, existing epidural catheter, trauma with life-threatening bleeding, chronic severe hepatic diseases, thrombocytopenia.

 

Special Precautions: Patients at risk of bleeding (eg, chronic liver disease, history of organ transplantation, chronic renal failure requiring dialysis, thrombocytopenia (less than 30,000/mm (3), history of recent stroke or recent GI ulceration, recent head or other trauma, known bleeding diathesis or a prothrombin time-INR greater than 3.0) (potential for bleeding). Patients with hypercoagulable conditions (eg, hereditary deficiencies of protein C, protein S, or antithrombin III ; suspected thromboembolism; presence of anticardiolipin antibody; resistance to activated protein C). Concurrent or recent use (within 7 days) of aspirin (greater than 650 mg/day), other antiplatelet agents, warfarin, or glycoprotein IIb/IIIa inhibitors; antithrombin III; thrombolytic agents (within 3 days); or heparin (therapeutic dose. Prior sensitivity or other unexpected untoward effects associated with use of other protein C/activated protein C formulations. Recent ischaemic stroke (within 3 months) or intracranial arteriovenous malformation or aneurysm. Pregnancy and breast-feeding.

ENOXAPARIN SODIUM

Dosage Form: Injection 20 mg/0.2 ml, 40 mg/0.4 ml, 60 mg/0.6 ml (prefilled syringe) (II)

 

Recommended Dose: For Infant > 2 months and children < 18 years: prophylaxis; Initial: 0.5 mg/kg every 12 hours, treatment; Initial: 1 mg/kg every 12 hours. 1. Prophylaxis of deep-vein thrombosis in surgical patients (s.c): 1. Moderate risk: 20 mg (2000 units) approx. 2 hours before surgery then 20 mg every 24 hours for 7-10 days. 2. High risk: 40 mg (4000 units) 12 hours before surgery then 40 mg for 7-10 days.  2. Prophylaxis of deep-vein thrombosis in medical patients (s.c): 40 mg (4000 units) every 24 hours for at least 6 days until patients ambulant (max, 14 days). 3.Treatment of deep-vein thrombosis (with or without pulmonary embolism):s.c: 1.5 mg/kg (150 units/kg) every 24 hours, for at least 5 days. 4. Unstable angina and non-Q-wave myocardial infarction, s.c: 1mg/kg (100 units/kg) every 12 hours for 2-8 days (min: 2 days).  

 

Indications: 1. Prevention of deep-vein thrombosis following hip or knee replacement surgery or abdominal surgery in patients at risk for thromboembolic complications. 2. Prevention of deep-vein thrombosis in medical patients at risk thromboembolic complications due to severely restricted mobility during acute illness. 3. Outpatients and inpatients treatment of acute deep-vein thrombosis without pulmonary embolism when administered in conjunction with warfarin sodium. 4. Prevention of ischemic complications of unstable angina and non-Q-wave myocardial infarction (when administered with aspirin).

 

Contra-Indications: Patients with active major bleeding, thrombocytopenia associated with a positive in vitro test for antiplatelet antibody or enoxaparin – induced platelet aggregation hypersensitivity to enoxaparin; known hypersensitivity to heparin or pork product.

 

Special Precautions: Do not administered intramuscularly, in patients with a history of heparin-induced thrombocytopenia, bacterial endocarditis, haemorrhagic stroke, recent CNS or ophtalmological surgery, bleeding diathesis, uncontrolled arterial hypertension, or a history of recent gastrointestinal ulceration and hemorrhage. Elderly and patients with renal insufficiency may show delayed elimination of enoxaparin, avoid use in lactation.

FACTOR IX COMPLEX

Dosage Form: Injection 550 iu/vial (I)

 

Recommended Dose: Initially 15-75 IU/kg every 6-24 hrs depending on half-life; to raise the concentration of factor IX to 15-39% in moderate bleeding and >50% in surgery.

 

Indications: Haemophilia B, reversal of coumarin-induced haemorrhage, bleeding episodes in haemophilia A.

 

Contra-Indications: Disseminated intravascular coagulation without prior treatment with heparin.

 

Special Precautions: Liver disease, high risk carrier of Hepatitis B. Do not administer with aminocaproic acid

FACTOR VIIa (RECOMBINANT)

Dosage Form: Injection 60 KIU (1.2 mg/vial) (I* - Neuroscience)

 

Criteria of use:

1. For intracerebral hematoma salvageable cases, less than 70 years, GCS more than 6/15, pupils not fixed and dilated, controlled at least 15 minutes apart.

2. For 15 patients per year

 

Recommended Dose: Initially 4.5 KIU (90 mcg)/ kg body wt IV bolus over 2-5 mins, followed by 3-6 KIU (60-120 mcg)/ kg body wt depending on type & severity of haemorrhage or surgery performed. Dosing interval: initially 2-3 hr to obtain haemostasis & until clinically improved.If continued therapy is needed, dose interval can be increased successively to every 4, 6, 8 or 12 hr.

 

Indications: Treatment of bleeding episodes & prevention of excessive bleeding associated w/ surgery in patients w/ inherited or acquired haemophilia w/ inhibitors to coagulation factors VIII or IX.

Contra-Indications: Hypersensitivity to murine or bovine protein.

 

Special Precautions: Advanced atherosclerotic disease, crush injury, septicaemia. Pregnancy & lactation.

FACTOR VIII [Anti-Haemophilic Factor]

Dosage Form: Injection 250 iu/vial, High purity (I)

 

Recommended Dose: According to individual needs.

 

Indications: Classical haemophilia A.

 

Special Precautions: Particularly in persons with previous transfusion of blood and plasma products, possibility of contacting viral hepatitis must be considered.

FONDAPARINUX SODIUM

Dosage Form: Injection 2.5 mg/0.5 ml (prefilled syringe) (I)

 

Criteria of use: For Post-op orthopedic patients, and management of patients with unstable angina/non-ST segment elevation myocardial infarction (UA/NSTEMI) and ST segment elevation myocardial infarction (STEMI)

 

Recommended Dose: 2.5 mg SC once daily administered 6 hr following surgical closure provided haemostasis has been established. Treat for 5-9 days. Non-ST segment elevation myocardial infarction, acute 2.5 milligrams (mg) daily subcutaneously for up to 8 days. Acute ST segment elevation myocardial infarction: initial 2.5 mg IV, followed by 2.5 mg subcutaneously once daily for the duration of hospitalization, up to 8 days.

 

Indications: Prevention of venous thromboembolic events (VTE) in patients undergoing major orthopaedic surgery of the lower limbs eg hip fracture, major knee surgery or hip replacement surgery.

 

Additional indications (refer P&T 66, 28 November 2008): Treatment of unstable angina or non-ST segment elevation myocardial infarction (UA/NSTEMI) in patients for whom urgent (120 mins) invasive management (PCI) is not indicated. Treatment of ST segment

elevation myocardial infarction (STEMI) in patients who are managed with thrombolytics or who initially are to receive no other form of reperfusion therapy.

 

Contra-Indications: Active clinically significant bleeding, acute bacterial endocarditis, severe renal impairment (CrCl <30 mL/min), body wt <50 kg.

 

Special Precautions: Increased haemorrhagic risk eg congenital or acquired coagulopathy, active ulcerative GI disease, recent intracranial haemorrhage or shortly after brain, spinal or ophth surgery, diabetic retinopathy, uncontrolled arterial HTN, moderate renal impairment (CrCl <30-50 mL/min), severe hepatic impairment. Measure platelet counts at baseline & end of treatment. Elderly. Pregnancy & lactation. Avoid concurrent administration w/ drugs that may increase haemorrhagic risk.

HEPARIN SODIUM

Dosage Form: Injection 1000 units/ml, 5000 units/ml vial (II)

 

Recommended Dose: By IV inj.: 5000U initially, then 5000-10000U every 4-6 hrs. Maintenance: 6000-12000U. IV infusion: 10000-20000U in dextrose saline over 12 hrs. By SC inj: 5000U before surgery, then every 12 hrs until patient is ambulant. Child: Initially 50U/kg by infusion followed by 100U/kg or 25U/kg/h every 4 hrs according to clotting time.

 

Indications: Prevention of post operative thrombosis, disseminated intra vascular coagulation, venous pulmonary thrombosis, deep vein thrombosis, or in maintaining catheter patency.

 

Contra-Indications: Haemophilia and other haemorrhagic disorders, peptic ulcer, threathened abortion, recent surgery, severe renal or hepatic disease, severe hypertension.

 

Special Precautions: Concomitant administration of oral anticoagulants such as aspirin and dipyridamole which affect platelet function. IM inj: risk of haematoma formation. Allergies, renal or hepatic disease, hypertension during menstruation, indwelling catheters, long-term SC use in pregnant women.

NADROPARIN CALCIUM

Dosage Form: Injection 7500 Axa ICU x 0.3 ml (I*)

 

Recommended Dose: Prophylaxis; general surgery: 7500 Axa ICU daily, 1st inj 2-4 hr before surgery (general anaesth): 100 Axa ICU kg/day for 3 days starting 12 hr before surgery, then 150 AXaICU/kg/day from 4th  post-po day onwards. Duration of prophylactic administration shoul be at least 10 days. Treatment;0.1mL/10kg body wt SC bd.

 

Indications: Prophylaxis & treatment of thromboembolic disorders.

 

Contra-Indications: Previous thrombocytopenia with nadroparin therapy, signs or increased risk of hemorrhage associated with hemostasis disorders except for disseminated intravascular coagulation not in hemorrhagic CVA, acute infective endocarditis.

 

Special Precautions: Hepatic or renal insufficiency, uncontrolled arterial hypertension, histoy of peptic ulceration, vascular chorioretinal disorder; post-op brain, spinal cord or eye surgery.

PROTAMINE SULPHATE

Dosage Form: Injection 1% (50 mg/5ml) (II)

 

Recommended Dose: By slow IV inj: 1 mg neutralises 100U of heparin at rate of 0.5 ml/min. Max dose: 50 mg (5 ml) over period of 10-15 min.

 

Indications: Heparin antagonist.

 

Contra-Indications: Not suitable for reversing the effect of oral anticoagulants. Intolerance to the drug.

 

Special Precautions: Overdose of protamine sulphate has an anticoagulant effect. Anaphylaxis in patients previously exposed to protamine through use of protamine containing insulins or during heparin neutralization.

TICLOPIDINE HYDROCHLORIDE

Dosage Form: Tablet 250 mg (I* - Physician)

 

Recommended Dose: 1 or 2 tablets daily during meals. Coronary artery bypass graft 250 mg orally BD. Placement stents in coronary artery in combination with aspirin  250 mg orally bd for 30 days. Thromboembolic stroke, prophylaxis 250 mg orally bd.

 

Indications: Maintenance of potency of coronary bypass grafts. Maintenance of patency of access sites in patients on chronic haemodialysis. Reducing risk of thrombotic stroke (fatal or non fatal) in patients who have experienced stroke precursors & in patients who have had a completed stroke.

 

Contra-Indications: Haemopathies & hemorrhagic diathesis where bleeding time is prolonged. Organic lesions with a tendency to bleed. History of leukopenia, thrombocytopenia & agranulocytosis.

 

Special Precautions: Avoid concomitant use of anticoagulant or aspirin in the absence of monitoring of laboratory parameters. Bleeding; hematoma. In the event of fever, sore throat or buccal ulceration, discontinue therapy.

TIROFIBAN HYDROCHLORIDE

Dosage Form: Injection 0.25 mg/ml (I* - Medical)

 

Criteria of use: Restricted to PM Zurkurnai for unstable angina/ NSTEMI post ‘percutaneous coronary intervention’.

 

Recommended Dose: 0.4 mcg/kg/min IV for 30 min then 0.1 mcg/kg/min for 12-24 hr after angioplasty/atherectomy

 

Indications: Acute coronary syndrome in patient undergoing angioplasty/atherectomy or managed medically

 

Contra-Indications: Aortic dissection, bleeding, major surgery, trauma, stroke within 30 days, concomitant use of another parenteral GPIIb/IIIa inhibitor, hemorrhagic stroke, history of intracranial hemorrhage, neoplasm, arteriovenous malformation, or aneurysm, hypersensitivity to tirofiban or other product components, pericarditis, severe hypertension (systolic BP greater than 180 mmHg and/or diastolic BP greater than 110 mmHg), thrombocytopenia following prior tirofiban administration

 

Special Precautions: Avoid unnecessary vascular and other trauma, concomitant use with thrombolytic agents (no data available) or drugs that affect hemostasis, discontinue tirofiban and heparin therapy if thrombocytopenia is confirmed, hemorrhagic retinopathy, in angioplasty or atherectomy (do not remove catheter sheath from femoral access site until 3-4 hr after discontinuation of heparin and until after documentation of activated clotting time (ACT) of less than 180 seconds and activated partial thromboplastin time (aPTT) of less than 45 seconds), platelet count below 150,000/mm(3), severe renal insufficiency, chronic hemodialysis.

TRANEXAMIC ACID

Dosage Form: Capsule 250 mg (II), Injection 100 mg/ ml, 5% (II)

 

Recommended Dose: Oral: 250 mg-1 g tds or qid. Slow IV: 1 g tds or 1-2 doses IM. By mouth, local fibrinolysis, 15-25 mg 2-3 times daily.

 

Indications: Prevention and treatment of haemorrhages due to fibrinolysis.

 

Contra-Indications: Intravascular coagulation, arterial or venous thrombosis, or surgery.

 

Special Precautions: Reduce dose in patients with renal impairment

VITAMIN K

Dosage Form: Injection 1 mg/ml, 10 mg/ml (as Phytomenadione) - (II)

 

Recommended Dose: 2.5-25 mg (exceptionally 50 mg) by IM/SC inj, repeated after 6-8 hrs if necessary. Severe bleeding: 10-20 mg by rate not exceeding 1 mg/min, followed by prothrombin level 3 hrs later. Not more than 40 mg should be given IV in 24 hrs. Haemorrhagic disease in newborn: 1 mg IM, if necessary further doses may be given 8 hourly, 2-10 mg for prothrombin deficiencies. Prophylaxis: 0.5-1 mg IM or may be given to the mother in dose of 1-5 mg by IM inj 12-24 hrs before delivery.

 

Indications: Haemorrhagic caused by anticoagulant therapy, hypoprothrombinaemia, prevention of neonatal haemorrhage.

 

Contra-Indications: Hypersensitivity to drug.

 

Special Precautions: IV inj should be given slowly and only when absolutely necessary. Not effective in overdosage with heparin.

WARFARIN SODIUM

Dosage Form: Tab 1 mg, 2 mg, 3 mg, 5 mg (II)

 

Recommended Dose: Initially 10-15mg daily. Maintenance 3-10 mg daily (determine prothrombin time: maintain prothrombin time at 1.2-2 times control).

 

Indications: Deep vein thrombosis, pulmonary embolism, transient ischemic attacks, thrombosis associated with prosthetic heart valves, or after cardiac bypass surgery.

 

Contra-Indications: Threatened abortion, pregnancy, ulcerative disorders, haemophilia, immediately after parturition or surgery, hepatic disorders, cerebrovascular accident, trauma, malignant hypertension, retinopathy, recent lumbar block anaesthesia, arterial aneurysm, infective endocarditis or acute pericarditis, thrombocytopenia.

 

Special Precautions: Impaired hepatic and renal function, severe hypertension, any condition where there is a risk of serious haemorrhage. Elderly females (>60 yrs).

9.10.2 Fibrinolytic Agents

ALTEPLASE (RECOMBINANT TISSUE PLASMINOGEN ACTIVATOR) (rtPA)

 

Dosage Form: Injection 50 mg/vial (I*)

 

Recommended Dose: Myocardial infarction, accelerated regimen (initiated within 6 hours), 15 mg by intravenous injection, followed by intravenous infusion of 50 mg over 30 minutes, then 35 mg over 60 minutes (total dose 100 mg over 90 minutes); lower doses in patients <65 kg. Myocardial infarction, initiated within 6-12 hours, 10 mg by intravenous injection followed by intravenous infusion of 50 mg over 60 minutes, then 4 infusions each of 10 mg over 30 minutes (total dose 100 mg over 3 hours; max. 1.5 mg/kg in patient <65 kg). Pulmonary embolism, 10 mg by intravenous infusion over 1-2 minutes followed by intravenous infusion of 90 mg over 2 hours; max. 1.5 mg/kg in patient <65 kg.

 

Indications: Acute myocardial infarction; pulmonary embolism

 

Contra-Indications: No central venous puncture (CVP line) or noncompressible arterial sticks. BP systolic 185, diastolic 110 unresponsive to nitrate or calcium antagonist; recent (within 1 month): cerebrovascular accident, gastrointestinal bleeding, trauma or surgery, prolonged external cardiac massage; intracranial neoplasm, suspected aortic dissection, arteriovenous malformation or aneurysm, bleeding diathesis, hemostatic defects, seizure occurring at the time of stroke, suspicion of subarachnoid hemorrhage.

 

Special Precautions: Bolus administration (increased risk of intracranial hemorrhage), recent major surgery (within 10 days), cerebrovascular diseases, recent gastrointestinal or genitourinary bleeding, recent trauma (within 10 days), hypertension (systolic BP greater than 180 mm Hg or diastolic BP greater than 110 mm Hg), acute pericarditis, subacute bacterial endocarditis, significant liver dysfunction, hemorrhagic ophthalmic conditions, septic thromphlebitis, advanced age (older than age 75), patients currently receiving oral anticoagulants , active menstrual bleeding.

STREPTOKINASE

Dosage Form: Injection 1,500,000 units (I)

 

Recommended Dose: IV infusion: 250000U over 30 min. Then 100000U every hour for up to 24-72 hrs according to condition. Myocardial infarction: 1500000U over 60 min, followed by aspirin 150 mg daily orally for at least 4 weeks. Intracoronary infusion: bolus of 200000U followed by infusion of 2000U/min for 60 minutes. Paediatric: IV infusion: bolus of 1000U-5000U/kg followed by 400-1200U/kg/h.

 

Indications: Fibrinolytic agent in thromboembolic disorders such as acute massive pulmonary embolism, arterial and venous occlusion, acute myocardial infarction, arterial and deep vein thrombosis.

 

Contra-Indications: Recent haemorrhage surgery, severe trauma, liver or kidney damage, coagulation defect, history of cerebrovasccular disease, recent streptococcal infection, or streptokinase therapy (>5 days & < 3 months previously), severe hypertension, arteriosclerosis, pulmonary disease with cavitation, severe bronchitis, acute pancreatitis, severe diabetes, pregnancy, potential GI or genito-urinary bleeding, active internal bleeding, recent CVA (within 2 months), intracranial/intraspinal surgery, intracranial neoplasm, severe hypertension, predisposition to bleeding, surgery or biopsy within 10 days.

 

Special Precautions: Mitral valve defects or atrial fibrillation, recent or concurrent anticoagulant/antiplatelet thaerapy. If streptokinase resistance is determined and resistance level exceeds 1 million IU, the drug should not be given. Invasive arterial/venous procedures, spontaneous bleeding, allergy/anaphylaxis.

9.10.3 Iron And Haematopoetic Agents

Refer Section 7.5

CYANOCOBALAMIN [Vitamin B12]

Dosage Form: Injection 1 mg/ml (1 ml, 10 ml) (II)

 

Recommended Dose: By IM inj.: 250-1000mcg on alternate days for 1-2 weeks, followed by 250mcg weekly until blood count is normal. Then maintain dose of 1000mcg monthly. Pernicious anaemia: 300mcg daily.

 

Indications: Pernicious anaemia, macrocytic anaemia, vitamin B12 deficiency.

 

Contra-Indications: Cyanocobalamin is not a suitable form of Vit. B12 for the treatment of optic neuropathies associated with raised plasma concentration of cyanocobalamin.

 

Special Precautions: Should not be given before diagnosis is fully established. Oral therapy is markedly inferior to parenteral therapy and should be used only in treatment of Vit. B12 deficiency with normal GI absorption.

FERRIC AMMONIUM CITRATE

Dosage Form: Mixture [P] 400 mg/5 ml (Padiatric) (II)

 

Recommended Dose: Up to 6g daily taken well diluted with water.

 

Indications: Treatment of iron deficiency anaemia.

 

Contra-Indications: In patients receiving repeated blood transfusion, anaemia not due to iron deficiency.

 

Special Precautions: Tetracyclines. Use straw to prevent discoloration of teeth. Care in patients with iron storage or iron-absorption diseases, haemoglobinopathies or existing disease.

FERROUS FUMARATE

Dosage Form: Tablet 200 mg (II)

 

Recommended Dose: Initially: 200 mg tds. Maintenance: 200 mg daily. Child: up to 1 yr: 35 mg tds., 1-5 yrs: 70 mg tds., 6-12 yrs: 140 mg tds.

 

Indications: Treatment of iron deficiency anaemia.

 

Contra-Indications: In patients receiving repeated blood transfusions or in anaemia not due to iron deficiency. Peptic ulcer, regional enteritis and ulcerative colitis.

 

Special Precautions: Concomitant administration of tetracycline and antacids decrease amount of iron absorbed.

FOLIC ACID

Dosage Form: Tablet 5 mg (II)

 

Recommended Dose: Initially 10-20 mg daily for 14 days. Maintenance: 2.5-10 mg daily. Prophylaxis of megaloblastic anaemia of pregnancy: 200-500 mcg daily.

 

Indications: Treatment of megaloblastic anaemia, anaemia of sprue, pregnancy and pellagra.

 

Contra-Indications: Megaloblastic anaemia secondary to Vit. B12 deficiency.

 

Special Precautions: Should not be given before diagnosis is fully established. Large continuous doses of folic acid may lower the blood concentration of Vit. B12.

IRON SUCROSE

Dosage Form: Injection 100 mg (I)

 

 Recommended Dose: By slow intravenous injection or by intravenous infusion, calculated according to body-weight and iron deficit, consult product literature; child not recommended

 

 Indications: iron-deficiency anaemia

 

Contra-Indications: history of allergic disorders including asthma, eczema and anaphylaxis; liver disease; infection

 

Special Precautions: oral iron therapy should not be given until 5 days after last injection; facilities for cardiopulmonary resuscitation must be at hand; pregnancy

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