Anapril, after hydrolysis to enalaprilate, inhibits Angiotensin Converting Enzyme (ACE). ACE is a peptidyl dipeptidase that catalyses the conversion of angiotensin I to the vasoconstrictor substance angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex. The beneficial effects of enalapril in hypertension and heart failure appear to result primarily from suppression of the renin-angiotensin aldosterone system
Anapril is used for-
- All grades of essential hypertension and renovascular hypertension either alone or in combination with other antihypertensive agents especially thiazide diuretics.
- Prevention of symptomatic heart failure.
- Treatment of congestive heart failure (adjunct), usually in combination with diuretics and digitalis.
- Prevention of coronary ischaemic events in patients with left ventricular dysfunction.
Anapril is also used either alone or as an adjunct in the treatment of angina, diabetic nephropathy and Raynaud's disease.
Anapril is also used to associated treatment for these conditions: Diabetic Nephropathy, High Blood Pressure (Hypertension), Symptomatic Congestive Heart Failure, Asymptomatic Left ventricular dysfunction
|Other Names||ánalapril, Enalapril, Enalaprila, Enalaprilum|
|Weight||5mg, 10mg, 20mg|
It is reported that less than 50% of enalaprilat is bound to human plasma proteins, based on limited data from binding studies of enalaprilat in human plasma both by equilibrium dialysis and by ultrafiltration.
|Therapeutic Class||Angiotensin-converting enzyme (ACE) inhibitors|
|Manufacturer||Eskayef Bangladesh Ltd|
|Last Updated:||June 23, 2021 at 11:20 am|
Table Of contents
Hypertension: Initially 5 mg once daily if used alone or 2.5 mg daily if used in addition to diuretic, in elderly patients or in patients with renal impairment. Usual maintenance dose is 10-20 mg once daily. However, in severe hypertension it may be increased to a maximum of 40 mg once daily.
Heart failure (adjunct) and asymptomatic left ventricular dysfunction: Initially 2.5 mg under close medical supervision. Usual maintenance dose is 20 mg daily in 1-2 divided doses
Dizziness and headache are more commonly reported side effects. Fatigue and asthenia were reported in 2-3% of patients. Other side effects occurred in less than 2% of patients and included hypotension, orthostatic hypotension, syncope, nausea, diarrhoea, muscle cramps, rash and cough.
Less frequently renal dysfunction, renal failure and oliguria have been reported. Angioedema, hyperkalemia and hyponatremia have also been reported rarely
Assess renal function; regular WBC counts in patient w/ collagen vascular disease eg SLE & scleroderma. Patient receiving immunosuppressive therapy; those prone to salt or water depletion. Pregnancy.
Combination with other antihypertensive agents such as b blockers, Methyldopa, calcium antagonists and diuretics may increase the antihypertensive efficacy. Adrenergic blocking drugs should only be combined with Anapril under careful supervision. Concomitant Propranolol may reduce the bioavailability of Anapril, but this does not appear to be of any clinical significance. Concomitant therapy with Lithium may increase the serum Lithium concentration.
- Avoid hypertensive herbs (e.g. bayberry, blue cohosh, cayenne, ephedra, and licorice). Additive hypertensive effects may occur.
- Avoid potassium-containing products. Potassium products increase the risk of hyperkalemia.
- Take with or without food. The absorption is unaffected by food.
Volume of Distribution
The volume of distribution of enalapril has not been established. Anaprilat is shown to penetrate into most tissuesm, in particular the kidneys and vascular tissuem, although penetration of the blood-brain barrier has not been demonstrated after administration at therapeutic doses. In dog studies, enalapril and enalaprilat cross the blood-brain barrier poorly. Minimal penetration occurs into breast milk but significant fetal transfer occurs. The drug crosses the placental barrier in rats and hamsters.
The average terminal half life of enalaprilat is 35-38 hours. The effective half life following multiple doses is 11-14 hours. The prolonged terminal half-life is due to the binding of enalaprilat to ACE.
Following oral administration in healthy male volunteers, the renal clearance was approximately 158 ± 47 mL/min. It is reported that enalapril and enalaprilat are undetectable in the plasma by 4 hours post-dosing.
Pregnancy & Breastfeeding use
Category D: Contraindicated in pregnancy. The drug is excreted in trace amount in human milk and caution should be exercised if given to nursing mothers.
Aortic stenosis or outflow tract obstruction. Renovascular disease. Severe resistant HTN. Peripheral vascular disease or generalized atherosclerosis.
Use in the elderly (over 65 years): The starting dose should be 2.5 mg. Enaril is effective in the treatment of hypertension in the elderly. The dose should be titrated according to need for the control of blood pressure.
- Lightheadedness, dizziness, or fainting
- Decrease in urine output
- Drowsiness, headache, or back pain
- Slow or irregular heartbeat.
- Fluids through an intravenous line (IV)
- Medications to increase blood pressure
- Other treatments based on complications that occur
- Closely monitoring the heart and lungs.