Antihypertensive, Angiotensin – Converting enzyme (ACE) inhibitor
Each tablet contains enalapril maleate 5 mg or 20 mg.
Hypertension: Enalapril is indicated for the treatment of hypertension. Enalapril is effective alone or in combination with other antihypertensive agents, especially a thiazide diuretic. The blood pressure lowering effects of enalapril and thiazides are approximately additive. Enalapril also used for renovascular hypertension (except in patients with bilateral renal artery stenosis).
Heart Failure: Enalapril is indicated for the treatment of symptomatic congestive heart failure, usually in combination with diuretics and digitalis therapy , for treatments of congestive heart failure not responding to other measures.
Asymptomatic left ventricular dysfunction:
In clinically stable asymptomatic patients with left ventricular dysfunction (ejection fraction ≤ 35 percent), enalapril decreases the rate of development of overt heart failure and decreases the frequency of hospitalization for heart failure.
Dosage and Administration:
Usual adult and adolescent dose:
Initial: Oral , 5mg once a day, the dosage being adjusted after one or two weeks according to clinical response.
Maintenace: Oral , 10 to 40 mg per day, as a single dose or in two divided doses.
An initial dose of 2.5 mg should be used in patients who are sodium – and water – depleted as a result of prior diuretic therapy, patients continuing to receive diuretic therapy, or patients with renal failure (creatinine clearance less than 30ml per minute). Such patients should be kept under medical supervision for at least two hours after this initial dose (and for an additional hour after blood pressure has stabilized), to watch for excessive hypotension effect.
Congestive heart failure , vasodilator:
Initial: Oral, 2.5mg once or twice a day, the dosage being adjusted after a few days or weeks according to clinical response.
Maintenance: Oral, 5 to 40mg per day, as a single dose or in two divided doses.
Asymptomatic left ventricular dysfunction:
Oral , 2.5mg two times a day titrated as tolerated up to a target dose of 20mg a day in divided doses.
Note: patients should be kept under medical supervision for at least two hours and until blood pressure has stabilized for an additional hour after the initial dose.
In patients with hyponatremia (serum sodium concentration less than 130mEq per liter) or serum creatinine greater than 1.6mg per deciliter, an initial dose of 2.5mg once a day is recommended. If possible, the dose of the diuretic should be reduced to decrease the likelihood of hypotension effect.
-Usual adult prescribing limits: 40mg per day.
-Usual pediatric dose: Safety and efficacy have not been established.
Dosage in renal insufficiency:
Generally, the intervals between the administration of Enalapril should be prolonged and /or the dosage reduced. Initial dose in mild impairment With creatinine clearance between 30 and 80 ml/min is 5mg.
In moderate to severe impairment with creatinine clearance lower than 30ml/min is 2.5 mg.
In dialysis patients is 2.5 mg on dialysis days.
Enalapril is contraindicated in patients who are hypersensitive to any components of this product and in patients with a history of medical problems especially angioedema related to previous treatment with an ACE-inhibitor, hepatic function impairment, hyperkalemina, renal artery stenosis, renal transplant, renal function impairment or sodium and volume depletion.
Anaphylactoid and possibly related reactions: Presumably because Angiotensin – converting enzyme inhibitors affect the metabolism of eicosanoids and polypeptides, including endogenous bradykinin, patients reciving ACE inhibitors may be subject to a variety of adverse reactions, some of them serious.
Angioedema: Angioedema of the face, extremities, lips, tongue, glottis and / or larynx has been reported in patients treated with angiotensin converting enzyme inhibitors, including enalapril. This may occur at any time during treatment. In such cases enalapril should be promptly discontinued and appropriate therapy and monitoring should be provided until complete and sustained resolution of signs and symptoms has occurred. In instances where swelling has been confined to the face and lips the condition has generally resolved without treatment, although antihistamines have been useful in relieving symptoms. Angioedema associated with laryngeal edema may be fatal. Where there is involvement of the tongue, glottis or larynx, likely to cause airway obstruction, appropriate therapy, e.g., subcutaneous epinephrine solution 1:1000 (0.3 ml to 0.5 ml) and / Checking patient airway, should be promptly provided.
Other possibly and rare reactions: Anaphylactoid reactions during desensitization, anaphylactoid reactions during membrane exposure, hypotension, neutropenia and agranulocytosis, hepatic failure, fetal / neonatal morbidity and mortality.
Aortic stenosis / Hypertrophic cardiomiopathy: Enalapril should be given with caution to patients with obstruction in the outflow of the left ventricle.
Surgery / Anesthesia: In patients undergoing major surgery or during anesthesia with agents that produce hypotension, enalapril may block angiotensin II formation secondary to compensatory renin release. If hypotension occurs and is considered to be due to this mechanism it can be corrected by volume expansion.
Usage in pregnancy:
Pregnancy categories: C. (first trimester) and D . (second and third trimester). When pregnancy is detected, enalapril should be discontinued as soon as possible.
Enalapril and Enalaprilat are detected in human milk in trace amounts. Caution should be made when enalapril is given to a nursing mother.
Safety and effectiveness in children have not been established.
Diuretics, may occasionally experience an excessive reduction of blood pressure with enalapril. The possibility of hypotensive effects with enalapril can be minimized by either discontinuing the diuretic or increasing the salt intake prior to initiation of treatment with enalapril. If it is necessary to continue the diuretic, therapy close medical supervision after the initial dose for at least two hours and until blood pressure has stabilized for at least an additional hour is recommended.
Agents causing rennin release: The antihypertensive effect of enalapril is augmented by antihypertensive agents that cause renin release (e.g.diuretics).
Non – steroidal anti – inflammatory agents:
In some patients with compromised renal function who are being treated with non – steroidal anti – inflammatory drugs, the co – administration of enalapril may result in a further deterioration of renal function. These effects are usually reversible.
Agents increasing serum potassium:
Enalapril attenuates potassium loss caused by thiazide – type diuretics.
Potassium sparing diuretics (e.g. spironolactone, triamteren, or amiloride) , potassium supplements or potassium – containing salt substitutes may lead to significant increases in serum potassium. Therefore, if concomitant use of these agents is indicated because of demonstrated hypokalemia, they should be used with caution and with frequent monitoring of serum potassium.
Potassium sparing agents should generally not be used in patients with heart failure receiving enalapril.
Lithium : Lithium toxicity has been reported in patients receiving lithium concomitantly with drugs which cause elimination of sodium , including ACE inhibitors. It is recommended that serum lithium levels be monitored frequently if enalparil is administered concomitantly with lithium.
Enalapril has been found to be generally tolerated in controlled clinical trials. Adverse experiences were mild and transient in nature. In clinical trials discontinuation of therapy due to clinical adverse experiences was required in 3.3 percent of patients with hypertension and in 5.7 percent of patients with heart failure. The frequency of adverse experiences was not related to total daily dosage within the usual dosage ranges. In patients with hypertension the overall percentage of patients treated with enalapril, reporting adverse experiences was comparable to placebo.
Incidence more frequent (more than 1 percent) : Fatigue, headache, dizziness, rash, hypotension, diarrhea, cough.
Incidence rare (less than 1 percent) : Renal dysfunction, decreased hemoglobin and hematocrit, pemphigus, bradycardia, hepatic failure, peripheral neuropathy, pneumonia.
Store below 30˚C.
Keep out of reach of children.