Enalapril Maleate

Enalapril Maleate is an angiotensin-converting enzyme (ACE) inhibitor. It is widely used to treat high blood pressure and heart failure and may be prescribed after a heart attack. It also lowers the chances of having a heart attack or stroke. Enalapril Maleate can be prescribed either alone or in combination with other medicines. It should be taken on an empty stomach. This medicine should be taken at the same time each day to get the most benefit. It is important to continue taking it regularly even if you feel well or even if your blood pressure is controlled. Most people with high blood pressure do not feel ill, but if you stop taking this medicine, your condition could get worse. This is a widely used medicine and is considered safe for long-term use. Making some changes in your lifestyle will also help lower your blood pressure. These may include regular exercise, losing weight, smoking cessation, reducing alcohol intake, and reducing the amount of salt in your diet as advised by your doctor. The most common side effects of this medicine include feeling dizzy or drowsy, headache, dry cough, fatigue, nausea, vomiting, diarrhea, stomach pain, and low blood pressure. Most of these are temporary and resolve with time. Talk to your doctor if any of the side effects bother you or do not go away. Before taking this medicine, let your doctor know if you have any kidney or liver problems. Pregnant or breastfeeding mothers should also consult their doctor before taking it. Your doctor may check your kidney function, blood pressure and potassium levels in your blood at regular intervals while you are taking this medicine. Enalapril Maleate works by reducing stress on the heart and relaxing blood vessels so that blood flows more smoothly and the heart can pump blood more efficiently. In heart failure, it is used as adjunctive therapy with non-potassium-sparing diuretics and, where appropriate, digitalis. In severe heart failure, treatment should always be initiated in hospital under close medical supervision and it improves symptoms, reduces mortality and hospitalization.

• Hypertension: All grades of essential hypertension and renovascular hypertension.
• Heart Failure: Enalapril Maleate should be used as an adjunctive therapy with non-potassium-sparing diuretics and, where appropriate, digitalis. In severe heart failure, treatment should always be initiated in hospital under close medical supervision. When used as an adjunct to conventional therapy in these patients, Enalapril Maleate improves symptoms, and reduces mortality and hospitalization. In mild to moderate heart failure, treatment should always be initiated under close medical supervision.
• Prevention of heart attack and stroke.

Angiotensin-converting enzyme (ACE) Inhibitors

ACE Inhibitor

Enalapril, 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.

Enalapril, a prodrug of enalaprilat, competitively inhibits ACE from converting angiotensin I to angiotensin II (a potent vasoconstrictor) resulting in increased plasma renin activity and reduced aldosterone (a hormone that causes water and Na retention) secretion. This promotes vasodilation and BP reduction.

Adult Dose:

• Hypertension: Initial: 2.5-5 mg PO qDay. Maintenance: 10-40 mg/day PO qDay or divided q12hr.
• Left Ventricular Dysfunction: Initial: 2.5 mg PO q12hr. May titrate up to 20 mg/day.
• Congestive Heart Failure: Initial: 2.5 mg PO qDay or q12hr. Maintenance: 5-40 mg/Day PO divided q12hr; titrate slowly q2Weeks.
• Hepatic impairment: No dosage adjustment required.

Child Dose (1 month to 16 years): Hypertension: Initial: 0.08 mg/kg/day PO or divided q12hr; not to exceed 5 mg/day. May increase PRN q2Weeks according to blood pressure not to exceed 0.58 mg/kg/day (or 40 mg/day).

Renal Dose: CrCl <30 mL/min: (PO) Initiate 2.5 mg; titrate to response; not to exceed 40 mg. Dialysis: 2.5 mg PO on day of dialysis; adjust dose on nondialysis days according to BP.

Elderly (over 65 years): Starting dose should be 2.5 mg. Enalapril is effective in the treatment of hypertension in the elderly. Some elderly patients may be more responsive to Enalapril than younger patients. The dose should be titrated according to need for the control of blood pressure. Maximum daily dose: 40 mg.

Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Enalapril Maleate may be taken with or without food, but it is better to take it at a fixed time.

If you miss a dose of Enalapril Maleate, skip it and continue with your normal schedule. Do not double the dose.

Common Side Effects: Decreased blood pressure, cough, increased potassium level in blood, fatigue, weakness, dizziness.

Other Side Effects: Severe hypotension and renal failure. Dizziness, headache, fatigue, asthenia, orthostatic hypotension, syncope, nausea, diarrhoea, muscle cramps, rash, cough.

Less Frequently: Renal dysfunction, renal failure, oliguria.

Rare: Myocardial infarction, chest pain, palpitations, rhythm disturbances, angina pectoris, pancreatitis, hepatitis, jaundice, abdominal pain, vomiting, dyspepsia, constipation, anorexia, stomatitis, depression, confusion, somnolence, insomnia, nervousness, paraesthesiae, vertigo, bronchospasm, asthma, dyspnoea, rhinorrhoea, sore throat and hoarseness, diaphoresis, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, pruritus, urticaria, alopecia, impotence, flushing, taste alteration, tinnitus, glossitis, blurred vision, etc. Angioneurotic oedema has been reported rarely.

Precautions: Enalapril Maleate may decrease alertness, affect your vision or make you feel sleepy and dizzy. Do not drive if these symptoms occur. It should be taken with or without food, preferably at the same time each day. Enalapril Maleate can make you feel dizzy for the first few days, so rise slowly if you have been sitting or lying down. You can also prefer taking it at bedtime to avoid dizziness throughout the day. Let your doctor know about any cough, or throat irritation that does not go away. It may increase the level of potassium in blood. Avoid taking potassium supplements and potassium-rich foods such as banana and broccoli.

Important Warnings: Pretreatment assessment of renal function: Assessment of renal function prior to initiation of therapy, and during treatment where appropriate. Symptomatic hypotension was seen rarely in uncomplicated hypertensive patients. It has been reported mainly in patients with severe heart failure and who have been volume-depleted by diuretic therapy. By initiating therapy with a small dose (2.5 mg Enalapril) the duration of any hypotensive effect may be lessened. Similar considerations in terms of initiating therapy with a small dose may apply also to patients with ischaemic heart or cerebrovascular disease in whom severe hypotension could result in a myocardial infarct or cerebrovascular accident. Enalapril should be used with caution in patients with renal insufficiency as they may require reduced or less frequent doses. A high incidence of anaphylactoid reactions have been reported in patients dialyzed with high flux membranes (e.g., AN 69) and treated concomitantly with an ACE inhibitor. This combination should therefore be avoided. Cough has been reported with the use of ACE inhibitors. Characteristically, the cough is non-productive, persistent and resolves after discontinuation of therapy. In patients undergoing major surgery or during anaesthesia with agents that produce hypotension, Enalapril blocks angiotensin II formation secondary to compensatory renin release. This may lead to hypotension which can be corrected by volume expansion. Enalapril should not be used in patients with aortic stenosis or outflow obstruction.

Contraindications:

• Hypersensitivity
• History of angioedema due to previous treatment with ACE inhibitors
• Bilateral renal artery stenosis
• Pregnancy
• Hypersensitivity to enalapril or any component

Drug Interactions:

• May potentiate hypotensive action with diuretics, other antihypertensives, TCAs, nitrates or anaesth.
• Concomitant admin with lithium carbonate may cause lithium toxicity.
• Increased risk of renal impairment with NSAIDs.
• May increase hyperkalaemic effect with K-sparing diuretics and supplements.
• Combination with beta-blockers, methyldopa, calcium antagonists, and diuretics may increase antihypertensive efficacy.
• Propranolol may reduce bioavailability of enalapril, but this does not appear to be of any clinical significance.
• Enalapril may elevate plasma potassium levels in patients with renal failure.

Food Interactions: It is unsafe to consume alcohol with Enalapril Maleate. Alcohol can adversely affect blood pressure and reduce the effectiveness of the medication.

Use in Pregnancy: Enalapril Maleate is unsafe to use during pregnancy as there is definite evidence of risk to the developing baby. However, the doctor may rarely prescribe it in some life-threatening situations if the benefits are more than the potential risks. Please consult your doctor. Enalapril is contraindicated in pregnancy.

Use in Lactation: Enalapril Maleate is probably safe to use during breastfeeding. Limited human data suggests that the drug does not represent any significant risk to the baby. Use of Enalapril Maleate immediately after childbirth should be avoided. Enalapril and enalaprilat are excreted in human milk; caution should be exercised if Enalapril is given to lactating mothers.

Pediatric Use: The paediatric use of Enalapril has not been studied. (1 month-16 years dosage available above)

Geriatric Use: Elderly (over 65 years): The starting dose should be 2.5 mg. Enalapril is effective in the treatment of hypertension in the elderly. Some elderly patients may be more responsive to Enalapril than younger patients.

Renal Impairment: Use with caution. CrCl <30 mL/min: Initiate 2.5 mg; not to exceed 40 mg. Regular monitoring of blood pressure, kidney function test, and potassium levels is recommended while you are taking this medicine.

Hepatic Impairment: Enalapril Maleate should be used with caution in patients with liver disease. Dose adjustment of Enalapril Maleate may be needed. Please consult your doctor. Inform your doctor if you experience fatigue, develop yellowing of the skin and eyes or white stools while taking this medicine.

Overdose: Enalapril is dialysable. The most prominent features of overdosage reported to date are marked hypotension, beginning some six hours after ingestion of tablets, concomitant with blockage of the renin-angiotensin system, and stupor. The recommended treatment of overdosage is intravenous infusion of normal saline solution. If ingestion is recent, induce emesis. Enalapril can be removed from the general circulation by haemodialysis.

Storage: Do not store above 25°C. Keep away from light and wet place. Keep out of reach of children.

Enalapril Maleate