Enalapril

What is Enalapril?

• Enalapril (Vasotec), is the maleate salt of enalapril, the ethyl ester of a long-acting angiotensin-converting enzyme inhibitor, enalaprilat.
• Enalapril is a pro-drug; following oral administration, it is bioactivated by hydrolysis of the ethyl ester to enalaprilat, which is the active angiotensin-converting enzyme inhibitor.

Enalapril structure

What are the uses of this medicine?

• Enalapril (Vasotec), is used alone or in combination with other medications to treat high blood pressure.
• It is also used in combination with other medications to treat heart failure.
• In asymptomatic patients with left ventricular dysfunction (ejection fraction ≤ 35%), enalapril maleate tablets, USP decrease the rate of development of overt heart failure and decrease the incidence of hospitalization for heart failure.

Enalaprilat

How does this medicine work?

• The maleate salt form of enalapril, a dicarbocyl-containing peptide and angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity.
• As a prodrug, enalapril is converted by de-esterification into its active form enalaprilat.
• Enalaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II.
• This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation.
• Enalapril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.

Enalapril 3D animation

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• who are hypersensitive to this product.
• with a history of angioedema related to previous treatment with an angiotensin-converting enzyme inhibitor.
• with hereditary or idiopathic angioedema.
• with diabetes, who use aliskiren.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• valsartan and sacubitril (Entresto) or if you have stopped taking it within the last 36 hours.
• if you have diabetes and you are taking aliskiren (Tekturna, in Amturnide, in Tekamlo, in Tekturna HCT).
• aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) such as indomethacin (Indocin, Tivorbex); diuretics ('water pills'); lithium (Lithobid); and potassium supplements.

Is this medicine FDA approved?

• Enalapril was approved for use in the United States in 1985 and current indications include hypertension, symptomatic heart failure and prevention of progression of left ventricular dysfunction.

How should this medicine be used?

Recommended dosage: For Hypertension:

• In patients who are currently being treated with a diuretic, symptomatic hypotension occasionally may occur following the initial dose of enalapril maleate tablets, USP. The diuretic should, if possible, be discontinued for 2 to 3 days before beginning therapy with enalapril maleate tablets.
• If the diuretic cannot be discontinued an initial dose of 2.5 mg should be used under medical supervision for at least 2 hours and until blood pressure has stabilized for at least an additional hour.
• The recommended initial dose in patients not on diuretics is 5 mg once a day.
• Dosage should be adjusted according to blood pressure response.
• The usual dosage range is 10 mg to 40 mg per day administered in a single dose or two divided doses.

For Heart Failure:

• Enalapril maleate tablets, USP are indicated for the treatment of symptomatic heart failure, usually in combination with diuretics and digitalis.
• The recommended initial dose is 2.5 mg.
• The recommended dosing range is 2.5 mg to 20 mg given twice a day.
• Doses should be titrated upward, as tolerated, over a period of a few days or weeks. The maximum daily dose administered in clinical trials was 40 mg in divided doses.

For Asymptomatic Left Ventricular Dysfunction:

• 2.5 mg twice daily and were titrated as tolerated to the targeted daily dose of 20 mg (in divided doses).

Pediatric Hypertensive Patients:

• The usual recommended starting dose is 0.08 mg/kg (up to 5 mg) once daily.
• Dosage should be adjusted according to blood pressure response.
• Doses above 0.58 mg/kg (or in excess of 40 mg) have not been studied in pediatric patients.

Administration:

• Enalapril comes as an immediate and extended-release (long-acting) tablet to take by mouth.
• It is usually taken once or twice a day with or without food.
• To help you remember to take enalapril, take it around the same time(s) every day.
• Your doctor will probably start you on a low dose of enalapril and gradually increase your dose.
• Enalapril controls high blood pressure and heart failure but does not cure them.
• Continue to take enalapril even if you feel well.
• Do not stop taking enalapril without talking to your doctor.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As an immediate and extended-release (long-acting) tablet

This medicine is available in fallowing brand namesː

• Vasotec

What side effects can this medication cause?

The most common side effects of this medicine may include:

• dizziness, fatigue, headache, cough, gastrointestinal upset and skin rash.

Less common, but serious side effects may include:

• hypersensitivity reactions, anaphylaxis and fetal or neonatal mortality

What special precautions should I follow?

• Angioedema, including laryngeal edema, may occur at any time during treatment with angiotensin-converting enzyme inhibitors, including enalapril. Patients should be so advised and told to report immediately any signs or symptoms suggesting angioedema.
• Patients should be cautioned to report lightheadedness, especially during the first few days of therapy.
• Patients should be told not to use salt substitutes containing potassium without consulting their physician.
• Patients should be told to report promptly any indication of infection (e.g., sore throat, fever) which may be a sign of neutropenia.
• As with all vasodilators, enalapril should be given with caution to patients with obstruction in the outflow tract of the left ventricle.
• Dosage reduction and/or discontinuation of the diuretic and/or enalapril maleate may be required in patients with changes in renal function.
• Elevated serum potassium was observed. Risk factors for the development of hyperkalemia include renal insufficiency, diabetes mellitus, and the concomitant use of potassium-sparing diuretics, potassium supplements and/or potassium-containing salt substitutes, which should be used cautiously, if at all, with enalapril maleate.
• Persistent nonproductive cough has been reported with all ACE inhibitors, always resolving after discontinuation of therapy. ACE inhibitor-induced cough should be considered in the differential diagnosis of cough.
• If you are having surgery, including dental surgery, tell the doctor or dentist that you are taking enalapril.
• Female patients of childbearing age should be told about the consequences of exposure to enalapril maleate during pregnancy. Discuss treatment options with women planning to become pregnant. Patients should be asked to report pregnancies to their physicians as soon as possible.
• Enalapril is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury.
• Enalapril and enalaprilat have been detected in human breast milk. Because of the potential for serious adverse reactions in nursing infants from enalapril, a decision should be made whether to discontinue nursing or to discontinue enalapril maleate, taking into account the importance of the drug to the mother.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• hypotension

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• The most likely manifestation of overdosage would be hypotension, for which the usual treatment would be intravenous infusion of normal saline solution.
• Enalaprilat may be removed from general circulation by hemodialysis and has been removed from neonatal circulation by peritoneal dialysis

Can this medicine be used in pregnancy?

• Pregnancy Category D.
• Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death.

Can this medicine be used in children?

• Antihypertensive effects of enalapril maleate have been established in hypertensive pediatric patients age 1 month to 16 years.
• Enalapril maleate is not recommended in neonates and in pediatric patients with glomerular filtration rate <30 mL/min/1.73 m2, as no data are available.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• Enalapril maleate

Inactive ingredients:

• corn starch, croscarmellose sodium, lactose monohydrate, magnesium stearate, pregelatinized starch, and sodium bicarbonate. In addition, the 2.5 mg tablets contain ferric oxide yellow, 5 mg tablets contain ferric oxide red and 10 mg and 20 mg tablets contain ferric oxide red and ferric oxide black.

Who manufactures and distributes this medicine?

• Manufactured in Slovenia by Lek Pharmaceuticals d.d. for
• Sandoz Inc., Princeton, NJ
• Product of India.

What should I know about storage and disposal of this medication?

• Store at 20°-25°C (68°-77°F).
• Keep container tightly closed.
• Protect from moisture.
• Dispense in a tight container as per USP, if product package is subdivided.

Common ACE inhibitors include the following:

• Benazepril
• Captopril
• Enalapril
• Fosinopril
• Lisinopril
• Moexipril
• Perindopril
• Quinapril
• Ramipril
• Trandolapril

• Dailymed label info on Enalapril
• FDA Enalapril

Enalapril Resources
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Common ACE inhibitors include the following:

• Benazepril
• Captopril
• Enalapril
• Fosinopril
• Lisinopril
• Moexipril
• Perindopril
• Quinapril
• Ramipril
• Trandolapril