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Enalaprilat

Enalapril is an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension and some types of chronic heart failure. Enalapril was the first member of the group of ACE inhibitors known as the dicarboxylate-containing ACE inhibitors. It is marketed by Merck & Co. (Merck, Sharp & Dohme) under the trade names, Renitec® and Vasotec®. more...

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Development

Enalapril was developed by researchers at Merck & Co. as part of their efforts to develop novel treatments for hypertension by modulating the renin-angiotensin-aldosterone (RAS) system.

The success of Squibb in developing the first inhibitor, captopril, provided a major impetus for Merck's research laboratories to develop a competing product. Captopril was not without its problems, however, as it was believed (and shown to be true) that the sulfhydryl-moeity of captoril was responsible for such adverse effects as metallic taste.

Enalaprilat

Enalaprilat, the first dicarboxylate-containing ACE inhibitor, was developed partly to overcome these limitations of captopril. The sulfhydryl-moeity was replaced by a carboxylate-moeity, but additional modifications were required in its structure-based design to achieve a similar potency to captopril.

Enalaprilat itself, however, was not without its problems. The consequence of the structural modifications was that it proved to be have unfavourable ionisation characteristics to allow sufficient potency for oral administration (in tablets). Thus enalaprilat was only suitable for intravenous administration. This was overcome by the researchers at Merck by the esterification of enalaprilat with ethanol to produce enalapril. As a prodrug, enalapril is metabolised in vivo to the active form enalaprilat by various esterases.

A prototype for others

Most importantly, perhaps, the QSAR-based modifications in structure serendipitously led to an improved understanding of the structure of ACE which aided in the development of subsequent carboxylate-containing ACE inhibitors.

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Focus on...enalaprilat
From Nursing, 3/1/98

USE THIS I.V ANTIHYPERTENSIVE DRUG FOR PRE BLOOD PRESSURE CONTROL

Mechanism of action: Enalaprilat (Vasotec I.V.) inhibits angiotensin-converting enzyme (ACE), preventing the conversion of angiotensin I to angiotensin II. This leads to vasodilation and decreased aldosterone secretion, decreasing blood pressure, preload, and afterload.

Indications: For mild to severe hypertension when oral therapy isn't practical.

Dosage (adults): For patients not receiving diuretics, administer 1.25 mg slow intravenous (I.V.) infusion over at least 5 minutes every 6 hours. For patients receiving diuretics, give 0.625 mg over at least 5 minutes, repeat in 1 hour if needed, then give 1.25 mg I.V. every 6 hours. Alternative: Enalaprilat may be diluted in 50 ml of D5W or 0.9% sodium chloride solution and infused over 15 to 20 minutes.

Pharmacokinetics:

onset of action, 15 minutes

peak effect, 1 to 4 hours

elimination half-life, 11 hours

duration of action, 6 hours

Adverse effects: transient orthostatic hypotension, tachycardia, bradycardia, persistent dry cough, angioedema, headache, dizziness, fatigue, neutropenia, thrombocytopenia, agranulocytosis, hypersensitivity reactions

Interactions: Enalaprilat increases the risk of hyperkalemia in patients with renal insufficiency or diabetes and those on potassium-sparing diuretics. When given with calcium channel blockers, diuretics, or sympathetic blockers, enalaprilat may cause additive hypotensive reactions. Enalaprilat may cause lithium toxicity if given with lithium.

Contraindications and precautions: Don't give to patients with a hypersensitivity to enalaprilat or a history of angioedema related to previous ACE inhibitor therapy. Use cautiously in patients with renal insufficiency and renal artery stenosis. Don't use in pregnant women.

Nursing considerations:

Closely monitor the patient's blood pressure response, cardiac rhythm, and hemodynamics (including central venous pressure and systemic vascular resistance).

Assess the patient's electrolyte levels and renal function.

Avoid potassium supplements and potassiumsparing diuretics.

Monitor the patient for respiratory distress or facial, lip, or tongue swelling, which are signs of angioedema.

Watch for signs and symptoms of infection. Carefully monitor the patient's fluid balance and correct hypovolemia if necessary.

Use cautiously with other medications that lower blood pressure (such as calcium channel blockers, diuretics, and sympathetic blockers).

Convert to oral medications when the patient's blood pressure is stable and he can safely take oral medications.

Sources: Mosby's Critical Care and Emergency Drug Reference, 2nd edition, J. Keen, et al, Mosby-Year Book, Inc.. 1996; Nursing98 Drug Handbook, Springhouse Corp., 1998; Physicians' Desk Reference, 51st edition, Medical Economics Data Production Co., 1997.

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