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Enalaprilat

Generic Name
Enalaprilat
Drug Type
Small Molecule
Chemical Formula
C18H24N2O5
CAS Number
76420-72-9
Unique Ingredient Identifier
Q508Q118JM

Overview

Enalaprilat is the active metabolite of the orally available pro-drug, enalapril. Used in the treatment of hypertension, enalapril is an ACE inhibitor that prevents Angiotensin Converting Enzyme (ACE) from transforming angiotensin I into angiotensin II. As angiotensin II is responsible for vasoconstriction and sodium reabsorption in the proximal tubule of the kidney, down-regulation of this protein results in reduced blood pressure and blood fluid volume. Enalaprilat was originally created to overcome the limitations of the first ACE inhibitor, captopril, which had numerous side effects and left a metallic taste in the mouth. Removal of the problematic thiol group from captopril resulted in enalaprilat, which was then modified further with an ester to create the orally available pro-drug enalapril. Enalaprilat is poorly orally available and is therefore only available as an intravenous injection for the treatment of hypertension when oral therapy is not possible.

Background

Enalaprilat is the active metabolite of the orally available pro-drug, enalapril. Used in the treatment of hypertension, enalapril is an ACE inhibitor that prevents Angiotensin Converting Enzyme (ACE) from transforming angiotensin I into angiotensin II. As angiotensin II is responsible for vasoconstriction and sodium reabsorption in the proximal tubule of the kidney, down-regulation of this protein results in reduced blood pressure and blood fluid volume. Enalaprilat was originally created to overcome the limitations of the first ACE inhibitor, captopril, which had numerous side effects and left a metallic taste in the mouth. Removal of the problematic thiol group from captopril resulted in enalaprilat, which was then modified further with an ester to create the orally available pro-drug enalapril. Enalaprilat is poorly orally available and is therefore only available as an intravenous injection for the treatment of hypertension when oral therapy is not possible.

Indication

Enalaprilat injection is indicated for the treatment of hypertension when oral therapy is not practical.

Associated Conditions

  • Diabetic Nephropathy
  • Heart Failure
  • Hypertension
  • Left Ventricular Dysfunction

FDA Approved Products

ENALAPRILAT
Manufacturer:HF Acquisition Co LLC, DBA HealthFirst
Route:INTRAVENOUS
Strength:1.25 mg in 1 mL
Approved: 2024/02/22
NDC:51662-1477
Enalaprilat
Manufacturer:Dr. Reddys Laboratories Inc
Route:INTRAVENOUS
Strength:2.5 mg in 2 mL
Approved: 2023/04/20
NDC:43598-169
Enalaprilat
Manufacturer:Dr. Reddys Laboratories Inc
Route:INTRAVENOUS
Strength:1.25 mg in 1 mL
Approved: 2023/04/20
NDC:43598-078

Singapore Approved Products

KORANDIL 20 TABLET 20MG
Manufacturer:Remedica Ltd.
Form:TABLET
Strength:20mg
Online:Yes
Approved: 2012/10/30
Approval:SIN14265P

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