Cilazapril

Absorption

Maximum plasma concentrations of cilazaprilat are reached within two hours after administration of cilazapril.

Toxicity

Limited data are available with regard to overdosage in humans. The most likely manifestations are hypotension, which may be severe, hyperkalaemia, hyponatraemia and renal impairment with metabolic acidosis. Treatment should be mainly symptomatic and supportive.

Description

Cilazapril is a prodrug form of the angiotensin converting enzyme (ACE) inhibitor cilazaprilat. In vivo, cilazapril (0.1 mg/kg) inhibits plasma ACE activity and inhibits the angiotensin I-induced pressor response in anesthetized rats and cats. It decreases systolic blood pressure in spontaneously hypertensive rats when administered at a dose of 30 mg/kg. Cilazapril (10 mg/kg, p.o.) decreases blood pressure in volume-depleted renal hypertensive dogs. Formulations containing cilazapril have been used in the treatment of hypertension.

Chemical properties

Off-White Solid

The Uses of Cilazapril

An ACE inhibitor. Hydrolyzed in vivo to the active diacid metabolite (Cilazaprilat). Antihypertensive.

The Uses of Cilazapril

An ACE inhibitor. Hydrolyzed in vivo to the active diacid metabolite (Cilazaprilat). Antihypertensive

Indications

Cilazapril is an ACE inhibtor class drug used in the treatment of hypertension and heart failure.

What are the applications of Application

Cilazapril is a potent ACE inhibitor

Background

Cilazapril is an ACE inhibtor class drug used in the treatment of hypertension and heart failure. It belongs to the angiotensin-converting enzyme inhibitors (ACE inhibitors) class of drugs. It is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat. It is branded as Inhibace in Canada and other countries, Vascace and Dynorm in a number of European countries, among many other names. None of these varieties are available in the United States.

Definition

ChEBI: Cilazapril is a pyridazinodiazepine resulting from the formal condensation of the carboxy group of cilazaprilat with ethanol. It is a drug used in the treatment of hypertension and heart failure. It has a role as a prodrug, an antihypertensive agent and an EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor. It is an ethyl ester, a pyridazinodiazepine and a dicarboxylic acid monoester. It is functionally related to a Cilazaprilat.

brand name

Inhibace (Hoffmann-LaRoche).

Pharmacokinetics

Cilazapril inhibits the production angiotensin II. By doing so, it decreases sodium and water reabsorption (via aldosterone) and it decreases vasoconstriction. The combined effect of this is a decrease in vascular resistance, and therefore, blood pressure. The absolute bioavailability of cilazaprilat after oral administration of cilazapril is 57% based on urinary recovery data. (The absolute bioavailability of cilazaprilat after oral administration of cilazaprilat is 19%.) Ingestion of food immediately before the administration of cilazapril reduces the average peak plasma concentration of cilazaprilat by 29%, delays the peak by one hour and reduces the bioavailability of cilazaprilat by 14%. These pharmacokinetic changes have little influence on plasma ACE inhibition.

Metabolism