Benazepril Hydrochloride
(British Approved Name Modified, US Adopted Name, rINNM)
Drug Nomenclature
INNs in main languages (French, Latin, Russian, and Spanish):
Pharmacopoeias. In US.
The United States Pharmacopeia 31, 2008, and Supplements 1 and 2 (Benazepril Hydrochloride). A white to off-white crystalline powder. Soluble in water, in alcohol, and in methyl alcohol. Store at a temperature below 30°, preferably between 15° and 30°.
Adverse Effects, Treatment, and Precautions
As for ACE inhibitors.
Interactions
As for ACE inhibitors.
Pharmacokinetics
Benazepril acts as a prodrug of the diacid benazeprilat, its active metabolite. At least 37% of an oral dose of benazepril is absorbed. Benazepril is almost completely metabolised in the liver to benazeprilat. Peak plasma concentrations of benazeprilat after an oral dose of benazepril have been achieved in 1 to 2 hours in the fasting state or 2 to 4 hours in the nonfasting state. Both benazepril and benazeprilat are about 95% bound to plasma proteins. Benazeprilat is excreted mainly in the urine; about 11 to 12% is excreted in the bile. The effective half-life for accumulation of benazeprilat is 10 to 11 hours after multiple doses of benazepril. The elimination of benazeprilat is slowed in renal impairment, although biliary excretion may compensate to some extent. Small amounts of benazepril and benazeprilat are distributed into breast milk.
Uses and Administration
Benazepril is an ACE inhibitor. It is used in the treatment of hypertension and heart failure.
Benazepril owes its activity to benazeprilat to which it is converted after oral dosage. The haemodynamic effects are seen within 1 hour of a single oral dose and the maximum effect occurs after about 2 to 4 hours, although the full effect may not develop for 1 to 2 weeks during chronic dosing. The haemodynamic action lasts for about 24 hours, allowing once-daily dosing. Benazepril is given orally as the hydrochloride. In the treatment of hypertension, the usual initial dose of benazepril hydrochloride is 10 mg once daily. An initial dose of 5 mg once daily is suggested for patients with renal impairment (see below) or who are receiving a diuretic; if possible the diuretic should be withdrawn 2 or 3 days before benazepril is started and resumed later if necessary.
The usual maintenance dose is 20 to 40 mg daily, which may be given in 2 divided doses if control is inadequate with a single dose; doses of up to 80 mg daily have been used.
In the treatment of heart failure the usual initial dose of benazepril hydrochloride is 2.5 mg once daily, adjusted according to response to a maximum dose of 20 mg daily.
Administration in children. Experience with benazepril in children is limited. US licensed product information recommends an initial oral dose of 200 micrograms/kg once daily for hypertension in children 6 years of age and over. Maintenance doses up to 600 micrograms/kg daily (maximum 40 mg daily) have been studied. Insufficient evidence is available to recommend doses for younger children or for any children with creatinine clearance below 30 mL/minute.
Administration in renal impairment. In patients with a creatinine clearance of less than 30 mL/minute, the initial dose of benazepril hydrochloride for hypertension is 5 mg once daily and the maintenance dose should not exceed 40 mg daily.
Preparations
The United States Pharmacopeia 31, 2008, and Supplements 1 and 2: Benazepril Hydrochloride Tablets.
Proprietary Preparations
Argentina: Boncordin †;
Belgium: Cibacen;
Brazil: Lotensin;
Canada: Lotensin;
Denmark: Cibacen;
France: Briem; Cibacene;
Germany; Cibacen;
Greece: Cibacen;
Hungary: Lotensin;
India: Benace;
Indonesia: Cibacen;
Ireland: Cibacen;
Israel: Cibacen;
Italy: Cibacen; Tensanil; Zinadril;
Mexico: Lotensin;
Netherlands: Cibacen;
Philippines: Cibacen;
Poland: Lisonid; Lotensin;
Russia: Lotensin;
South Africa; Cibace;
Spain: Cibacen; Labopal;
Switzerland: Cibacen;
Turkey: Cibacen;
United States of America (US and USA): Lotensin;
Venezuela: Lotensin.
Multi-ingredient
Argentina: Adrebloc †; Amlopril; Amzepril †; Arteriosan Plus; Coroval B; llduc Duo; Pelmec Duo; Terloc Duo;
Brazil: Lotensin H;
France: Briazide; Cibadrex;
Germany; Benazeplus; Benazepril comp; Benazepril HCT; Cibadrex;
Greece: Cibadrex;
Hungary: Lotensin HCT;
India: Amace-BP;
Italy: Cibadrex; Tensadiur; Zinadiur;
Netherlands: Cibadrex;
Poland: Lotensin HCT;
South Africa; Cibadrex;
Spain: Cibadrex; Labodrex;
Switzerland: Cibadrex;
Turkey: Cibadrex;
United States of America (US and USA): Lotensin HCT; Lotrel;
Venezuela: Amlibon B.
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