Quinapril Hydrochloride
(British Approved Name Modified, US Adopted Name, rINNM)
Drug Nomenclature
Pharmacopoeias. In US.
The United States Pharmacopeia 31, 2008, and Supplements 1 and 2 (Quinapril Hydrochloride). A white to off-white powder, with a pink cast at times. Freely soluble in aqueous solvents.
Suspension. Extemporaneous formulations of quinapril 1 mg/mL made by adding crushed Accupril tablets (Pfizer, US) to the following vehicles were found to be stable for 6 weeks when stored at 5°:
• Kphos 15% (Beach, US), Bicitra 15% (Draxis Pharma, US), OraSweet 70% (Paddock, US)
• Kphos 15%, Bicitra 15%, OraSweet SF 70%
• Kphos 15%, Bicitra 15%, simple syrup 70%
The suspension containing OraSweet SF was considered to be the formulation of choice.
Adverse Effects, Treatment, and Precautions
As for ACE inhibitors.
Breast feeding. After of a single dose of quinapril 20 mg in 6 women, quinapril was detected in the breast milk in a milk to plasma ratio of 0.12; no quinaprilat was detected. It was estimated that the dose received by the infant would only be about 1.6% of the maternal dose.
Interactions
As for ACE inhibitors.
Antibacterials. Quinapril has been reported to reduce the absorption of tetracyclines due to the presence of magnesium carbonate in the tablet formulation.
Pharmacokinetics
Quinapril acts as a prodrug of the diacid quinaprilat, its active metabolite. About 60% of an oral dose of quinapril is absorbed. Quinapril is metabolised mainly in the liver to quinaprilat and inactive metabolites. Peak plasma concentrations of quinaprilat are achieved within 2 hours of an oral dose of quinapril. Quinaprilat is about 97% bound to plasma proteins. After an oral dose, quinapril is excreted in the urine and faeces, as quinaprilat, other metabolites, and unchanged drug, with the urinary route predominating; up to 96% of an intravenous dose of quinaprilat is excreted in the urine.
The effective half-life for accumulation of quinaprilat is about 3 hours after multiple doses of quinapril; a long terminal phase half-life of 25 hours may represent strong binding of quinaprilat to angioten sinconverting enzyme.
The pharmacokinetics of both quinapril and quinaprilat are affected by renal and hepatic impairment. Dialysis has little effect on the excretion of quinapril or quinaprilat.
Small amounts of quinapril are distributed into breast milk.
Uses and Administration
Quinapril is an ACE inhibitor. It is used in the treatment of hypertension and heart failure.
Quinapril is converted in the body to its active metabolite quinaprilat. 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 use. The haemodynamic action persists for about 24 hours, allowing once-daily dosing. Quinapril is given orally as the hydrochloride, but doses are expressed in terms of the base. Quinapril hydrochloride 10.8 mg is equivalent to about 10.0 mg of quinapril. In the treatment of hypertension the initial dose is 10 mg of quinapril once daily. Since there may be a precipitous fall in blood pressure in some patients when starting therapy with an ACE inhibitor, the first dose should preferably be given at bedtime. An initial dose of 2.5 mg daily is recommended in the elderly, in patients with renal impairment, or in those taking a diuretic; if possible, the diuretic should be withdrawn 2 or 3 days before quinapril is started and resumed later if necessary.
The usual maintenance dose is 20 to 40 mg daily, as a single dose or divided into 2 doses, although up to 80 mg daily has been given.
In the management of heart failure, severe first-dose hypotension on introduction of an ACE inhibitor is common in patients on loop diuretics, but their temporary withdrawal may cause rebound pulmonary oedema. Thus treatment should begin with a low dose under close medical supervision. Quinapril is given in an initial dose of 2.5 mg daily. Usual maintenance doses range from 10 to 20 mg daily, as a single dose or divided into 2 doses; up to 40 mg daily has been given. Quinaprilat may be given intravenously in patients unable to take quinapril orally; doses range from 1.25 to 10 mg twice daily.
Preparations
The United States Pharmacopeia 31, 2008, and Supplements 1 and 2: Quinapril Tablets.
Proprietary Preparations
Argentina: Accupril;
Australia: Accupril; Acquin; Asig; Filpril;
Austria: Accupro;
Belgium: Accupril;
Brazil: Accupril;
Canada: Accupril;
Chile: Accupril;
Czech Republic: Accupro;
Denmark: Accupro;
Finland: Accupro;
France: Acuitel; Korec;
Germany; Accupro; QuinaLich;
Greece: Accupron;
Hong Kong; Accupril;
Hungary: Accupro; Acumerck;
Indonesia: Accupril;
Italy: Accuprin; Acequin; Quinazil;
Japan: Conan;
Malaysia: Accupril †;
Mexico: Acupril;
The Netherlands: Acupril;
New Zealand: Accupril;
Philippines: Accupril;
Poland: Accupro; Acurenal; AprilGen;
Portugal; Acupril; Vasocon;
Russia: Accupro;
South Africa: Accupril; Quinaspen;
Singapore: Accupril †;
Spain: Acuprel; Acuretic; Ectren; Lidaltrin;
Sweden: Accupro;
Switzerland: Accupro;
Thailand: Accupril;
Turkey: Acuitel;
United Kingdom (UK): Accupro; Quinil;
United States of America (US and USA): Accupril;
Venezuela: Accupril; Quinalar; Solpres.
Multi-ingredient
Argentina: Accuretic;
Australia: Accuretic;
Austria; Accuzide;
Belgium: Accuretic; Co-Quinapril;
Canada: Accuretic;
Chile: Accuretic;
Czech Republic: Accuzide; Stadapress;
Finland: Accupro Comp;
France: Acuilix; Koretic;
Greece: Accuretic; Quimea;
Hungary: Accuzide;
Ireland: Accuretic;
Italy: Accuretic; Acequide; Quinazide;
The Netherlands: Acuzide;
New Zealand: Accuretic;
Philippines: Accuzide;
Poland: Accuzide;
Portugal: Acuretic;
South Africa: Accuretic;
Spain: Bicetil; Lidaltrin Diu;
Sweden: Accupro Comp;
Switzerland: Accuretic;
Turkey: Accuzide;
United Kingdom (UK): Accuretic;
United States of America (US and USA): Accuretic; Quinaretic;
Venezuela: Accuretic; Quinaretic.
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