Fosinopril Sodium
(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 (Fosinopril Sodium). Store in airtight containers at a temperature of 20° to 25°, excursions permitted between 15° and 30°.
Adverse Effects, Treatment, and Precautions
As for ACE inhibitors.
Interactions
As for ACE inhibitors.
Pharmacokinetics
Fosinopril acts as a prodrug of the diacid fosinoprilat, its active metabolite. About 36% of an oral dose of fosinopril is absorbed. Fosinopril is rapidly and completely hydrolysed to fosinoprilat in both gastrointestinal mucosa and liver. Peak plasma concentrations of fosinoprilat are achieved about 3 hours after an oral dose of fosinopril. Fosinoprilat is more than 95% bound to plasma proteins. It is excreted both in urine and in the faeces via the bile; it has been detected in breast milk. The effective half-life for accumulation of fosinoprilat after multiple doses of fosinopril is about 11.5 hours in patients with hypertension and about 14 hours in patients with heart failure.
Renal impairment. Total body clearance of fosinoprilat, the active metabolite of fosinopril, is slower in patients with renal impairment. However, pharmacokinetic studies in patients with varying degrees of impairment, including those requiring dialysis, indicate that decreases in renal clearance may be compensated for, at least in part, by increases in hepatic clearance.
Uses and Administration
Fosinopril is an ACE inhibitor. It is used in the treatment of hypertension and heart failure.
Fosinopril owes its activity to fosinoprilat to which it is converted after oral doses. The haemodynamic effects are seen within 1 hour of a single oral dose and the maximum effect occurs after 2 to 6 hours, although the full effect may not develop for several weeks during chronic dosing. The haemodynamic action lasts for about 24 hours, allowing once-daily dosing. Fosinopril is given orally as the sodium salt.
In the treatment of hypertension, the initial dose of fosinopril sodium is 10 mg 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. Usual maintenance doses range from 10 to 40 mg once daily. In patients already taking diuretic therapy the diuretic should be withdrawn if possible several days before starting fosinopril, and resumed later if necessary.
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. Fosinopril sodium is given in an initial dose of 10 mg once daily and, if well tolerated, increased to a maximum of 40 mg once daily. An initial dose of 5 mg may be given in patients at high risk of hypotension.
Preparations
The United States Pharmacopeia 31, 2008, and Supplements 1 and 2: Fosinopril Sodium and Hydrochlorothiazide Tablets; Fosinopril Sodium Tablets.
Single-ingredient Preparations
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.
Australia: Monopril; Austria: Fositens; Belgium: Fosinil; Brazil: Monopril; Canada: Monopril; Chile: Monopril; Czech Republic: Monopril; Denmark: Monopril; France: Fozitec; Germany: Dynacil; Fosinorm; Greece: Monopril; Sinopril¤; Hong Kong: Monopril; Hungary: Monopril; India: Fovas; Israel: Vasopril; Italy: Eliten; Fosipres; Tensogard; Malaysia: Monopril; Mexico: Monopril; Netherlands: NewAce; Norway: Monopril¤; Portugal: Fositen; Russia: Monopril (Моноприл); South Africa: Monopril; Singapore: Monopril; Spain: Fosinil¤; Fositens; Hicarlex¤; Hiperlex; Tenso Stop; Tensocardil; Sweden: Monopril; Switzerland: Fositen; Thailand: Monopril; United Kingdom: Staril; United States: Monopril; Venezuela: Monopril
Multi-ingredient Preparations
Australia: Monoplus; Austria: Aceplus; Fosicomb; Belgium: Foside; Brazil: Monoplus; Chile: Monopril Plus; France: Foziretic; Germany: Dynacil comp; Fosinorm comp; Greece: Fozide; Monoplus; Israel: Vasopril Plus; Italy: Elidiur; Fosicombi; Tensozide; Netherlands: Diurace; South Africa: Monozide; Spain: Fositens Plus; Hiperlex Plus; Tenso Stop Plus; Sweden: Monopril comp; Switzerland: Fosicomp; Thailand: Monoplus; United States: Monopril-HCT
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