Imidapril Hydrochloride

(British Approved Name Modified, rINNM)

Drug Nomenclature

INNs in main languages (French, Latin, Russian, and Spanish):

Synonyms: Imidapriilihydrokloridi; Imidapril, hidrocloruro de; Imidaprilhydroklorid; Imidaprili Hydrochloridum; TA-6366
BAN: Imidapril Hydrochloride [BANM]
INN: Imidapril Hydrochloride [rINNM (en)]
INN: Hidrocloruro de imidapril [rINNM (es)]
INN: Imidapril, Chlorhydrate d’ [rINNM (fr)]
INN: Imidaprili Hydrochloridum [rINNM (la)]
INN: Имидаприла Гидрохлорид [rINNM (ru)]
Chemical name: (S)-3-{N-[(S)-1-Ethoxycarbonyl-3-phenylpropyl]-l-alanyl}-1-methyl-2-oxoimidazoline-4-carboxylic acid hydrochloride
Molecular formula: C20H27N3O6,HCl =441.9
CAS: 89371-37-9 (imidapril); 89396-94-1 (imidapril hydrochloride)
ATC code: C09AA16

Adverse Effects, Treatment, and Precautions

As for ACE inhibitors.

Interactions

As for ACE inhibitors.

Pharmacokinetics

Imidapril acts as a prodrug of the diacid imidaprilat, its active metabolite. After oral doses, imidapril is rapidly but incompletely absorbed; absorption is about 70% and is reduced in the presence of food. Imidapril is metabolised in the liver to imidaprilat. The bioavailability of imidaprilat is about 42% after oral doses of imidapril, and peak plasma concentrations of imidaprilat are reached in about 7 hours. Both imidapril and imidaprilat are moderately bound to plasma proteins. About 40% of an oral dose is excreted in the urine, the rest in the faeces. The terminal half-life of imidaprilat is more than 24 hours. Imidapril and imidaprilat are removed by haemodialysis.

Uses and Administration

Imidapril is an ACE inhibitor. It is used in the treatment of hypertension. Imidapril owes its activity to imidaprilat, to which it is converted after oral doses. The maximum haemodynamic effect occurs 6 to 8 hours after a dose, although the full effect may not develop for several weeks during chronic dosing. Imidapril is given orally as the hydrochloride.

In the treatment of hypertension, the usual initial dose of imidapril hydrochloride is 5 mg once daily, before food. 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 atbedtime. An initial dose of 2.5 mg daily should be used in the elderly, in patients with renal or hepatic impairment, or in those receiving a diuretic; if possible, the diuretic should be withdrawn 2 or 3 days before imidapril is started and resumed later if necessary. The usual maintenance dose is 10 mg daily, although up to 20 mg daily may be given if required. The maximum dose for elderly patients is 10 mg daily.

Preparations

Proprietary Preparations

Argentina: Tanatril;

Austria; Tanatril;

Czech Republic: Tanatril;

Finland: Tanatril;

France: Tanatril;

Germany; Tanatril;

Greece: Tanatril;

Hong Kong; Tanatril;

India: Tanatril;

Indonesia: Tanapress;

Japan: Novarok † Tanatril;

Malaysia: Tanatril;

Philippines: Norten; Vascor;

Poland: Tanatril;

Portugal: Cardipril; Tanatril †;

Singapore: Tanatril;

Spain: Hipertene;

Thailand: Tanatril;

United Kingdom (UK): Tanatril.

Multi-ingredient

Philippines: Norplus; Vascoride.


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