High Blood Pressure / Hypertension

Trandolapril

By Cardiologist on September 17th, 2010

Drug Nomenclature

Pharmacopoeias. In Europe.

European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Trandolapril). A white or almost white powder. Practically insoluble in water; sparingly soluble in dehydrated alcohol; freely soluble in dichloromethane. Protect from light.

Adverse Effects, Treatment, and Precautions

As for ACE inhibitors.

Interactions

As for ACE inhibitors.

Pharmacokinetics

Trandolapril acts as a prodrug of the diacid trandolaprilat, its active metabolite. After oral doses of trandolapril the bioavailability of trandolaprilat is 40 to 60%. Trandolapril is metabolised in the liver to trandolaprilat and to some inactive metabolites. Peak plasma concentrations of trandolaprilat are achieved 4 to 6 hours after an oral dose of trandolapril. Trandolaprilat is more than 80% bound to plasma proteins. About 33% of an oral dose of trandolapril is excreted in the urine, mainly as trandolaprilat; the rest is excreted in the faeces. The effective half-life for accumulation of trandolaprilat is 16 to 24 hours after multiple doses of trandolapril. Impaired renal function decreases the excretion of trandolaprilat. Trandolaprilat is removed by haemodialysis.

Uses and Administration

Trandolapril is an ACE inhibitor. It is used in the treatment of hypertension and in left ventricular dysfunction following myocardial infarction.

Trandolapril owes its activity to trandolaprilat to which it is converted after oral doses. The haemodynamic effects are seen about 1 hour after an oral dose and the maximum effect occurs after 8 to 12 hours. The haemodynamic action lasts for at least 24 hours, allowing once-daily dosing.

In the treatment of hypertension the initial oral dose is 500 micrograms 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. In patients already taking a diuretic, the diuretic should be stopped, if possible, 2 to 3 days before starting trandolapril and resumed later if necessary. In patients with co-existing heart failure treatment with trandolapril should begin under close medical supervision. The usual maintenance dose for hypertension is 1 to 2 mg once daily, although up to 4 mg daily may be given, as a single dose or in 2 divided doses.

In myocardial infarction, treatment with trandolapril may be started 3 days after the infarction in an initial dose of 500 micrograms once daily, gradually increased to a maximum of 4 mg once daily. A reduction in dosage may be necessary in patients with renal impairment (see below).

Administration in renal impairment. The initial dose of trandolapril in patients with renal impairment should not exceed 500 micrograms daily. UK licensed product information states that the maximum maintenance dose should be 2 mg daily in patients with a creatinine clearance of less than 10 mL/minute.

Preparations

Proprietary Preparations

Argentina: Nortensin †;

Australia: Gopten; Odrik Tranalpha;

Austria; Gopten

Brazil: Gopten; Odrik †;

Canada: Mavik;

Czech Republic: Gopten; Tanap;

Denmark: Gopten; Odrik;

Finland: Gopten †;

France: Gopten †; Odrik

Germany; Gopten; Udrik

Greece: Afenil; Odrik

Hungary: Gopten;

Indonesia: Gopten;

Ireland: Gopten; Odrik

Italy: Gopten;

Japan: Odric; Preran;

Mexico: Gopten †;

The Netherlands: Gopten; Odrik

Norway: Gopten;

New Zealand: Gopten; Odrik

Poland: Gopten;

Portugal: Gopten; Odrik

Russia: Gopten;

South Africa: Gopten †; Mavik

Spain: Gopten; Odrik

Sweden: Gopten;

Switzerland: Gopten;

Turkey: Gopten;

United Kingdom (UK): Gopten; Odrik;

United States of America (US and USA): Mavik.

Multi-ingredient

Argentina: Tarka †;

Australia: Tarka;

Austria: Tarka;

Canada: Tarka;

Czech Republic: Tarka;

Denmark: Tarka;

Finland: Tarka †;

France: Ocadrik †; Tarka;

Germany; Tarka; Udramil †;

Greece: Tarka; Ziaxel;

Hungary: Tarka;

Indonesia: Tarka;

Italy: Tarka;

Mexico: Tarka;

The Netherlands: Tarka; Ziaxel;

New Zealand: Ziaxel;

Philippines: Tarka;

Poland: Tarka;

Portugal: Tarka; Ziaxal;

Russia: Tarka;

South Africa; Tarka;

Spain: Tarka; Tricen;

Sweden: Tarka;

Switzerland: Tarka;

Turkey: Tarka;

United Kingdom (UK): Tarka;

United States of America (US and USA): Tarka;

Venezuela: Tarka.

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