Trandolapril

Biochem/physiol Actions

Trandolapril is an ACE inhibitor. Trandolapril differs from other ACE inhibitors in that it has a longer biological half-life and a high degree of lipophilicity.

Drug interactions

Potentially hazardous interactions with other drugs Anaesthetics: enhanced hypotensive effect. Analgesics: antagonism of hypotensive effect and increased risk of renal impairment with NSAIDs; hyperkalaemia with ketorolac and other NSAIDs. Antihypertensives: increased risk of hyperkalaemia, hypotension and renal failure with ARBs and aliskiren. Bee venom extract: possible severe anaphylactoid reactions when used together. Ciclosporin: increased risk of hyperkalaemia and nephrotoxicity. Cytotoxics: increased risk of angioedema with everolimus. Diuretics: enhanced hypotensive effect; hyperkalaemia with potassium-sparing diuretics. ESAs: increased risk of hyperkalaemia; antagonism of hypotensive effect. Gold: flushing and hypotension with sodium aurothiomalate. Lithium: reduced excretion (possibility of enhanced lithium toxicity). Potassium salts: increased risk of hyperkalaemia. Tacrolimus: increased risk of hyperkalaemia and nephrotoxicity.

Metabolism

Trandolapril is metabolised in the liver to the active trandolaprilat and to some inactive metabolites. About 33% of an oral dose of trandolapril is excreted in the urine, mainly as trandolaprilat; the rest is excreted in the faeces.

Brand name

Odrik; Udrik; Gopten

General Description

Trandolapril, 1-[2-(1-ethoxycarbonyl-3-phenylpropylamino)propionyl]octahydroindole-2-carboxylicacid (Mavik), is an indole-containing ACE inhibitorthat is structurally related to most of the precedingagents discussed. Enalapril is very similar to trandolapril,with the primary difference occurring in the heterocyclicsystems. The pyrrolidine of enalapril has been replacedwith an octahydroindole system. Much like enalaprilate,trandolapril must be hydrolyzed to tranolaprilate, which isthe bioactive species.