Трандолаприл

Описание

Trandolapril is a new ACE inhibitor that is rapidly hydrolyzed, mainly in the liver, to its biologically active form, trandolaprilat. Compared with all other ACE inhibitors, trandolaprilat is reported to have the highest lipophilicity and the most prolonged ACE inhibitory activity. In hypertensive patients, trandolapril at a dose of 2 mg reduces blood pressure consistently throughout the 24 hour period after intake, making it one of the best once a day antihypertensive drugs. It has also been demonstrated to inhibit aortic atherosclerosis in the hyperlipidemic rabbit.

Химические свойства

White or almost white powder.

Использование

Trandolapril has been used as an angiotensin-converting enzyme (ACE) inhibitor to study its effects on responsiveness of human retinal endothelial cells (HRECs) to vascular endothelial growth factor (VEGF).

Общее описание

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.