Zofenopril calcium

Описание

Zofenopril calcium was introduced as a second-generation angiotensinconverting enzyme (ACE) inhibitor for the treatment of acute myocardial infarction. Zofenopril, rapidly hydrolyzed by cardiac esterase, is actually a S-benzoyl prodrug of the active component zofenopril-sulfhydryl (zofenoprilat), the latter being the ACE inhibitor responsible for the improvement of postischemic contractile function and for the reduction of cardiac cell death. It was suggested that ACE inhibition alone was not sufficient to explain the cardioprotective effects; the antioxidant properties demonstrated in vitro and in viva could partly explain the strong anti-ischemic effects. In rats with CHF after myocardial infarction, zofenopril attenuated ventricular enlargement and cardiac hypertrophy. It was also shown in isolated globally ischemic rat hearts that the cardioprotective effect of zofenopril was stereoselective. Clinical studies in healthy volunteers comparing zofenopril with enalapril demonstrated that the rate of hydrolysis of the former was faster; at 30 or 60 mg, ACE was completely inhibited in most volunteers until 12h after administration. In patients with anterior acute myocardial infarction, a g-week treatment with zofenopril significantly reduced the incidence of death or severe CHF and also improved the chance of surviving the next year.

Химические свойства

Off-White to Light Yellow Crystalline Solid

Использование

Angiotensin-converting enzyme ACE inhibitor. A prodrug that is de-esterified to the active inhibitor, the sulfhydryl group containing metabolite, Zofenoprilat

Определение

ChEBI: An organic calcium salt that is the hemicalcium salt of zofenopril. A prodrug for zofenoprilat.