Delapril HCl is an ester prodrug which can inhibit the activity of angiotensin I converting enzyme in the blood. It is an antihypertensive effect.
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HazMat fee for 500 gram (Estimated)
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The results of worldwide clinical studies indicate that angiotensin converting enzyme (ACE) inhibitors, exemplified by Captopril and enalapril, are very useful for treatment of hypertension. Delapril HCl, the hydrochloride salt form of delapril, is a lipophilic, non-sulfhydryl ACE inhibitor with antihypertensive activity[1]. In dogs given 10 mg/kg of [14C]delapril, 72% of the dose was absorbed. Plasma levels of M-I (an active metabolite of delapril) peaked within 0.4 hour of administration (Cmax 0.9 μg/mL), then declined biphasically with half-lives of 0.3 and 2.8 hours. When delapril (3 mg/kg) is administered orally to spontaneously hypertensive rats (SHR) for 2 weeks, the tissue ACE inhibitory activity, especially on aortic wall vascular ACE, was more marked than captopril (30 mg/kg) and enalapril (3 mg/kg), whereas all inhibitors were about equally effective on plasma ACE. Moreover, the effect of delapril on tissue ACE lasted longer than on the circulatory system. At oral doses of 1-10 mg/kg, delapril exerted marked and long-lasting antihypertensive action in RAS-dependent models of hypertension, such as 2-kidney, l-clip hypertensive rats and dogs. In stroke-prone SHR and in SHR with chronic renal failure, delapril (10 and 30 mg/kg/day orally for 32 and 28 days, respectively) was also able to improve survival rate significantly and prevented the development of symptoms of cardiac and renal injury, such as stroke, cardiac hypertrophy, and renal sclerosis[2].
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