Efficacy and safety of spirapril in mild-to-moderate hypertension.
Spirapril is a new angiotensin-converting enzyme (ACE) inhibitor. It is a prodrug with a resorption of about 50%. The active metabolite spiraprilat reaches maximal plasma concentration within 2-3 h after oral administration. Spirapril can be administered once daily because of its long duration of action caused by an elimination half-life of about 40 h. It undergoes renal and hepatic elimination. In contrast to other ACE inhibitors it has a narrow dose range; therefore, the recommended dose is 6 mg for most patients without the need for dose titration. Spirapril has no relevant drug interactions. In several studies, spirapril was given to patients with mild-to-moderate essential hypertension at doses of 1-24 mg/day. There was an identical blood pressure lowering effect at doses of 6-24 mg/day; doses of 1-3 mg/day were less effective. Twenty-four-hour blood pressure monitoring showed a trough:peak ratio up to 0.84. In studies comparing the effect of spirapril with enalapril, lisinopril, trandolapril or captopril, spirapril was at least as effective as the other substances. Besides treating uncomplicated mild-to-moderate essential hypertension, spirapril can be used in patients with diseases accompanying hypertension such as heart and renal diseases, diabetes mellitus, and lipid disturbances. Possible advantages of spirapril compared to other ACE inhibitors are the dual mechanism of elimination, the lack of need for dose titration and a low incidence of cough.
Hayduk
K
K
Marien-Hospital Düsseldorf, Germany.
Kraul
H
H
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000009:adverse effects / Q000494:pharmacology*; D002986:Clinical Trials as Topic; D004347:Drug Interactions; D004656:Enalapril / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D006973:Hypertension / Q000145:classification / Q000188:drug therapy*; D011355:Prodrugs / Q000494:pharmacology
D000806:Angiotensin-Converting Enzyme Inhibitors; D011355:Prodrugs; D004656:Enalapril; C052555:spirapril; C076884:spiraprilat