Zofenopril

A prodrug form of zofenoprilat

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5mg

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Background

Zofenopril is a prodrug form of the angiotensin-converting enzyme (ACE) inhibitor zofenoprilat.¹ Zofenopril is hydrolyzed by cardiac esterases in vivo to form zofenoprilat. It inhibits ACE with an IC₅₀ value of 0.9 nM in heart tissue homogenates and inhibits cardiac ACE activity in isolated perfused rat hearts. It reduces mean arterial blood pressure in two kidney-one clip renal hypertensive (2K-1C) rats and spontaneously hypertensive rats (SHRs) when administered at doses of 2.2, 6.6, and 22 mg/kg.² Unlike the ACE inhibitor ramipril , zofenopril does not affect bronchoalveolar lavage fluid (BALF) levels of bradykinin or prostaglandin E₂ or increase coughing induced by citric acid in guinea pigs.³

1.Grover, G.J., Sleph, P.G., Dzwonczyk, S., et al.Effects of different angiotensin-converting enzyme (ACE) inhibitors on ischemic isolated rat hearts: Relationship between cardiac ACE inhibition and cardioprotectionJ. Pharmacol. Exp. Ther.257(3)919-929(1991) 2.DeForrest, J.M., Waldron, T.L., Krapcho, J., et al.Preclinical pharmacology of zofenopril, an inhibitor of angiotensin I converting enzymeJ. Cardiovasc. Pharmacol.13(6)887-894(1989) 3.Cialdai, C., Giuliani, S., Valenti, C., et al.Differences between zofenopril and ramipril, two ACE inhibitors, on cough induced by citric acid in guinea pigs: Role of bradykinin and PGE2Naunyn Schmiedebergs Arch. Pharmacol.382(5-6)455-461(2010)