Cilazapril is the monoethyl ester prodrug form of a potent, specific. long-acting antihypertensive inhibitor of angiotensin-converting enzyme (ACE). The biochemical and pharmacological properties of this compound have been compared with those of captopril and enalapril. In all test systems, cilazapril was the most potent and the longest acting. The active diacid of cilazapril was more potent than the corresponding diacid of enalapril in inhibiting the cleavage of angiotensin I and of Hip-His-Leu by ACE in vitro, in antagonising the angiotensin I-induced contractions of the isolated ileum of the guinea pig, in potentiating the vasodepressor responses to bradykinin, and in reducing the angiotensin I-induced rise in blood pressure of the rat. Parent drug absorption and diacid bioavailability in the rat were higher than for enalapril, and the inhibition of plasma ACE of longer duration. Single doses of cilazapril were more potent than enalapril in lowering the blood pressure of spontaneously hypertensive rats (SHR) and two-kidney renal hypertensive rats. On repeated daily oral dosing to SHR, both compounds had a cumulative antihypertensive effect. The acute antihypertensive effect was enhanced by simultaneous treatment with hydrochlorothiazide.

Angiotensin I↗

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[Solitary rectal ulcer syndrome].

The solitary rectal ulcer syndrome is an infrequent entity consisting of a rectal lesion, caused by straining during defecation; it is characterized by specific histological changes. The condition is most frequent in adults between 30 and 50 years of age, but a few pediatric cases have been reported. Five patients (4 boys) are presented. All suffered from moderate rectal bleeding, straining, tenesmus and mucous discharge. One of them had clinical and endoscopic evidence of rectal prolapse. On defecography all children showed failure of pelvic floor relaxation during straining. Endoscopic evaluation showed single or multiple ulcers in four patients and a nodular fibrotic lesion in one. The histopathology of the rectal mucosa revealed replacement of the stroma of the lamina propria by collagen, lack of orientation of smooth muscle fibers and considerable hyperthopy of the muscularis mucosae. Medical treatment was satisfactory in four patients, one case required transabdominal rectopexy for relief of his symptoms. The most appropriate form of treatment has not been determined, but surgery should be used when prolapse is a prominent clinical feature. Greater awareness of this condition will lead to more frequent diagnosis.

Adolescent↗

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