Zaltidine: An Effective but Hepatotoxic H₂-Receptor Antagonist

Abstract

Zaltidine is a new H₂-receptor antagonist. This study compares the safety and efficacy of zaltidine with those of placebo in the short-term treatment of duodenal ulcer. One hundred and thirty-five patients were randomly allocated to 4 weeks' treatment with either 150 mg zaltidine once daily or placebo. Fifty-nine were treated for a full 4 weeks with zaltidine before the trial was stopped. Healing rates after 4 weeks of zaltidine and placebo were 86% and 19%, respectively (p < 0.001). Five patients in the zaltidine group had increased serum aminotransferase levels at the final (4-week) visit. The values normalized when treatment was stopped. Liver biopsy specimens provide strong evidence of drug-induced injury. Hepatic damage was associated with plasma levels of zaltidine in the upper half of the observed range. Zaltidine appears to be an effective treatment of duodenal ulcer. However, the incidence of hepatic damage (8%) seems higher than with commonly used H₂-receptor antagonists.

Key Words:

• Clinical trial
• drug idiosyncrasy
• duodenal ulcer
• hepatitis
• histamine H₂ blockers
• peptic ulcer
• zaltidine