Erythromycin acistrate is a new 2'-acetyl esther
prodrug of
erythromycin, whose structure resembles that of
erythromycin estolate. However, in toxicological studies, it does not have the problems of hepatotoxicity. To assess its effects on hepatic functions in clinical practice, the liver parameters of patients with respiratory tract or skin
infections were monitored during
therapy. In total 1549 patients were treated for 7-14 days. In addition, 127 patients with suspected
viral infections served as controls. There were no significant differences in serum
aspartate aminotransferase (ASAT),
alanine aminotransferase (ALAT),
gamma-glutamyltransferase (gamma-GT) or
alkaline phosphatase (
APHOS) values between the
erythromycin acistrate or control groups at the beginning or end of
therapy. ASAT values increased moderately in 2.4% and clearly in 0.3% of patients treated, but also decreased in 2.0%. ALAT values were moderately increased in 9.9%, clearly increased in 0.6% and normalized in 3.5% of the patients. gamma-GT values increased moderately in 3.5% and and clearly in 0.3%, but decreased to normal in 3.3% of the patients.
APHOS was moderately elevated in 1.0% of the patients and normalized in 1.3%. The correlation of changes between the different liver
enzymes was poor. Only ten patients (0.6%) had two or more clearly elevated liver
enzyme values by the end of the
therapy, of whom five had increased liver
enzyme activities before the treatment, two had underlying disease explaining the changes and in only three patients out of 1549 (0.2%) could hepatic changes be attributed to
erythromycin acistrate therapy. These changes were reversible. The results demonstrate the hepatic safety of
erythromycin acistrate in clinical practice. Concomitant food intake did not affect the safety profile.