Clindamycinの代謝に関する研究
1970 年 18 巻 8 号 p. 1025-1030
詳細
1970 年 18 巻 8 号 p. 1025-1030
The metabolism of clindamycin, a new lincomycin derivative, was investigated and the following results were obtained.
1) A part of clindamycin is changed into N-demethyl-clindamycin in rats and dogs.
2) One hour blood level of rats with 80 mg/kg phenobarbital pretreatment is higher than those without treatment, andin vitroinactivation study showed the activity in the liver of rat treated as above is less decreased than those non-treated. These studies seem to indicate that a part of clindamycin is metabolized rapidly to the more active N-demethyl-clindamycin in rats pretreated with phenobarbital.
3) N-Demethyl-clindamycin was not found in dog plasma at five hours after 100 mg/kg intravenous administration. Biliary and urinary excretion studies showed as follows : biliary excretion, 1.4-4.4 mcg/ml. urinary recovery, O. 035% of administrated clindamycin.
4) The antibacterial activity of N-demethyl-clindamycin is about two times active than that of clindamycinin vitro. In comparison with clindamycin there is no difference in antibacterial spectrum.
5) It seems that N-demethyl-clindamycin is not directly responsible for the slight histological degeneration, which was found in rat liver after large dose clindamycin administration.
