Abstract: Cyclosporine A (CSA) is an immunosuppressant drug, metabolized mainly by CYP3A4 that is one of the Cytochrome P450 enzymes. Clindamycin (CLN) is a lincosamide antibiotic, inducing CYP3A4 activity in vitro and thereby may alter CSA pharmacokinetics (PK). The current research was performed to investigate the PK parameters changes of CSA up on co-administrating with CLN in healthy male rabbits. Twelve healthy male rabbits randomly were selected and divided into two groups: Control set (n=6) in which the rabbits were received oral normal saline CSA solution (10 mg/kg/day), meanwhile rabbits in the test group (n=6) were treated with oral normal saline CSA solution (10 mg/kg/day) concomitantly with normal saline solution of CLN (8 mg/kg/day) at the same time for 7 days. Blood samples (2 mL) were collected and CSA concentrations were measured in whole blood at the predetermined time points by using Chemiluminescenct Immunoassay (CLIA) detection kit. PK proﬁles of CSA for both groups in the control and test groups including Cmax, tmax, AUC0-24, AUC0-∞, t½ and Ke were compared. The results showed a statistically insignificant differences in the PK parameters of CSA alone or combined with CLN with P>0.05. In conclusion, it has been found that CLN does not affect the CSA PK. Further confirmation of our findings is requiered in humans before these results can be applied in patient care.
Key words: Cyclosporine, clindamycin, drug interaction, pharmacokinetic, CYP3A4