Abstract: AIM: To evaluate the effects of Danshen Injection on rabbit cytochrome P450 (CYP450) activity by Cocktail probe drugs.METHODS: Male rabbits were randomly divided into three test groups and one control group. The test groups were treated with Danshen Injection (i.v.) at three dosages (low, midst and high dosage), and the control group was treated with physiological saline. The plasma concentrations of probe drugs(caffeine,metoprolol and dapsone) were determined by HPLC. Effects of Danshen Injection on CYP450 activity were observed by comparing the concentration-time curves and pharmacokinetic parameters of probe drugs. RESULTS: The three dosages of Danshen Injection inhibited the CYP2D6 activity(P＜0.05, or P＜0.01), but had no effects on the activities of CYP1A2 and CYP3A4. CONCLUSION: Danshen Injection can inhibit CYP2D6 activity in rabbit, but has no effect on CYP1A2 and CYP3A4. When Danshen Injection is used in clinic, attention should be paid to the inhibition effect on CYP2D6 to avoid CYP2D6-mediated drug interaction, and to promote safe and rational drug use.

Key words: Cytochrome P450(CYP450), Danshen Injection, Cocktail probe drugs