Effect of aprepitant on pharmacokinetics of cancer chemotherapy patients with oral oxycodone controlled release tablets
- VernacularTitle:阿瑞匹坦对癌症化疗患者口服羟考酮控释片药代动力学的影响
- Author:
Shaozhi WANG
;
Lianhai CHAI
;
Yong ZHANG
;
Zhihong QIU
- Publication Type:Journal Article
- Keywords:
aprepitant;
oxycodone;
pharmacokinetics
- From:
Chinese Journal of Biochemical Pharmaceutics
2015;(6):133-136
- CountryChina
- Language:Chinese
-
Abstract:
Objective To investigate effect of the mild CYP3A4 inhibitor aprepitant on the pharmacokinetics of orally administered controlled-release ( CR) oxycodone.Methods This study designed was an single-sequence with two phases in cancer patients with pain who continued to be administered orally with multiple doses of CR oxycodone every 8 or 12 hours.Plasma concentration of oxycodone and its metabolites were measured up to 8 hours after administration as follows: on day 1, CR oxycodone was administered alone; on day 2, CR oxycodone was administered with aprepitant (125 mg, at the same time of oxycodone dosing in the morning).The steady-state trough concentrations ( Css) were measured from day 1 to day 3.Results Aprepitant increased the area under the plasma concentration-time curve (AUC0-8) of oxycodone by 25%(P<0.001) and of oxymorphone by 34% (P<0.001), as well as decreased the AUC0-8 of noroxycodone by 14% (P<0.001).Moreover, aprepitant increased Css of oxycodone by 57%(P=0.001) and of oxymorphone by 36% (P <0.001) and decreased Css of noroxycodone by 24% (P =0.02) at day 3 compared to day 1.Conclusion The clinical use of aprepitant in patients receiving multiple doses of CR oxycodone for cancer pain significantly altered plasma concentration levels, but would not appear to need modification of the CR oxycodone dose.
