重视中药作用于肠道CYP3A4、P-gp后对口服药物生物利用度的影响

Bioavailability of Oral Drugs Following Chinese Materia Medica's Action on CYP3A4 and P-gp in Intestine

目的:提高中西药品联合使用的合理性。方法:归纳中药或中药化学成分对肠道细胞色素P450酶3A4(CYP3A4)及P-糖蛋白(P-gp)的抑制或诱导作用而改变口服底物药物生物利用度参数的机制,并结合文献资料分析说明。结果:五味子、当归、吴茱萸次碱、银杏内酯A等对CYP3A4有抑制或诱导作用;黄芩、贯叶连翘、柚皮素、金丝桃素等对P-gp有抑制或诱导作用。中药及中药化学成分作用肠道CYP3A4、P-gp对底物药物生物利用度参数的改变作用,可影响药品使用的安全性和有效性。结论:临床医药专业技术人员应重视中西药联合使用中存在的药物相互作用,才能促进用药合理性的提高。

OBJECTIVE： To promote rational combined use of Chinese Chinese materia medica with western medicines. METHODS： The mechanisms for Chinese materia medica and its chemical compositions to change the bioavailability of orally taken substrates by its inhibiting or inducing intestinal CYP3A4 and P- gp were summarized, and which were analyzed by combining the literature. RESULTS： Fructus Schisandrae, Radix Angelicae Dahuricae, Radix Angelicae Sinensis, Rutae- earpine, Ginkgolide A etc could inhibit or induce the CYP3A4 enzyme; Radix Scutellariae, common St.Johnwort herb with root, Naringenin, Hypericin etc could inhibit or induce P - gp. The change of the parameters of the bioavailability of substrate drugs caused by Chinese materia medica and its chemical compositions through acting on intestinal CYP3A4 and P - gp could influence the drug safety and efficacy. CONCLUSION： Clinicians and pharmacists should attach importance to the drug interactions in the concomitant use of Chinese traditional medicines and western drugs so as to promote rational drug use.