抗真菌药物对人肝微粒体中齐多夫定葡萄糖醛酸化的比较作用。
Comparative effects of antifungal agents on zidovudine glucuronidation by human liver microsomes.
作者信息
Sampol E, Lacarelle B, Rajaonarison J F, Catalin J, Durand A
机构信息
Laboratoire de pharmacocinétique, Faculté de pharmacie, Marseille, France.
出版信息
Br J Clin Pharmacol. 1995 Jul;40(1):83-6. doi: 10.1111/j.1365-2125.1995.tb04540.x.
Abstract
Zidovudine (ZDV) is extensively metabolised by the liver to an inactive glucuronide (GZDV). Since ZDV is often administered with antimycotic drugs, we studied the effect of six systemic antifungal agents on the in vitro glucuronidation of ZDV by human liver microsomes. 5-fluorocytosine and itraconazole had no inhibitory effect whereas amphotericine B, ketoconazole, miconazole and fluconazole inhibited in vitro GZDV formation (Ki values were 0.13, 0.08, 0.18 and 1.4 mM respectively).
摘要
齐多夫定（ZDV）在肝脏中广泛代谢为无活性的葡萄糖醛酸苷（GZDV）。由于ZDV常与抗真菌药物联合使用，我们研究了六种全身性抗真菌剂对人肝微粒体体外ZDV葡萄糖醛酸化的影响。5-氟胞嘧啶和伊曲康唑无抑制作用，而两性霉素B、酮康唑、咪康唑和氟康唑抑制体外GZDV的形成（Ki值分别为0.13、0.08、0.18和1.4 mM）。
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