Rieth H, Sauerbrey N
Medizinischen Abteilung der Pfizer GmbH, Karlsruhe, BRD.
Wien Med Wochenschr. 1989 Aug 31;139(15-16):370-4.
Fluconazole is a new systemic antifungal agent from the class of triazoles. Its efficacy was documented in clinical studies of patients with candidosis and cryptococcosis. Due to the influence on human cytochrome-P-450-dependent enzymes, special attention should be paid, in the development of new antifungal agents, to the inhibition of the metabolization of other simultaneously given substances and to the inhibition of steroid hormone synthesis in the gonads and adrenal glands. The interaction studies carried out with frequently administered drugs such as oral contraceptives, cimetidine, warfarin, tolbutamide, and cyclosporin (transplantation patients) allow the concomitant intake of these substances with fluconazole. Concomitant anti-coagulant treatment requires a precautionary monitoring of prothrombin time; it may be necessary in individual cases to reduce the anticoagulant dosage. The intake of oral hypoglycemics of the tolbutamide type requires monitoring of blood glucose, although blood glucose lowering effects were not found. One interaction study carried out with phenazone showed the low metabolization tendency of fluconazole. Approximately 80% of the administered fluconazole dose appeared in the urine unchanged. Studies in male and female subjects with multiple doses of fluconazole (4 weeks) did not show any significant effects on the endocrinology and steroid synthesis in man.
氟康唑是一种新型的三唑类全身性抗真菌药。其疗效已在念珠菌病和隐球菌病患者的临床研究中得到证实。由于其对人细胞色素P - 450依赖性酶有影响,在开发新型抗真菌药时,应特别关注其对同时服用的其他物质代谢的抑制作用以及对性腺和肾上腺类固醇激素合成的抑制作用。与常用药物如口服避孕药、西咪替丁、华法林、甲苯磺丁脲和环孢素(移植患者)进行的相互作用研究表明,这些物质可与氟康唑同时服用。同时进行抗凝治疗时,需要对凝血酶原时间进行预防性监测;个别情况下可能需要减少抗凝剂剂量。虽然未发现降血糖作用,但服用甲苯磺丁脲类口服降糖药时需要监测血糖。与非那宗进行的一项相互作用研究表明氟康唑的代谢倾向较低。所给予的氟康唑剂量约80%以原形出现在尿液中。对男性和女性受试者多次服用氟康唑(4周)的研究未显示对人体内分泌学和类固醇合成有任何显著影响。