Perfect J R, Savani D V, Durack D T
Antimicrob Agents Chemother. 1986 Apr;29(4):579-83. doi: 10.1128/AAC.29.4.579.
Itraconazole and fluconazole, two new triazoles, were examined for their antifungal activity in rabbits. Fluconazole easily crossed the blood-cerebrospinal fluid barrier, and active drug was eliminated in high concentrations in the urine. On the other hand, itraconazole did not cross the blood-cerebrospinal fluid barrier in measurable amounts, and urine concentrations were variable. Despite differences in pharmacokinetics at the site of infection, both agents were equally effective in treating cryptococcal meningitis and candida pyelonephritis in animals. By using a ketoconazole-resistant strain of Candida albicans, we showed that there was cross-resistance in vivo between these two new triazole compounds.
对两种新型三唑类药物伊曲康唑和氟康唑在兔体内的抗真菌活性进行了研究。氟康唑易于穿过血脑脊髓液屏障,活性药物在尿液中以高浓度排出。另一方面,伊曲康唑未能以可测量的量穿过血脑脊髓液屏障,尿液浓度也各不相同。尽管在感染部位的药代动力学存在差异,但这两种药物在治疗动物隐球菌性脑膜炎和念珠菌性肾盂肾炎方面同样有效。通过使用对酮康唑耐药的白色念珠菌菌株,我们表明这两种新型三唑类化合物在体内存在交叉耐药性。