Perfect J R, Wright K A, Hobbs M M, Durack D T
Department of Medicine, Duke University Medical Center, Durham, North Carolina 27710.
Antimicrob Agents Chemother. 1989 Oct;33(10):1735-40. doi: 10.1128/AAC.33.10.1735.
We studied the pharmacokinetics and in vivo antifungal action of SCH39304, a new antifungal azole compound, in rabbits. It crossed the blood-cerebrospinal fluid barrier in the presence or absence of meningeal inflammation, reaching approximately 60% of the simultaneous concentrations in serum. In the treatment of experimental cryptococcal meningitis, SCH39304 was as effective as fluconazole in reducing yeast counts in the subarachnoid space. SCH39304 and fluconazole both were highly effective against candida endophthalmitis, sterilizing the vitreous humor and the choroid and retina. SCH39304 suppressed candida endocarditis and reduced yeast counts in the kidney at all doses tested. SCH39304 was effective in the treatment of experimental cryptococcal meningitis and disseminated candidiasis. Further investigations in humans are warranted.
我们在兔体内研究了新型抗真菌唑类化合物SCH39304的药代动力学及体内抗真菌作用。无论有无脑膜炎症,它均可穿过血脑屏障,其浓度约为同时期血清浓度的60%。在治疗实验性隐球菌性脑膜炎时,SCH39304在降低蛛网膜下腔酵母菌数量方面与氟康唑效果相当。SCH39304和氟康唑对念珠菌性眼内炎均有高效,可使玻璃体液、脉络膜和视网膜除菌。在所有测试剂量下,SCH39304均可抑制念珠菌性心内膜炎并减少肾脏中的酵母菌数量。SCH39304对实验性隐球菌性脑膜炎和播散性念珠菌病的治疗有效。有必要在人体中进行进一步研究。