Burger D M, Kraayeveld C L, Meenhorst P L, Mulder J W, Hoetelmans R M, Koks C H, Beijnen J H
Department of Pharmacy, Slotervaart Hospital, Amsterdam, The Netherlands.
Pharm World Sci. 1995 Nov 24;17(6):218-21. doi: 10.1007/BF01870615.
It has been hypothesized that didanosine has a low efficacy in the prevention and treatment of patients with the dementia complex of acquired immunodeficiency syndrome (AIDS) because "... the drug has not been detected in the cerebrospinal fluid". We investigated didanosine concentrations in cerebrospinal fluid (CSF) and plasma of four patients with AIDS who were using didanosine chronically. Didanosine levels, 4 h after the last drug administration, averaged 0.16 (+/- 0.03) mumol/l in CSF and 0.70 (+/- 0.27) mumol/l in plasma. When compared with historical data from patients using zidovudine, didanosine concentrations in CSF appeared to be approximately half (on a molar base) those of zidovudine concentrations in the CSF. Whether this difference in CSF levels is the explanation for the presumed lower efficacy of didanosine in the prevention and treatment of AIDS dementia complex remains to be proven. However, it is clear from this study, in contrast with earlier suggestions, that didanosine is able to pass the blood-CSF barrier in human immunodeficiency virus-infected individuals.
据推测，去羟肌苷在预防和治疗获得性免疫缺陷综合征（AIDS）所致痴呆综合征患者方面疗效不佳，原因是“……在脑脊液中未检测到该药物”。我们调查了4例长期使用去羟肌苷的AIDS患者脑脊液（CSF）和血浆中的去羟肌苷浓度。末次给药4小时后，脑脊液中去羟肌苷水平平均为0.16（±0.03）μmol/L，血浆中为0.70（±0.27）μmol/L。与使用齐多夫定患者的历史数据相比，脑脊液中去羟肌苷浓度（以摩尔计）似乎约为齐多夫定脑脊液浓度的一半。脑脊液水平的这种差异是否能解释去羟肌苷在预防和治疗AIDS痴呆综合征方面疗效较低，仍有待证实。然而，与早期观点相反，本研究明确表明，去羟肌苷能够在人类免疫缺陷病毒感染个体中通过血脑屏障。
