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.2002 Aug;54(2):125-30.
doi: 10.1046/j.1365-2125.2002.01634.x.

Enantioselective distribution of albendazole metabolites in cerebrospinal fluid of patients with neurocysticercosis

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Enantioselective distribution of albendazole metabolites in cerebrospinal fluid of patients with neurocysticercosis

O M Takayanagui et al. Br J Clin Pharmacol.2002 Aug.

Abstract

Aims: Albendazole (ABZ) is effective in the treatment of neurocysticercosis. ABZ undergoes extensive metabolism to (+) and (-)-albendazole sulphoxide (ASOX), which are further metabolized to albendazole sulphone (ASON). We have investigated the distribution of (+)-ASOX (-)-ASOX, and ASON in cerebrospinal fluid (CSF) of patients with neurocysticercosis.

Methods: Twelve patients with a diagnosis of active brain parenchymal neurocysticercosis treated with albendazole for 8 days (15 mg kg(-1) day(-1)) were investigated. On day 8, serial blood samples were collected during the dose interval (0-12 h) and one CSF sample was taken from each patient by lumbar puncture at different time points up to 12 h after the last albendazole dose. Albendazole metabolites were determined in CSF and plasma samples by h.p.l.c. using a Chiralpak AD column and fluorescence detection. Population curves for CSF albendazole metabolite concentration vs time were constructed.

Results: The mean plasma/CSF ratios were 2.6 (95% CI: 1.9, 3.3) for (+)-ASOX and 2.7 (95% CI: 1.8, 3.7) for (-)-ASOX, with the two-tailed P value of 0.9873 being non-significant. These data indicate that the transport of ASOX through the blood-brain barrier is not enantioselective, but rather depends on passive diffusion. The present results suggest the accumulation of the (+)-ASOX metabolite in the CSF of patients with neurocysticercosis. The CSF AUC(+)/AUC(-) ratio was 3.4 for patients receiving albendazole every 12 h. The elimination half-life of both ASOX enantiomers in CSF was 2.5 h. ASOX was the predominant metabolite in the CSF compared with ASON; the CSF AUC(ASOX)/AUC(ASON) ratio was approximately 20 and the elimination half-life of ASON in CSF was 2.6 h.

Conclusions: We have demonstrated accumulation of the (+)-ASOX metabolite in CSF, which was about three times greater than the (-) antipode. ASOX concentrations were approximately 20 times higher than those observed for the ASON metabolite.

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Figure 1
Figure 1
CSF concentrationsvs time population curves for (+)-ASOX (−)-ASOX and ASON for 12 patients with neurocysticercosis after treatment for 8 days with albendazole at the dose of 7.5 mg/12 h (only one CSF sample was collected from each patient at different time points during the dose interval).
Figure 2
Figure 2
Plasma concentrationsvs time curves for (+)-ASOX (▪), (−)-ASOX (•) and ASON (▴). Data presented as mean±s.e. mean for 12 patients with neurocysticercosis after treatment for 8 days with albendazole (7.5 mg/12 h).
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