Enantioselective kinetic disposition of albendazole sulfoxide in patients with neurocysticercosis

Enantioselective kinetic disposition of albendazole sulfoxide in patients with neurocysticercosis

Author Marques, MPD Google Scholar
Takayanagui, O. M. Google Scholar
Bonato, P. S. Google Scholar
Santos, SRCJ Google Scholar
Lanchote, V. L. Google Scholar
Institution Universidade Federal de São Paulo (UNIFESP)
Universidade de São Paulo (USP)
Abstract The enantioselectivity of the kinetic disposition of albendazole sulfoxide (ASOX) was investigated in 18 patients with neurocysticercosis treated with a multiple dose regimen of albendazole for 8 days (5 mg/kg every 8 h). Serial blood samples were collected on the eighth day of treatment during the last dose interval, with prorogation up to 12 h. Albendazole sulfone (ASON) and enantiomers of ASOX were analyzed in plasma samples by HPLC using a Chiralpak(R) AD column and detection by fluorescence. the pharmacokinetic parameters showing statistically significant differences between the (+) ASOX and (-) ASOX enantiomers are presented as respective means (95% CI) as follows: maximum plasma concentration, C-max = 301.6 (179.7-423.5) vs 54.9 (21.9-87.9) ng.ml(-1); elimination half-life, t(1/2) = 5.2 (4.1-6.3) vs 3.3 (2.8-3.8) h, area under the plasma concentration-time curve, AUC(ss)(0-8) - 1719.2 (978.62-459.8) vs 261.4 (102.9-419.8) ng.h.ml(-1) and apparent clearance, Cl/fm = 5.8 (3.8-7.8) vs 54.0 (35.2-72.7) l.h(-1).kg(-1). the mean value of 9.2 (7.6-10.9) for the AUC((+)(0-8)-ASOX)/AUC((-)(0-8)-ASOX) ratio demonstrated plasma accumulation of the (+) enantiomer. Sulfone formation capacity, expressed by the AUC(ss)(0-8) ratio ASON/ASOX + ASON, was 8.0 (7.0-8.9). the present data indicate enantioselectivity in the kinetic disposition of ASOX in patients with neurocysticercosis. Chirality 11:218-223, 1999. (C) 1999 Wiley-Liss, Inc.
Keywords albendazole sulfoxide
enantioselectivity, pharmacokinetics, cysticercosis, metabolism
patient
Language English
Date 1999-01-01
Published in Chirality. New York: Wiley-liss, v. 11, n. 3, p. 218-223, 1999.
ISSN 0899-0042 (Sherpa/Romeo, impact factor)
Publisher Wiley-Blackwell
Extent 218-223
Origin http://dx.doi.org/10.1002/(SICI)1520-636X(1999)11:3<218
Access rights Closed access
Type Article
Web of Science ID WOS:000078845200008
URI http://repositorio.unifesp.br/handle/11600/26004

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