Enantiomers of sulfoxide of albendazole: cerebrospinal fluid and plasma levels and therapeutic efficacy in the treatment of patients with neurocysticercosis

THESES

Enantiomers of sulfoxide of albendazole: cerebrospinal fluid and plasma levels and therapeutic efficacy in the treatment of patients with neurocysticercosis (Abstract)^*. Thesis. Ribeirão Preto, 2003.

Newton Satoru Odashima^**

Neurocysticercosis (NCC) is a severe problem of public health in the developing countries that acquires special concern in our region, where it is an endemic disease with proteiform manifestations and high mortality and morbidity. As well as the advance in the field of diagnosis through computerized tomography (CT), nuclear magnetic resonance (MRI) and the study of cerebrospinal fluid (CSF), the development of effective medicines against the parasite has been propitiating adequate treatment to a lot of cases, while the albendazole is regarded as the first choice medicine. The sulfoxide of albendazole, the main metabolite of albendazole, is a chiral compound. So far, the exact influence of each enantiomer in the eradication of parasite in human being is unknown.

The present study aimed the analysis of the concentration of albendazole metabolites (sulfoxide of albendazole + and -), in plasma and CSF of patients with active neurocysticercosis, searching for an correlation between that concentrations and efficacy of treatment.

The group of patients was composed by 25 adults, 14 of which showed only parenchymal cystic lesions, 7 indicated only extraparenchymal lesions and 4 cases with coexistence of intra and extraparenchymal lesions. The number of lesions was defined by CT and/or MRI before and after the minimum period of 6 months from the beginning of the treatment which consisted in albendazole (dose of 15 mg/kg/day during 8 days).

The samples of sera and CSF were collected in the steady state, through the dose interval of 8 and 12 hours.

Among the 18 cases with parenchymal cysts, 11 cases presented total resolution of the lesions and 7 cases partial resolution. The respective mean concentration of albendazole sulfoxide dextrogyre in CSF were 145.7 ng/ml and 58.0 ng/ml. Among the 11 cases with extraparenchymal cysts, 4 cases had response to the treatment and 7 cases showed no difference after the treatment. All the metabolites studied in plasma or CSF demonstrated higher concentrations in the group with response.

This study suggests that in the treatment of patients with parenchymal forms of the disease, the higher concentrations in the CSF of (+) albendazole sulfoxide were correlated with higher efficacy. In the group with extraparenchymal lesions we were not able to link any enantiomer with a higher efficacy. However, it was clear that the doses of medication must be adjusted as long as the lower levels of metabolites were associated with failure in treatment.

Key words: central nervous system cysticercosis, treatment, sulfoxide of albendazole, enantiomers.

*

Avaliação dos níveis de enantiômeros de sulfóxido de albendazol no LCR e plasma na eficácia terapêutica da neurocisticercose (Resumo). Tese de Doutorado, Universidade de São Paulo (Área: Neurologia). Orientador: Osvaldo Massaiti Takayanagui

**

Address: Departamento de Neurologia, Hospital das Clínicas da FMRP, Campus Universitário USP, 14048-900 Ribeirão Preto SP - Brasil

Publication Dates

• Publication in this collection
  22 Sept 2008
• Date of issue
  June 2003