Therapy for neurocysticercosis has advanced during the last 20 years with the advent of albendazole (Zentel) and praziquantel (Cysticide). Albendazole is the current medication of choice for the treatment of neurocysticercosis and is recommended for symptomatic patients with multiple viable cysts in the brain parenchyma. Albendazole may also be useful in extraparenchymal cysticercosis, especially in the subarachnoid racemose form, when complete surgical resection of the cysts is usually impracticable. Currently, there is an intense debate over the value and safety of anticysticercal therapy. Causes for failure of anticysticercal therapy include high inter-individual variability in plasma concentration of albendazole sulfoxide and the complex interactions of several drugs with the albendazole metabolite. Furthermore, albendazole sulfoxide is an enantiomeric mixture of (+)- and (-)-albendazole sulfoxide with accumulation of the (+)-enantiomer in the cerebrospinal fluid. However, the question over which enantiomer is effective against cysticerci remains to be clarified.