High-dose praziquantel for neurocysticercosis: serum and CSF concentrations

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Abstract
Serum and CSF concentrations of praziquantel were analyzed in 8 patients with active neurocysticercosis aged 35 .+-. 16 (mean .+-. sd) years, in order to determine factors that may improve the therapeutic ratio. Praziquantel was given orally at 6-h intervals for 10 days at a daily dose of 100 mg/kg. Serum concentrations were determined at 1, 2 and 4 h, and CSF concentrations at 2 h after the morning dose. Peak serum contentrations occurred between 1 and 2 h after administration. There was a trend towards a drop in serum concentration from Days 1 through 5 to 10 of therapy. A fourfold increase in oral dose led to an eightfold rise in serum and CSF concentration, indicating saturation of hepatic metabolism. There were linear correlations (p < 0.01) between serum and CSF concentrations of praziquantel, indicating free flow across the blood-brain barrier, above an apparent threshold, which may be related to occupation of plasma protein-binding sites. The results indicate that monitoring of serum concentrations may be clinically useful.

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