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Phenytoin and carbamazepine decrease oral bioavailability of praziquantel

Clinical Neurology Unit, Hospital Nossa Senhora das Graças, Curitiba, Brazil (Drs. Bittencourt and Gracia)
Department of Medicine, Merck Indústries Químicas, Rio de Janeiro, Brazil (Drs. Martins and Fernandes)
Merck Institut für Experimentelle Arsneimittelforschung, Grafing, Germany (Drs. Diekmann and Jung)
Central Scientific Services, E. Merck, Darmstadt, Germany (Drs. Diekmann and Jung).

Antiepileptic drugs, especially carbamazepine and phenytoin, are potent liver enzyme inducers. Since praziquantel, the drug used to treat neurocysticercosis, undergoes extensive liver first-pass metabolism, we carried out a prospective study to verify whether there was a decrease in oral bioavailability induced by carbamazepine and phenytoin. Carbamazepine and phenytoin significantly decreased concentrations of praziquantel, due to increased clearance secondary to induction of first pass-liver metabolism. The magnitude of the decrease is surprisingly high and may be responsible for failures of treatment.

Address correspondence and reprint requests to Prof. P.R.M. Bittencourt, Hospital Nossa Senhora das Graças, Rua Alcides Munhoz, 433, 80510 Curitiba, Brazil.

Funded by a specific grant of E. Merck, of Darmstadt, Germany.

Received June 20, 1991. Accepted for publication in final form November 12, 1991.

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