Source: Medicines and Medical Devices Safety Authority (NZ) Revision Year: 2017 Publisher: Bayer New Zealand Limited, 3 Argus Place, Hillcrest, North Shore, Auckland 0627, Free phone: 0800 233 988
Pharmacotherapeutic group: Antihelmintics
ATC code: P02BA01
Praziquantel is 2-(cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-4H-pyrazino (2,1a) isoquinolin-4-one. CAS Number: 55268-74-1
Praziquantel is a white crystalline powder of bitter taste. The compound is stable under normal conditions and melts at 136°C-140°C with decomposition. The active substance is hygroscopic. Praziquantel is easily soluble in chloroform and dimethylsulfoxide, soluble in ethanol and very slightly soluble in water. The molecular formula is C19H24N2O2.
The structural formula is as follows:
Animal studies show that praziquantel induces a rapid contraction of schistosomes by a specific effect on the permeability of the cell membrane. The medicine further causes vacuolisation and disintegration of the schistosome tegument. The effect is more marked on the adult than on young worms.
After oral administration praziquantel is rapidly absorbed (80%). It is, however, subject to first pass effect and extensive metabolism. One hour after administration approximately 6% only of the medicine in serum is in the unmetabolised form. Both the unchanged medicine and the metabolites are excreted primarily by the kidneys.Maximal serum concentration is achieved 1-3 hours after dosing. The half life of praziquantel in serum is 0.8-1.5 hours.
Preclinical data reveal no special hazard for humans based on studies of systemic toxicity, genotoxicity, carcinogenic potential, toxicity to reproduction.
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