History

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Praziquantel was developed in the laboratories for parasitological research of Bayer AG in Germany (Elberfeld) 30 years ago (in the mid 1970's). Since then it has proven indispensable in more and more indications and is recognized as such by the World Health Organization.

Pharmacokinetics

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Praziquantel is well (approximately 80%) absorbed from the GI Tract. Due to extensive first pass metabolization only relatively small amounts enter systemic circulation. Praziquantel has a serum halflife of 0.8 to 1.5 hours (metabolites 4 to 5 hours) in adults with normal renal and liver function. In patients with significantly impaired liver function (Child Pugh classes B and C) the serum halflife is increased to 3 to 8 hours. Praziquantel and its metabolites are mainly excreted in the urine, within 24 hours after a single oral dose 70 to 80% are recovered in urine, but less than 0.1% are found as the unchanged drug.

Mode of Action

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Although the mode of action is not exactly known presently, there is experimental evidence that Praziquantel increases the permeability of the membranes of parasite cells (certain schistosomes) for calcium ions. The drug thereby induces contraction of the parasites resulting in paralysis in the contracted state. The dying parasites are dislodged from their site of action in the host organism and may enter systemic circulation or may be destroyed by host immune reaction (phagocytosis). Additional mechanisms - focal disintegrations and disturbances of oviposition (laying of eggs) - are seen in other types of sensitive parasites.

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