Patient w/ cardiac abnormalities, cerebral cysticercosis, history of epilepsy and/or other signs of potential CNS involvement (e.g. subcutaneous nodules suggestive of cysticercosis). Moderate to severe hepatic impairment. Pregnancy.
This drug may cause dizziness or drowsiness, if affected, do not drive or operate machinery during or 24 hr after treatment.
Monitor LFTs; patients w/ cardiac irregularities during therapy; monitor for seizures; culture urine or faeces for ova prior to treatment.
CYP enzyme-inducing drugs (e.g. carbamazepine, dexamethasone, phenobarbital, phenytoin) may decrease plasma concentrations of praziquantel. CYP enzyme inhibitors (e.g. cimetidine, erythromycin, itraconazole, ketoconazole) may increase plasma concentrations of praziquantel. Potentially Fatal: Concomitant use w/ rifampicin may cause subtherapeutic concentrations of praziquantel.
Description: Mechanism of Action: Praziquantel is a pyrazinoisoquinoline anthelmintic agent w/ a broad spectrum of activity against trematodes (flukes) and cestodes (tapeworms). It increases the cell permeability to Ca in schistosomes, causing strong contractions and paralysis of worm musculature leading to detachment of suckers from the blood vessel walls and to dislodgement. Pharmacokinetics: Absorption: Rapidly absorbed from the GI tract (>80%). Time to peak plasma concentration: 1-4 hr. Distribution: Distributed into the CSF and enters breast milk. Plasma protein binding: Approx 80%. Metabolism: Undergoes rapid and extensive hepatic metabolism via hydroxylation by CYP2B1 and CYP3A4 isoenzymes to inactive metabolites. Excretion: Via urine, mainly as metabolites. Plasma elimination half-life: Approx 1-1.5 hr (parent drug); approx 4 hr (metabolites).
P02BA01 - praziquantel ; Belongs to the class of quinoline derivatives and related substances used as antitrematodals.
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