Drug information of Praziquantel
Mechanism of effect
Increases cell membrane permeability to calcium in schistosomes causing the worm to dislodge following the paralysis of worm musculature
Praziquantel effects the permeability of the cell membrane resulting in the contraction of schistosomes. The drug further causes vacuolization and disintegration of the schistosome tegument. The effect is more marked on adult worms compared to young worms.
An increased calcium influx may play an important role. Secondary effects are inhibition of glucose uptake, lowering of glycogen levels and stimulation of lactate release. The action of praziquantel is limited very specifically to trematodes and cestodes; nematodes (including filariae) are not affected.
Absorption: ~80% (oral)
Distribution: CSF concentration is 14-20% of plasma concentration
Protein Bound: ~80%
Metabolism: Extensive first-pass effect
Half-life 0.8-1.5 hr (parent drug); 4.5 hr (metabolites)
Peak Plasma Time: 1-3 hr
Excretion: Urine (99% as metabolites)
20 mg/kg PO TID for 1 day (at intervals 4-6 hr)
75 mg/kg/d divided PO TID for 1 day (at intervals 4-6 hr)
<4 years: Safety and efficacy not established
≥4 years: 20 mg/kg PO TID for 1 day (at intervals 4-6 hr)
< 4 years: Safety and efficacy not established
≥4 years: 75 mg/kg/d divided PO TID for 1 day (at intervals 4-6 hr)
Drug contraindicationshypersensitivity to this drug
Side effectsDiarrhea , Headache , nausea , vomiting , vertigo , urticaria , fever , itching , difficulty urinating , Abdominal pain , Rash , Appetite suppression
InteractionsRifabutin , Rifapentine , Albendazol , Oxecarbazepin , Bosentan , Primidone , Tenofovir , Rifampin , Pentobarbital , Chloroquine , Fosphenytoin , nafcillin , Cimetidine , Phenobarbital , Phenytoin , Hydroxychloroquine , Carbamazepine , Enzalutamide , Efavirenz , Etravirine , Dabrafenib
Coadministration with moderate CYP3A4 inducers (eg, phenytoin, phenobarbital, carbamazepine, dexamethasone) may reduce blood levels
Use with caution in patients with cardiac abnormalities.
It is recommended to hospitalize patients with cerebral cysticercosis for the duration of treatment.
Use with caution in patients with moderate-to-severe hepatic impairment
Use not recommended in patients with a history of seizures or signs of central nervous system involvement .
Points of recommendation
Swallow quickly with water, otherwise risk of regurgitation due to bitter taste
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