Dosing and uses of Biltricide (praziquantel)
Adult dosage forms and strengths
tablet
- 600mg
Schistosomiasis
20 mg/kg PO TID for 1 day (at intervals 4-6 hr)
Clonorchiasis, Opisthorchiasis
75 mg/kg/d divided PO TID for 1 day (at intervals 4-6 hr)
Cysticercosis (Off-label)
50-100 mg/kg/d divided q8hr PO for 14 days
Flukes (Off-label)
75 mg/kg/d PO divided TID for 1-2 days
Tapeworms (Off-label)
5-10 mg/kg as single dose or 25 mg/kg if hymenolepis nana
Pediatric dosage forms and strengths
tablet
- 600mg
Schistosomiasis
<4 years: Safety and efficacy not established
≥4 years: 20 mg/kg PO TID for 1 day (at intervals 4-6 hr)
Clonorchiasis, Opisthorchiasis
< 4 years: Safety and efficacy not established
≥4 years: 75 mg/kg/d divided PO TID for 1 day (at intervals 4-6 hr)
Cysticercosis (Off-label)
<4 years: Safety and efficacy not established
≥4 years: 50-100 mg/kg/d divided TID PO for 30 days
Flukes (Off-label)
<4 years old: Safety and efficacy not established
≥4 years old: 75 mg/kg/d PO divided TID for 1-2 days
Tapeworms (Off-label)
<4 years old: Safety and efficacy not established
≥4 years old: 5-10 mg/kg as single dose or 25 mg/kg if hymenolepis nana
Biltricide (praziquantel) adverse (side) effects
1-10%
Appetite loss
Dizziness
Drowsiness
Headache
Malaise
CSF reaction syndrome in patients treated for neurocysticercosis
Abdominal pain
Nausea
Vomiting
Diaphoresis
<1%
Diarrhea
Fever
Itching
Rash
Urticaria
Postmarketing Reports
Eosinophilia
Pruritus, rash Abdominal pain, anorexia, bloody diarrhea, vomiting
Allergic reaction (generalized hypersensitivity, including polyserositis)
Arrhythmia (including bradycardia, ectopic rhythms, ventricular fibrillation, AV blocks)
Fatigue, somnolence, asthenia, vertigo
Convulsions
Myalgia
Warnings
Contraindications
Hypersensitivity
Intraocular cysticercosis
Strong CYP450 inducers
- Coadministration with strong CYP450 inducers (eg, rifampin) is contraindicated since therapeutically effective blood levels of praziquantel may not be achieved
- In patients receiving rifampin who need immediate treatment for schistosomiasis, alternative agents for schistosomiasis should be considered
- If treatment with praziquantel is necessary, rifampin should be discontinued 4 weeks before praziquantel administration
- Treatment with rifampin can be restarted 1 day after completion of praziquantel treatment
Cautions
Swallow quickly with water, otherwise risk of regurgitation due to bitter taste
Coadministration with moderate CYP3A4 inducers (eg, phenytoin, phenobarbital, carbamazepine, dexamethasone) may reduce blood levels
Pregnancy and lactation
Pregnancy category: B
Lactation: enters breast milk, do not nurse on the day of taking drug & 72 hr thereafter
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Biltricide (praziquantel)
Mechanism of action
Increases cell membrane permeability to calcium in schistosomes causing the worm to dislodge following the paralysis of worm musculature
Pharmacokinetics
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)