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praziquantel (Biltricide)

 

Classes: Anthelmintics

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)