(pray zi KWON tel)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Biltricide: 600 mg [scored]
Brand Names: U.S.
Increases the cell permeability to calcium in schistosomes, causing strong contractions and paralysis of worm musculature leading to detachment of suckers from the blood vessel walls and to dislodgment
CSF concentration is 14% to 20% of plasma concentration
Extensive first-pass effect; metabolized by the liver to hydroxylated and conjugated metabolites
Urine ~80% (>99% as metabolites)
Time to Peak
Serum: 1-3 hours
Parent drug: 0.8-1.5 hours; Metabolites: 4.5 hours
Special Populations: Renal Function Impairment
Excretion may be delayed in patients with renal impairment, but accumulation of unchanged drug would not be expected.
Special Populations: Hepatic Function Impairment
Cmax, AUC, and half-life were significantly elevated in patients with moderate to severe liver impairment.
Use: Labeled Indications
Helminths: Treatment of infections caused by the following: All species of Schistosoma (eg, Schistosoma mekongi, S. japonicum, S. mansoni, S. hematobium) and the liver flukes Clonorchis sinensis/Opisthorchis viverrini
Cysticercosis and many intestinal tapeworms
Hypersensitivity to praziquantel or any component of the formulation; ocular cysticercosis; concomitant administration with strong cytochrome P450 (CYP450) inducers, such as rifampin
Schistosomiasis: Oral: 20 mg/kg/dose 3 times daily at 4- to 6-hour intervals for 1 day
Manufacturer’s labeling: 25 mg/kg/dose 3 times daily at 4- to 6-hour intervals for 1 day
Alternate recommendations (off-label dose): 25 mg/kg/dose 3 times daily for 2 days (Drugs for Parasitic Infections 2013)
Cysticercosis (off-label use): Oral: 50 mg/kg/day divided every 8 hours for 14 days (Takayanagui, 2004)
Tapeworms (off-label use): Oral: 5-10 mg/kg as a single dose (25 mg/kg for Hymenolepis nana) (Liu, 1996)
Refer to adult dosing.
Children ≥4 years and Adolescents: Refer to adult dosing.
Dosing: Renal Impairment
No dosage adjustment necessary.
Dosing: Hepatic Impairment
There are no dosage adjustments provided in manufacturer’s labeling. However, total drug exposure in moderate-to-severe impairment is increased.
Administer tablets with water during meals. Tablets should be promptly swallowed to avoid bitter taste that may cause gagging or vomiting. Tablets may be halved or quartered; do not chew.
Store below 30°C (86°F).
Aminoquinolines (Antimalarial): May decrease the serum concentration of Anthelmintics. Monitor therapy
ARIPiprazole: CYP2D6 Inhibitors (Weak) may increase the serum concentration of ARIPiprazole. Management: Monitor for increased aripiprazole pharmacologic effects. Aripiprazole dose adjustments may or may not be required based on concomitant therapy and/or indication. Consult full interaction monograph for specific recommendations. Monitor therapy
Bosentan: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Cimetidine: May increase the serum concentration of Praziquantel. Monitor therapy
CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
CYP3A4 Inducers (Strong): May decrease the serum concentration of Praziquantel. Management: Avoid concomitant use of praziquantel with strong CYP3A4 inducers. Discontinue rifampin 4 weeks prior to initiation of praziquantel therapy. Rifampin may be resumed the day following praziquantel completion. Avoid combination
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Praziquantel. Monitor therapy
Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates. Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification
Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Grapefruit Juice: May increase the serum concentration of Praziquantel. Monitor therapy
Osimertinib: May increase the serum concentration of CYP3A4 Substrates. Osimertinib may decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Siltuximab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
St John's Wort: May decrease the serum concentration of CYP3A4 Substrates. Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy
Frequency not defined. May be more frequent and/or serious in patients with a heavy worm burden.
Central nervous system: Dizziness, headache, malaise
Gastrointestinal: Abdominal distress, nausea
<1% (Limited to important or life-threatening): Abdominal pain, atrioventricular block, bloody diarrhea, bradycardia, cardiac arrhythmia, ectopic beats, eosinophilia, hypersensitivity, hypersensitivity reaction, myalgia, paradoxical reaction (in schistosomiasis), polyserositis, pruritus, seizure, serum sickness (in schistosomiasis; Jarisch-Herxheimer-like reaction), skin rash, ventricular fibrillation, vomiting
• Cardiovascular disease: Use with caution in patients with cardiac abnormalities.
• Cerebral cysticercosis: It is recommended to hospitalize patients with cerebral cysticercosis for the duration of treatment.
• Hepatic impairment: Use with caution in patients with moderate-to-severe hepatic impairment; reduced liver drug metabolism may result in higher and longer lasting plasma concentrations of unmetabolized praziquantel.
• Schistosomiasis: Praziquantel may not be effective against migrating shistosomulae; observational data indicate that praziquantel treatment in the acute phase of the infection may not prevent progression from asymptomatic to acute shistosomiasis, or from asymptomatic/acute disease to chronic disease. In addition, use in patients with shistosomiasis may be associated with clinical deterioration such as paradoxical reactions or serum sickness Jarisch-Herxheimer-like reactions, which is a sudden inflammatory immune response likely caused by the release of shistosomal antigens. Such reactions typically occur during the acute disease phase, and may lead to life-threatening events such as respiratory failure, encephalopathy, and/or cerebral vasculitis.
• Seizures: Use not recommended in patients with a history of seizures or signs of central nervous system involvement (eg, subcutaneous nodules suggestive of cysticercosis); may exacerbate condition.
Concurrent drug therapy issues:
• Drug/drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information. Therapeutic levels of praziquantel may not be achieved with concurrent administration of strong inducers of cytochrome P450 (eg, rifampin); concurrent use is contraindicated.
• Patient information: Patients should be instructed to not drive or operate machinery on the day of treatment and the day after treatment.
Liver function tests; monitor patients with cardiac irregularities during treatment; monitor for seizures; culture urine or feces for ova prior to instituting therapy
Pregnancy Risk Factor
Adverse effects have not been observed in animal reproduction studies. Use in pregnant women only if clearly needed.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience headache or dyspepsia. Have patient report immediately to prescriber severe dizziness or syncope (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.
More about praziquantel
- Other brands: Biltricide