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Pronunciation
(pray zi KWON tel)
Generic Available (U.S.)
No
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Use: Labeled Indications
Treatment of all stages of schistosomiasis caused by all Schistosoma species; treatment of infection (clonorchiasis and opisthorchiasis) due to liver flukes
Use: Unlabeled
Cysticercosis and many intestinal tapeworms
Pregnancy Risk Factor
B
Pregnancy Considerations
Adverse effects have not been observed in animal reproduction studies. There are no adequate and well-controlled studies in pregnant women. Use in pregnant women only if clearly needed.
Lactation
Enters breast milk/not recommended
Breast-Feeding Considerations
Appears in breast milk at a concentration of ¼ that of maternal serum. Women should be advised to not breast-feed on the day of treatment and for 72 hours after treatment.
Contraindications
Hypersensitivity to praziquantel or any component of the formulation; ocular cysticercosis; concurrent use with strong CYP3A4 inducers, particularly rifampin
Warnings/Precautions
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with cardiac abnormalities.
• Cerebral cysticercosis: Patients with cerebral cysticercosis require hospitalization.
• Hepatic impairment: Use with caution in patients with moderate-to-severe hepatic impairment.
• 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:
• Strong inducers of cytochrome P450: Therapeutic levels of praziquantel may not be achieved with concurrent administration of strong inducers of cytochrome P450 (eg, rifampin); concurrent use is contraindicated.
Other warnings/precautions:
• Patient information: Patients should be instructed to not drive or operate machinery on the day of treatment and the day after treatment.
Adverse Reactions
Frequency not defined.
Central nervous system: Dizziness, fever, headache, malaise
Dermatologic: Urticaria (rare)
Gastrointestinal: Abdominal discomfort, nausea
Postmarketing and/or case reports: Allergic reaction, anorexia, arrhythmia, AV block, bloody diarrhea, bradycardia, ectopic rhythms, eosinophilia, hypersensitivity, liver enzymes increased, myalgia, polyserositis, pruritus, seizure, somnolence, ventricular fibrillation, vertigo, vomiting, weakness
Metabolism/Transport Effects
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits CYP2D6 (weak)
Drug Interactions
Aminoquinolines (Antimalarial): May decrease the serum concentration of Anthelmintics. Risk C: Monitor therapy
Cimetidine: May increase the serum concentration of Praziquantel. Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Risk X: Avoid combination
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. Risk X: Avoid combination
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Risk D: Consider therapy modification
Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Herbs (CYP3A4 Inducers): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
Ketoconazole: May increase the serum concentration of Praziquantel. Management: Praziquantel dose may need to be reduced when used with ketoconazole. Risk D: Consider therapy modification
Ketoconazole (Systemic): May increase the serum concentration of Praziquantel. Management: Praziquantel dose may need to be reduced when used with ketoconazole. Risk D: Consider therapy modification
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Storage
Store below 30°C (86°F).
Mechanism of Action
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
Pharmacodynamics/Kinetics
Absorption: Oral: 80%
Protein binding: ~80%
Metabolism: Extensive first-pass effect
Half-life elimination: Parent drug: 0.8-1.5 hours; Metabolites: 4.5 hours
Time to peak, serum: 1-3 hours
Excretion: Urine ~80% (>99% as metabolites)
Dosage
Oral: Children ≥4 years and Adults:
Schistosomiasis: 20 mg/kg/dose 3 times/day for 1 day at 4- to 6-hour intervals
Clonorchiasis/opisthorchiasis: 25 mg/kg/dose 3 times/day for 1 day at 4- to 6-hour intervals
Cysticercosis (unlabeled use): 50 mg/kg/day divided every 8 hours for 14 days (Takayanagui, 2004)
Tapeworms (unlabeled use): 5-10 mg/kg as a single dose (25 mg/kg for Hymenolepis nana) (Liu, 1996)
Administration: Oral
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.
Monitoring Parameters
Culture urine or feces for ova prior to instituting therapy
Patient Education
Tablets may be halved or quartered; do not chew. Increase dietary intake of fruit juices. All family members and close friends should also be treated. To reduce possibility of reinfection, wash hands and scrub nails carefully with soap and hot water before handling food, before eating, and before and after toileting. Keep hands out of mouth. Disinfect toilet daily and launder bed linens, undergarments, and nightclothes daily with hot water and soap. Do not go barefoot and do not sit directly on grass or ground. May cause dizziness, fainting, lightheadedness, abdominal pain, nausea, or vomiting. Report unusual fatigue, persistent dizziness, CNS changes, change in color of urine or stool, or easy bruising or unusual bleeding.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause dizziness or drowsiness
Mental Health: Effects on Psychiatric Treatment
None reported
Nursing: Physical Assessment/Monitoring
Worm infestations are easily transmitted; all close family members should be treated. Instruct patient/caregiver on transmission prevention.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, oral:
Biltricide®: 600 mg [scored]
Pricing: U.S. (www.drugstore.com)
Tablets (Biltricide)
600 mg (6): $93.22
References
Garcia HH, Evans CAW, Nash TE, et al, “Current Consensus Guidelines for Treatment of Neurocysticercosis,” Clin Microbiol Rev, 2002, 15(4):747-56.
Liu LX and Weller PF, “Antiparasitic Drug,” N Engl J Med, 1996, 334(18):1178-84.
Takayanagui OM, “Therapy for Neurocysticercosis,” Expert Rev Neurother, 2004, 4(1):129-39.
International Brand Names
Lexi-Comp.com
Last full review/revision January 2012
Content last modified January 2012
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