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Pronunciation
(pray zi KWON tel)
U.S. Brand Names
Generic Available
No
Canadian Brand Names
Pharmacologic Category
Use: Labeled Indications
All stages of schistosomiasis caused by all Schistosoma species pathogenic to humans; clonorchiasis and opisthorchiasis
Use: Unlabeled/Investigational
Cysticercosis and many intestinal tapeworms
Pregnancy Risk Factor
B
Lactation
Enters breast milk
Contraindications
Hypersensitivity to praziquantel or any component of the formulation; ocular cysticercosis
Warnings/Precautions
Disease-related concerns:
• Cerebral cysticercosis: Patients with cerebral cysticercosis require hospitalization.
• Hepatic impairment: Use with caution in patients with severe hepatic impairment.
Concurrent drug therapy issues:
• Strong inducers of cytochrome P450: Use caution with concurrent administration of strong inducers of cytochrome P450; therapeutic levels of praziquantel may not be achieved.
Adverse Reactions
1% to 10%:
Central nervous system: Dizziness, drowsiness, headache, malaise, CSF reaction syndrome in patients being treated for neurocysticercosis
Gastrointestinal: Abdominal pain, loss of appetite, nausea, vomiting
Miscellaneous: Diaphoresis
<1%: Diarrhea, fever, itching, rash, urticaria
Metabolism/Transport Effects
Inhibits CYP2D6 (weak)
Drug Interactions
Aminoquinolines (Antimalarial): May decrease the serum concentration of Anthelmintics. Risk C: Monitor therapy
Cimetidine: May decrease the metabolism of Praziquantel. Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
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
Rifampin: May decrease the serum concentration of Praziquantel. Risk X: Avoid combination
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%
Distribution: CSF concentration is 14% to 20% of plasma concentration; enters breast milk
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 (99% as metabolites)
Dosage
Children >4 years and Adults: Oral:
Schistosomiasis: 20 mg/kg/dose 2-3 times/day for 1 day at 4- to 6-hour intervals
Flukes (unlabeled use): 25 mg/kg/dose every 8 hours for 1-2 days
Cysticercosis (unlabeled use): 50 mg/kg/day divided every 8 hours for 14 days
Tapeworms (unlabeled use): 10-20 mg/kg as a single dose (25 mg/kg for Hymenolepis nana)
Clonorchiasis/opisthorchiasis: 3 doses of 25 mg/kg as a 1-day treatment
Administration: Oral
Tablets may be halved or quartered.
Patient Education
Take exactly as directed for full course of medication. Tablets may be chewed, swallowed whole, or crushed and mixed with food. 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, or lightheadedness (use caution when driving or engaging in tasks that require alertness until response to drug is known); or abdominal pain, nausea, or vomiting (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help). 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
See Warnings/Precautions and Contraindications for use cautions. Worm infestations are easily transmitted, all close family members should be treated. Instruct patient/caregiver on appropriate use, transmission prevention, possible side effects/appropriate interventions, and adverse symptoms to report (see Patient Education).
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet [tri-scored]: 600 mg
Pricing: U.S. (www.drugstore.com)
Tablets (Biltricide)
600 mg (6): $88.87
References
de Silva N, Guyatt H, and Bundy D, “Anthelmintics. A Comparative Review of Their Clinical Pharmacology,” Drugs, 1997, 53(5):769-88.
“Drugs for Parasitic Infections,” Med Lett Drugs Ther, 1998, 40(1017):1-12.
King CH and Mahmoud AA, “Drug Five Years Later: Praziquantel,” Ann Intern Med, 1989, 110(4):290-6.
Liu LX and Weller PF, “Antiparasitic Drug,” N Engl J Med, 1996, 334(18):1178-84.
International Brand Names
Lexi-Comp.com
Last full review/revision July 2009
Content last modified July 2009
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