Praziquantel

Trade Names:
Biltricide
- Tablets 600 mg

Pharmacology

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Increases cell membrane permeability in susceptible worms, resulting in loss of intracellular calcium, massive contractions, and paralysis of their musculature. Phagocytes are thus able to attach to worms, causing their death.

Pharmacokinetics

Absorption

Rapidly absorbed (80%). T _max is 1 to 3 h.

Distribution

CSF levels are 14% to 20% of plasma concentration. Appears in breast milk. Protein binding is 80% to 85%.

Metabolism

Extensive first-pass metabolism, rapidly metabolized to inactive mono- and polyhydroxylated derivatives.

Elimination

Urine (as metabolites), small amounts in feces. Serum t _½ is 0.8 to 1.5 h.

Special Populations

Moderate to severe; plasma concentration were significantly elevated in one study.

Indications and Usage

Infections caused by Schistosoma mekongi , S. japonicum , S. mansoni , S. hematobium , liver flukes, Clonorchis sinensis , and Opisthorchis viverrini .

Unlabeled Uses

Treatment of neurocysticercosis, tissue flukes (opisthorchis, felineus, Paragonimus westermani , Fasciola hepatica ), intestinal flukes ( Heterophyes heterophyes , Fascilopsis buski ), and intestinal cestodes ( Diphyllobothrium latum , Taenia saginata , T. solium , Dipylidium caninum , Hymenolepsis nana ), and schistosomiasis (in concurrent use with oxamniquine).

Contraindications

Ocular cysticercosis.

Dosage and Administration

PO 60 mg/kg in 3 equally divided doses every 4 to 6 h for 1 day.

PO 75 mg/kg in 3 equally divided doses every 4 to 6 h for 1 day.

General Advice

• Administer tablets during meals with liquids.
• Instruct patient not to chew tablets.

Storage/Stability

Store at room temperature.

Drug Interactions

Plasma levels of praziquantel may be elevated, increasing the pharmacologic and adverse effects.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Malaise; headache; fever; drowsiness; dizziness.

Dermatologic

Urticaria.

GI

Abdominal discomfort, with or without nausea.

Hepatic

Increased liver enzymes.

Precautions

Pregnancy

Category B .

Lactation

Excreted in breast milk. Lactating women should avoid breastfeeding on day of treatment and for subsequent 72 h.

Children

Safety and efficacy not established in children younger than 4 yr of age.

Patient Information

• Explain that treatment lasts only 1 day for most parasitic infections.
• Instruct patient to take drug with liquids during meals and not to chew tablets.
• Advise patient to have all family members examined for infestation.
• Instruct patient to report the following symptoms to health care provider: malaise, headache, dizziness, abdominal pain, nausea, urticaria, or fever.
• Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.

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