Biltricide: The Definitive Treatment for Schistosomiasis

Biltricide

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Product dosage: 600mg
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Synonyms Praziquantel

Biltricide (praziquantel) is the global therapeutic standard for the treatment of schistosomiasis and liver fluke infections. As a broad-spectrum anthelmintic, it is recognized by the World Health Organization as an essential medicine, pivotal in public health initiatives aimed at controlling and eliminating these parasitic diseases. Its mechanism of action induces rapid paralysis and tegumental damage in susceptible parasites, leading to their eradication from the host. This product card provides a comprehensive, expert-level overview of its pharmacology, clinical application, and safety profile for healthcare professionals.

Features

• Active Ingredient: Praziquantel 600 mg per scored tablet.
• Pharmacologic Class: Pyrazinoisoquinoline anthelmintic.
• Mechanism of Action: Induces severe spasms and tetanic paralysis in the parasite’s musculature by increasing cell membrane permeability to calcium ions. This is followed by vacuolization and disintegration of the tegument, making the parasite susceptible to host immune attacks.
• Pharmacokinetics: Undergoes extensive first-pass metabolism, resulting in low systemic bioavailability, which is significantly increased by a high-fat meal. Protein binding is approximately 80%. The half-life of unchanged praziquantel is short (1-1.5 hours), while its metabolites have a half-life of 4-6 hours. Primarily excreted renally as metabolites.
• Spectrum of Activity: Highly effective against all major Schistosoma species pathogenic to humans (S. haematobium, S. mansoni, S. japonicum, S. mekongi, S. intercalatum). Also effective against liver flukes (Clonorchis sinensis, Opisthorchis viverrini) and intestinal flukes (Fasciolopsis buski, Heterophyes heterophyes, Metagonimus yokogawai).

Benefits

• High Cure Rates: Achieves parasitological cure rates exceeding 85% for most schistosome species with a single-day treatment regimen, as confirmed by egg reduction in stool or urine exams.
• Broad-Spectrum Efficacy: A single agent effective against the majority of trematode infections that burden human populations, simplifying treatment protocols in endemic areas.
• Well-Tolerated Profile: The adverse effect profile is generally mild and transient, often related to the host’s reaction to dying parasites rather than direct drug toxicity, facilitating high compliance in mass drug administration programs.
• Critical Public Health Impact: Serves as the cornerstone of WHO-recommended preventive chemotherapy programs, reducing parasite burden, reversing morbidity in infected individuals, and interrupting transmission cycles in communities.
• Simple Dosing Regimen: Weight-based dosing allows for easy administration in both clinical and field settings, making it suitable for large-scale control efforts.

Common use

Biltricide is indicated for the treatment of infections caused by trematodes (flukes). Its primary use is against schistosomiasis (bilharzia), a disease affecting hundreds of millions in tropical and subtropical regions, particularly in sub-Saharan Africa. It is also employed for the treatment of food-borne trematodiases, such as clonorchiasis (Chinese liver fluke) and opisthorchiasis, which are prevalent in parts of Asia and Eastern Europe. Its use is critical in both individual patient care and community-wide mass drug administration (MDA) campaigns aimed at morbidity control and transmission reduction.

Dosage and direction

Dosing is strictly weight-based and varies depending on the infecting parasite species. The tablets are scored and should be swallowed whole with liquid during a meal to enhance absorption. They should not be chewed due to their intensely bitter taste, which can cause gagging or vomiting.

• Schistosomiasis:
  • S. haematobium, S. mansoni, S. intercalatum: 40 mg/kg body weight as a single oral dose or as two divided doses administered 4-6 hours apart.
  • S. japonicum, S. mekongi: 60 mg/kg body weight as a single oral dose or as two or three divided doses over one day (e.g., 20 mg/kg TID).
• Liver Flukes (Clonorchiasis/Opisthorchiasis): 75 mg/kg total dose, administered as 25 mg/kg TID in a single day.
• Other Flukes: Dosing varies; consult current treatment guidelines.

A practical dosing chart is often used in the field:

Precautions

• Hepatic Impairment: Use with caution in patients with severe hepatic impairment, as metabolism may be altered. However, the drug is not contraindicated.
• Cardiac Conditions: Caution is advised in patients with a history of cardiac arrhythmias or other significant heart disease due to reports of rare cardiac events.
• Ocular Cysticercosis: Extreme caution is required. Destruction of the parasite within the eye can cause irreversible local damage. Treatment must be managed by a specialist in a controlled setting with concomitant corticosteroid therapy.
• Pregnancy: While animal studies have not shown direct teratogenic effects, the benefit of treatment in pregnant women with schistosomiasis must be weighed against the potential risk. The WHO recommends its use in pregnant and lactating women when the indication is clear.
• Lactation: Praziquantel is excreted in human milk at concentrations approximately 25% of maternal serum levels. The WHO considers its use compatible with breastfeeding, as the infant dose received is subtherapeutic.

Contraindications

Biltricide is contraindicated in patients with a known history of hypersensitivity to praziquantel or any component of the formulation. Its use is also contraindicated for the treatment of cysticercosis located in the eye, as previously noted.

Possible side effect

Most adverse reactions are mild to moderate, appear within a few hours of ingestion, are transient, and are directly linked to the parasite’s death and the host’s immunological response.

• Very Common (>10%): Abdominal pain or discomfort, nausea, vomiting, headache, dizziness, malaise.
• Common (1-10%): Pruritus, urticaria, low-grade fever, drowsiness, diarrhea.
• Uncommon (0.1-1%): Sweating, eosinophilia, bloody diarrhea.
• Rare (<0.1%): Cardiac arrhythmias, seizures (primarily in patients with neurocysticercosis not pre-treated with corticosteroids), elevated liver enzymes.

Drug interaction

• Enzyme Inducers (e.g., Carbamazepine, Phenytoin, Phenobarbital, Rifampin): These drugs significantly increase the metabolism of praziquantel, leading to subtherapeutic plasma levels and potential treatment failure. Concomitant use should be avoided. If unavoidable, consider a higher praziquantel dose and monitor efficacy closely.
• Enzyme Inhibitors (e.g., Cimetidine, Ketoconazole, Itraconazole): May increase praziquantel plasma levels, potentially increasing the incidence of adverse effects. Monitor patients closely.
• Chloroquine: May decrease plasma concentrations of praziquantel.
• Grapefruit Juice: May inhibit the metabolism of praziquantel, increasing its bioavailability and potentially its side effects.

Missed dose

As Biltricide is typically administered as a single or one-day course, the concept of a “missed dose” primarily applies to the divided-dose regimens. If a dose is missed within the treatment day, it should be taken as soon as possible. However, if it is almost time for the next scheduled dose, the missed dose should be skipped, and the regular dosing schedule resumed. The total daily dose should not be doubled. For a single-dose regimen, if a dose is missed or vomited, consult a healthcare provider for re-dosing instructions.

Overdose

There is no specific antidote for praziquantel overdose. Reported symptoms in cases of significant overdose include intensification of the known side effects: severe nausea, vomiting, dizziness, drowsiness, and sweating. In extreme cases, convulsions or arrhythmias could occur. Management is supportive and symptomatic. Gastric lavage may be considered if performed soon after ingestion. Monitor vital signs and provide appropriate supportive care.

Storage

Store Biltricide tablets below 30°C (86°F). Keep the container tightly closed to protect from light and moisture. Keep out of reach of children. Do not use after the expiration date printed on the packaging.

Disclaimer

This information is intended for educational and informational purposes for healthcare professionals and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of a physician or other qualified health provider with any questions you may have regarding a medical condition or before administering any drug. Dosing and indications may change; always refer to the most current official prescribing information or national treatment guidelines.

Reviews

• “The cornerstone of our schistosomiasis control program. Its efficacy and the practicality of a single-day regimen are unmatched. The side effects are manageable and a small price to pay for the clinical and public health benefits.” – Infectious Disease Specialist, Sub-Saharan Africa.
• “From a pharmacological standpoint, praziquantel’s unique mechanism of action and its critical role as an essential medicine make it a fascinating and vital tool. The interactions with enzyme inducers are a key clinical consideration.” – Clinical Pharmacologist, Europe.
• “We have successfully used it in MDA campaigns for years. The weight-based tablet chart makes community distribution feasible. High patient acceptance due to the short treatment duration.” – Public Health Officer, WHO.