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Biltricide ( Praziquantel )
Biltricide (praziquantel) is a broad-spectrum anthelmintic agent indicated for the treatment of infections caused by various species of parasitic flatworms, including schistosomiasis (all species of Schistosoma), clonorchiasis (Clonorchis sinensis), opisthorchiasis (Opisthorchis viverrini), paragonimiasis (Paragonimus westermani), and intestinal tapeworm infections caused by Taenia saginata, Taenia solium, Diphyllobothrium latum, and Hymenolepis nana. It belongs to the pyrazinoisoquinoline class of anthelmintics and works primarily by causing a rapid and sustained influx of calcium ions across the parasite's tegumental membrane, leading to instantaneous, irreversible contraction and spastic paralysis of the worm's musculature. In addition, praziquantel disrupts the integrity of the parasite's outer tegument, exposing previously concealed surface antigens to the host immune system, which then facilitates immune-mediated destruction and elimination of the damaged parasites. This dual mechanism of action—muscular paralysis and tegumental disruption—makes praziquantel highly effective against a wide range of trematodes and cestodes.
Usual adult dose: The dosage of praziquantel is strictly dependent on the specific parasitic infection being treated and the patient's body weight. For Schistosoma haematobium, Schistosoma mansoni, and Schistosoma intercalatum infections, the recommended dose is 40 mg per kilogram of body weight administered as a single oral dose or divided into two doses given 4 to 6 hours apart on a single day. For Schistosoma japonicum and Schistosoma mekongi, a total dose of 60 mg per kilogram is recommended, divided into two or three doses over one day. For clonorchiasis and opisthorchiasis, the recommended dose is 75 mg per kilogram per day divided into three doses for 1 to 2 days. For paragonimiasis, 75 mg per kilogram per day divided into three doses for 2 to 3 days is recommended. For intestinal tapeworm infections, including Taenia saginata and Diphyllobothrium latum, a single oral dose of 5 to 10 mg per kilogram is usually sufficient. For Hymenolepis nana (dwarf tapeworm), a higher single dose of 15 to 25 mg per kilogram is recommended. For Taenia solium (pork tapeworm) intestinal infections, a single dose of 5 to 10 mg per kilogram is used; however, caution is essential to exclude concurrent neurocysticercosis before treatment. Tablets should be taken with food and swallowed whole with a full glass of water; they may be divided into segments if required for accurate weight-based dosing. The tablets have a bitter taste, so they should not be chewed, and dividing them precisely along the scored markings is essential.
Dosage form: Tablets: 600 mg (white to off-white, ovaloid, film-coated, scored into four segments). Each tablet is deeply scored with three cross marks, allowing it to be divided into four equal portions of approximately 150 mg each, facilitating precise weight-based dosing across a wide range of body weights. This quarter-scored design is particularly important in pediatric and low-body-weight patients where exact milligram-per-kilogram calculations are essential.
Onset of action: Following oral administration, praziquantel is rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations achieved within 1 to 3 hours. The onset of the paralytic effect on susceptible parasites occurs within minutes of drug exposure in vitro; in vivo, tegumental damage and parasite paralysis begin within the first hour following peak plasma concentrations. In schistosomiasis, cessation of egg production and the beginning of worm elimination occur within the first 24 to 48 hours. Clinical improvement, including resolution of acute symptoms such as fever and abdominal pain, is typically observed within days to weeks, depending on the parasite burden and the chronicity of infection.
Duration of action: The elimination half-life of praziquantel is approximately 0.8 to 1.5 hours in healthy individuals; however, the half-life of its active metabolites is approximately 4 to 6 hours. Despite the short plasma half-life, the antiparasitic effect is sustained and generally curative with a single day of treatment for most indications, due to the irreversible nature of the tegumental and muscular damage inflicted on the parasites. Praziquantel is extensively metabolized in the liver via the cytochrome P450 system, and its metabolites are excreted primarily in the urine (60% to 80%) within 24 hours of dosing.
Alcohol recommendation: Alcohol consumption should be avoided during treatment with Biltricide and for at least 24 hours after the last dose. Praziquantel is extensively metabolized by hepatic cytochrome P450 enzymes, and alcohol may alter hepatic metabolism, potentially affecting the drug's pharmacokinetics and efficacy. Furthermore, alcohol can exacerbate the central nervous system side effects of praziquantel, including dizziness, drowsiness, headache, and impaired coordination. Patients should not drive or operate machinery for at least 24 hours following treatment, and the addition of alcohol significantly compounds the risk of sedation and accident. Complete abstinence from alcohol for the duration of therapy is strongly recommended.
Most common side effects: In the treatment of schistosomiasis, the most frequently reported adverse effects are abdominal discomfort or pain, nausea, vomiting, diarrhea, headache, dizziness, drowsiness, malaise, fatigue, and urticaria. These effects are generally mild to moderate, transient, and resolve spontaneously within 24 to 48 hours. Importantly, many of these symptoms—particularly abdominal pain, nausea, headache, and fever—may be attributable to the host immune response to dying and disintegrating parasites rather than to the drug itself. In patients with heavy parasitic loads, more pronounced systemic reactions may occur. When used for neurocysticercosis, praziquantel must be administered under close medical supervision with concomitant corticosteroid cover, as the inflammatory response to dying cysticerci in the brain can precipitate seizures, elevated intracranial pressure, and meningoencephalitis. Praziquantel is contraindicated in patients with ocular cysticercosis, as parasite death within the eye may cause irreversible intraocular damage. It is also contraindicated in patients with known hypersensitivity to praziquantel or any of its excipients. Concomitant administration with strong cytochrome P450 inducers such as rifampicin or certain anticonvulsants may substantially reduce praziquantel plasma levels, compromising therapeutic efficacy, while CYP450 inhibitors such as cimetidine may increase plasma concentrations. In patients with severe hepatic impairment, dose reduction or alternative therapy may be considered.
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