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Generic Praziquantel
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 and Opisthorchis felineus), paragonimiasis (Paragonimus westermani and other species), fasciolopsiasis (Fasciolopsis buski), 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 through a dual mechanism of action. First, praziquantel causes a rapid and sustained influx of calcium ions across the parasite's tegumental membrane, leading to immediate tetanic contraction and spastic paralysis of the worm's musculature. Second, it disrupts the structural integrity of the parasite's outer tegument, exposing previously concealed surface antigens to the host immune system, which then facilitates immune-mediated phagocytosis, adherence, and elimination of the damaged parasites. This unique combined mechanism renders praziquantel highly effective against a wide range of trematodes (flukes) and cestodes (tapeworms).
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 fasciolopsiasis, a single dose of 15 to 25 mg per kilogram is usually effective. For intestinal tapeworm infections, including Taenia saginata, Taenia solium, and Diphyllobothrium latum, a single oral dose of 5 to 10 mg per kilogram is sufficient. For Hymenolepis nana (dwarf tapeworm), a higher single dose of 15 to 25 mg per kilogram is recommended due to the potential for internal autoinfection. Tablets should be taken with food and swallowed whole with a full glass of water. They may be divided into segments along the scored markings to accommodate precise weight-based dosing. The tablets have a distinctly bitter taste and should not be chewed. For Taenia solium infections, it is crucial to exclude concurrent neurocysticercosis before treatment, as the death of cerebral cysticerci can precipitate severe neurological reactions.
Dosage form: Tablets: 600 mg (white to off-white, ovaloid, film-coated, scored into four segments). Each tablet features three deep score lines, allowing the tablet to be divided into four equal quarters of approximately 150 mg each. This quarter-scored design facilitates accurate weight-based dosing across a wide range of body weights, which is particularly important in pediatric patients, low-body-weight adults, and mass drug administration programs where precise 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; tegumental damage and spastic paralysis begin within the first hour following peak plasma concentrations. In schistosomiasis, cessation of egg production and the initiation of worm elimination commence within the first 24 to 48 hours after treatment. Clinical improvement, including resolution of acute symptoms such as fever, abdominal pain, and hematuria, is typically observed within days to weeks, depending on the parasite burden, the species involved, and the chronicity of the 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 hydroxylated metabolites is approximately 4 to 6 hours. Despite the relatively 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, primarily CYP3A4, and its metabolites are excreted predominantly in the urine (60% to 80%) within 24 hours of dosing, with the remainder eliminated in the feces.
Alcohol recommendation: Alcohol consumption should be avoided during treatment with praziquantel and for at least 24 hours after the last dose. Praziquantel undergoes extensive hepatic metabolism via the cytochrome P450 enzyme system, and alcohol may alter hepatic metabolic pathways, potentially affecting the drug's pharmacokinetics and therapeutic efficacy. Furthermore, alcohol can exacerbate the central nervous system side effects of praziquantel, including dizziness, drowsiness, headache, fatigue, and impaired coordination. Patients should not drive or operate machinery for at least 24 hours following treatment, and the concomitant use of alcohol significantly compounds the risk of sedation and accidents. Complete abstinence from alcohol for the duration of therapy is strongly recommended to ensure treatment safety and efficacy.
Most common side effects: In the treatment of schistosomiasis, the most frequently reported adverse effects are abdominal discomfort or pain, nausea, vomiting, diarrhea, anorexia, headache, dizziness, drowsiness, malaise, fatigue, fever, and urticaria. These effects are generally mild to moderate in severity, transient, and resolve spontaneously within 24 to 48 hours. It is important to note that many of these symptoms—particularly abdominal pain, nausea, headache, and fever—may be attributable to the host immune response to dying and disintegrating parasites and the release of parasitic antigens rather than to the drug itself. In patients with heavy parasitic loads, more pronounced systemic reactions may occur, including intense abdominal cramping, bloody diarrhea, and high fever. 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 and vision loss. 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, phenytoin, carbamazepine, and dexamethasone may substantially reduce praziquantel plasma levels, potentially compromising therapeutic efficacy and leading to treatment failure. Conversely, CYP450 inhibitors such as cimetidine, ketoconazole, and grapefruit juice may increase plasma concentrations and the risk of toxicity. In patients with severe hepatic impairment or decompensated liver disease, dose reduction or alternative therapeutic strategies may be considered.
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