BILTRICIDE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BILTRICIDE (BILTRICIDE).
Praziquantel increases the permeability of cell membranes to calcium ions in susceptible schistosomes and other trematodes, causing sustained contraction and paralysis of the worm musculature, leading to detachment from blood vessel walls and eventual death.
| Metabolism | Extensively metabolized by the liver, primarily by cytochrome P450 enzymes (CYP3A4), to inactive hydroxylated metabolites. |
| Excretion | Renal excretion accounts for approximately 80-90% of elimination, primarily as metabolites; biliary/fecal excretion is minor (<10%). |
| Half-life | Terminal elimination half-life is approximately 0.8-1.5 hours for praziquantel; clinical significance: short half-life necessitates multiple dosing for sustained antiparasitic effect. |
| Protein binding | Approximately 80-85% bound to serum albumin. |
| Volume of Distribution | Volume of distribution is approximately 2-3 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is approximately 80% due to extensive first-pass metabolism; higher with food. |
| Onset of Action | Oral: Onset of antiparasitic action occurs within 30 minutes to 2 hours after administration. |
| Duration of Action | Duration of action is approximately 4-6 hours after a single oral dose; clinical note: repeated dosing over 1 day is typical for schistosomiasis. |
60 mg/kg/day orally in 3 divided doses (20 mg/kg/dose) for 1 day.
| Dosage form | TABLET |
| Renal impairment | No dosage adjustment required for any degree of renal impairment. |
| Liver impairment | No specific Child-Pugh based adjustments; contraindicated in hepatocellular carcinoma or history of hepatic encephalopathy; use caution in severe liver disease. |
| Pediatric use | 4 years and older: 60 mg/kg/day in 3 divided doses for 1 day; maximum single dose 2 g. |
| Geriatric use | No specific adjustments; use standard adult dosing with monitoring for adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for BILTRICIDE (BILTRICIDE).
| Breastfeeding | Praziquantel is excreted into breast milk in small amounts; M/P ratio not established. After a single dose, milk levels low; consider pumping and discarding milk for 24-48 hours post-dose. Use with caution in nursing mothers. |
| Teratogenic Risk | Praziquantel (Biltricide) is FDA Pregnancy Category B. Animal studies show no teratogenic effects but embryotoxicity at high doses. Human data limited; no increased risk of major malformations reported. Avoid in first trimester unless essential; use in second/third trimester if benefit outweighs risk. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to praziquantel or any component of the formulation","Ocular cysticercosis (due to risk of irreversible ocular damage from inflammatory response)","Concurrent use with rifampin (significantly reduces praziquantel plasma concentrations)","Children under 1 year of age (safety not established)"]
| Precautions | ["Avoid grapefruit juice during treatment due to increased praziquantel exposure.","May cause transient neurologic symptoms in patients with cerebral schistosomiasis or neurocysticercosis due to inflammatory reaction around dying parasites.","Use with caution in patients with hepatic impairment (Child-Pugh class B or C) as metabolism may be reduced.","May exacerbate cysticercosis if used without corticosteroids in neurocysticercosis.","Potential for cardiac arrhythmias in patients with ventricular arrhythmias or electrolyte disturbances (rare)."] |
| Food/Dietary | Take with food to enhance bioavailability. Avoid grapefruit juice as it may increase drug levels. Alcohol may worsen CNS side effects and is not recommended. |
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| Fetal Monitoring |
| Monitor for maternal adverse effects (headache, dizziness, abdominal pain, urticaria). No specific fetal monitoring required; routine prenatal care adequate. In case of neurocysticercosis, monitor for increased intracranial pressure or seizures during treatment. |
| Fertility Effects | No known adverse effects on human fertility. Animal studies show no impairment of fertility at therapeutic doses. |
| Clinical Pearls | Administer with food to increase absorption and reduce GI side effects. Use with caution in hepatic impairment; dose adjustment may be necessary. Monitor for neuropsychiatric effects (e.g., dizziness, headache) especially in patients with CNS involvement of schistosomiasis. Avoid in patients with ocular cysticercosis due to risk of intraocular inflammation; treat ocular lesions first with corticosteroids. |
| Patient Advice | Take this medication with a meal to improve absorption and reduce stomach upset. · Do not chew or crush the tablets; swallow them whole. · Complete the full course of treatment even if you feel better. · You may experience dizziness, drowsiness, or headache; avoid driving or operating heavy machinery until you know how the drug affects you. · Inform your doctor if you have liver disease or are taking other medications. · Contact your doctor if you experience severe headache, seizures, or vision changes. |