Clonorchiasis
Infection by Opisthorchis viverrini
Schistosomiasis
藥理
Anthelmintic
Systemic: Vermicidal; precise mechanism of action unknown, but may involve synergy between praziquantel and the host's humoral immune response in S. mansoni; praziquantel is rapidly taken up by helminths and also appears to increase permeability of helminth's cell membrane, leading to a loss of intracellular calcium; massive contraction and paralysis of the helminth's musculature rapidly result; after exposure to praziquantel, tegument in neck region of adult helminths develops blebs, which appear to burst and disintegrate; praziquantel also produces intense vacuolization at several sites in tegument of adult schistosomes; in S. mansoni, this is followed by phagocytic attachment to parasite and, ultimately, death.
藥動學
Absorption
Systemic: Rapidly absorbed
Metabolism
Systemic: Hepatic: First-pass
Excretion
Systemic: Fecal: small amounts; Renal: 72 to 80%
Elimination Half Life
Systemic: Praziquantel: 0.8 to 1.5 h
Metabolites: 4 to 6 h
禁忌症
concomitant use with strong CYP inducers such as rifampin
hypersensitivity to praziquantel or any excipients
ocular cysticercosis
懷孕分類
B(FDA)
B1(AUS)
哺乳分類
WHO: Compatible with breastfeeding.
Micromedex: Infant risk cannot be ruled out.
Clonorchiasis
25 mg/kg ORALLY 3 times over 1 day (at 4 to 6 hr intervals)
Infection by Opisthorchis viverrini
25 mg/kg ORALLY 3 times over 1 day (at 4 to 6 hr intervals)
Schistosomiasis
20 mg/kg ORALLY 3 times over 1 day (at 4 to 6 hr intervals)
小兒調整劑量
General Dosage Information
Safety in children less than 4 yr old has not been established
Clonorchiasis
25 mg/kg ORALLY 3 times over 1 day (at 4 to 6 hr intervals)
Infection by Opisthorchis viverrini
25 mg/kg ORALLY 3 times over 1 day (at 4 to 6 hr intervals)
Schistosomiasis
20 mg/kg ORALLY 3 times over 1 day (at 4 to 6 hr intervals)
腎功能調整劑量
Dose adjustments for renal impairment are not considered necessary
肝功能調整劑量
A) Patients with hepatosplenic schistosomiasis and moderate to severe liver impairment (Child-Pugh classes B and C) may experience reduced metabolism of praziquantel resulting in higher and more prolonged plasma concentrations. B) Liver blood flow is reduced in advanced stages of schistosomiasis. Antipyrine clearance may remain unchanged or be slightly reduced. Chronic liver disease secondary to schistosomiasis is not true cirrhosis and hepatocyte dysfunction is reported to be minimal until the very last stages of the disease. Dosage recommendations for patients with liver disease are controversial
安定性
Oral route
1) Praziquantel (Biltricide(R)) tablets should be stored at temperatures below 86 degrees Fahrenheit (30 degrees Celsius)