Biltricide (Praziquantel) Drug Information: Clinical Pharmacology

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May 25, 2012

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Schistosomiasis »

What is schistosomiasis?

Schistosomiasis is a disease that is caused by parasites (genus Schistosoma) that enter humans by attaching to the skin, penetrating it, and then migrating through the venous system to the portal veins where the parasites produce eggs and eventually, the symptoms of acute or chronic disease (for example, fever, abdominal discomfort, blood in stools). This disease is also known as bilharziasis, bilharzia, bilharziosis, and snail fever or, in the acute form, Katayama fever. Theodore Bilharz identified the parasite Schistosoma hematobium in Egypt in 1851. Schistosomiasis is the second most prevalent tropical disease in the world; malaria is the first. The disease is found mainly in developing countries in Africa, Asia, South America, the Middle East, and the Caribbean. About 207 million people in at least 74 countries are estimated to have the disease. In the U.S., it is diagnosed in tourists who have visited these developing...

Read the Schistosomiasis article »

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CLINICAL PHARMACOLOGY

Praziquantel induces a rapid contraction of schistosomes by a specific effect on the permeability of the cell membrane. The drug further causes vacuolization and disintegration of the schistosome tegument.

After oral administration BILTRICIDE (praziquantel) is rapidly absorbed (80%), subjected to a first pass effect, metabolized and eliminated by the kidneys. Maximal serum concentration is achieved 1-3 hours after dosing. The half-life of praziquantel in serum is 0.8-1.5 hours.

Special Populations

The pharmacokinetics of praziquantel were studied in 40 patients with Schistosoma mansoni infections with varying degrees of hepatic dysfunction (See table 1). In patients with schistosomiasis, the pharmacokinetic parameters did not differ significantly between those with normal hepatic function (Group 1) and those with mild (Child-Pugh class A) hepatic impairment. However, in patients with moderate-to-severe hepatic dysfunction (Child-Pugh class B and C), praziquantel half-life, Cmax, and AUC increased progressively with the degree of hepatic impairment. In Child-Pugh class B, the increases in mean half-life, Cmax, and AUC relative to Group 1 were 1.58-fold, 1.76-fold, and 3.55-fold, respectively. The corresponding increases in Child-Pugh class C patients were 2.82-fold, 4.29-fold, and 15-fold for half-life, Cmax, and AUC.

Table 1: Pharmacokinetic parameters of praziquantel in four groups of patients with varying degrees of liver function following administration of 40 mg/kg under fasting conditions.

Patient Group	Half-life (hr)	Tmax (hr)	Cmax (μg/mL)	AUC (μg/mL* hr)
Normal hepatic function (Group 1)	2.99 ± 1.28	1.48 ±0.74	0.83 ± 0.52	3.02 ±0.59
Child-Pugh A (Group 2)	4.66±2.77	1.37 ± 0.61	0.93± 0.58	3.87 ±2.44
Child-Pugh B (Group 3)	4.74 ±2.16^a	2.21 ± 0.78^a,b	1.47 ±0.74^a,b	10.72 ±5.53^a,b
Child-Pugh C (Group 4)	8.45 ±2.62^a,b,c	3.2 ± 1.05^a,b,c	3.57 ±1.30^a,b,c	45.35 ± 17.50^a,b,c
a) p < 0.05 compared to Group 1 b) p < 0.05 compared to Group 2 c) p < 0.05 compared to Group 3