Brand Name: Biltricide
Generic Name: Praziquantel

Mechanism of Action: 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. The effect is more marked on adult worms compared to young worms. An increased calcium influx may play an important role.

Secondary effects are inhibition of glucose uptake, lowering of glycogen levels and stimulation of lactate release. The action of praziquantel is limited very specifically to trematodes and cestodes; nematodes (including filariae) are not affected.

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

For the treatment of infections due to the following species of schistosoma: (S. haematobium, S. japonicum, S. mansoni, and S. mekongi), and infections due to the liver flukes C. sinensis/O. viverrini. (Approval of this indication was based on studies in which the two species were not differentiated.)

Nephrotoxic effects of praziquantel have not been observed. Since 80% of praziquantel and its derivatives are excreted in the kidneys, excretion may be delayed in patients with impaired renal function.

Caution should be taken in patients with uncompensated liver insufficiency or with hepatosplenic schistosomiasis. Because of reduced drug metabolization in the liver, considerably higher and longer lasting concentrations of unmetabolized praziquantel can occur in the vascular system and/or collateral circulation, leading to prolonged plasma half-life. If necessary, the patient may be hospitalized for the duration of treatment. Mild increases in liver enzymes have also been reported in some patients.

Patients suffering from cardiac irregularities should be monitored during treatment.

When schistosomiasis or fluke infection is found in patients living in or coming from areas with endemic human cysticercosis, it is advisable to hospitalize the patient for the duration of treatment.