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Active ingredient: Praziquantel - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Anthelmintics

Dosage Forms

  • Liquid
  • Paste
  • Solution
  • Tablet

Brands / Synonyms

Biltricide; Biltricide

Indications

For the treatment of infections due to all species of schistosoma.

Pharmacology

Praziquantel is an anthelmintic used in most schistosome and many cestode infestations. Praziquantel effects the permeability of the cell membrane resulting in the contraction of schistosomes. 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.

Mechanism of Action

Praziquantel works by causing severe spasms and paralysis of the worms' muscles. This paralysis is accompanied - and probably caused - by a rapid Ca 2+ influx inside the schistosome. Morphological alterations are another early effect of praziquantel. These morphological alterations are accompanied by an increased exposure of schistosome antigens at the parasite surface. The worms are then either completely destroyed in the intestine or passed in the stool. An interesting quirk of praziquantel is that it is relatively ineffective against juvenile schistosomes. While initially effective, effectiveness against schistosomes decreases until it reaches a minimum at 3-4 weeks. Effectiveness then increases again until it is once again fully effective at 6-7 weeks. Glutathione S-transferase (GST), an essential detoxification enzyme in parasitic helminths, is a major vaccine target and a drug target against schistosomiasis.

Absorption

Rapidly absorbed (80%)

Toxicity

Not Available

Biotrnasformation / Drug Metabolism

renal

Contraindications

BILTRICIDE® should not be given to patients who previously have shown hypersensitivity to the drug. Since parasite destruction within the eye may cause irreparable lesions, ocular cysticercosis should not be treated with this compound.

Drug Interactions

No data are available regarding interaction of BILTRICIDE® with other drugs.

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