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Pharmacological particulars
Pharmacotherapeutic group: Anthelmintic. ATC vet code: QP52AA51
Pharmacodynamic properties
This product contains anthelmintics active against gastrointestinal roundworms and tapeworms. The product contains two active substances, as follows: Pyrantel embonate (pamoate), a tetrahydropyrimidine derivative and Praziquantel, a partially hydrogenated pyrazinoisoquinoline derivative. Pyrantel acts as a cholinergic agonist. Its mode of action is to stimulate nicotinic cholinergic receptors of the parasite, induce spastic paralysis and thereby allow expulsion from the gastrointestinal (GI) system by peristalsis. Praziquantel is very rapidly absorbed and distributed throughout the parasite. Both in vitro and in vivo studies have shown that praziquantel causes severe damage to the parasite integument, resulting in contraction and paralysis. There is an almost instantaneous tetanic contraction of the parasite musculature and a rapid vacuolization of the syncytial tegument. This rapid contraction has been explained by changes in divalent cation fluxes, especially calcium. In this fixed combination, pyrantel is active against the following ascarids: Toxocara cati, and Toxascaris leonina. Praziquantel is effective against tapeworms in particular Dipylidium caninum and Taenia taeniaeformis. Since it contains praziquantel, the product is effective against Echinococcus multilocularis.
Pharmacokinetic particulars
Praziquantel is rapidly absorbed, metabolised and distributed in the body. It is also believed to be excreted back into the intestinal lumen by the mucous membrane. Following administration of the product to cats, peak plasma concentrations of praziquantel were achieved by approximately 2 hours. Pyrantel is poorly absorbed so it is expected that a large proportion of the administered dose remains in the GIT where it exerts its therapeutic effect and it is excreted largely unchanged in the faeces. Following administration of the product to cats, peak plasma concentrations of pyrantel were achieved by approximately 3 hours.