Pharmacotherapeutic group: endectocide, anthelmintic Flukicide.
ATCvet code: QP54AA51.
Pharmacodynamic properties
Ivermectin is a broad spectrum endectocide of the avermectin family. Ivermectin is isolated after purification and hydrogenation of the avermectin family compounds which are obtained from the fermentation of the soil organism Streptomyces avermitilis.
Ivermectin is a macrocyclic-lactone derivative which has a broad and potent antiparasitic activity against nematodes and arthropods. It acts by inhibiting nerve impulses. Ivermectin binds selectively and with high affinity to glutamate-gated chloride ion channels which occur in invertebrate nerve.and muscle cells. This leads to an increase in the permeability of the cell membrane to chloride ions with hyperpolarization of the nerve or muscle cell, resulting in paralysis and death of the relevant parasites. Compounds of this class may also interact with other ligand-gated chloride channels, such as those gated by the neurotransmitter gammaaminobutyric acid (GABA). The margin of safety for compounds of this class is attributable to the fact that mammals do not have glutamate-gated chloride channels. The macrocyclic lactones have a low affinity for other mammalian ligand-gated chloride channels and they do not readily cross the blood-brain barrier.
Clorsulon inhibits glycolytic enzymes of Fasciola hepatica (3-phosphoglycerate kinase and phosphoglyceromutase). This enzymatic inhibition effectively blocks the Embden-Myerhof glycolytic pathway and thereby deprives the fluke of its main source of metabolic energy.
Pharmacokinetic properties
After subcutaneous injection of the product at the dose of 1 ml per 50 kg (200 j.lg/kg of ivermectin and 2 mg/kg of c1orsulon), mean maximum concentrations of 26 ng/ml for ivermectin and 2.8 j.lg/ml for c1orsulon were reached at 35 hours for ivermectin and 9 hours for c1orsulon.