metadata toggle
Pharmacological particulars
Pharmacotherapeutic group: endectocides, avermectins. ATC vet code: QP54AA01.
Pharmacodynamic properties
Ivermectin is a mixture of two compounds belonging to the avermectin family, which are a macrocyclic lactone group of endectocides. Avermectin is a microbial metabolite of the soil organism Streptomyces avermilitis.
It is generally accepted that ivermectin exerts its action in two main ways, interference with neurotransmission and opening chloride ion channels. The effect of ivermectin on the parasitic CNS is considered to operate through glutamate-mediated chloride channels. Compounds of this class may also interact with other ligand-gated chloride channels, such as those gated by the neurotransmitter gamma- aminobutyric acid (GABA).
The opening of pre-synaptic chloride ion channels results in an efflux of chloride ions and depolarisation of the nerve terminal. These effects interfere with normal neurotransmission between nerves and muscles, resulting in parasite paralysis and eventual death.
Pharmacokinetic particulars
After administration of the product, the ivermectin is absorbed through the skin into the circulation of the treated animal. The maximum concentration in plasma occurs around 70 hours after application. Peak concentrations of about 7ng/ml are obtained.
The residual antiparasitic effect of ivermectin is due to its persistence, which in turn is due part to its long intrinsic half life (t1/2β of approximately 210 hours), in part to its relatively high plasma protein binding (80% in cattle; binding remains relatively constant over time) and in part to the nature and type of the ivermectin formulation.
Elimination is in the faeces (via biliary excretion). Over 60% of the dose is excreted after 3 days.