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Pharmacological particulars
Pharmacodynamic properties
Imidacloprid, 1-(6-Chloro-3-pyridylmethyl)-N-nitro-imidazolidin-2-ylideneamine is an ectoparasiticide belonging to the chloronicotinyl group of compounds. Chemically, it is more accurately described as a chloronicotinyl nitroguanidine. Imidacloprid is effective against larval flea stages and adult fleas. Flea larvae in the pet’s surroundings are killed after contact with a pet treated with the product. Imidacloprid has a high affinity for the nicotinergic acetylcholine receptors in the post-synaptic region of the central nervous system (CNS) of the flea. The ensuing inhibition of cholinergic transmission in insects results in paralysis and death. Due to the weak nature of the interaction with mammalian nicotinergic receptors and the postulated poor penetration through the blood-brain barrier in mammals, it has virtually no effect on the mammalian CNS. Imidacloprid has minimal pharmacological activity in mammals.
Moxidectin, 23-(O-methyloxime)-F28249 alpha is a second-generation macrocyclic lactone of the milbemycin family. It is a parasiticide which is active against many internal and external parasites. Moxidectin is active against larval stages (L3, L4) of Dirofilaria immitis. It is also active against gastrointestinal nematodes. Moxidectin interacts with GABA and glutamate-gated chloride channels. This leads to opening of the chloride channels on the postsynaptic junction, the inflow of chloride ions and induction of an irreversible resting state. The result is flaccid paralysis of affected parasites, followed by their death and/or expulsion.
Pharmacokinetic properties
After topical administration of the product, imidacloprid is rapidly distributed over the animal’s skin within one day of application. It can be found on the body surface throughout the treatment interval. Moxidectin is absorbed through the skin, reaching maximum plasma concentrations approximately 4 to 9 days after treatment in dogs. Following absorption from the skin, moxidectin is distributed systemically and is slowly eliminated from the plasma as manifested by detectable moxidectin concentrations in plasma throughout the treatment interval of one month.