Pharmacotherapeutic group: ectoparasiticides, insecticides and repellents, pyrethrins and pyrethroids, Flumethrin combinations
ATCvet code: QP53AC55
Pharmacodynamic properties
Imidacloprid is an ectoparasiticide belonging to the chloronicotinyl group of compounds. Chemically, it can be classified as a chloronicotinyl nitroguanidine.
Imidacloprid is active against larval flea stages, adult fleas and lice. Activity against Ctenocephalides felis starts immediately after application of the collar in the cat. Efficacy against fleas (Ctenocephalides felis and Ctenocephalides canis) starts within 48 hours after application of the collar in the dog.
In addition to the indications listed under section 'Indications for use' an activity against Ctenocephalides canis has been demonstrated in the cat and Pulex irritans fleas has been demonstrated in both cats and dogs.
Imidacloprid has a high affinity for the nicotinergic acetylcholine receptors in the postsynaptic 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.
Flumethrin is an ectoparasiticide of the synthetic pyrethroid group. According to current knowledge the synthetic pyrethroids interfere with the sodium channel of nerve cell membranes, resulting in a delay in repolarization of the nerve and finally killing of the parasite. In studies on structure-activity relationship of a number of pyrethroids interference with receptors of a certain chiral conformation was noted thereby causing a selective activity on ectoparasites. No anti-cholinesterase activity was noted with these compounds. Flumethrin is responsible for the product’s acaricidal activity and also prevents production of fertile eggs by its lethal effect on female ticks. In an in-vitro study 5 to 10 % of Rhipicephalus sanguineus ticks exposed to a sublethal dose of 4 mg flumethrin/L laid eggs which had a modified appearance (shrivelled, dull and dry) indicating a sterilising effect.
In addition to the tick species listed under section 'Indications for use' activity has been demonstrated against Ixodes hexagonus, I. scapularis and the non-European tick species Dermacentor variabilis and the Australian paralysis tick I. holocyclus.
The veterinary medicinal product provides repellent (anti-feeding) activity against the claimed ticks, thus preventing repelled parasites from taking a blood meal and thereby indirectly aids in the reduction of the risk of Vector-Borne Disease transmission.
Cats
In addition to the indications listed under 'indications for use for each target species' activity against Ixodes hexagonus and the non-European tick species Amblyomma americanum has been demonstrated.
The veterinary medicinal product provides repellent (anti-feeding) activity against the claimed ticks, thus preventing repelled parasites from taking a blood meal and thereby indirectly aids in the reduction of the risk of Vector-Borne Disease transmission. Indirect protection against the transmission of Cytauxzoon felis (transmitted by Amblyomma americanum ticks) has been shown in one laboratory study in a small number of animals at one month after treatment, thereby reducing the risk of diseases caused by this pathogen under the conditions of this study.
Dogs
The veterinary medicinal product provides repellent (anti-feeding) activity against the claimed ticks, thus preventing repelled parasites from taking a blood meal and thereby indirectly aids in the reduction of the risk of Canine Vector-Borne Disease transmission.
In addition to the pathogens listed in section 3.2, indirect protection against the transmission of Babesia canis canis (by Dermacentor reticulatus ticks) has been shown in one laboratory study at day 28 after treatment, and indirect protection against the transmission of Anaplasma phagocytophilum (by Ixodes ricinus ticks) has been shown in one laboratory study at 2 months after treatment, thereby reducing the risk of diseases caused by these pathogens under the conditions of these studies.
Data from efficacy studies against sand flies (Phlebotomus perniciosus) showed a variable sand fly repellent (anti-feeding) efficacy ranging from 65 to 89% for 7-8 months following initial application of the collar. Data from 3 clinical field studies performed in endemic areas indicate a significant reduction in the risk of Leishmania infantum transmission by sand flies in treated dogs compared to non-treated dogs. Depending on the infection pressure by sand flies the efficacy in the reduction of the risk of infection with leishmaniosis ranged from 88.3 to 100%.
The collars were able to improve the Sarcoptes scabiei infestation in pre-infested dogs leading to a full cure after three months.
Pharmacokinetic particulars
Both active ingredients are slowly and continuously released in low concentrations from the polymer matrix system of the collar towards the animal. Both actives are present in the animal’s haircoat in acaricidal/insecticidal concentrations during the entire efficacy period. The active substances spread from the site of direct contact over the entire skin surface. Target animal overdose and serum kinetic studies have established that imidacloprid reached the systemic circulation transiently while flumethrin was mostly not measurable. Oral absorption of both active substances is not relevant for the clinical efficacy.
Environmental properties
See section 'Special precautions for the disposal of unused veterinary medicinal product or waste materials derived from the use of such products'