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Pharmacology

A winning combination: Two ingredients, one innovative product. The winning combination of Imidacloprid – the fast topical flea control known from Advantage® – and Permethrin, one of the most effective pyrethroids. Working together they create a perfect team: advantix® for perfect protection. Because 1+1 makes for more than 2.

Imidacloprid – the known ingredient from the fast topical flea control – Advantage®

Imidacloprid is an ectoparasiticide belonging to the chloronicotinyl group of compounds. Chemically, it can be classified as a chloronicotinyl nitroguanidine. Imidacloprid is effective against adult fleas and larval flea stages. In addition to the adulticide flea efficacy of Imidacloprid, a larvicidal flea efficacy in the surroundings of the treated pet has been demonstrated. Larval stages in the dog's immediate surroundings are killed following contact with a treated animal. It has a high affinity for the nicotinergic acetylcholine receptors in the post-synaptic region of the central nervous system (CNS) in insects. The ensuing inhibition of cholinergic transmission in insects results in paralysis and death of the parasite.

Permethrin – a type I pyrethroide

Permethrin belongs to the type I class of pyrethroid acaricides and insecticides and also acts as a repellent. Pyrethroids affect the voltage-gated sodium channels in vertebrates and non-vertebrates. Pyrethroids are so called “open channel blockers” affecting the sodium ion channel by increasing the channel's mean open time thus leading to hyperexcitability and death of the parasite.

Two proven ingredients with enhanced activity

In the combination of both substances, it has been shown that Imidacloprid functions as the activator of arthropod ganglion and therefore increases the efficacy of permethrin.

  • First Imidacloprid activates the nicotinergic acetylcholine receptor and increases the excitability and the frequency of the spikes produced.
  • Second, as a result, more sodium channels are opened and the pyrethroid can interact much better with its target site. In this way Imidacloprid, combined with Permethrin, overwhelms the nervous system of the parasite with neurotoxic activity beyond results of the compounds alone, leading to a more profound and quicker paralysis and death of the arthropods.

Imidacloprid-activated neuron and the Permethrin-enhanced action potential.  Click the picture to enlarge

         

Fig. 4: Nervous system activity of a resting nerve (a); Imidacloprid and Permethrin alone (b, c) and a combination of both (d)
Imidacloprid, combined with Permethrin, overwhelms the nervous system of the parasite with neurotoxic activity.
 Click the picture to enlarge

advantix® repels and kills

advantix® provides repellent (anti-feeding) activity against ticks, sand flies and mosquitoes, thus preventing the repelled parasites from taking a blood meal and thus reducing the risk of disease transmission (e.g. Lyme borreliosis, babesiosis, anaplasmosis, ehrlichiosis, rickettsiosis, leishmaniosis). However, there may be an attachment of single ticks or bites by single sand flies or mosquitoes. For this reason, a transmission of infectious diseases by these parasites cannot be completely excluded if conditions are unfavourable. advantix® provides repellent (anti-feeding) activity against stable flies thereby assisting in the prevention of fly-bite dermatitis.

advantix® is indicated for dermal administration. Following topical application in dogs, the solution rapidly distributes over the body surface of the animal. Both active substances remain detectable on the skin and hair of the treated animal for 4 weeks.

Acute dermal studies in the rat and target animal, overdose and serum kinetic studies have established that systemic absorption of both active substances after application on intact skin is low, transient and not relevant for the clinical efficacy.

 
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