Selamectin

Last updated
Selamectin
Selamectin Structural Formulae V.1.svg
Selamectin sf.gif
Clinical data
Trade names Revolution, Stronghold, Revolt
Other names25-cyclohexyl-25-de(1-methylpropyl)-5-deoxy-22,23-dihydro-5-(hydroxyimino)-avermectin B1 monosaccharide [1]
AHFS/Drugs.com International Drug Names
Routes of
administration
Topical
ATCvet code
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.250.168 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C43H63NO11
Molar mass 769.973 g·mol−1
3D model (JSmol)
  • C[C@H]1CC[C@]2(C[C@@H]3C[C@H](O2)C/C=C(/[C@H]([C@H](/C=C/C=C/4\CO[C@H]\5[C@@]4([C@@H](C=C(/C5=N/O)C)C(=O)O3)O)C)O[C@H]6C[C@@H]([C@H]([C@@H](O6)C)O)OC)\C)O[C@@H]1C7CCCCC7
  • InChI=1S/C43H63NO11/c1-24-11-10-14-30-23-50-40-36(44-48)27(4)19-33(43(30,40)47)41(46)52-32-20-31(16-15-25(2)38(24)53-35-21-34(49-6)37(45)28(5)51-35)54-42(22-32)18-17-26(3)39(55-42)29-12-8-7-9-13-29/h10-11,14-15,19,24,26,28-29,31-35,37-40,45,47-48H,7-9,12-13,16-18,20-23H2,1-6H3/b11-10+,25-15+,30-14+,44-36-/t24-,26-,28-,31+,32-,33-,34-,35-,37-,38-,39-,40+,42+,43+/m0/s1 X mark.svgN
  • Key:AFJYYKSVHJGXSN-XHKIUTQPSA-N X mark.svgN
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Selamectin (trade names Selehold manufactured by KRKA, Selarid manufactured by Norbrook Laboratories Limited, Revolution and Stronghold manufactured by Zoetis, Revolt manufactured by Aurora Pharmaceuticals, Senergy manufactured by Virbac, among others) is a topical parasiticide and anthelminthic used on dogs and cats. It treats and prevents infections of heartworms, fleas, ear mites, sarcoptic mange (scabies), and certain types of ticks in dogs, and prevents heartworms, fleas, ear mites, hookworms, and roundworms in cats. It is structurally related to ivermectin and milbemycin. Selamectin is not approved for human use.

Contents

Usage

The drug is applied topically. It is isopropyl alcohol based, packaged according to its varying dosage sizes and applied once monthly. It is not miscible in water. [2]

Mode of action

Selamectin disables parasites by activating glutamate-gated chloride channels at muscle synapses. Selamectin activates the chloride channel without desensitization, allowing chloride ions to enter the nerve cells and causing neuromuscular paralysis, impaired muscular contraction, and eventual death.[ citation needed ]

The substance fights both internal and surface parasitic infection. Absorbed into the body through the skin and hair follicles, it travels through the bloodstream, intestines, and sebaceous glands; parasites ingest the drug when they feed on the animal's blood or secretions.[ citation needed ]

Side effects

Selamectin has been found to be safe and effective in a 2003 review. [3]

Selamectin has high safety ratings, with less than 1% of pets displaying side effects [ citation needed ]. In cases where side-effects do occur, they most often include passing irritation or hair loss at the application site. Symptoms beyond these (such as drooling, rapid breathing, lack of coordination, vomiting, or diarrhea) could be due to shock as a result of selamectin killing heartworms or other vulnerable parasites present at high levels in the bloodstreams of dogs.[ citation needed ] This would be a reaction due to undetected or underestimated infections prior to using the medication, rather than an actual allergic reaction to the drug itself.[ citation needed ]

Similar products

Main rival products for dogs include ivermectin (trade names Stromectol, Ivermec and others) or milbemycin oxime (Interceptor) for heartworms, imidacloprid and moxidectin (Advocate), fipronil (Frontline) or lufenuron (Program) for fleas, or the combination milbemycin oxime/lufenuron (Sentinel) for both.[ citation needed ]

Related Research Articles

<span class="mw-page-title-main">Scabies</span> Human disease

Scabies is a contagious skin infestation by the mite Sarcoptes scabiei. The most common symptoms are severe itchiness and a pimple-like rash. Occasionally, tiny burrows may appear on the skin. In a first-ever infection, the infected person usually develops symptoms within two to six weeks. During a second infection, symptoms may begin within 24 hours. These symptoms can be present across most of the body or just certain areas such as the wrists, between fingers, or along the waistline. The head may be affected, but this is typically only in young children. The itch is often worse at night. Scratching may cause skin breakdown and an additional bacterial infection in the skin.

<span class="mw-page-title-main">Mange</span> Type of skin disease caused by parasitic mites

Mange is a type of skin disease caused by parasitic mites. Because various species of mites also infect plants, birds and reptiles, the term "mange", or colloquially "the mange", suggesting poor condition of the skin and fur due to the infection, is sometimes reserved for pathological mite-infestation of nonhuman mammals. Thus, mange includes mite-associated skin disease in domestic mammals, in livestock, and in wild mammals (for example, foxes, coyotes, cougars and wombats. Severe mange caused by mites has been observed in wild bears. Since mites belong to the arachnid subclass Acari, another term for mite infestation is acariasis.

<span class="mw-page-title-main">Demodicosis</span> Medical condition

Demodicosis, also called Demodex folliculitis in humans and demodectic mange or red mange in animals, is caused by a sensitivity to and overpopulation of Demodex spp. as the host's immune system is unable to keep the mites under control.

<span class="mw-page-title-main">Ivermectin</span> Medication for parasite infestations

Ivermectin is an antiparasitic drug. After its discovery in 1975, its first uses were in veterinary medicine to prevent and treat heartworm and acariasis. Approved for human use in 1987, it is used to treat infestations including head lice, scabies, river blindness (onchocerciasis), strongyloidiasis, trichuriasis, ascariasis and lymphatic filariasis. It works through many mechanisms to kill the targeted parasites, and can be taken by mouth, or applied to the skin for external infestations. It belongs to the avermectin family of medications.

<i>Dirofilaria immitis</i> Species of worm that causes parasitic disease in animals

Dirofilaria immitis, also known as heartworm or dog heartworm, is a parasitic roundworm that is a type of filarial worm, a small thread-like worm, that causes dirofilariasis. It is spread from host to host through the bites of mosquitoes. There are four genera of mosquitoes that transmit dirofilariasis, Aedes, Culex, Anopheles, and Mansonia. The definitive host is the dog, but it can also infect cats, wolves, coyotes, jackals, foxes, ferrets, bears, seals, sea lions and, under rare circumstances, humans.

<span class="mw-page-title-main">Moxidectin</span> Chemical compound

Moxidectin is an anthelmintic drug used in animals to prevent or control parasitic worms (helminths), such as heartworm and intestinal worms, in dogs, cats, horses, cattle and sheep. Moxidectin kills some of the most common internal and external parasites by selectively binding to a parasite's glutamate-gated chloride ion channels. These channels are vital to the function of invertebrate nerve and muscle cells; when moxidectin binds to the channels, it disrupts neurotransmission, resulting in paralysis and death of the parasite.

<span class="mw-page-title-main">Lufenuron</span> Chemical compound

Lufenuron is the active ingredient in the veterinary flea control medication Program, and one of the two active ingredients in the flea, heartworm, ringworm and anthelmintic medicine milbemycin oxime/lufenuron (Sentinel).

<span class="mw-page-title-main">Ear mite</span> Common name of many species of mites that live in the ears of animals and humans

Ear mites are mites that live in the ears of animals and humans. The most commonly seen species in veterinary medicine is Otodectes cynotis. This species, despite its name, is also responsible for 90% of ear mite infections in felines.

<i>Cheyletiella</i> Genus of mites

Cheyletiella is a genus of mites that live on the skin surface of dogs, cats, and rabbits.

<span class="mw-page-title-main">Avermectin</span> Drugs to treat parasitic worms and insect pests

The avermectins are a series of drugs and pesticides used to treat parasitic worms and insect pests. They are a group of 16-membered macrocyclic lactone derivatives with potent anthelmintic and insecticidal properties. These naturally occurring compounds are generated as fermentation products by Streptomyces avermitilis, a soil actinomycete. Eight different avermectins were isolated in four pairs of homologue compounds, with a major (a-component) and minor (b-component) component usually in ratios of 80:20 to 90:10. Avermectin B1, a mixture of B1a and B1b, is the drug and pesticide abamectin. Other anthelmintics derived from the avermectins include ivermectin, selamectin, doramectin, eprinomectin.

The combination milbemycin oxime/lufenuron is a parasite control drug in which the active ingredient, milbemycin oxime, eliminates worms, while a second active ingredient, lufenuron, arrests the development of eggs and larvae, preventing them from maturing and continuing the infestation of an animal. This combination is registered for animal use only. To achieve efficacy, the treatment is administered once monthly, together with food, in a dosage suitable for the weight of the affected animal. The usual ratio is 500 μg milbemycin oxime and 10 mg lufenuron/kg body weight. Novartis indicates the proper dosage by color-coding the packages.

<span class="mw-page-title-main">Thelaziasis</span> Medical condition

Thelaziasis is the term for infestation with parasitic nematodes of the genus Thelazia. The adults of all Thelazia species discovered so far inhabit the eyes and associated tissues of various mammal and bird hosts, including humans. Thelazia nematodes are often referred to as "eyeworms".

<span class="mw-page-title-main">Milbemycin oxime</span> Chemical compound

Milbemycin oxime, sold under the brand name Interceptor among others, is a veterinary medication from the group of milbemycins, used as a broad spectrum antiparasitic. It is active against worms (anthelmintic) and mites (miticide).

<span class="mw-page-title-main">Pyriprole</span> Chemical compound

Pyriprole is for veterinary use on dogs against external parasites such as fleas and ticks.

<span class="mw-page-title-main">Mites of domestic animals</span> Type of parasite of domestic animals

Mites that infest and parasitize domestic animals cause disease and loss of production. Mites are small invertebrates, most of which are free living but some are parasitic. Mites are similar to ticks and both comprise the order Acari in the phylum Arthropoda. Mites are highly varied and their classification is complex; a simple grouping is used in this introductory article. Vernacular terms to describe diseases caused by mites include scab, mange, and scabies. Mites and ticks have substantially different biology from, and are classed separately from, insects. Mites of domestic animals cause important types of skin disease, and some mites infest other organs. Diagnosis of mite infestations can be difficult because of the small size of most mites, but understanding how mites are adapted to feed within the structure of the skin is useful.

<span class="mw-page-title-main">Fluralaner</span> Chemical compound

Fluralaner (INN) is a systemic insecticide and acaricide that is administered orally or topically. The U.S. Food and Drug Administration (FDA) approved it under the trade name Bravecto for flea treatment in dogs in May 2014 and Bravecto Plus as a topical treatment for cats in November 2019, with warnings about possible side effects in both species. The EU approved the drug in February 2014. Australia approved it for the treatment and prevention of ticks and fleas on dogs in January 2015. For treating mites in chickens, a solution for use in drinking water is available under the name Exzolt; it was introduced by the EU in 2017.

<span class="mw-page-title-main">Lotilaner</span> Chemical compound

Lotilaner, sold under the brand name Xdemvy, is an ectoparasiticide (anti-parasitic) medication used for the treatment of blepharitis caused by infestation by Demodex. It is used as an eye drop.

Imidacloprid/moxidectin, sold under the brand names Advantage Multi for Dogs and Advantage Multi for Cats among others, is a medicine for dogs and cats to treat heartworm, fleas, sarcoptic mange, intestinal parasites and ear mites.

<span class="mw-page-title-main">Sarolaner</span> Chemical compound

Sarolaner, sold under the brand name Simparica, is an ectoparasiticide veterinary medication for the treatment of flea and tick infestations in dogs. It is also used off-label to control sarcoptic mange and demodectic mange.

References

  1. Bishop BF, Bruce CI, Evans NA, Goudie AC, Gration KA, Gibson SP, et al. (August 2000). "Selamectin: a novel broad-spectrum endectocide for dogs and cats". Veterinary Parasitology. 91 (3–4): 163–176. doi:10.1016/s0304-4017(00)00289-2. PMID   10940519.
  2. "Revolt Topical - FDA prescribing information, side effects and uses". Drugs.com.
  3. Pipano E (2003). "Recent Developments In The Control Of Ectoparasites And Endoparasites Of Dogs And Cats With Selamectin". Israel Journal of Veterianry Medicine. 58 (2–3). Archived from the original on April 14, 2008. Retrieved 2008-07-05.