Selamectin

Selamectin
Clinical data
Trade names	Revolution, Stronghold, Revolt
Other names	25-cyclohexyl-25-de(1-methylpropyl)-5-deoxy-22,23-dihydro-5-(hydroxyimino)-avermectin B1 monosaccharide
AHFS/Drugs.com	International Drug Names
License data	US DailyMed: Selamectin;
Routes of; administration	Topical
ATCvet code	QP54AA05 (WHO) QP53BX55 (WHO);
Legal status
Legal status	US: ℞-only; EU: Rx-only;
Identifiers
CAS Number	220119-17-5 ;
PubChem CID	9578507;
ChemSpider	16738655 ;
UNII	A2669OWX9N;
ChEMBL	ChEMBL160777 ;
CompTox Dashboard (EPA)	DTXSID6045903 ;
ECHA InfoCard	100.250.168
Chemical and physical data
Formula	C43H63NO11
Molar mass	769.973 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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 ; Key:AFJYYKSVHJGXSN-XHKIUTQPSA-N ;
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Selamectin, sold under the brand name Revolution, among others, is a topical parasiticide and anthelminthic used on dogs and cats.^[2] 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.^{[citation needed]} It is structurally related to ivermectin and milbemycin.^{[citation needed]} Selamectin is not approved for human use.^{[citation needed]}

Veterinary uses

Selamectin is applied topically.^[2] 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.^{[citation needed]} Absorbed into the body through the skin and hair follicles, it travels through the bloodstream, intestines, and sebaceous glands;^{[citation needed]} 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.^[5]

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]}

Society and culture

Brand names

Selamectin is sold under various brand names including Selehold, manufactured by KRKA, Selarid manufactured by Norbrook Laboratories Limited, Revolution and Stronghold manufactured by Zoetis, Revolt manufactured by Aurora Pharmaceuticals, and Senergy manufactured by Virbac.

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]}

References

^ 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.{{cite journal}}: CS1 maint: overridden setting (link)
^ ^a ^b ^c ^d "Revolution- selamectin solution". DailyMed. 1 December 2023. Retrieved 6 February 2024.
^ "Evicto EPAR". European Medicines Agency. 1 August 2019. Retrieved 26 June 2024.
^ "Stronghold EPAR". European Medicines Agency. 25 March 2008. Retrieved 29 June 2024.
^ 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 14 April 2008. Retrieved 5 July 2008.

[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.{{cite journal}}: CS1 maint: overridden setting (link)

[Revolution_FDA_label-2] "Revolution- selamectin solution". DailyMed. 1 December 2023. Retrieved 6 February 2024.

[3] "Evicto EPAR". European Medicines Agency. 1 August 2019. Retrieved 26 June 2024.

[4] "Stronghold EPAR". European Medicines Agency. 25 March 2008. Retrieved 29 June 2024.

[5] 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 14 April 2008. Retrieved 5 July 2008.

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