Selamectin

Selamectin

File:Selamectin Structural Formulae V.1.svg
File:Selamectin sf.gif
Clinical data
Trade names	Revolution, Stronghold
AHFS/Drugs.com	International Drug Names
Routes of administration	Topical
Identifiers
CAS Number	220119-17-5 N
ATCvet code	QP54AA05 (WHO) QP53BX55 (WHO)
PubChem	CID: 9578507
ChemSpider	16738655
UNII	A2669OWX9N Y
ChEMBL	CHEMBL160777 N
Chemical data
Formula	C43H63NO11
Molecular mass	769.96 g/mol
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 (trade names Revolution, Stronghold) is a topical parasiticide and antihelminthic used on dogs and cats, distributed by Zoetis, a former Pfizer subsidiary. 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 also removes 2 types of lungworm in cats (Aelurostrongylus abstrusus, Eucoleus aerophilus) and one type of lungworm in dogs (Eucoleus aerophilus). It is structurally related to ivermectin and milbemycin. Selamectin is not approved for human use.

Usage

The drug is applied topically. It is waterfast, and does not lose its effectiveness with bathing. It is packaged according to its varying dosage sizes, and is applied once monthly.

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.

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.

Side effects

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

Selamectin has high safety ratings, with less than 1% of pets displaying side effects. 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. This would be a reaction due to undetected infections prior to using the medication, rather than an actual allergic reaction to the drug itself.

Similar products

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

External links

• Pfizer Canada