Selamectin (UK-124,114)
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Product Description
Selamectin is a semi-synthetic avermectin antiparasitic drug widely used in veterinary medicine, known by its brand name Revolution®. It is a topical agent works by enhancing the release of gamma-aminobutyric acid (GABA) at parasite neuromuscular junctions, leading to paralysis and death of the parasite. It is effective against a broad spectrum of internal and external parasites, including fleas, ear mites, hookworms, roundworms, and certain ticks, and helps prevent heartworm disease caused by Dirofilaria immitis. Structurally similar to ivermectin, selamectin has a methoxime group at the C-5 position, which enhances its safety profile and topical efficacy. It is absorbed through the skin into the bloodstream and excreted primarily in feces. Selamectin is generally safe when used as directed, with mild side effects such as temporary hair loss or skin irritation at the application site. It should not be used in sick, debilitated, or underweight animals.
Additional Information
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Similar Products: Other products used for parasite control include ivermectin, milbemycin oxime, moxidectin, fipronil, and lufenuron.
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Human Use: Not approved for human use.
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Solubility: Not water-miscible.
Uses
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Veterinary Medicine:
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Dogs: Treats and prevents heartworms, fleas, ear mites, sarcoptic mange (scabies), and certain ticks (e.g., American dog tick).
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Cats: Treats and prevents heartworms, fleas, ear mites, hookworms, and roundworms.
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Effectiveness: Effective against both internal (endoparasites like heartworms) and external parasites (ectoparasites like fleas).
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Application: Applied topically to the skin, typically on the back of the neck.
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Brand Names: Marketed under brand names such as Revolution and Stronghold.
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Mechanism of Action
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Neuromuscular Paralysis: Selamectin activates glutamate-gated chloride channels in parasite muscle synapses, leading to an influx of chloride ions into nerve cells. This causes hyperpolarization, neuromuscular paralysis, impaired muscle contraction, and ultimately the death of the parasite.
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Distribution: After topical application, it is absorbed through the skin and hair follicles, distributing via the bloodstream, intestines, and sebaceous glands. Parasites ingest it when feeding on the host's blood or secretions.
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Molecular Formula (MF): C₄₃H₆₃NO₁₁
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Molecular Weight (MW): 770 g/mol
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IUPAC Name: (1R,4S,5'S,6R,6'S,8R,10E,12S,13S,14E,16E,20R,21Z,24S)-6'-cyclohexyl-24-hydroxy-21-hydroxyimino-12-[(2R,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
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Structure Description: Selamectin is a macrocyclic lactone with a complex structure featuring multiple rings, including a spiroketal moiety, an oxime group, and a disaccharide-like component (though it's a monosaccharide derivative). It is derived from avermectin B1 through selective hydrolysis and oximation. Its SMILES notation is: C[C@H]1CC[C@]2(C[C@@H]3CC@HC/C=C(/C@HO[C@H]6CC@@HOC)\C)O[C@@H]1C7CCCCC7.
Safety and Side Effects
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Safety Profile: Generally well-tolerated with side effects occurring in less than 1% of treated animals.
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Common Side Effects: Temporary irritation or hair loss at the application site.
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Rare Side Effects: Drooling, rapid breathing, lack of coordination, vomiting, or diarrhea, often due to the rapid die-off of parasites like heartworms rather than direct toxicity from the drug.
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Usage Guidance: Should be used under veterinary guidance.