エプリノメクチン
エプリノメクチンは、主に牛の局所用ポアオン(滴下)液として使用される、非常に効果的な**アベルメクチン系抗寄生虫薬**です。胃腸内線虫、肺虫、ウシバエ幼虫、シラミ、ヒゼンダニ、ツノバエなど、さまざまな内部および外部寄生虫に対して広範な駆虫効果を発揮します。 - **主な利点**: 牛に対して規定通りに使用した場合、**休薬期間(搾乳および食肉)が不要**であり、酪農および肉牛農家にとって非常に利便性が高いです。 - **適応外使用**: 馬のキュウセンダニ(*Psoroptic* mange)やウサギの耳ダニ(*Psoroptes cuniculi*)の治療にも有効性が示されています。 *臨床のポイント*: マクロライド系抗寄生虫薬として、イベルメクチンと同様の安全性を持ちますが、反芻動物における局所吸収を最適化するように特別に処方されています。
作用機序: Eprinomectin exerts its antiparasitic effect by binding selectively to **glutamate-gated chloride ion channels** found in invertebrate nerve and muscle cells. - **Mechanism**: Binding → Increased cell membrane permeability to chloride ions → Hyperpolarization of the nerve/muscle cell → **Paralysis and death** of the parasite. - It also enhances the release of **gamma-aminobutyric acid (GABA)** at presynaptic neurons, which acts as an inhibitory neurotransmitter, blocking post-synaptic stimulation. - *Safety*: Mammals are generally unaffected because they lack glutamate-gated chloride channels, and macrocyclic lactones do not readily cross the mammalian blood-brain barrier (BBB) under normal conditions.
動物種別の用量
- Treatment and prevention of fleas, ticks, nematodes (including feline lungworm and Capillaria plica), and prevention of heartworm disease · Monthly application · topical · monthly · 1 month per application · Apply appropriate pipette size based on cat's body weight.
- Treatment of psoroptic (P. equi) mange · 500 micrograms/kg (0.5 mg/kg) topically once weekly for 4 treatments · topical · once weekly · 4 treatments · Author's suggest getting informed consent before use.
- Ear mites (Psoroptes cuniculi) in rabbits · 5 mg/kg topically, twice at 14 day intervals · topical · twice at 14 day intervals · 2 treatments · One small study (6 subjects) showed partial response.
- Labeled indications (gastrointestinal roundworms, cattle grubs, lice, mange mites, horn flies, lungworms) · 1 mL per 10 kg (22 lb) body weight applied topically along backline in a narrow strip from the withers to the tailhead · topical · once
用量は獣医療従事者向けの臨床リファレンスです。必ず最新の添付文書と個々の患者で確認してください。
投与経路
禁忌
- Oral administration
- Intravenous administration
- Cats weighing < 0.6 kg
- Kittens < 7 weeks of age
- Dogs (not intended for use)
有害事象
- Ineffectiveness for parasite control (reported in FDA database)
- Anorexia
- Udder hypogalactia
- Mild clumping of the hair at the application site
薬物相互作用
- ciclosporin · Potential interaction as both are P-glycoprotein substrates; none reported clinically · minor
- itraconazole · Potential interaction as both are P-glycoprotein substrates; none reported clinically · minor
- loperamide · Potential interaction as both are P-glycoprotein substrates; none reported clinically · minor
- steroids · Potential interaction as both are P-glycoprotein substrates; none reported clinically · minor
- opiates · Potential interaction as both are P-glycoprotein substrates; none reported clinically · minor
- P-glycoprotein substrates (e.g., ciclosporin, itraconazole, loperamide, steroids, opiates) · Theoretical potential for interaction due to shared P-glycoprotein efflux pump mechanisms, though none have been clinically reported. · minor
モニタリング
- Clinical efficacy (parasite clearance)
- Adverse reactions (anorexia, milk production in dairy cattle)
- Efficacy of parasite control
- Application site reactions (hair clumping, alopecia, erythema)
過量投与
Calves given up to 5X dosage showed no signs of adverse effects. One subject (of 6) showed signs of mydriasis when given a 10X dose.
VetSheet の薬剤リファレンスは、獣医療従事者向けの臨床意思決定支援を目的としており、専門的判断やメーカーの最新添付文書に代わるものではありません。