도라멕틴

항기생충약 - 아버멕틴계

도라멕틴은 아버멕틴계 항기생충약에 속하는 **대식환 락톤(macrocyclic lactone)** 약물입니다. - **산업동물 용도**: 소와 돼지의 다양한 위장관 선충, 폐충, 안충, 쇠파리 유충, 이, 옴 진드기 치료를 위한 주사제 및 스팟온(pour-on) 제제로 FDA 승인을 받았습니다. - **반려동물 용도**: 개와 고양이에서 주로 **전신성 모낭충증** 및 식도선충증 치료를 위해 허가 외(extra-label)로 사용됩니다. > **임상 요점**: 매우 효과적이지만 소동물에서의 사용은 전적으로 허가 외 사용이며, 특히 MDR1(ABCB1) 유전자 돌연변이가 있는 목양견 품종에서는 심각한 신경독성 위험이 있습니다.

작용 기전: Doramectin exerts its antiparasitic effect by binding to **glutamate-gated chloride channels** found in invertebrate nerve and muscle cells. - **Mechanism**: Binding → increases membrane permeability to chloride ions → cellular hyperpolarization → **flaccid paralysis and death** of the parasite. - It also enhances the release of **gamma-aminobutyric acid (GABA)** at presynaptic neurons, further inhibiting nerve transmission. - **Mammalian Safety**: Mammals lack glutamate-gated chloride channels, and avermectins typically do not cross the intact mammalian blood-brain barrier (where GABA receptors reside) due to the **P-glycoprotein efflux pump**. Toxicity occurs when this pump is deficient (e.g., MDR1 mutation) or overwhelmed by massive overdoses.

동물 종별 용량

Cats

Feline demodicosis (D. cati, D. gatoi) · 600 micrograms/kg (0.6 mg/kg) · SC · once per week · Extra-label. Get informed consent from owner. Alternative treatments include Lime sulfur dips or amitraz.

Cattle

Labeled indications (Injectable) · 200 micrograms/kg (1 mL per 110 lb. body weight) · SC/IM · once · Beef Quality Assurance guidelines recommend SC administration as the preferred route.
Labeled indications (Pour-on) · 500 micrograms/kg (1 mL per 22 lb. body weight) · topical · once · Administer topically along the mid-line of the back in a narrow strip between the withers and tailhead.

Swine

Labeled indications · 300 micrograms/kg (1 mL per 75 lb. body weight) · IM · once · Intramuscular injections should be administered into the muscular region of the neck.

SmallMammals

P. cuniculi infestations (Rabbits) · 200 micrograms/kg · IM · once · once

Dogs

Treatment of generalized demodicosis · 600 micrograms/kg · PO · once daily · Until 60 days without improvement · Extra-label. If improvement is not seen after 60 days, an alternative therapy should be used.
Treatment of generalized demodicosis · 600 micrograms/kg (0.6 mg/kg) · SC · once per week · Extra-label. Get informed consent from owner.

투여 경로

POIMSCtopical

금기

Dogs with MDR1-allele mutations (relative/absolute depending on dose)
Female dairy cattle 20 months of age or older
Calves to be processed for veal

이상반응

Injection site blemishes (IM administration)
Pupil dilation (mydriasis) in dogs
Lethargy
Blindness
Coma (especially in MDR1-mutant dogs)

모니터링

Clinical efficacy (resolution of parasites/lesions)
Signs of neurotoxicity in off-label species (dogs/cats)

과용량

In field trials, no toxic signs were seen in cattle given up to 25X the recommended dose. In breeding animals (bulls, and cows in early and late pregnancy), a dose 3 times the recommended dose had no effect on breeding performance.

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