莫西克丁
Moxidectin
Semi-synthetic methoxime derivative of nemadectin
別名: Cydectin · ProHeart · Advantage Multi · Quest · ComboCare · Advocate · Bravecto Plus · Endectrid · Moxiclear · Prinovox · CL-301423 · Moxidectina · Moxidectinum
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Prevention of heartworm disease, adult fleas, hookworms, roundworms, and whipworms (Advantage Multi) | 10 mg/kg imidacloprid with 2.5 mg/kg moxidectin once a month by topical administration | topical | q30d | — | 🌎 NA |
| Heartworm prevention, hookworms (ProHeart 6) | 0.05 mL of the constituted suspension/kg body weight (provides 0.17 mg moxidectin/kg) | SC | q6mo | — | 🌎 NA |
| Scabiocidal therapy | 0.25 mg/kg SC every 7 days for three treatments OR 0.4 mg/kg PO every 3-4 days for 3-6 weeks | SC/PO | q7d or q3-4d | 3-6 weeks | 🌎 NA |
| Generalized demodicosis | 0.2-0.4 mg/kg PO once a day | PO | q24h | Until parasitic cure (averages 112 days) | 🌎 NA |
| Treatment of canine sarcoptic mange | 10 mg/kg body weight imidacloprid and 2.5 mg/kg body weight moxidectin | topical | q14d | 3 occasions | 🌍 EU |
| Flea, lice, mite, nematode treatment and heartworm/angiostrongylosis prevention | 10 mg/kg body weight imidacloprid and 2.5 mg/kg body weight moxidectin | topical | monthly | Ongoing for prevention | 🌍 EU |
- Prevention of heartworm disease, adult fleas, hookworms, roundworms, and whipworms (Advantage Multi): For dogs 3-9 lb = 0.4 mL; 9.1-20 lb = 1 mL; 20.1-55 lb = 2.5 mL, 55.1-88 lb = 4 mL.
- Heartworm prevention, hookworms (ProHeart 6): Do not overdose growing puppies. Mix at least 30 minutes prior to use.
- Scabiocidal therapy: May cause toxicity in ABCB1 mutant genotype dogs.
- Generalized demodicosis: May cause toxicity in ABCB1 mutant genotype dogs.
- Treatment of canine sarcoptic mange: Apply via spot-on pipette.
- Flea, lice, mite, nematode treatment and heartworm/angiostrongylosis prevention: Frequent shampooing may reduce efficacy.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Prevention of heartworm disease, adult fleas, ear mites, hookworms, and roundworms (Advantage Multi) | 10 mg/kg imidacloprid/1 mg/kg moxidectin once a month by topical administration | topical | q30d | — | 🌎 NA |
| Feline Aelurostrongylosis (Aelurostrongylus abstrusus) | One to three topical applications of 1 mg/kg moxidectin (in combination with imidacloprid) | topical | 1-3 applications | — | 🌎 NA |
| Flea, mite, nematode treatment and heartworm prevention | 10 mg/kg body weight imidacloprid and 1.0 mg/kg body weight moxidectin | topical | monthly | Ongoing for prevention | 🌍 EU |
| Flea/tick control and heartworm/nematode prevention (Bravecto Plus) | 280 mg/ml fluralaner and 14 mg/ml moxidectin (volume based on weight) | topical | q12w for flea/tick control, q8w for heartworm prevention | Ongoing | 🌍 EU |
- Prevention of heartworm disease, adult fleas, ear mites, hookworms, and roundworms (Advantage Multi): For cats 2-5 lb = 0.23 mL; 5.1-9 lb = 0.4 mL; 9.1-18 lb = 0.8 mL.
- Flea, mite, nematode treatment and heartworm prevention: Apply via spot-on pipette. Severe effects may be seen if applied to cats with adult heartworm disease.
- Flea/tick control and heartworm/nematode prevention (Bravecto Plus): Not for use in kittens <9 weeks or cats <1.2 kg.
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Gastrointestinal parasites (Oral Gel) | Dial in the weight of the animal on the syringe | PO | single dose | — | 🌎 NA |
| Mucosal stages of small strongyles | 400 micrograms/kg PO | PO | single dose | — | 🌎 NA |
- Gastrointestinal parasites (Oral Gel): Horses weighing more than 1250 lb require additional gel from a second syringe.
牛
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Internal and external parasites (Pour-On) | 1 mL (5 mg)/10 kg (22 lb) bodyweight applied directly to the hair and skin along the top of the back | topical | single dose | — | 🌎 NA |
| Internal and external parasites (Injectable) | 0.2 mg/kg [1 mL for each 110 lb (50 kg) of bodyweight] subcutaneously | SC | single dose | — | 🌎 NA |
羊
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Internal parasites | 0.2 mg/kg [1 mL per 11 lb (1 mL per 5 kg) bodyweight] PO (drench) | PO | single dose | — | 🌎 NA |
| Gastrointestinal helminthes in Camelids (NWC) | 0.2 mg/kg | PO | single dose | — | 🌎 NA |
- Gastrointestinal helminthes in Camelids (NWC): Regimen of choice for camelids.
山羊
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Internal parasites | Twice the sheep dose (0.4 mg/kg) | PO | single dose | — | 🌎 NA |
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
莫西克丁 (Moxidectin) 是一種強效的第二代巨環內酯類（阿維菌素/米爾貝黴素亞類）抗寄生蟲藥物，廣泛應用於小動物及大動物獸醫學中。
主要藥理特徵包括：
- 廣效性：對多種體內線蟲（蛔蟲、鉤蟲、鞭蟲、心絲蟲幼蟲）及體外節肢動物（跳蚤、蟎蟲、蝨子、牛皮蠅蛆）均有效。
- 高脂溶性：莫西克丁的脂溶性約為伊維菌素 (Ivermectin) 的 100 倍。這使其能在組織中廣泛分佈、半衰期延長，並能製成長效緩釋劑型（例如 6 個月注射型心絲蟲預防藥）。
- ABCB1 (MDR1) 安全性：雖然帶有 ABCB1-1∆ 基因突變的犬隻對巨環內酯類藥物敏感，但在 FDA 核准的標準標籤劑量下（滴劑與口服心絲蟲預防），莫西克丁對這些品種通常是安全的。然而，若超仿單高劑量使用（例如治療毛囊蟲症），可能會引發嚴重的神經毒性。
本藥物有多種劑型，包括外用滴劑（常與益達胺 imidacloprid 結合使用）、緩釋注射液、口服凝膠及澆潑劑。
作用機制
Moxidectin exerts its antiparasitic effects by disrupting the neurological function of invertebrates:
- Glutamate-Gated Chloride Channels (GluCl): Moxidectin binds selectively and with high affinity to GluCl channels present in invertebrate nerve and muscle cells → increases membrane permeability to chloride ions → causes cellular hyperpolarization → results in flaccid paralysis and death of the parasite.
- GABA Receptors: It also enhances the release of gamma-aminobutyric acid (GABA) at presynaptic neurons, further blocking post-synaptic stimulation.
Mammalian Safety: Mammals do not possess GluCl channels. Furthermore, the P-glycoprotein (P-gp) efflux pump at the mammalian blood-brain barrier actively prevents moxidectin from entering the central nervous system, protecting mammalian GABA receptors from exposure.
安全性與警告
禁忌症
- Hypersensitivity to the drug
- Dogs not tested for heartworm infection prior to use
- Sick, debilitated, or underweight dogs (specifically for the 6-month injectable)
- Female dairy cattle of breeding age
- Horses intended for food purposes
- Foals younger than 4 months of age
- Kittens < 9 weeks of age
- Dogs < 7 weeks of age
- Dogs with Class 4 heartworm disease
- Cats < 1.2 kg (for fluralaner combination)
- Breeding males (for fluralaner combination)
不良反應
- Dogs: Lethargy, vomiting, ataxia, anorexia, diarrhea, nervousness, weakness, polydipsia, pruritus
- Dogs (Injectable): Rare but serious reports of anaphylaxis, liver disease, autoimmune hemolytic disease, convulsions
- Cats: Recumbency (rare)
- Horses: Minimal at labeled doses; CNS depression and coma reported in foals at high doses
- Cattle: Minimal to nonexistent at labeled doses
- Transient pruritus at application site
- Erythema at application site
- Hypersalivation (if licked)
- Emesis and haematemesis
- Diarrhoea
- Pyrexia
- Tachypnoea
- Mydriasis
- Severe systemic reactions in cats with adult heartworm disease
注意事項
Heartworm Testing: Always test dogs for existing heartworm infections before initiating moxidectin therapy. Adult heartworms and microfilariae should be removed prior to therapy.
- ABCB1 (MDR1) Mutants: Safe at standard labeled preventative doses. However, off-label high doses (e.g., for demodicosis or scabies) can cause severe neurotoxicity in herding breeds with this mutation.
- Body Condition: Animals with very low body fat (neonates, cachexia) may experience significantly higher serum levels due to the drug's extreme lipophilicity, making them more prone to adverse reactions.
- Vaccinations: Caution is advised when administering the 6-month sustained-release injection concurrently with vaccinations, as anaphylaxis has been reported.
藥物相互作用
Effects may be potentiated by moxidectin; concurrent use is generally not advised.
May inhibit the efflux pump at the blood-brain barrier, potentially increasing the risk of moxidectin neurotoxicity, especially in dogs with the ABCB1-1∆ mutation.
Increased risk of neurological toxicity due to competitive inhibition at the blood-brain barrier
Additive toxicity and increased risk of adverse neurological effects
監測
- Heartworm status prior to initiation of therapy
- Fecal egg count reduction testing (FECRT) in horses (target >95% reduction to monitor for resistance)
- Signs of neurotoxicity, especially in herding breeds or animals with low body fat
- Heartworm status (antigen/microfilariae testing) prior to initiating preventative therapy
- Resolution of clinical signs of parasitic infection
- Application site for erythema or pruritus
藥物動力學
半衰期
吸收
Highly lipophilic (100 times that of ivermectin).
分佈
Volumes of distribution are very high due to extreme lipophilicity. Animals with very low body fat (neonates, cachexia) may have significantly higher serum levels than normal patients.
代謝
Hepatic metabolism (inferred from macrocyclic lactone class properties).
排除
Long duration of plasma residence (14-15 days in cattle). After SC injection in cows, approximately 5% of the dose can be passed to the suckling calf.
過量
Moxidectin generally has a wide margin of safety when administered at labeled doses.
- Dogs: Dosages up to 300X (1120 mcg/kg) demonstrated little to no effects in normal dogs. However, in dogs with the ABCB1 (MDR1) mutant genotype, toxicity can be seen at doses as low as 90 mcg/kg.
- Clinical Signs of Toxicity: Dysorexia, hypersalivation, mydriasis, fasciculations, ataxia, tremors, seizures, vomiting, hyperesthesia, and recumbency/coma.
- Treatment: Supportive care. Intravenous fat emulsion (IVFE) has been successfully used to treat toxicity associated with macrocyclic lactones due to their highly lipid-soluble nature.
可用產品
劑型
- Sustained-release injection (microspheres)
- Topical solution (spot-on)
- Pour-on solution
- Injectable solution
- Oral drench
- Oral gel
- Topical spot-on: 10 mg/kg imidacloprid + 1.0 mg/kg moxidectin (Cats)
- Topical spot-on: 10 mg/kg imidacloprid + 2.5 mg/kg moxidectin (Dogs)
- Topical spot-on: 280 mg/ml fluralaner + 14 mg/ml moxidectin (Cats - Bravecto Plus)
獸醫用
- ProHeart 6: 10% Sustained-Release Injectable (598 mg/vial)
- Cydectin Pour-On for Cattle: 0.5% (5 mg/mL)
- Cydectin Injectable Solution: 10 mg/mL
- Cydectin Oral Drench for Sheep: 1 mg/mL
- Quest Oral Gel: 20 mg/mL
- Quest Plus Oral Gel: 20 mg/mL moxidectin + 125 mg/mL praziquantel
- Advantage Multi for Cats: 10 mg/mL moxidectin + 100 mg/mL imidacloprid
- Advantage Multi for Dogs: 25 mg/mL moxidectin + 100 mg/mL imidacloprid
- Advocate spot-on solution
- Bravecto Plus spot-on solution
- Endectrid spot-on solution
- Moxiclear spot-on solution
- Prinovox spot-on solution
各地核准狀態
停藥期: cattle meat 14-65 days depending on formulation
POM-V classification.
POM-V classification.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
ProHeart 6: Store unconstituted product at or below 25°C (77°F) and protect from light. Once constituted, stable for 4 weeks under refrigeration at 2°-8°C (36°-46°F). Cydectin injection/drench: Store at or below 25°C (77°F) and protect from light. Cydectin Pour-on: Store at or below room temperature; do not freeze. Quest gel: Store at room temperature (59°F-86°F); avoid freezing.
飼主須知
- 心絲蟲檢測：在開始使用本藥物前，您的寵物必須先進行心絲蟲檢測。若寵物已感染心絲蟲卻使用本藥，可能會引發嚴重的副作用。
- 使用方法：若使用外用滴劑，請直接點在頸部基部或肩胛骨之間的皮膚上（撥開毛髮），確保寵物無法舔舐。在滴劑乾燥前，請將治療過的寵物與其他寵物及兒童隔離數小時。
- 副作用：請觀察寵物是否有嗜睡、嘔吐、步態不穩（共濟失調）或過度流口水等症狀。若發現任何神經學異常跡象，請立即聯絡您的獸醫師。
- ProHeart 6 (長效注射劑)：若您的愛犬接受了 6 個月效期的注射劑，請務必閱讀獸醫師提供的寵物主人資訊表，並在注射後的幾天內密切觀察是否有過敏反應（如臉部腫脹、蕁麻疹、嚴重嗜睡）。
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