多殺菌素
Spinosad
Spinosyn A and Spinosyn D
別名: Comfortis · Natroba · Extinosad · Trifexis · Spinosyn A & B · XDE-105 · Spinosyn D
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
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
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 or treatment of fleas infestations | 30-60 mg/kg (minimum dosage of 30 mg/kg) PO once monthly with food. | PO | q30d | 1 month | 🌎 NA |
| Flea infestation | 45-70 mg/kg | PO | q28d | — | 🌍 EU |
- Prevention or treatment of fleas infestations: Must be given with food for optimal absorption.
- Flea infestation: Give with or immediately after food.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Flea infestation | 50-75 mg/kg | PO | q28d | — | 🌍 EU |
- Flea infestation: Give with or immediately after food.
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
概覽
多殺菌素 (Spinosad) 是一種全身性口服大環內酯類殺蟲劑，源自天然土壤細菌 Saccharopolyspora spinosa。主要用於預防和治療犬隻的跳蚤 (Ctenocephalides felis) 感染。
主要臨床優勢：
- 起效迅速： 30分鐘內開始殺死跳蚤，4小時內完全殺滅，能在成蟲產卵前將其殺死，有效打破跳蚤生命週期。
- 防水性佳： 由於是全身性（口服）給藥，其療效完全不受游泳、洗澡或使用皮膚病洗毛精的影響。
臨床要點： 雖然主要作為除蚤成蟲劑，但初步研究顯示，在較高的仿單標示外劑量下，24小時內對壁蝨 (R. sanguineus*) 也有很高的殺滅效果（儘管未正式標示用於控制壁蝨）。
- 貓咪使用注意事項： 雖然本專論指出未核准用於貓，但 FDA 後來已核准了貓專用的 Comfortis 劑型。請務必參考最新的產品標示以獲取貓咪劑量資訊。
作用機轉
Spinosad targets the insect nervous system through a unique mechanism distinct from other parasiticides:
- Primary Pathway: Acts as an agonist at the nicotinic acetylcholine D-alpha receptors → causes motor neuron activation → leads to involuntary muscle contractions and tremors → prolonged exposure results in paralysis and rapid flea death.
- Secondary Pathway: Opens GABA-gated chloride channels in insects, similar to the mechanism of other macrocyclic lactones, further contributing to neuromuscular paralysis.
Because mammalian nicotinic receptors are structurally different from insect receptors, spinosad exhibits a high margin of safety in dogs.
安全性與警告
禁忌症
- Cats (per this specific monograph's label status)
- Dogs with known pork or soy allergies (chewable tablets contain pork proteins and hydrolyzed soy)
- Dogs and cats weighing < 1.2 kg
- Dogs and cats < 14 weeks of age
- Dogs with MDR1 mutation (relative contraindication due to increased risk of adverse effects)
不良反應
- Vomiting (most common)
- Depression/lethargy
- Diarrhea
- Pruritus
- Trembling
- Hypersalivation
- Seizures (rare)
- Vomiting (occasional)
- Lethargy (rare)
- Diarrhoea (rare)
- Anorexia (rare)
- Ataxia (rare)
注意事項
Use with caution in breeding females and dogs with pre-existing epilepsy, as higher than labeled dosages may decrease the seizure threshold. Safe use in breeding males has not been evaluated. The chewable tablets contain pork proteins and hydrolyzed soy; use cautiously in dogs with severe food allergies to these ingredients.
藥物交互作用
Concurrent use with high extra-label doses of ivermectin (e.g., for demodicosis) increases the risk of neurotoxicity. However, spinosad is safe to use with standard low-dose heartworm preventatives.
Increased risk of severe neurological toxicity. Do not use in combination.
Competition for P-glycoprotein efflux pump, potentially increasing digoxin levels.
Competition for P-glycoprotein efflux pump, potentially increasing doxorubicin toxicity.
監測
- Flea control efficacy
- Adverse gastrointestinal or neurologic effects
- Efficacy of flea control
- Gastrointestinal tolerance (vomiting)
- Adverse neurological signs
藥物動力學
半衰期
吸收
Peak plasma levels for spinosyn A and D occur in about 2 and 3 hours, respectively, when administered with food.
分佈
Extensively bound to canine plasma proteins.
代謝
Undergoes hepatic metabolism.
排除
Excreted in milk at levels approximately 2.5X of that found in plasma.
過量
Spinosad has a wide margin of safety. The oral LD50 in mice is >5000 mg/kg. In canine dose tolerance studies (up to 16.7X the normal dose for 10 days), the primary sign was routine vomiting. No significant changes in hematology or coagulation were noted, though mild elevations in ALT and phospholipidosis (vacuolation) of lymphoid tissue occurred.
可用產品
劑型
- Chewable tablets
- Topical suspension (human)
- 90 mg chewable tablet
- 140 mg chewable tablet
- 270 mg chewable tablet
- 425 mg chewable tablet
- 665 mg chewable tablet
- 1040 mg chewable tablet
- 1620 mg chewable tablet
獸醫用
- Spinosad Chewable Tablets: 140 mg, 270 mg, 560 mg, 810 mg, 1620 mg (Comfortis)
- Comfortis chewable tablets (90 mg, 140 mg, 270 mg, 425 mg, 665 mg, 1040 mg, 1620 mg)
- Trifexis chewable tablets (spinosad + milbemycin oxime)
人用標示
- Spinosad 0.9% topical suspension in 120 mL (Natroba)
各地核准狀態
POM-V
POM-V
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Chewable tablets should be stored at 20-25°C (68-77°F), excursions permitted between 15-30°C (59-86°F).
飼主須知
給藥指南
- 隨餐餵食： 必須與食物一起服用，藥物才能被狗狗的身體充分吸收。
- 嘔吐處理： 如果狗狗在服藥後一小時內嘔吐，您應該再給予一次完整劑量以確保防護效果。
- 忘記服藥： 如果忘記給藥，請在想起來時盡快隨餐補餵，然後從該日期起恢復每月一次的給藥計畫。
重要提示： 這些咀嚼錠雖然是牛肉口味，但實際上含有豬肉蛋白和水解大豆。如果您的狗狗對豬肉或大豆有已知的食物過敏，請務必告知您的獸醫師。
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