米替福新
Miltefosine
Hexadecylphosphocholine
別名: Milteforan · Impavido · Miltex · D-18506 · HDPC · hexadecilfosfocolina · hexadecylphosphocholine · miltefosiini · miltefosina · miltéfosine · miltefosinum
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 |
|---|---|---|---|---|---|
| Canine leishmaniasis | 2 mg/kg PO | PO | once a day | 28 days | 🌎 NA |
| Canine leishmaniasis (alternative treatment to meglumine antimoniate) | 2 mg/kg PO | PO | once daily | 28 days | 🌎 NA |
| Leishmaniosis | 2 mg/kg | PO | q24h | 28 days | 🌍 EU |
- Canine leishmaniasis: Poured onto food, with a full or partial meal.
- Canine leishmaniasis (alternative treatment to meglumine antimoniate): Use with allopurinol (10 mg/kg PO q12h, orally for at least 6 months).
- Leishmaniosis: It is particularly important that the full course is completed and given with allopurinol. Pour on feed to reduce digestive side effects.
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
米替福新 (Miltefosine) 是一種口服抗利什曼原蟲藥物，主要在獸醫學中用於治療犬利什曼原蟲症 (CanL)，這是一種由細胞內寄生蟲（嬰兒利什曼原蟲）引起的嚴重全身性疾病。
- 最初是作為抗腫瘤（抗癌）藥物開發的。
- 臨床要點：雖然它能顯著降低寄生蟲量並改善臨床症狀，但極少能達到完全的寄生蟲學治癒。使疾病進入緩解期是主要的治療目標。
- 與別嘌醇 (Allopurinol) 併用時，療效會顯著提升。
- 在人類醫學中屬於孤兒藥，在美國並無商業化的獸醫標籤產品，但在流行地區（如歐洲）被廣泛使用。
作用機轉
Miltefosine is an alkylphosphocholine (phospholipid derivative). Its exact mechanism against Leishmania is multifactorial:
- Inhibits macrophage penetration: Interacts with glycosomes and glycosylphosphatidyl-inositol (GPI) anchors that are essential for the parasite's intracellular survival.
- Enzyme inhibition: Inhibits phospholipase → disrupts parasite membrane signal transduction and lipid metabolism.
- Apoptosis induction: Triggers apoptosis-like cell death in the parasite by disrupting lipid rafts in the cell membrane.
- Additionally, miltefosine exhibits mild antineoplastic, immunomodulatory, and antiviral properties.
安全性與警告
禁忌症
- Hypersensitivity to miltefosine
- Pregnant animals
- Lactating animals
- Breeding animals
- Pregnancy
- Lactation
不良反應
- Vomiting (most common)
- Diarrhea
- Inappetence
- Potential nephrotoxicity
- Potential hepatotoxicity
- Vomiting (moderate, transient)
- Diarrhoea (moderate, transient)
注意事項
Resistance Warning: Do not underdose, as subtherapeutic levels significantly increase the risk of developing drug-resistant Leishmania strains.
- Use with extreme caution in patients with severe hepatic dysfunction.
- While leishmaniasis itself causes kidney and liver damage, miltefosine has a lower risk of severe renal tubular damage compared to meglumine antimoniate, though monitoring is still required.
監測
- Baseline and periodic renal function
- Hepatic enzymes
- Adverse effects (especially vomiting)
- Patient weight
- Clinical signs of leishmaniosis
- Gastrointestinal signs (vomiting, diarrhoea)
藥物動力學
半衰期
吸收
High oral bioavailability of 94% in dogs. Peak plasma levels occur around 5 hours post-dose.
分佈
Widely distributed throughout major organs, including the brain. Intravascularly, it is approximately equally distributed in the plasma and erythrocytes.
代謝
Not extensively metabolized; primarily acts unchanged.
排除
Mainly eliminated via the feces, with approximately 10% of a dose eliminated unchanged. Renal elimination appears negligible.
過量
Overdoses are likely to cause severe gastrointestinal signs (vomiting, diarrhea, anorexia). In cases of massive overdose, there is a potential for hepatic, renal, and retinal toxicity.
There is no specific antidote for miltefosine overdose; treatment should consist of prompt gastrointestinal decontamination (if recent and patient is asymptomatic) followed by aggressive supportive care (IV fluids, antiemetics, hepatoprotectants).
可用產品
劑型
- Capsules
- Oral solution: 20 mg/ml
獸醫用
- Miltefosine Oral Solution: 20 mg/mL in 30 mL, 50 mL & 90 mL vials (Milteforan)
- Milteforan 20 mg/ml oral solution
人用標示
- Miltefosine capsules: 10 mg, 50 mg (Impavido)
各地核准狀態
Authorized for veterinary use in specific countries such as Spain and Germany.
A Special Treatment Authorization (STA) is required to obtain this product in the UK.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
This veterinary medicinal product does not require any special storage conditions. Avoid freezing the solution.
飼主須知
重要安全警告：已知本藥物會導致胎兒畸形。孕婦或備孕婦女絕對不可接觸本藥物。
- 給藥方式：請務必將本藥物倒在食物上（伴隨全餐或部分餐食）給予。這能顯著降低胃部不適和嘔吐的機率。
- 處理注意事項：給予藥液時請戴上拋棄式手套，因為它可能引起皮膚反應。請勿搖晃藥瓶（以避免產生泡沫）。
- 寵物互動：服藥後，請勿讓接受治療的犬隻立即舔舐人類。
- 副作用：嘔吐是非常常見的副作用。如果您的狗狗出現嚴重嘔吐、食慾不振或腹瀉，請聯繫您的獸醫師尋求建議（他們可能會開立止吐藥物）。
VetSheet 藥物參考供合格獸醫專業人員作臨床決策輔助之用，不能取代專業判斷或廠商最新仿單。