銻酸甲胺
Meglumine Antimoniate
1-Deoxy-1-methylamino-D-glucitol antimoniate
別名: Glucantime · meglumine antimonate · N-methylglucamine antimoniate · RP-2168 · antimony meglumine · Protostib · Antimoniate de meglumine
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
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各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Leishmaniasis (First line treatment) | 75-100 mg/kg SC once daily for 4-8 weeks, with allopurinol (10 mg/kg PO twice daily for at least 6-12 months. | SC | q24h | 4-8 weeks | 🌎 NA |
| Leishmaniasis | 100 mg/kg SC daily for 3-4 weeks; better results are obtained with longer durations (4-6 weeks) of treatment. Protocol with allopurinol may reduce relapse rates: meglumine antimoniate as above with allopurinol at 20-40 mg/kg PO daily for a minimum of 3 weeks. Followed with long-term treatment with allopurinol (alone) at 20-40 mg/kg PO daily or intermittently (one week treatment per month). | SC | q24h | 3-6 weeks | 🌎 NA |
| Leishmaniasis | 100 mg/kg/day SC until resolution; with allopurinol at 20 mg/kg PO q12h for 9 months. | SC | q24h | Until resolution | 🌎 NA |
| Leishmaniosis | 75-100 mg/kg | SC | q24h (or divided q12h) | 3-4 weeks | 🌍 EU |
- Leishmaniasis (First line treatment): Used in combination with allopurinol.
- Leishmaniasis: Longer duration (4-6 weeks) yields better results.
- Leishmaniasis: Used in combination with allopurinol.
- Leishmaniosis: Often used in combination with allopurinol (10 mg/kg PO q12h for 6-12 months).
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Leishmaniosis (off-label) | 50 mg/kg | SC | q24h | 3-4 weeks | 🌍 EU |
- Leishmaniosis (off-label): Use with extreme caution; cats may be more sensitive to toxicity.
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
銻酸甲胺是一種五價銻化合物，主要用於治療犬隻的利什曼原蟲症 (Leishmaniasis)（可單獨使用或與別嘌呤醇 allopurinol 併用）。
- 臨床重點：本藥無法完全根除病原體，治療期長且費用高昂。
- 抗藥性：已有多起抗藥性報告，併用別嘌呤醇可降低抗藥性風險。
- 安全性：對心臟、肝臟或腎臟功能不全的病患具相對禁忌，需極度謹慎使用。
作用機制
Meglumine antimoniate selectively inhibits leishmanial enzymes required for glycolytic and fatty acid oxidation → disruption of parasite bioenergetics → decreased ATP production → death of the organism.
- Synergy: When used with allopurinol (a leishmaniostatic agent that disrupts RNA synthesis), the combination provides synergistic efficacy and helps prevent the emergence of resistant strains.
- Mechanistic Pearl: While the exact mechanism remains partially elucidated, it is widely believed that pentavalent antimony (SbV) acts as a prodrug and is reduced to the more toxic and active trivalent antimony (SbIII) within the acidic environment of the macrophage phagolysosome, where the amastigotes reside.
安全性與警告
禁忌症
- Previous hypersensitivity to meglumine antimoniate
- Severe renal, hepatic, or cardiac failure (relative contraindication; weigh risks vs. benefits)
- Severe renal impairment
- Hepatic failure
- Cardiac disease
不良反應
- Injection site reactions (cutaneous abscesses, cellulitis, pain)
- Lethargy
- Gastrointestinal effects (inappetence, vomiting)
- Transient increases in liver enzymes
- Nephrotoxicity (tubular damage, proximal tubule cell vacuolization, coagulative necrosis)
- Pain and swelling at the injection site
- Nephrotoxicity (proteinuria, elevated BUN/creatinine)
- Anorexia
- Hepatotoxicity (rare)
- Myalgia/arthralgia
注意事項
Extreme caution is advised in patients with pre-existing renal, hepatic, or cardiac insufficiency.
- Renal Impairment: Decreased renal function can lead to significant drug accumulation and an increased risk of severe toxicity. In dogs with severe renal failure (IRIS stages III-IV), correction of fluid and acid-base imbalances prior to treatment with allopurinol alone is recommended before considering antimonials.
- Hypersensitivity: Hypersensitivity reactions have been reported in humans; avoid in patients with known allergies to the drug.
- Pregnancy: Teratogenic effects (fetal resorptions, bone abnormalities) have been noted in animal models. Weigh risks versus benefits carefully.
藥物相互作用
Meglumine antimoniate may prolong QT interval further with increased risk for arrhythmias
Increased risk of nephrotoxicity
Increased risk of nephrotoxicity
監測
- Efficacy (PCR preferred)
- CBC (baseline and periodic)
- Liver enzymes (baseline and periodic)
- Renal function tests (serum creatinine, BUN) (baseline and periodic)
- Serum lipase and amylase (baseline and periodic)
- Urinalysis (baseline and periodic)
- Urinalysis (specifically for proteinuria/UPC ratio)
- BUN and Creatinine
- Liver enzymes (ALT, AST, ALP)
- Complete Blood Count (CBC)
- Clinical signs of injection site reactions
藥物動力學
半衰期
吸收
Systemic bioavailability is approximately 92% after subcutaneous or intramuscular injections in dogs.
分佈
Highest tissue concentrations are found in the liver, spleen, and skin.
代謝
Pentavalent antimony is believed to undergo in vivo reduction to trivalent antimony, which is the more active leishmanicidal form.
排除
Rapidly excreted primarily via the kidneys; within 9 hours of dosing, 80% of the antimony is excreted in the urine.
過量
No specific overdose information is available. Depending on the dosage, a single massive overdose could potentially cause renal, hepatic, pancreatic, and hematologic toxicity.
Clinically, gastrointestinal effects (severe vomiting) and profound lethargy would be the most likely immediate outcomes.
Management: Observe the patient closely, provide supportive care (IV fluids to protect renal function), and contact an animal poison control center for further guidance.
可用產品
劑型
- Injection solution (1.5 g meglumine antimoniate / 5 mL, equivalent to 425 mg pentavalent antimony)
- Injectable: 300 mg/ml solution
獸醫用
- None approved in the USA. May be available via the CDC.
- Glucantime 300 mg/ml solution for injection
人用標示
- Glucantime® / Glucantim® solution containing 1.5 grams of meglumine antimoniate (425 mg pentavalent antimony) per 5 mL (Available in Europe, Brazil, Venezuela; None in the USA)
- Glucantime 1.5 g/5 ml solution for injection
各地核准狀態
Approved in several EU countries (e.g., France, Spain, Italy) for canine leishmaniosis.
Available as POM-V.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Unless otherwise specified by the manufacturer, commercially available ampules should be stored below 40°C, preferably between 15°-30°C; protect from freezing.
飼主須知
- 治療期長且費用高：請理解本藥物的療程通常相當漫長，且整體治療費用可能十分高昂。
- 無法完全治癒：本藥物主要用於控制病情，極難達到「完全治癒」（徹底根除體內原蟲）的效果，復發是有可能的。
- 副作用觀察：注射部位可能會出現腫脹或硬塊。若發現寵物出現食慾不振、嘔吐或極度疲倦，請立即聯繫獸醫師。
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