アンチモン酸メグルミン
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
VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
動物種別用量
🌎 NA — North America🌍 EU — Europe
犬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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).
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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.
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
概要
アンチモン酸メグルミンは、犬のリーシュマニア症の治療に使用される5価アンチモン化合物です（アロプリノールと併用または単独使用）。
- 臨床上のポイント: 病原体を完全に排除することは難しく、治療は長期にわたり高額になる可能性があります。
- 耐性: 治療に対する耐性が報告されており、アロプリノールの併用が推奨されます。
- 安全性: 心不全、肝不全、または腎不全の患者には相対的禁忌であり、極めて慎重な投与が必要です。
作用機序
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・警告
禁忌
- Previous hypersensitivity to meglumine antimoniate
- Severe renal, hepatic, or cardiac failure (relative contraindication; weigh risks vs. benefits)
- Severe renal impairment
- Hepatic failure
- Cardiac disease
有害事象
- 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.
医薬品相互作用
Meglumine antimoniate may prolong QT interval further with increased risk for arrhythmias
Increased risk of nephrotoxicity
Increased risk of nephrotoxicity
監視
- 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
薬物動態
半減期
吸収
Systemic bioavailability is approximately 92% after subcutaneous or intramuscular injections in dogs.
分布
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.
消失
Rapidly excreted primarily via the kidneys; within 9 hours of dosing, 80% of the antimony is excreted in the urine.
過剰投与
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.
製品
製剤
- Injection solution (1.5 g meglumine antimoniate / 5 mL, equivalent to 425 mg pentavalent antimony)
- Injectable: 300 mg/ml solution
動物用医薬品
- None approved in the USA. May be available via the CDC.
- Glucantime 300 mg/ml solution for injection
ヒト用医薬品
- 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
規制ステータス
Approved in several EU countries (e.g., France, Spain, Italy) for canine leishmaniosis.
Available as POM-V.
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Unless otherwise specified by the manufacturer, commercially available ampules should be stored below 40°C, preferably between 15°-30°C; protect from freezing.
飼主向け情報
- 長期かつ高額な治療: 治療は長期間に及び、費用が高額になる可能性があることをご理解ください。
- 完全な治癒は困難: この薬は症状をコントロールするためのものであり、体内から寄生虫を「完全に排除（完治）」することは困難です。
- 副作用の観察: 注射部位の反応（腫れなど）に注意してください。食欲不振、嘔吐、または極度の疲労が見られた場合は、すぐに獣医師にご連絡ください。
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