메글루민 안티모니에이트
Meglumine Antimoniate
1-Deoxy-1-methylamino-D-glucitol antimoniate
다른 이름: Glucantime · meglumine antimonate · N-methylglucamine antimoniate · RP-2168 · antimony meglumine · Protostib · Antimoniate de meglumine
VetSheet 수의사 팀 검수업데이트 2026년 4월 5일근거 기반 수의학 참고자료
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
동물 종별 용량
🌎 NA — North America🌍 EU — Europe
개
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| 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).
고양이
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| 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.
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
개요
메글루민 안티모니에이트는 개에서 리슈만편모충증(Leishmaniasis) 치료에 사용되는 5가 안티몬 화합물입니다(알로푸리놀과 병용 또는 단독 사용).
- 임상 요점: 병원체를 완전히 제거하기는 어려우며, 치료 기간이 길고 비용이 많이 들 수 있습니다.
- 내성: 치료에 대한 내성이 보고되었으며, 알로푸리놀과의 병용이 내성 발생 위험을 줄일 수 있습니다.
- 안전성: 심장, 간 또는 신장 기능 부전 환자에게는 상대적 금기이며 극도의 주의가 필요합니다.
작용 기전
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.
안전성·주의사항
금기사항
- Previous hypersensitivity to meglumine antimoniate
- Severe renal, hepatic, or cardiac failure (relative contraindication; weigh risks vs. benefits)
- Severe renal impairment
- Hepatic failure
- Cardiac disease
부작용
- 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
주의
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.
약물 상호작용
Meglumine antimoniate may prolong QT interval further with increased risk for arrhythmias
Increased risk of nephrotoxicity
Increased risk of nephrotoxicity
모니터링
- 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
약동학
반감기
흡수
Systemic bioavailability is approximately 92% after subcutaneous or intramuscular injections in dogs.
분포
Highest tissue concentrations are found in the liver, spleen, and skin.
대사
Pentavalent antimony is believed to undergo in vivo reduction to trivalent antimony, which is the more active leishmanicidal form.
배설
Rapidly excreted primarily via the kidneys; within 9 hours of dosing, 80% of the antimony is excreted in the urine.
과다투여
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.
제품
제형
- Injection solution (1.5 g meglumine antimoniate / 5 mL, equivalent to 425 mg pentavalent antimony)
- Injectable: 300 mg/ml solution
동물용의약품
- None approved in the USA. May be available via the CDC.
- Glucantime 300 mg/ml solution for injection
인용의약품
- 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
규제 현황
Approved in several EU countries (e.g., France, Spain, Italy) for canine leishmaniosis.
Available as POM-V.
규제 데이터 없음: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
보관·안정성
Unless otherwise specified by the manufacturer, commercially available ampules should be stored below 40°C, preferably between 15°-30°C; protect from freezing.
보호자 정보
- 장기 및 고비용 치료: 이 약물을 이용한 치료는 장기간 지속될 수 있으며 비용이 많이 들 수 있음을 이해해야 합니다.
- 완치 어려움: 이 약물은 증상 조절을 목적으로 하며, 체내에서 기생충을 '완전히 제거(완치)'하는 것은 거의 불가능합니다.
- 부작용 관찰: 주사 부위의 반응(부종 등)을 주의 깊게 살펴보세요. 식욕 부진, 구토 또는 극심한 무기력증이 나타나면 즉시 수의사에게 연락하십시오.
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