アンチモン酸メグルミン
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.
動物種別の用量
- Leishmaniosis (off-label) · 50 mg/kg · SC · q24h · 3-4 weeks · Use with extreme caution; cats may be more sensitive to toxicity.
- 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 · Used in combination with allopurinol.
- 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 · Longer duration (4-6 weeks) yields better results.
- Leishmaniasis · 100 mg/kg/day SC until resolution; with allopurinol at 20 mg/kg PO q12h for 9 months. · SC · q24h · Until resolution · Used in combination with allopurinol.
- Leishmaniosis · 75-100 mg/kg · SC · q24h (or divided q12h) · 3-4 weeks · Often used in combination with allopurinol (10 mg/kg PO q12h for 6-12 months).
用量は獣医療従事者向けの臨床リファレンスです。必ず最新の添付文書と個々の患者で確認してください。
投与経路
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
- Vomiting
- Hepatotoxicity (rare)
- Myalgia/arthralgia
薬物相互作用
- Agents that can prolong QT interval (e.g., tricyclic antidepressants, disopyramide, quinidine, procainamide) · Meglumine antimoniate may prolong QT interval further with increased risk for arrhythmias
- Aminoglycosides · Increased risk of nephrotoxicity · major
- NSAIDs · Increased risk of nephrotoxicity · moderate
モニタリング
- 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
過量投与
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.
VetSheet の薬剤リファレンスは、獣医療従事者向けの臨床意思決定支援を目的としており、専門的判断やメーカーの最新添付文書に代わるものではありません。