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スチボグルコン酸ナトリウム

Sodium Stibogluconate

Sodium Antimony Gluconate

抗リーシュマニア薬IVSCIM犬

別名: Pentostam · Sodium antimony gluconate · stiboglucat-natrium · natriumstibogluconat-9-wasser · solusurmin · sodio stibogluconato · natrii stibogluconas · Stibogluconate sodium

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

30-50 mg/kg IV or SC dailyIV/SC· q24h· 3-4 weeks
— 🐕

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
Treatment of cutaneous leishmaniasis30-50 mg/kg IV or SC dailyIV/SCq24h3-4 weeks🌎 NA
Treatment of visceral leishmaniasis30-50 mg/kg IV or SC q24hIV/SCq24hone month🌎 NA
  • Treatment of visceral leishmaniasis: Has severe side effects and may not be obtainable in the USA; allopurinol alone is usually used initially.

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。

診察中ですか？VetSheet の AI が薬剤・用量・投与期間を構造化された診察記録に直接記入します。VetSheet の仕組みを見る

概要

スチボグルコン酸ナトリウムは、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。米国では市販されておらず、CDCを通じて入手可能です。重篤な副作用のリスクがあるため、慎重な投与が求められます。

作用機序

The exact mechanism of action of sodium stibogluconate remains incompletely elucidated.

  • ​Prodrug Hypothesis:​ It is widely hypothesized to act as a prodrug, where the pentavalent antimony (SbV) is reduced to the more toxic trivalent antimony (SbIII) within the host macrophage or the parasite itself.
  • ​Bioenergetic Disruption:​ It is believed to interfere with the parasite's bioenergetics by reducing ATP and GTP synthesis in susceptible Leishmania amastigotes, ultimately leading to parasite death.

安全性・警告

禁忌

  • Pre-existing cardiac arrhythmias
  • Significantly impaired renal function
  • Previous serious adverse reaction to a dose of stibogluconate
  • Severe renal impairment
  • Severe hepatic impairment

有害事象

  • Increased AST levels
  • Pain on injection
  • Musculoskeletal pain
  • Hemolytic anemia
  • Leukopenia
  • Vomiting
  • Diarrhea
  • Pancreatitis
  • Myocardial injury and arrhythmias
  • Renal toxicity
  • Shock
  • Sudden death
  • Thrombophlebitis (with IV administration)
  • Nephrotoxicity
  • Hepatotoxicity
  • Injection site pain
  • Lethargy
  • Anorexia
  • Myalgia/Arthralgia
  • Cardiac arrhythmias (rare)

注意事項

Contraindicated in patients with pre-existing cardiac arrhythmias or significantly impaired renal function.

  • ​Duration Warning:​ The incidence of adverse effects reportedly increases significantly if the drug is administered for longer than 2 months.
  • ​Pregnancy:​ Has not been shown to cause fetal harm, but should be withheld during pregnancy unless the benefits clearly outweigh the risks.
  • ​Nursing:​ Controversial; the manufacturer states it should not be used in nursing mothers, though some human pediatric guidelines consider it compatible.

医薬品相互作用

Amphotericin BMajor

Increased risk of nephrotoxicity

AllopurinolMinor

Synergistic antileishmanial effect (often used together clinically)

監視

  • CBC
  • Liver enzymes (especially AST)
  • Renal function tests
  • ECG (for myocardial injury/arrhythmias)
  • Bone marrow cultures for Leishmania
  • Clinical efficacy
  • Renal function (BUN, Creatinine, SDMA, Urinalysis)
  • Hepatic enzymes (ALT, AST, ALP)
  • Pancreatic enzymes (cPLI, Lipase)
  • ECG (for arrhythmias)

薬物動態

半減期

犬0.6-1.5 hours

吸収

Well absorbed following intramuscular or subcutaneous injection.

分布

In dogs, steady-state volume of distribution is 0.25 L/kg.

代謝

Pentavalent antimony is partially reduced to the more toxic and active trivalent antimony in vivo.

消失

The main route of excretion is via the kidneys; glomerular filtration rate determines the excretion rate. Clearance in dogs is 1.71 L/kg/hr.

過剰投与

In the unlikely event of a parenterally administered overdose, it is suggested to immediately contact an animal poison control center.

  • ​Chelation Therapy:​ Potentially, antimony toxicity can be managed by chelating agents such as ​dimercaptosuccinic acid (DMSA)​ or d-penicillamine to enhance excretion.

製品

製剤

  • Injection: 100 mg (of antimony)/mL
  • Injectable: 100 mg/ml solution

ヒト用医薬品

  • Sodium Stibogluconate (sodium antimony gluconate) 100 mg (of antimony)/mL for injection in 6 mL and 100 mL (Pentostam)
  • Pentostam 100 mg/ml solution for injection

規制ステータス

European Union✓ 承認済み処方箋医薬品EMA
🐕 Dogs

POM (Prescription Only Medicine)

United Kingdom✓ 承認済み処方箋医薬品VMD
🐕 Dogs

POM (Prescription Only Medicine)

規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

保管・安定性

Store at temperatures below 25°C (76°F) and protect from freezing and exposure to light. After removing the first dose, the vial should not be used after one month.

飼主向け情報

飼い主は、この病気（リーシュマニア症）の公衆衛生上の影響（国によって異なる）を理解する必要があります。治療を行っても予後は要注意であり、治療に伴うリスクと費用についても考慮する必要があります。

VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。