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葡萄糖酸銻鈉

Sodium Stibogluconate

Sodium Antimony Gluconate

抗利什曼原蟲藥IVSCIM狗

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

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

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

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。

各物種劑量

🌎 NA — North America🌍 EU — Europe

狗

適應症劑量途徑頻次療程地區
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.

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概覽

葡萄糖酸銻鈉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）。在美國無市售，需透過疾病管制與預防中心（CDC）取得。此藥物具有潛在的嚴重副作用，需謹慎使用。

作用機制

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.

安全性與警告

禁忌症

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

不良反應

  • 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.

藥物相互作用

Amphotericin BMajor

Increased risk of nephrotoxicity

AllopurinolMinor

Synergistic antileishmanial effect (often used together clinically)

監測

  • 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)

藥物動力學

半衰期

狗0.6-1.5 hours

吸收

Well absorbed following intramuscular or subcutaneous injection.

分佈

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.

排除

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.

過量

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.

可用產品

劑型

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

人用標示

  • 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

各地核准狀態

European Union✓ 已核准處方藥EMA
🐕 Dogs

POM (Prescription Only Medicine)

United Kingdom✓ 已核准處方藥VMD
🐕 Dogs

POM (Prescription Only Medicine)

暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

儲存與穩定性

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.

飼主須知

寵物主人應了解此疾病（利什曼原蟲症）潛在的公共衛生影響（視所在國家而定）。即使接受治療，預後仍持保留態度。請務必了解治療的潛在風險及相關的高昂費用。

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