VetSheet

白消安

Busulfan

1,4-butanediol dimethanesulfonate

抗腫瘤藥 - 烷化劑POIV狗貓

別名: Myleran · Busulfex · Busulivex · Mielucin · Misulban · bussulfam · busulfanum · busulphan · CB-2041 · GT-41 · myelosan · NSC-750 · WR-19508

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

2-4 mg/m2PO· once daily

這是依體表面積（mg/m²）計算的劑量；給藥前須先將體重換算為體表面積。

劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。

各物種劑量

🌎 NA — North America🌍 EU — Europe

狗

適應症劑量途徑頻次療程地區
Adjunctive therapy of chronic granulocytic leukemias or polycythemia vera2-4 mg/m2POonce daily—🌎 NA
  • Adjunctive therapy of chronic granulocytic leukemias or polycythemia vera: NOT mg/kg. Rarely used in veterinary medicine.

貓

適應症劑量途徑頻次療程地區
Adjunctive therapy of chronic granulocytic leukemias or polycythemia vera2-4 mg/m2POonce daily—🌎 NA
  • Adjunctive therapy of chronic granulocytic leukemias or polycythemia vera: NOT mg/kg. Rarely used in veterinary medicine.

劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。

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概覽

​白消安 (Busulfan)​ 是一種強效的​雙功能烷化抗腫瘤藥物​，在獸醫學中主要用於小動物的​慢性粒細胞白血病 (CML)​ 和​真性紅細胞增多症 (Polycythemia vera)​ 的輔助治療。

  • ​臨床要點​：由於新型標靶療法（如用於真性紅細胞增多症的羥基脲）的出現，它在常規獸醫臨床中已不常用，但對於特定的骨髓增生性疾病仍是一個可行的選擇。
  • 它具有引起​嚴重骨髓抑制​的顯著風險，需要進行嚴格的血液學監測。
  • 治療可能會因快速的腫瘤溶解和細胞破壞而升高血清尿酸水平，有時需要同時使用別嘌醇 (Allopurinol) 治療以預防尿酸性腎病。

作用機轉

Busulfan is a cell cycle-phase nonspecific alkylating agent.

  • Mechanism: It undergoes intracellular hydrolysis to release methanesulfonate groups → forms reactive carbonium ions → alkylates DNA by cross-linking guanine bases on DNA strands.
  • Pathway: DNA cross-linking → inhibition of DNA replication and RNA transcription → apoptosis (programmed cell death).
  • Target: It exhibits highly selective toxicity toward cells of the granulocytic series and myeloid precursors in the bone marrow, making it particularly effective against myeloproliferative diseases.

安全性與警告

禁忌症

  • Patients with known hypersensitivity to busulfan
  • Patients who have shown resistance to the drug in the past
  • Pregnancy (FDA Category D), unless potential benefits outweigh the risks
  • Nursing dams

不良反應

  • Myelosuppression (anemia, leukopenia, thrombocytopenia)
  • Pancytopenia (can take months to years for recovery)
  • Bronchopulmonary dysplasia with pulmonary fibrosis (uncommon, chronic use)
  • Uric acid nephropathy
  • Stomatitis

注意事項

Warning: Only veterinarians with the experience and resources to monitor the toxicity of this agent should administer this drug.

  • Bone Marrow Depression: The risk versus benefits of therapy must be carefully considered in patients with preexisting bone marrow depression or concurrent infections.
  • Radiation Therapy: Additive bone marrow depression may occur in patients undergoing concomitant radiation therapy.
  • Teratogenicity: Mutagenic in mice and may potentially cause a variety of fetal abnormalities. Avoid during pregnancy unless absolutely necessary.

藥物交互作用

Acetaminophen

Use within 72 hours prior to busulfan can reduce busulfan clearance by reducing glutathione concentrations in tissues and blood.

Cyclophosphamide

Can potentially reduce clearance of busulfan, probably by competing for available glutathione.

Itraconazole

Potential decreased busulfan clearance.

Myelosuppressant agents

Concurrent use with other bone marrow depressant medications may result in additive myelosuppression.

Phenytoin

Possible increased clearance of busulfan.

Thioguanine

Used concomitantly with busulfan may result in hepatotoxicity.

監測

  • CBC (Complete Blood Count)
  • Serum uric acid
  • Clinical efficacy

藥物動力學

吸收

Well absorbed after oral administration.

分佈

Distribution characteristics are not well described in animals, but in humans, drug concentrations in the CSF are nearly equal to those found in plasma. Unknown if it enters maternal milk.

代謝

Rapidly, hepatically metabolized to at least 12 different metabolites.

排除

Slowly excreted into the urine.

過量

There is limited experience with busulfan overdoses. The LD50 in mice is 120 mg/kg.

  • Chronic vs Acute: Chronic overdosage is more likely to cause serious bone marrow suppression than is an acute overdose.
  • Treatment: Any overdose should be treated seriously with standard gut emptying protocols used when appropriate and supportive therapy initiated when required.
  • Antidote: There is no known specific antidote for busulfan intoxication.

可用產品

劑型

  • Oral tablets
  • Injection solution

人用標示

  • Busulfan Oral Tablets: 2 mg; Myleran (GlaxoSmithKline); (Rx)
  • Busulfan Injection Solution: 6 mg/mL in 10 mL single-use amps with syringe filters; Busulfex (Otsuka America); (Rx)

各地核准狀態

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

儲存與穩定性

Busulfan tablets should be stored in well-closed containers at room temperature.

飼主須知

​重要安全警告​：白消安是一種強效化療藥物。請極度小心處理，以保護您自己、您的家人和環境。

  • ​藥物處理​：處理藥物時請務必戴上一次性手套。處理後請徹底洗手。請勿壓碎、剝開或切半藥片。
  • ​排泄物管理​：在給藥後至少 48-72 小時內，請將寵物的排泄物（尿液、糞便、嘔吐物）視為危險物質。清理時請戴上手套，並將廢棄物密封於塑膠袋中丟棄。
  • ​不良反應徵兆​：如果您發現以下毒性徵兆，請​立即​聯繫您的獸醫：
    • 異常出血或不明原因的瘀傷（血小板低下的徵兆）
    • 嗜睡、嚴重抑鬱或虛弱（貧血的徵兆）
    • 發燒或感染跡象（白血球低下的徵兆）
    • 呼吸急促或呼吸困難
    • 排尿習慣改變

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