白消安
**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。
作用機制: 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.
各物種劑量
- Adjunctive therapy of chronic granulocytic leukemias or polycythemia vera · 2-4 mg/m2 · PO · once daily · NOT mg/kg. Rarely used in veterinary medicine.
- Adjunctive therapy of chronic granulocytic leukemias or polycythemia vera · 2-4 mg/m2 · PO · once daily · NOT mg/kg. Rarely used in veterinary medicine.
劑量為合格獸醫專業人員的臨床參考。請務必對照最新藥品仿單及個別病患確認。
給藥途徑
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
藥物相互作用
- 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
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.
VetSheet 藥物參考供持牌獸醫專業人員作臨床決策輔助之用,不能取代專業判斷或廠方最新藥品說明書。