博來黴素
Bleomycin
Bleomycin sulfate
別名: Blenoxane · Blenamax · Bleocin · Bileco · Blanoxan · bleomycin sulphate · bleomycini sulfas · Bleo-S · Bleo-cell · Bleolem · Blio · Blocamicina · Bonar · Oil Bleo · Tecnomicina
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
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 |
|---|---|---|---|---|---|
| Antineoplastic therapy (General guide) | 10 Units mg/m2 (NOT mg/kg) or 0.3-0.5 mg/kg | Parenteral | Varies (e.g., once daily for a few days then once weekly, or once weekly at the start) | Do not exceed total maximum dosage of 125-200 mg/m2 | 🌎 NA |
- Antineoplastic therapy (General guide): 1 Unit = 1 mg. Consultation with a veterinary oncologist is strongly recommended.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Antineoplastic therapy (General guide) | 10 Units mg/m2 (NOT mg/kg) or 0.3-0.5 mg/kg | Parenteral | Varies (e.g., once daily for a few days then once weekly, or once weekly at the start) | Do not exceed total maximum dosage of 125-200 mg/m2 | 🌎 NA |
- Antineoplastic therapy (General guide): 1 Unit = 1 mg. Consultation with a veterinary oncologist is strongly recommended.
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。
概覽
博來黴素是一種源自Streptomyces verticillus的糖肽類抗腫瘤抗生素。
主要臨床用途：
- 用於犬貓淋巴瘤、鱗狀細胞癌 (SCC)、畸胎瘤和非功能性甲狀腺腫瘤的輔助治療。
- 電化學療法 (ECT)： 當與病灶內電穿孔技術結合使用時，博來黴素非常有效，能顯著增加局部腫瘤（如貓鼻鏡鱗狀細胞癌、犬肥大細胞瘤）的細胞內藥物濃度。
毒性特徵： 與許多傳統化療藥物不同，博來黴素通常不會對骨髓造成嚴重抑制。然而，它具有引起肺纖維化和皮膚毒性的顯著風險。這種獨特的毒性特徵是因為肺部和皮膚缺乏能使該藥物失去活性的博來黴素水解酶 (bleomycin hydrolase)。
作用機轉
Bleomycin acts primarily by inducing single- and double-strand DNA breaks.
- Mechanism: The drug possesses a DNA-binding domain and an iron-binding domain. It binds to DNA and chelates intracellular Fe²⁺ (ferrous iron).
- Oxidative Cleavage: The Bleomycin-Fe²⁺ complex reacts with oxygen to generate highly reactive oxygen species (ROS), such as superoxide and hydroxyl radicals → oxidative cleavage of the DNA phosphodiester backbone.
- Cell Cycle: It is considered cell-cycle phase-specific, primarily arresting cells in the G2 and M phases.
- Resistance: Mediated by decreased cellular uptake, increased DNA repair mechanisms, or increased cellular expression of bleomycin hydrolase (the enzyme responsible for its degradation).
安全性與警告
禁忌症
- Prior hypersensitivity reactions to the drug
- Preexisting pulmonary disease
- Adverse pulmonary effects from prior therapy
- Pregnancy (unless owners accept the associated teratogenic risks)
不良反應
- Fever
- Anorexia
- Vomiting
- Allergic reactions (including anaphylaxis)
- Alopecia
- Skin rashes
- Stomatitis
- Pneumonitis
- Pulmonary fibrosis (potentially fatal)
- Thrombocytopenia (mild)
- Leukopenia (mild)
- Decreased hemoglobin
- Renal toxicity
- Hepatotoxicity
注意事項
Bleomycin is a toxic drug with a low therapeutic index; it should only be used by personnel equipped to actively monitor patients and handle complications. Use very cautiously in patients with significant renal impairment (dosage reduction may be necessary). It is teratogenic (FDA Category D). To reduce the likelihood of fatal pulmonary toxicity, a total maximum cumulative dosage of 125-200 mg/m2 should not be exceeded.
藥物交互作用
Bleomycin sensitizes lung tissue to oxygen. Use of general anesthetics can cause rapid deterioration of pulmonary function and post-operative pulmonary fibrosis, even at safe inspired oxygen concentrations.
Prior or concomitant use can lead to increased hematologic, mucosal, and pulmonary toxicities.
監測
- Efficacy (tumor response)
- Pulmonary Toxicity: Chest radiographs (baseline and regularly, e.g., q1-2 weeks), lung auscultation (monitor for dyspnea and fine rales)
- Blood chemistry (renal and hepatic function markers)
- Hematologic profiles (CBC)
- Total cumulative dose accumulation (do not exceed 125-200 mg/m2)
藥物動力學
半衰期
吸收
Not appreciably absorbed from the gut; must be administered parenterally.
分佈
Mainly distributed to the lungs, kidneys, skin, lymphatics, and peritoneum.
代謝
Inactivated by the enzyme bleomycin hydrolase, which is abundant in most tissues but notably deficient in the skin and lungs.
排除
In humans, 60-70% of a dose is excreted as active drug in the urine.
過量
No specific information was located in the monograph. Because of the high toxicity and low therapeutic index of the drug, it is critical to determine dosages carefully. Overdosage would likely manifest as severe exacerbations of acute toxicities (anaphylaxis, fever, vomiting) and accelerated onset of delayed toxicities (pulmonary fibrosis, stomatitis).
可用產品
劑型
- Powder for injection
人用標示
- Bleomycin Sulfate Lyophilized Powder for Injection after reconstitution: 15 Units & 30 Units per vial
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
Powder for injection should be kept refrigerated. After reconstituting with sterile saline, water, or dextrose, the resulting solution is stable for 24 hours. Bleomycin is less stable in dextrose solutions than in saline. While reportedly stable in normal saline for at least 2 weeks at room temperature and 4 weeks refrigerated, use within 24 hours is recommended because the solution contains no preservatives.
飼主須知
重要警告： 博來黴素可能導致嚴重且可能不可逆的肺部損傷。
- 呼吸變化： 密切觀察寵物的呼吸狀況。如果發現咳嗽、喘息、呼吸急促或呼吸困難，請立即聯繫您的獸醫。
- 皮膚和口腔潰瘍： 注意是否出現脫毛、皮疹或口腔潰瘍（口炎）。如果寵物口腔敏感，請提供軟食。
- 一般症狀： 給藥後不久可能會出現輕微發燒、食慾不振和嘔吐。
- 麻醉風險： 如果您的寵物將來需要進行手術或麻醉，您必須告知獸醫團隊牠曾接受過博來黴素治療。該藥物會使肺部對氧氣治療變得高度敏感，需要特殊的麻醉方案。
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