多柔比星 / 阿黴素
Doxorubicin
Doxorubicin Hydrochloride
別名: Doxil · Adriamycin RDF · Adriamycin PFS · Rubex · Caelyx · Myocet · cloridrato de doxorrubicina · doxorubicin hydrochloride liposome · doxorubicini hydrochloridum · liposomal doxorubicin hydrochloride · NSC-123127 · Hydroxydaunorubicin
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
這是按體表面積（mg/m²）計算的劑量；給藥前須先把體重換算為體表面積。
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 |
|---|---|---|---|---|---|
| Antineoplastic | 30 mg/m2 IV every 2-3 weeks | IV | every 2-3 weeks | — | 🌎 NA |
| Lymphoma, sarcomas, carcinomas | 30 mg/m2 (Use 1 mg/kg in dogs weighing <10 kg) | IV | q3wk | Maximum total cumulative dose not to exceed 240 mg/m2 | 🌍 EU |
- Antineoplastic: Depending on the protocol used. Maximum cumulative dose = 240 mg/m2.
- Lymphoma, sarcomas, carcinomas: Administer over a minimum of 10 minutes into side port of freely running 0.9% NaCl.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Antineoplastic | 20-30 mg/m2 IV every 2-4 weeks | IV | every 2-4 weeks | — | 🌎 NA |
| Lymphoma, soft tissue sarcomas | 1 mg/kg or 20-25 mg/m2 | IV | q3-5wk | Maximum total cumulative dose not to exceed 240 mg/m2 | 🌍 EU |
- Antineoplastic: Depending on the protocol used. Maximum cumulative dose is usually 240 mg/m2.
- Lymphoma, soft tissue sarcomas: Nephrotoxicity is a major risk in cats, especially at cumulative dosages >100 mg/m2.
雪貂
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Antineoplastic | 30 mg/m2 IV every 3 weeks | IV | every 3 weeks | — | 🌎 NA |
- Antineoplastic: Depending on the protocol used.
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。
概覽
多柔比星 (Doxorubicin) 是一種蒽環類抗生素，也是小動物獸醫腫瘤學中最廣泛使用的抗腫瘤藥物之一。由於其鮮紅的顏色和強烈的副作用，常被俗稱為「小紅莓 (Red Devil)」。它可作為單一藥物或在多藥物聯合化療方案中使用。
- 廣效性：對犬貓的多種惡性腫瘤高度有效，包括淋巴瘤、癌、白血病和肉瘤。
- 來源：最初從 Streptomyces peucetius 中分離出來。
- 臨床要點：雖然具有抗菌特性，但其強烈的細胞毒性使其完全無法作為抗感染藥物使用。它是一種強烈的發泡劑 (vesicant)；必須極度小心確保靜脈通路暢通，以防止嚴重的血管外滲漏損傷。
作用機制
Doxorubicin is a cell-cycle non-specific cytotoxic agent with multiple mechanisms of action:
- Topoisomerase II Inhibition: Intercalates between DNA base pairs and inhibits topoisomerase II → prevents DNA resealing → causes double-strand DNA breaks → triggers apoptosis.
- Macromolecular Synthesis Inhibition: Directly inhibits DNA synthesis, DNA-dependent RNA synthesis, and protein synthesis.
- Free Radical Generation: Undergoes electron reduction to form anthracycline semiquinone free radicals (often iron-mediated) → causes severe oxidative stress and lipid peroxidation.
- Clinical Pearl: The heart is particularly susceptible to doxorubicin-induced oxidative damage because cardiac tissue has inherently low levels of catalase, an enzyme necessary to neutralize hydrogen peroxide. This is the primary mechanism behind its cumulative cardiotoxicity.
安全性與警告
禁忌症
- Pre-existing severe myelosuppression
- Impaired cardiac function
- Patients who have reached the total cumulative dose limit of doxorubicin and/or daunorubicin
- Cats with pre-existing renal insufficiency
不良反應
- Bone marrow suppression (nadir 5-10 days)
- Cardiac toxicity (acute arrhythmias and cumulative cardiomyopathy)
- Nephrotoxicity (particularly in cats)
- Gastroenteritis (anorexia, vomiting, diarrhea)
- Alopecia
- Stomatitis
- Immediate hypersensitivity/anaphylaxis (primarily in dogs)
- Severe tissue ulceration and necrosis (if extravasated)
注意事項
WARNING: Severe Vesicant & Cardiotoxin
- Extravasation Risk: Doxorubicin is extremely irritating to tissues. Perivascular administration can cause severe tissue ulceration and necrosis. Must be administered IV slowly (over at least 10 minutes) via a perfectly placed, free-flowing catheter. If extravasation occurs, treat immediately (e.g., topical DMSO or IV dexrazoxane).
- Cardiotoxicity: Risk increases greatly when cumulative dose exceeds 240 mg/m2 in dogs (and likely cats). Breeds predisposed to cardiomyopathy (Dobermans, Great Danes, Rottweilers, Boxers) require extremely careful monitoring.
- MDR1/ABCB1 Mutation: Actively transported by p-glycoprotein. Dogs with MDR1 mutations (Collies, Australian Shepherds, etc.) are at high risk for severe toxicity. Dose reduction of 25-30% is recommended.
- Hypersensitivity: Immediate reactions (urticaria, facial swelling, hypotension) can occur, especially in dogs. Pretreatment with antihistamines (e.g., diphenhydramine) or dexamethasone is often recommended.
- Handling: Teratogenic and embryotoxic. Prepare in a biological safety cabinet. Wear gloves. Wash immediately if skin contact occurs.
藥物相互作用
May potentiate the toxic effects of doxorubicin
Potentially could increase risk for cardiotoxicity associated with doxorubicin
Decreased carbamazepine levels
Increased risk of toxicity for both agents; carefully weigh risks versus benefits
May increase doxorubicin blood levels (AUC); doxorubicin may potentiate and prolong hematologic toxicity; coma and seizures have been reported in human patients
Can increase doxorubicin and doxorubicinol (active metabolite) levels
May reduce doxorubicin effectiveness; use together not recommended in humans
Doxorubicin may decrease phenytoin levels
May increase elimination and reduce blood levels of doxorubicin
May inhibit doxorubicin metabolism
May increase doxorubicin levels
Increased risk for bleeding
Increased risk for neutropenia
Increases plasma clearance of doxorubicin
Causes a reduction in serum digoxin levels
Incompatible in syringe/line; leads to precipitate formation
Incompatible in syringe/line; leads to precipitate formation
Incompatible in syringe/line; leads to precipitate formation
Increased risk of toxicity
監測
- Efficacy of tumor response
- CBC with platelets (monitor for myelosuppression, nadir at 5-10 days)
- ECG and/or echocardiogram (especially in dogs with pre-existing heart disease or predisposed breeds)
- Hepatic function prior to and during therapy
- Urinalysis, serum creatinine, and BUN (especially in cats due to nephrotoxicity risk)
藥物動力學
半衰期
吸收
Not absorbed from the GI tract. Must be administered IV. Extremely irritating to tissues if administered SC or IM.
分佈
Rapidly and widely distributed after IV injection. Does not appreciably enter the CSF. Highly bound to tissue and plasma proteins. Probably crosses the placenta and is distributed into milk.
代謝
Metabolized extensively by the liver and other tissues via aldo-keto reductase primarily to doxorubicinol, which is active; other inactive metabolites are also formed.
排除
Primarily excreted in the bile and feces. Only about 5% is excreted in the urine within 5 days of dosing. Eliminated in a triphasic manner.
過量
Inadvertent acute overdosage may be manifested by severe exacerbations of adverse effects (profound myelosuppression, severe GI toxicity, acute cardiotoxicity). A lethal dose for dogs has been reported as 72 mg/m2.
Treatment: Supportive and symptomatic therapy is required. Dexrazoxane may be useful to help prevent cardiac toxicity and should be considered in cases of massive overdose.
可用產品
劑型
- Lyophilized powder for injection
- Aqueous injection
- Liposomal injection
人用標示
- Doxorubicin HCl (Conventional) Lyophilized Powder for Injection: 10 mg, 20 mg, 50 mg, and 150 mg vials (Adriamycin RDF, generic)
- Doxorubicin HCl (Conventional) Injection (aqueous): 2 mg/mL in 5 mL, 10 mL, 25 mL, and 100 mL (Adriamycin PFS, generic)
- Doxorubicin, Liposomal Injection: 20 mg in 10 mL & 50 mg in 30 mL single-use vials (Doxil)
各地核准狀態
POM (Prescription Only Medicine). Must be handled by trained personnel.
POM-V. Cytotoxic handling precautions apply.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Lyophilized powder: Store away from direct sunlight in a dry place. Reconstituted powder (with 0.9% NaCl) is stable for 24 hours at room temperature and 48 hours refrigerated. Aqueous injection: Stable for 18 months when refrigerated (2-8°C) and protected from light.
飼主須知
接受多柔比星治療的寵物主人重要須知：
- 紅色尿液：多柔比星本身是紅色的，治療後 1 到 2 天內寵物的尿液呈現橘色到紅色是完全正常的。這不是血尿，也無害。
- 安全處理排泄物：藥物會透過寵物的排泄物排出。請避免皮膚直接接觸尿液或糞便。治療後犬隻的尿液中可能殘留藥物長達 21 天，糞便中也會殘留數天。清理排泄物時請戴上手套，並徹底洗手。
- 身體接觸：在寵物接受化療期間，請勿讓寵物舔舐人類的皮膚，特別是兒童或免疫力低下者的臉部。
- 預期副作用：治療後 2 到 5 天常見輕微食慾不振和偶爾嘔吐。
- 何時應聯繫獸醫：如果您的寵物出現嚴重極度抑鬱、異常出血、瘀傷或血便，請立即聯繫您的獸醫。
- 脫毛：某些寵物（特別是毛髮持續生長的犬種，如貴賓犬或㹴犬）可能會出現脫毛或毛髮變稀疏的現象。
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