米托蒽醌
Mitoxantrone
Mitoxantrone hydrochloride
別名: Novantrone · L-232315 · DHAD · dihydroxyanthracenedione dihydrochloride · mitoxantroni hydrochloridum · NSC-301739 · Mitoxantrone hydrochloride · Mitozantrone
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 |
|---|---|---|---|---|---|
| Transitional cell carcinoma | 5 mg/m2 IV every 21 days with piroxicam (0.3 mg/kg PO once daily) | IV | every 21 days | — | 🌎 NA |
| Lymphoma, squamous cell carcinoma, transitional cell carcinoma, mammary gland tumors, etc. | 6 mg/m2 IV every 2-3 weeks | IV | every 2-3 weeks | — | 🌎 NA |
| Single rescue agent for lymphoma | 5.5-6 mg/m2 IV every 3 weeks | IV | every 3 weeks | — | 🌎 NA |
| Rescue agent for canine lymphoma | 6 mg/m2 IV every 2-3 weeks | IV | every 2-3 weeks | — | 🌎 NA |
| Transitional cell carcinoma after laser ablation of the primary tumor | 5 mg/m2 IV every 3 weeks for 4 treatments | IV | every 3 weeks | 4 treatments | 🌎 NA |
- Rescue agent for canine lymphoma: Check CBC on day 7 after treatment and the protocol can be repeated on day 14 or 21 if the dog attains complete or partial response. Combining with DTIC (dacarbazine) may improve response rate.
- Transitional cell carcinoma after laser ablation of the primary tumor: Piroxicam was given at a dosage of 0.3 mg/kg PO once daily for the remaining life of the dog.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Soft-tissue sarcomas | 6-6.5 mg/m2 IV given every 3-4 weeks for 4-6 treatments | IV | every 3-4 weeks | 4-6 treatments | 🌎 NA |
| Effective dose (general) | 6.5 mg/m2 IV every 2-3 weeks | IV | every 2-3 weeks | — | 🌎 NA |
| Single rescue agent for lymphoma | 6-6.5 mg/m2 IV every 3 weeks | IV | every 3 weeks | — | 🌎 NA |
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
米托蒽醌（Mitoxantrone）是一種合成的蒽醌類（anthracenedione）抗腫瘤藥物，在獸醫腫瘤學中用於治療犬貓的多種惡性腫瘤。
主要臨床應用：
- 淋巴瘤： 常在第一線化療方案（如CHOP）失效時作為救援藥物。
- 癌（Carcinomas）： 對移行細胞癌（TCC）、鱗狀細胞癌、腎腺癌和甲狀腺癌有效。
- 肉瘤（Sarcomas）： 用於纖維肉瘤、血管外皮細胞瘤和乳腺腺癌。
臨床要點：
- 結構上與蒽環類藥物（如阿黴素 doxorubicin）相似，但缺乏氨基糖基團，這大幅減少了自由基的產生，因此其心臟毒性遠低於阿黴素。
- 由於其腎臟清除率極低（約10%），對於患有腎功能不全的貓來說，是比阿黴素更安全的替代選擇。
- 由於其深藍色外觀及強效作用，在獸醫腫瘤學中常被俗稱為「藍色閃電（blue thunder）」。
作用機轉
Mitoxantrone exerts its cytotoxic effects through multiple mechanisms:
- DNA Intercalation: It inserts itself between DNA base pairs, causing structural distortion.
- Electrostatic Interaction: Nonintercalative binding to DNA further stabilizes the drug-DNA complex.
- Topoisomerase II Inhibition: (Pharmacological addition) It inhibits the enzyme Topoisomerase II, preventing the religation of DNA strands and leading to double-strand DNA breaks.
- Synthesis Inhibition: Ultimately inhibits both DNA and RNA synthesis.
While it is not strictly cell-cycle phase specific, it demonstrates the highest activity during the S phase (DNA synthesis phase) of the cell cycle.
安全性與警告
禁忌症
- Severe pre-existing myelosuppression
- Concurrent active infection
- Significantly impaired cardiac function
- Patients with prior extensive cytotoxic drug or radiation exposure (relative)
- Pregnancy (FDA Category D) and nursing mothers
- Concurrent infection
- Hepatic disease
不良反應
- Dose-dependent GI distress (vomiting, anorexia, diarrhea)
- Bone marrow depression (neutropenia, sepsis; nadir typically around day 10)
- Non-regenerative anemia
- Lethargy
- Seizures (specifically noted in cats)
- Blue-green discoloration of urine and sclera (benign)
- Tissue necrosis or phlebitis (if extravasated, though less severe than doxorubicin)
- Rarely: conjunctivitis, jaundice, renal failure, allergic reactions, thrombocytopenia
- Gastrointestinal signs (vomiting, anorexia, diarrhoea)
- Bone marrow depression (WBC nadir generally at 10 days)
- Seizure activity (reported in cats)
- Blue discoloration of urine and sclera (very rare)
- Acute renal failure (anecdotal in cats)
注意事項
Handling Precautions: Mitoxantrone is a cytotoxic agent. Strict adherence to safe handling, administration, and disposal protocols for chemotherapeutic agents is mandatory to protect veterinary personnel.
Extravasation Risk: While generally considered an irritant rather than a severe vesicant like doxorubicin, extravasation can still cause tissue necrosis. Ensure a perfectly placed, clean IV catheter before administration.
Organ Function: Use with caution in patients with impaired hepatic function or hyperuricemia/hyperuricuria.
藥物交互作用
Cardiotoxicity risks may be enhanced in patients that have previously received these therapies to the mediastinum.
Concurrent use may significantly increase the risk of severe infection.
Additive bone marrow depression; use with extreme caution.
Increased risk of vaccine-induced infection; should be used with extreme caution or avoided during therapy.
Increased risk of severe bone marrow depression
Increased risk of severe immunosuppression and infection
Chemically incompatible
監測
- CBC with differential and platelets (especially around day 7-10 to check for nadir)
- Tumor measurements/efficacy
- Chest radiographs, ECG, or other cardiac function tests (if cardiac symptomatology is present)
- Liver function tests (if jaundice or clinical signs of hepatotoxicity occur)
- Serum uric acid levels (for susceptible patients)
- Complete Blood Count (CBC), especially WBC count around day 10 post-administration
- Gastrointestinal signs (vomiting, diarrhoea, appetite)
- Renal parameters (especially in cats)
- Hepatic function
- Cardiac function (echocardiogram) if pre-existing disease exists
藥物動力學
吸收
Administered IV; rapidly and extensively distributed.
分佈
Highest concentrations found in the liver, heart, thyroid, and red blood cells. Approximately 78% bound to plasma proteins in humans.
代謝
Metabolized in the liver.
排除
The majority of the drug is excreted unchanged in the urine. Renal clearance is minimal (~10%).
過量
Due to the narrow therapeutic index and potential for serious toxicity (profound myelosuppression, severe GI mucosal damage, sepsis), dosage determinations must be made with extreme care. Overdose management is primarily supportive, focusing on aggressive fluid therapy, broad-spectrum antibiotics to manage sepsis secondary to neutropenia, and potentially the use of recombinant granulocyte-colony stimulating factors (G-CSF) to accelerate bone marrow recovery.
可用產品
劑型
- Injection solution concentrate: 2 mg/mL
- Injectable: 2 mg/ml
人用標示
- Mitoxantrone HCl for Injection Solution Concentrate: 2 mg/mL, preservative free in 10 mL, 12.5 mL, & 15 mL multi-dose vials (Novantrone®)
- Novantrone 2 mg/ml injection
各地核准狀態
POM (Prescription Only Medicine)
POM (Prescription Only Medicine)
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store at room temperature. Do not mix or use the same IV line with heparin infusions as a precipitate may form. It is not recommended to mix with other IV drugs. While the manufacturer recommends not freezing, one study showed it maintained cytotoxic effects when frozen and thawed over a 12-month period.
飼主須知
重要化療安全須知 您的寵物正在接受強效的化學治療藥物。在治療後的6天內，藥物及其代謝物可能會出現在寵物的尿液中，糞便中則可達7天。
- 排泄物處理： 清理尿液、糞便或嘔吐物時，請務必戴上拋棄式手套。將排泄物雙層裝袋後再丟入一般垃圾桶。處理完畢後請徹底洗手。
- 顏色變化： 您可能會發現寵物的尿液變成藍綠色，或者眼白（鞏膜）帶有輕微的藍色。請不要驚慌——這是藥物本身深藍色染料造成的正常且無害的現象。
- 需注意的副作用： 密切觀察寵物是否有食慾不振、嘔吐、腹瀉或極度疲倦的現象。由於此藥物會降低白血球數量，您的寵物感染的風險會增加。
- 何時該聯絡獸醫師： 如果您的寵物發燒、嚴重嘔吐/腹瀉，或者貓咪出現任何癲癇（抽搐）症狀，請立即聯絡您的獸醫師。
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