氮芥 (Mechlorethamine)
Mechlorethamine
Mechlorethamine hydrochloride
別名: Mustargen · Caryolysine · Onco-Cloramin · Nitrogen mustard · Mustine · HN2 · Chlormethine hydrochloride · Chlorethazine hydrochloride · NSC-762 · WR-147650
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 |
|---|---|---|---|---|---|
| Lymphoma rescue (MOPP protocol) | 3 mg/m2 IV | IV | given on days 0 and 7 (or days 0 and 14) of a 28 day protocol | 28 day cycles | 🌎 NA |
- Lymphoma rescue (MOPP protocol): Given as part of a protocol that includes vincristine (or vinblastine), procarbazine, and prednisone (or prednisolone).
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Lymphoma rescue (MOPP protocol) | 3 mg/m2 IV | IV | given on days 0 and 7 (or days 0 and 14) of a 28 day protocol | 28 day cycles | 🌎 NA |
- Lymphoma rescue (MOPP protocol): Given as part of a protocol that includes vincristine (or vinblastine), procarbazine, and prednisone (or prednisolone).
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
Mechlorethamine（氮芥）是一種強效的細胞週期非特異性抗腫瘤藥物。在歷史上，它是第一個用於化學治療的氮芥類烷化劑。
在獸醫學中，它主要作為淋巴網狀內皮腫瘤的輔助治療，特別是作為復發性犬貓淋巴瘤的MOPP救援方案（Mechlorethamine, Oncovin [長春新鹼], Procarbazine, Prednisone）中的「M」。
臨床要點： 氮芥是一種強烈的起泡劑（vesicant）。在靜脈注射時必須極度小心以避免藥物外滲，否則會導致嚴重的組織壞死和脫落。由於價格大幅上漲和供應問題，一些獸醫腫瘤學家在救援方案中會使用放線菌素D (dactinomycin) 或洛莫司汀 (CCNU) 來替代。
它也可以透過體腔內注射來治療惡性胸腔和腹腔積液，作為硬化劑促使漿膜表面沾黏。
作用機轉
Mechlorethamine is a bifunctional alkylating agent.
- Mechanism: It undergoes intramolecular cyclization to form a highly reactive aziridinium ion. This ion reacts with nucleophilic sites on DNA (primarily the N7 position of guanine).
- Pathway: Alkylation → Cross-linking of DNA strands (interstrand and intrastrand) → Inhibition of DNA replication and RNA transcription → Cell death (apoptosis).
- It is cell cycle-phase nonspecific, meaning it can kill cells in any phase of the cell cycle, though it is most toxic to rapidly dividing cells.
- When given intracavitarily, it induces a strong inflammatory response on serous membranes, leading to sclerosis and obliteration of the cavity space.
安全性與警告
禁忌症
- Known infection
- Prior anaphylactic reaction to mechlorethamine
- Pregnancy (Category D teratogen)
- Anemia (relative)
- Bone marrow depression (relative)
- Tumor cell infiltration into bone marrow (relative)
- Patients who have received previous extensive chemotherapy or radiotherapy (relative)
不良反應
- Bone marrow depression (leukopenia, thrombocytopenia)
- Vomiting
- Nausea
- Ototoxicity (with high doses or regional perfusion)
- Alopecia
- Hyperuricemia
- Hepatotoxicity
- Peripheral neuropathy
- GI ulcers
- Severe tissue sloughing (if extravasated)
注意事項
Extravasation Risk: Mechlorethamine is a potent vesicant. Extravasation will cause severe tissue necrosis and sloughing. Ensure a perfectly placed, clean IV catheter before administration.
Hazardous Drug: This is a highly toxic antineoplastic agent. Strict hazardous drug handling protocols (gloves, gowns, biologic safety cabinet, closed-system transfer devices) must be utilized to protect veterinary personnel.
Teratogenicity: It is a known teratogen and can suppress gonadal function. Pregnant women should absolutely avoid handling this drug or the patient's waste.
Hyperuricemia: May raise serum uric acid levels; allopurinol may be required in susceptible patients.
藥物交互作用
May increase the risk of severe infection.
Additive bone marrow depression; use with extreme caution.
Increased risk of vaccine-induced infection or decreased vaccine efficacy; use with caution or avoid.
監測
- CBC with platelets (at least every 1-2 weeks until stable; then every 3 months)
- Liver function tests (initially before starting treatment and then every 3-4 months)
- Injection site for any signs of extravasation (redness, swelling, pain)
藥物動力學
吸收
Must be given IV for systemic use due to severe tissue irritation. Incompletely absorbed after intracavitary administration.
分佈
Rapidly distributed but highly reactive.
代謝
Rapidly (within minutes) inactivated after injection.
排除
Rapidly degraded in the body.
過量
Because of the extreme toxic potential of this agent, overdoses must be strictly avoided. Dosages must be calculated carefully (usually based on Body Surface Area in m2). Overdose will likely result in profound, potentially fatal myelosuppression and severe gastrointestinal toxicity.
可用產品
劑型
- Powder for injection
人用標示
- Mechlorethamine Powder for Injection: 10 mg; Mustargen® (Lundbeck)
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
Store the unconstituted powder at room temperature. Mechlorethamine is highly unstable in neutral or alkaline aqueous solutions and rapidly degrades. It must be administered immediately after preparation. Unused portions of reconstituted drug can be neutralized by adding equal volumes of 5% sodium thiosulfate and 5% sodium bicarbonate, allowed to stand for 45 minutes, and then discarded appropriately.
飼主須知
重要安全警告： 氮芥是一種強效的化療藥物。孕婦、哺乳期婦女和兒童在治療後至少 48-72 小時內，絕對不應接觸此藥物或清理寵物的排泄物（尿液、糞便、嘔吐物）。
- 監控注射部位： 如果藥物漏出血管，會造成嚴重的組織損傷。請每天檢查靜脈注射部位。如果您發現注射部位有任何發紅、腫脹、疼痛或寵物舔舐該處，請立即聯繫您的獸醫。
- 腸胃不適： 噁心和嘔吐是常見的副作用。您的獸醫可能會開立止吐藥物以幫助您的寵物保持舒適。
- 感染風險： 此藥物會降低白血球數量，使您的寵物更容易受到感染。請讓牠們遠離生病的動物，並觀察是否有生病的跡象，如嗜睡或發燒。
- 哺乳期寵物： 如果哺乳期的母犬/貓正在接受此藥物治療，幼犬或幼貓必須改用代乳品餵養。
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