洛莫司汀
Lomustine
1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU)
別名: CeeNu · Belustine · Cecenu · CiNU · Citosta · Lomeblastin · Lucostine · Prava · CCNU · Gleostine · lomustinum · NSC-79037 · RB1509 · WR-139017
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 (CNS neoplasms, lymphomas, mast cell tumors, histiocytic sarcomas) | 50-90 mg/m2 | PO | every 2-6 weeks | — | 🌎 NA |
| All uses (brain tumours, mast cell tumours, lymphoma, histiocytic sarcoma) | 60-80 mg/m2 | PO | q3-4wk | As directed by oncologist | 🌍 EU |
- Antineoplastic (CNS neoplasms, lymphomas, mast cell tumors, histiocytic sarcomas): Dosed in mg/m2, NOT mg/kg. Exact protocol depends on indication.
- All uses (brain tumours, mast cell tumours, lymphoma, histiocytic sarcoma): S-Adenosylmethionine and silybin may be used to prevent or treat hepatotoxicity.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Antineoplastic (CNS neoplasms, lymphomas, mast cell tumors) | 60 mg/m2 | PO | every 6 weeks | — | 🌎 NA |
| Antineoplastic (CNS neoplasms, lymphomas, mast cell tumors) | 10 mg | PO | every 3 weeks | — | 🌎 NA |
| All uses | 30-60 mg/m2 | PO | q4-6wk | As directed by oncologist | 🌍 EU |
- Antineoplastic (CNS neoplasms, lymphomas, mast cell tumors): Administered as a single 10 mg total dose.
- All uses: Dose is suggested but not well established. Specialist advice should be sought, as dosing intervals may need to be increased due to delayed myelosuppression.
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
洛莫司汀（通常稱為 CCNU）是一種高脂溶性的亞硝基脲類烷化抗腫瘤藥物。由於其高脂溶性，它能輕易穿透血腦屏障，這使其在治療中樞神經系統 (CNS) 惡性腫瘤方面具有獨特的價值。
主要獸醫適應症：
- 肥大細胞瘤 (MCTs)： 常作為犬貓的一線或救援療法。
- 組織細胞肉瘤： 被認為是犬局部或播散性組織細胞肉瘤的首選治療方法。
- 淋巴瘤： 常作為復發性多中心型淋巴瘤的救援藥物，或作為上皮性（皮膚）淋巴瘤的主要藥物。
- 中樞神經系統腫瘤： 用於原發性腦腫瘤（如神經膠質瘤）或轉移性中樞神經系統病變。
臨床要點： 洛莫司汀以在犬隻身上引起延遲性、累積性且可能不可逆的肝毒性而聞名。許多獸醫腫瘤學家強烈建議同時給予保肝藥物（如 SAMe 和水飛薊素）。
作用機轉
Lomustine is a cell cycle-phase nonspecific antineoplastic drug, meaning it is toxic to cancer cells regardless of their current phase in the division cycle.
- Alkylating Activity: It undergoes spontaneous decomposition in vivo to form reactive intermediates. These intermediates transfer alkyl groups to DNA and RNA → causing cross-linking of DNA strands → preventing DNA replication and RNA transcription.
- Carbamoylation: The drug also causes carbamoylation of cellular proteins (specifically lysine residues) → inhibits DNA repair enzymes, preventing the cancer cell from fixing the alkylation damage, ultimately leading to apoptosis.
安全性與警告
禁忌症
- Pre-existing severe bone marrow depression
- Active infections
- Pregnancy (Teratogenic - FDA Category D)
- Nursing/lactating animals
- Pre-existing bone marrow suppression
- Pre-existing liver disease
- Pregnancy and lactation
不良反應
- Bone marrow depression (anemia, thrombocytopenia, leukopenia) - nadirs typically at 1-6 weeks
- Hepatotoxicity (delayed, cumulative, chronic, and irreversible in dogs)
- Stomatitis
- Alopecia
- Corneal de-epithelization
- Renal toxicity (rare)
- Pulmonary infiltrates or fibrosis (rare)
- Myelosuppression (dose-limiting; severe neutropenia and thrombocytopenia)
- Hepatotoxicity (cumulative, dose-related, potentially irreversible in dogs)
- Gastrointestinal toxicity (vomiting, diarrhea, anorexia)
注意事項
Use only when potential benefits outweigh risks in patients with pre-existing anemia, bone marrow depression, pulmonary function impairment, current infection, impaired renal function, or sensitivity to lomustine. Extreme caution is required in patients who have received previous chemotherapy or radiotherapy due to compromised bone marrow reserves. Hepatotoxicity in dogs can be severe, delayed, and irreversible. Teratogenic in laboratory animals; suppresses gonadal function. Nursing puppies/kittens should receive milk replacer if the mother is treated.
藥物交互作用
May increase the risk of severe infection due to additive immunosuppression.
Additive bone marrow depression; concurrent use should be avoided or strictly monitored.
Increased risk of vaccine-induced infection or decreased vaccine efficacy; use with extreme caution or avoid during therapy.
Increased risk of severe and potentially fatal bone marrow suppression.
Altered metabolism of lomustine, which requires hepatic microsomal enzyme hydroxylation. Use with caution.
Enhances the toxicity of lomustine (reported in humans).
監測
- CBC with platelets one week after dosing and prior to next dose (If platelets < 200,000/mcl, stop therapy until thrombocytopenia is resolved)
- Liver function tests (ALT, AST, ALP, Bilirubin) initially before starting treatment and then every 3-4 months
- Complete Blood Count (CBC) including platelets, particularly 7-14 days post-administration (and up to 6 weeks in cats)
- Liver function tests (ALT, AST, ALP, Bilirubin) prior to every dose
- Clinical signs of gastrointestinal toxicity
藥物動力學
半衰期
吸收
Absorbed rapidly and extensively from the GI tract. Some absorption occurs after topical administration.
分佈
Lomustine and its active metabolites are widely distributed in the body. Highly lipophilic. While parent lomustine is not detected in the CSF, its active metabolites cross the blood-brain barrier and are detected in substantial concentrations.
代謝
Metabolized extensively in the liver to both active and inactive metabolites.
排除
Eliminated primarily in the urine.
過量
Because of the severe potential toxicity of the drug (profound myelosuppression and hepatotoxicity), overdoses should be treated aggressively.
- Employ gut emptying protocols (emesis, activated charcoal) immediately if exposure was recent and the patient is asymptomatic.
- Provide aggressive supportive care and monitor CBC and liver enzymes closely.
- Consult an animal poison control center or a veterinary oncologist for specific guidance.
可用產品
劑型
- Capsules
- 40 mg oral capsule
人用標示
- Lomustine Capsules: 10 mg, 40 mg & 100 mg with mannitol; CeeNu® (Bristol Labs Oncology); (Rx)
- 10 mg capsule
- 40 mg capsule
- 100 mg capsule
各地核准狀態
POM (Prescription Only Medicine). Handled under cascade.
POM-V. Handled under the prescribing cascade.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store capsules in well-closed containers at room temperature. Expiration dates of two years are assigned after manufacture.
飼主須知
重要安全與操作指南：
- 細胞毒性防護： 洛莫司汀是一種化療藥物。處理膠囊時請戴上一次性手套。請勿打開、壓碎或剝開膠囊。
- 廢物處理： 服藥後長達 24 小時內（某些療程建議 48-72 小時的防護），可在寵物的尿液和糞便中檢測到藥物及其有毒代謝物。清理尿液、糞便或嘔吐物時請戴上手套，事後徹底洗手。孕婦或免疫力低下者應避免接觸該藥物或寵物的排泄物。
何時應聯繫獸醫：
- 洛莫司汀會引起嚴重的骨髓抑制和肝臟損傷。
- 如果您的寵物出現感染跡象、發燒、異常瘀傷或出血、眼白或牙齦發黃（黃疸）、持續嘔吐、腹瀉，或者變得精神萎靡和生病，請立即聯繫您的獸醫。
VetSheet 藥物參考供合格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商最新仿單。