苯丁酸氮芥
Chlorambucil
4-[bis(2-chloroethyl)amino]benzenebutanoic acid
別名: Leukeran · Chloraminophene · Linfolysin · CB-1348 · NSC-3088 · WR-139013 · chlorambucilum · chlorbutinum
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
0.1-0.2 mg/kg PO once daily or every other dayPO· q24h or q48h
— 🐕
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 |
|---|---|---|---|---|---|
| Adjunctive therapy for glomerulonephritis | 0.1-0.2 mg/kg PO once daily or every other day | PO | q24h or q48h | — | 🌎 NA |
| Canine lymphoma (first level treatment when combination chemo is declined) | 6-8 mg/m2 (NOT mg/kg) PO every other day | PO | q48h | — | 🌎 NA |
| Lymphoproliferative disease; macroglobulinemia | 2-4 mg/m2 (NOT mg/kg) PO q24-48h | PO | q24-48h | — | 🌎 NA |
| Pemphigus complex | 0.2 mg/kg q24-48h | PO | q24-48h | — | 🌎 NA |
| Pemphigus complex | 0.1-0.2 mg/kg once daily initially until marked improvement (or 75% improvement) of clinical signs (may require 4-8 weeks). Then alternate day dosing is begun and maintained for several weeks. | PO | q24h initially, then q48h | Several weeks | 🌎 NA |
| Adjunctive treatment of inflammatory bowel disease | 1.5 mg/m2 (NOT mg/kg) PO every other day | PO | q48h | — | 🌎 NA |
| Chronic lymphocytic leukaemia | 2-6 mg/m2 initially until remission achieved, then at reduced dosage/frequency; OR 0.2 mg/kg for 7 days then 0.1 mg/kg for maintenance; OR 20 mg/m2 every 1-2 weeks | PO | q24h or q1-2wk | Until remission, then maintenance | 🌍 EU |
| Lymphoma | 15-20 mg/m2 with prednisolone; OR 2-6 mg/m2; OR 1.4 mg/kg as single dose substitute for cyclophosphamide in CHOP-type protocols | PO | q2wk (15-20 mg/m2) or q24-48h (2-6 mg/m2) | Protocol dependent | 🌍 EU |
| Pemphigus complex | 0.1-0.2 mg/kg initially until marked improvement, then alternate-day dosing | PO | q24h initially, then q48h | Often for several weeks | 🌍 EU |
| Protein-losing enteropathy and other immune-mediated diseases | 2-6 mg/m2 until clinical remission, then tapered to the minimum effective dose | PO | q24h | Until remission, then tapered | 🌍 EU |
| Metronomic chemotherapy | 4 mg/m2 | PO | q24h | Ongoing | 🌍 EU |
- Canine lymphoma (first level treatment when combination chemo is declined): Used in combination with Prednisone 40 mg/m2 PO daily for 7 days then every other day. Perform CBC every 2-3 weeks.
- Pemphigus complex: With Prednisone 2-4 mg/kg PO divided q12h
- Pemphigus complex: Used in combination with corticosteroids. Alternately decrease chlorambucil and corticosteroids until lowest possible dose is attained.
- Chronic lymphocytic leukaemia: Give with food. Often used with prednisolone 40 mg/m2 p.o. q24h for 7 days then 20 mg/m2 q48h.
- Lymphoma: Give with food.
- Pemphigus complex: Give with food. Used in combination with corticosteroids.
- Protein-losing enteropathy and other immune-mediated diseases: Give with food.
- Metronomic chemotherapy: Give with food.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Refractory or severe IBD (Cats > 4 kg) | 2 mg (total dose) PO q48 hours (every other day) for 2-4 weeks then tapered to the lowest effective dose (2 mg per cat q72-96 hours; every 3rd to 4th day) | PO | q48h initially, then q72-96h | Indefinite | 🌎 NA |
| Refractory or severe IBD (Cats < 4 kg) | 2 mg (total dose) q72 hours (every 3rd day) | PO | q72h | — | 🌎 NA |
| Severe IBD or intestinal lymphoma | 15 mg/m2 (NOT mg/kg) PO once per day for 4 consecutive days, repeated every 3 weeks | PO | q24h for 4 days, repeat q3w | — | 🌎 NA |
| Lymphocytic-plasmacytic enteritis (LPE) - Method 1 | Initial dose is 2 mg/m2 (NOT mg/kg) PO for 4-7 days, then decreased to 1 mg/m2 (NOT mg/kg) for 7 days. If clinical signs are lessening, continue daily dosing but only every other week | PO | Variable | — | 🌎 NA |
| Lymphocytic-plasmacytic enteritis (LPE) - Method 2 | Large cats (>7 lb.) 2 mg PO twice weekly; smaller cats (<7 lb) 1 mg PO twice weekly | PO | Twice weekly | — | 🌎 NA |
| Severe IBD / Lymphoma (Alternative to prednisolone) | For cats < 2 kg: 2 mg (total dose) PO once weekly. For cats > 2 kg: 2 mg (total dose) PO once every 4 days. | PO | Once weekly or q4d | — | 🌎 NA |
| Pemphigus complex or other immune-mediated dermatoses | 2 mg (total dose per cat) every 48 hours | PO | q48h | — | 🌎 NA |
| Generalized pemphigus foliaceous | 0.1-0.2 mg/kg PO q24-48h | PO | q24-48h | — | 🌎 NA |
| Idiopathic dermatitis | 0.2 mg/kg PO q24-48h | PO | q24-48h | — | 🌎 NA |
| Adjunctive treatment of FIP | 20 mg/m2 (NOT mg/kg) every 2-3 weeks | PO | q2-3w | — | 🌎 NA |
| Lymphocytic leukemia | 6 mg/m2 (2 mg/5.3 kg cat) PO every other day | PO | q48h | — | 🌎 NA |
| Immune-mediated disease | >4 kg: 2 mg (total dose); <4 kg: 2 mg (total dose) | PO | q48h (>4 kg) or q72h (<4 kg) | 2-4 weeks, then tapered to lowest effective dose | 🌍 EU |
| Chronic lymphocytic leukaemia | 2 mg/m2 OR 20 mg/m2 | PO | q48h (2 mg/m2) or q14d (20 mg/m2) | Ongoing | 🌍 EU |
| Low grade/small cell lymphoma | 20 mg/m2 | PO | q14d | Ongoing | 🌍 EU |
| Substitute for cyclophosphamide in CHOP protocol | 1.4 mg/kg | PO | Once | Single dose | 🌍 EU |
| Feline pemphigus foliaceus or severe feline eosinophilic granuloma complex | 0.1-0.2 mg/kg initially until marked improvement, then alternate-day dosing | PO | q24h initially, then q48h | Often for several weeks | 🌍 EU |
- Refractory or severe IBD (Cats > 4 kg): Second choice after corticosteroids
- Severe IBD or intestinal lymphoma: In combination with prednisolone. Alternatively, may dose at 2 mg (total dose) per cat every 4 days indefinitely.
- Lymphocytic-plasmacytic enteritis (LPE) - Method 1: Administer with prednisolone. Common for patients to develop anemia.
- Lymphocytic-plasmacytic enteritis (LPE) - Method 2: Slowly taper to lowest effective dose after 4-6 weeks.
- Pemphigus complex or other immune-mediated dermatoses: May be used in combination with or as an alternative to steroids.
- Generalized pemphigus foliaceous: Add if poor response to prednisolone alone.
- Idiopathic dermatitis: Closely monitor during treatment.
- Adjunctive treatment of FIP: With Prednisolone 4 mg/kg PO once daily
- Lymphocytic leukemia: With prednisolone 5 mg/cat/day. Supplemental cobalamin and folate/B-complex vitamins should also be given.
- Immune-mediated disease: Give with food.
- Chronic lymphocytic leukaemia: Give with food. With or without prednisolone.
- Low grade/small cell lymphoma: Give with food. Used with prednisolone.
- Substitute for cyclophosphamide in CHOP protocol: Give with food.
- Feline pemphigus foliaceus or severe feline eosinophilic granuloma complex: Give with food. Used in combination with corticosteroids.
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Adjunctive therapy in treating lymphoma using the LAP protocol | 20 mg/m2 (NOT mg/kg) PO every 2 weeks | PO | q2w | — | 🌎 NA |
- Adjunctive therapy in treating lymphoma using the LAP protocol: Alternating with cytosine arabinoside and Prednisone 1.1-2.2 mg/kg PO every other day.
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
苯丁酸氮芥是一種氮芥衍生物，在獸醫學中主要用作抗腫瘤和免疫抑制劑。
- 臨床要點： 在貓科醫學中備受青睞，用於治療嚴重的自體免疫疾病（如炎症性腸病、落葉型天皰瘡）和小細胞（低惡性度）胃腸道淋巴瘤，因為與環磷醯胺或硫唑嘌呤等其他烷化劑相比，它對貓的毒性顯著較低且耐受性更好。
- 它也可用於各種腫瘤疾病，包括淋巴性白血病、多發性骨髓瘤、真性紅血球增多症和巨球蛋白血症。
- 由於其可能引起骨髓抑制，治療期間必須常規監測全血球計數 (CBC)。
作用機制
Chlorambucil is a cell-cycle nonspecific alkylating agent.
- Mechanism: It works by forming highly reactive carbonium ions that cross-link with cellular DNA → prevents DNA transcription and replication → disrupts nucleic acid function → ultimately leads to cell death (apoptosis).
- Its immunosuppressive effects are secondary to its cytotoxic action on rapidly dividing lymphoid cells.
安全性與警告
禁忌症
- Known hypersensitivity or resistance to the drug
- Pregnancy (potential teratogen)
不良反應
- Myelosuppression (anemia, leukopenia, thrombocytopenia)
- Gastrointestinal toxicity (vomiting, diarrhea)
- Alopecia and delayed hair regrowth (especially in Poodles and Kerry Blue Terriers)
- Neurotoxicity (rare; facial twitching, myoclonus, agitation, seizures)
注意事項
Important Warnings:
- Myelosuppression: Use with extreme caution in patients with preexisting bone marrow depression or active infections.
- Toxicity: Higher dosages increase the likelihood of toxicity. Nadirs usually occur within 7-14 days of starting therapy.
- Reproductive Safety: Potential teratogen. Avoid during pregnancy unless benefits clearly outweigh risks. Documented to cause irreversible infertility in male humans.
- Handling: Caregivers should wear gloves when handling this medication to prevent accidental exposure.
藥物相互作用
Chloramphenicol
Additive bone marrow depression
Flucytosine
Additive bone marrow depression
Amphotericin B
Additive bone marrow depression
Colchicine
Additive bone marrow depression
Azathioprine
Increased risk of infection and immunosuppression
Cyclophosphamide
Increased risk of infection and immunosuppression
Cyclosporine
Increased risk of infection and immunosuppression
Corticosteroids
Increased risk of infection and immunosuppression
Hepatic cytochrome P450 stimulatorsMajor
Increases cytotoxic effects of chlorambucil
PrednisoloneMinor
Synergistic effect in the management of lymphoid neoplasia
監測
- Clinical efficacy
- CBC and Platelets (once weekly or every other week initially; once stable, monthly or every 3-6 months)
- Uric acid levels (if warranted)
- Liver enzymes (if warranted)
藥物動力學
吸收
Rapidly and nearly completely absorbed after oral administration; peak levels occur in about one hour.
分佈
Highly bound to plasma proteins. Crosses the placenta. Unknown if it crosses the blood-brain barrier, but neurological side effects have been reported.
代謝
Extensively metabolized in the liver, primarily to phenylacetic acid mustard, which is active.
排除
Phenylacetic acid mustard is further metabolized to other metabolites that are excreted in the urine.
過量
The oral LD50 in mice is 123 mg/kg. In humans, acute overdoses up to 5 mg/kg resulted in neurologic toxicity (seizures) and pancytopenia (nadirs at 1-6 weeks post ingestion).
- Treatment: Consists of gut emptying when appropriate (beware of rapidly changing neurologic status if inducing vomiting).
- Monitoring: CBCs several times a week for several weeks should be performed. Blood component therapy may be necessary.
可用產品
劑型
- tablets
- oral suspension (compounded)
人用標示
- Chlorambucil Oral Tablets (film-coated): 2 mg; Leukeran® (GlaxoSmithKline); (Rx)
各地核准狀態
European Union✗ 未核准處方藥EMA
POM (Prescription Only Medicine). Handled under strict cytotoxic drug regulations.
United Kingdom✗ 未核准處方藥VMD
POM. Handled under strict cytotoxic drug regulations.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Tablets should be stored in light-resistant, well-closed containers under refrigeration (2-8°C; 36-46°F). Tablets can be stored at a maximum of 30°C (86°F) up to one week. Compounded oral suspensions (2 mg/mL) retain 90% potency for 7 days at 5°C; room temperature storage causes rapid decomposition.
飼主須知
寵物主人重要須知
- 給藥方式： 請嚴格按照獸醫的指示給藥。未經獸醫同意，請勿自行更改劑量或突然停藥。
- 安全操作： 由於這是一種化療藥物，處理藥片或懸浮液時請戴上手套。處理後請徹底洗手。孕婦應完全避免接觸此藥物。
- 注意事項： 如果發現任何毒性跡象，請立即向獸醫報告。這包括異常出血、不明原因的瘀傷、尿液或糞便帶血、嚴重嗜睡、感染跡象（如發燒）或呼吸急促。
- 監測： 您的寵物需要定期進行血液檢查，以確保藥物不會過度抑制其骨髓功能。
VetSheet 藥物參考供持牌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方最新藥品說明書。