클로람부실
Chlorambucil
4-[bis(2-chloroethyl)amino]benzenebutanoic acid
다른 이름: Leukeran · Chloraminophene · Linfolysin · CB-1348 · NSC-3088 · WR-139013 · chlorambucilum · chlorbutinum
VetSheet 수의사 팀 검수업데이트 2026년 4월 5일근거 기반 수의학 참고자료
0.1-0.2 mg/kg PO once daily or every other dayPO· q24h or q48h
— 🐕
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
동물 종별 용량
🌎 NA — North America🌍 EU — Europe
개
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| 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.
고양이
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| 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.
말
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| 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.
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
개요
클로람부실은 질소 머스타드 유도체로 수의학에서 주로 항종양제 및 면역억제제로 사용됩니다.
- 임상 요점: 고양이의 중증 자가면역 질환(예: 염증성 장질환, 낙엽성 천포창) 및 소세포(저등급) 위장관 림프종 치료에 매우 선호됩니다. 이는 시클로포스파미드나 아자티오프린과 같은 다른 알킬화제에 비해 고양이에게 독성이 현저히 낮고 내약성이 좋기 때문입니다.
- 또한 림프구성 백혈병, 다발성 골수종, 진성 적혈구증가증, 거대글로불린혈증을 포함한 다양한 종양성 질환에도 사용됩니다.
- 골수 억제를 유발할 수 있으므로 치료 중 전체 혈구 계산(CBC)의 정기적인 모니터링이 필수적입니다.
작용 기전
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.
안전성·주의사항
금기사항
- Known hypersensitivity or resistance to the drug
- Pregnancy (potential teratogen)
부작용
- 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)
주의
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.
약물 상호작용
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
모니터링
- 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)
약동학
흡수
Rapidly and nearly completely absorbed after oral administration; peak levels occur in about one hour.
분포
Highly bound to plasma proteins. Crosses the placenta. Unknown if it crosses the blood-brain barrier, but neurological side effects have been reported.
대사
Extensively metabolized in the liver, primarily to phenylacetic acid mustard, which is active.
배설
Phenylacetic acid mustard is further metabolized to other metabolites that are excreted in the urine.
과다투여
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.
제품
제형
- tablets
- oral suspension (compounded)
인용의약품
- Chlorambucil Oral Tablets (film-coated): 2 mg; Leukeran® (GlaxoSmithKline); (Rx)
규제 현황
European Union✗ 미승인처방전의약품EMA
POM (Prescription Only Medicine). Handled under strict cytotoxic drug regulations.
United Kingdom✗ 미승인처방전의약품VMD
POM. Handled under strict cytotoxic drug regulations.
규제 데이터 없음: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
보관·안정성
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.
보호자 정보
반려동물 보호자를 위한 중요 정보
- 투여: 수의사의 지시에 따라 정확하게 이 약을 투여하십시오. 수의사와 상의 없이 복용량을 변경하거나 갑자기 중단하지 마십시오.
- 안전한 취급: 이 약은 항암제이므로 알약이나 현탁액을 만질 때는 장갑을 착용하십시오. 취급 후에는 손을 철저히 씻으십시오. 임산부는 이 약의 취급을 완전히 피해야 합니다.
- 주의할 점: 독성 징후가 나타나면 즉시 수의사에게 알리십시오. 여기에는 비정상적인 출혈, 원인 불명의 멍, 소변이나 대변의 피, 심한 무기력, 감염 징후(예: 발열) 또는 호흡 곤란이 포함됩니다.
- 모니터링: 약물이 골수를 과도하게 억제하지 않는지 확인하기 위해 반려동물은 정기적인 혈액 검사를 받아야 합니다.
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