아자티오프린

Azathioprine

Azathioprine / Azathioprine Sodium

다른 이름: Imuran · Azasan · Azathioprinum · BW-57322 · NSC-39084

VetSheet 수의사 팀 검수업데이트 2026년 4월 5일근거 기반 수의학 참고자료

Initially 2 mg/kg PO once daily for 2 weeks, then tapered to 2 mg/kg PO every other day for 2-4 weeks, then 1 mg/kg PO every other day.PO· q24h then tapered· Long-term

체중— 🐕

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
Inflammatory bowel disease	Initially 2 mg/kg PO once daily for 2 weeks, then tapered to 2 mg/kg PO every other day for 2-4 weeks, then 1 mg/kg PO every other day.	PO	q24h then tapered	Long-term	🌎 NA
Immune-mediated anemia, colitis, immune-mediated skin disease, and acquired myasthenia gravis	2 mg/kg PO once daily (q24h); long-term therapy 0.5-1 mg/kg PO every other day	PO	q24h then q48h	Long-term	🌎 NA
Adjunctive therapy in myasthenia gravis in non-responsive patients	Initially, 1 mg/kg PO once daily. If neutrophil and platelet counts are normal after 2 weeks, dose is increased to 2 mg/kg PO once daily.	PO	q24h	Until clinical remission	🌎 NA
Lymphoplasmacytic enteritis (if poor response to prednisolone)	2 mg/kg PO once daily for 5 days, then on alternate days to prednisolone	PO	q24h then q48h	Long-term	🌎 NA
Severe cases of immune-mediated hemolytic anemia (IMHA)	2.2 mg/kg PO once daily (q24h)	PO	q24h	Long-term	🌎 NA
Acute immune-mediated hemolytic anemia (IMHA) with glucocorticoids	1-2 mg/kg PO once daily	PO	q24h	Long-term maintenance	🌎 NA
Severe and refractory inflammatory bowel disease	2.2 mg/kg PO once daily	PO	q24h	Long-term	🌎 NA
Adjunctive treatment of ocular fibrous histiocytomas	2 mg/kg PO daily for 2 weeks, reevaluate, and reduce to 1 mg/kg every other day for 2 weeks, then 1 mg/kg once weekly for 1 month	PO	Tapering schedule	10 weeks	🌎 NA
Prevention of rejection of MHCmatched renal allografts (with cyclosporine)	1-5 mg/kg PO every other day	PO	q48h	Long-term	🌎 NA
Perianal fistulas (anal furunculosis)	Initially 2 mg/kg PO once daily (q24h)... Then reduce to 2 mg/kg PO every other day (q48h) and continued for 12 weeks... After 12 weeks, reduce dose to 1 mg/kg PO every other day (q48h)	PO	Tapering schedule	12 months	🌎 NA
Glomerulonephritis	2 mg/kg PO once daily	PO	q24h	Unspecified	🌎 NA
Chronic hepatitis (to reduce inflammation)	2.2 mg/kg PO once daily in combination with corticosteroids... Azathioprine dose is given every other day after 1-2 weeks.	PO	q24h then q48h	Long-term	🌎 NA
Immune-mediated diseases (e.g., IMHA, polyarthritis)	2 mg/kg p.o. q24h for a maximum of 2-3 weeks, then 0.5-2 mg/kg p.o. q48h	PO	q24h initially, then q48h	Max 2-3 weeks for initial q24h dosing, then maintenance	🌍 EU

Inflammatory bowel disease: May take 2-6 weeks before beneficial effects are seen.
Immune-mediated anemia, colitis, immune-mediated skin disease, and acquired myasthenia gravis: With prednisolone administered on the alternate days.
Adjunctive therapy in myasthenia gravis in non-responsive patients: Taper to every other day when clinical remission occurs. Discontinue if WBC <4,000 cells/mcL or neutrophils <1,000 cells/mcL.
Severe cases of immune-mediated hemolytic anemia (IMHA): In addition to prednisone. Tapered gradually.
Acute immune-mediated hemolytic anemia (IMHA) with glucocorticoids: Used for long-term maintenance as steroid side effects become intolerable.
Severe and refractory inflammatory bowel disease: A lag time of 3-5 weeks is expected before clinical improvement is noted.
Perianal fistulas (anal furunculosis): Dose reduced based on clinical response or myelosuppression markers.
Glomerulonephritis: Immunosuppressive treatment is controversial.
Immune-mediated diseases (e.g., IMHA, polyarthritis): Often used in conjunction with corticosteroids. Clinical response may take up to 6 weeks.

고양이

적응증	용량	경로	빈도	기간	지역
Severe and refractory inflammatory bowel disease	0.3 mg/kg PO once every other day	PO	q48h	Long-term	🌎 NA
Immune-mediated diseases	Not recommended	PO	Not recommended	Not recommended	🌍 EU

Severe and refractory inflammatory bowel disease: Must be used with extreme caution due to myelotoxicity. May take 3-5 weeks for beneficial effects.
Immune-mediated diseases: Cats often develop severe, non-responsive fatal leucopenia and thrombocytopenia.

페렛

적응증	용량	경로	빈도	기간	지역
Inflammatory bowel disease	0.9 mg/kg PO q24-72h	PO	q24-72h	Unspecified	🌎 NA

Inflammatory bowel disease: Used alongside prednisone and dietary management.

말

적응증	용량	경로	빈도	기간	지역
Immunosuppressive	3 mg/kg PO q24h	PO	q24h	Unspecified	🌎 NA
Autoimmune skin diseases (e.g., pemphigus foliaceous)	13 mg/kg PO q24h for 1 month, then every other day (q48h)	PO	q24h then q48h	Long-term	🌎 NA

Immunosuppressive: Appears to be a relatively safe immunosuppressive treatment in the horse.
Autoimmune skin diseases (e.g., pemphigus foliaceous): Used as a steroid-sparing drug. May cause thrombocytopenia.

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개요

아자티오프린(Azathioprine)은 수의학에서 주로 개를 대상으로 면역 매개성 용혈성 빈혈(IMHA), 염증성 장질환(IBD), 중증 근무력증, 천포창 등 다양한 면역 매개성 및 자가면역 질환을 치료하는 데 널리 사용되는 강력한 퓨린 길항제 계열의 면역억제제입니다.

핵심 임상 정보:

스테로이드 절약 효과: 코르티코스테로이드(프레드니손 또는 프레드니솔론 등)와 함께 투여되는 경우가 많습니다. 이 병용 요법을 통해 질병의 관해를 유지하면서 스테로이드 용량을 점진적으로 줄일 수 있어 장기적인 스테로이드 부작용을 최소화할 수 있습니다.
지연된 약효 발현: 아자티오프린은 속효성 약물이 아닙니다. 완전한 면역억제 임상 효과를 얻으려면 일반적으로 2~6주가 필요합니다. 따라서 급성으로 생명을 위협하는 자가면역 위기 상황에서 단독 제제로 사용하는 것은 적합하지 않습니다.
종 특이적 민감성: 고양이는 아자티오프린에 매우 민감하여 골수 억제가 쉽게 발생합니다. 이는 고양이가 선천적으로 티오퓨린 메틸트랜스퍼라제(TPMT) 효소 수치가 낮기 때문입니다. 고양이에게 이 약을 사용하는 것은 논란의 여지가 많으며 일반적으로 피해야 합니다.
독성 위험: 가장 심각한 부작용은 골수 억제(백혈구 감소증, 빈혈, 혈소판 감소증)입니다. 개에서는 간 독성과 급성 췌장염도 주의해야 할 위험 요소입니다.

작용 기전

Azathioprine is a prodrug that must be metabolized to exert its effects.

Pathway: Azathioprine is rapidly converted in the body (primarily in erythrocytes and the liver) to 6-mercaptopurine (6-MP).
6-MP is further metabolized into active thioguanine nucleotides (TGNs).
Mechanism: These active metabolites act as purine antagonists. They are falsely incorporated into cellular DNA and RNA, which inhibits purine metabolism, RNA/DNA synthesis, and cellular mitosis.
Immunological Effect: Because lymphocytes (T-cells and B-cells) lack a salvage pathway for purine synthesis and rely heavily on de novo synthesis, they are profoundly affected. This leads to a marked suppression of delayed hypersensitivity and cellular immunity, with a lesser effect on humoral antibody responses.

안전성·주의사항

금기사항

Known hypersensitivity to azathioprine
Cats (generally contraindicated due to severe, potentially fatal myelotoxicity)

부작용

Bone marrow suppression (leukopenia, anemia, thrombocytopenia)
Gastrointestinal distress (vomiting, diarrhea, anorexia)
Acute pancreatitis
Hepatotoxicity
Poor hair growth
Increased susceptibility to secondary infections
Increased risk of neoplastic illnesses with long-term use

주의

Black Box Warning Equivalent: Azathioprine is a known mutagen and teratogen. Pregnant women or those trying to conceive should avoid handling this medication. If handling is necessary, strict use of protective gloves is required.

Hepatic Dysfunction: Use with extreme caution in patients with pre-existing liver disease, as hepatotoxicity is a known adverse effect.
Thiopurine Methyltransferase (TPMT) Deficiency: Dogs have variable TPMT activity (similar to humans). Dogs with low TPMT activity are at a significantly higher risk for severe bone marrow suppression.
Tapering: In recovering patients (e.g., IMHA), withdrawal of the drug must be tapered very slowly over several months. Rapid withdrawal can trigger a rebound hyperimmune response and fatal relapse.
Pregnancy/Nursing: FDA Category D (human). Distributed into milk; use milk replacer if the dam is treated.

약물 상호작용

ACE Inhibitors (e.g., benazepril, enalapril)

Increased potential for hematologic toxicity

AllopurinolMajor

Decreases hepatic metabolism of azathioprine; significantly increases toxicity risk. Dose of azathioprine must be reduced to 1/4 to 1/3 of the usual dose if used concurrently.

Aminosalicylates (e.g., sulfasalazine, mesalamine, olsalazine)

Increased risk for azathioprine toxicity

Non-depolarizing muscle relaxants (e.g., pancuronium, tubocurarine)

Neuromuscular blocking activity may be inhibited or reversed by azathioprine

CorticosteroidsModerate

Often used together intentionally, but carries a greater potential risk for overall toxicity development

Drugs affecting myelopoiesis (e.g., trimethoprim/sulfa, cyclophosphamide)

Increased potential for hematologic toxicity (additive bone marrow suppression)

Warfarin

Potential for reduced anticoagulant effect

AminosalicylatesModerate

Increased risk of azathioprine toxicity.

ACE inhibitorsMajor

May increase the potential for haematological adverse events (e.g., severe anaemia or leucopenia).

모니터링

Hemograms (CBC including platelets): Monitor closely; initially every 1-2 weeks, then every 1-2 months on maintenance therapy. Reduce dose by 25% if WBC drops to 5,000-7,000 cells/mcL. Discontinue if WBC < 5,000 cells/mcL until resolved.
Liver function tests (ALT, AST, ALP, Bilirubin)
Serum amylase/lipase (if pancreatitis is suspected)
Clinical efficacy and signs of secondary infection

약동학

흡수

Poorly absorbed from the gastrointestinal tract.

분포

Rapidly taken up by lymphocytes and erythrocytes. Distributed into milk.

대사

Rapidly metabolized to mercaptopurine (6-MP). Mercaptopurine is further metabolized to several other compounds via pathways including thiopurine methyltransferase (TPMT). Cats have naturally low TPMT activity, making them highly susceptible to toxicity.

배설

Metabolites are excreted primarily by the kidneys. Only minimal amounts of azathioprine or mercaptopurine are excreted unchanged.

과다투여

There is limited specific information regarding acute overdose of azathioprine in veterinary patients.

Decontamination: If ingestion was recent, use standard protocols to empty the GI tract (emesis induction, activated charcoal).
Treatment: Provide aggressive supportive care. Monitor hematologic parameters closely for delayed bone marrow suppression.
Consultation: Contact an animal poison control center for the most up-to-date guidance.

제품

제형

Tablets
Injection (powder for reconstitution)
Compounded oral suspension

인용의약품

Azathioprine Tablets: 50 mg, 75 mg & 100 mg (Azasan®, Imuran®, generic)
Azathioprine Sodium Injection: 100 mg (as sodium)/vial in 20 mL vials (generic)

규제 현황

European Union✓ 승인됨처방전의약품EMA

POM (Prescription Only Medicine). Handled under cascade using human formulations.

United Kingdom✓ 승인됨처방전의약품VMD

POM-V / POM. Handled under the prescribing cascade.

규제 데이터 없음: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

보관·안정성

Tablets should be stored at room temperature in well-closed containers and protected from light. Sodium powder for injection should be stored at room temperature and protected from light; after reconstitution, it must be used within 24 hours as it contains no preservatives. Compounded oral suspensions have optimal stability between pH 5.5 and 6.5 and should be protected from light.

보호자 정보

반려동물 보호자를 위한 중요 안내:

인내심이 필요합니다: 이 약은 효과가 나타나기까지 시간이 걸립니다. 반려동물의 상태가 호전되는 것을 보려면 수 주가 걸릴 수 있습니다. 수의사와 상의 없이 임의로 투약을 중단하지 마십시오.
안전 및 취급 주의: 아자티오프린은 사람의 DNA에 영향을 줄 수 있는 강력한 약물입니다. 알약을 만진 후에는 반드시 손을 깨끗이 씻으십시오. 임신 중이거나 임신을 계획 중이거나 수유 중인 경우 이 약을 만지지 마십시오. 부득이하게 만져야 할 경우 반드시 보호 장갑을 착용하십시오.
부작용 관찰: 이 약은 면역 체계를 억제하고 골수에 영향을 줄 수 있으므로 반려동물이 감염되거나 출혈이 발생할 위험이 높아집니다.
수의사에게 연락해야 할 때: 반려동물에게 비정상적인 출혈, 원인 모를 멍, 창백한 잇몸, 발열, 식욕 부진, 구토, 설사 또는 무기력증 등의 증상이 나타나면 즉시 수의사에게 연락하십시오.
철저한 모니터링: 약물이 골수나 간을 손상시키지 않는지 확인하기 위해 반려동물은 (특히 처음 몇 달 동안) 자주 혈액 검사를 받아야 합니다. 예약된 재진 일정을 반드시 지켜주십시오.

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