Also found in: Dictionary, Thesaurus, Encyclopedia, Wikipedia.


Apo-Azathioprine (CA), Azasan, Gen-Azathioprine (CA), Immunoprin (UK), Imuran, Novo-Azathioprine (CA)

Pharmacologic class: Purine antagonist

Therapeutic class: Immunosuppressant

Pregnancy risk category D

FDA Box Warning

• Drug may cause chronic immunosuppression, increasing neoplasia risk. Physicians using it should be familiar with this risk and with possible hematologic toxicities and mutagenic potential in both sexes.


Prevents proliferation and differentiation of activated B and T cells by interfering with synthesis of purine, DNA, and RNA


Injection: 100-mg vial

Tablets: 50 mg, 75 mg, 100 mg

Indications and dosages

To prevent rejection of kidney transplant

Adults and children: Initially, 3 to 5 mg/kg/day P.O. or I.V. as a single dose. Give on day of transplantation or 1 to 3 days before day of transplantation; then 3 to 5 mg/kg/day I.V. after surgery until patient can tolerate P.O. route. Maintenance dosage is 1 to 3 mg/kg/day P.O.

Rheumatoid arthritis

Adults and children: Initially, 1 mg/kg P.O. or I.V. in one or two daily doses. Increase dosage in steps at 6 to 8 weeks and thereafter at 4-week intervals; use dosage increments of 0.5 mg/kg/day, to a maximum dosage of 2.5 mg/kg/day. Once patient stabilizes, decrease in decrements of 0.5 mg/kg/day to lowest effective dosage.

Dosage adjustment

• Renal disease

• Concurrent allopurinol therapy

• Elderly patients

Off-label uses

• Crohn's disease

• Myasthenia gravis

• Chronic ulcerative colitis


• Hypersensitivity to drug

• Pregnancy or breastfeeding


Use cautiously in:

• chickenpox, herpes zoster, impaired hepatic or renal function, decreased bone marrow reserve

• previous therapy with alkylating agents (cyclophosphamide, chlorambucil, melphalan) for rheumatoid arthritis

• elderly patients

• women of childbearing age.


• Give after meals.

• Be aware that I.V. administration is intended for use only when patients can't tolerate oral medications.

Adverse reactions

CNS: malaise

EENT: retinopathy

GI: nausea, vomiting, diarrhea, stomatitis, esophagitis, anorexia, mucositis, pancreatitis

Hematologic: anemia, thrombocytopenia, leukopenia, pancytopenia

Hepatic: jaundice, hepatotoxicity

Musculoskeletal: muscle wasting, joint and muscle pain

Skin: rash, alopecia

Other: chills, fever, serum sickness, neoplasms, serious infection


Drug-drug. Allopurinol: increased therapeutic and adverse effects of azathioprine

Angiotensin-converting enzyme (ACE) inhibitors, co-trimoxazole: severe leukopenia

Anticoagulants, cyclosporine: decreased actions of these drugs

Atracurium, pancuronium, tubocurarine, vecuronium: reversal of these drugs' actions

Drugs affecting bone marrow and bone marrow cells (such as ACE inhibitors, co-trimoxazole): severe leukopenia

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, amylase, aspartate aminotransferase, bilirubin: increased levels

Albumin, hemoglobin, uric acid: decreased levels

Urine uric acid: decreased level

Drug-herbs. Astragalus, echinacea, melatonin: interference with immunosuppressant action

Patient monitoring

Monitor CBC, platelet level, and liver function test results.

• Assess for signs and symptoms of hepatotoxicity (clay-colored stools, pruritus, jaundice, and dark urine).

• Watch for signs and symptoms of infection.

• Monitor for bleeding tendency and hemorrhage.

Patient teaching

Tell patient that drug lowers resistance to infection. Instruct him to immediately report fever, cough, breathing problems, chills, and other symptoms.

Instruct patient to immediately report unusual bleeding or bruising.

• Tell patient that drug effects may not be obvious for up to 8 weeks in immunosuppression and up to 12 weeks for rheumatoid arthritis relief.

Emphasize importance of avoiding pregnancy during therapy and for 4 months afterward.

• Caution patient to avoid activities that may cause injury. Tell him to use soft toothbrush and electric razor to avoid gum and skin injury.

• Advise patient to minimize GI upset by eating small, frequent servings of food and drinking plenty of fluids.

• Tell patient he'll undergo regular blood testing during therapy.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.


A trademark for the drug azathioprine.


a trademark for an immunosuppressive (azathioprine).


A thiolated purine analogue/immunosuppressant used to prevent rejection of heart, kidney, lung and other allografts, acting primarily on T cells; it is used in rheumatoid arthritis and myasthenia gravis.

Adverse effects
Dose-related marrow suppression—leukopaenia, thrombocytopaenia, macrocytic anaemia); GI tract—nausea, vomiting, diarrhoea, fever, malaise, myalgia, liver enzyme defects, hepatotoxicity, pancreatitis. Azathiprineshould not be given with allopurinol.

Azathioprine is 6-mercaptopurine with a side chain to protect the labile sulfhydryl group, which is split off in the liver; full metabolic activity follows addition of ribose 5-phosphate from phosphoribosyl pyrophosphate that is metabolised to the cytotoxic derivative 6-mercaptopurine.


Azathioprine, see there.


A brand name for AZOTHIAPRINE.
References in periodicals archive ?
Currently available in over 100 countries worldwide, Imuran is indicated for the treatment of organ rejection in transplants.
Imuran researchers evaluated 160 patients from 8 countries who had been treated up to 12 years previously with pig skin grafts for severe burns, pig pancreatic islet cells for diabetes, or who had their blood perfused outside the body (extracorporeal perfusion) through pig spleens, kidneys, or livers.
Azathioprine tablets USP, 75 aaiPharma Imuran tablets
Azathioprine is marketed by Glaxo Wellcome as Imuran and by Roxane Laboratories as a generic.
Today I am taking the immunosuppressant drug Imuran, and I'm on a very rigid exercise program.
s Imuran, an immunosuppressive antimetabolite, and is indicated as an adjunct for preventing rejection in renal homotransplantation.
trial are switched to Imuran (azathioprine), a lesser immunosuppressive, Dr.
Among suggested treatments are Accutane, thalidomide, methotrexate, Imuran, Plaqueil, gold and intralesional Kenalog.
Allopurinol is contraindicated in patients taking Imuran, as both medications cause a decrease in WBC.
Side effects include an increased risk of infection with Imuran, and nausea and vomiting with Purinethol.
Immunosuppression consisted of Imuran [R], prednisone, cyclosporine, and antithymocyte globulin.