of infection. Modify Therapy/Monitor Closely. Owing to potential additive immunosuppressive effects, consider duration of effect and mechanism of action of these therapies if coadministeredupadacitinibContraindicated (1)azathioprine, upadacitinib. Either increases effects of the other by immunosuppressive effects; risk of infection. Contraindicated.ustekinumabSerious - Use Alternative (1)azathioprine and ustekinumab both increase immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.valoctocogene roxaparvovecMonitor Closely (1)azathioprine and valoctocogene roxaparvovec both increase Other (see comment). Use Caution/Monitor. Medications that may cause hepatotoxicity when combined with valoctogene roxaparvovec may potentiate the risk of elevated liver enzymes. Closely monitor these medications and consider alternative medications in case of potential drug interactions.varicella virus vaccine liveSerious - Use Alternative (1)azathioprine decreases effects of varicella virus vaccine live by pharmacodynamic antagonism. Contraindicated. Immunosuppressants also increase risk of infection with concomitant live vaccines.warfarinMonitor Closely (1)azathioprine decreases effects of warfarin by unspecified interaction mechanism. Use Caution/Monitor.yellow fever vaccineSerious - Use Alternative (1)azathioprine decreases effects of yellow fever vaccine by pharmacodynamic antagonism. Contraindicated. Immunosuppressants also increase risk of infection with concomitant live vaccines.zidovudineMonitor Closely (1)azathioprine, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.zoster vaccine liveSerious - Use Alternative (1)azathioprine decreases effects of zoster vaccine live by pharmacodynamic antagonism. Contraindicated. Immunosuppressants also increase risk of infection with concomitant live vaccines.zoster vaccine recombinantMonitor Closely (1)azathioprine decreases effects of zoster vaccine recombinant by pharmacodynamic antagonism. Use Caution/Monitor. Immunosuppressive therapies may reduce the effectiveness of zoster vaccine recombinant. >10% Leukopenia (28-50%) Infection (20%) <1% Lymphoma Frequency Not Defined Abdominal pain Alopecia Arthralgia Bacterial, fungal, protozoal, viral infections Bone marrow suppression Diarrhea Fever Hepatotoxicity Macrocytic anemia Myalgia Nausea or vomiting Rash Skin cancer Steatorrhea Sweet syndrome (acute febrile neutrophilic dermatosis) Thrombocytopenia Black Box Warnings Chronic immunosuppression with this purine antimetabolite increases neoplasia risk, mutagenic risk, and hematologic toxicities Reported malignancies include posttransplant lymphoma and hepatosplenic T-cell lymphoma (HSTCL) in patients with inflammatory bowel disease Prescribing physicians should be familiar with mutagenic potential and with possible hematologic toxicitiesContraindications Documented hypersensitivity Pregnancy, lactation Rheumatoid arthritis: Patients previously treated with alkylating agents Cautions Long-term use increases risk of neoplasia Increased risk of infection and hepatotoxicity; monitor liver function periodically; hepatic sinudoidal obstruction syndrome reported; discontinue therapy if suspected Cases of JC virus-associated infection resulting in progressive multifocal leukoencephalopathy (PML), sometimes fatal, reported in patients treated with immunosuppressants, including azathioprine Severe leukopenia, thrombocytopenia, anemias including macrocytic anemia, and/or pancytopenia may occur; severe bone marrow suppression may also occur; patients with or nucleotide diphosphatase (NUDT15) deficiency may be at an increased risk of myelotoxicity if patient receiving conventional doses of drug; delayed hematologic suppression may occur; prompt reduction in dosage or temporary withdrawal of drug may be necessary if there is rapid fall in or persistently low leukocyte count, or other evidence of bone marrow depression; leukopenia does not correlate with therapeutic effect; therefore dose should not be increased intentionally to lower white blood cell count In patients with severe myelosuppression, consider evaluation for TPMT and NUDT15 deficiency; consider alternative therapy in patients with homozygous TPMT or NUDT15 deficiency and reduced dosages in patients with heterozygous deficiency Patients receiving immunosuppressants, are at increased risk for bacterial, viral, fungal,protozoal, and opportunistic infections, including reactivation of latent infections; these infections may lead to serious, including fatal outcomes Frequency of gastrointestinal adverse effects (nausea and vomiting) may decrease with dividing dose or administering after meals Hepatosplenic T-cell lymphoma Rare postmarketing cases of HSTCL reported primarily in adolescent and young adult patients with Crohn disease and ulcerative colitis treated with tumor necrosis factor (TNF) blockers Reports have also included 1 patient being treated for psoriasis and 2 patients being treated for rheumatoid arthritis HSTCL is an aggressive, rare type of T-cell lymphoma that is usually fatal Most reported cases with TNF blockers have occurred in context of concomitant treatment with azathioprine or 6-mercaptopurine (6-MP), though cases have been reported with azathioprine or 6-MP alone In the FDA Adverse Event Reporting System (AERS) database, the literature, and the HSTCL Cancer Survivors' Network, HSTCL cases have been identified in association with the following drugs: infliximab (20), etanercept (1), adalimumab (2), infliximab/adalimumab (5), certolizumab (0), golimumab (0), azathioprine (12), 6-MP (3) Pregnancy category: D Lactation: Drug excreted at low levels in breast milk; use not recommendedPregnancy Categories A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk. B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available. Mechanism of Action Purine antimetabolite, converted to 6-MP; may inhibit synthesis of DNA, RNA, and proteins; interferes with cellular metabolism; may inhibit mitosis Absorption Well absorbed orally Duration: Variable (crosses placenta) Peak plasma time: PO, 1-2 hr Peak plasma concentration: <1 mcg/mL Distribution Protein bound: 30% Metabolism Metabolized in liver Metabolites: 6-MP, 6-thiouric acid Elimination Half-life: Parent drug, 12 min; 6-MP, 0.7-3 hr; slightly prolonged in end-stage renal disease Dialyzable: Partially Excretion: Urine (primarily as metabolites) Oral suspension of 50 mg/mL requires extemporaneous compounding by pharmacist IV Incompatibilities Stable in neutral or acid solutions; in alkaline solutions, hydrolyzed to 6-MP IV Administration Can be administered by IV push over 5 minutes at concentration not exceeding 10 mg/mL Can be further diluted with NS or D5W and administered by intermittent infusion over 30-60 minutes (usual approach); however, infusions over periods ranging from 5 minutes to 8 hours have been done Storage Store powder at room temperature (25°C); reconstituted solution is stable for 2 weeks at room temperature but may be less stable under refrigeration Protect from light Because there are no preservatives, drug must be used within 24 hours BRAND FORM. UNIT PRICE PILL IMAGE azathioprine oral- 50 mg tabletazathioprine oral- 50 mg tabletazathioprine oral- 75 mg tabletazathioprine oral- 50 mg tabletazathioprine oral- 50 mg tabletazathioprine oral- 100 mg tabletazathioprine oral- 100 mg tabletazathioprine oral- 50 mg tabletazathioprine oral- 75 mg tabletImuran oral- 50 mg tabletAzasan oral- 100 mg tabletAzasan oral- 75 mg tabletCopyright © 2010 First DataBank, Inc.Print Patient Educationazathioprine oral AZATHIOPRINE - ORAL (AY-za-THYE-oh-preen) COMMON BRAND NAME(S): Imuran WARNING: Azathioprine may rarely increase your risk of developing certain types of cancer (such as lymphoma, skin cancer). This risk is higher in people using azathioprine after an organ transplant and in children/young adults being treated for certain bowel diseases (such as Crohn's disease, ulcerative colitis). Keep all medical and lab appointments. Tell your doctor right away if you develop any of the following symptoms: unusual skin changes, change in the appearance/size of moles, unusual growths/lumps, swollen lymph nodes, swollen abdomen, unexplained weight loss, night sweats.This medication may decrease bone marrow function, an effect that may lead to a low number of blood cells such as red cells, white cells, and platelets. This effect can cause anemia, decrease your body's ability to fight an infection, or cause easy bruising/bleeding. Tell your doctor right away if you develop any of the following symptoms: unusual tiredness, pale skin, signs of infection (such as sore throat that doesn't go away, fever, chills), easy bruising/bleeding. USES: Azathioprine is used to prevent organ rejection in people who have received a kidney transplant. It is usually taken along with other medications to allow your new kidney to function normally. Azathioprine is also used to treat rheumatoid arthritis. In this condition, the body's defense system (immune system) attacks healthy joints. Azathioprine belongs to a class of drugs known as immunosuppressants. It works by weakening the immune system to help your body accept the new kidney as if it were your own (in the case of an organ transplant) or to prevent further damage to your joints (in the case of rheumatoid arthritis).Talk to your doctor about the risks and benefits of azathioprine, especially when used by children and young adults. HOW TO USE: Take this medication by mouth as directed by your doctor, usually once or twice daily. Take this medication with food to reduce stomach upset.The dosage is based on your medical condition, weight, and response to treatment. Do not increase your dose or use this drug more often or for longer than prescribed. Your condition will not improve any faster, and your risk of serious side effects will increase.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time(s) each day.For the treatment of arthritis, it may take up to 2 months before your symptoms get better. Tell your doctor if your condition does not get better after 3 months of treatment.Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets. SIDE EFFECTS: See also Warning section.Nausea or vomiting may occur. Taking this medication after meals may help lessen these effects. Temporary hair loss may also occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.People using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.Tell your doctor right away if you have any serious side effects, including: diarrhea, new or worsening joint/muscle pain.Get medical help right away if you have any very serious side effects, including: symptoms of liver disease (such as nausea/vomiting that doesn't stop, stomach/abdominal pain, dark urine, yellowing eyes/skin).This medication may increase your risk of getting a rare but very serious (possibly fatal) brain infection (progressive multifocal leukoencephalopathy-PML). Get medical help right away if you have any of these side effects: clumsiness, loss of coordination/balance, weakness, sudden change in your thinking (such as confusion, difficulty concentrating, memory loss), difficulty talking/walking, seizure, vision changes.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345. PRECAUTIONS: Before taking azathioprine, tell your doctor or pharmacist if you are allergic to it, or to mercaptopurine; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease, liver disease, cancer, certain enzyme disorders (TPMT deficiency, NUDT15 deficiency).This medication may increase your risk of developing skin cancer. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors. Your doctor may direct you to avoid phototherapy while you use this product. Ask your doctor for details.Azathioprine can make you more likely to get infections or may make current infections worse. Stay away from anyone who has an infection that may easily spread (such as chickenpox, COVID-19, measles, flu). Talk to your doctor if you have been exposed to an infection or for more details.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Tell your health care professional that you are using azathioprine before having any immunizations/vaccinations. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.Since this drug can be absorbed through the skin and lungs and may