Azathioprine: MedlinePlus Drug Information (2022)

pronounced as (ay za thye' oh preen)

  • Why is this medication prescribed?
  • How should this medicine be used?
  • Other uses for this medicine
  • What special precautions should I follow?
  • What special dietary instructions should I follow?
  • What should I do if I forget a dose?
  • What side effects can this medication cause?
  • What should I know about storage and disposal of this medication?
  • In case of emergency/overdose
  • What other information should I know?
  • Brand names

Azathioprine may increase your risk of developing certain types of cancer, especially skin cancer and lymphoma (cancer that begins in the cells that fight infection). If you have had a kidney transplant, there may be a higher risk that you will develop cancer even if you do not take azathioprine. Tell your doctor if you have or have ever had cancer and if you are taking or have ever taken alkylating agents such as chlorambucil (Leukeran), cyclophosphamide (Cytoxan), or melphalan (Alkeran) for cancer. To decrease the risk that you will develop skin cancer, avoid prolonged or unnecessary exposure to sunlight and wear protective clothing, sunglasses, and sunscreen. Tell your doctor immediately if you notice any changes in your skin or any lumps or masses anywhere in your body.

Some teenage and young adult males who took azathioprine alone or with another medication called a tumor necrosis factor (TNF) blocker to treat Crohn's disease (a condition in which the body attacks the lining of the digestive tract causing pain, diarrhea, weight loss, and fever) or ulcerative colitis (a condition which causes swelling and sores in the lining of the colon [large intestine] and rectum) developed hepatosplenic T-cell lymphoma (HSTCL). HSTCL is a very serious type of cancer that often causes death within a short period of time. Azathioprine has not been approved by the Food and Drug Administration (FDA) for the treatment of Crohn's disease or ulcerative colitis, but doctors may sometimes prescribe azathioprine to treat these conditions. If you develop any of these symptoms during your treatment, call your doctor immediately: stomach pain; fever; unexplained weight loss; night sweats or easy bruising or bleeding.

Azathioprine can cause a decrease in the number of blood cells in your bone marrow, which may cause serious or life-threatening infections. The risk that the number of blood cells that you have will decrease is highest if you have a genetic (inherited) risk factor. Your doctor may order a test before or during your treatment to see if you have this risk factor. Taking certain medications may also increase the risk that your blood cells will decrease, so tell your doctor if you are taking any of the following: angiotensin converting enzyme (ACE) inhibitors such as benazepril (Lotensin), captopril, enalapril (Vasotec), fosinopril, lisinopril (Prinivil, Zestril), moexipril (Univasc), perindopril (Aceon), quinapril (Accupril), Ramipril (Altace), or trandolapril (Mavik); trimethoprim and sulfamethoxazole (Bactrim, Septra); and ribavirin (Copegus, Rebetol, Virazole). If you experience any of the following symptoms, call your doctor immediately: unusual bleeding or bruising; excessive tiredness; pale skin; headache; confusion; dizziness; fast heartbeat; difficulty sleeping; weakness; shortness of breath; and sore throat, fever, chills, and other signs of infection. Your doctor will order tests before, during, and after your treatment to see if your blood cells are affected by this medication.

Talk to your doctor about the risks of taking this medication.

(Video) Azathioprine - Pharmacology, mechanism of action, side effects,

Azathioprine is used with other medications to prevent transplant rejection (attack of the transplanted organ by the immune system) in people who received kidney transplants. It is also used to treat severe rheumatoid arthritis (a condition in which the body attacks its own joints, causing pain, swelling, and loss of function) when other medications and treatments have not helped. Azathioprine is in a class of medications called immunosuppressants. It works by decreasing the activity of the body's immune system so it will not attack the transplanted organ or the joints.

Azathioprine comes as a tablet to take by mouth. It is usually taken once or twice a day after meals. Take azathioprine at around the same time(s) every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take azathioprine exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

If you are taking azathioprine to treat rheumatoid arthritis, your doctor may start you on a low dose and gradually increase your dose after 6-8 weeks and then not more than once every 4 weeks. Your doctor may gradually decrease your dose when your condition is controlled. If you are taking azathioprine to prevent kidney transplant rejection, your doctor may start you on a high dose and decrease your dose gradually as your body adjusts to the transplant.

Azathioprine controls rheumatoid arthritis but does not cure it. It may take up to 12 weeks before you feel the full benefit of azathioprine. Azathioprine prevents transplant rejection only as long as you are taking the medication. Continue to take azathioprine even if you feel well. Do not stop taking azathioprine without talking to your doctor.

Azathioprine is also used to treat ulcerative colitis (a condition which causes swelling and sores in the lining of the colon [large intestine] and rectum) and Crohn's disease. Talk to your doctor about the possible risks of using this medication for your condition.

This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

(Video) Spotlight on Testing: Therapeutic drug monitoring (TDM) of thiopurine drugs

Before taking azathioprine,

  • tell your doctor and pharmacist if you are allergic to azathioprine, any other medications, or any of the ingredients in azathioprine tablets. Ask your doctor or pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention the medications mentioned in the IMPORTANT WARNING section and any of the following: allopurinol (Zyloprim); aminosalicylates such as mesalamine (Apriso, Asacol, Pentasa, others), olsalazine (Dipentum), and sulfasalazine (Azulfidine); and anticoagulants ('blood thinners') such as warfarin (Coumadin). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor if you have any type of infection, or if you have or have ever had kidney disease.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. You should use birth control to be sure you or your partner will not become pregnant while you are taking this medication. Call your doctor if you or your partner become pregnant while you are taking azathioprine. Azathioprine may harm the fetus.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking azathioprine.
  • do not have any vaccinations during or after your treatment without talking to your doctor.

Unless your doctor tells you otherwise, continue your normal diet.

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

Azathioprine may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • nausea
  • vomiting
  • diarrhea

Some side effects can be serious. If you experience any of the following symptoms or those listed in the IMPORTANT WARNING section, call your doctor immediately.

  • rash
  • fever
  • weakness
  • muscle pain

This medication may cause other side effects. Call your doctor if you have any unusual problems while you are taking azathioprine.

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

(Video) The Genetics of Thiopurine Response

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom).

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA's Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services at 911.

Symptoms of overdose may include the following:

  • nausea
  • vomiting
  • diarrhea
  • sore throat, fever, chills, and other signs of infection
(Video) Mercaptopurine and Allopurinol drug interaction

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

Last Revised - 04/15/2019

Browse Drugs and Medicines

(Video) Imuran (Azathioprine)

FAQs

What drug class is azathioprine? ›

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).

What should I avoid while taking azathioprine? ›

Wear protective clothing and hats, and stay out of direct sunlight between the hours of 10 am and 3 pm Avoid sunlamps and tanning beds. While you are being treated with azathioprine, and after you stop treatment with it, do not have any immunizations (vaccines) without your doctor's approval.

What should be monitored while taking azathioprine? ›

Taking azathioprine can sometimes affect your liver, kidneys or bone marrow. You will have blood tests to check your liver function, kidney function and blood count before you start taking this medicine.

What are the side effects of taking azathioprine? ›

Rare
  • Bloating.
  • decreased appetite.
  • diarrhea (severe)
  • fever (sudden)
  • headache.
  • muscle or joint pain.
  • nausea (severe)
  • pains in the stomach, side, or abdomen, possibly radiating to the back.
1 Apr 2022

What is the drug azathioprine used for? ›

Azathioprine is used with other medications to prevent transplant rejection (attack of the transplanted organ by the immune system) in people who received kidney transplants.

What is the mechanism of action of azathioprine? ›

Mechanism of action

Azathioprine inhibits purine synthesis. Purines are needed to produce DNA and RNA. By inhibiting purine synthesis, less DNA and RNA are produced for the synthesis of white blood cells, thus causing immunosuppression.

Why is azathioprine taken at night? ›

Do not stop using this medicine without first checking with your doctor. Azathioprine sometimes causes nausea or vomiting. Taking this medicine after meals, in divided doses, or at bedtime may lessen stomach upset.

Can I take vitamin D with azathioprine? ›

No interactions were found between azathioprine and Vitamin D3. However, this does not necessarily mean no interactions exist. Always consult your healthcare provider.

When is the best time to take azathioprine? ›

Azathioprine is best taken on an empty stomach, at least 1 hour before or 3 hours after food or milk. Swallow your tablets whole with a drink of water. Do not break, chew or crush the tablets. Missed dose: If you forget to take your azathioprine dose, take it as soon as you remember.

How long can you stay on azathioprine? ›

How long will I be taking it? If tolerated, you will probably be on azathioprine for up to 5 years. Do not stop taking your medicine unless your doctor tells you to, even if you feel well.

How toxic is azathioprine? ›

Conclusions: From this study, it was estimated at 6% the risk of toxicity by the administration of azathioprine and 6-mercaptopurine to patients in Joinville.

How safe is azathioprine? ›

About side effects, azathioprine is a relatively well tolerated drug and even indefinite use seems safe. The main theoretical risks of prolonged use would be the myelotoxicity, hepatotoxicity, and the development of cancer.

Which is stronger azathioprine or methotrexate? ›

These results demonstrate MTX to be superior to AZA in the treatment of rheumatoid arthritis, with a more rapid clinical improvement which is sustained after 1 year, accompanied by a lower rate of serious adverse reactions.

Is azathioprine an anti inflammatory? ›

Azathioprine is an anti-inflammatory medicine used to treat rheumatoid arthritis and other inflammatory conditions. It works by suppressing the blood cells that cause inflammation.

Is azathioprine a cytotoxic drug? ›

Cyclophosphamide, azathioprine, chlorambucil, and methotrexate are cytotoxic drugs used most commonly for the purpose of immunosuppression.

How do you start azathioprine? ›

Azathioprine is usually given as tablets, taken once or twice daily. They should be swallowed whole and taken with or after food. Your doctor will advise you about the correct dose, which will depend on how much you weigh. But you'll usually start on a low dose of about 50mg, your doctor may increase this if necessary.

Does azathioprine make you sleepy? ›

Azathioprine oral tablet doesn't cause drowsiness, but it can cause other side effects.

Can you take omeprazole with azathioprine? ›

Interactions between your drugs

No interactions were found between Imuran and omeprazole. However, this does not necessarily mean no interactions exist. Always consult your healthcare provider.

What is azathioprine FDA approved for? ›

IMURAN is indicated as an adjunct for the prevention of rejection in renal homotransplantation. It is also indicated for the management of active rheumatoid arthritis to reduce signs and symptoms.

Why is azathioprine cytotoxic? ›

The cytotoxicity of azathioprine is due, in part, to the incorporation of 6-TGN into DNA. 6-MP undergoes two major inactivation routes (Figure 1). One is thiol methylation, which is catalyzed by the enzyme thiopurine S-methyltransferase (TPMT), to form the inactive metabolite methyl-6-MP (6-MeMP).

Which of the following is the most expected side effect of azathioprine? ›

Nausea, vomiting, or diarrhea. Flu-like symptoms (chills, aches, headache, or fatigue).

Can you drink milk with azathioprine? ›

Azathioprine may be taken with food or on an empty stomach, but patients should standardise the method of administration. The dose should not be taken with milk or dairy products (see Section 4.2).

Can I take paracetamol with azathioprine? ›

No interactions were found between azathioprine and Pharmacist Paracetamol.

Can you take azathioprine and prednisone together? ›

Interactions between your drugs

No interactions were found between azathioprine and prednisone.

Is azithromycin and azathioprine the same? ›

Azithromycin is a macrolide antibiotic indicated for Community Acquired Pneumonia (CAP) and Pelvic Inflammatory Disease (PID). Azathioprine is an immunosuppressive and antineoplastic agent used to prevent transplant rejection and for other conditions such as Crohn's disease and rheumatoid arthritis.

Can azathioprine cause liver damage? ›

Azathioprine, like other thiopurines, can also cause chronic liver injury and long term therapy has been linked to the development of portal hypertension and nodular regenerative hyperplasia.

Is Imuran a high risk medication? ›

Imuran may cause a rare type of lymphoma (cancer) of the liver, spleen, and bone marrow that can be fatal. This has occurred mainly in teenagers and young men with Crohn's disease or ulcerative colitis. However, anyone with an inflammatory autoimmune disorder may have a higher risk of lymphoma.

Why does azathioprine cause hair loss? ›

Azathioprine inhibits mitosis of hair matrix resulting in abrupt onset of loss of anagen hair resulting rapid onset and progression of alopecia.

Is azathioprine used to treat myasthenia gravis? ›

Drugs that suppress the immune system are used in people with myasthenia gravis (MG) because MG is an autoimmune disorder that results from production of abnormal antibodies. Azathioprine has been used as a treatment for MG since 1967.

How effective is azathioprine? ›

Overall remission rates (including all patients treated with azathioprine) were 45% and 58% for Crohn's disease and ulcerative colitis, respectively.

What is the brand name for azathioprine? ›

Azathioprine is an immunosuppressive antimetabolite that lowers the body's immune system used to prevent the body from rejecting a transplanted kidney. Azathioprine is also used to treat symptoms of rheumatoid arthritis. Azathioprine is available under the following different brand names: Azasan, and Imuran.

What is azathioprine 50mg? ›

Azathioprine is an antimetabolite which is used as an immunosuppressant, either as monotherapy or more often in combination with other drugs (mainly corticosteroids) and procedures which modulate the immune response. Therapeutic effect may be apparent only after weeks or months.

Does azathioprine make you gain weight? ›

No, Imuran (azathioprine) itself is not causing your weight gain. Perhaps the drug is sufficiently controlling the disease to allow for more complete food absorption. If you're concerned about your weight, note that most weight reduction diets are well-tolerated in Crohn's disease patients.

Is Imuran the same as methotrexate? ›

Methotrexate is most often used for rheumatoid arthritis, while Imuran is used extensively in patients with kidney transplants. Both are well tolerated. Side effects are similar. Both can affect the liver and blood counts and must be monitored with regular bloodwork.

Can you take methotrexate and azathioprine together? ›

Thus, combination therapy with azathioprine and methotrexate is a safe and effective long-term therapy for difficult to treat patients. The combination therapy has no additional severe toxicities.

How azathioprine inhibit purine synthesis? ›

Azathioprine inhibits DNA and RNA synthesis by preventing interconversion among the precursors of purine synthesis and suppressing de novo purine synthesis.

What drugs interact with azathioprine? ›

View interaction reports for azathioprine and the medicines listed below.
  • Aspirin Low Strength (aspirin)
  • Aspirin Low Strength (aspirin)
  • Calcium 600 D (calcium / vitamin d)
  • Calcium 600 D (calcium / vitamin d)
  • Cymbalta (duloxetine)
  • Cymbalta (duloxetine)
  • Fish Oil (omega-3 polyunsaturated fatty acids)

Is there an alternative to azathioprine? ›

Azathioprine (AZA) is usually used for this purpose but must be withdrawn in up to 10% of patients because of adverse events. Mycophenolate mofetil (MMF) is of proven efficacy and safety in transplantation and in some autoimmune disorders.

How does azathioprine cause bone marrow suppression? ›

The drug inhibits both DNA and RNA synthesis and recent studies indicate that the immunosuppressive action of this drug results predominantly from a block in the production of interleukin-2 [1,2]. Bone marrow suppression due to this drug is reported in 14-35% patients [3].

Do I need to take folic acid with Imuran? ›

Interactions between your drugs

No interactions were found between folic acid and Imuran.

What are azathioprine and cyclophosphamide? ›

Azathioprine is a cell-specific drug[18,19] and affects the T helper and CD4 naïve cells[18,19] and affects both the cell-mediated and humoral immunity. [18,19,20] Cyclophosphamide suppresses all the proliferating lymphoid cells and alkylates some resting cells.

Can azathioprine be cut in half? ›

You should take azathioprine with or immediately after food to help reduce stomach upsets. The tablets should not be cut in half as this can create amounts of dust that could cause side effects to your and those around you. Never take more than the dose prescribed by your doctor.

What should I avoid while taking azathioprine? ›

Wear protective clothing and hats, and stay out of direct sunlight between the hours of 10 am and 3 pm Avoid sunlamps and tanning beds. While you are being treated with azathioprine, and after you stop treatment with it, do not have any immunizations (vaccines) without your doctor's approval.

What are the contraindications of azathioprine? ›

Contraindications
  • Hypersensitivity.
  • Pregnancy or plan for pregnancy: Contraception recommended. ...
  • Breastfeeding as 6-MP was present in breast-milk of women who take azathioprine.
  • Unknown TPMT status or deficient TPMT activity due to the high risk of myelosuppression.
  • Known malignancy.
  • Clinically active infection.
8 May 2022

How does azathioprine work in Crohn's disease? ›

It helps to reduce irritation and swelling (inflammation) in the intestines. It also decreases the long-term need for steroids. For that reason, it is sometimes referred to as a "steroid-sparing" drug. In some cases, this medication is used by itself.

What is the drug azathioprine used for? ›

Azathioprine is used with other medications to prevent transplant rejection (attack of the transplanted organ by the immune system) in people who received kidney transplants.

What class of drugs is azathioprine? ›

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).

What is the mechanism of action of azathioprine? ›

Mechanism of action

Azathioprine inhibits purine synthesis. Purines are needed to produce DNA and RNA. By inhibiting purine synthesis, less DNA and RNA are produced for the synthesis of white blood cells, thus causing immunosuppression.

What type of immunosuppressant is azathioprine? ›

Azathioprine, sometimes known by other names such as Imuran or Azapress, is a disease-modifying anti-rheumatic drug (DMARD). It works by reducing the activity of the body's immune system, which may be overactive in some conditions.

Is azathioprine a cyclosporine? ›

Imuran (Azathioprine)

Neoral (cyclosporine) is good at preventing rejection of a transplanted organ, and is also used for treating rheumatoid arthritis and psoriasis.

Is azathioprine at cell inhibitor? ›

Azathioprine is also a potent inhibitor of mixed lymphocyte culture responses and can readily suppress the in vitro generation of cytotoxic T cells.

Is azathioprine a Thiopurine? ›

The thiopurines (ie, azathioprine [AZA] and mercaptopurine, also known as 6-mercaptopurine [6-MP]) exert a glucocorticoid-sparing effect for patients with inflammatory bowel disease (IBD) who cannot maintain remission when glucocorticoids are tapered or withdrawn.

When is the best time to take azathioprine? ›

Azathioprine is best taken on an empty stomach, at least 1 hour before or 3 hours after food or milk. Swallow your tablets whole with a drink of water. Do not break, chew or crush the tablets. Missed dose: If you forget to take your azathioprine dose, take it as soon as you remember.

How long can you stay on azathioprine? ›

How long will I be taking it? If tolerated, you will probably be on azathioprine for up to 5 years. Do not stop taking your medicine unless your doctor tells you to, even if you feel well.

How toxic is azathioprine? ›

Conclusions: From this study, it was estimated at 6% the risk of toxicity by the administration of azathioprine and 6-mercaptopurine to patients in Joinville.

What drugs interact with azathioprine? ›

View interaction reports for azathioprine and the medicines listed below.
  • Aspirin Low Strength (aspirin)
  • Aspirin Low Strength (aspirin)
  • Calcium 600 D (calcium / vitamin d)
  • Calcium 600 D (calcium / vitamin d)
  • Cymbalta (duloxetine)
  • Cymbalta (duloxetine)
  • Fish Oil (omega-3 polyunsaturated fatty acids)

Can you take omeprazole with azathioprine? ›

Interactions between your drugs

No interactions were found between Imuran and omeprazole. However, this does not necessarily mean no interactions exist. Always consult your healthcare provider.

Can you eat grapefruit with azathioprine? ›

Drug and food interactions

Grapefruit and grapefruit juice can increase the levels of cycloSPORINE in your body and should generally not be consumed during treatment.

Which is stronger azathioprine or methotrexate? ›

These results demonstrate MTX to be superior to AZA in the treatment of rheumatoid arthritis, with a more rapid clinical improvement which is sustained after 1 year, accompanied by a lower rate of serious adverse reactions.

Why is azathioprine cytotoxic? ›

The cytotoxicity of azathioprine is due, in part, to the incorporation of 6-TGN into DNA. 6-MP undergoes two major inactivation routes (Figure 1). One is thiol methylation, which is catalyzed by the enzyme thiopurine S-methyltransferase (TPMT), to form the inactive metabolite methyl-6-MP (6-MeMP).

Is azathioprine a cytotoxic drug? ›

Cyclophosphamide, azathioprine, chlorambucil, and methotrexate are cytotoxic drugs used most commonly for the purpose of immunosuppression.

What does TPMT do to azathioprine? ›

Patients with TPMT deficiency treated with standard doses of azathioprine or 6-mercaptopurine are at significantly increased risk of myelosuppression, bleeding, infection, and death associated with increased levels of cytotoxic 6-thioguanine nucleotide levels in the red blood cells.

How does azathioprine work in Crohn's disease? ›

It helps to reduce irritation and swelling (inflammation) in the intestines. It also decreases the long-term need for steroids. For that reason, it is sometimes referred to as a "steroid-sparing" drug. In some cases, this medication is used by itself.

What happens when you stop azathioprine? ›

If you stop taking it suddenly: If you're taking this drug for a kidney transplant and you stop taking it suddenly, you may experience transplant rejection and kidney failure. If you're taking this drug for RA and you stop taking it suddenly, your symptoms of RA may come back again.

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