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Azathioprine, an FDA-approved immunosuppressant, is used to treat autoimmune disorders such as Crohn’s disease and rheumatoid arthritis. Its active ingredient, Azathioprine, inhibits immune responses, reducing inflammation and symptoms. Available in tablet form, strengths typically range from 25 to 100mg. The medication is taken once or twice a day, either with or without food, after consulting a healthcare professional. Common side effects include vomiting, nausea, and fatigue. Precautions include monitoring for side effects and avoiding infections due to suppressed immunity. If a dose is missed, take it soon unless it’s close to the next dose. Get medical help immediately if you suspect you have overdosed. Keep away from moisture and heat at room temperature. Adhering to healthcare provider guidance is crucial for safe and effective use.

Product Overview

Azathioprine is an FDA-approved medication used primarily to treat autoimmune diseases such as ulcerative colitis, Crohn’s disease, and rheumatoid arthritis. The active ingredient is Azathioprine, which belongs to a class of drugs known as immunosuppressants. It decreases inflammation and relieves symptoms associated with autoimmune conditions by suppressing the immune system. Azathioprine can help prevent the body from attacking its tissues by inhibiting certain immune responses.

Azathioprine is available in tablet form and comes in various strengths, typically ranging from 25mg to 100mg per tablet. A person’s response to medication and the specific condition being treated determines the dosage and frequency of administration. It is usually taken orally once or twice daily with or without food. It is typically prescribed to patients with autoimmune diseases who have had limited success with other treatments. It would help if you discussed it with your healthcare professional before starting Azathioprine, as it may not be suitable for everyone.

Common side effects of Azathioprine are nausea, vomiting, diarrhea, and fatigue. Monitor potential side effects carefully and seek medical attention if they occur according to your healthcare provider’s instructions. Additionally, precautions should be taken to avoid exposure to infectious agents while taking Azathioprine due to its immunosuppressive effects. In case of a missed dose, taking it as soon as possible is recommended unless it is almost time for the next scheduled dose. In case of overdose, immediate medical attention should be sought. Azathioprine should be kept at room temperature distant from moisture and heat, and out of reach of children. Patients should adhere to their healthcare provider’s guidance and warnings while taking Azathioprine to ensure safe and effective use.

Uses of Azathioprine

It is used for the:

  • Prevention of organ rejection in transplant patients
  • Treatment of Rheumatoid arthritis

How to Use Azathioprine?


Strengths and Form

Form: Oral tablets

Strengths: 25 mg, 50 mg, 100 mg

Recommended Dosage for Different Patients

For Adults with Rheumatoid Arthritis:

  • The starting dose is 1 mg/kg (50 to 100 mg) orally or IV daily, given in 1 or 2 divided doses.
  • The maximum dose is 2.5 mg/kg orally or IV daily.
  • The duration is at least 12 weeks.
  • Approximately 25 mg/day may be increased after 6 to 8 weeks, and at 4-week intervals if necessary.
  • The risk of toxicities can be reduced by gradually reducing the dose.
  • The therapeutic response usually occurs after six to eight weeks of therapy. Refractory patients are those who do not improve after 12 weeks.

For Adults with Crohn’s Disease – Acute:

  • The recommended dose is 1.5- 4 mg/kg daily for 10 days up to 52 weeks.

For Adults with Crohn’s Disease – Maintenance:

  • The recommended dose is 1.5- 4 mg/kg daily for 10 days up to 52 weeks.

For Adults with Chronic Inflammatory Demyelinating Polyradiculoneuropathy:

  • The recommended dose is 2- 3 mg/kg orally once daily for up to 9 months.

For Adults with Atopic Dermatitis:

  • The recommended dose is 2.5 mg/kg orally once daily, in the morning, for up to 3 months.

For Adults with Sarcoidosis:

  • The starting dose is 2 mg/kg daily when combined with prednisolone 0.6- 0.8 mg/kg daily, with prednisolone lowered to 0.1 mg/kg within 2 or 3 months.
  • The maintenance dose is 2 mg/kg daily with prednisolone 0.1 mg/kg daily for 21- 22 months.

For Adults with Ulcerative Colitis:

  • An intravenous dose of 20 to 40 mg/kg over 36 hours or three infusions of 8 hours each over three days is typically recommended.
  • Immediately following the IV dose, oral Azathioprine is administered: two mg per kilogram once a day starting the next day.
  • Initially, 50 mg per day was prescribed, followed by 2 to 2.5 mg/kg daily combined with mesalamine 500 mg orally 3 times daily. 

For Adults with Uveitis:

  • The starting dose is 1 to 1.5 mg/kg orally daily combined with prednisolone and cyclosporine

For Adults with Multiple Sclerosis:

  • A dose of 1.5 mg/kg daily should be titrated over 1 month, followed by 50 mg increments every six months, and 8 million international units of interferon beta-1b administered on alternate days.
  • The maintenance dose is 2 mg/kg daily.

For Adults with Systemic Lupus Erythematosus:

  • One to three mg/kg actual body weight (ABW)/day orally or intravenously is recommended.
  • Prednisone (1 mg/kg/day) and oral cyclophosphamide (1 to 2 mg/kg/day) are prescribed for 8 to 10 weeks in diffuse proliferative lupus glomerulonephritis followed by azathioprine 50 to 100 mg daily after tapering to a maintenance dose of 5 to 10 mg/day.

For Adults with Chronic Active Hepatitis:

  • A monthly dose of 1 to 2 mg/kg is recommended with prednisolone (5 to 15 mg/day) for a minimum of one year (on average 5 years).

For Adults with Takayasu’s Arteritis:

  • In combination with prednisolone tapering, the recommended dose is 2 mg/kg ABW daily for one year.

Recommended Pediatric Dose for Atopic Dermatitis

  • For those aged 17 and older, take 2.5 mg/kg every morning for three months.

Recommended Pediatric Dose for Organ Transplant Rejection Prophylaxis:

  • At the time of transplantation, the initial dosage is three to five mg/kg orally or intravenously once daily.
  • Ideally, 1 to 3 mg/kg/day should be administered orally or intravenously.

Recommended Pediatric Dose for Eczema:

  • A dosage of 2.5 to 3.5 mg/kg per day is recommended for patients older than 6 years with a thiopurine methyltransferase level of normal.

Recommended Pediatric Dose for Systemic Lupus Erythematosus:

  • A dose of 23 mg/kg daily (maximum 150 mg/day) is recommended for children over 5 years old.
  • It is recommended to titrate the dose to maintain a white blood cell count between 3 and 4 x 10(3) cells per milliliter.

Renal Dose Adjustments:

  • No specific guidelines on what dosages are required; however, lower doses may be necessary.

Liver Dose Adjustments:

  • A dose adjustment may be necessary; however, no specific guidelines have been provided.

Dose Adjustments:

  • It may be necessary to reduce dosage or consider alternative therapies in patients with reduced thiopurine S-methyltransferase activity.
  • Allopurinol should be used with Azathioprine at 25% to 33%. TPMT activity may require further dose reductions or alternative treatments in patients with low or absent TPMT activity.

[Note: These Azathioprine dosage recommendations may differ from individual to individual. Discuss it with your healthcare professional, and they’ll decide your dosage accordingly.]

How to Take It?

  • Always take Azathioprine exactly as prescribed by your doctor. 
  • Azathioprine can be taken with or without food. However, some people may experience stomach upset when taking it on an empty stomach, so you may want to take it with food if you experience discomfort.
  • Try to take Azathioprine at the same time each day to help you remember. You can choose a time that fits your daily routine, such as morning or evening.
  • Take the tablets with a full glass of water and swallow them whole. Avoid crushing, chewing, or breaking them, as this could affect the release of the medication.
  • Even if you feel better, you should not stop taking Azathioprine suddenly without consulting your healthcare provider. Stopping abruptly can result in the worsening of your condition or withdrawal symptoms.
  • Your doctor may want to monitor your blood counts and liver function regularly while taking Azathioprine to check for potential side effects or complications.

[Note: Your healthcare professional will decide the correct amount of Azathioprine for you based on your condition. They may adjust your Azathioprine dosage as needed over time.]

How Does Azathioprine Work?

Azathioprine is a purine analog that suppresses the immune system by inhibiting DNA and RNA synthesis in immune cells like T and B lymphocytes. Converted into active metabolites, primarily 6-mercaptopurine (6-MP), it disrupts these nucleic acid processes crucial for cell replication and function. By dampening immune response, Azathioprine is effective in treating autoimmune diseases like rheumatoid arthritis and inflammatory bowel disease and preventing organ transplant rejection. However, its immunosuppressive effects can increase susceptibility to infections and necessitate careful monitoring during treatment.

Important Safety Information

Side Effects

Common side effects of Azathioprine may include:

  • Nausea
  • Vomiting
  • Diarrhea
  • Loss of appetite
  • Upset stomach
  • Fatigue
  • Hair loss
  • Skin rash
  • Increased susceptibility to infections
  • Pancreatitis

Mild side effects of Azathioprine may include:

  • Headache
  • Dizziness
  • Muscle aches
  • Mild allergic reactions (irritation or hives)

Adverse side effects of Azathioprine may include:

  • Bone marrow suppression leads to decreased white blood cell, red blood cell, and platelet counts
  • Hepatotoxicity (liver damage)
  • Certain cancer risks, such as lymphoma or skin cancer
  • Severe allergic reactions
  • Stevens-Johnson syndrome (rare but serious skin reaction)
  • Pancreatitis (inflammation of the pancreas)
  • Interstitial lung disease (rare)
  • Myelosuppression, leading to anemia, leukopenia, and thrombocytopenia
  • Gastrointestinal disturbances such as gastritis, ulceration, or bleeding

[Note: This list may not cover all possible Azathioprine side effects. Always discuss with your healthcare giver for medical advice about side effects.]


Immunosuppression: Azathioprine suppresses the immune system, increasing the risk of infections. Patients taking Azathioprine should avoid contact with infected individuals and immediately report any signs of infection to their healthcare provider.

Bone Marrow Suppression: Azathioprine can cause bone marrow suppression, leading to decreased production of white blood cells, red blood cells, and platelets. Regular observation of blood cell counts is necessary during treatment.

Increased Risk of Cancer: Long-term use of Azathioprine may increase certain cancer risks, including lymphoma and skin cancer. Patients should discuss treatment’s potential risks and benefits with their healthcare provider.

Hepatotoxicity: Azathioprine can cause liver damage, including hepatotoxicity and liver function abnormalities. Performing liver function tests before and after treatment is essential.

Pregnancy Risk: Azathioprine may cause fetal harm when administered to pregnant women. Women in their childbearing age should use effective contraception during treatment with Azathioprine and discuss the advantages and risks with their healthcare provider if pregnancy is planned or suspected.

Allergic Reactions: Serious allergic reactions, including anaphylaxis, may occur with Azathioprine. If patients suffer symptoms such as difficulty breathing, swelling of their faces or throats, or severe rashes, they should seek immediate medical attention.

Pancreatitis: Azathioprine may cause pancreatitis, which can be severe and potentially life-threatening. Symptoms of pancreatitis, like vomiting, nausea, and abdominal pain, should be monitored closely.

Interstitial Lung Disease: Azathioprine may cause interstitial lung diseases, such as pneumonitis and pulmonary fibrosis. Patients should contact their healthcare provider whenever respiratory symptoms worsen or become new.

Skin Reactions: As well as Stevens-Johnson syndrome, Azathioprine has been associated with toxic epidermal necrolysis (TEN). Patients should discontinue Azathioprine and seek medical attention if they develop a severe rash or blistering skin reaction.

Drug Interactions: Azathioprine may interact with other medications, including allopurinol and ACE inhibitors, potentially increasing the risk of adverse effects. All medications should be disclosed to the healthcare provider before Azathioprine is started.


  • Before starting Azathioprine, inform your doctor about any allergies or medical conditions you have.
  • Tell your doctor about all the medications you are taking to avoid potential interactions.
  • Avoid contact with people with infections while taking Azathioprine, as it may increase your risk of getting sick.
  • Consult your doctor if you experience any signs of infection, such as sore throat, fever, or cough.
  • Attend regular appointments for blood tests to monitor your blood cell counts and liver function.
  • Use effective contraception if you are of childbearing age, as Azathioprine may cause harm to the fetus.
  • Discuss the risks and benefits of azathioprine treatment if you are pregnant or planning to become pregnant.
  • You should consult a doctor immediately when you encounter signs of an allergic reaction like problem breathing, puffiness of the face or throat, or chest tightness.
  • Watch for signs of pancreatitis like intense abdominal pain, nausea, or vomiting, and inform your doctor if you experience any.
  • It is important to be aware of the possibility of skin reactions, such as rash or blistering, and discontinue Azathioprine if you develop severe skin symptoms.
  • Report any new or worsening respiratory symptoms, such as cough or difficulty breathing, to your doctor, as they could indicate interstitial lung disease.
  • Inform healthcare providers of your azathioprine treatment before undergoing surgical procedures or receiving vaccinations.

Azathioprine Contraindications

It is contraindicated in the:

  • Those who have shown hypersensitivity to the drug.
  • Azathioprine may cause neoplasia in patients previously treated with alkylating agents (cyclophosphamide, chlorambucil, melphalan, etc.).

Missed Dose

  • If you forget a dose of Azathioprine, take it when you remember. But skip the missed one if it’s close to your next dose.
  • Don’t double your dose to compensate for a missed one. This can worsen the side effects.

[Note: If you have missed a dose of Azathioprine and are still deciding when to take the next dose, immediately consult your doctor or pharmacist.]


Overdosing on Azathioprine may cause symptoms like nausea, vomiting, diarrhea, unusual bruising or bleeding, extreme fatigue, pale skin, or signs of infection. It’s important not to take more than the prescribed dose of Azathioprine to avoid potential complications.

[Note: If you overdosed on Azathioprine, get medical help instantly or call the Poison Help line at 1-800-222-1222.]


  • Keep azathioprine tablets at room temperature, ideally between 68°F to 77°F.
  • Store them away from moisture and excessive heat.
  • Keep Azathioprine in its original packaging.
  • Store azathioprine in a place that is distant from children and pets.
  • Avoid storing Azathioprine in the bathroom or kitchen, where humidity levels fluctuate.
  • Do not transfer Azathioprine to different containers unless instructed by your pharmacist or healthcare provider.
  • If you have unused or expired Azathioprine, dispose of it properly.

[Note: Consult with your healthcare practitioner about the proper disposal of unused Azathioprine tablets and any questions you may have regarding their storage.]

Azathioprine Interactions

  • Leflunomide
  • Rotavirus vaccine (live attenuated, oral)
  • Live Attenuated Varicella-Zoster Virus
  • Measles Vaccine (Live)
  • Aspirin (Aspir 81 and Aspirin Low Strength)
  • Benadryl (diphenhydramine)
  • Calcium 600 D (calcium/vitamin D)
  • Cymbalta (duloxetine)
  • Eliquis (apixaban)
  • Fish Oil (omega-3 polyunsaturated fatty acids)
  • Flonase (fluticasone nasal)
  • Humira (adalimumab)
  • Iron Sulfate (ferrous sulfate)
  • Lexapro (escitalopram)
  • Lipitor (atorvastatin)
  • Lyrica (pregabalin)
  • Metoprolol Succinate ER (metoprolol)
  • Metoprolol Tartrate (metoprolol)
  • Nexium (esomeprazole)
  • Paracetamol (acetaminophen)
  • Plaquenil (hydroxychloroquine)
  • Remicade (infliximab)
  • Singulair (montelukast)
  • Symbicort (budesonide / formoterol)
  • Synthroid (levothyroxine)
  • Tylenol (acetaminophen)
  • Vitamin B12 (cyanocobalamin)
  • Vitamin C (ascorbic acid)
  • Vitamin D2 (ergocalciferol)
  • Vitamin D3 (cholecalciferol)
  • Zofran (ondansetron)
  • Zoloft (sertraline)
  • Zyrtec (cetirizine)

[Note: This list is not complete, and Azathioprine may interact with other drugs. If you take prescription, over-the-counter, or herbal medicines, tell your doctor about them.]

Azathioprine Alternatives

[Note: Your healthcare professional will select the best Azathioprine alternative. You should not use these alternative medications without consulting your healthcare provider first. You may experience serious side effects if you take them on your own. 

Frequently Asked Questions

How long does an Azathioprine tablet take to start working?

Azathioprine may take about 3 to 12 weeks before you notice any benefits. Continue taking the medication even if you don’t see immediate improvement. Patience is key, as the efficacy of Azathioprine is not immediately apparent.

How should I take Azathioprine?

It would help if you took Azathioprine exactly as directed by your healthcare professional. Swallow the tablets whole with a drink of water, and do not chew them. You can take them with or without food. The dose depends on your body weight and the reason for taking it. For example, after a transplant, the usual dose is between 1mg and 2.5mg per kilogram of body weight, taken daily.

How long do I need to take an Azathioprine tablet?

You’ll likely need to take Azathioprine long-term for the rest of your life. Your healthcare professional will determine the duration based on your specific condition. Regular monitoring and adjustments may be necessary.

Can I drink alcohol while taking Azathioprine?

While alcohol does not directly affect how Azathioprine works, both substances can impact your liver. It’s advisable to keep alcohol consumption to a minimum. National guidelines recommend no more than 14 units of alcohol per week for men and women.

How does Azathioprine affect liver function?

Azathioprine can affect the liver, especially when combined with alcohol. Regular liver function tests are essential during Azathioprine therapy to monitor any potential adverse effects.

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