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What is Azathioprine?

Azathioprine is a prescription drug that belongs to a class called immunosuppressants, which lowers the activity of the immune system.

It is FDA-approved for the treatment of active rheumatoid arthritis and as an add-on therapy to help prevent kidney transplant rejection. Reducing immune activity, it can help ease joint pain and swelling and support the body in accepting a transplanted kidney.

It is usually prescribed to adults with moderate to severe rheumatoid arthritis who have not responded well to other treatments, and to patients who have received a kidney transplant and need long-term protection.

Because it affects immune function, regular monitoring by a healthcare provider is important. 

Patients looking to buy azathioprine in Canada should have a valid prescription and proper medical supervision.

Indications and Benefits of Azathioprine

Azathioprine is used to manage immune-related conditions and support transplant success.

What Are the Benefits of Azathioprine?

FDA-approved indications:

  • Treatment of active Rheumatoid Arthritis in adults
  • Adjunct therapy to prevent Kidney Transplant Rejection

Clinical benefits:

  • Helps reduce joint pain, swelling, and stiffness in rheumatoid arthritis.
  • Can improve physical function in patients who did not respond to other treatments.
  • Supports long-term survival of transplanted kidneys when used with other therapies.
  • Clinical studies show improved disease control in rheumatoid arthritis compared to placebo, with meaningful symptom relief in a subset of patients.
  • Helps lower the risk of immune-related damage to a transplanted organ.

Common off-label uses

  • Management of inflammatory bowel disease, such as Crohn’s disease and ulcerative colitis.
  • Treatment of autoimmune conditions like lupus, autoimmune hepatitis, and severe skin disorders.
  • Used in some cases of myasthenia gravis and multiple sclerosis when other options are not suitable.

Azathioprine Drug Information

Fact Category Fact Details
Generic Name Azathioprine
Azathioprine Class Immunosuppressant
Primary Use Used with other drugs to help prevent kidney transplant rejection and to treat severe active rheumatoid arthritis when other treatments have not helped
Additional Benefit Helps reduce immune system activity to protect a transplanted kidney and lower joint pain, swelling, and loss of function in rheumatoid arthritis
Available Form Oral tablet
Method of Administration Taken by mouth, usually after meals
Frequency Usually once or twice daily, as prescribed
Storage Instructions Store at room temperature, tightly closed, away from heat and moisture. Keep out of reach of children
Pregnancy and Breastfeeding May harm the fetus. Patients should tell their doctor if they are pregnant, planning pregnancy, or breastfeeding. Birth control is recommended during treatment
Drug Interactions May interact with ACE inhibitors, trimethoprim and sulfamethoxazole, ribavirin, and other drugs that affect blood cell counts or immune function
Manufacturer Brand names include Azasan and Imuran

How Azathioprine Works

Azathioprine, an immunosuppressant, works by lowering the activity of the immune system. After you take it, your body turns it into active forms that slow down how quickly certain immune cells grow and multiply.

These immune cells are the ones that can attack your own joints in rheumatoid arthritis or a transplanted kidney. By reducing this response, azathioprine helps prevent damage and keeps inflammation under control.

This effect builds over time, so it may take several weeks to notice improvement, especially for joint symptoms.

In transplant care, it starts helping right away but is used long-term to maintain protection.

Azathioprine works inside cells by interfering with the process they use to make new genetic material, which limits the ability of immune cells to keep attacking. Because it affects how the immune system functions, regular monitoring is needed to make sure it is working safely and effectively.

Brand Name Options

Azathioprine is available under the brand names Imuran and Azasan.

These brands contain the same active ingredient and are used for the same approved conditions, including rheumatoid arthritis and the prevention of kidney transplant rejection.

Availability may vary depending on the pharmacy and location, but both options follow the same safety and prescribing standards.

Azathioprine Dose

The dose of azathioprine depends on your condition, body weight, and how your body responds to treatment.

What Dosage Strengths Does Azathioprine Come In?

Azathioprine is available in oral tablet forms, most commonly in 50 mg, 75 mg, and 100 mg strengths.

The dose is usually based on body weight, so your healthcare provider may adjust your daily amount over time to find the safest and most effective dose.

  • Oral tablets: 50 mg, 75 mg, 100 mg
  • Injection (for IV use in clinical settings)

Dosage Chart

Condition Starting Dose Maintenance Dose Maximum Dose
Kidney transplant rejection prevention 3 to 5 mg per kg daily (at time of transplant) 1 to 3 mg per kg daily Adjusted based on response and tolerance
Rheumatoid arthritis 1 mg per kg daily (single or divided dose) Up to 2.5 mg per kg daily (adjusted gradually) 2.5 mg per kg daily

Azathioprine Usage Guide

Follow these steps to take azathioprine safely and correctly:

Step-by-Step Instructions

  • Take azathioprine exactly as prescribed by your doctor
  • Take it by mouth once or twice daily, usually after meals, to help reduce stomach upset
  • Swallow the tablet with water
  • Take it at the same time each day to keep a steady level in your body
  • Do not stop taking it, even if you feel well, unless your doctor tells you to

If Given as an Injection

  • Azathioprine injection is given in a healthcare setting
  • It is administered into a vein by a trained professional
  • Do not attempt to inject this yourself at home

Important Things to Avoid

  • Avoid stopping or changing your dose without medical advice
  • Limit sun exposure and use sunscreen, as this drug may increase skin sensitivity
  • Do not receive vaccines unless your doctor approves
  • Tell your doctor about all other drugs you are taking

How to Know It Is Working

  • For rheumatoid arthritis, you may notice less joint pain and swelling over time
  • For transplant patients, it helps protect the transplanted kidney from rejection
  • It may take several weeks, up to 12 weeks, to feel the full benefit

Side Effects

Azathioprine can cause mild and serious side effects. Some are more common, while others are rare but may need urgent care

Common Side Effects

Side Effect Frequency
Nausea and vomiting About 12% in rheumatoid arthritis patients
Diarrhea Reported, frequency not specified
Rash Reported, frequency not specified
Hair loss Reported, frequency not specified
Fever, joint pain, muscle pain Reported, frequency not specified

Serious Side Effects

Side Effect What to Do
Low white blood cells (leukopenia) Can occur in over 50% of transplant patients and about 28% of rheumatoid arthritis patients. Seek medical attention right away if you have signs of infection
Serious infections Up to 20% in transplant patients. Seek medical attention right away for fever, chills, or sore throat
Liver problems May cause liver injury. Seek medical attention right away for yellowing of skin or eyes
Low platelets or anemia May cause bleeding, bruising, or weakness. Seek medical attention right away
Pancreatitis or lung inflammation Rare but serious. Seek medical attention right away
Increased risk of cancer (lymphoma, skin cancer) Watch for unusual lumps or skin changes and seek medical attention right away

Missed Dose

If you miss a dose of azathioprine, take it as soon as you remember on the same day. If it is close to your next scheduled dose, skip the missed dose and continue with your regular daily schedule. Do not take two doses at the same time or extra doses to make up for the missed one.

If you are unsure what to do, contact your healthcare provider for guidance.

Overdose

An overdose of azathioprine may cause nausea, vomiting, diarrhea, and signs of infection such as sore throat, fever, or chills due to low blood cell counts.

If an overdose is suspected, call right away or go to the nearest emergency room. If the person collapses, has trouble breathing, or cannot be awakened, call 911 immediately.

There is no specific antidote for azathioprine overdose. Treatment focuses on supportive care and close medical monitoring.

Storage Information

Store azathioprine tablets at room temperature between 20 degrees Celsius and 25 degrees Celsius. Keep the tablets in the original container, tightly closed, and away from excess heat and moisture. Do not store in the bathroom.

Protect from light by keeping the tablets in their original packaging.

There are no special storage changes after opening. Do not freeze this product.

Keep azathioprine out of reach of children and pets. For expired or unused tablets, do not flush them down the toilet. Use a take-back program or ask your pharmacist about safe disposal options.

Warnings and Precautions

Azathioprine carries a black box warning for increased risk of malignancy and serious infections. 

Long-term use may raise the risk of lymphoma and skin cancer. Severe and sometimes fatal bone marrow suppression can occur, leading to low blood cell counts and increased risk of infection and bleeding.

Precautions

  • Bone marrow suppression: May cause low white blood cells, red blood cells, and platelets
  • Serious infections: Increased risk due to weakened immune system
  • Malignancy risk: Includes lymphoma and skin cancer, especially with long-term use
  • Hypersensitivity reactions: May include fever, rash, and muscle pain
  • Liver toxicity: Can cause liver injury with long-term use
  • Drug interactions: Some drugs may increase toxicity or require dose adjustments
  • Vaccinations: Avoid live vaccines unless approved by your doctor

Patients Who Need Extra Caution

  • Patients with kidney or liver impairment
  • Patients with active infections
  • Pregnant or breastfeeding patients
  • Patients with known genetic enzyme deficiencies affecting drug metabolism
  • Elderly patients who may be more sensitive to side effects

Monitoring Requirements

  • Regular blood tests to check blood cell counts
  • Liver function tests to monitor for toxicity
  • Ongoing medical checkups to assess response and safety

Close medical supervision is required throughout treatment with azathioprine.

Contraindications

Azathioprine should not be used in the following situations:

  • Hypersensitivity to azathioprine: Do not use if you have had an allergic reaction to azathioprine or any of its ingredients, as this may cause serious reactions.
  • Pregnancy: Azathioprine may harm the unborn baby and increase the risk of miscarriage or early delivery. It should be avoided unless clearly directed by a healthcare provider.
  • Breastfeeding: The drug can pass into breast milk and may affect a nursing infant.
  • Severe enzyme deficiency, such as low or absent TPMT activity: Patients with this condition are at high risk of severe bone marrow suppression, which can lead to life-threatening infections and bleeding.
  • Active serious infection: Azathioprine weakens the immune system and may worsen infections or make them harder to control.
  • Existing malignancy: Use may increase the risk of cancer progression due to immune suppression.

Azathioprine Interactions

Azathioprine can interact with certain drugs that affect the immune system, blood cells, or how the drug is broken down in the body.

Drug or Substance What Happens What to Do
Allopurinol Increases azathioprine levels, raising the risk of severe bone marrow suppression Dose adjustment is required, and close monitoring is needed
Febuxostat Strongly increases azathioprine levels, leading to serious toxicity Avoid using together
ACE inhibitors such as lisinopril or enalapril May increase the risk of low white blood cells Monitor blood counts closely
Live vaccines Reduced immune response and risk of infection Avoid live vaccines during treatment
Other immunosuppressants, such as adalimumab Higher risk of infection and immune suppression Use with caution and monitor closely
Ribavirin Can reduce effectiveness and increase toxicity risk Avoid combination or monitor closely
Trimethoprim and sulfamethoxazole May increase the risk of bone marrow suppression Monitor blood counts

Alternatives

Drug Name Generic Name Drug Class Key Difference from Azathioprine Best For
Trexall methotrexate disease-modifying antirheumatic drug Works by slowing down the immune system in a different way and is often used earlier in treatment People with rheumatoid arthritis starting treatment
Humira adalimumab biologic TNF blocker Targets a specific part of the immune system instead of lowering it overall People with autoimmune conditions need targeted therapy
Xeljanz tofacitinib JAK inhibitor A targeted oral option that blocks signals that cause inflammation People who prefer a pill instead of injections
Skyrizi risankizumab interleukin inhibitor Focuses on a specific immune pathway instead of general suppression People with conditions like psoriasis or Crohn’s disease
Tremfya guselkumab interleukin inhibitor Targets a specific immune signal linked to inflammation People who need a biologic treatment option

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Frequently Asked Questions

Buying Azathioprine from Canada

Yes. Azathioprine is a prescription drug, and the FDA label states it is Rx only. Pharma Giant also requires a valid prescription before the order can be reviewed and processed.

Rules can vary depending on your situation, so it is best to speak with your healthcare provider and review current import guidance. In general, patients looking at Canadian pharmacies usually want to make sure the pharmacy requires a prescription and follows proper pharmacy standards.

The usual process is to add the product to your cart, go to checkout, create an account or sign in, and submit your prescription. After that, the pharmacy team reviews the prescription and prepares the order for shipping once approved.

Pharma Giant allows prescription submission through the online RX uploader, by email, or by fax. The site guidance specifically lists upload, email, and fax as the main ways to send in your prescription.

If your prescription includes authorized refills, you can usually request another order based on those refill instructions. It is still important to stay in touch with your prescriber, since azathioprine often needs ongoing lab monitoring.

Pharma Giant states that orders are shipped through Canada Post Express and that tracking is provided. Delivery typically takes about 4 to 10 business days, although customs inspection may sometimes cause delays.

FDA-Prescription, Off-Label Information, and Limitations

Azathioprine is FDA-approved to treat active rheumatoid arthritis and to help prevent kidney transplant rejection. It is usually used when other treatments have not worked well enough or are not suitable. It works by lowering immune system activity.

Yes. Doctors may prescribe azathioprine for off-label uses such as Crohn’s disease, ulcerative colitis, lupus, and other autoimmune conditions. These uses are based on clinical experience and research, even though they are not FDA-approved indications.

Not always. For rheumatoid arthritis, it is usually used when other treatments like methotrexate are not effective or cannot be used. Your doctor will decide if it is appropriate based on your condition and treatment history.

Yes. Azathioprine requires regular blood tests to monitor for side effects like low blood cell counts and liver problems. It may not be suitable for patients with certain infections, enzyme deficiencies, or a history of serious reactions.

Dosage & Administration

The FDA-based patient guidance says azathioprine is usually taken once or twice daily after meals and at about the same time each day. Taking it on a regular schedule can help keep treatment consistent and may also help with stomach upset.

The FDA label describes azathioprine as a tablet taken by mouth, but the patient instructions do not specifically say to crush it. Because handling and dosing can matter with this drug, ask your pharmacist before crushing, splitting, or changing how you take the tablet.

Adverse Reactions

People with a known allergy to azathioprine should not take it. The FDA label also warns that some patients are at higher risk of serious bone marrow problems, infections, and certain cancers, so careful screening and monitoring are important before and during treatment.

The FDA label warns that long-term immunosuppression with azathioprine can increase the risk of malignancy, including skin cancer and lymphoma. Because the drug lowers immune activity, the body may be less able to detect and control abnormal cell growth over time.

Pregnancy should be discussed carefully with the prescribing clinician. Azathioprine may harm the fetus, and patients should tell their doctor if they are pregnant, planning pregnancy, or breastfeeding.

Food & Drug Interactions

The patient guidance says to talk with your doctor or pharmacist before starting, stopping, or changing other drugs while taking azathioprine. The label also warns about important interactions with drugs such as allopurinol, febuxostat, ACE inhibitors, and other treatments that can affect blood counts or immune function.

The FDA label does not give a specific alcohol rule in the patient instructions, but azathioprine can affect the liver in some patients. Because of that, it is best to ask your prescriber whether alcohol is safe for you based on your liver health and other drugs you take.

Storage & Travel

Store azathioprine at room temperature in the original container, tightly closed, and away from excess heat and moisture. For travel, keep it in its labeled container and protect it from heat and humidity so your dosing stays consistent while you are away.

Drug Comparison

That depends on why azathioprine was prescribed. Other options may include different immunosuppressants, disease-modifying drugs, or biologic treatments, but the right choice depends on the condition being treated, past response, and safety factors, so this decision should be made with your prescriber.

Disclaimer

Pharma Giant provides medical information to help you better understand medications and medical conditions.This content is for informational use only and does not replace advice from a licensed medical practitioner. Consult your doctor or pharmacist before starting or changing any medication. All our partners follow strict safety standards set by their country’s health authorities to make sure you receive safe and high-quality medications.

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