Buy Azathioprine
Azathioprine

0.85
Used to prevent organ rejection and treat severe inflammatory and autoimmune conditions.


Ingredient
Availability
In Stock
Delivery
Airmail (14-21 days) | EMS trackable (5-9 days)
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Product Sheet

Alternative/Local Brand
Imuran
Active Ingredient(s)
Azathioprine
Primary Category
Immune Suppression
Therapeutic Class
Antineoplastic and immunomodulating agents, Immunosuppressants, Other immunosuppressants
Pharmacological Class
Purine analogue
Indications
Organ transplant rejection prevention, Rheumatoid arthritis, Crohn's disease, Ulcerative colitis
Contraindications
Hypersensitivity to mercaptopurine, Pregnancy (unless benefit outweighs risk), Severe infection
Minor Side Effects
Nausea, Loss of appetite, Vomiting
Moderate Side Effects
Increased risk of infection, Hair thinning, Skin rash, Malaise
Serious Side Effects
Bone marrow suppression, Leukopenia, Pancreatitis, Liver damage, Increased risk of certain cancers
Dosage Forms
Tablet, Injection
Administration Route
Oral
Mechanism of Action
It works by reducing the activity of the body's immune system, which helps prevent it from attacking a transplanted organ or its own healthy tissues in autoimmune diseases.
Prescription Status
Rx
Patient Summary
Used to prevent organ rejection and treat severe inflammatory and autoimmune conditions.
Onset Time
Weeks or months for full effect
Duration
Several days after last dose
Storage Instructions
Store at room temperature and protect from light.
Drug Interactions
Allopurinol, Warfarin, ACE inhibitors, Live vaccines
Age Restrictions
Use with caution in children.
Pregnancy Use
Potential risk to the foetus; check with a specialist.
Alternative Drugs
Methotrexate, Mycophenolate mofetil, Ciclosporin

Azathioprine: Generic Medication Overview

Azathioprine is an immunosuppressive medication classified under Autoimmune Care. It is available in pill form in strengths of 25 mg and 50 mg and is prescribed only with a doctor's order in Hong Kong. The drug is regulated by the Hong Kong Department of Health and the Pharmacy and Poisons Board, which classifies it as a prescription-only product. Azathioprine is marketed internationally under several brand names, including Imuran and Azasan, but the active ingredient remains the same.

How Azathioprine Works in the Body

Azathioprine is a pro-drug that is converted in the body to 6-mercaptopurine (6-MP) and then to active thioguanine nucleotides. These metabolites interfere with purine synthesis, a critical pathway for DNA and RNA production. By limiting the availability of purines, azathioprine reduces the proliferation of T- and B-lymphocytes, the immune cells that drive many autoimmune and inflammatory processes.

  • Onset of action: Therapeutic effects typically appear after 2-4 weeks of consistent dosing.
  • Duration: The immunosuppressive effect persists as long as the drug is taken; abrupt discontinuation can lead to a rebound of immune activity.
  • Metabolism: After oral administration, azathioprine is rapidly absorbed and undergoes hepatic conversion. The enzyme thiopurine methyltransferase (TPMT) influences how much active metabolite is produced, affecting both efficacy and toxicity.

Conditions Treated by Azathioprine

Azathioprine is approved by regulatory agencies (FDA, EMA, and Hong Kong health authorities) for several autoimmune and transplant-related indications:

  • Organ transplantation: Prevention of acute rejection in kidney, liver, and heart transplants.
  • Rheumatoid arthritis: Management of moderate to severe disease when conventional disease-modifying antirheumatic drugs (DMARDs) are insufficient.
  • Inflammatory bowel disease (IBD): Maintenance therapy for Crohn’s disease and ulcerative colitis.
  • Systemic lupus erythematosus (SLE): Adjunctive treatment for patients with severe organ involvement.
  • Autoimmune hepatitis: Used when first-line steroids are inadequate or cause intolerable side effects.

These indications reflect the drug’s ability to dampen an overactive immune response across a range of conditions.

Evidence-Based Off-Label Uses

Some clinical studies have explored azathioprine for conditions that lack formal approval:

  • Dermatologic autoimmune disorders (e.g., pemphigus vulgaris). Small case series suggest benefit, but large-scale randomized trials are lacking.
  • Multiple sclerosis (as an adjunct to disease-modifying therapies). Evidence remains limited and primarily observational.

Off-label use of azathioprine requires medical supervision and individualized risk assessment. Patients should discuss potential benefits and risks with a qualified healthcare provider before initiating therapy for these unapproved indications.

Who Should Not Use Azathioprine?

Absolute Contraindications

  • Known hypersensitivity to azathioprine or any of its components.
  • Pregnancy: Classified as Category D; associated with fetal malformations and miscarriage.
  • Lactation: Excreted in breast milk; not recommended.
  • Active, uncontrolled infection (including tuberculosis, HIV).
  • Severe TPMT deficiency (identified by pre-treatment testing).

Relative Contraindications

  • Moderate hepatic impairment (elevated transaminases).
  • Renal dysfunction (creatinine clearance < 30 mL/min).
  • Elderly patients (increased susceptibility to myelosuppression).
  • Concurrent use of other potent immunosuppressants (e.g., cyclosporine) without close monitoring.

Special Populations

  • Pregnant or breastfeeding individuals should avoid azathioprine unless the benefits clearly outweigh the risks.
  • Pediatric patients may receive weight-based dosing but require stringent laboratory monitoring.

Safety Profile and Interactions

Common Side Effects

  • Nausea, vomiting, and loss of appetite.
  • Mild leukopenia or neutropenia (often reversible with dose adjustment).
  • Transient elevation of liver enzymes.

Serious Adverse Events

  • Severe bone-marrow suppression leading to pancytopenia.
  • Hepatotoxicity (clinically significant hepatitis).
  • Pancreatitis (rare but potentially life-threatening).
  • Increased long-term risk of certain malignancies, particularly lymphomas and skin cancers.

Drug Interactions

  • Allopurinol (or febuxostat): Inhibits xanthine oxidase, raising azathioprine metabolite levels and risk of toxicity; dose reduction of azathioprine to one-third is typically advised.
  • Warfarin: Azathioprine may potentiate anticoagulant effect; INR should be monitored closely.
  • Other immunosuppressants (e.g., corticosteroids, mycophenolate): Combined therapy increases infection risk and may require dose adjustments.

Food and Lifestyle Interactions

  • Live vaccines should be avoided while taking azathioprine due to reduced immune response.
  • Alcohol can exacerbate hepatotoxicity; moderation is recommended.
  • No specific dietary restrictions, but a balanced diet supports overall health during immunosuppression.

If you are taking other prescription or over-the-counter medicines, supplements, or herbal products, inform your healthcare provider before starting azathioprine.

How to Take Azathioprine

  • Standard dosing: Adults typically begin with 50 mg once daily (approximately 1-2 mg/kg body weight). Dosage may be increased gradually, guided by clinical response and laboratory values, up to a maximum of 2-3 mg/kg per day. The 25 mg tablets allow fine-tuning of the total daily dose.
  • Administration: Swallow the pill whole with a glass of water. It may be taken with or without food; consistency helps maintain steady blood levels.
  • Missed dose: Take the missed dose the next day; do not double-dose to catch up.
  • Overdose: Symptoms may include severe nausea, vomiting, abdominal pain, and profound bone-marrow suppression. Seek emergency medical care; there is no specific antidote, but supportive care and possible use of granulocyte-colony stimulating factor (G-CSF) may be indicated.
  • Discontinuation: Azathioprine should be tapered rather than stopped abruptly, especially after long-term use, to reduce the risk of disease flare. A physician will devise a tapering schedule based on the underlying condition.

Monitoring and Follow-Up

  • Baseline tests before initiation: CBC with differential, liver function panel, renal function, and TPMT activity.
  • Ongoing monitoring:
  • CBC weekly for the first month, then every 2-4 weeks once stable.
  • Liver enzymes every 2-4 weeks initially, then monthly.
  • Renal function as clinically indicated.
  • Clinical assessments: Patients should report signs of infection, unusual bruising, or persistent gastrointestinal symptoms promptly.
  • Regular follow-up appointments allow dose adjustments and early detection of adverse effects.

Storage and Handling

  • Store azathioprine tablets at room temperature (20-25 °C), away from moisture, heat, and direct sunlight.
  • Keep the container tightly closed and out of reach of children and pets.
  • Do not use the medication after the expiration date printed on the packaging.
  • Dispose of unused tablets according to local pharmacy or waste-disposal guidelines; do not flush them down the toilet.

Medication-Specific Glossary

Thiopurine methyltransferase (TPMT)
An enzyme that metabolizes azathioprine’s active metabolites; genetic variations affect drug toxicity risk.
Myelosuppression
Decreased production of blood cells (red cells, white cells, platelets) leading to anemia, infection susceptibility, and bleeding tendency.
Azathioprine metabolite
The active form, primarily 6-mercaptopurine, which interferes with purine synthesis to suppress immune cell proliferation.
Hepatotoxicity
Liver injury caused by drug exposure, indicated by elevated liver enzymes or clinical hepatitis.
Immunosuppression
Reduction of the immune system’s activity, intentionally induced to treat autoimmune diseases or prevent organ rejection.

Medical Disclaimer

This article provides educational information about azathioprine and is not a substitute for professional medical advice. Treatment decisions, including use for unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Azathioprine FAQ

Can I travel internationally with azathioprine, and are there any customs restrictions?

Azathioprine is a prescription-only medication, so you should carry it in its original labeled container with a copy of the prescription or a doctor’s letter. Hong Kong, the United States, the United Kingdom, Canada, and most European countries allow personal import of prescribed immunosuppressants provided documentation is present. Check the destination country’s specific import regulations before travel.

Will azathioprine show up on a standard drug test for employment or sports?

Standard workplace drug screens typically target substances of abuse (e.g., opioids, amphetamines) and do not test for immunosuppressive agents like azathioprine. However, certain sports governing bodies may request a comprehensive medication list, and azathioprine must be disclosed to avoid potential therapeutic use exemptions.

What do azathioprine tablets look like, and are there imprint codes that vary by region?

In Hong Kong, the 25 mg tablets are usually round, white, and may bear the imprint “AZA 25”. The 50 mg tablets are often round, white with a score line, and imprinted “AZA 50”. Branding and imprint specifics can differ between manufacturers, so always verify the label against the prescription.

How does azathioprine differ from mycophenolate mofetil in terms of mechanism?

Both drugs suppress the immune system, but azathioprine inhibits purine synthesis by converting to thioguanine nucleotides, whereas mycophenolate mofetil blocks the enzyme inosine monophosphate dehydrogenase, selectively reducing guanosine nucleotide production. This distinction leads to slightly different side-effect profiles and dosing considerations.

Is it safe to receive a flu vaccine while taking azathioprine?

Yes. Inactivated vaccines such as the seasonal influenza shot are generally safe and recommended for patients on azathioprine because they do not contain live virus. Live vaccines (e.g., varicella, yellow fever) should be avoided unless the immunosuppression level is very low.

What happens if I miss a dose for several days in a row?

Missing multiple consecutive doses can reduce the drug’s immunosuppressive effect, potentially leading to disease flare-ups. Resume dosing at the previously prescribed amount after a brief interruption, but do not double-dose. Contact your healthcare provider for personalized guidance.

Can azathioprine be taken with food or does it affect absorption?

Azathioprine can be taken with or without food; food does not significantly alter its absorption. Consistency in how you take the medication (always with food or always empty-stomach) may help maintain steady blood levels.

How long does it typically take to see improvement in autoimmune disease symptoms?

Clinical improvement usually begins 2-4 weeks after starting therapy, but full therapeutic effect may require 3-6 months of consistent dosing and monitoring. Patience and regular follow-up are essential for optimal outcomes.

TPMT activity determines how quickly the body converts azathioprine to its active metabolites. Low or absent TPMT activity can cause dangerous accumulation, leading to severe bone-marrow suppression. Testing helps clinicians choose a safe starting dose or consider alternative therapy.

Are there cost differences between brand-name and generic azathioprine in Hong Kong?

Generic azathioprine is typically less expensive than brand-name versions such as Imuran, as the active ingredient is identical and manufacturing costs are lower. Prices can vary by pharmacy and insurance coverage, but the therapeutic efficacy remains the same.

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