Azathioprine 2025: Uses, Dosage, Side Effects, and Pricing Guide

Essential Highlights

• Azathioprine is a commonly prescribed immunosuppressant available as generic and branded forms like Imuran and Azasan, primarily used to manage rheumatoid arthritis and prevent kidney transplant rejection.
• It functions by suppressing the immune system to prevent it from attacking joints in rheumatoid arthritis or a transplanted kidney.
• Long-term use carries risks including increased chances of certain cancers (lymphoma, leukemia, skin cancers) and serious side effects such as low blood cell counts, infections, and gastrointestinal issues.

Critical Safety Warnings

Azathioprine includes FDA boxed warnings highlighting serious risks. Patients and healthcare providers must be vigilant about these potential dangers.

• Prolonged use may elevate the risk of cancers like lymphoma, leukemia, and skin malignancies.

Additional Precautions

• Immune suppression increases susceptibility to infections.
• Initial treatment may cause adverse reactions such as nausea, vomiting, diarrhea, rash, fever, fatigue, muscle pain, liver damage, dizziness, and low blood pressure.

These symptoms typically emerge within the first weeks of therapy and usually resolve upon discontinuation.

• Risk of low blood cell counts necessitates regular blood monitoring; dosage adjustments may be required.

What is Azathioprine?

Azathioprine is a prescription immunosuppressant available as oral tablets and injectable forms. It is marketed under brand names Imuran and Azasan, as well as generic versions which are generally more affordable.

Often prescribed as part of combination therapy, it is essential to follow your healthcare provider's instructions carefully.

Primary Uses

Azathioprine treats rheumatoid arthritis by preventing immune-mediated joint damage and helps prevent rejection of transplanted kidneys by suppressing immune responses against the new organ.

Mechanism of Action

Belonging to immunosuppressants, azathioprine reduces immune system activity, thereby protecting joints in RA and preventing immune attack on transplanted kidneys.

Side Effects of Azathioprine

While it does not cause drowsiness, azathioprine can produce several side effects.

Common Side Effects

• Reduced white blood cell counts
• Infections
• Gastrointestinal issues such as nausea, diarrhea, and vomiting

Serious Side Effects

Seek immediate medical attention if you experience severe symptoms including:

• Gastrointestinal hypersensitivity: nausea, vomiting, diarrhea, rash, fever, muscle aches, elevated liver enzymes, liver damage, dizziness, or low blood pressure.
• Pancreatitis with severe abdominal pain and fatty stools.
• Extreme fatigue or significant weight loss.
• Severe allergic reactions: wheezing, chest tightness, itching, or swelling of face, lips, tongue, or throat.

Most serious reactions occur early in treatment and resolve after discontinuation.

Drug Interactions

Azathioprine may interact with various medications, vitamins, or herbal supplements, potentially altering its effectiveness or increasing side effects. Inform your healthcare provider of all substances you are taking.

Notable Interactions Include:

• Gout medications: Allopurinol and febuxostat can increase azathioprine levels, raising side effect risks; dosage adjustments or avoidance may be necessary.
• Inflammatory bowel disease drugs: Aminosalicylates may increase bleeding risks when combined.
• TNF-modifiers: Drugs like adalimumab, certolizumab, infliximab, and golimumab can increase infection risk when used with azathioprine.
• Immune system affecting drugs: Cotrimoxazole may further reduce white blood cells, enhancing infection risk.
• Blood pressure medications: ACE inhibitors may elevate blood disorder risks.
• Blood thinners: Warfarin effectiveness may decrease; close monitoring is essential.
• Hepatitis C treatment: Ribavirin can increase azathioprine levels.
• Vaccines: Live vaccines may cause adverse effects; inactivated vaccines may be less effective.

Important Warnings and Precautions

Allergy Alert

Severe allergic reactions can occur, including breathing difficulty, throat or tongue swelling, and hives. Immediate emergency care is required.

Special Considerations

• TPMT Deficiency: Genetic deficiency increases risk of blood disorders; testing is recommended.
• Low blood cell counts: Requires monitoring and potential dose adjustments.
• Existing infections: Immune suppression may worsen infections.
• Liver issues: Monitoring liver function is crucial, especially post-kidney transplant.

Use During Pregnancy and Nursing

Azathioprine is contraindicated for rheumatoid arthritis during pregnancy but may be considered for transplant rejection prevention with careful risk-benefit assessment. It passes into breast milk, so nursing is generally not recommended.

Age Considerations

Safety and efficacy are not established for children under 18 or seniors over 65.

Dosage Guidelines

Dosing depends on age, condition severity, and individual response. Always follow your healthcare provider’s instructions.

Forms and Strengths

• Generic oral tablets: 25 mg, 50 mg, 75 mg, 100 mg
• Imuran oral tablets: 50 mg
• Azasan oral tablets: 25 mg, 50 mg, 75 mg, 100 mg

Kidney Transplant Dosage (Adults)

• Starting dose: 3–5 mg/kg daily at transplant time, sometimes 1–3 days prior.
• Maintenance dose: 1–3 mg/kg daily.

Rheumatoid Arthritis Dosage (Adults)

• Initial dose: 50–100 mg once daily or divided into two doses.
• Incremental increases after 6–8 weeks by 0.5 mg/kg/day as needed.
• Max dose: 2.5 mg/kg/day.
• Dose reductions may occur every 4 weeks.

Special Dosage Considerations

• Kidney impairment and TPMT deficiency may require dose adjustments.

Administration Tips

• Take after meals to minimize stomach upset.
• Store at 59°F to 77°F (15°C to 25°C), away from light, moisture, and do not freeze.
• Carry medication in original labeled container, especially while traveling.

Monitoring and Follow-up

• Regular blood tests to monitor blood counts, liver, and kidney function.
• TPMT enzyme testing before starting treatment.
• Watch for signs of infection or organ rejection.

Missed Dose and Overdose Instructions

If a dose is missed, take it as soon as possible unless it’s near the next scheduled dose. Never double dose. Overdose symptoms include nausea, vomiting, diarrhea, sore throat, fever, and chills. Seek immediate medical help if overdose is suspected.

Effectiveness Indicators

For kidney transplant patients, absence of rejection symptoms and normal kidney function tests indicate effectiveness. For rheumatoid arthritis, reduced joint pain, swelling, and improved mobility after approximately 12 weeks suggest benefit.

Alternatives and Consultation

Other treatment options exist for rheumatoid arthritis and transplant rejection prevention. Discuss with your healthcare provider to determine the best therapy tailored to your needs.

Note: This information aims to provide current, accurate data but does not replace professional medical advice. Always consult your healthcare provider before starting or changing any medication.

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