Azathioprine

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Generic Name of Azathioprine - Learn More

Azathioprine

Azathioprine Precaution - What You Need to Know

Before initiating treatment with Azathioprine, patients must consult with their healthcare provider due to the following precautions:

- Bone Marrow Suppression: Azathioprine can cause bone marrow suppression, leading to leukopenia, thrombocytopenia, or anemia. Regular blood tests are necessary to monitor blood cell counts, particularly during the first few months of treatment.
- Infections: Azathioprine suppresses the immune system, increasing the risk of infections. Patients should be closely monitored for any signs of infection, and live vaccines should be avoided due to the risk of infection from weakened vaccines.
- Liver Toxicity: Azathioprine can cause liver toxicity, so liver function should be regularly assessed. Elevated liver enzymes or jaundice may indicate liver damage, and the medication may need to be discontinued or adjusted.
- Pregnancy and Lactation: Azathioprine is classified as a pregnancy category D drug, meaning it may cause harm to the fetus. It should only be used during pregnancy if the benefits outweigh the risks. It is also excreted in breast milk, so breastfeeding is not recommended during treatment.
- Caution in Patients with TPMT Deficiency: Patients with thiopurine methyltransferase (TPMT) deficiency are at increased risk of severe myelosuppression with Azathioprine use. Genetic testing for TPMT activity is recommended before starting treatment to assess the appropriate dose.
- Kidney Disease: Azathioprine should be used cautiously in patients with preexisting kidney dysfunction, as impaired renal function may affect drug metabolism.

Azathioprine Indication - Uses and Benefits

Azathioprine is primarily used to treat a variety of conditions, particularly autoimmune diseases and organ transplant recipients:

- Autoimmune Diseases: Azathioprine is used to manage diseases where the immune system attacks the body’s own tissues, such as:
- Rheumatoid Arthritis: To suppress immune activity in autoimmune joint inflammation.
- Systemic Lupus Erythematosus (SLE): To prevent flare-ups and manage the disease.
- Crohn’s Disease and Ulcerative Colitis: To control inflammation in the digestive tract.
- Autoimmune Hepatitis: To manage inflammation in the liver.

- Organ Transplantation: It is used as an immunosuppressive agent to prevent organ rejection following kidney, liver, heart, or other organ transplants. Azathioprine works by inhibiting the proliferation of immune cells that would attack the transplanted organ.

Azathioprine Contraindications - Important Warnings

Azathioprine should not be used in the following situations:

- Hypersensitivity: Patients with a known hypersensitivity or allergic reaction to Azathioprine or its components should avoid its use.
- Severe Liver Disease: Azathioprine is contraindicated in patients with severe liver disease due to its potential to worsen liver function.
- Pregnancy: Azathioprine should be avoided during pregnancy unless absolutely necessary, as it has been associated with birth defects, miscarriage, and preterm birth.
- Active Infections: Azathioprine should not be given to patients with active infections, as it can further suppress the immune system, exacerbating the infection.
- TPMT Deficiency: Azathioprine is contraindicated in individuals with TPMT (thiopurine methyltransferase) deficiency without dose adjustment, as they may experience severe bone marrow suppression.

Azathioprine Side Effects - What to Expect

Common side effects associated with Azathioprine include:

- Gastrointestinal Disturbances: Nausea, vomiting, diarrhea, and abdominal pain are common early side effects, especially at higher doses.
- Bone Marrow Suppression: Azathioprine can cause leukopenia (reduction in white blood cells), thrombocytopenia (reduction in platelets), and anemia (reduction in red blood cells), increasing the risk of infections and bleeding.
- Liver Toxicity: Elevated liver enzymes, jaundice (yellowing of the skin or eyes), and other signs of liver damage can occur, requiring frequent liver function monitoring.
- Infections: Due to immune suppression, patients on Azathioprine are at an increased risk for opportunistic infections, including bacterial, fungal, and viral infections.
- Pancreatitis: Azathioprine may lead to inflammation of the pancreas (pancreatitis), which can be severe and require immediate discontinuation of the drug.

Serious adverse effects include:

- Bone Marrow Failure: Azathioprine-induced bone marrow failure can lead to severe neutropenia and anemia, which are life-threatening conditions requiring immediate medical attention.
- Cancer Risk: Long-term use of Azathioprine may increase the risk of developing lymphomas or other types of cancer, particularly in patients who have undergone organ transplantation.

Azathioprine Pregnancy Category ID - Safety Information

4

Azathioprine Mode of Action - How It Works

Azathioprine works by inhibiting the synthesis of purines, which are essential building blocks of DNA and RNA. As a purine analogue, Azathioprine interferes with the proliferation of immune cells, particularly T lymphocytes, by blocking the enzymes required for purine metabolism.

- Immunosuppressive Effect: By preventing the proliferation of immune cells, Azathioprine suppresses immune responses, thus helping to prevent the immune system from attacking the body’s own tissues in autoimmune diseases or from rejecting transplanted organs.
- Metabolism: Azathioprine is metabolized in the liver to 6-mercaptopurine, which exerts the immunosuppressive effects. This conversion is influenced by the enzyme TPMT, and genetic variation in TPMT levels can affect how well the drug works and how toxic it may be for an individual.

Azathioprine Drug Interactions - What to Avoid

Azathioprine can interact with several other medications, affecting its efficacy and safety:

- Allopurinol: The combination of Azathioprine with allopurinol, a medication used for gout, can significantly increase Azathioprine’s toxicity, especially in patients with TPMT deficiency. Dose reduction of Azathioprine is necessary when used with allopurinol.
- ACE Inhibitors: The concurrent use of angiotensin-converting enzyme (ACE) inhibitors with Azathioprine may increase the risk of myelosuppression and renal toxicity, requiring close monitoring.
- Vaccines: Azathioprine suppresses the immune system, which may reduce the efficacy of live vaccines (e.g., measles, mumps, rubella vaccine). Live vaccines should be avoided in patients receiving Azathioprine.
- Warfarin: Azathioprine may enhance the effects of warfarin, an anticoagulant, increasing the risk of bleeding. Regular monitoring of INR (International Normalized Ratio) is advised when Azathioprine is used alongside warfarin.
- Rifampin: The antibiotic rifampin can reduce the efficacy of Azathioprine by increasing its metabolism, thus requiring dose adjustments.

It is essential to inform healthcare providers of all current medications, including over-the-counter drugs and supplements, to prevent any harmful interactions.

Azathioprine Adult Dose - Recommended Dosage

The dosing of Azathioprine varies depending on the condition being treated:

- For Autoimmune Diseases: The typical starting dose for adults is 1-3 mg/kg body weight per day. The dose may be adjusted based on clinical response and tolerance, and regular blood tests are required to monitor for bone marrow suppression.
- For Organ Transplantation: In transplant recipients, the dose usually starts at 3-5 mg/kg body weight per day, with adjustments made based on the patient’s response and blood counts.

- The dose may need to be reduced in cases of liver impairment, bone marrow suppression, or when combined with other medications that affect Azathioprine metabolism.

Azathioprine Child Dose - Dosage for Children

In pediatric patients, the dosing of Azathioprine is similar to adults, typically based on weight:

- For Autoimmune Diseases or Transplantation: The recommended dose is usually 1-3 mg/kg body weight per day for children. The dose should be carefully adjusted according to the child's response to therapy and the monitoring of blood cell counts.

It is essential for patients, including children, to consult their healthcare provider before starting Azathioprine to ensure the proper dosing and to minimize the risk of side effects.

Azathioprine Renal Dose - Dosage for Kidney Conditions

Azathioprine should be used with caution in patients with renal impairment, as renal dysfunction can reduce the elimination of the drug and increase the risk of toxicity. In cases of mild to moderate renal impairment, the dose of Azathioprine should be reduced, and kidney function should be closely monitored. Severe renal impairment may require further dose adjustment or discontinuation of the drug.