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Azathioprine
| Generic Name | Azathioprine |
| Brand Names/Synonymes | ATP, Azamun, Azanin, Azasan, Azathioprin, Azathioprine Sodium, Azatioprin, Azothioprine, Ccucol, Imuran, Imurek, Imurel, Muran, Rorasul
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| Habit Forming? |
No |
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| Requires Prescription? |
Yes |
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| Drug Class |
Immunosuppressant, antirheumatic
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| Pharmacology |
Azathioprine is a chemotherapy drug, now rarely used for chemotherapy but more for immunosuppression in organ transplantation and autoimmune disease such as rheumatoid arthritis or inflammatory bowel disease or Crohn's disease.
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| Time Lapse Before Drug Works |
6 to 8 weeks |
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MeSH Classification
Organic Chemicals: Sulfur Compounds: Thionucleosides: Azathioprine
Indication
For use as an adjunct in the prevention of rejection in renal homotransplantation. Also for the management of severe, active rheumatoid arthritis unresponsive to rest, aspirin or other nonsteroidal anti-inflammatory drugs, or to agents in the class of which gold is an example. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed)
Other Uses
Azathioprine is also used to treat ulcerative colitis (a condition in which sores develop in the intestine causing pain and diarrhea). Talk to your doctor about the possible risks of using this drug for your condition. This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.
Mechanism of Action
Azathioprine antagonizes purine metabolism and may inhibit synthesis of DNA, RNA, and proteins. It may also interfere with cellular metabolism and inhibit mitosis. The mechanism of action of azathioprine in rheumatoid arthritis is not known but is most likely related to its immunosuppresive action.
Possible Adverse Reactions
| SYMPTOMS |
WHAT TO DO |
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LIFE-THREATENING SYMPTOMS
Rapid heart rate, sudden fever, muscle or joint pain, cough, shortness of breath. |
Seek emergency treatment immediately.
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COMMON SYMPTOMS
Infection or low blood count causing fever and chills; back pain; cough; painful urination; anemia (tiredness or weakness); nausea; vomiting; loss of appetite |
Continue. Call doctor. |
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INFREQUENT SYMPTOMS
Jaundice (yellow eyes, skin); skin rash. |
Discontinue. Call doctor right away. |
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RARE SYMPTOMS
Low platelet count causing bleeding or bruising; tarry or black stools; bloody urine; red spots under skin; severe abdominal pain; mouth sores. |
Discontinue. Call doctor right away. |
The two cytotoxic drugs most commonly used as immunosuppressants are azathioprine and cyclophosphamide. Both interfere with DNA synthesis and have their major pharmacological action on dividing tissues. They were developed originally to treat cancer and, after observations that they were cytotoxic to dividing lymphocytes, were found to be immunosuppressive as well. The use of these compounds is limited by a range of toxic effects on tissues that have in common the property of continuous cell division. These effects include decreased immune function, as well as anemia, leukopenia, thrombocytopenia, damage to intestinal epithelium, hair loss, and fetal death or injury. As a result of their toxicity, these drugs are used at high doses only when the aim is to eliminate all dividing lymphocytes, and in these cases treated patients require subsequent bone marrow transplantation to restore their hematopoietic function. They are used at lower doses, and in combination with other drugs such as corticosteroids, to treat unwanted immune responses.
Azathioprine, and cyclophosphamide are teratogenic and reduce fertility.
KEY TERMS
Immunosuppressive Drugs - Agents that suppress immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-CELLS or by inhibiting the activation of HELPER CELLS. While immunosuppression has been brought about in the past primarily to prevent rejection of transplanted organs, new applications involving mediation of the effects of INTERLEUKINS and other CYTOKINES are emerging.
Antirheumatic Drugs - Drugs that are used to treat rheumatoid arthritis.
More Information:
1. The MedMasterTM Patient Drug Information database, American Society of Health-System Pharmacists, Inc.
2. National Library of Medicine - Medical Subject Headings
3. DrugBank database, Wishart DS et al., DrugBank: a comprehensive resource for in silico drug discovery and exploration
4. Complete Guide to Prescription and Nonprescription Drugs, H. Winter Griffith, M.D.
5. Immunobiology : the immune system in health and disease / Charles A. Janeway, Jr. [et al.]
6. Spinal Cord Medicine Principles and Practice Vernon W. Lin, M.D., Ph.D.
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