Last Updated on May 23, 2023
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What is azathioprine?
The active ingredient azathioprine is an immunosuppressant, a drug that suppresses the immune system. This is necessary in organ transplants and autoimmune diseases such as multiple sclerosis. The drug has been used successfully in medicine for over fifty years. Possible side effects of azathioprine include nausea, vomiting and bone marrow suppression. Read about the effects of azathioprine, dosage and administration.
How Azathioprine works?
Azathioprine is a prodrug, i.e. a substance that is only converted into the active ingredient in the body. As a prodrug, azathioprine interferes with the formation of the genetic building blocks. As a result, certain types of cells that multiply rapidly are no longer formed in sufficient numbers. These include the T and B cells of the immune system.
In transplantation, foreign tissue (such as organs) is implanted into a patient. Normally, your immune system would immediately attack the foreign tissue, leading to a rejection reaction. Azathioprine (sometimes in combination with other drugs) keeps the immune system in check so that the body does not attack the new tissue.
In autoimmune diseases, where the body attacks its own tissues, azathioprine is also a valuable therapeutic to suppress the overactive immune system.
Absorption, degradation and elimination of azathioprine
After ingestion, the drug is absorbed from the intestine into the blood. The highest blood levels are reached one to two hours after ingestion. After about four hours, half of the active ingredient has been metabolized. Within a day, about half of the azathioprine taken leaves the body through the urine.
When should you use Azathioprine?
The active ingredient azathioprine is used in combination with other immunosuppressants to prevent organ transplant rejection.
The drug is also used in autoimmune diseases when the anti-inflammatory drug cortisone is not tolerated or its dosage needs to be reduced. Examples of such autoimmune diseases are rheumatoid arthritis (chronic inflammation of the joints), autoimmune hepatitis (inflammation of the liver) and certain skin diseases such as lupus erythematosus. Use is usually long-term.
How is Azathioprine used?
The immunosuppressant is taken in tablet form. The dose depends on the goal of therapy and body weight; the usual dose of azathioprine is one to five milligrams per kilogram of body weight per day.
The tablets should be taken with a meal to reduce the risk of nausea. They should not be broken or crushed. If crushing is absolutely necessary, do not allow the tablet dust or broken edge to come into contact with the skin (the active ingredient is mutagenic and potentially carcinogenic).
What side effects does Azathioprine?
More than one in ten people treated with azathioprine experience side effects such as infections, low white blood cells (leukopenia), nausea, loss of appetite and vomiting.
Benign or malignant tumours, low blood platelet counts (thrombocytopenia), anaemia, inflammation of the pancreas or liver dysfunction occur in one in ten to one in one hundred patients.
What should I watch out for when taking azathioprine?
Azathioprine can interact with a number of other drugs:
The gout medications oxipurinol and thiopurinol interfere with the purine metabolism like azathioprine, and the immunosuppressant cannot be broken down very slowly. The dosage of the immunosuppressant must therefore be reduced.
Other drugs used for inflammatory bowel diseases (such as mesalazine, olsalazine and sulfasalazine) also inhibit the breakdown of azathioprine. Crohn’s disease and ulcerative colitis are the two most common inflammatory bowel diseases.
Azathioprine inhibits the formation of blood cells in the bone marrow. This effect can be increased by the use of other medicines. This includes high blood pressure medicines from the ACE inhibitor group (ramipril, enalapril, etc.), cotrimoxazole (antibiotic), cimetidine (stomach acid inhibitor) and indomethacin (painkiller).
Patients with liver or kidney disease should be given very low doses of azathioprine. This immunosuppressant should not be used in patients with severe liver dysfunction.
As a mutagenic and potentially carcinogenic drug, azathioprine must not be used in pregnant or breastfeeding women. Azathioprine should not be used in children and adolescents under the age of 18 due to insufficient data on efficacy and safety.
How to get Azathioprine?
Azathioprine is a prescription medicine in every dose, so it is only available from pharmacies on prescription.
How long has Azathioprine known?
Azathioprine was first produced as a chemotherapy drug in 1957 by scientists George Hitchings and Gertrude Elion. In the years that followed, it was discovered that the drug could also suppress immune responses. Combined with cortisone, it led to the first successful kidney transplant (1962). Azathioprine was partially replaced by cyclosporine (another immunosuppressant) in 1978, but is still in use.