Azathioprine
Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.
More about the experts All content is checked by medical journalists.The active ingredient azathioprine is an immunosuppressant, i.e. a drug that suppresses the immune system. This is necessary for organ transplants and autoimmune diseases such as multiple sclerosis. The active ingredient has been used successfully in medicine for over fifty years. Possible azathioprine side effects include nausea, vomiting, and bone marrow inhibition. Here you can read everything you need to know about the effect of azathioprine, dosage and use.
This is how azathioprine works
Azathioprine is a so-called prodrug, i.e. a substance that is only converted into its actual active form in the body. As such, the active ingredient intervenes in the regeneration of the building blocks of the genetic make-up and inhibits them. In particular, cell types that multiply quickly can no longer be sufficiently formed. These include, in particular, the T and B cells of the immune system.
During transplants, foreign tissue (such as organs) is implanted in a patient. Normally, his immune system would take immediate action against the foreign tissue, causing a rejection reaction. Azathioprine keeps the immune system (sometimes in combination with other active ingredients) in check so that the body does not attack the new tissue.
Azathioprine is also a valuable therapeutic agent for autoimmune diseases in which the body attacks its own tissue, in order to suppress the overactive immune system.
Azathioprine uptake, breakdown and excretion
After ingestion, the active ingredient 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 is broken down. About half of the amount of azathioprine ingested leaves the body in the urine within a day.
When is azathioprine used?
The active ingredient azathioprine is used in combination with other immunosuppressive active ingredients to prevent rejection in organ transplants.
In addition, the active ingredient is used in autoimmune diseases when the anti-inflammatory cortisone is not tolerated or the dosage needs to be reduced. Examples of such autoimmune diseases are rheumatoid arthritis (chronic inflammation of the joints), Crohn's disease and ulcerative colitis (inflammatory bowel disease), multiple sclerosis, autoimmune hepatitis (inflammation of the liver) and certain autoimmune diseases such as lupus erythematosus. The application is usually long-term.
This is how azathioprine is used
The immunosuppressant is taken in the form of tablets. The dose depends on the therapy goal and body weight; The usual azathioprine dosage is one to five milligrams per kilogram of body weight per day.
The tablets should be taken with sufficient liquid at least one hour before or three hours after a meal or milk consumption in order not to hinder the absorption of the active substance from the intestine. They should not be divided or crushed. If sharing is absolutely necessary, the skin should not come into contact with the tablet dust or the break edge (the active ingredient is mutagenic and potentially carcinogenic).
What are the side effects of azathioprine?
Azathioprine side effects such as infections, lack of white blood cells (leukopenia), nausea, loss of appetite and vomiting occur in more than one in ten people treated.
One in ten to one hundredth patients develops benign or malignant tumors, a lack of blood platelets (thrombocytopenia), anemia, inflammation of the pancreas or liver dysfunction.
What should be considered when taking azathioprine?
Azathioprine can interact with a number of other active substances:
The gout active ingredients allopurinol, oxipurinol and thiopurinol, like azathioprine, intervene in the purine metabolism, which means that the immunosuppressant can only be broken down very slowly. If taken at the same time, the dose of the immunosuppressant must therefore be reduced.
Other active ingredients that are used in inflammatory bowel diseases (such as mesalazine, olsalazine and sulfasalazine, inhibit the breakdown of azathioprine. Crohn's disease and ulcerative colitis are the two most common chronic inflammatory bowel diseases.
Azathioprine inhibits the production of blood cells in the bone marrow. This effect can be intensified by taking other active ingredients at the same time. This applies to antihypertensive drugs from the group of ACE inhibitors (ramipril, enalapril etc.), cotrimoxazole (antibiotic), cimetidine (gastric acid inhibitor) and indomethacin (pain reliever).
Azathioprine should only be used in very low doses in patients with liver and kidney problems. In the case of severe liver dysfunction, the immunosuppressant must not be used at all.
As a mutagenic and possibly carcinogenic active ingredient, azathioprine must not be used in pregnant or breastfeeding women. The immunosuppressant should not be used in children and adolescents under 18 years of age either, as insufficient data on its effectiveness and safety are available.
How to get medicines with azathioprine
Azathioprine is a prescription drug in any dosage, so it is only available at the pharmacy after a doctor's prescription.
How long has azathioprine been 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 active ingredient can also suppress immune reactions. In combination with a cortisone, the first successful kidney transplant succeeded. Azathioprine was partially replaced by cyclosporine (another immunosuppressant) in 1978, but is still in use.
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