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Last Updated on January 15, 2019

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The active ingredient Azathioprine is an immunosuppressant, thus an agent that suppresses the immune system. This is necessary in organ transplantation and autoimmune diseases such as multiple sclerosis. The drug is already successfully used for over fifty years in medicine. Possible side effects include Azathioprine as nausea, vomiting and myelosuppression. Here you can read everything about the effect of Azathioprine, Dosage and administration.

How Azathioprine works

is a so-called prodrug Azathioprine, that is, a substance which is converted into the actual active drug only in the body. As such, the active ingredient in the formation of the meshes of the genetic building blocks and inhibits it. Thus, in particular cell types, which multiply rapidly, no longer be adequately formed. This includes particularly the T- and B-cells of the immune system.

When transplants is implanted a patient foreign tissue (such as organs). Normally, your immune system would immediately take action against the foreign tissue, resulting in a rejection reaction. Azathioprine keeps the immune system (still partially in combination with other agents) as far in chess that the body does not attack the new tissue.

Also in autoimmune diseases in which the body attacks its own tissues, Azathioprine is a valuable therapeutic to suppress the overactive immune system.

Up, degradation and excretion of Azathioprine

After taking the drug from the intestine is absorbed into the blood. The highest blood levels are reached one to two hours after ingestion. After about four hours, the half of the active substance is degraded. Within a day, leaving about half of ingested Azathioprine amount the body through the urine.

When to use Azathioprine?

The active ingredient Azathioprine is used in combination with other immunosuppressive agents for the prevention of rejection in organ transplantation.

In addition, the drug comes in autoimmune diseases apply if the anti-inflammatory drug cortisone is not tolerated or its dosage should be reduced. Examples of such autoimmune diseases are rheumatoid arthritis (chronic inflammation of the joints), autoimmune hepatitis (inflammation of liver) and certain skin diseases such as lupus erythematosus. The application is usually carried out in the long term.

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How is Azathioprine used

The immunosuppressant is taken in pill form. The dose depends on the goal of therapy and body weight; usual dose of Azathioprine is a one to five milligrams per kilogram of body weight per day.

The tablets should be taken with sufficient liquid at a meal to reduce the risk of nausea. They should not be divided, or crushed. If a parts strictly necessary, the skin should not be with the tablet dust or the broken edge coming into contact (the active substance is mutagenic and potentially carcinogenic).

What side effects does Azathioprine?

With more than one in ten patients treated occur Azathioprine side effects such as infections, lack of white blood cells (leukopenia), nausea, loss of appetite and vomiting.

With every tenth to hundredth patients develop benign or malignant tumors, low platelet count (thrombocytopenia), anemia, inflammation of the pancreas or liver dysfunction.

What should be considered when taking Azathioprine?

Azathioprine may enter into interactions with a number of other active ingredients:

The gout agents, oxipurinol and thiopurinol grab as Azathioprine in the purine metabolism, whereby the immunosuppressive just can not be broken down very slowly. Concomitant administration therefore the dosage of the immunosuppressive agent must be reduced.

Also, other active ingredients, which 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 inflammatory bowel diseases.

Azathioprine inhibits the formation of blood cells in bone marrow. This effect can be enhanced by the concomitant use of other drugs. This applies, for example high blood pressure medicines from the group of ACE inhibitors (Ramipril, Enalapril etc.), cotrimoxazole (antibiotic), cimetidine (gastric acid inhibitors) and Indomethacin (painkillers).

In patients with liver and kidney disease Azathioprine must be metered very low. In case of severe hepatic dysfunction the immunosuppressant may not be applied.

As a mutagenic and potentially carcinogenic drug may Azathioprine not be used in pregnant and breastfeeding women. Even in children and adolescents under 18 years the immunosuppressant should not be used, as insufficient data on efficacy and safety are available.

How to obtain drugs with Azathioprine

Azathioprine is in each dose a prescription medication, so only available by medical prescription at the pharmacy.

How long has Azathioprine known?

Azathioprine was first produced in 1957 as a chemotherapeutic agent by the scientists George Hitchings and Gertrude Elion. In the years that followed it was discovered that the drug can also suppress immune responses. In combination with a cortisone succeeded in the result, the first successful kidney transplant (1962). Azathioprine was established in 1978 partially replaced by ciclosporin (another immunosuppressant), but is still in use.