Active Ingredients

Cyclosporine – Effect, Application & Risks

Cyclosporine

Cyclosporine is a drug that belongs to the immunosuppressants . It is obtained from the sac fungi Cylindrocarpon lucidum and Tolypocladium inflatum. Chemically, it is a cyclic peptide made up of eleven amino acids .

What is cyclosporine?

Cyclosporine is an immunosuppressant with a narrow therapeutic index. The gap between its intended therapeutic effect and its toxic effect is very small. Therefore, a blood level check must always be carried out when it is used.

Cyclosporine has a depressant effect on the immune system . It is therefore used in diseases that are characterized by an overreaction of the immune system. This includes the group of autoimmune diseases . Cyclosporine is also used to suppress rejection reactions in organ transplants .

It is a cyclic peptide made up of eleven amino acids. It occurs in higher concentrations in the Norwegian sac fungi Cylindrocarpon lucidum and Tolypocladium inflatum. Therefore, it is isolated from these fungi. Today, cyclosporine is synthetically produced for medical use. When isolated, it is a white solid that dissolves in alcohol , methanol, chloroform, or ether. It is administered orally as a capsule or tablet, or parenterally, bypassing the digestive tract (e.g. through an injection).

Due to its immunosuppressive effects, cyclosporine can also cause several side effects when used . However, the drug has revolutionized medicine in terms of rejection reactions in organ transplants. The survival time of the patients could be increased significantly. The active ingredient was discovered in the early 1970s by the Swiss microbiologists Hartmann Stähelin and Jean-François Borel.

Pharmacological action

The pharmacological action of cyclosporine is based on its inhibitory effect on the enzyme calcineurin. Calcineurin activates the synthesis of interleukins by stimulating the corresponding genes . The enzyme calcineurin is contained in T-lymphocytes and from there controls the synthesis of interleukin 2. As a messenger substance , interleukin 2 causes inflammatory reactions that serve to defend against foreign proteins ( bacteria , viruses ).

In autoimmune diseases, however, the body’s own proteins are attacked. To stimulate the immune system, calcineurin attaches itself to the protein NF-AT and dephosphorylates it. In the dephosphorylated state, this protein stimulates the corresponding genes to transcribe interleukins, which are responsible for the immune response.

This reaction cascade is inhibited by cyclosporine. To do this, cyclosporine attaches itself to certain receptors on the T lymphocytes. There it binds to so-called immunophilins (intracellular binding proteins) and forms a complex with them. This complex in turn binds to calcineurin. As a result, this enzyme is blocked and can no longer activate the transcription factor NF-AT by dephosphorylation. The further formation of interleukins stops, which weakens the body’s immune reactions.

Medical Application & Use

Cyclosporine is widely used in autoimmune diseases, psoriasis , inflammatory skin diseases, rheumatic diseases or organ transplants. In the case of autoimmune diseases, the immune system attacks its own body and, in the case of organ transplants, it attacks the transplanted organs in the form of rejection reactions. Organ transplant patients in particular benefit from the use of this drug. Since its use, the survival time of those affected has increased drastically.

Severe autoimmune diseases such as ulcerative colitis or glomerulonephritis can also be treated well. In ulcerative colitis, the intestines are attacked by the body’s own immune system. This disease is characterized by severe intestinal inflammation that can eventually destroy the intestines as well. Glomerulonephritis is an abacterial inflammation of the glomeruli of the kidneys . If left untreated, it can lead to severe kidney failure.

Psoriasis (psoriasis) can also be treated well by using cyclosporine. In inflammation of the conjunctiva and cornea , cyclosporine is used by topical application. Drugs containing cyclosporine are applied to the affected areas.

Typically, cyclosporine is also used in neurodermatitis . Atopic dermatitis is an inflammatory, highly itchy skin disease caused by allergic reactions . Finally, an important area of ​​application is rheumatoid arthritis . Rheumatoid arthritis is an autoimmune disease, in which the immune system attacks the body’s own joints.

Cyclosporine’s treatment spectrum also includes severe inflammatory eye diseases that can lead to blindness . Cyclosporine treatment is life-saving in many cases (organ transplants, severe organ-destroying autoimmune diseases). It also improves the quality of life of many patients with chronic inflammatory diseases.

Risks & side effects

Unfortunately, cyclosporine cannot be used without restrictions because it can cause many side effects. The side effects and contraindications result largely from the weakening of the immune system. Patients with infections must not be treated with cyclosporine. Immunosuppression could make the infection worse. Pregnant and breastfeeding women should also not be treated with cyclosporine, as the drug could have a harmful effect on the child.

The simultaneous use of phototherapy for psoriasis and treatment with cyclosporine increases the risk of skin cancer . Therapy with cyclosporine is also counterproductive in the case of kidney damage, since the kidneys can be further damaged. Overall, the use of cyclosporine increases the susceptibility to infection , which can be attributed to the reduced immune response . Gastrointestinal disturbances may occur initially, leading to diarrhea , nausea , and vomiting . Furthermore, the development of edema is possible. There may also be an increase in body hair .

The list of possible side effects is very long. However, these do not have to occur. However, indigestion , headaches , gingivitis or high blood pressure are more common. Therefore, blood tests and blood pressure measurements should be carried out regularly during treatment with cyclosporine .

Lisa Newlon
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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.