Ciclosporin A

Introduction - What is Ciclosporin A?

Ciclosporin A is an immunosuppressant, i.e. an active ingredient that suppresses the immune system and thus downregulates an immune response. For example, ciclosporin A can be used after the transplantation of various organs to prevent the body's immune system from attacking the foreign organ (transplant). Ciclosporin A is also used after a bone marrow transplant to prevent the stem cells used from being rejected. It can also be used to treat many autoimmune diseases.

Indications for ciclosporin A

As an immunosuppressive substance, Ciclosporin A prevents an unwanted reaction of the immune system against various cells. This results in the two most important indications for ciclosporin A:

• Transplants

• Autoimmune diseases

Ciclosporin A after transplants

In transplants, foreign material in the form of organs (kidneys, liver, lungs, heart, etc.), tissues (muscles, bones, skin, etc.) or cells (stem cells) is transplanted from a donor body into the recipient (sick person) ( transfer). Typically, the immune system reacts to the transplant with a pronounced immune reaction, as it recognizes it as “foreign” and wants to fight it off. This leads to a rejection reaction, the transplant can be damaged and may have to be removed again. In the worst case, the excessive activity of the immune system can lead to life-threatening complications. In order to moderate this reaction of the immune system, ciclosporin A is used alongside other immunosuppressants. It is important to strictly adhere to the correct active level, the patient must strictly adhere to the intake times planned by the doctor!

Find out more about the topic Organ transplants

Ciclosporin A in autoimmune diseases

Another important indication for cyclosporine A are autoimmune diseases. Here, too, there is a pronounced reaction of the immune system, albeit on the body's own cells. Well-known examples are rheumatoid arthritis (joint inflammation), psoriasis and the thyroid disease Hashimoto's thyroiditis. Ciclosporin A can be used to alleviate the symptoms, especially in the case of pronounced autoimmune processes.

Another area of ​​application are chronic inflammatory bowel diseases such as ulcerative colitis or Crohn's disease.

Read more about here Autoimmune diseases

Active ingredient and effect

Ciclosporin A is an active ingredient in the group of immunosuppressants. Ciclosporin uses a complex mechanism of action to prevent so-called cytokines (proteins that are required for an immune reaction in the body) from being formed. Ciclosporin A also has an effect on lymphocytes, an important group of cells that are also required to develop an immune response. Normally these lymphocytes need a molecular signal in order to become active, attack foreign substances and multiply. Treatment with Ciclosporin A can prevent both the activation and the proliferation of lymphocytes. The production of the cytokines normally takes place inside certain lymphocytes (the T lymphocytes). By inhibiting certain factors inside these T lymphocytes, fewer cytokines are produced and an immune response is suppressed or not occurring at all. Due to its properties, ciclosporin A has a very specific effect on a certain factor (Calcineurin) in T lymphocytes. This has the advantage that many other body functions can continue to run unhindered and fewer side effects occur, which is often a major problem with cortisone, which is also immunosuppressive. The active ingredient ciclosporin is obtained from the Norwegian mushroom species Beauveria nivea. There are several subspecies of ashlar mushrooms (Tolypocladium inflatum and Clindrocarpon lucidum).

Here you can learn more about the mechanisms of the Immune system

Side effects

Ciclosporin A is a drug that intervenes very strongly in processes of the immune system. This allows it to develop its strong effects, but at the same time it also causes many different side effects.
In the area of ​​blood formation, cyclosporine A leads to a reduction in various types of cells. The most common occurrence is a reduced number of leukocytes (white blood cells), but thrombocytes (blood platelets) and erythrocytes (red blood cells) can also be affected, this is referred to as aplastic anemia.
Ciclosporin A also often causes unspecific side effects such as headache, rise in blood pressure, nausea, vomiting, abdominal pain and diarrhea.
In addition, taking ciclosporin A can cause side effects in the nervous system. Both the central nervous system (brain and spinal cord) and the peripheral nervous system can be affected, inflammation of the nerves or even brain damage with confusion, disorientation and impaired consciousness.
Muscle cramps, fever and fatigue are also possible side effects of cyclosporine A.
While the liver is usually unaffected, ciclosporin A can affect the kidneys and cause kidney dysfunction. Effects on the endocrine system can lead to menstrual disorders, increased body hair and acne.

Ciclosporin A is a very potent drug, but also rich in side effects. If you experience any side effects from cyclosporine A, please speak to your doctor, who can then decide how to proceed!

Does ciclosporin A also cause hair loss?

Hair loss is not a typical side effect of ciclosporin A. In contrast to many other immune system active ingredients, which prevent the division and thus the reproduction of cells (including at the hair roots), ciclosporin A does not lead to hair loss. Instead, changes in the hormone balance tend to lead to increased body hair, which is a very unpleasant side effect, especially for women. The changed hormone levels not only lead to irregularities in the menstrual cycle, they can also cause an intensified male hair pattern with an increase in hair growth on the stomach, chest and face. Ciclosporin A is even used as an anti-hair loss agent in some cases.

Find out more here to the Hair loss

Interactions

Ciclosporin A is an active ingredient that is mainly processed in the liver and is also excreted through it. An important enzyme in this metabolic pathway is the so-called CYP3A4, which is involved in the excretion of many drugs. Ciclosporin A can therefore interact with all drugs that are also processed via CYP3A4. Medicines that inhibit CYP3A4 therefore lead to increased concentrations and thus increased effects of ciclosporin A. These include, for example, contraceptives, metoclopramide (against nausea) and prednisolone (a cortisone). Many antibiotics (especially from the group of macrolides and azole antibiotics) can cause interactions with ciclosporin A. In addition, even some foods such as grapefruit juice cause such an interaction.

The opposite effect, i.e. a weakening of the effect, occurs with so-called inducers of CYP3A4. These lead to an increased formation of the enzyme and thus indirectly to an increased excretion of ciclosporin A. The inducers of CYP3A4 include, for example, the antibiotic rifampicin or the herbal antidepressant St. John's wort (more precisely the hyperforin it contains).

Effectiveness of the pill

As already mentioned, ciclosporin A is metabolized in the liver by the enzyme CYP3A4, so all contraceptives that are also broken down in the liver or specifically by this enzyme can interact with ciclosporin A. Since the "pill" (i.e. the oral contraceptives) is also metabolized via CYP3A4, it inhibits the breakdown of ciclosporin A and thus increases the concentration and effect undesirably.

You can find out more about the topic here "Pill"

Contraindications - When should ciclosporin A not be given?

As with any other drug, the main contraindication for ciclosporin A is an allergy to the active ingredient or other components of the drug. In addition, it must not be combined with drugs that affect the enzyme CYP3A4. Dose reductions may need to be considered if such a combination is unavoidable. Further contraindications for ciclosporin A are malignant (malignant) diseases, since immunosuppression increases the risk of malignant degeneration. In the case of liver and kidney damage, cyclosporin A may only be given in special cases and with great caution. Furthermore, cyclosporine A can unbalance electrolytes (blood salts), which among other things leads to increased potassium, which is particularly dangerous for people with heart disease.

Use during pregnancy and breastfeeding

There are currently insufficient studies on the use of ciclosporin during pregnancy and breastfeeding. Animal experiments on rabbits and rats have shown that ciclosporin A can damage the child during pregnancy and while breastfeeding, which is why tests with ciclosporin A could not be carried out on humans during these phases. However, there are individual case reports of children whose mothers were treated with ciclosporin A during pregnancy. They have an increased risk of premature birth, and there was usually no organic damage. Due to the lack of data, however, a general statement is not possible. As a precaution, we advise against taking it during pregnancy and breastfeeding!

You can get an overview of the topic at pregnancy or Medication in Pregnancy or. Medication during breastfeeding

Eye drops with ciclosporin A

Ciclosporin A eye drops are used for severe inflammation of the eyes.The ciclosporin reduces the immune response in the eye, fewer inflammatory substances are produced and thus potential eye damage is reduced. For particularly severe inflammation of the cornea with dry eyes, these eye drops are the first choice. Ciclosporin A can also be used for endogenous uveitis (inflammation in the eye) caused by one's own body. It is either taken systemically in the form of tablets or given directly into the eyes as the active ingredient in the eye drops. Treatment with eye drops with cyclosporine A is often sufficient if you drip it into your eyes once a day before going to sleep. Since the eyes are then closed for several hours and are not stressed, the eye drops can work particularly well. Contraindications for eye drops with ciclosporin A exist in case of an allergy or hypersensitivity to the active substance. In addition, the eye drops must not be used at the same time as preparations containing cortisone. Even if there is a possibility of an infection in the eye, it should not be used because the active ingredient prevents the body from fighting the pathogens. Side effects of the eye drops are eye pain and increased watering of the eyes.

Dosages

Ciclosporin A is available in different dosages. Typical tablet dosages are 25 mg, 50 mg, or 100 mg. After a transplant, a dose of 10 to 15 mg per kilogram of body weight per day should be taken. As a rule, half the amount is taken in the morning and the other half in the evening. When administered via the vein, on the other hand, a dosage of 3 to 5 mg per kg of body weight is usually sufficient. After a period of 2 weeks, the dose may be reduced slightly depending on the response of the immune system. In the case of autoimmune diseases, the daily dose is usually somewhat lower, with a target dose of 5 mg per kg of body weight per day. In order to maintain the ideal amount of the active ingredient in the body, regular measurements of the drug level (i.e. the concentration in the blood) are necessary.

How much does Ciclosporin A cost?

In most cases, the costs for therapy with cyclosporine A are covered by the health insurance company or private health insurance. The drug should only be used if there is a medical indication, in which case the health insurance companies are obliged to pay the costs. Depending on the dosage (25 mg, 50 mg, 100 mg), 100 tablets of Ciclosporin A are available for 50 to 350 euros. Eye drops with ciclosporin A can be bought for 100 to 350 euros, depending on the concentration of the active ingredient and the pack size. For infusions with ciclosporin A, the prices also vary greatly depending on the concentration of the active ingredient and the size of the pack. All drugs that contain cyclosporine A require a prescription and are therefore not freely available in pharmacies.

Ciclosporin A and alcohol - are they compatible?

Like all drugs that are metabolized, broken down and excreted in the liver, alcohol can lead to changes in the concentration of cyclosporin A. Although there is no direct interaction between the two substances (ciclosporin A and alcohol), they can both cause liver damage. Anyone who already has a damaged liver due to increased alcohol consumption must expect increased complications when taking ciclosporin A. It is best to refrain from consuming alcohol while taking ciclosporin A, otherwise the liver will become overloaded and one or both substances will break down more slowly.

Alternatives to ciclosporin A

Ciclosporin A is a very effective and well-tested substance in the field of immunosuppressants, which is why the active ingredient is often used in the corresponding indications. Different alternatives can be used depending on the type of disease. Autoimmune diseases and diseases from the rheumatic type can be treated with cortisone, azathioprine, methotrexate, cyclophpsphamide and sulfasalazine, for example. Tacrolimus can also be used as an immunosuppressant for transplants or autoimmune diseases. There are also a number of so-called biologicals, substances that attack a specific point in the course of the immune response.

You can find one here Overview of all immunosupressants

Further information

• Immunosuppressants
• immune system
• Organ transplant
• Autoimmune diseases
• inflammatory bowel disease

Exclusion of liability / disclaimer

We would like to point out that medication must never be discontinued, applied or changed independently without consulting your doctor.
Please note that we cannot claim that our texts are complete or correct. The information may be out of date due to current developments.