Active ingredient and effect | Ciclosporin A

Active ingredient and effect

Ciclosporin A is an active ingredient of the immunosuppressive group. By means of a complex mechanism of action, Ciclosporin prevents the formation of so-called cytokines (proteins required for an immune reaction in the body). In addition, Ciclosporin A has an effect on lymphocytes, an important group of cells that are also needed for the formation of an immune reaction.

Normally, these lymphocytes need a molecular signal to become active, attack foreign substances and multiply. Treatment with Ciclosporin A can prevent both activation and proliferation of the lymphocytes. The production of 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 absent. 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 bodily functions can continue to run unhindered and fewer side effects occur, which is often a major problem with the likewise immunosuppressive cortisone. The active substance Ciclosporin is extracted from the Norwegian fungus species Beauveria nivea. These are several subspecies of tubular fungi (Tolypocladium inflatum and Clindrocarpon lucidum).

Side effects

Ciclosporin A is a drug that strongly interferes with processes of the immune system. This allows it to unfold its strong effect, but also causes many different side effects. In the area of blood formation, Ciclosporin A leads to a reduction of various cell types.

The most common is a reduced number of leukocytes (white blood cells), but thrombocytes (blood platelets) and erythrocytes (red blood cells) can also be affected, this is called aplastic anemia. Ciclosporin A also frequently causes unspecific side effects such as headaches, an increase in blood pressure, nausea, vomiting, abdominal pain and diarrhea. In addition, taking Ciclosporin A can cause side effects in the area of the nervous system.Both the central nervous system (brain and spinal cord) and the peripheral nervous system can be affected, nerve inflammation or even brain damage with confusion, disorientation and disturbances of consciousness can occur.

Muscle cramps, fever and fatigue are also possible side effects of Ciclosporin A. While the liver is usually not affected, Ciclosporin A can affect the kidneys and lead to kidney dysfunction. Effects on the endocrine system can lead to menstrual disorders, increased body hair and acne.

Ciclosporin A is therefore a very potent drug, but also has many side effects. If you should experience side effects from Ciclosporin A, please talk to your treating physician, who can then decide on the further procedure! Hair loss is not a typical side effect of Ciclosporin A.

In contrast to many other immune system agents, which prevent the division and thus the proliferation of cells (also at the hair root), Ciclosporin A does not lead to hair loss. Instead, due to changes in the hormone balance, it rather leads to increased body hair, a very unpleasant side effect, especially for women. Thus, the changed hormone levels not only lead to irregularities in the menstrual cycle, they can also cause an increased male pattern of hair growth with an increase in hair growth on the belly, chest area and face.

In some cases, Ciclosporin A is even used as a hair loss remedy. Ciclosporin A is an active ingredient that is mainly processed in the liver and is also excreted via the liver. An important enzyme of 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. Drugs that inhibit CYP3A4 therefore lead to increased concentrations and thus to an increased effect of Ciclosporin A. These include contraceptives, metoclopramide (for nausea) and prednisolone (a cortisone).

Also 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 can cause such an interaction. The opposite effect, i.e. a weakening of the effect, occurs with so-called inductors of CYP3A4.

These lead to an increased formation of the enzyme and thus indirectly to an increased excretion of Ciclosporin A. Among the inducers of CYP3A4 are, for example, the antibiotic rifampicin or the herbal antidepressant St. John’s wort (more precisely, the hyperforin it contains). As already mentioned, Ciclosporin A is metabolized in the liver via the enzyme CYP3A4, so all contraceptives that are also broken down in the liver or specifically via this enzyme can interact with Ciclosporin A.

Since the “pill” (i.e. oral contraceptives) is also metabolized via CYP3A4, it inhibits the breakdown of Ciclosporin A and thus increases the concentration or effect undesirably. As with any other drug, the most important contraindication for Ciclosporin A is an allergy to the active ingredient or other components of the drug. Furthermore, it must not be combined with drugs that influence the enzyme CYP3A4.

If necessary, dose reductions must be considered if such a combination is unavoidable. Other contraindications for Ciclosporin A are malignant diseases, as immunosuppression increases the risk of malignant degeneration. Ciclosporin A may also be given to patients with liver and kidney damage only in special cases and with great caution.

In addition, Ciclosporin A can bring the electrolytes (blood salts) out of balance, which leads to increased potassium, among other things, which is particularly dangerous for people with heart disease. For the intake of Ciclosporin during pregnancy and lactation there is currently no sufficient study situation. In animal experiments on rabbits and rats, it was shown that Ciclosporin A can cause damage to the child during pregnancy and lactation, which is why no tests with Ciclosporin A could be carried out on humans in 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 organic damage was usually not detected. Due to the lack of data, a general statement is not possible, however, and we advise against taking Ciclosporin A during pregnancy and lactation as a precaution!You can get an overview of the topic under Pregnancy or Medicines in Pregnancy or Medicines during Breastfeeding