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Cyclosporin is a cyclic 11 amino acid polypeptide produced by the fungus Tolypocladium inflatum. Cyclosporin is a potent drug that acts as an immunosuppressant (that is, it inhibits the production of antibodies and immune cells by various agents called immunosuppressants).

What is cyclosporine used for?

  • prevention of transplant rejection

This applies to the majority of patients who have previously taken other immunosuppressive drugs, and for whom they have not fulfilled their role and are still at risk of transplant rejection. Ciclosporin prevents rejection of heart, kidney, liver, pancreas, small intestine, lung and skin allografts. Allogeneic means that it is a tissue or organ transplant from an individual of the same species.

  • in "graft versus host" disease

Cyclosporine significantly weakens the "graft versus host" reaction after bone marrow transplantation - it is an undesirable physiological reaction taking place in the organism of the transplant recipient under the influence of antigen-foreign lymphocytes introduced from the donor. The graft versus host disease entity is usually very severe and can even lead to the death of the patient.

  • with uveitis

This applies to the vision-threatening intermediate or posterior uveitis, especially when traditional treatments are ineffective, do not bring the desired effects or cause life or he alth-threatening side effects.

  • inflamed cornea

and precisely in the local treatment of severe keratitis in adults with dry eye syndrome, who did not improve despite the use of preparations designed to moisturize the eye, the so-called artificial tears.

  • in the treatment of nephrotic syndrome
  • with rheumatoid arthritis
  • to treat psoriasis
  • with atopic dermatitis

Immunosuppressive drugs are administered in the treatment of many autoimmune diseases. In their course, the immune system attacks its own cells and tissues (treats them as an enemy), which results in permanent damage.

Drugs inhibit the response of the systemimmune system, thanks to which they extend the periods of disease remission and alleviate symptoms in order to increase the patient's quality of life.

They are most often used in the aforementioned rheumatoid arthritis, psoriasis, but also in diseases such as

  • lupus
  • pemphigus
  • ulcerative enteritis
  • Crohn's disease

Contraindications to the use of cyclosporine

Like every drug, cyclosporine cannot always be used despite its indications.

The main contraindication is hypersensitivity to the active substance or any of the ingredients.

In addition, it should also be remembered that cyclosporine affects the entire body of the patient and it is not always beneficial for him. Therefore, before starting therapy, especially when the body is weakened, a thorough interview and research should be conducted.

The effect of cyclosporine on the body

Cyclosporine, like other immunosuppressive drugs, unfortunately increases the risk of developing lymphomas and other malignancies, mainly skin cancers. Due to the potential risk of skin malignancies, patients treated with cyclosporine should avoid excessive exposure to sunlight and should not be exposed to UVB radiation or photochemotherapy.

Cyclosporin, like other immunosuppressive drugs, also increases the risk of developing all kinds of infections: bacterial, fungal, parasitic, and viral, often caused by opportunistic microorganisms (i.e. those that cause infections, but only in people with lowered immunity, and they do not harm he althy people, whose body can deal with them without any problems).

Increased levels of creatinine and urea may be a frequent and serious complication of cyclosporine treatment. The concentration is dose-dependent and most often resolves after dose reduction. However, in the course of long-term treatment, changes in the structure of the kidneys may occur which are not so easy to treat. Therefore, renal function should be monitored during treatment with cyclosporine. Kidney function should be carefully monitored in the elderly and in children.

Ciclosporin may also cause a transient dose-dependent increase in serum bilirubin and increase in liver enzymes. This situation occurs most often in people with other comorbidities and a generally weakened organism. In people after organ transplants, unfortunately, these disorders very often lead to death. Therefore, it should be carefullymonitor liver function, and in the event of disturbances, it may be necessary to reduce the dose or switch to another drug.

Before treatment and after about a month of treatment with cyclosporine, it is also recommended to measure the level of blood lipids (i.e. total cholesterol, HDL, LDL and triglycerides).

In the event of an increase in lipids, a dietary change should be considered, and if this does not work, a reduction in the dose of ciclosporin may be necessary. It should be remembered that an increase in blood cholesterol, especially the "bad" cholesterol, may lead to serious diseases of the heart and the entire circulatory system. And this can be very dangerous for an already weakened organism.

Ciclosporin increases the risk of hyperkalaemia (increase in the concentration of potassium in the blood serum), especially in patients with known impaired renal function.

Caution should also be exercised when taking cyclosporine with potassium-sparing diuretics, ACE inhibitors, angiotensin receptor antagonists and drugs containing potassium concomitantly, and in patients on a high-potassium diet. In such a situation, it is recommended to regularly check the concentration of potassium in the blood plasma in order to avoid excess of it. It's also a good idea to take a closer look at your diet and lower your potassium intake if necessary.

Cyclosporine also increases the clearance (or excretion) of magnesium, which can lead to hypomagnesaemia (i.e. reduced levels of magnesium in the body). Therefore, you should remember to regularly control the concentration of this element in the blood, and if necessary, change your diet, introduce foods rich in magnesium or use magnesium supplementation.

When and with whom to be careful when using cyclosporine?

  • when using the drug in patients with psoriasis and atopic dermatitis

This mainly applies to elderly patients. They should only be treated for disabling psoriasis or atopic dermatitis, with regular kidney function checks, blood pressure measurements, and lipids checked.

Before starting treatment with cyclosporine, you should also undergo a thorough examination, preferably a biopsy of skin lesions uncharacteristic of psoriasis. Especially in cases where there is a risk that they are neoplastic changes or precancerous conditions.

  • during erythromycin therapy

Oral administration of erythromycin should be avoided as it has the ability to increase the concentration of cyclosporin in the blood. If no alternative treatment is available, he recommendsblood levels of ciclosporin and kidney function should be carefully monitored, and more attention should be paid to any disturbing symptoms. Simultaneous intake of cyclosporin and erythromycin increases the likelihood of side effects.

  • for malignant skin cancers

People with malignant skin cancers or precancerous skin conditions should be treated with cyclosporine only after appropriate treatment of these lesions and only if there is no other possibility of effective therapy, and then this treatment should be under strict medical supervision.

  • in case of skin infection with golden staph

Infection of the skin with staphylococcus aureus is not a contraindication to the use of the drug, but therapy with appropriate antibacterial drugs should be carried out in parallel, so that the entire body is not infected.

How and when to take cyclosporine?

Cyclosporine is taken orally, the doctor decides how often and in what doses after a thorough interview and basic tests.

It is best to take it with a meal, but be careful not to drink grapefruit juice during this time. This juice increases the effect of cyclosporine. To avoid drug interactions, do not drink grapefruit juice or eat grapefruit at least 4 hours before and 4 hours after taking the medicine.

You must not combine cyclosporine with preparations containing St. John's wort. This plant reduces the concentration of the drug in the blood plasma, which can lead to rejection of the transplant.

Cyclosporine and pregnancy and breastfeeding

Cyclosporin during pregnancy can only be used for life reasons, i.e. when it is a "life-saving" drug.

Experience with the use of the drug during pregnancy is limited.

Few studies have been conducted on animals only.

Breastfeeding is also not recommended as cyclosporine passes into breast milk and this can have an unpredictable effect on your baby.

Cyclosporine in the treatment of animals

Cyclosporine has been used in veterinary medicine for over twenty years. This drug is used, inter alia, in veterinary dermatology in the case of diseases such as:

  • atopic dermatitis
  • autoimmune diseases (e.g. pemphigus deciduous)
  • inflammation of the sebaceous glands
  • and in other, less common diseases

Cyclosporin side effects

Like all drugs, cyclosporine can cause side effects. They will not be the same in every patient. Theirthe intensity may also be different. It all depends on the general condition of the patient, other comorbidities and medications taken at the same time.

The main and most common side effects are:

  • hyperlipidemia, i.e. an increase in blood cholesterol levels (it may cause the development of atherosclerosis)
  • muscle tremors
  • excessive hair growth on the skin of the body and face
  • headaches and difficult-to-control hypertension
  • renal dysfunction
  • increased blood sugar (hyperglycemia)
  • increase in serum uric acid levels (hyperuricemia)
  • high potassium levels (hyperkalemia)
  • low levels of magnesium (hypomagnesaemia)
  • nausea, vomiting, stomach ache, diarrhea
  • seizures, confusion, disorientation
  • personality changes, agitation, insomnia, vision changes
  • blindness, coma, paralysis of part or all of the body, neck stiffness, loss of coordination

If the patient notices these or other disturbing symptoms during cyclosporine therapy, he should immediately see a doctor.

It should be remembered that the extreme irresponsibility is e.g. changing the dose independently or discontinuing treatment. This may endanger not only he alth, but also the life of the patient.

About the authorKarolina NowakA pharmaceutical technician by education. Currently, he is professionally fulfilled working in a pharmacy. Empathetic, sensitive and fond of contact with other people. Privately, a lover of a good book.

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