"Cyclosporine": instructions for use. "Cyclosporin A": the instruction. Eye drops with cyclosporine

In nature, there are substances that can suppress cellular and humoral immunity in the animal body, carried out by T-lymphocytes. This allowed the successful organ transplantation and treatment of diseases associated with immune system disorders. One such natural compound is cyclosporin.

Description

The discovery of this substance is associated with the study of fungal strains of Tolypocladium inflatum and Cylindrocarpon lucidum. Biologically active substances synthesized by them, such as cyclosporin A and C, exhibit immunological activity against blood lymphocyte cells. This feature was first discovered in 1972 by scientists from the Swiss laboratory of the company Sandoz. It was found that the chemical structure of cyclosporin is a neutral lipophilic cyclic endecapeptide with a pronounced specific immunosuppressive effect.

Preparations based on it have a selective effect on T-lymphocytes, suppress cellular and humoral immunity. Cyclosporine in the blood inhibits the production of lymphokines, which reduces lymphocyte activity, but does not affect the process of hematopoiesis and the work of phagocytes, which indicates the selective action of this compound in the body.

Dosage forms

Be sure to accompany the medication containing cyclosporine, instructions for use. Among other things, it includes information on the form of release of the medicine. Preparations with this substance are released as:

• Soft capsules with a dosage of 25, 50 and 100 milligrams;
• Alcohol solution for oral administration with 100 milligrams of cyclosporine in one milliliter of solution;
• Oily solution for oral administration with 100 milligrams of cyclosporine in one milliliter of solution;
• Concentrate for making a solution for infusion with 50 and 650 milligrams of cyclosporine in one milliliter;
• Eye drops with 500 micrograms of cyclosporine in one milliliter.

Depending on the dosage form, the application will be different: for internal administration, for injection, for topical administration.

It is believed that the rate of absorption of the active component, the time of accumulation of the highest concentration in the blood, capsules and internal solution are considered equivalent.

The drug "Ciclosporin": analogues

On the pharmaceutical market, there are a number of medicines manufactured in the same pharmaceutical form and having practically the same effect. The active substance in them is cyclosporin. Instructions for the use of synonyms of immunosuppressants are considered as interchangeable medicines for the suppression of immune reactions.

Among the encapsulated drugs in the soft gelatin shell and liquid solutions, the original is the drug "Sandimmun Neoral" manufactured by the Swiss pharmaceutical company Novartis. The remaining drugs are considered to be reproduced in the likeness of the first created composition with the substance cyclosporin. Analogues such as the preparations "Cyclosporine Hexal", "Ecoral", "Cycloprene", "Cyclosporin A", are released in the form of capsules or solution for internal administration or injections.

Their main purpose is to reduce rejection during transplantation of internal organs or bone marrow. They are also treated with autoimmune diseases, as evidenced by the instructions for use applied to the preparation "Ciclosporin". Analogs have the same characteristics and indications for use.

The mechanism of action of the drug "Ciclosporin A"

The effect of all immunosuppressive drugs is based on the selective effect on T-lymphocytes. Not an exception and the drug "Cyclosporin A". The instruction details the basic pharmacodynamic mechanisms of the action of the active component, which combines with the receptor formations within the cells. There is a decrease in the production of interleukins and interferon, the expression of IL-2 receptors decreases.

The medication "Ciclosporin A" reduces the production of antibodies directed at the cells and tissues of the body, which they consider to be foreign and destroy. This feature allows to reduce immunological disorders and reduce the activity of autoimmune diseases.

The effectiveness of "Ciclosporin A" against allografts is great. The reason for the rejection of transplanted tissues and organs is the activation of immunity, created by T cells. They are actively beginning to be produced under the influence of transplantation antigens and to affect the cells of the graft, leading to their death.

The action of the immunosuppressant leads to blocking of the T cell link and inhibition of T lymphocytes arising from immune reactions. Consequently, the effectiveness of the drug "Cyclosporin A" (the instruction indicates this) is achieved only after suppressing antigens of the graft. By destroying the relationship between the antigen and the antibody, necrosis of the cells of the transplanted organs is prevented.

Why use

Indication for the use of the drug "Ciclosporin" instruction for use divides into two categories.

The first is transplantation or transplantation of donor tissues and organs. The medication is used to prevent the rejection of a grafted organ or tissue. Usually, skin, heart, bone marrow, lungs, liver, kidney, pancreas are used as transplants. It is possible to use the drug to eliminate rejection when using other immunosuppressors. The second category includes autoimmune diseases in severe form. Also, the remedy is prescribed at low efficacy of other drugs.

What diseases are treated with the drug "Ciclosporin"? Instructions for use in the number of indications distinguishes acute forms of atopic dermatitis and neurodermatitis, manifestations of psoriasis, rheumatoid arthritis, in which small joints are affected and inflamed. It is possible to use in uveitis in the middle and posterior regions of the eye, when the choroid and retina inflame, and the nephrotic syndrome of hormone-dependent and hormone-resistant nature.

Rules of admission

Treatment with the drug is recommended only under medical supervision in a hospital. Usually, internal use or intravenous drip is used, although preference is given to ingestion of the solution or capsules.

The utensils used to prepare a solution for intravenous injection should be made of glass, and not of polyvinyl chloride, so that there is no reaction with castor oil.

To dilute the concentrate used physiological 0.9-percent solution of sodium chloride or a 5-percent solution of glucose. It is practiced dilution in proportions from 1:20 to 1: 100, depending on the purpose. The drug is injected slowly, from two to six hours.

Before transplanting organs or tissues, a solution of cyclosporine is preset in advance, in about four to ten hours. To prevent manifestations of allergies, antiallergic treatment and other immunosuppressants are administered in parallel. After two weeks of intravenous administration, the drug is switched to oral administration. The daily dose prescribed by a doctor is taken twice in twelve hours.

Capsules are drunk whole, not opening the shell, washed down with water. The preparation in liquid form before use inside is diluted with water for drinking in a glass beaker. The instructions detail how to unpack the package and how to dial the solution with a graduated syringe from a glass vial to properly select the right amount of the drug. After consuming the solution, rinse the container with water and drink this liquid so that there is no dose loss.

Contraindicated concomitant medication and grapefruit juice, which reduces the effect of the drug, and during the treatment is prohibited from vaccinating live and weakened whey from rubella, poliomyelitis, measles, mumps.

Dosage

When transplantation to adults, the reception starts with a daily dose of 10-14 milligrams per kilogram of weight. At the end of seven to fourteen days of treatment, the concentration of cyclosporine in the blood is measured. It affects the rate of absorption and transformation in the body. This indicator is important to monitor in order to prevent side effects and exclude the negative interaction with other drugs. After that, the daily dose of this drug is reduced to 3-6 milligrams per kilogram of weight, it is divided into two uses. The therapeutic content of cyclosporin in the plasma ranges from 110 to 410 nanograms per milliliter.

After a kidney transplant, taking a medication in a dose of less than three to four mg per kilogram of weight can provoke organ rejection.

Bone marrow transplantation requires the use of a combination of cyclosporine and methotrexate. A couple of days before the start of the transplant, the patient is started to inject intravenously from 2.5 to 5 milligrams of substance per kilogram of weight per day.

After switching to treatment capsules begin with a daily dose of 12.5 milligrams per kilogram of weight, which is taken twice. Therapy with this amount of drug lasts from three to six months. Gradually, you need to reduce the dosage until the end of the treatment period.

To eliminate the acute condition, the daily dosage of the drug is used from 12.5 to 15 milligrams per kilogram of weight (taken in two approaches). Fifty days later, the dosage is reduced by five percent per week, and after five months, the drug is stopped. In the case of a second reaction, additional medication "Ciclosporin" is given. Instructions for use, reviews contain information on the survival of transplanted organs (heart, liver). According to statistics, in one year it reaches eighty percent.

Treatment of autoimmune diseases requires a special approach to the choice of dose for each disease.

Through the use of the drug "Ciclosporin", the instruction manual recommends the treatment of severe uveitis. It is necessary to start with a daily dose of 5-10 milligrams per kilogram of weight and adhere to it until the inflammatory process decreases and the visual function normalizes. The course of treatment is from three to sixteen months. With severe lesions, a combination with prednisolone in a dose of 200 to 600 micrograms per kilogram of patient weight is possible.

With a severe form of psoriasis, the daily dose is 2.5 milligrams per kilogram of weight, taking in two approaches. Dosage is increased by 1 milligram per kilogram of weight, but not more than 5 milligrams per kilogram, if after thirty days after the beginning of therapy there are no improvements. Admission is canceled after six weeks if treatment is ineffective.

Nephrotic syndrome with normal renal function in adults is treated using the dosage of the drug to 6 milligrams per kilogram of weight, in children - up to 5 milligrams per kilogram of weight. If the kidney function is impaired, the dosage is not more than 2.5 milligrams per kilogram of weight.

In the course of drug treatment, the content of cyclosporin in the blood plasma is monitored. For therapeutic effectiveness, its concentration in the blood in the amount of 60-160 nanograms per milliliter is required.

During the first three months, monitoring of serum creatinine levels should be mandatory, since an increase in this indicator may signal the onset of organ transplant rejection or kidney damage. For people with normal kidney function, the analysis is performed every fourteen days, if there are abnormalities, the creatinine score is measured every seven days. At a concentration of this index above 200 μmol per liter for adults and above 140 μmol per liter for children, the drug is canceled.

Because of the possible toxic effects of the drug, periodic monitoring of bilirubin, urea, amylase, magnesium and potassium ions in the blood is performed, the activity of liver enzymes is determined.

Rheumatoid arthritis in severe form during the first month and a half is treated with Cyclosporine at a daily dosage of 2.5 milligrams per kilogram of weight, with subsequent therapy the daily dose should not exceed 4 milligrams per kilogram of body weight. If the drug is poorly tolerated, it can be reduced to a minimally effective dose. Possible combination of the drug "Ciclosporin" with a small amount of glucocorticosteroids or non-steroidal anti-inflammatory drugs.

Heavy forms of atopic dermatitis are treated by taking a medication a day at a dose of 2.5 milligrams per kilogram of weight. In the absence of effect, after fourteen days, a maximum daily dosage of 5 milligrams per kilogram of weight is prescribed. If there is an improvement in the condition, a gradual decrease in the dose of the drug is recommended.

How is cyclosporin used for eyes? Eye drops

Immunosuppressive agents have found application in ophthalmology for the treatment of dry keratoconjunctivitis. Cyclosporine is also used for these purposes. Eye drops with its content (0.05 percent) are produced under the trade name "Restasis".

This drug belongs to the group of medicines used to protect and moisturize the cornea of the eye. The drug is produced in single-dose vials of 0.4 milligrams with a content of one milliliter of a solution of 500 μg of active substance.

What is the pharmacotherapeutic effect of cyclosporine? Eye drops produce anti-inflammatory, immunomodulating effect, inhibit the production of lacrimal secretion during dry keratoconjunctivitis.

How to use the drug "Restasis"

Locally, the "Restasis" agent containing cyclosporine is used. Instructions for use Eye drops recommend first shaking in a vial to get a homogeneous opaque white emulsion. Only after this, you can proceed to instill drops into the conjunctival sac of the diseased eye. This procedure is carried out twice a day, every twelve hours. When using the drug, do not touch the edge of the vial of the eye mucosa to prevent infection from entering the solution. It is important to remember that the drug should be used immediately after opening the bottle, the remaining solution is no longer used, it is disposed of.

Do not carry out treatment with the drug "Restasis" when wearing contact lenses. They are removed before using the solution, and it can be re-inserted after fifteen minutes.

Application for animals of cyclosporine

Currently, this immunosuppressive agent is also used to treat autoimmune diseases in dogs and other animals.

Initially, only people used cyclosporine. "Sandimmun" - an oily solution containing this substance, when used by different patients, caused different concentrations of the active component in the plasma.

Later, a more modern form was created - ultra-micronized cyclosporine ("Neoral"). It caused the formation of microemulsion during the interaction with the liquid. This resulted in improved absorption and bioavailability of the drug as opposed to an oily solution that is not recommended for use in animals.

The creator of the veterinary form of the drug is considered to be Novartis. The licensed medication was issued in 2003 under the name "Atopika", it is intended for therapy of atopic dermatitis in animals. Until then, unofficially, immunosuppressants were used in transplanting kidneys to cats and dogs to eliminate the symptoms of inflammatory processes.

Symptoms of atopic dermatitis usually manifest in young dogs and cats aged from six months to three years. This is a chronic disease characterized by recurrent relapses. It requires lifelong treatment with a drug containing cyclosporine. Instructions for use for animals means "Atopika" indicates the possibility of using its long period effectively and safely.

With simultaneous intake of food and medicine, there may be changes in absorption, so it is recommended to take this medicine two hours after or before meals.

Among the undesirable consequences from the use of the drug, most often there are disorders in the digestive system, but they are manifested in a mild form. Other side effects are signs of hypertrichosis, gingival hyperplasia and hyperplastic dermatitis. With a decrease in the dosing of the drug, their gradual disappearance occurs.

The administration of cyclosporine reduces the growth and development of causative agents of staphylococcal infections and malasseous dermatitis, in a therapeutic dose it does not cause renal failure, hypertension, and the formation of neoplasms. All these facts indicate a low level of risk of complications during long-term treatment of atopic dermatitis in dogs.