Cyclosporine (Cyclosporine A, Sandimmune)
Cyclosporine (cyclosporine A, sandimmun, sandimmun neoral) is the main drug used in the treatment of autoimmune diseases and organ transplantation for the prophylaxis and prevention of transplant rejection reactions. The main mechanism of action is inhibition of the development of immunity reactions of the cellular type.
Main diseases in which cyclosporine is used:
- Psoriasis;
- Atopic dermatitis;
- Rheumatoid arthritis;
- Behcet's disease;
- Autoimmune pathologies of kidneys (chronic nephritic syndrome, nephrotic syndrome);
- Iridocyclitis;
- Rejection of transplanted organs and tissues.
A special feature of taking cyclosporine is the individual selection of dosage, taking into account the biological characteristics of the patient: weight, age, condition of the gastrointestinal tract, liver, and kidneys. Such a strict approach is due to the toxic effect of the drug, which increases when therapeutic concentrations of the drug are exceeded in the blood.
Cyclosporine is absorbed in the intestine, its bioavailability is 30%, increasing depending on the duration of medication and the dosage. Maximum concentration in plasma is reached in 1 to 5 hours. It is mainly excreted in bile. The optimal concentration is considered to be 300-800 ng/ml. Usually, the doctor sets for each patient a certain concentration of cyclosporine in the blood, which must be maintained throughout the entire period of the therapeutic course.
According to the latest clinical trials, in half of the patients, the level of cyclosporine in the blood was 10% higher than the target. Dose control based on drug concentration levels 2 hours after administration allowed reducing the average dose of cyclosporine from 3.5 ± 1.4 to 2.8 ± 1 mg/kg. Cyclosporine levels are monitored in the laboratory by drug monitoring, which helps to increase the effectiveness of treatment, as well as to avoid or reduce the severity of cyclosporine side effects:
From the nervous system: general weakness, fatigue, headache, paresthesia, convulsions, tremor. Patients after liver transplantation have symptoms of encephalopathy, visual impairment, and impaired coordination of movements.
From the digestive system: loss of appetite, nausea, vomiting, abdominal pain, diarrhea, pancreatitis.
From the genitourinary system: impaired renal function, the development of interstitial fibrosis.
From the cardiovascular system: increased blood pressure.
Other side effects: gynecomastia, dysmenorrhea, hirsutism, acne, hypertrichosis, gum hypertrophy, edema, weight gain. Complication of the course of infectious diseases. Malignant and lymphoproliferative diseases.
Laboratory: increase in liver enzymes, bilirubin, creatinine, urea, uric acid. Anemia, leukopenia, and thrombopenia. Hyperkalemia, hypomagnesemia.
Read more about the drug cyclosporine here.