PREDNISOLON 5mg

Instructions for use

PREDISOLON RENEWED table. 5 mg No. 100

Composition

1 tablet contains:

active substance:

prednisolone 0.001 g 0.005 g

Excipients:

sucrose 0.0300 g 0.1500 g

potato starch 0.0185 g 0.0925 g

stearic acid 0.0005 g 0.0025 g

Dosage form

pills

Description

The tablets are white, flat-cylindrical, chamfered, with or without an "R" marking on one side.

Pharmacodynamics

Prednisolone is a synthetic glucocorticoid drug, a dehydrated analog of hydrocortisone. It has anti-inflammatory, anti-allergic, immunosuppressive effects, increases the sensitivity of beta-adrenergic receptors to endogenous catecholamines. Interacts with specific cytoplasmic receptors (receptors for glucocorticosteroids are found in all tissues, especially in the liver) to form a complex that induces the formation of proteins (including enzymes that regulate vital processes in cells). Protein metabolism: reduces the amount of globulins in the plasma, increases the synthesis of albumin in the liver and kidneys (with an increase in the albumin / globulin ratio), reduces the synthesis and enhances the catabolism of protein in muscle tissue. Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (fat accumulation occurs mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia. Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract; increases the activity of glucose-6-phosphatase (increasing the flow of glucose from the liver into the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); promotes the development of hyperglycemia. Water and electrolyte metabolism: retains sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, reduces bone mineralization. The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils and mast cells; inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes (especially lysosomal) and organelle membranes. Acts at all stages of the inflammatory process: inhibits the synthesis of prostaglandins at the level of arachidonic acid (lipocortin inhibits phospholipase A2, inhibits the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes that promote inflammation, allergies, etc.), the synthesis of "pro-inflammatory interleukin-1" ( , tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors. The immunosuppressive effect is caused by the involution of lymphoid tissue caused by the inhibition of the proliferation of lymphocytes (especially T-lymphocytes), suppression of the migration of B-cells and the interaction of T- and B-lymphocytes, inhibition of the release of cytokines (interleukin-1, 2; gamma-interferon) from lymphocytes and macrophages and a decrease in the formation of antibodies. The antiallergic effect develops as a result of a decrease in the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, a decrease in the number of circulating basophils, suppression of the development of lymphoid and connective tissue, a decrease in the number of T- and B-lymphocytes, mast cells , decrease in the sensitivity of effector cells to allergy mediators, inhibition of antibody production, changes in the body's immune response. In obstructive respiratory diseases, the action is mainly due to the inhibition of inflammatory processes, the prevention or reduction of the severity of edema of the mucous membranes, a decrease in eosinophilic infiltration of the submucous layer of the bronchial epithelium and the deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucosa. Increases the sensitivity of small and medium-sized bronchial beta-adrenergic receptors to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production. Suppresses the synthesis and secretion of adrenocorticotropic hormone and, secondarily, the synthesis of endogenous glucocorticosteroids. It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

Pharmacokinetics

When taken orally, prednisone is well absorbed from the gastrointestinal tract. The maximum concentration in the blood is reached within 1-1.5 hours after oral administration. Up to 90% of the drug binds to plasma proteins: transcortin (cortisol-binding globulin) and albumin. Prednisolone is metabolized in the liver, partly in the kidneys and other tissues, mainly by conjugation with glucuronic and sulfuric acids. The metabolites are inactive. It is excreted in the bile and urine by glomerular filtration and is reabsorbed by the tubules by 80-90%. Take 20% of the dose

are passed by the kidneys unchanged. The plasma half-life after oral administration is 2-4 hours.

Indications for use

- Systemic connective tissue diseases (systemic lupus erythematosus, scleroderma, periarteritis nodosa, dermatomyositis, rheumatoid arthritis);

- acute and chronic inflammatory diseases of the joints: gouty and psoriatic arthritis, osteoarthritis (including post-traumatic), polyarthritis (including senile), periarthritis of the shoulder, ankylosing spondyloarthritis (ankylosing spondylitis), juvenile arthritis, Still's syndrome in adults , bursitis, nonspecific tendosynovitis, synovitis and epicondylitis;

- acute rheumatism, rheumatic carditis, chorea minor;

- bronchial asthma, asthmatic status;

- acute and chronic allergic diseases, incl. allergic reactions to drugs and food, serum sickness, urticaria, allergic rhinitis, Quincke's edema, drug exanthema, hay fever, etc.;

- skin diseases: pemphigus, psoriasis, eczema, atopic dermatitis (widespread neurodermatitis), contractual dermatitis (affecting a large surface of the skin), toxidermia, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), bullous herpetiformis dermatitis, Stevens syndrome Johnson;

- cerebral edema (including against the background of a brain tumor or associated with surgery, radiation therapy or head trauma) after prior parenteral administration;

- allergic eye diseases (allergic forms of conjunctivitis);

- inflammatory diseases of the eyes: sympathetic ophthalmia, severe sluggish anterior and posterior uveitis, optic neuritis;

- primary or secondary adrenal insufficiency (including the condition after removal of the adrenal glands);

- congenital adrenal hyperplasia;

- kidney disease of autoimmune genesis (including acute glomerulonephritis);

- nephrotic syndrome;

- subacute thyroiditis;

- diseases of the blood and hematopoietic system: agranulocytosis, panmyelopathy, autoimmune hemolytic anemia, lympho- and myeloid leukemia, lymphogranulomatosis, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocytic anemia), congenital anemia;

- interstitial lung diseases: acute alveolitis, pulmonary fibrosis, stage II-III sarcoidosis;

- tuberculous meningitis, pulmonary tuberculosis, aspiration pneumonia (in combination with specific chemotherapy);

- beryllium disease, Leffler's syndrome (not amenable to other therapy);

- lung cancer (in combination with cytostatics);

- multiple sclerosis;

- gastrointestinal diseases: ulcerative colitis, Crohn's disease, local enteritis;

- hepatitis, hypoglycemic conditions;

- prevention of the graft rejection reaction during organ transplantation;

- hypercalcemia against the background of oncological diseases, nausea and vomiting during cytostatic therapy;

- myeloma.

Contraindications

For short-term use for health reasons, the only contraindication is hypersensitivity to prednisolone or drug components. In children, during the growth period, glucocorticosteroids should be used only for absolute indications and under the close supervision of the attending physician.

Application during pregnancy and lactation

During pregnancy (especially in the first trimester), it is used only for health reasons. With prolonged therapy during pregnancy, fetal growth impairment is possible. When used in the third trimester of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn. Since glucocorticosteroids pass into breast milk, if it is necessary to use the drug during breastfeeding, it is recommended to stop breastfeeding.

Side effects

The frequency of development and the severity of side effects depends on the duration of use, the size of the dose used and the possibility of observing the circadian rhythm of the drug administration.

When using the drug, the following side effects may occur.

From the endocrine system: decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing's syndrome (moon face, pituitary obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscular) , delayed sexual development in children.

From the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding and perforation of the wall of the gastrointestinal tract, increased or decreased appetite, indigestion, flatulence, hiccups. In rare cases - an increase in the activity of "hepatic" transaminases and alkaline phosphatase.

From the side of the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development