Prednisolone - instructions for use, dose, side effects, contraindications

active substance:
prednisolone	0.001 grams	0.005 g
Excipients:
sucrose	0.0300 grams	0.1500 g
potato starch	0.0185 g	0.0925 g
stearic acid	0.0005 g	0.0025 grams

Description:

Tablets of white color, Plain cylindrical, with bevel, with marking "R" on one side or without it.

Pharmacotherapeutic group:glucocorticosteroid

ATX: & nbsp

H.02.A.B.06 Prednisolone

Pharmacodynamics:

Prednisolone is a synthetic glucocorticoid drug, a dehydrated analog of hydrocortisone. Provides anti-inflammatory, antiallergic, immunosuppressive action, increases the sensitivity of beta-adrenergic receptors to endogenous catecholamines.

Interacts with specific cytoplasmic receptors (receptors for glucocorticosteroids are present in all tissues, especially in the liver), with the formation of a complex inducing the formation of proteins (including enzymes that regulate vital processes in cells).

Protein metabolism: reduces the number of globulins in plasma, increases the synthesis of albumin in the liver and kidneys (with increasing albumin / globulin ratio), reduces synthesis and enhances protein catabolism in muscle tissue.

Lipid exchange: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat occurs mainly in the area of 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 (increased intake 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-electrolyte exchange: retards sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, reduces the mineralization of bone tissue.

Anti-inflammatory effect is associated with the suppression of the release of eosinophils and mast cells by inflammatory mediators; inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in the permeability of capillaries; stabilization of cell membranes (especially lysosomal) and membranes of organelles. It acts on all stages of the inflammatory process: it inhibits the synthesis of prostaglandins at the level of arachidonic acid (lipocortin depresses phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, promoting inflammation, allergies, etc.), the synthesis of "pro-inflammatory cytokines" (interleukin-1 , tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors.

Immunodepressive effect caused by the involution of lymphoid tissue,inhibition of the proliferation of lymphocytes (especially T-lymphocytes), suppression of B-cell migration and 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.

Antiallergic effect develops as a result of reduced synthesis and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils histamine and other biologically active substances, a decrease in the number of circulating basophils, suppression of lymphoid and connective tissue development, decrease in the number of T- and B-lymphocytes, mast cells, sensitivity of effector cells to mediators of allergy, inhibition of antibody formation, changes in the immune response of the body.

In obstructive airway diseases effect is due mainly the inhibition of inflammatory processes, prevention or reduction of severity of mucosal edema, reduction of eosinophil infiltration bronchial epithelium submucosal layer and deposition in the bronchial mucosa of circulating immune complexes and erozirovaniya inhibition and mucosal desquamation.Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchial tubes 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:

Ingestion prednisolone well absorbed from the gastrointestinal tract. The maximum concentration in the blood is reached after 1-1.5 hours after oral administration. Up to 90% of the drug binds to plasma proteins: transcortin (cortisol-binding globulin) and albumins. Prednisolone metabolized in the liver, partially in the kidneys and other tissues, mainly by conjugation with glucuronic and sulfuric acids. Metabolites are inactive.

It is excreted with bile and urine by glomerular filtration and by 80-90% reabsorbed by tubules. 20% of the dose is excreted by the kidneys unchanged. The half-life from plasma after oral administration is 2-4 hours.

Indications:

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

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

- acute rheumatism, rheumatic carditis, small chorea;

- bronchial asthma, asthmatic status;

- acute and chronic allergic diseases, incl. allergic reactions to medicines and foods, whey

disease, urticaria, allergic rhinitis, Quincke's edema, drug exanthema, pollinosis, etc .;

- Skin diseases: pemphigus, psoriasis, eczema, atopic dermatitis (common neurodermatitis), contracted dermatitis (with large skin lesions), toxicermy, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), bullous herpetiform dermatitis, Stevens-Johnson syndrome ;

- edema of the brain (incl.on a background of a brain tumor or associated with surgery, radiation therapy or head trauma) after previous parenteral administration;

- allergic eye diseases (allergic forms of conjunctivitis);

- inflammatory eye diseases: 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;

- blood diseases and hematopoiesis: agranulocytosis, panmyelopathy, autoimmune hemolytic anemia, lymphoid and myeloid leukemia, lymphogranulomatosis, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocyte anemia), congenital (erythroid) hypoplastic anemia;

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

- tuberculosis meningitis, pulmonary tuberculosis, aspiration pneumonia

(in combination with specific chemotherapy);

- berylliosis, 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 graft rejection during organ transplantation;

- hypercalcemia on the background of cancer, nausea and vomiting during cytostatic therapy;

- myeloma disease.

Contraindications:

For short-term use according to vital indications, the only contraindication is hypersensitivity to prednisolone or the components of the drug.

In children during growth, glucocorticosteroids should be used only in absolute indications and under the close supervision of the treating physician.

Carefully:

Diseases of the gastrointestinal tract: peptic ulcer of stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with perforation or abscessing, diverticulitis.

Parasitic and infectious diseases of a viral, fungal or bacterial nature (current or recent, including recent contact with a patient): herpes simplex, herpes zoster (viremic phase), chicken pox, measles; amebiasis, strongyloidiasis; systemic mycosis; active and latent tuberculosis.

The use in severe infectious diseases is permissible only against the background of specific therapy.

Pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination.

Immunodeficiency conditions (including AIDS or HIV infection). Diseases of the cardiovascular system, incl. recently suffered myocardial infarction (in patients with acute and subacute myocardial infarction, the spread of the necrosis foci, slowing the formation of scar tissue and, as a result, rupture of the heart muscle), severe chronic heart failure, hypertension, hyperlipidemia.

Endocrine diseases: diabetes (including violation tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease, obesity (III-IV degree).

Severe chronic renal and / or hepatic insufficiency, nephrourolythiasis.

Hypoalbuminemia and conditions predisposing to its occurrence.

Systemic osteoporosis, myasthenia gravis gravis, acute psychosis, poliomyelitis (except for the form of bulbar encephalitis), open and closed angle glaucoma, pregnancy.

Pregnancy and lactation:

When pregnancy (especially in the first trimester) is used only for life indications. With prolonged therapy during pregnancy, a violation of fetal growth is possible. When used in the III trimester of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

As glucocorticosteroids pass into breast milk, if breastfeeding is necessary during breastfeeding, breast-feeding should be discontinued.

Dosing and Administration:

The dose of the drug and the duration of treatment is determined by the doctor individually, depending on the indications and severity of the disease.

The entire daily dose of the drug is recommended to take a single or double daily dose - every other day, taking into account the circadian rhythm of the endogenous secretion of glucocorticosteroids in the interval from 6 to 8 am.A high daily dose can be divided into 2-4 doses, with a large dose taken in the morning. Tablets should be taken during or immediately after meals, with a small amount of liquid.

In acute conditions and as a substitute therapy for adults prescribe at an initial dose of 20-30 mg / day, the maintenance dose is 5-10 mg / day. If necessary, the initial dose may be 15-100 mg / day, supporting - 5-15 mg / day.

For children the initial dose is 1-2 mg / kg of body weight per day in 4-6 receptions, supporting - 300-600 mkg / kg per day.

When the therapeutic effect is obtained, the dose is gradually reduced - 5 mg, then 2.5 mg at intervals of 3-5 days, canceling at first later receptions.

With prolonged use of the drug, the daily dose should be reduced gradually. Long-term therapy can not be stopped suddenly! The withdrawal of the maintenance dose is slower the longer the glucocorticosteroid therapy is used.

In case of stressful influences (infection, allergic reaction, trauma, surgery, mental overload) to avoid exacerbation of the underlying disease, the dose of prednisolone should be temporarily increased (at 1.5-3, and in severe cases 5-10 times).

Side effects:

The frequency of development and severity of side effects depends on the duration of the application, the amount of dose used and the possibility of observing the circadian rhythm of prescribing the drug.

When using the drug, the following side effects can be noted.

From the endocrine system: depression of glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, oppression of the adrenal gland function, Itenko-Cushing syndrome (lunar face, obesity of the pituitary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae), delay in 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 gastrointestinal wall, increased or decreased appetite, digestive disorders, flatulence, hiccough. In rare cases - increased activity of "liver" transaminases and alkaline phosphatase.

From the side of the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased manifestation of heart failure, ECG changes characteristic of hypokalemia,increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction - the spread of the focus of necrosis, slowing the formation of scar tissue, which can lead to rupture of the heart muscle.

From the nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor, cerebral palsy, headache, convulsions.

From the sense organs: posterior subcapsular cataract, an increase in intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral infections of the eyes, trophic changes in the cornea, exophthalmos.

From the side of metabolism: increased excretion of calcium, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating.

Caused by mineralocorticoid activity: fluid and sodium retention in the body (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia,Myalgia or muscle spasm, unusual weakness and fatigue).

From the musculoskeletal system: slowing growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rare - pathological fractures, aseptic necrosis of the humeral head and femur), rupture of tendons of muscles, steroid myopathy, loss of muscle mass (atrophy).

From the skin and mucous membranes: delayed healing of wounds, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, acne, striae, a tendency to develop pyoderma and candidiasis.

Allergic reactions: skin rash, itching, anaphylactic shock.

Other: development or exacerbation of infections (the emergence of this side effect is facilitated by jointly used immunosuppressants and vaccination), leukocyturia, withdrawal syndrome.

Overdose:

Symptoms: it is possible to strengthen the above described side effects. It is necessary to reduce the dose of the drug.

Treatment: symptomatic.

Interaction:

With the simultaneous administration of prednisolone with:

- inducers of "liver" microsomal enzymes (phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) - its concentration decreases;

- diuretics (especially "thiazide" and inhibitors of carbonic anhydrase) and amphotericin B - the excretion of potassium from the body increases and the risk of developing heart failure increases;

- sodium-containing drugs - leads to the development of edema and increased blood pressure;

- cardiac glycosides - their tolerance is worsened and the likelihood of developing ventricular extrasystole (due to induced hypokalemia) is increased;

- muscle relaxants - hypokalemia caused by prednisolone, can increase the severity and duration of muscle blockade;

- indirect anticoagulants - weakens (less intensifies) their effect (dose adjustment required);

- anticoagulants and thrombolytic - increases the risk of bleeding from ulcers in the gastrointestinal tract;

- ethanol and non-steroidal anti-inflammatory drugs (NSAIDs) - the risk of erosive and ulcerative lesions in the gastrointestinal tract and bleeding increases (in combination with NSAIDs, a reduction in the dose of glucocorticosteroids due to the summation of the therapeutic effect is possible in combination with NSAIDs in the treatment of arthritis);

- paracetamol - the risk of hepatotoxicity increases (induction of hepatic enzymes and the formation of a toxic metabolite of paracetamol);

- acetylsalicylic acid - accelerates its excretion and reduces the concentration in the blood (with the withdrawal of prednisolone, the level of salicylates in the blood increases and the risk of side effects increases);

- insulin and oral hypoglycemic drugs, hypotensive drugs - their effectiveness decreases;

- vitamin D - its effect on calcium absorption in the intestine decreases;

- Growth hormone - the effectiveness of the latter decreases;

- prazikvantelom - the concentration of the latter decreases;

- M-holinoblokatorami (including antihistamines and tricyclic antidepressants) and nitrates - contributes to increased intraocular pressure;

- isoniazid and mexelitin - increases their metabolism (especially in "slow" acetylators), which leads to a decrease in their plasma concentrations.

- inhibitors of carbonic anhydrase and "loop" diuretics - increases the risk of osteoporosis;

- indomethacin - displaces prednisolone from association with albumin, increasing the risk of developing its side effects;

- adrenocorticotropic hormone - the effect of prednisolone is increased;

- ergocalciferol and parathyroid hormone - prevent the development of osteopathy, caused by prednisolone;

- cyclosporine and ketoconazole - slowing the metabolism of prednisolone, may in some cases increase its toxicity;

- androgens and steroid anabolic drugs - the development of peripheral edema and hirsutism, the appearance of acne;

- estrogens and oral estrogen-containing contraceptives - the clearance of prednisolone decreases, which can be accompanied by an increase in the severity of its action;

- mitotane and other inhibitors of the function of the adrenal cortex - may necessitate an increase in the dose of prednisolone;

- living antiviral vaccines and against other types of immunizations - the risk of virus activation and the development of infections increases;

- antipsychotic drugs (neuroleptics) and azathioprine - increases the risk of developing cataracts;

- antacids - reduces the absorption of prednisolone;

- antithyroid drugs - decreases, and with thyroid hormones - the clearance of prednisolone increases;

- immunosuppressant drugs - the risk of developing infections and lymphoma or other lymphoproliferative disorders associated with the Epstein-Barr virus increases.

With long-term therapy prednisolone increases the content of folic acid.

Special instructions:

During treatment with the drug (especially prolonged), it is necessary to observe the oculist, control blood pressure, the state of water electrolyte balance, as well as patterns of peripheral blood and blood glucose levels.

In order to reduce side effects, it is possible to prescribe antacids, and also to increase the intake of potassium in the body (diet, potassium preparations). Food should be rich in proteins, vitamins, with a restriction of fat, carbohydrates and table salt.

The effect of the drug is enhanced in patients with hypothyroidism and liver cirrhosis. The drug may enhance existing emotional instability or psychotic disorders. When referring to a psychosis in an anamnesis, the drug in high doses is prescribed under the strict supervision of a doctor.

In stressful situations during maintenance treatment (for example, surgical operations, trauma or infectious diseases), a correction of the dose of the drug should be made in connection with an increase in the need for glucocorticosteroids.

It should be carefully monitored for patients within a year after the end of prolonged therapy with the drug in connection with the possible development of a relative deficiency of the adrenal cortex in stressful situations.

In case of sudden cancellation, especially in case of prior application of high doses, it is possible to develop a withdrawal syndrome (anorexia, nausea, blocking, generalized musculoskeletal pain, general weakness), as well as exacerbation of the disease for which the drug was prescribed.

During treatment with the drug should not be vaccinated due to a decrease in its effectiveness (immune response).

Assigning the drug for intercurrent infections, septic states and tuberculosis, it is necessary to simultaneously perform antibiotic treatment with bactericidal action.

At children during long treatment by a preparation careful monitoring over dynamics of growth and development is necessary. Children who were in contact with sick measles or chickenpox during the treatment period prophylactically prescribe specific immunoglobulins. Due to the weak mineralocorticoid effect for replacement therapy for adrenal insufficiency, the drug is used in combination with mineralocorticoids.

Patients with diabetes should monitor blood glucose and, if necessary, correct therapy.

An x-ray control of the osteoarticular system (images of the spine, hands) is shown.

In patients with latent infectious diseases of the kidneys and urinary tract, the drug is able to cause leukocyturia, which can be of diagnostic significance.

The drug increases the content of metabolites of 11- and 17-oxyketocorticosteroids.

Effect on the ability to drive transp. cf. and fur:There is no information.

Form release / dosage:

Tablets, 1 mg and 5 mg.

Packaging:

For 10, 14 tablets per contour cell package of polyvinyl chloride film and aluminum foil.

5, 10 contiguous cell packs of 10 tablets or 8 out-of-round cell packs of 14 tablets with instruction but are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-002459

Date of registration:07.02.2012

The owner of the registration certificate:UPDATE OF PFC, CJSC UPDATE OF PFC, CJSC Russia

Manufacturer: & nbsp

UPDATE, PFC CJSC Russia

Representation: & nbspUPDATE OF PFC, CJSCUPDATE OF PFC, CJSC

Information update date: & nbsp28.08.2015

Illustrated instructions

Instructions

Prednisolone (Prednisolone)