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

Suppresses the release of pituitary beta-lipotropin, but does not reduce the concentration of circulating beta-endorphin. Oppressing the secretion of thyroid-stimulating hormone and follicle-stimulating hormone.

Increases the excitability of the central nervous system, reduces the number of lymphocytes and eosinophils, increases erythrocytes (stimulates the production of erythropoietins). Interacts with the cytoplasmic receptors of glucocorticosteroids and forms a complex penetrating into the nucleus of the cell, and stimulates the synthesis of mRNA; the latter induces the formation of proteins, including lipocortin, that mediate cellular effects. Lipocortin depresses phospholipase A2, inhibits the release of arachidonic acid, and suppresses the synthesis of endoperoxides, prostaglandins, leukotrienes, which promote inflammation, allergies, and others.

Protein metabolism: reduces the amount of protein in the plasma (due to globulins) with an increase in the coefficientalbumin / globulin, increases the synthesis of albumins in the liver and kidneys; enhances protein catabolism in muscle tissue.

Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (the 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, leading to an increase in the intake of glucose from the liver into the blood; increases the activity of phosphoenolpyruvate-carboxylase and the synthesis of aminotransferases, leading to the activation of gluconeogenesis, promotes the development of hyperglycemia.

Water-electrolyte exchange: detains sodium ions and water in the body, stimulates the excretion of potassium ions (mineralocorticoid activity), reduces the absorption of calcium ions from the gastrointestinal tract, reduces the mineralization of bone tissue, increases the excretion of calcium ions by the kidneys.

Anti-inflammatory effect is associated with inhibition of eosinophil release by inflammatory mediators; inducing the formation of lipocortin and reducing the number of mast cells,producing hyaluronic acid; with a decrease in the permeability of capillaries; stabilization of cell membranes and membranes of organelles (especially lysosomal).

Antiallergic effect develops as a result of suppression of synthesis and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils of histamine and other biologically active substances, 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 chronic obstructive pulmonary disease the action is mainly based on inhibition of inflammatory processes, inhibition of development or prevention of edema of the mucous membranes, inhibition of eosinophilic infiltration of the submucosal layer of bronchial epithelium, deposition of circulating immune complexes in the mucous membrane of the bronchi, and inhibition of erosion and desquamation of the mucosa.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 due to oppression or reduction of its production.

Anti-shock and antitoxic action is associated with an increase in blood pressure (by increasing the concentration of circulating catecholamines and restoring the sensitivity of adrenoreceptors to them, as well as vasoconstriction), a decrease in the permeability of the vascular wall, membrane-protective properties, activation of liver enzymes involved in the metabolism of endo- and xenobiotics.

Immunodepressive effect is caused by oppression of T-lymphocyte proliferation, suppression of B-lymphocyte migration and interaction of T and B lymphocytes, inhibition of release of cytokines (interleukin-1, interleukin-2; interferon gamma) from lymphocytes and macrophages.

Suppresses the synthesis and secretion of adrenocorticotropic hormone and, secondarily, the synthesis of endogenous glucocorticosteroids.

Pharmacokinetics:

Absorption is high, the time to reach the maximum concentration (TC_mOh) with oral intake - 1-1.5 hours.In plasma, most (90%) of prednisolone binds to the transcortb(corticosteroid-binding globulin) and albumins.

Metabolised in the liver, kidneys, small intestine, bronchi, mainly by conjugation with glucuronic and sulfuric acids. Metabolites are inactive. The half-life (T_1/2) - 2-4 hours It is deduced by kidneys - 20% unchanged.

Indications:

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

Acute and chronic inflammatory joint diseases: gouty and psoriatic arthritis, osteoarthritis (including posttraumatic), polyarthritis, humerous periarthritis, ankylosing spondylitis (Bechterew's disease), juvenile arthritis, Still's syndrome in adults, bursitis, nonspecific tendosynovitis, synovitis and epicondylitis.

Rheumatic fever, acute rheumatic heart disease.

Bronchial asthma.

Acute and chronic allergic diseases: allergic reactions to medicines and food products, serum sickness, urticaria, allergic rhinitis, angioedema, drug exanthema, pollinosis.

Skin diseases: pemphigus, psoriasis, eczema, atopic dermatitis, diffuse neurodermatitis, contact dermatitis (with damage to the large surface of the skin), toxicermy, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), bullous herpetiform dermatitis, malignant exudative erythema (syndrome Stevens-Johnson). The cerebral edema (including, against a background of a brain tumor or associated with surgery, radiation therapy or head trauma) after a prior application parenteral forms of corticosteroids.

Allergic eye diseases: allergic corneal ulcers, 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 hyperplasia of the adrenal glands.

Kidney disease of autoimmune genesis (including acute glomerulonephritis); nephrotic syndrome.

Subacute thyroiditis.

Diseases of the blood: agranulocytosis, panmielopatiya, autoimmune hemolytic anemia, acute lymphoid and myeloid leukemia, Hodgkin's disease, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (red cell anemia), congenital (erythroid) hypoplastic anemia.

Lung diseases: acute alveolitis, pulmonary fibrosis, stage II-III sarcoidosis.

Tuberculous 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.

Diseases of the gastrointestinal tract: ulcerative colitis, Crohn's disease, local enteritis.

Hepatitis.

Prevention of graft rejection during organ transplantation.

Hypercalcemia on the background of cancer.

Myeloma disease.

Contraindications:

Hypersensitivity to prednisolone.

Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.

Carefully:

Parasitic and infectious diseases of viral,fungal or bacterial (currently or recently transferred, including recent contact with the patient): herpes simplex, herpes zoster (viremic phase), chicken pox, measles; amoebiasis, strongyloidiasis (or suspected); systemic mycosis; active or latent tuberculosis. Application in severe infectious diseases is permissible only against the background of specific antimicrobial therapy.

Post-vaccination period (period duration 8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency conditions (including AIDS or HIV infection).

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 threat of perforation or abscess formation, diverticulitis. Diseases of the cardiovascular system, including the recently transferred myocardial infarction (in patients with acute and subacute myocardial infarction it is possible to spread the focus of necrosis, slow the formation of scar tissue and, as a consequence, break the heart muscle), decompensated chronic heart failure, arterial hypertension, hyperlipidemia ).

Endocrine diseases: diabetes mellitus (including impaired glucose tolerance), 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 and lactation:

During pregnancy, the drug is used only if the potential benefit to the mother exceeds the potential risk to the fetus.

With prolonged therapy during pregnancy, it is possible to not overgrow the upper palate, impaired fetal growth.

In the third trimester of pregnancy - the risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in a newborn.

Glucocorticosteroids pass into breast milk, if necessary, during the lactation period, breastfeeding 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 endogenous secretions of glucocorticosteroids in the range from 6 to 8 hours of the morning. A high daily dose can be divided into 2-4 doses, with a large dose taken in the morning.

The drug should be taken during or immediately after a meal, with a small amount of liquid.

In acute conditions and as a replacement therapy, adults are prescribed in an initial dose of 20-30 mg / day, the maintenance dose is 5-10 mg / day. If necessary, the initial dose may be 15 g 100 mg / day, maintaining d 5-15 mg / day. h

For children, the initial dose is 1-2 mg / kg of body weight per day in 4-6 receptions, supporting - 0.3-0.6 mcg / kg per day.

When the therapeutic effect is obtained, the dose is gradually reduced by 5 mg, then by 2.5 mg at intervals of 3-5 days, canceling at a later stage later. With prolonged use of the drug 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.

Under 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 depend on the duration of application, the amount of dose used and the possibility of observing the circadian rhythm of the appointment.

From the endocrine system: a decrease in 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, myasthenia, striae), delay of sexual development in children.

From the digestive system: nausea, vomiting, pancreatitis, a "steroid" stomach ulcer and 12intestines, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increase or decrease in appetite, flatulence, hiccough.In rare cases - increased activity of "liver" transaminases and alkaline phosphatase.

From the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of chronic heart failure, changes in the electrocardiogram, 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, increased 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 ions, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating.

Caused by mineralocorticosteroid activity (ISS activity) - delay fluid and sodium ions (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

From the musculoskeletal system: slowing the growth and processes of ossification in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and thigh bone), rupture of muscle tendons, steroid myopathy, muscle loss (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, perioral dermatitis, exanthema.

Allergic reactions: generalized (skin rash, skin itching, anaphylactic shock), local allergic reactions.

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

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

It is possible to strengthen the above described side effects.

It is necessary to reduce the dose of Prednisolone.

Treatment: symptomatic.

Interaction:

Prednisolone increases the toxicity of cardiac glycosides (because of the resulting hypokalemia, the risk of arrhythmias increases).

Accelerates the removal of acetylsalicylic acid, reduces its concentration in the blood (with the abolition of prednisolone, the concentration of salicylates in the blood increases and the risk of side effects increases).

With simultaneous use with live antiviral vaccines and against other types of immunizations, increases the risk of virus activation and the development of infections.

Increases the metabolism of isoniazid, mexiletine (especially in "fast" acetylators), which leads to a decrease in their plasma concentrations.

Increases the risk of hepatotoxic reactions of paracetamol (induction of microsomal liver enzymes and the formation of a toxic metabolite of paracetamol).

Increases (with prolonged therapy) the content of folic acid.

Hypokalemia caused by prednisolone may increase the severity and duration of muscle blockade against the background of muscle relaxants.

In high doses reduces the effect of somatropin.

Antacids reduce the absorption of prednisolone.

Prednisolone reduces the effect of hypoglycemic and hypotensive drugs increases the anticoagulant effect of coumarin derivatives.

Weaken the influence of vitamin D on the absorption of calcium ions in the lumen of the intestine.

Ergocalciferol and parathyroid hormone interfere with the development of osteopathy caused by prednisolone.

Reduces the concentration of praziquantel in the blood.

Cyclosporine (inhibits metabolism) and ketoconazole (reduces clearance) increase the toxicity of prednisolone.

Thiazide diuretics, inhibitors of carbonic anhydrase, amphotericin B increase the risk of hypokalemia and heart failure, sodium-containing drugs - edema and increased blood pressure.

Nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol increase the risk of ulceration of the gastrointestinal mucosa and bleeding, in combination with NSAIDs for the treatment of arthritis, it is possible to reduce the dose of prednisolone due to the summation of the therapeutic effect.

Indomethacin, displacing prednisolone from association with albumin, increases the risk of developing its side effects.

Amphotericin B and carbonic anhydrase inhibitors increase the risk of osteoporosis.

The therapeutic effect of prednisolone is reduced under the influence of phenytoin, barbiturates, ephedrine, theophylline, rifampicin and other inducers of "hepatic" microsomal enzymes (an increase in metabolic rate).

Mitotane and other "inhibitors of adrenal cortex function may necessitate an increase in the dose of prednisolone.

The clearance of prednisolone rises against the background of thyroid hormones.

Immunosuppressants increase the risk of infection and lymphoma or other lymphoproliferative disorders caused by the Epstein-Barr virus.

Estrogens (including oral estrogen-containing contraceptives) reduce the clearance of prednisolone, prolong the half-life of T_1/2, enhance its therapeutic and toxic effects.

The emergence of hirsutism and acne is facilitated by the simultaneous use of prednisolone and other steroid hormonal drugs - androgens, estrogens, anabolic, oral contraceptives.

Tricyclic antidepressants can increase the severity of depression caused by the use of prednisolone (not shown for the therapy of these side effects).

The risk of developing cataracts increases with other corticosteroids, antipsychotic drugs (neuroleptics), carbutamide and azathioprine.

Simultaneous administration with m-holinoblokatorami (including antihistamines, tricyclic antidepressants with m-holinoblokiruyuschey activity), nitrates contributes to the development of increased intraocular pressure.

Antithyroid drugs reduce the clearance of prednisolone.

Special instructions:

Before starting treatment, the patient should be examined for possible contraindications. Clinical examination should include examination of the cardiovascular system, X-ray examination of the lungs, examination of the stomach and duodenum; urinary system, organs of vision;

Before and during the treatment with prednisolone, it is necessary to monitor the general blood test, glycemia and glucosuria, and the electrolyte content in the plasma.

With intercurrent infections, septic conditions and tuberculosis, simultaneous antibiotic therapy is necessary.

During treatment should not be immunized.

With a sudden reversal, especially in the case of previous use of high doses, there is a syndrome of "cancellation" of prednisolone: anorexia, nausea, blocking, generalized musculoskeletal pain, general weakness.

After cancellation, a relative insufficiency of the adrenal cortex persists for several months. If during this period there are stressful situations, appoint (according to indications) for a while prednisolone, if necessary in combination with mineralocorticosteroids.

Children who were in contact with sick measles or chickenpox during the treatment period prophylactically prescribe specific immunoglobulins.

To reduce side effects, it is justified to prescribe anabolic steroids, increasing the intake of potassium ions with food.

In Addison's disease, simultaneous administration of barbiturates should be avoided - the risk of acute adrenal insufficiency (addisonic crisis).

In children during growth prednisolone It should be used only under absolute indications and under very careful supervision of the attending physician.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, 5 mg.

Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 10, 20, 30, 40, 50, 60, 100 tablets in cans of polymeric.

Each jar or 1, 2, 3, 4, 5, 6, 10 contour mesh packages with instructions for use are placed in a pack of cardboard for consumer containers.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

2 of the year.

The drug should not be used after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001472

Date of registration:02.02.2012

The owner of the registration certificate:URALBIOFARM, OJSC URALBIOFARM, OJSC Russia

Manufacturer: & nbsp

URALBIOFARM, OJSC Russia

Information update date: & nbsp28.08.2015

Illustrated instructions

Instructions

Prednisolone (Prednisolon)