Prednisolonum

General characteristics. Structure:

Active ingredient: Prednisolonum - 5 mg.

Excipients: silicon dioxide colloid; potato starch: stearic acid; magnesium stearate; talc; povidone; starch corn; lactoses monohydrate.

Pharmacological properties:

Pharmacodynamics. Prednisolonum — synthetic glucocorticoid drug, the dehydrogenated hydrocortisone analog. Renders the antiinflammatory, antiallergic, desensibilizing, antishock, anti-toxic and immunodepressive effect.
Interacts with specific cytoplasmatic receptors and forms the complex getting into a cell kernel. stimulates synthesis of matrix RNA (MRNK); the last induces formation of proteins, including a lipokortin. mediating cellular effects. Lipokortin oppresses a phospholipase A 2, suppresses release of arachidonic acid and suppresses synthesis of endoperoxides, prostaglandins, the leukotrienes promoting processes of an inflammation, an allergy, etc.
Suppresses release by a hypophysis of adrenocorticotropic hormone and for the second time - synthesis of endogenous glucocorticosteroids. Oppresses secretion of thyritropic and follicle-stimulating hormones.
Reduces quantity of lymphocytes and eosinophils, increases - erythrocytes (stimulates production of erythropoetins).
Protein metabolism: reduces amount of protein in plasma (at the expense of globulins) with increase in coefficient albumine/globulin, increases synthesis of albumine in a liver and kidneys: strengthens a protein catabolism in muscular tissue.
Lipidic exchange: increases synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat is preferential in the field of a shoulder girdle, the person, a stomach), leads to development of a hypercholesterolemia.
Carbohydrate metabolism: increases absorption of carbohydrates from digestive tract; increases activity of glyukozo-6-phosphatase. the glucose leading to increase in receipt from a liver in blood; increases activity of a fosfoenolpiruvatkarboksilaza and synthesis of aminotransferases. leading to activation of a gluconeogenesis.
Water and electrolytic exchange: detains sodium and water in an organism, stimulates potassium removal (mineralokortikoidny activity), reduces absorption of calcium from digestive tract, "washes away" calcium from bones, increases its removal by kidneys.
The antiinflammatory effect is connected with release oppression by eosinophils and mast cells of mediators of an inflammation, induction of formation of a lipokortin and reduction of quantity of the mast cells producing hyaluronic acid; with reduction of permeability of capillaries, stabilization of cellular membranes and membranes of organellas (especially lizosomalny).
The antiallergic effect develops as a result of suppression of synthesis and secretion of mediators of an allergy, braking of release from sensitized mast cells and basophiles of a histamine and other biologically active agents, reduction of number of the circulating basophiles, suppression of development of adenoid and connecting tissue, decrease in number of T - and V-lymphocytes, mast cells, decrease in sensitivity of effector cells to mediators of an allergy, oppression of antibodyformation, change of an immune response of an organism.
At obstructive respiratory diseases action is based, mainly, on braking of inflammatory processes, oppression of development or the prevention of hypostasis of mucous membranes, braking of eosinophilic infiltration of a submucosal layer of an epithelium of bronchial tubes and adjournment in a mucous membrane of bronchial tubes of the circulating cell-bound immune complexes. There is a braking of an erozirovaniye and desquamation of a mucous membrane. Prednisolonum increases sensitivity of beta adrenoceptors of bronchial tubes of small and average caliber to endogenous catecholamines and exogenous sympathomimetics, reduces viscosity of slime due to oppression or reduction of its products.
Antishock and anti-toxic action is connected with increase in arterial pressure (due to increase in concentration of the circulating catecholamines and recovery of sensitivity to them of adrenoceptors, and also vasoconstriction), decrease in permeability of a vascular wall, membranoprotektorny properties, activation of the enzymes of a liver participating in Endo's metabolism - and xenobiotics.
The immunodepressive effect is caused by oppression of proliferation of lymphocytes (especially T lymphocytes), suppression of migration of V-cells and interactions of T - and In - lymphocytes, braking of release of cytokines (Interlaken - 1, Interlaken - 2; scale - interferon) from lymphocytes and macrophages and decrease in antibody formation.
Slows down connective tissue reactions during inflammatory process and reduces a possibility of formation of cicatricial fabric.

Pharmacokinetics. Absorption - high, maximum concentration in blood at oral administration is reached in 1 - 1.5 h. In plasma to 90% of Prednisolonum contacts proteins: transcortinum (kortizolsvyazyvayushchy globulin) and albumine.
It is metabolized in a liver, kidneys, a small bowel, bronchial tubes. The oxidized forms glyukuronizirutsya or sulphated. Metabolites are inactive. An elimination half-life - 2-4 h. It is removed with bile and urine by glomerular filtering and for 80 - 90% it reabsorbirutsya by tubules. 20% are removed by kidneys in not changed look.

Indications to use:

Endocrine disturbances: primary and secondary adrenal insufficiency (including a state after removal of adrenal glands); inborn adrenal struma; subacute thyroiditis; hypoglycemic states.
General diseases of connecting fabric:
pseudorheumatism; system lupus erythematosus; dermatomyositis; scleroderma: nodular periarteritis.
Acute rheumatism, acute carditis, hysterical chorea.
Acute and chronic inflammatory diseases of joints: humeroscapular periarthritis; ankylosing spondylitis (Bekhterev's disease); gouty and psoriasis arthritis; osteoarthrosis (including posttraumatic); polyarthritis; juvenile arthritis, Steel's syndrome at adults; bursitis; nonspecific tendosinovit; synovitis; epicondylitis.
Acute and chronic allergic diseases:
allergic reactions to medicines and foodstuff; medicinal dieback; serum disease; small tortoiseshell; pollinosis; Quincke's disease: allergic rhinitis.
Bronchial asthma, asthmatic status.
Diseases of blood and system of a hemopoiesis: autoimmune hemolitic anemia; acute lympho-and myeloid leukoses; lymphogranulomatosis, Werlhof's disease; agranulocytosis; panmyelopathia; secondary thrombocytopenia at adults; eritroblastopeniya (erythrocyte anemia); inborn (erythroidal) hypoplastic anemia.
Skin diseases:
pemphigus; eczema, psoriasis, exfoliative dermatitis; atopic dermatitis; diffusion neurodermatitis; contact dermatitis (with defeat of a big surface of skin); toxidermia; seborrheal dermatitis; toxic epidermal necrolysis (Lyell's disease); violent herpetiform dermatitis; malignant exudative erythema (Stephens-Johnson's syndrome).
Allergic and inflammatory diseases of eyes:
allergic helcomas; allergic forms of conjunctivitis; sympathetic ophthalmia; heavy slow lobbies and back uveites; optic neuritis.
Digestive tract diseases:
ulcer colitis; disease Krone; hepatitis; local enteritis.
Lung cancer (in a combination with cytostatic drugs).
Multiple myeloma.
Diseases of lungs:
acute alveolitis, pneumosclerosis, sarcoidosis of the II-III stage.
Diseases of kidneys of autoimmune genesis (including acute glomerulonephritis). nephrotic syndrome.
Tubercular meningitis, pulmonary tuberculosis.
Aspiration pneumonia (in a combination to specific chemotherapy).
Berylliosis, Leffler's syndrome (which is not giving in to other therapy).
Multiple sclerosis.
Wet brain (including against the background of a tumor of a brain or connected with surgical intervention, radiation therapy or an injury of the head) after preliminary parenteral use.
Prevention of reaction of graft rejection at organ transplantation.
Hypercalcemia against the background of oncological diseases. Nausea and vomiting when performing cytostatic therapy.

Route of administration and doses:

The dose and duration of treatment is selected the doctor in an individual order depending on indications and disease severity.
Usually daily dose is accepted once or accept a double dose every other day, in the morning, in the range from 6 to 8 o'clock in the morning.
The high daily dose can be distributed on 2-4 receptions, at the same time in the mornings it is necessary to accept a high dose. A pill should be taken in time or directly after food, washing down with a small amount of liquid.

At acute states and as replacement therapy by the adult appoint 20-30 mg/days in an initial dose, the maintenance dose makes - 5-10 mg/days. At some diseases (a nephrotic syndrome, some rheumatic diseases) appoint higher doses. Treatment is stopped slowly, gradually reducing a dose. If in the anamnesis there are psychoses, high doses are appointed under strict control of the doctor.
Doses for children: an initial dose - 1-2 mg/kg/days in 4-6 receptions, supporting - 0.3-0.6 mg/kg/days.
At appointment it is necessary to consider a day-night secretory rhythm of glucocorticosteroids: appoint big in the morning (or all) a part of a dose.

Features of use:

Before an initiation of treatment of the patient it has to be inspected regarding identification of possible contraindications. Clinical inspection has to include a research of cardiovascular system, X-ray inspection of lungs, a research of a stomach and a 12-perstny gut; systems of urination, organ of sight.
Prior to the beginning of and during performing steroid therapy it is necessary to control the general blood test, concentration of glucose in blood and urine, electrolytes in plasma.
During the period treatment by glucocorticosteroids, especially in high doses, is not recommended to carry out vaccination because of decrease in its efficiency.
Average and high doses of glucocorticosteroids can cause increase in arterial pressure.
At tuberculosis drug can be appointed only together with antitubercular drugs.
At intercurrent infections. septic states simultaneous performing antibiotic treatment is necessary.
At prolonged treatment glucocorticosteroids it is necessary to appoint potassium in order to avoid a hypopotassemia.

At Addison's disease drug should not be accepted along with barbiturates because of danger of development of acute adrenal insufficiency (addisonichesky crisis).
Glucocorticosteroid hormones can cause delay of growth in children and teenagers. Purpose of drug every other day usually allows to avoid or minimize probability of development of such side effect.
Frequency of side reactions increases in advanced age.
At sudden cancellation, especially in case of use of high doses, there is a syndrome of "cancellation" of glucocorticosteroids: loss of appetite, nausea, block, generalized musculoskeletal pains, adynamy.
The probability of adrenal insufficiency as a result of administration of drug and the complications interfaced to it can be reduced, carrying out gradual drug withdrawal. After drug withdrawal adrenal insufficiency can last for months therefore at any stressful situation in this period it is necessary to resume hormonal therapy.
At a hypothyroidism and at cirrhosis effect of glucocorticosteroid hormones can amplify.

It is necessary to warn patients about that in advance. that they and their relatives should avoid contacts with patients with chicken pox, measles, herpes. In cases when system treatment is carried out by glucocorticosteroids or treatment by glucocorticosteroid drugs was carried out in the next 3 months, and at the same time the patient was not vaccinated, it is necessary to appoint specific immunoglobulins.
Treatment by glucocorticosteroid drugs demands medical control at a diabetes mellitus (including in the family anamnesis), osteoporosis (in the period of a postmenopause the risk is higher), a hypertension, chronic psychotic reactions (glucocorticosteroid hormones can cause mental disturbances and increase emotional instability), tuberculosis in the anamnesis, glaucoma, a steroid myopathy, stomach ulcer and a 12-perstny gut, epilepsy, an eye herpes simplex (danger of perforation of a cornea).
Owing to weak mineralokortikoidny effect for replacement therapy at adrenal insufficiency Prednisolonum is used from mineralokortikoida.
At patients with a diabetes mellitus it is necessary to control the content of glucose of blood and if necessary to korrigirovat therapy.

Influence on ability to driving and working mechanisms.
Similar influence of drug is unknown.

Side effects:

Frequency of development and expressiveness of side effects depend on duration of use, size of the used dose and a possibility of observance of a circadian rhythm of purpose of Prednisolonum.
- From endocrine system: oppression of function of adrenal glands, decrease in tolerance to glucose, a "steroid" diabetes mellitus or manifestation of a latent diabetes mellitus, an Icenco-Cushing syndrome (a crescent-shaped face, obesity of pituitary type, a hirsutism, increase in arterial pressure, a dysmenorrhea, an amenorrhea, a myasthenia, striya), delay of growth and a delay of sexual development at children.
- From digestive tract: oral candidiasis, nausea, vomiting, pancreatitis, "steroid" stomach ulcer and 12-perstny gut, erosive esophagitis, bleedings and perforation of digestive tract, increase or loss of appetite, meteorism, hiccups. In rare instances - increase in activity of "hepatic" transaminases and an alkaline phosphatase.
- From cardiovascular system: increase in arterial pressure, arrhythmia, bradycardia; development (at predisposed patients) or strengthening of expressiveness of chronic heart failure, ECG change characteristic of a hypopotassemia, hypercoagulation, fibrinferments. Patients with an acute and subacute myocardial infarction have a distribution of the center of a necrosis, delay of formation of cicatricial fabric that can lead to a rupture of a cardiac muscle.
- From a nervous system: delirium, disorientation, euphoria, hallucinations, maniac-depressive psychosis, depression, paranoia, increase in intracranial pressure, nervousness or concern, sleeplessness, dizziness, вертиго. cerebellum pseudoneoplasm, headache, spasms.
- From sense bodys: a back subkapsulyarny cataract, increase in intraocular pressure with possible injury of an optic nerve, tendency to development of consecutive bacterial, fungal or viral infections of eyes, trophic changes of a cornea, an exophthalmos.
- From a metabolism: a hypocalcemia, increase in body weight, negative nitrogenous balance (the increased disintegration of proteins), the increased sweating.
The side effects caused by mineralokortikoidny activity - a delay of liquid and sodium (peripheral hypostases), a hypernatremia, a gipokaliyemichesky syndrome (a hypopotassemia, arrhythmia, a mialgiya or a spasm of muscles, weakness and fatigue).
- From a musculoskeletal system: delay of growth and processes of ossification at children (premature closing of epiphyseal regions of growth), osteoporosis (it is very rare - pathological fractures of bones, an aseptic necrosis of a head humeral and a femur), a rupture of sinews of muscles, a "steroid" myopathy. decrease in muscle bulk (atrophy).
- From integuments and mucous membranes: the slowed-down healing of wounds, petechias, ecchymomas, thinning of skin, hyper - or hypopigmentation, eels, striya, tendency to development of a pyoderma and candidiases.
Diseases of kidneys and urinary tract: the speeded-up night urination, an urolithiasis owing to the raised excretion of calcium and phosphate.
Diseases of immune system: generalized (skin rash, skin itch, acute anaphylaxis) and local allergic reactions.
Others: development or an exacerbation of infections (emergence of this side effect is promoted jointly by the applied immunodepressants and vaccination), a leukocyturia.

Interaction with other medicines:

Phenobarbital, Phenytoinum, rifampicin, ephedrine, аминоглутетимид, Aminophenazonum (inductors of "hepatic" microsomal enzymes) reduce therapeutic effect of glyukokortikosteriodny hormones.
Increase in a dose of insulin and peroral hypoglycemic drugs because of weakening of hypoglycemic action can be required.
Perhaps both strengthening, and easing of anticoagulating effect at reception of indirect anticoagulants (dose adjustment is required).
Anticoagulants and trombolitik - the risk of development of bleedings from ulcers in digestive tract increases.
Non-steroidal anti-inflammatory drugs:
Acetylsalicylic acid - Prednisolonum accelerates its removal and reduces concentration in blood. After cancellation of glucocorticosteroid drugs increase in concentration of salicylates and development of intoxication is possible; in view of ulcerogenic effect of salicylates the risk of development of gastrointestinal bleeding and ulcerations increases.
Indometacin - increases risk of side effects of Prednisolonum (replacement by Prednisolonum indometacin from bonds with albumine).
The risk of development of a hypopotassemia increases at reception of Amphotericinum In, diuretics, theophylline, cardiac glycosides.
Inhibitors of a karboangidraza and "loopback" diuretics can increase risk of development of osteoporosis.
At reception of estrogen and oral estrogensoderzhashchy contraceptives the clearance of glucocorticosteroids decreases, the elimination half-life is extended, therapeutic and toxic effects of Prednisolonum amplify.
Haemo toxicity of a methotrexate increases.
Reduces the stimulating influence of a somatropin on growth.
Vitamin D - decreases its influence on absorption of calcium in intestines:
The praziquantel - decreases its concentration;
M-holinoblokatory (including antihistaminic drugs and tricyclic antidepressants) and nitrates - promotes increase in intraocular pressure;
The isoniazid and мексилетин - Prednisolonum increases their metabolism (especially at "slow" atsetilator) that leads to decrease in their plasma concentration.
Adrenocorticotropic hormone strengthens effect of Prednisolonum.
Ergocalciferol and parathormone interfere with development of the osteopathy caused by Prednisolonum.
Cyclosporine and кетоконазол, slowing down Prednisolonum metabolism, can increase its toxicity in some cases.
Glucocorticosteroids reduce hypotensive effect of anti-hypertensive drugs.
Co-administration of androgens and steroid anabolic drugs with Prednisolonum promotes development of peripheral hypostases and a hirsutism, appearance of eels.
Mitotanum and other inhibitors of function of bark of adrenal glands can cause need of increase in a dose of Prednisolonum.
At simultaneous use with live antiviral vaccines and against the background of other types of immunization increases risk of activation of viruses and development of infections.
Immunodepressants increase risk of development of infections and a lymphoma or other limfoproliferativny disturbances connected with Epstein's virus - Barrel.
Antipsychotic means (neuroleptics) and Azathioprinum increase risk of development of a cataract at purpose of Prednisolonum.
Co-administration of antacids reduces Prednisolonum absorption.
At simultaneous use with anti-thyroid drugs decreases, and with thyroid hormones - the clearance of Prednisolonum increases.

Contraindications:

The only contraindication for short-term use according to vital indications is hypersensitivity to Prednisolonum or components of drug.
At children in a growth period glucocorticosteroids have to be applied only according to absolute indications and under especially careful observation of the attending physician.
With care it is necessary to appoint Prednisolonum at the following states and diseases:
Parasitic and infectious diseases of the virus, fungal or bacterial nature (now or recently postponed, including recent contact with the patient): the herpes simplex surrounding herpes (a viremichesky phase), chicken pox, measles; amebiasis, strongyloidosis; system mycosis; active and latent tuberculosis. Use at serious infectious diseases is admissible only against the background of specific therapy.
Pre-and the postvaccinal periods (the period lasting 8 weeks to and 2 weeks after vaccination), lymphadenitis after BTsZh inoculation.
Immunodeficiency (including AIDS or VPCh-infection). Digestive tract diseases: a peptic ulcer of a stomach and a 12-perstny gut, an esophagitis, gastritis, an acute or latent round ulcer, recently created intestines anastomosis, ulcer colitis with threat of perforation or abscessing, a diverticulitis.
Diseases of cardiovascular system, including recently postponed myocardial infarction (at patients with an acute and subacute myocardial infarction distribution of the center of a necrosis, delay of formation of cicatricial fabric and, as a result of it is possible. rupture of a cardiac muscle), dekompensirovanny chronic heart failure, arterial hypertension, lipidemia.

Endocrine diseases: a diabetes mellitus (including disturbance of tolerance to carbohydrates), a thyrotoxicosis, a hypothyroidism, Itsenko-Cushing's disease, obesity (the III-IV degree).
Heavy chronic renal and/or liver failure, нефроуролитиаз.
The hypoalbuminemia and states contributing to its emergence.
System osteoporosis, gravis myasthenia, acute psychosis, poliomyelitis (except for a form of bulbar encephalitis), open and closed-angle glaucoma.

Use during pregnancy and a lactation.
During pregnancy use of Prednisolonum is possible if the estimated advantage for mother exceeds potential risk for a fruit.
In the I trimester of pregnancy Prednisolonum is applied only according to vital indications.
At long therapy during pregnancy the possibility of a growth disorder of a fruit is not excluded. In case of use in the III trimester of pregnancy there is a danger of emergence of an atrophy of bark of adrenal glands at a fruit that can demand performing replacement therapy from the newborn.
As glucocorticosteroids get into breast milk, in case of need uses of drug during breastfeeding feeding by a breast are recommended to be stopped.

Overdose:

In case of by-effects it is necessary to reduce Prednisolonum dose.
There is no specific antidote, a symptomatic treatment. Control of blood electrolytes is necessary.

Storage conditions:

List B. To store at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 5 mg:
100 tablets in the polypropylene bottle corked by a cover with control of the first opening. One bottle in a cardboard pack with the enclosed application instruction.