Metilprednizolon-FS

General characteristics. Structure:

Active agent: Methylprednisolonum - 4 mg or 8 mg;

Excipients: lactoses monohydrate (tabletoza), starch corn / potato, sodium of starch glikolit (type A), magnesium stearate, silicon colloid anhydrous.

Pharmacological properties:

Pharmacodynamics. Metilprednizolon-FS – a synthetic glucocorticosteroid – Prednisolonum analog. On activity it is close to Prednisolonum, but has practically no mineralokortikoidny activity that provides the best portability. Has the antiinflammatory, desensibilizing and antiallergenic effect. Has also antishock, anti-toxic and immunodepressive properties. Unlike tsitostatik, immunodepressive Metilprednizolona-FS properties are not connected with mitostatichesky action, and are result of suppression of different stages of an immunogenesis: migrations of stem cells of marrow, migration of V-cells and interaction of T - and V-lymphocytes.
Like other corticosteroids, Metilprednizolon-FS slows down release of cytokines (interleykin 1 and 2, and? - interferon) from lymphocytes and macrophages, release by eosinophils of mediators of an inflammation oppresses, reduces metabolism of arachidonic acid. Stimulating steroid receptors, induces formation of a special class of proteins – the lipokortin having antiedematous activity.
In rather high doses slows down development of adenoid and connecting tissue, including a reticuloendothelium; reduces quantity of the mast cells which are the place of formation of hyaluronic acid; suppresses activity of hyaluronidase and promotes reduction of permeability of capillaries. Synthesis detains and accelerates disintegration of proteins. Has lipolytic and lipogenetichesky activity.

Pharmacokinetics. After intake of Metilprednizolon-FS it is quickly soaked up preferential in proximal department of a small intestine. Forms the weak dissociated bonds with albumine and transcortinum. In the connected state there are from 40 to 90% of drug. The volume of distribution of Metilprednizolona-FS makes 61 l. Drug is metabolized preferential in a liver. The main metabolites - 20-? - hydroxymethylprednisolonum and 20-?-gidroksi-6-? - Methylprednisolonum. Metabolites are allocated mainly with urine in the form of glucuronides, sulfates and not conjugated connections. Conjugation tests occur generally in a liver, to a lesser extent – in kidneys. The clearance of Metilprednizolona-FS makes 383 l/day; an elimination half-life - 165 minutes.

Indications to use:

Primary or secondary insufficiency of bark of adrenal glands; rheumatic diseases (a pseudorheumatism, an osteoarthritis, the bursitis ankylosing a spondylitis, a system lupus erythematosus); skin diseases: pemphigus, exfoliative dermatitis, severe forms of psoriasis, contact dermatitis, allergic dermatitis; bronchial asthma; chronic obstructive respiratory diseases; sarcoidosis; serum disease; medicinal allergies; seasonal and usual allergic rhinitis; autoimmune hemolitic anemia; idiopathic Werlhof's disease; inborn erythroidal hypoplastic anemia; ulcer colitis; disease Krone; palliative treatment of some forms of a tumoral disease (leukemia and lymphoma).

Route of administration and doses:

Drug is accepted inside. Doses are selected individually depending on disease severity, reaction of the patient and presumable term of treatment.
As a rule, it is necessary to adhere within several days to a high initial dose which depending on a disease can make from 4 to 48 mg a day. In mild cases purpose of small doses is sufficient. High initial doses of drug can be required at multiple sclerosis (200 mg a day), wet brain (200 - 1 000 mg a day), organs transplantation (to 7 mg/kg a day). If at adequate treatment the clinical effect is absent, Metilprednizolon-FS needs to cancel and appoint other drugs gradually. After achievement of therapeutic effect it is necessary to define an adequate dose of drug for the supporting treatment. For this purpose the initial dose through small periods is reduced to that minimum level at which the satisfactory clinical effect remains. Usually (depending on expressiveness of symptoms) it is necessary to reach the minimum maintenance dose of 4 - 12 mg of Metilprednizolona-FS a day.
At treatment of bronchial asthma and chronic obstructive diseases of lungs originally Metilprednizolon-FS appoint in a dose 32 - 40 mg a day. Then every 4 day the dose is lowered by 8 mg. In 3 - 4 weeks of treatment reception of tablets is stopped or passed to inhalation glucocorticosteroids. At a severe form of asthma, at long therapy the minimum dose of Metilprednizolona-FS makes 4 - 8 mg a day. Therapy has to be circadian, alternating therapy in
the majority of cases it is impossible. In the presence of night and morning attacks the daily dose can be divided into two receptions: 2/3 doses in the morning and 1/3 doses in the evening (between 18:00 and 20.00 hour).
At an acute alveolitis the initial dose for inclusion in the first week makes 32 - 40 mg a day (in 1 or 2 receptions). Then the dose is gradually reduced with transition to single daily dose.
At a pneumosclerosis the initial dose makes 24 - 32 mg a day in a combination with Azathioprinum or Penicillaminum. Then the dose is gradually reduced to the level which is defined individually: 4 - 8 mg a day.
At a sarcoidosis the initial dose makes 32 - 40 mg a day in 2 receptions prior to effect of drug, then pass to a single dose of drug and within 4 - 6 weeks the dose is gradually reduced.
At a pollinosis, allergic rhinitis of Metilprednizolon-FS use in addition to antihistaminic drugs and local antiallergic means in case of their insufficient efficiency and danger of damage of airways. In these cases of Metilprednizolon-FS, as a rule, apply in an initial dose 16 mg a day during the first 4 days, then during the next 4 days reduce a dose to 8 mg a day. Administration of drug is stopped in 8 days. If the reached effect insufficient, it is possible to prolong administration of drug up to 2 - 3 weeks in a daily dose of 4 - 8 mg.
At skin diseases the initial dose of Metilprednizolona-FS can make from 80 to 160 mg a day depending on severity and a form of a disease. The dose is quickly reduced as the general duration of treatment usually does not exceed 2 - 4 weeks. Only in some cases administration of drug can be prolonged up to several months.
At treatment of autoimmune diseases depending on severity and a form the initial dose makes 40 - 60 mg a day. Then the dose decreases to supporting which reception can be necessary within several years. In case of acute forms it is possible pulse therapy high doses.
At rheumatic damage of joints the initial dose of Metilprednizolona-FS makes 16 - 24 mg a day. At visceral rheumatism – to 60 mg a day. Then the dose is gradually reduced, reaching a maintenance dose no more than 8 mg a day.
At autoimmune hemolitic anemia the initial dose of Metilprednizolona-FS makes 80 - 160 mg a day. At achievement of effect (usually for 2 weeks from the beginning of reception) the dose is gradually reduced to supporting.
At ulcer colitis and a disease Krone the initial dose of Metilprednizolona-FS makes 40 - 80 mg a day. Then the dose is gradually reduced. At ulcer colitis therapy needs to be finished as soon as possible. If at a disease the Krone is necessary longer therapy, then it is necessary to reach the alternating mode of use.
At replacement therapy at insufficiency of bark of adrenal glands of Metilprednizolon-FS apply in a dose 4 - 8 mg a day. If necessary combine with drugs of mineralokortikoid.

Features of use:

Treatment needs to be carried out under control of the doctor.
Metilprednizolon-FS use in two modes: in the form of circadian therapy and alternating therapy. At circadian therapy drug is accepted after food, preferential after a breakfast, without chewing, washing down with necessary amount of liquid. In some cases, for example in the presence of morning and night attacks at patients with obturatsionny diseases of lungs, the daily dose can be divided into two receptions: 2/3 doses in the morning and 1/3 doses in the evening (between 18:00 and 20.00 hour).
At alternating therapy drug is accepted every second day in the doubled dose after a breakfast (between 6:00 and 8.00 hour), without chewing and washing down with enough liquid.

Side effects:

Disturbances of water and electrolytic balance: a delay of sodium and liquid in an organism, chronic heart failure at cardiological patients, arterial hypertension, loss of potassium and a gipokaliyemichesky alkalosis.
From a musculoskeletal system: steroid myopathy, muscular weakness, osteoporosis, pathological fractures of vertebras, Sharko's arthropathy.
From a digestive tract: ulcers of a gastroduodenal zone with probability of perforation and bleeding, gastric bleedings, pancreatitis, an esophagitis, perforation of intestines.
From skin: deterioration in processes of regeneration, a petechia and ecchymomas, thinning of skin, hypo - and a hyperpegmentation.
Metabolic disturbances: negative nitrogenous balance owing to a catabolism of proteins.
Neurologic disturbances: increase in intracranial pressure, cerebellum pseudoneoplasm, mental disturbances and convulsive attacks.
Endocrine disturbances: disturbances of a menstrual cycle, a cushingoid syndrome, suppression of pituitary and adrenal system, decrease in tolerance to carbohydrates, manifestation of a latent diabetes mellitus, increase in need for insulin or peroral gipoglikemiziruyushchy means at patients with a diabetes mellitus, a growth inhibition at children.
From organs of sight: back subkapsulyarny cataract, increase in intraocular pressure and exophthalmos.
From immune system: "greasing" of a clinical picture available and activation of latent infections, opportunistic infections, hypersensitivity reactions (including an anaphylaxis), suppression of reactions in tests with skin allergens.

Interaction with other medicines:

At combined use with rifampicin, Phenytoinum, barbiturates the effect of Metilprednizolona-FS decreases. The oral contraceptives containing estrogen strengthen action of Metilprednizolona-FS.
At use of Metilprednizolona-FS together with non-steroidal anti-inflammatory drugs the risk of gastrointestinal bleedings increases.
At combined use with Metilprednizolonom-FS efficiency of peroral antidiabetic drugs, anticoagulants – derivative coumarin, Somatotropinum decreases.
At combined use of Metilprednizolona-FS with prazikvantely the maintenance of a prazikvantel in blood can decrease. Combined use of Metilprednizolona-FS with Chloroquinum, Hydroxychloroquinum, metlokviny increases risk of development of a myopathy, cardiomyopathy. Effect of cardiac glycosides amplifies at combined use with Metilprednizolonom-FS. Combined use of Metilprednizolona-FS with saluretics and purgatives increases potassium loss.

Contraindications:

Use of Metilprednizolona-FS is contraindicated at raised
sensitivity to drug. Prolonged use of Metilprednizolona-FS is contraindicated at acute viral infections (shingles, simple deprive, chicken pox); at HbsAG-positive active chronic hepatitis; damages of lymph nodes after a tuberculosis inoculation; epidemic parotitis; during the period of 6 weeks to and up to 2 weeks after preventive inoculations.
Use of Metilprednizolona-FS is not recommended to women during pregnancy and feeding by a breast. In need of use of drug it is necessary to compare carefully risk from its use for a fruit or the child and advantage for mother.

Overdose:

The acute overdose of Metilprednizolona-FS in clinic is not described. At prolonged use of drug development of a cushingoid syndrome is possible.

Storage conditions:

To store in the unavailable to children, protected from light place at a temperature of 15 - 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging; on 3 blister strip packagings in a pack cardboard.