Methypredum

General characteristics. Structure:

Active ingredient: 4 mg of Methylprednisolonum.

Excipients: lactose, starch corn, gelatin, magnesium stearate, talc, water
cleared.

The synthetic steroid drug having the pharmakodinamichesky properties similar to a hydrocortisone or cortisol at the same time possessing it is considerable big antiinflammatory action while the mineralkortikoidny effect and a hypopotassemia are twice less, than at use of cortisol and hydrocortisone. The diabetogenic effect is insignificant.

Pharmacological properties:

Pharmacodynamics. The effect of Methylprednisolonum (6-L-methylcortisone), as well as other GKS, is implemented through interaction with steroid receptors in cell cytoplasm. The steroid-receptor complex is transported in a cell kernel, connects to DNA and changes a transcription of genes for the majority of proteins. GKS oppress synthesis of numerous proteins, various enzymes causing destruction of joints (at a pseudorheumatism), and also the cytokines playing an important role in immune and inflammatory responses. Induce synthesis of a lipokortin — key protein of neuroendocrinal interaction of GKS that leads to reduction of an inflammatory and immune response.

GKS, including Methylprednisolonum, suppress or interfere with development of the fabric answer to many thermal, mechanical, chemical, infectious and immunological agents. Thus, glucocorticoids work symptomatic, reducing displays of a disease without impact on the reason. The antiinflammatory effect of Methylprednisolonum at least by 5 times exceeds efficiency of a hydrocortisone.

Endocrine effects of Methylprednisolonum include suppression of secretion of AKTG, inhibition of products of endogenous cortisol, at prolonged use — a partial atrophy of bark of adrenal glands. Influences metabolism of calcium, vitamin D, carbohydrate, protein and lipidic metabolism therefore at prolonged use of GKS are possible increase in level of glucose in blood, decrease in density of a bone tissue, the phenomenon of a muscular atrophy and dislipidemiya. GKS also promote increase in the ABP, modulation of behavior and mood. Methylprednisolonum has practically no mineralokortikoidny activity.

Pharmacokinetics. Bioavailability of Methylprednisolonum at intake usually makes more than 80%, the maximum concentration in blood serum is reached in 1–2 h, the elimination half-life lasts 2–3 h. About 77% of Methylprednisolonum contact proteins of a blood plasma, communication with transcortinum is insignificant. Distribution volume — 1–1,5 l/kg. Methylprednisolonum is metabolized to inactive metabolites. The specific CYP enzymes providing its transformation are not known. The average clearance makes 6,5 ml/kg/min., duration of antiinflammatory effect — 18–36 h. About 5% of drug are removed from an organism with urine.

Indications to use:

The states demanding system therapy of GKS — inflammatory and general rheumatic diseases, autoimmune diseases, allergic states, an acute anaphylaxis, OH and other diseases of lungs, and also for cerebral decompression (for example at wet brain against the background of new growths), reaction of graft rejection; some dermatological, hematologic, hepatic, neurologic (for example multiple sclerosis, heavy pseudoparalytic myasthenia), renal and gastrointestinal diseases (for example nonspecific ulcer colitis, disease Krone). Methylprednisolonum is also used as an antiemetic when carrying out chemotherapy and as a component of schemes of treatment of leukoses, lymphoma and a malignant multiple myeloma.

Route of administration and doses:

The initial dose depends on character and disease severity. The initial peroral dose for adults makes from 8 to 96 mg a day. At achievement of positive clinical effect the dose is gradually reduced. The maintenance dose has to be minimum effective, for adults it usually makes 4–12 mg/days in one step in the morning. At prolonged treatment there can be adequate an administration of drug every other day. To children appoint in lower dose.

Features of use:

Methylprednisolonum, as well as other glucocorticoids, can promote an exacerbation of some diseases.

GKS should be applied with care and under medical control at patients with AG, congestive heart failure, mental disorders, a diabetes mellitus (or diabetes in the family anamnesis), pancreatitis, with pathology of a digestive tract (a round ulcer, a local ileitis, ulcer colitis or a diverticulitis with the increased risk of bleeding and perforation), osteoporosis, glaucoma and with predisposition to thrombophlebitis. Patients with disturbance of a blood coagulation have to be under medical control.

GKS can complicate diagnosis of damages of a digestive tract as promote reduction of expressiveness of a pain syndrome. Mask hyper parathyroidism stage of latency.

At long therapy by Methypredum it is necessary to consider a question of purpose of biphosphonates sick osteoporosis or with risk factors of its development. Risk factors of osteoporosis are age 65 years, frequent changes in the anamnesis or in the family anamnesis, an early menopause (up to 45 years), a premenopauzalny amenorrhea and small body weight are more senior. The risk of development of osteoporosis can be minimized by regulation of a dose of Methypredum, reducing it to minimum effective.

Long reception of GKS suppresses a pituitary and adrenal axis that leads to development of secondary insufficiency of the kortikoadrenalovy answer which is followed by complications and exacerbations of diseases.

For minimization of side effects the full daily dose of Methylprednisolonum needs to be accepted in the morning according to a circadian rhythm of endogenous development of cortisol.

At a hypothyroidism or a serious illness of a liver because of the strengthened effect of Methylprednisolonum it is necessary to reduce a dose.

At long reception at children growth delay is possible. Therefore treatment has to be limited to administration of drug in the minimum doses during the shortest time.

Elderly patients of GKS need to appoint with care because of the increased risk of development of side effects (a round ulcer, osteoporosis and an ulceration of skin).

At prolonged use of GKS therapy should be stopped gradually, for several weeks in order to avoid development of a withdrawal and serious complications. Long therapy should not stop suddenly and in case of pregnancy.

Side effects:

From a digestive tract: dyspepsia, increase in appetite, round ulcers with perforation and bleeding, a gullet ulcer, gullet candidiasis, pancreatitis, perforation of a gall bladder.

From a musculoskeletal system: proximal myopathy, osteoporosis, rupture of sinews, muscular weakness.

Disturbances of water and electrolytic balance: a delay of sodium and water in an organism, AG, a gipokaliyemichesky alkalosis, a hypopotassemia, chronic heart failure.

From skin: regeneration delay, skin atrophy, acne rash.

From endocrine system and metabolism: suppression гипоталамо - a pituitary and adrenal axis, growth delay, disturbance of a menstrual cycle, an amenorrhea, the cushingoid person, a hirsutism, increase in body weight, decrease in tolerance to carbohydrates, increase in need for insulin and peroral gipoglikemiziruyushchy drugs.

From the mental sphere: eufobiya, depression, sleeplessness, aggravation of an exacerbation of schizophrenia.

From an organ of sight: increase in intraocular pressure, glaucoma, papilledema, cataract, thinning of a cornea and sclera, aggravation of viral and fungus diseases of eyes, exophthalmos.

From immune system: immunosuppression, masking of infections, suppression of reactions to skin tests, hypersensitivity.

Others: opportunistic infections, tuberculosis recurrence, leukocytosis, tendency to thromboembolisms, indisposition.

Drug withdrawal symptoms: fever, mialgiya, arthralgia, insufficiency of adrenal glands.

Interaction with other medicines:

Antikholinesterazny means: use of corticosteroids and antikholinesterazny means can cause muscular weakness in patients with a myasthenia.

Anticoagulants: at combined use with glucocorticoids strengthening and reduction of effect of anticoagulants can be noted. Parenteral administration of Methylprednisolonum strictly exponentiates thrombolytic action of antagonists of vitamin K (флуиндион, аценокумарол).

Salicylates and other non-steroidal anti-inflammatory drugs: parallel purpose of salicylates, indometacin and other non-steroidal anti-inflammatory drugs can increase probability of an ulceration of a mucous membrane of a stomach. Methylprednisolonum can promote reduction of level of salicylates in blood serum, increasing their renal clearance.

Hypoglycemic drugs: Methylprednisolonum can partially suppress hypoglycemic effect of peroral antidiabetic means and insulin.

Inductors of enzymes, for example barbiturates, Phenytoinum, Primidonum, carbamazepine, and rifampicin, increase system clearance of Methylprednisolonum, thereby reducing effects of Methylprednisolonum almost twice.

CYP3A4 inhibitors, for example erythromycin, кларитромицин, кетоконазол, итраконазол and тролеандомицин, increase elimination and level of Methylprednisolonum in a blood plasma which can strengthen therapeutic and side effects of Methylprednisolonum.

Estrogen can strengthen effects of Methylprednisolonum, slowing down his metabolism. It is not recommended to regulate Methylprednisolonum doses to the women accepting oral contraceptives which can promote not only increase in an elimination half-life, but also development of atypical immunosuppressive effects of Methylprednisolonum.

Amphotericinum, diuretics and easy purgatives: Methylprednisolonum can increase removal of potassium from an organism at the patients receiving at the same time these drugs.

Immunodepressants: Methylprednisolonum has the additive immunosuppressive properties that can increase therapeutic effects or risk of development of various side reactions at reception together with other immunodepressants. Only some of these effects can be explained with pharmacokinetic interactions. Glucocorticoids improve antiemetic efficiency of other antiemetic drugs used in parallel at therapy by the anticarcinogenic drugs causing vomiting. It was reported about rare attacks of convulsions at parallel reception of Methylprednisolonum and cyclosporine.

Immunization: glucocorticoids can reduce the immunizing efficiency of vaccines and increase risk of neurologic complications. Use of therapeutic (immunosuppressive) doses of glucocorticoids together with live virus vaccines can increase risk of development of viral diseases.

Others: it was reported about two serious cases of an acute myopathy at the elderly patients receiving a doksakarium chloride and Methylprednisolonum in high doses. At long therapy glucocorticoids can reduce effect of Somatotropinum.

Contraindications:

Hypersensitivity to Methylprednisolonum or any other component of drug.

Existence acute/chronic virus (chicken pox, shingles, simplex herpes), bacterial infections, inactive or active forms of tuberculosis without performing parallel antimicrobic or specific therapy.

Tuberculosis, and also other acute/persistent bacterial and viral infections at insufficient security of an organism antibiotiko-and chemotherapy.

Overdose:

Methylprednisolonum does not cause acute intoxication. At chronic intoxication which is shown by epinephral suppression it is necessary to reduce a dose gradually. At peroral overdose the gastric lavage and reception of absorbent carbon is recommended. The antidote of Methylprednisolonum does not exist.

Storage conditions:

To store at the room temperature (15-25 °C) in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

30 tablets in a polyethylene plastic jar, in cardboard packaging.