Methylprednisolone

Chemical name

(6альфа,11бета)-11,17,21-Три гидрокси-6-метилпрегн��-1,4-диен-3,20-дион

Gross

C22-H30-O5

Characteristics

White or belovaty crystalline powder odourless well soluble in ethanol, dioxane and methanol, poorly soluble in acetone and chloroform, it is very poorly soluble in the air, practically insoluble in water.

Of drugs

Drugs, the anti-inflammatory, protiwallergicescoe, immunodepressivne. Mechanism противовоспалительно го the result of higher product липокортинов inhibiting фосфолипазу A and hindering либерацию арахидоновой acid from membrane phospholipids, followed oppression synthesis of cyclic эндоперекисей, NG, тромбоксана, оксикислот and лейкотриенов. Affects all phases of inflammation. Stabilizing лизосом membranes, reduces withdrawal of lysosomal enzymes inhibits fusion гиалуронидазы, blood capillaries and education экссудата inflammation, improves reduces products лимфокинов (интерлейкина 1 and 2 гамма-интерферона) in Lymphocytes and макрофагах inhibits migration of macrophages, the infiltration and granulation, suppresses the release эозинофилами inflammation mediators, reduces collagen production and mucopolysaccharides activity фибробластов.Противо��ллергический effect evolved as a result of a decrease in the synthesis and secreta mediators allergies, braking release of sensitised fat cells and bazofilov gistamina and other biologically active substances, reducing the number of circulating bazofilov, suppression of limfoidna and connective tissue, reducing air and B-limfozitov, fat cells, reducing the sensitivity of effector cells to mediatoram allergies, antiteloobrazovania oppression, changes Immune Response �рганизма.Иммунодепре ссия by inwaluciei limfoidna tissue oppression proliferation of lymphocytes (especially T), down B-kletok migration and interaction of air and B-limfozitov, braking release limfokinov and products Antitel.okazavaet pronounced effect on the metabolism : reduces synthesis and increases the breakdown of protein in muscle, increases protein synthesis in the liver, the synthesis of higher fatty acids and triglycerides is the redistribution of fat and giperglikemia, stimulates glikoneogenez increases of glycogen in the liver and muscles, in violation of bone mineralization �кани.Метилпреднизоло на acetate, a product for injecting the slow absorption and long duration. Duration of action (18-36 h) depends on the introduction of solubility used drug forms, and the dose of the patient. After the / m of 80 mg product it continued for 12 h, and supressivne effect on the plasma eye there for the next 17 days. The ingestion rapidly and completely absorbed. When the / m to a drawn succinate, slower-acetate (early it through 48 hours). Biotransformation occurs in the liver. Passes through GEB and placenta, enters the breast milk. Place in the form of metabolites mainly urine. T_1/2 is about 2 hours

Indications

Primary or secondary адренокортикальная deficiency (in combination with минералокортикоидами) Аддисона disease, congenital гиперплазия надпочечников, негнойный тиреоидит, гиперкальциемия associated with the cancer process, shock (anaphylactic, Burns trauma, кардиогенный), brain swelling, severe trauma, the additional therapy for acute during or worsening neurologic diseases : псориатический arthritis, rheumatoid arthritis (including ювенильный) ancylosing спондилит, acute or podostry bursitis, acute Baby tendoshinovit, acute gouty arthritis, traumatic arthritis, sinovit osteoarthritis, epikondilit; kollagenozy (exacerbation or maintenance therapy) : systemic lupus red, acute revmocardit, system dermatomiozit (polimiozit); skin diseases : vesicular disease, bullezny gerpetiformny dermatitis, syndrome Stevens-Johnson, exfoliativei dermatitis, mikozy, psoriasis, seborainey dermatitis; allergic diseases : seasonal and permanent allergic rhinitis, savorotocnaya disease, bronchial asthma, allergic reactions caused by the drugs, contact dermatitis, atopic dermatitis; anaphylacticskie and anaphylactoidnye reaction, urticaria in transfuzii; eye diseases : allergic corneal ulcers, herpes zoster ophthalmicus, inflammation of the front segment, diffuse and uveit horioidit, sympathetic oftalmia, allergic conjunctivitis, keratit, horioretinit, optic neuritis, irit and iridotsyklit; Diseases to the respiratory system (with the chemotherapy) : symptomatic sarkoidoz, Leffler syndrome, berillios, pulmonary tuberculosis, pneumonia aspirate; hematologic diseases : trombozitopenica idiopathic purpura in adults, secondary anaemia in adults acquired (Autoimmune) Hemolytic Anemia, eritroblastopenia, gipoplastical congenital anaemia, agranulozitos, acute lymphatic and mieloidnyi leukaemia; leukaemia and lymphomas in adults; mieloma, lung cancer (in combination with zitostatikami); digestive diseases : Ulcerative colitis, ulcerative disease, a local enteritis, hepatitis; neurological diseases : multiple sclerosis, infants, tuberculosis meningitis (with the chemotherapy); trihinoz; suppression of the immune incompatibility with organ transplantation; nausea and vomiting in zitostaticescoy Terapii.vodnuu suspension metilprednizolona acetate give affected tissue with kelloidah, gipertroficskih localized lesions and infiltratah, red ribbon inhabitants, psoriaticakih blyashkah, chronic neirodermite, diskoidna red volchanke, lipoidnom diabeticescom nekrobiose, alopetion, tough tumors aponeurozov and tendons.

Contraindications

Hypersensitivity, acute and chronic bacterial or viral diseases without химиотерапевтической protection, systemic fungal infections, active tuberculosis, AIDS, latent tuberculosis, intestinal whales (in the near history), long heart failure or hypertension, severe violation of the liver and kidneys, эзофагит, gastritis, acute or латентная пептическая ulcers, diabetes mellitus, male, glaucoma, severe osteoporosis, hypothyroidism, mental disorders, poliomyelitis (with the exception of �ульбарно-энцефаличес ких Forms), lymphoma after BCG vaccination, pregnancy, breast-feeding (for the suspension), the period of coverage; vnutrisustavnogo to use, artificial joint, a breach of blood coagulation, vnutrisustavna fracture, periartikuliarny infectious process (including in history); for the prevention of respiratory distress-sindroma the newborn amnionitis, breeding bleeding, infections mother platzentarnaya failure, Premature tanks Ploda.protivopokazan premature births.

Side-Effects

Syndrome Иценко - Кушинга have atrophied надпочечников crust, the menstrual cycle, гирсутизм, impotence, the prevalence of stunting among children, стероидный diabetes, глюкозурия, increased body mass index, a negative balance of nitrogenous whose sodium and water, swelling, loss of potassium гипокалиемический алкалоз, reduced tolerance to carbohydrates, пептические stomach ulcer and duodenal ulcer with possible perforation and bleeding, nausea, vomiting, Ulcerative ezofagit, pancreatitis, pregnant stomach, headache, dizziness, increased vnutricerepnogo pressure psevdoopujol companion, mental disorders, convulsions, hypertension, female heart failure, arrhythmia and hypotension, trombofilia, reduced resistance to infectious diseases, sterile abscesses, the vnutriglaznogo pressure exofthalm, back subkapsuliarnaya cataracts, blindness, muscle weakness, steroidnaya miopatia, reduced muscle mass osteoporosis (especially women and children), the gap tendons, compression fracture of vertebrae, aseptic necrosis of the head of the humerus and femur, a pathological fracture of the long bones, artropatia type sprays, thinning and atrophy of lasers, skin and subcutaneous tissue deterioration regeneration petehii, revolution, societies face, piodermia, kandidozy, hypothesis and hyperpigmentation, ekhimozy, allergic reactions : urticaria, anaphylactic shock, bronhospazm.

Specific guidance

With long-term use should be reduced calorie intake, the consumption of potassium, reduced-sodium. Calculating doses in children better than kg body weight, and m ^ 2 surface. Do not mix with other intravenous solutions.

Patient interaction

Ciclosporin (oppressing metabolism) and ketokonazol (reduces Cl) increased toxicity. Phenobarbital, dimedrol, phenytoin, rifampicin, etc. induktora liver enzymes increase speed off and reduce the wash. Makes an aspirin reduces its level in the blood (for the lifting of metilprednizolona salicilata level in the blood increases, and increases the risk of side effects). Step increases ACTG. Antatsida (stripping down), salicilata, butadion, indometacin increase the likelihood izgyazwlenia nervous stomach, kalisberegate drugs-heavy giperkaliemii, amphotericin B and inhibitors carboangidraza - gipokaliemii, heart failure, osteoporosis, heart-glycosides arrhythmias, sodium preparations eye and гипертензии.Эргокаль��иферол and parathyroid from osteopathy caused metilprednizolonom. High doses metilprednizolona reduce the effectiveness of соматотропина.Снижае�� activity protivodiabeticakih oral means, the effectiveness of vaccines (live vaccine against metilprednizolona can cause disease). Mitotan and other inhibitors of crust napochechnikov may require increasing doses.

Overdosing

Symptoms : oedema, hypertension, a protein in the urine, reducing the filtering adults, gipokaliemia, Cardiopatia.lechenie : antatsida, big diurez and potassium chlorate, with depression and psihozah-dose reduction or elimination of drug and the appointment fenotiazinovykh drugs or lithium salts (Tricyclic antidepressants are not recommended).

Precautions

With long-term use, there is a need to control the гипоталамо-гипофизар��о-надпочечниковой system, the level of glucose in the blood serum, the ophthalmic research. Is not recommended to be in the deltoid muscle. When in / to and / m to be a change seats injections. Intraarticular software are no more than 1 in 3 Weeks Contraindicated intratekalnoe a suspension metilprednizolona acetate : contains (as some forms metilprednizolona sodium succinate) benzyl alcohol, a potentially dangerous to the local application of the nervous tissue. It may promote or accession infections caused by micro-organisms (including viruses, fungi, protozoa) and parasites (glista). The risk of complications increases with the increase of dose or combined with metilprednizolona etc. иммунодепрессантами.��еобходимо with caution applied to nonspecific yazvennom kolite, divertikulah, heavy gravis. Patients receiving doses of immune metilprednizolona should be warned about the danger of contact with diseased chicken smallpox and measles. With long-term use in children may slow growth. Complete course it is gradually reducing the dose. Cancellation may be accompanied by pain in the abdomen and pain, weakness, nausea, headache, головокружением, increased body temperature, loss of appetite, decrease in body mass index.

Dosing and Administration

Inside (on the morning after delivery), intravenous (in / in, in / m, sinoviale bags, and vagina, in the cavity of joints, in the area of skin damage) and inside Rektalno.vesroslam 4-60 mg / day once or in divided doses. Initial dose, 40 mg / sut. In some cases, up to 100 mg / sut. Supporting dose-4-12 mg / sut. The maximum daily dose is 250 Mg.detam : if insufficient napochechnikov inside 0.14 mg / kg or 4 mg / m ^ 2 per day in March reception in / m is the same dose in two days or 0,039-0,0585 mg / kg / day daily; On the testimony of others - into 0,417-1,67 mg / kg or 12,5-50 mg / m ^ 2 in three divided doses, in / m 0,139-0,835 mg / kg or 4,16-25 mg / m ^ 2 every 24 hours Adults for a / m, a 4-60 mg / day (depo-forma - 40-120 mg). B / in (пульс-терапия ") being 30 mg / kg метилпреднизолона succinate for 30 minutes and, if necessary, re-every six hours Внутрисуставно in синовиальные bags, and vagina, 20-60 mg, in the arm and abdomen плевральную to 100 mg, эпидурально-up to 80 mg, in / in-100-500 mg, in the area of skin damage-20-60 mg. With restraint in клизмой язвенном колите impose 40-120 mg, for cupping nausea and vomiting adults, in the dose of 250 mg for 20 minutes before and after 6 h after administration of drugs, children not less than 25 mg / сут.При occurrence of spontaneous remission treatment discontinued.

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