Pharmacological action Methylprednisolone 4 mg
SCS. In the systemic use of anti-inflammatory, antiallergic, desensitizing, antishock, anti-toxic and immunosuppressive effects.
For external and local application of therapeutic activity of methylprednisolone is caused by an anti-inflammatory, antiallergic and antiexudative (due to vasoconstriction effect) effect.
By anti-inflammatory activity than hydrocortisone in 5 times, has almost no mineralocorticoid activity.
Inhibits the function of leukocytes and tissue macrophages. Inhibits the release of interleukin-1, interleukin 2, interferon gamma from lymphocytes and macrophages.
Methylprednisolone inhibits the release of pituitary ACTH (and again – the synthesis of endogenous corticosteroids) and β-lipotropin, but does not reduce the level of circulating β-endorphin. Inhibits the secretion of TSH and FSH.
Interacts with specific cytoplasmic receptors and forms a complex that penetrates the cell nucleus, and stimulates the synthesis of mRNA, the latter induces the formation of proteins (including lipokortina), mediating cellular effects. Lipokortina inhibits the activity of phospholipase A2, which leads to suppression of arachidonic acid release, inhibition of prostaglandin synthesis, endoperekisey, leukotrienes, which are factors in inflammation and allergic reactions. Inhibits the release of COX (especially COX-2), which also helps to reduce the production of prostaglandins.
Contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes on inflammation. Decreases capillary permeability caused by histamine release.
Methylprednisolone has a pronounced dose-dependent effect on the metabolism of proteins, fats and carbohydrates.
Decreases in plasma protein (due to globulin) with an increase in the coefficient of albumin / globulin, albumin synthesis increases in liver and kidney.
It has a catabolic effect in the lymphoid and connective tissue, muscle, adipose tissue, skin, bone tissue. Osteoporosis and Cushing’s syndrome are the main factors limiting the long-term therapy with corticosteroids. As a result, the catabolic actions may suppress growth in children.
Stimulates the synthesis of fatty acids and triglycerides, redistribute adipose tissue (fat accumulation occurs predominantly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.
Increases absorption of carbohydrates from the gastrointestinal tract, increases the activity of glucose-6-phosphatase, which leads to increased revenues of glucose from the liver into the blood, stimulates gluconeogenesis.
Delays sodium ions and water in the body, stimulates the excretion of potassium, calcium absorption decreases from the digestive tract, promotes the leaching of calcium from the bones, increases the excretion of calcium by the kidneys.
At high doses of methylprednisolone may increase the excitability of brain tissue and helps to reduce the threshold of convulsive readiness.
Anti-inflammatory effect associated with inhibition of eosinophil release of inflammatory mediators, inducing the formation of lipokortina and reduce the number of mast cells that produce hyaluronic acid, with a decrease in the permeability of capillaries, stabilizing cell membranes and membrane organelles (especially lysosomal).
Antiallergic effect is caused by 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 that reduce the number of circulating basophils, suppressing the development of lymphoid and connective tissue, reduction of circulating lymphocytes (T-and B-cells) , mast cells, reducing the sensitivity of effector cells to the mediators of allergy, depression antibody production, changes in immune response.
In COPD the effect is mainly based on inhibition of inflammatory processes, inhibition or prevention of swelling of the mucous membranes, inhibition of eosinophilic infiltration of the submucosa of bronchial epithelium, deposition in the bronchial mucosa of circulating immune complexes, as well as braking erozirovaniya and desquamation of the mucosa. Increases the sensitivity of β-adrenergic receptors of bronchial small-and medium-sized to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus through oppression or reduce its production.
Antishock and anti-toxic effect associated with elevated blood pressure (by increasing the concentration of circulating catecholamines and restore sensitivity to adrenergic receptors, and vasoconstriction), decrease the permeability of the vascular wall, oxidant properties, activation of liver enzymes involved in the metabolism of endo-and xenobiotics.
Immunosuppressive effect is caused by inhibition of the release of cytokines (interleukin-1, interleukin-2), interferon gamma from lymphocytes and macrophages.
Inhibits the activity of fibroblasts and collagen production, reduces the possibility of the formation of scar tissue.
Stimulates excess production of hydrochloric acid and pepsin in the stomach, which increases the risk of peptic ulcers.
Pharmacokinetics Methylprednisolone 4 mg
After oral administration, is well absorbed from the gastrointestinal tract. Metabolized in the liver. T1 / 2 is about 2 hours excreted as metabolites primarily in urine.
Statement Methylprednisolone 4 mg
For oral use, on / in a (normal form of duration) and i / m injection (depot form): primary or secondary adrenal insufficiency, congenital adrenal hyperplasia, nonsuppurative thyroiditis, hypercalcemia due to tumor disease, rheumatic diseases, collagen diseases, pemphigus, bullous dermatitis herpetiformis, severe erythema multiforme, exfoliative dermatitis, severe psoriasis, severe seborrheic dermatitis, severe allergic disease, severe acute and chronic allergic and inflammatory processes involving the eye, symptomatic sarcoidosis, Loeffler’s syndrome (unresponsive to other therapies), berylliosis, focal or disseminated pulmonary tuberculosis (in conjunction with appropriate antituberculous chemotherapy), idiopathic thrombocytopenic purpura in adults, secondary thrombocytopenia in adults, acquired (autoimmune) hemolytic anemia, erythroblastopenia (erythrocytic anemia), congenital (erythroid) hypoplastic anemia, acute leukemia in children, palliative therapy for malignant tumors, in order to achieve remission of nephrotic syndrome in a critical period in ulcerative colitis and regional enteritis, multiple sclerosis exacerbation, due to cerebral edema, or swelling associated with surgery, radiation therapy, brain injury, shock due to failure of the cortex adrenal or resistant to standard therapy, tuberculous meningitis with subarachnoid block or threat thereof (together with antituberculosis chemotherapy), trichinosis with damage to the nervous system or myocardium, organ transplantation, short-term therapy in diseases of the musculoskeletal rheumatic and non-specific origin.
For the introduction of the synovial fluid or soft tissue (depot form): adjuvant therapy in acute synovitis, rheumatoid arthritis, gouty arthritis, epicondylitis, tenosynovitis nonspecific, post-traumatic osteoarthritis.
For an introduction to pathological foci (depot form): keloid scars, hypertrophic localized, infiltrative and inflammatory foci in lichen planus, psoriatic plaques, granuloma annular, neurodermatitis, discoid lupus erythematosus, diabetic lipoid necrobiosis, alopecia areata, cystic tumors of aponeurosis or tendon.
Dosage regimen Methylprednisolone 4 mg
Individual, depending on the indications, treatment regimens, the dosage form employed, the age of the patient’s clinical situation.
Side effect Methylprednisolone 4 mg
From the Endocrine: menstrual irregularities, adrenal suppression, Cushing’s syndrome, suppression of pituitary-adrenal axis, decreased carbohydrate tolerance, diabetes, steroid or a manifestation of latent diabetes mellitus, growth retardation in children, delayed sexual development in children.
Part of the digestive system: nausea, vomiting, steroid gastric and duodenal ulcers, pancreatitis, esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases – increase in liver transaminases and alkaline phosphatase.
From the Metabolic: Negative nitrogen balance due to protein catabolism, increased excretion of calcium from the body, hypocalcemia, weight gain, increased sweating.
Cardio-vascular system: potassium loss, alkalosis gipokaliemichesky, arrhythmia, bradycardia (up to heart failure), steroid myopathy, heart failure (the development or worsening of symptoms), ECG changes typical of hypokalemia, increased blood pressure, hypercoagulability, thrombosis. In patients with acute myocardial infarction – the spread of foci of necrosis, slowing the formation of scar tissue that can lead to rupture of the heart muscle.
On the part of the musculoskeletal system: slowing growth and ossification in children (premature closure of epiphyseal growth zones), osteoporosis (very rare – pathological fractures, aseptic necrosis of head of humerus and femur), muscle tendon rupture, muscle weakness, steroid myopathy, a decrease muscle mass (atrophy).
CNS: headache, increased intracranial pressure, delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor cerebellar seizures.
On the part of the vision: posterior subcapsular cataracts, increased intraocular pressure (with possible damage to the optic nerve), trophic changes of the cornea, exophthalmos, the propensity to develop secondary infections (bacterial, fungal, viral).
Dermatological reactions: petechiae, ecchymosis, thinning and fragility of the skin, hyper-or hypopigmentation, acne, striae, susceptibility to the development of pyoderma and candidiasis.
Reactions due to immunosuppressive effects: slowing of regenerative processes, reduced resistance to infections.
For parenteral administration: in rare cases of anaphylactic and allergic reactions, hyper-or hypopigmentation, atrophy of skin and subcutaneous fat, increased after intrasinovialnogo applications such as Charcot arthropathy, sterile abscess, when introduced into the pockets on the head – blindness.
Contraindications Methylprednisolone 4 mg
For short-term use for health reasons – increased sensitivity to methylprednisolone.
For intra-and entered directly into the lesion: previous arthroplasty, abnormal bleeding (endogenous or caused by the use of anticoagulants), intra-articular fracture, infection (sepsis) inflammation in joints and periarticular infections (including history), and common infectious disease, marked periarticular osteoporosis, no evidence of inflammation in the joints (“dry” joint, such as osteoarthritis, without synovitis), marked bone destruction and deformation of the joint (marked joint space narrowing, ankylosis), instability of the joint as a result of arthritis, aseptic necrosis of the form joint epiphyses of bones.
For external use: bacterial, viral, fungal skin diseases, tuberculosis, skin, cutaneous manifestations of syphilis, skin tumors, post-vaccination period, violating the integrity of the skin (ulcers, wounds), children (up to 2 years, with itching in the anal area – up to 12 years), rosacea, acne vulgaris, perioral dermatitis.
For use in ophthalmology: bacterial, viral, fungal diseases of the eye, ocular tuberculosis, trachoma, ocular epithelial integrity violation.
Pregnancy and breastfeeding Methylprednisolone 4 mg
In the I trimester is used in cases where the expected benefit of therapy to the mother outweighs the potential risk to the fetus. Long-term use during pregnancy causes fetal growth disturbance. In the III trimester of pregnancy there is a danger of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.
In the period of lactation is used in cases where the expected benefits of therapy to the mother outweighs the potential risk to the infant.
Cautions Methylprednisolone 4 mg
C used cautiously in parasitic and infectious diseases of viral, fungal or bacterial origin (currently or recently transferred, including the recent contact with a patient) – Herpes simplex, herpes zoster (viremicheskaya phase), chicken pox, measles, amoebiasis, strongyloidiasis (or suspect), systemic mycosis, active and latent tuberculosis. Application for serious infectious diseases is permissible only against specific therapy.
Be wary of over 8 weeks before and 2 weeks after vaccination), and lymphadenitis after BCG vaccination, and immunodeficiency (including AIDS or HIV infection).
Be wary of diseases of the digestive tract: gastric ulcers and duodenal ulcers, esophagitis, gastritis, acute or latent peptic ulcer, the newly created anastomosis of the intestine, ulcerative colitis, with the threat of perforation or abscess formation, diverticulitis.
Be wary of diseases of the cardiovascular system, including after recent myocardial infarction (in patients with acute and subacute myocardial necrosis may spread the fire, slowing the formation of scar tissue and thereby break the heart muscle), decompensated congestive heart failure, hypertension, hyperlipidemia), and endocrine diseases – diabetes ( including breach of tolerance to carbohydrates), hyperthyroidism, hypothyroidism, Cushing’s disease, severe renal and / or liver failure, nefrourolitiaz, with hypoalbuminemia and conditions that predispose to its occurrence, with systemic osteoporosis, myasthenia gravis, acute psychosis , obesity (III-IV degree), and poliomyelitis (except bulbar form of encephalitis), and Open-angle-closure glaucoma.
If necessary, intra be used with caution in patients with severe general condition, failure (or brevity) of the 2 previous injections (taking into account individual properties used SCS).
Is not effective in septic shock (possibly increasing mortality).
With stress during therapy shown to increase the dose of GCS.
With tuberculosis may use only in conjunction with appropriate antituberculous therapy.
After taking a few days cancellation should be done gradually.
Intradermal administration should not be deep. Depo-form does not introduce non-recommended methods (including I / O).
In the period of treatment not to conduct any kinds of vaccinations.
The children in the use of corticosteroids during growth is possible only if absolutely indicated and under particularly close medical supervision.
Drug Interactions Methylprednisolone 4 mg
While the use of barbiturates may decrease the effectiveness of methylprednisolone.
With the simultaneous use of NSAIDs may increase the risk of erosive and ulcerative lesions of the gastrointestinal tract.
With the simultaneous use of methylprednisolone with oral anticoagulants, heparin increased or decreased anticoagulant action, with salicylates – may decrease the action of salicylates, with thiazide diuretics, furosemide – may potentiate hypokalemia.
In an application with glibenclamide, metformin, insulin decreases the effectiveness of hypoglycemic agents, with ketoconazole, itraconazole – increases the concentration of methylprednisolone in plasma MTX – synergism immunosuppressive action, with neostigmine, pyridostigmine – myasthenic crisis may develop, with pancuronium – Reduction of neuromuscular blockade, with salbutamol – increased efficiency and potential toxicity of salbutamol, with rifampicin – an increase in the clearance of methylprednisolone.
While the use of phenytoin, phenobarbital increases the clearance of methylprednisolone and decrease efficiency.
With the simultaneous use of phenytoin may decrease, with cyclosporine – the inhibition of metabolism of cyclosporine and methylprednisolone, with erythromycin – is likely to inhibit the metabolism of methylprednisolone.
