Metipred, tablets 4 mg 30 pcs

Methylprednisolone is a synthetic glucocorticosteroid drug. It has anti-inflammatory, anti-allergic, immunosuppressive effects, increases the sensitivity of beta-adrenoreceptors to endogenous catecholamines.

It interacts with specific cytoplasmic receptors (all tissues have receptors for glucocorticosteroids (GCS), especially with liver) with the formation of a complex, inducing the formation of proteins (including enzymes regulating cells). Protein metabolism: reduces the number of globulins in the plasma, increases the synthesis of albumin in the liver and kidneys (with an increase in albumin/globulin ratio), reduces synthesis and increases catabolism of protein in muscle tissue.

Lipid metabolism:

increases the synthesis of higher fatty acids and triglycerides, redistributes fat (fat accumulation occurs primarily in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia

Carbohydrate metabolism:

increases absorption of carbohydrates from the gastrointestinal tract; increases glucose-6-phosphatase activity (increasing glucose entry from the liver into the blood); increases phosphoenolpyruvate carboxylase activity and aminotransferase synthesis (activation of gluconeogenesis); promotes hyperglycemia.

Water-electrolyte metabolism:

retains sodium and water in the body, stimulates potassium excretion (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, reduces bone mineralization. Anti-inflammatory effect is connected with inhibition of release of inflammatory mediators by eosinophils and mast cells; induction of formation of lipocortins and reduction of number of mast cells producing hyaluronic acid; reduction of capillary permeability and stabilization of cell membranes (especially lysosomal) and organelle membranes.

It acts on all stages of the inflammatory process: inhibits the synthesis of prostaglandins at the level of arachidonic acid (lipocortin inhibits phospholipase A2, inhibits the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, contributing to inflammatory processes, allergies and others).), the synthesis of “pro-inflammatory cytokines” (interleukin 1, tumor necrosis factor alpha, etc.), increases the resistance of the cell membrane to the action of various damaging factors.

The immunosuppressive effect is caused by involution of lymphoid tissue, inhibition of lymphocyte proliferation (especially T-lymphocytes), suppression of B-cell migration and interaction between T- and B-lymphocytes, inhibition of cytokine release (interleukin-1, 2 interferon) from lymphocytes and macrophages and decrease of antibody formation.

The anti-allergic effect is developed as a result of decrease of synthesis and secretion of allergy mediators, inhibition of release of histamine and other biologically active substances from sensitized mast cells and basophils. biologically active substances, decrease of the number of circulating basophils, T- and B-lymphocytes, mast cells; suppression of lymphoid and connective tissue development, decrease of sensitivity of effector cells to allergy mediators, suppression of antibody formation, changes in the body’s immune response.

In obstructive respiratory tract diseases the action is caused mainly by inhibition of inflammatory processes, prevention or reduction of mucous membrane edema, decrease of eosinophilic infiltration of submucous layer of bronchial epithelium and deposition of circulating immune complexes in bronchial mucosa and also inhibition of erosion and mucosa desquamation.

It increases sensitivity of beta-adrenoreceptors of small and medium caliber bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces mucus viscosity by reducing its production. Inhibits synthesis and secretion of adrenocorticotropic hormone (ACTH) and secondary to synthesis of endogenous GCS. Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

Indications

Systemic connective tissue diseases (SLE, scleroderma, periarteritis nodosa, dermatomyositis, rheumatoid arthritis);

acute and chronic inflammatory diseases of the joints – gouty and psoriatic arthritis, osteoarthritis (including post-traumatic).Posttraumatic), polyarthritis (including arthritis tendencies), arthritis tendencies (including arthritis tendencies in the legs), and arthritis tendencies in the arms.ч. periarthritis, ankylosing spondylitis (Behterev’s disease), juvenile arthritis, Still’s syndrome in adults, bursitis, nonspecific tenosynovitis, synovitis and epicondylitis; Acute rheumatism, rheumatic carditis, minor chorea;

bronchial asthma, asthmatic status;

acute and chronic allergic diseases (includingч.

allergic reactions to medicines and foods, serum sickness, urticaria, allergic rhinitis, Quincke’s edema, drug exanthema, pollinosis);

Skin diseases – vesicles, psoriasis, eczema, atopic dermatitis (widespread neurodermitis), contractile dermatitis (with involvement of a large skin surface), toxiderma, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell syndrome), bullous herpetiform dermatitis, Stevens-Johnson syndrome; brain edema (incl.ч. in the background of a brain tumor or associated with surgery, radiation therapy, or head trauma) after prior parenteral use of GCS;

allergic eye disease – allergic forms of conjunctivitis;

Inflammatory eye disease – sympathetic ophthalmia, severe flaccid anterior and posterior uveitis, optic neuritis; primary or secondary adrenal insufficiency (including conditions after adrenal removal.

congenital adrenal hyperplasia; autoimmune kidney disease (including acute glomerulonephritis);

nephrotic syndrome;

subacute thyroiditis; diseases of the blood and hematopoietic system – agranulocytosis, panmyelopathy, autoimmune hemolytic anemia, lymph and myeloid leukemia, lymphogranulomatosis, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocytic anemia), congenital (erythroid) hypoplastic anemia;

interstitial lung diseases – acute alveolitis, pulmonary fibrosis, stage II-III sarcoidosis;

Tuberculous meningitis, pulmonary tuberculosis, aspiration pneumonia (in combination with specific chemotherapy); berylliosis, Leffler syndrome (not amenable to other therapy);

lung cancer (in combination with cytostatics); multiple sclerosis;

ulcerative colitis, Crohn’s disease, localized enteritis;

Hepatitis;

Hypoglycemic conditions;

prevention of transplant rejection reactions in organ transplants; hypercalcemia in the background of cancer, nausea and vomiting in cytostatic therapy; myeloma disease.

Active ingredient

Composition

Tablets. 1 tablet:

– methylprednisolone 4 or 16 mg;

excipients:

lactose monohydrate,

corn starch,

magnesium stearate,

gelatin,

talc,

purified water.

How to take, the dosage

Overly, during or immediately after meals, with a small amount of liquid.

The full daily dose of the drug is recommended to be taken once or twice daily dose taken every other day with regard to circadian rhythm of endogenous GCS secretion between 6 and 8 a.m.

The high daily dose can be divided into 2-4 doses, with a higher dose to be taken in the morning. The starting dose of the drug may be 4 to 48 mg of methylprednisolone per day, depending on the nature of the disease.

Lower doses are usually sufficient for less severe disease, although some people may need higher doses.

High doses may be required for diseases and conditions such as multiple sclerosis (200 mg/day), brain edema (200-1000 mg/day) and organ transplantation (up to 7 mg/kg/day). If a satisfactory clinical effect is not obtained after a sufficient period of time, the drug should be withdrawn and another therapy should be prescribed to the patient.

In children the dose is determined by the physician with regard to weight or body surface area. In adrenal insufficiency – orally 0.18 mg/kg or 3.33 mg/m2 per day in 3 doses, in other indications – 0.42-1.67 mg/kg or 12.5-50 mg/m2 per day in 3 doses.

In long-term use of the drug the daily dose should be reduced gradually. Long-term therapy should not be stopped suddenly!

Interaction

Simultaneous administration of methylprednisolone: with inducers of hepatic microsomal enzymes (phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration (increased metabolic rate); with diuretics (especially thiazide-like and carboanhydrase inhibitors) and amphotericin B leads to increased potassium excretion and increased risk of heart failure;

Carboanhydrase inhibitors and “loop” diuretics may increase the risk of osteoporosis;

with sodium-containing drugs promotes edema and increased BP;

With cardiac glycosides leads to poor tolerance to them and increased likelihood of ventricular extrasytole (due to hypokalemia caused);

with indirect anticoagulants contributes to weakening (rarely increasing) their action (requires dose adjustment); With anticoagulants and thrombolytics it leads to increased risk of GIT ulcers bleeding;

With ethanol and NSAIDs it increases the risk of erosive-ulcerative lesions in the GIT and bleeding (in combination with NSAIDs in the treatment of arthritis the dosage of GCS may be reduced due to the summation of therapeutic effect);

With indomethacin increases the risk of side effects of methylprednisolone (displacement by indomethacin of methylprednisolone from binding to albumin); with paracetamol increases the risk of hepatotoxicity (induction of liver enzymes and formation of toxic metabolite of paracetamol);

with acetylsalicylic acid accelerates its excretion and reduces its concentration in blood (when methylprednisolone is cancelled the level of salicylates in blood increases and the risk of side effects increases);

with insulin and oral hypoglycemic drugs, hypotensive agents reduces their effectiveness; with vitamin D reduces its effect on intestinal calcium absorption;

with STH reduces the effectiveness of the latter;

with praziquantel reduces the concentration of the latter;

with m-cholinoblockers (including antihistamines and tricyclic antidepressants) and nitrates increases intraocular pressure; with isoniazid and mexiletine increases their metabolism (especially in “slow” acetylators), which leads to a decrease in their plasma concentrations.

ACTH increases the effect of methylprednisolone. Ergocalciferol and parathormone prevent the development of osteopathy caused by methylprednisolone. Cyclosporine and ketoconazole, slowing the metabolism of methylprednisolone, may in some cases increase its toxicity.

The simultaneous administration of androgens and steroid anabolic drugs with methylprednisolone promotes the development of peripheral edema, hirsutism and the appearance of acne. Estrogens and oral estrogen-containing contraceptives decrease clearance of methylprednisolone, which may be accompanied by an increase in the severity of its effects.

Mitotan and other inhibitors of adrenal cortex function may necessitate increasing the dose of methylprednisolone. When used concomitantly with live antiviral vaccines and against a background of other types of immunization, it increases the risk of virus activation and development of infections. Immunosuppressants increase the risk of developing infections and lymphoma or other lymphoproliferative disorders associated with Epstein-Barr virus.

Antipsychotics (neuroleptics) and azathioprine increase the risk of cataracts when methylprednisolone is prescribed. Concomitant administration of antacids reduces absorption of methylprednisolone.

Concomitant use with antithyroid drugs decreases and with thyroid hormones increases clearance of methylprednisolone.

Pharmaceutical interaction

Pharmaceutical incompatibility of methylprednisolone with other intravenous drugs is possible. It is recommended to administer it separately from other drugs (intravenously bolus or via another IV, as a second solution).

Special Instructions

Prepared solution for parenteral administration should be stored at 15° to 20°C and used within 12 h. If the prepared solution is stored in the refrigerator at 2° to 8°C, it can be used within 24 hours.

During treatment with Metipred (especially long-term) it is necessary to monitor the ophthalmologist, BP, water-electrolyte balance, as well as peripheral blood picture and blood glucose concentration. In order to reduce side effects antacids may be prescribed, as well as to increase potassium intake into the body (diet, potassium supplements).

The diet should be rich in proteins, vitamins, with restriction of fats, carbohydrates and table salt. The action of the drug is increased in patients with hypothyroidism and cirrhosis. The drug may aggravate existing emotional instability or psychotic disorders.

When a history of psychosis is indicated, Metipred in high doses is prescribed under strict medical supervision. Caution should be used in acute and subacute myocardial infarction due to the possibility of spreading the focus of necrosis, delayed formation of scar tissue and rupture of the heart muscle.

In stressful situations during maintenance treatment (including surgery, trauma, infectious diseases), the drug dose should be adjusted due to increased need for GCS. In case of abrupt withdrawal, especially in case of previous use of high doses, withdrawal syndrome may develop (anorexia, nausea, lethargy, generalized muscular-skeletal pain, general weakness) and exacerbation of the disease for which Metipred was prescribed.

Vaccination should not be performed during treatment with Metipred in connection with a decrease in the immune response and, consequently, a decrease in the effectiveness of the vaccine. When prescribing Metipred for intercurrent infections, septic conditions and tuberculosis, antibiotics with bactericidal action must be treated at the same time.

In children during long-term treatment with Metipred it is necessary to monitor closely the dynamics of growth and development. Children who have been in contact with patients with measles or chickenpox during treatment are prophylactically prescribed specific immunoglobulins. Due to the weak mineralocorticoid effect for replacement therapy in adrenal insufficiency Metipred is used in combination with mineralocorticoids.

In patients with diabetes mellitus the blood glucose concentration should be monitored and if necessary the dose of hypoglycemic agents should be adjusted. Radiological monitoring of the bone and joint system (images of the spine, hand) is indicated. Metipred in patients with latent renal and urinary tract infections may cause leukocyturia, which may be of diagnostic value. Metipred increases metabolites of 11- and 17-oxyketocorticosteroids.

Contraindications

The only contraindication for short-term use for vital signs is hypersensitivity to methylprednisolone or components of the drug.

In children during growth, GCS should be used only for absolute indications and under close medical supervision.

The drug should be used with caution in the following diseases and conditions: Gastrointestinal diseases – gastric and duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, IBD with the threat of perforation or abscessing, diverticulitis; parasitic and infectious diseases of viral, fungal, or bacterial nature (current or recent, including recent exposure) – herpes simplex, herpes zoster (viremic phase), varicella, measles, amebiasis, strongyloidiasis, systemic mycosis; Active and latent tuberculosis (use in severe infectious diseases is allowed only against the background of specific therapy); pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination, immunodeficiency conditions (including AIDS or HIV infection).Cardiovascular diseases (including recent myocardial infarction – patients with acute and subacute myocardial infarction may have spread necrosis, delayed scar tissue formation and, therefore, rupture of the heart muscle), severe chronic heart failure, hypertension, hyperlipidemia, endocrine diseases – diabetes mellitus (including diabetes mellitus, and hyperlipidemia), and other immune diseases.ч. carbohydrate tolerance disorders), thyrotoxicosis, hypothyroidism, Icenko-Cushing’s disease, obesity (III-IV degree); severe chronic renal and/or hepatic insufficiency, nephrourolithiasis; Hypoalbuminemia and conditions predisposing to its occurrence; systemic osteoporosis, myasthenia gravis, acute psychosis, poliomyelitis (except for bulbar encephalitis), open- and closed-angle glaucoma; pregnancy.

Side effects

Endocrine system disorders: decreased glucose tolerance, steroid diabetes mellitus, manifestation of latent diabetes mellitus, depressed adrenal function, Icenko-Cushing’s syndrome (moon-shaped face, pituitary obesity, hirsutism, increased BP, dysmenorrhea, amenorrhea, muscle weakness, stretch marks), delayed sexual development in children.

Digestive system disorders: nausea, vomiting, pancreatitis, steroid gastric and duodenal ulcer, erosive esophagitis, gastrointestinal bleeding, perforation of the gastrointestinal wall, appetite disorders, digestive disorders, flatulence, hiccups; rarely – increased liver transaminase and ALP activity.

Cardiovascular system disorders: arrhythmias, bradycardia (up to cardiac arrest); in predisposed patients, development or worsening of the severity of heart failure, ECG changes characteristic of hypokalemia, increased BP, hypercoagulation, thrombosis; in patients with acute and subacute myocardial infarction, spread of necrosis focus, delayed formation of scar tissue, which may lead to rupture of the heart muscle may occur.

CNS and peripheral nervous system disorders: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness, anxiety, insomnia, dizziness, vertigo, cerebellar pseudotumor, headache, seizures.

Sensory organs: Posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, susceptibility to the development of secondary bacterial, fungal or viral eye infections, trophic changes of the cornea, exophthalmus, sudden loss of vision (when parenteral administration in the head, neck, nasal cavities, scalp may deposit drug crystals in the vessels of the eye).

Metabolism disorders: increased calcium excretion, hypocalcemia, increased body weight, negative nitrogen balance (increased protein breakdown), increased sweating; caused by mineralocorticoid activity – fluid and sodium retention (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

Muscular system disorders: growth retardation and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely – pathological bone fractures, aseptic necrosis of the humeral and femoral head), rupture of muscle tendons, steroid myopathy, decrease of muscle mass (atrophy).

Dermatological reactions: delayed wound healing, petechiae, ecchymoses, skin thinning, hyper- or hypopigmentation, steroid acne, stretch marks, tendency to develop pyoderma and candidiasis.

Allergic reactions: skin rash, itching, anaphylactic shock, local allergic reactions.

Local reactions when parenteral administration: burning, numbness, pain, tingling at the injection site, infection of the injection site; necrosis of surrounding tissues, scar formation at the injection site, skin and subcutaneous tissue atrophy in case of injection (injection into the deltoid muscle is especially dangerous).

Others: development or exacerbation of infections (the appearance of this side effect is promoted by co-administration of immunosuppressants and vaccination), leukocyturia, withdrawal syndrome, “flushes” of blood to the head.

Overdose

Symptoms: possible worsening of the above side effects.

Treatment: symptomatic. It is necessary to reduce the dose of Metipred.

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