Metipred, pills 4mg, 30pcs

Composition

Pills. 1 tab. :

– methylprednisolone 4 or 16 mg;

excipients:

lactose monohydrate,

corn starch,

magnesium stearate,

gelatin,

talc,

purified water.

Pharmacological action

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

It interacts with specific cytoplasmic receptors (receptors for glucocorticosteroids (GCS) are present in all tissues, especially in the liver) to form a complex that induces the formation of proteins (including enzymes that regulate vital processes in cells. ) Protein metabolism: reduces the amount of globulins in plasma, increases the synthesis of albumins in the liver and kidneys (with an increase in the albumin / globulin ratio), reduces protein synthesis and increases catabolism in muscle tissue.

Lipid metabolism:

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

Carbohydrate metabolism:

increases the absorption of carbohydrates from the gastrointestinal tract; increases the activity of glucose-6-phosphatase (increased glucose intake from the liver to the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); promotes the development of hyperglycemia.

Water-electrolyte exchange:

detains sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, reduces the mineralization of bone tissue. The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils and mast cells; induction of the formation of lipocortins and a decrease in the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; 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 release of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes that contribute to the processes of inflammation, allergies, etc. ), the synthesis of “pro-inflammatory cytokines” (interleukin 1, tumor necrosis factor alpha, etc. ); increases the resistance of the cell membrane to various damaging factors.

The immunosuppressive effect is due to the induced involution of lymphoid tissue, inhibition of lymphocyte proliferation (especially T-lymphocytes), suppression of B-cell migration and interaction of T – and B-lymphocytes, inhibition of the release of cytokines (interleukin-1,2; interferon gamma) from lymphocytes and macrophages, and a decrease in antibody formation.

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

In obstructive diseases of the respiratory tract, the effect is mainly due to inhibition of inflammatory processes, prevention or reduction of the severity of mucosal edema, reduction of eosinophilic infiltration of the submucosal layer of the bronchial epithelium and deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucosa.

Increases the sensitivity of small and medium-sized bronchial beta-adrenergic receptors to endogenous catecholamines and exogenous sympathomimetics, reduces mucus viscosity by reducing its production. Inhibits the synthesis and secretion of adrenocorticotropic hormone (ACTH) and, secondarily, the synthesis of endogenous corticosteroids. It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

Indications

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

acute and chronic inflammatory diseases of the joints – gout and psoriatic arthritis, osteoarthritis (including PTSD), polyarthritis (including the elderly), frozen shoulder, ankylosing spondylitis (Bechterew’s disease), juvenile arthritis, still’s syndrome in adults, bursitis, unspecified tendosynovitis, synovitis and epicondylitis, acute rheumatic fever, rheumatic carditis, chorea;

bronchial asthma, asthmatic status;

acute and chronic allergic diseases (including allergic reactions to medications and food products, serum sickness, urticaria, allergic rhinitis, angioedema, drug rash, hay fever);

skin diseases – pemphigus, psoriasis, eczema, atopic dermatitis (common neurodermatitis), contract dermatitis (with the defeat of the large surface of the skin), the toxicoderma, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell’s syndrome), bullous dermatitis herpetiformis, the Stevens-Johnson syndrome; brain edema (including on the background of a brain tumor or associated with surgery, radiation therapy, or head injury) after a preliminary parenteral corticosteroids;

allergic eye disease and allergic conjunctivitis;

inflammatory diseases of the eye – sympathetic ophthalmia, heavy sluggish front and posterior uveitis, optic neuritis; primary or secondary adrenal insufficiency (including state after removal of the adrenal glands);

congenital adrenal hyperplasia; kidney disease of autoimmune origin (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 (RBC anemia), congenital (erythroid) hypoplastic anemia;

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

tuberculous meningitis, pulmonary tuberculosis, aspiration pneumonia (in combination with a specific chemotherapy); the beryllium syndrome Leffler (not amenable to other therapy);

lung cancer (in combination with cytostatics); multiple sclerosis

ulcerative colitis, Crohn’s disease, local enteritis;

hepatitis;

hypoglycemic States;

prevention of graft rejection in organ transplants; hypercalcemia on the background of cancer, nausea and vomiting during cytostatic therapy; multiple myeloma.

Contraindications

For short-term use for vital indications, the only contraindication is hypersensitivity to methylprednisolone or the components of the drug.

In children during the growth period, corticosteroids should be used only according to absolute indications and with careful medical supervision.

With caution, the drug should be prescribed for the following diseases and conditions: diseases of the gastrointestinal tract – peptic ulcer of the stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, UC with the threat of perforation or abscessing, diverticulitis; parasitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently transferred, including recent contact with the patient) – simple herpes zoster (viremic phase), chickenpox, measles, amoebiasis, strongyloidosis, 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 states (including AIDS or HIV infection); diseases of the cardiovascular system (recent myocardial infarction-patients with acute and subacute myocardial infarction may spread necrosis, slow the formation of scar tissue and, as a result, rupture of the heart muscle), severe chronic heart failure, arterial hypertension, hyperlipidemia; endocrine diseases – diabetes mellitus (including impaired tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Itsenko – Cushing’s disease, obesity (Grade III – IV); severe chronic renal and/or hepatic insufficiency, nephrourolithiasis; hypoalbuminemia and conditions predisposing to its occurrence; systemic osteoporosis, myasthenia gravis, acute psychosis, polio (except for the form of bulbar encephalitis), open-and angle-closure glaucoma; pregnancy.

Side effects

From the endocrine system: reduced glucose tolerance, steroid diabetes mellitus, manifestation of latent diabetes mellitus, adrenal suppression, Itsenko-Cushing syndrome (moon-shaped face, pituitary obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae), delayed sexual development in children.

From the digestive system: nausea, vomiting, pancreatitis, steroid ulcers of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding, perforation of the gastrointestinal tract wall, impaired appetite, digestive disorders, flatulence, hiccups; rarely-increased activity of hepatic transaminases and alkaline phosphatase.

From the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); in predisposed patients, the development or increase in the severity of heart failure, ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis; in patients with acute and subacute myocardial infarction, the spread of necrosis may occur, the formation of scar tissue may slow down, which can lead to rupture of the heart muscle.

From the central nervous system and peripheral nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness, restlessness, insomnia, dizziness, vertigo, pseudotumor of the cerebellum, headache, convulsions.

From the sensory organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral infections of the eyes, trophic changes in the cornea, exophthalmos, sudden loss of vision (with parenteral use in the head, neck, nasal concha, scalp, crystals of the drug may be deposited in the vessels of the eye).

From the side of metabolism: increased calcium excretion, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating; due to mineralocorticoid activity-fluid retention and sodium (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

From the musculoskeletal system: slowing of growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely – pathological bone fractures, aseptic necrosis of the head of the humerus and femur), muscle tendon rupture, steroid myopathy, decreased muscle mass (atrophy).

Dermatological reactions: delayed wound healing, petechiae, ecchymosis, thinning of the skin, hyper-or hypopigmentation, steroid acne, striae, tendency to develop pyoderma and candidiasis.

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

Local reactions with parenteral use: burning, numbness, pain, tingling at the injection site, infection of the injection site; rarely-necrosis of surrounding tissues, scarring at the injection site, atrophy of the skin and subcutaneous tissue with intravenous use (especially dangerous introduction to the deltoid muscle).

Others: the development or exacerbation of infections (the appearance of this side effect is promoted by jointly used immunosuppressants and vaccination), leukocyturia, withdrawal syndrome, ” hot flashes ” of blood to the head.

Interaction

Co-use of methylprednisolone: with inducers of hepatic microsomal enzymes (phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration (increase metabolism); with diuretics (especially thiazidetype and carbonic anhydrase inhibitors) and amphotericin b leads to increased excretion of potassium and increase the risk of development of heart failure;

the carbonic anhydrase inhibitors and loop diuretics can increase the risk of osteoporosis;

with sodium drugs contributes to the development of edema and increase in blood pressure;

with cardiac glycosides leads to a deterioration of their tolerance and increased likelihood of developing ventricular extrasystolia (because it causes hypokalemia);

with indirect anticoagulants contributes to the weakening (strengthening less) their actions (requires dose adjustment); with anticoagulants and thrombolytics increase the risk of bleeding from ulcers in the gastrointestinal tract;

ethanol and NSAIDs enhances the risk of erosive-ulcerative lesions in the gastrointestinal tract and the development of hemorrhage (in combination with NSAIDs in the treatment of arthritis may reduce the dose of GCS due to summation of therapeutic effect);

with Indometacin increases the risk of side effects of methylprednisolone (displacement of Indometacin methylprednisolone connection with albumin); with paracetamol increases the risk of hepatotoxicity (induction of hepatic enzymes and formation of a toxic metabolite of paracetamol);

with acetylsalicylic acid-accelerates its excretion and reduces the concentration in the blood (the abolition of methylprednisolone levels of salicylates in the blood increases, and increases the risk of side effects);

with insulin and oral hypoglycemic agents, antihypertensive agents reduced their effectiveness; vitamin D decreases its effect on calcium absorption in the intestine;

with growth hormone reduced the effectiveness of the latter;

with praziquantel reduces the concentration of the latter;

with m-holinoblokatorami (including antihistamines, and tricyclic antidepressants) and nitrate promotes increase in intraocular pressure; with isoniazid and mexiletine increases their metabolism (especially in slow acetylators), which leads to a decrease in their plasma concentrations.

ACTH enhances the action of methylprednisolone. Ergocalciferol and parathyroid hormone inhibit the development of osteopathy caused by methylprednisolone. Cyclosporine and ketoconazole, slowing down the metabolism of methylprednisolone, can in some cases increase its toxicity.

Simultaneous use of androgens and steroid anabolic drugs with methylprednisolone contributes to the development of peripheral edema, hirsutism and acne. Estrogens and oral estrogen-containing contraceptives reduce the clearance of methylprednisolone, which may be accompanied by an increase in the severity of its action.

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

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

When used concomitantly with antithyroid drugs, the clearance of methylprednisolone decreases, and with thyroid hormones, the clearance of methylprednisolone increases.

Pharmaceutical interaction

Possible pharmaceutical incompatibility of methylprednisolone with other intravenous drugs. It is recommended to be administered separately from other drugs (IV bolus, or through another dropper, as a second solution).

How to take, course of use and dosage

Inside, during or immediately after a meal, with a small amount of liquid.

The entire daily dose of the drug is recommended to be taken once or twice a daily dose — every other day, taking into account the circadian rhythm of endogenous corticosteroid secretion in the interval from 6 to 8 hours in the morning.

A high daily dose can be divided into 2-4 doses, while a large dose should be taken in the morning. The initial dose of the drug can range from 4 to 48 mg of methylprednisolone per day, depending on the nature of the disease.

For less severe diseases, lower doses are usually sufficient, although some patients may require 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 discontinued and another type of therapy should be prescribed to the patient.

For children, the dose is determined by the doctor, taking into account the mass or surface of the body. With adrenal insufficiency-inside 0.18 mg / kg or 3.33 mg / m2 per day in 3 doses, with other indications-0.42-1.67 mg / kg or 12.5-50 mg / m2 per day in 3 doses.

With prolonged use of the drug, the daily dose should be reduced gradually. Long-term therapy should not be stopped abruptly!

Overdose

Symptoms: the side effects described above may increase.

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

Special instructions

Store the prepared solution for parenteral use at a temperature of 15° to 20°C and use it for 12 hours. If the prepared solution is stored in the refrigerator at a temperature of 2°to 8°C, it can be used for 24 hours.

During treatment with Metipred (especially long-term), it is necessary to observe an optometrist, monitor blood pressure, the state of water and electrolyte balance, as well as the picture of peripheral blood and blood glucose concentration. In order to reduce side effects, you can prescribe antacids, as well as increase the intake of potassium in the body (diet, potassium preparations).

Food should be rich in protein, vitamins, with a limited content of fats, carbohydrates and table salt. The effect of the drug is enhanced in patients with hypothyroidism and cirrhosis of the liver. The drug may increase existing emotional instability or psychotic disorders.

If 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, slowing the formation of scar tissue and rupture of the heart muscle.

In stressful situations during maintenance treatment (incl.surgical operations, trauma, infectious diseases), the dose of the drug should be adjusted due to the increased need for corticosteroids. With sudden withdrawal, especially in the case of previous use of high doses, withdrawal syndrome may develop (anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness), as well as exacerbation of the disease for which Metipred was prescribed.

During treatment with Metipred, vaccination should not be carried out due to 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, it is necessary to simultaneously treat with antibiotics of bactericidal action.

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

In patients with diabetes mellitus, the concentration of glucose in the blood should be monitored and, if necessary, the dose of hypoglycemic agents should be adjusted. X-ray monitoring of the osteoarticular system (images of the spine, hand) is shown. Metipred in patients with latent infectious diseases of the kidneys and urinary tract can cause leukocyturia, which may have diagnostic significance. Metipred increases the content of metabolites of 11-and 17-hydroxyketocorticosteroids.

Storage conditions

At a temperature of 15-25 °C

Shelf life

5 years

Active ingredient

Methylprednisolone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Eczema, Osteoarthritis and Arthritis, Dermatitis, Hepatitis, Allergies, Bronchial Asthma, Crohn ‘s Disease