Metipred - instructions for use, analogs, reviews and release forms (4 mg tablets, injections in injections) hormonal drug for the treatment of rheumatoid arthritis, in gynecology in adults, children and in planning pregnancy. Alcohol

In this article you can get acquainted with the instructions for the use of a hormonal drug Meti. There are reviews of visitors to the site - consumers of this medication, as well as opinions of physicians specialists on the use of Metipred in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Metipred in the presence of existing structural analogues.Use for the treatment of rheumatoid arthritis and use in gynecology in adults, children, as well as in planning pregnancy and lactation. Interaction of the drug with alcohol.

Meti - synthetic glucocorticosteroid (GCS). Has anti-inflammatory, antiallergic, immunosuppressive action, increases the sensitivity of beta-adrenoreceptors to endogenous catecholamines.

It interacts with specific cytoplasmic receptors (receptors for GCS are present in all tissues, especially in the liver), with the formation of a complex inducing the formation of proteins (including enzymes that regulate vital processes in cells).

The effect of methylprednisolone (the active substance of the drug Metipred) on protein metabolism: reduces the number of globulins in plasma, increases the synthesis of albumins in the liver and kidneys (with increasing albumin / globulin ratio), reduces synthesis and enhances protein catabolism in muscle tissue.

The effect of methylprednisolone on lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (fat accumulation occurs predominantly in the region of the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.

The effect of methylprednisolone on carbohydrate metabolism: increases the absorption of carbohydrates from the digestive tract, increases the activity of glucose-6-phosphatase (increases the intake of glucose from the liver into the blood), increases the activity of phosphoenolpyruvate carboxylase and synthesis of aminotransferases (activates gluconeogenesis), promotes the development of hyperglycemia.

The effect of methylprednisolone on water-electrolyte metabolism: retards sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the digestive tract, reduces the mineralization of bone tissue.

The anti-inflammatory effect is associated with the suppression of the release of eosinophils and mast cells by inflammatory mediators, inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid, with a decrease in capillary permeability, stabilization of cell membranes (especially lysosomal) and organelle membranes. Effects on all stages of the inflammatory process: inhibits the synthesis of prostaglandins at the level of arachidonic acid (lipocortin depresses phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endopersides, leukotrienes,contributing, incl. processes of inflammation, allergies), the synthesis of proinflammatory cytokines (including interleukin 1, tumor necrosis factor alpha), increases the resistance of the cell membrane to the action of various damaging factors.

Immunosuppressive effect is caused by induced lymphoid tissue involution, suppression of lymphocyte proliferation (especially T-lymphocytes), suppression of B-cell migration and interaction of T and B lymphocytes, inhibition of release of cytokines (interleukin-1, 2, gamma-interferon) from lymphocytes and macrophages and a decrease in the formation of antibodies.

The antiallergic effect develops as a result of a decrease in the synthesis and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils of histamine and other biologically active substances, a decrease in the number of circulating basophils, T- and B-lymphocytes, mast cells, suppression of lymphoid and connective tissue development, sensitivity of effector cells to mediators of allergy, inhibition of antibody formation, changes in the immune response of the body.

In obstructive airway disease,inhibition of inflammatory processes, prevention or reduction of the degree of edema of the mucous membranes, a decrease in the eosinophilic infiltration of the submucosal layer of bronchial epithelium and the deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucosa. Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchial tubes to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.

Suppresses the synthesis and secretion of ACTH and, again, the synthesis of endogenous GCS.

It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

Composition

Methylprednisolone + auxiliary substances.

Pharmacokinetics

When ingested quickly absorbed, the absorption is more than 70%. Exposed to the effect of "first passage" through the liver.

With intramuscular injection, the absorption is complete and fast enough. Bioavailability with the / m introduction is 89%.

Metabolized mainly in the liver. Metabolites (11-keto- and 20-hydroxy compounds) do not possess glucocorticoid activity and are excreted predominantlykidneys. Within 24 hours about 85% of the administered dose is found in the urine, and about 10% - in the stool. Penetrates through the blood-brain barrier (GEB) and the placental barrier. Metabolites are found in breast milk.

Indications

For oral administration:

• systemic connective tissue diseases (SLE, scleroderma, nodular periarteritis, dermatomyositis, rheumatoid arthritis);
• acute and chronic inflammatory diseases of the joints - gouty and psoriatic arthritis, osteoarthritis (including post-traumatic), polyarthritis (including senile), humeropathy periarthritis, ankylosing spondylitis (Bechterew's disease), juvenile arthritis, Still's syndrome in adults, bursitis, nonspecific tenosynovitis, synovitis and epicondylitis;
• acute rheumatism, rheumatic carditis, small chorea;
• bronchial asthma, asthmatic status;
• acute and chronic allergic diseases (including allergic reactions to medicines and food products, serum sickness, urticaria, allergic rhinitis, Quincke's edema, drug exanthema, pollinosis);
• Skin diseases - pemphigus, psoriasis, eczema, atopic dermatitis (common neurodermatitis),contracted dermatitis (with the defeat of a large surface of the skin), toxicermy, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), bullous herpetiform dermatitis, Stevens-Johnson syndrome;
• cerebral edema (including on the background of a brain tumor or associated with surgical intervention, radiation therapy or head trauma) after a previous parenteral application of GCS;
• allergic eye diseases - allergic forms of conjunctivitis;
• inflammatory diseases of the eyes - sympathetic ophthalmia, severe sluggish anterior and posterior uveitis, optic neuritis;
• primary or secondary adrenal insufficiency (including the condition after removal of the adrenal glands);
• congenital adrenal hyperplasia;
• kidney disease of autoimmune genesis (including acute glomerulonephritis);
• nephrotic syndrome;
• subacute thyroiditis;
• blood diseases and hematopoiesis system - agranulocytosis, panmyelopathy, autoimmune hemolytic anemia, lympho- and myeloid leukemia, lymphogranulomatosis, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocyte anemia), congenital (erythroid) hypoplastic anemia;
• interstitial lung diseases - acute alveolitis, pulmonary fibrosis, stage II-III sarcoidosis;
• tuberculosis meningitis, pulmonary tuberculosis, aspiration pneumonia (in combination with specific chemotherapy);
• berylliosis, Leffler's syndrome (not amenable to other therapy);
• lung cancer (in combination with cytostatics);
• multiple sclerosis;
• ulcerative colitis, Crohn's disease, local enteritis;
• hepatitis;
• hypoglycemic conditions;
• prevention of graft rejection during organ transplantation;
• hypercalcemia on the background of cancer, nausea and vomiting during cytostatic therapy;
• myeloma disease.

Parenteral (emergency therapy for conditions requiring rapid increase in the concentration of GCS in the body):

• shock conditions (burn, traumatic, operational, toxic, cardiogenic) with ineffectiveness of vasoconstrictors, plasma-substituting drugs and other symptomatic therapy;
• allergic reaction (acute severe), transfusion shock, anaphylactic shock, anaphylactoid reactions;
• edema of the brain (including against a background of a brain tumor or associated with a surgical intervention,radiation therapy or head trauma);
• bronchial asthma (severe form), asthmatic status;
• SLE, rheumatoid arthritis;
• acute adrenal insufficiency;
• thyrotoxic crisis;
• acute hepatitis, hepatic coma;
• Reduction of inflammatory phenomena and prevention of cicatricial narrowing (with poisoning by cauterizing fluids).

Forms of release

Tablets 4 mg.

Lyophilizate for the preparation of solution for intravenous and intramuscular injection (injections in ampoules for injection) 250 mg.

Instructions for use and dosage

The dose of the drug and the duration of treatment is determined by the doctor individually, depending on the indications and severity of the disease.

Pills

The whole daily dose of the drug is recommended to take either a single or double daily dose - every other day, taking into account the circadian rhythm of endogenous secretion of GCS in the interval from 6 to 8 am. A high daily dose can be divided into 2-4 doses, with a large dose taken in the morning. Tablets should be taken during or immediately after meals, with a small amount of liquid.

The initial dose of the drug can be from 4 mg to 48 mg of methylprednisolone per day, depending on the nature of the disease.With less severe diseases, it is usually sufficient to use lower doses, although higher doses may be required for individual patients. High doses may be required for such diseases and conditions as multiple sclerosis (200 mg per day), cerebral edema (200-1000 mg per day) and organ transplantation (up to 7 mg / kg per day). If a satisfactory clinical effect is not obtained after a sufficient period of time, the drug should be withdrawn and another type of therapy administered to the patient.

To 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 / m 2 per day in 3 divided doses.

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

Lyophilizate for the preparation of solution for intravenous and intramuscular administration

Parenteral drug is administered in the form of slow IV injections or IV infusions, as well as IM injections.

The injection solution is prepared by adding the solvent to the lyophilisate vial immediately before use.The prepared solution contains 62.5 mg / ml methylprednisolone.

As additional therapy for life-threatening conditions, 30 mg / kg body weight IV is administered for at least 30 minutes. The administration of this dose can be repeated every 4-6 hours for no more than 48 hours.

Pulse therapy in the treatment of diseases in which GCS-therapy is effective, with exacerbations of diseases and / or with ineffectiveness of standard therapy.

To improve the quality of life for cancer, at the terminal stage, 125 mg per day IV is administered daily for up to 8 weeks.

In chemotherapy, characterized by a slight or moderate vomiting effect, 250 mg IV for at least 5 minutes for 1 hour before the introduction of the chemotherapeutic drug, at the beginning of chemotherapy, and after its termination. In chemotherapy characterized by severe emetic action, 250 mg IV is administered for at least 5 minutes in combination with appropriate doses of Metoclopramide or butyrofenone 1 hour prior to the administration of the chemotherapy drug, then 250 mg IV at the beginning of chemotherapy and after it .

With other indications, the initial dose is 10-500 mg IV depending on the nature of the disease. For a short course in severe acute conditions, higher doses may be required.The initial dose, not exceeding 250 mg, should be administered IV for at least 5 minutes, doses above 250 mg administered for at least 30 minutes. Subsequent doses are administered intravenously or intramuscularly, and the duration of the intervals between administrations depends on the patient's response to therapy and on his clinical condition.

Children should be given lower doses (but not less than 0.5 mg / kg per day), but when choosing a dose, first of all, the severity of the condition and the patient's reaction to therapy, rather than age and body weight, are taken into account.

Side effect

• decreased glucose tolerance;
• steroid diabetes mellitus;
• manifestation of latent diabetes mellitus;
• oppression of adrenal function;
• Isenko-Cushing syndrome (lunar face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae);
• nausea, vomiting;
• steroid ulcer of the stomach and duodenum;
• erosive esophagitis;
• gastrointestinal bleeding;
• perforation of the gastrointestinal wall;
• a violation of appetite;
• flatulence;
• hiccough;
• arrhythmias;
• bradycardia (up to cardiac arrest);
• in predisposed patients, the development or intensification of heart failure;
• increased blood pressure;
• thromboses;
• euphoria;
• hallucinations;
• affective insanity;
• depression;
• paranoia;
• increased intracranial pressure;
• nervousness;
• anxiety;
• insomnia;
• dizziness;
• headache;
• convulsions;
• increased intraocular pressure with possible damage to the optic nerve;
• propensity to develop secondary bacterial, fungal or viral infections of the eyes;
• sudden loss of vision (with parenteral administration in the area of ​​the head, neck, nasal concha, scalp may deposition of drug crystals in the vessels of the eye);
• weight gain;
• increased sweating;
• slowing growth and ossification processes in children (premature closure of epiphyseal growth zones);
• osteoporosis (very rare - pathological bone fractures, aseptic necrosis of the head of the humerus and femur);
• rupture of muscle tendons;
• decrease in muscle mass (atrophy);
• thinning of the skin;
• hyper or hypopigmentation;
• steroid acne;
• stria;
• propensity to develop pyoderma and candidiasis;
• skin rash;
• itching;
• anaphylactic shock;
• local allergic reactions;
• burning, numbness, pain, tingling at the injection site;
• infection of the injection site;
• development or exacerbation of infections (the emergence of this side effect is facilitated by jointly used immunosuppressants and vaccination);
• "tides" of blood to the head.

Contraindications

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

Children in the period of growth of glucocorticosteroids (GCS) should be used only in absolute indications and with careful observation of the doctor.

With caution should prescribe the drug in the following diseases and conditions:

• Gastrointestinal diseases - peptic ulcer of stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, NJA with perforation or abscessing, diverticulitis;
• parasitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently transferred, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles, amebiasis, strongyloidiasis, systemic mycosis; active and latent tuberculosis (use in severe infectious diseases is permissible only on the background of specific therapy);
• pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination, immunodeficiency (including AIDS or HIV infection);
• diseases of the cardiovascular system (including the recently transferred myocardial infarction - in patients with acute and subacute myocardial infarction it is possible to spread the focus of necrosis, slow the formation of scar tissue and, as a result, break the heart muscle), severe chronic heart failure, arterial hypertension, hyperlipidemia;
• endocrine diseases - diabetes mellitus (including a violation of carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itenko-Kyushing's disease, obesity (3-4 degrees);
• severe chronic renal and / or hepatic insufficiency, nephrourolythiasis;
• hypoalbuminemia and conditions predisposing to its occurrence;
• systemic osteoporosis, myasthenia gravis, acute psychosis, poliomyelitis (except for the form of bulbar encephalitis), open and closed angle glaucoma;
• pregnancy.

Application in pregnancy and lactation

In pregnancy (especially in the first trimester), the drug should be used only for life indications.

As glucocorticosteroids penetrate into breast milk, if it is necessary to use the drug during lactation (breastfeeding), it is recommended to stop breastfeeding.

Use in children

Children in the period of growth of glucocorticosteroids (GCS) should be used only in absolute indications and with careful observation of the doctor.

Children during long-term treatment by Metipred need careful monitoring of the dynamics of growth and development.

special instructions

Store the prepared solution for parenteral administration at a temperature of 15 to 20 degrees Celsius and use for 12 hours.

During treatment with Metipred (especially long-term) it is necessary to observe the oculist, monitor blood pressure, the state of water-electrolyte balance, as well as patterns of peripheral blood and glucose concentration in the blood.

In order to reduce side effects, it is possible to prescribe antacids, and also to increase the intake of potassium in the body (diet, potassium preparations). Food should be rich in proteins, vitamins, with a restriction of fat, carbohydrates and table salt.

The effect of the drug is enhanced in patients with hypothyroidism and liver cirrhosis.The drug may enhance existing emotional instability or psychotic disorders. When referring to a psychosis in an anamnesis, Metipred in high doses is prescribed under the strict supervision of a doctor.

With caution should be used in acute and subacute myocardial infarction in connection with 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 (including surgical operations, trauma, infectious diseases), a correction of the dose of the drug should be made in connection with an increase in the need for glucocorticosteroids (GCS).

In case of sudden cancellation, especially in case of prior application of high doses, it is possible to develop withdrawal syndrome (anorexia, nausea, inhibition, generalized musculoskeletal pain, general weakness), as well as aggravation of the disease for which Metipred was appointed.

During treatment, Metipred should not be vaccinated due to a decrease in the immune response and, as a result, a decrease in the effectiveness of the vaccine.

Assigning Metipred with intercurrent infections, septic states and tuberculosis, it is necessary to simultaneously perform antibiotic treatment of bactericidal action.

Children during long-term treatment by Metipred need careful monitoring of the dynamics of growth and development. Children who were in contact with sick measles or chickenpox during the treatment period prophylactically prescribe specific immunoglobulins.

Due to the weak mineralocorticoid effect for replacement therapy with adrenal insufficiency, Metipred is used in combination with mineralocorticoids.

Patients with diabetes should monitor the concentration of glucose in the blood and, if necessary, adjust the dose of hypoglycemic agents.

An x-ray control of the osteoarticular system (images of the spine, hands) is shown.

Metipred in patients with latent infectious diseases of the kidneys and urinary tract can cause leukocyturia, which can be of diagnostic significance.

Drug Interactions

The simultaneous appointment of Metipred:

• with inducers of hepatic microsomal enzymes (phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration (increase in metabolic rate);
• with diuretics (especially thiazide-like and carbonic anhydrase inhibitors) and amphotericin B leads to increased excretion of potassium from the body and an increased risk of developing heart failure; inhibitors of carbonic anhydrase and "loop" diuretics may increase the risk of osteoporosis;
• with sodium-containing drugs promotes the development of edema and increased blood pressure;
• with cardiac glycosides leads to a deterioration in their tolerability and an increased likelihood of developing ventricular extrasystole (due to induced hypokalemia);
• with indirect anticoagulants contributes to weakening (less intensification) of their action (dose adjustment is required);
• with anticoagulants and thrombolytics leads to an increased risk of bleeding from ulcers in the gastrointestinal tract;
• with ethanol (alcohol) and non-steroidal anti-inflammatory drugs (NSAIDs) contributes to increased risk of erosive and ulcerative lesions in the gastrointestinal tract and development of bleeding (in combination with NSAIDs in the treatment of arthritis, there may be a reduction in the dose of GCS due to the summation of the therapeutic effect);
• with indomethacin increases the risk of side effects of methylprednisolone (displacement of indomethacin methylprednisolone from bonding with albumins);
• with paracetamol increases the risk of hepatotoxicity (induction of hepatic enzymes and the formation of a toxic metabolite of paracetamol);
• with acetylsalicylic acid accelerates its excretion and reduces the concentration in the blood (when methylprednisolone is canceled, the level of salicylates in the blood increases and the risk of side effects increases);
• with insulin and oral hypoglycemic drugs, hypotensive drugs reduce their effectiveness;
• with vitamin D, its effect on calcium absorption in the intestine is reduced;
• with STH, the effectiveness of the latter decreases;
• with praziquantel reduces the concentration of the latter;
• with m-holinoblokatorami (including antihistamines and tricyclic antidepressants) and nitrates helps increase intraocular pressure;
• with isoniazid and mexiletine increases their metabolism (especially in "slow" acetylators), which leads to a decrease in their plasma concentrations.

Ergocalciferol and parathyroid hormone interfere with the development of osteopathy caused by methylprednisolone.

Cyclosporine and ketoconazole, while slowing the metabolism of methylprednisolone, may in some cases increase its toxicity.

Simultaneous with the appointment of androgens and anabolic steroid drugs with metipred contributes to the development of peripheral edema, hirsutism and acne.

Estrogens and estrogen-containing oral contraceptives reduce the clearance of methylprednisolone, which may be accompanied by increased severity of his actions.

Mitotane and other inhibitors of adrenal cortex function may necessitate an increase in the dose of Metipred.

With simultaneous use with live antiviral vaccines and against other types of immunization increases the risk of virus activation and the development of infections.

Immunosuppressants increase the risk of infection and lymphoma or other lymphoproliferative disorders associated with the Epstein-Barr virus.

Antipsychotic drugs (antipsychotics) and azathioprine increase the risk of developing cataracts when prescribing methylprednisolone.

Simultaneous administration of antacids reduces the absorption of Metipred.

While the use of antithyroid drugs decreases, and a thyroid hormone - increased clearance of methylprednisolone.

Pharmaceutical interaction

Pharmaceutical incompatibility of Metipred with other intravenously administered drugs is possible.It is recommended to inject it separately from other drugs (iv bolus, or through another dropper, as a second solution).

Analogues of the drug Metizred

Structural analogs for the active substance:

• Depot Medrol;
• Lemodus;
• Medrol;
• Solu Medrol;
• Urbazon.

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