Active substanceMethylprednisoloneMethylprednisolone
Similar drugsTo uncover
  • Depo-Medrol®
    suspension for injections 
  • And
    lyophilizatesolution w / m in / in 
  • Lemodus
    lyophilizate w / m in / in 
    Hemofarm AD     Serbia
  • Lemodus
    pills inwards 
    Hemofarm AD     Serbia
  • Medrol®
    pills inwards 
  • Methylprednisolone-native
    pills inwards 
    NATIVA, LLC     Russia
  • Meti
    lyophilizate w / m in / in 
    Orion Corporation     Finland
  • Meti
    pills inwards 
    Orion Corporation     Finland
  • Metipred® Orion
    lyophilizate w / m in / in 
    Orion Corporation     Finland
  • Solu-Medrol®
    lyophilizate w / m in / in 
  • Dosage form: & nbsplyophilizate for the preparation of solution for intravenous and intramuscular administration
    Composition:

    1 bottle contains:

    active substance: methylprednisolone sodium succinate in recalculation for methylprednisolone - 250 mg;

    Excipients: sodium hydroxide 12.5 mg.

    Solvent - water for injection 4 ml.

    Description:

    Lyophilized powder of white or slightly yellowish color, hygroscopic.

    Solvent (water for injections) is a clear, colorless liquid.

    Pharmacotherapeutic group:Glucocorticosteroid
    ATX: & nbsp

    H.02.A.B.04   Methylprednisolone

    Pharmacodynamics:

    Methylprednisolone is a synthetic glucocorticosteroid drug. Has anti-inflammatory, antiallergic, immunosuppressive action, increases the sensitivity of beta-adrenoreceptors to endogenous catecholamines.

    Interacts with specific cytoplasmic receptors (receptors for glucocorticosteroids (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.)

    Protein metabolism: reduces the number of globulins in the 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.

    Lipid metabolism: increases synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat occurs mainly in the area of ​​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 (an increase in the intake of glucose fromliver into the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); promotes the development of hyperglycemia.

    Water-electrolytic exchange: retards 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 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 the permeability of capillaries; stabilization of cell membranes (especially lysosomal) and membranes of organelles. Acts on all phases of the inflammatory process: inhibits prostaglandin synthesis for arachidonic acid level (Lipokortin inhibits phospholipase A2 suppresses liberatiou arachidonic acid inhibits the biosynthesis endoperekisey, leukotrienes contribute inflammation, allergies, etc.), Synthesis of "proinflammatory cytokine" (interleukin 1, tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors.

    Immunodepressive effect is caused by induced lymphoid tissue involution, suppression of lymphocyte proliferation (especially T-lymphocytes), suppression of B-cell migration and T-B-lymphocyte interaction, 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 the development of lymphoid and connective tissue, reducing the sensitivity of effector cells to mediators of allergy, inhibition of antibody formation, changes in the immune response of the body.

    In obstructive airway diseases, the effect is mainly due to inhibition of inflammatory processes, prevention or reduction of mucosal edema, a decrease in the eosinophilic infiltration of the submucosal layer of the 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 adrenocorticotropic hormone (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.

    Pharmacokinetics:

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

    Time to reach the maximum concentration in blood plasma (Cmax) with intramuscular injection - 0.5-1 hour. FROMmafter intravenous administration at a dose of 30 mg / kg for 20 minutes, or intravenous drip in a dose of 1 g for 30-60 minutes, reaches 20 μg / ml. After intramuscular administration of 40 mg after about 2 hours, C max is achieved, which is 34 μg / ml.

    The connection with plasma proteins is 62% regardless of the dose administered (only binds to albumin).

    The half-life of plasma from parenteral administration is 2.3-4 hours and probably does not depend on the route of administration.Due to intracellular activity, there is a pronounced difference between the half-life of methylprednisolone from the blood plasma and the half-life from the body as a whole (approximately 12 to 36 hours).

    Pharmacotherapeutic action is maintained even when the level of the drug in the blood is no longer determined.

    Metabolized mainly in the liver, metabolites (11-keto and 20-hydroxy compounds) do not have SCS activity and are excreted mainly by the kidneys (about 85% of the administered dose is detected within 24 hours in urine, and about 10% in feces). Penetrates through the blood-brain barrier and placental barrier. Metabolites are found in breast milk.

    Indications:

    Emergency therapy for conditions requiring a rapid increase in glucocorticosteroid concentrations in the body:

    - Shock conditions (burn, traumatic, operational, toxic, cardiogenic) - with ineffectiveness of vasoconstrictors, plasma-substituting drugs and other symptomatic therapy.

    - Allergic reactions (acute severe forms), hemotransfusion shock, anaphylactic shock, anaphylactoid reactions.

    - Edema of the brain (incl.on a background of a brain tumor or associated with surgical intervention, radiation therapy).

    - Bronchial asthma (severe form), asthmatic status.

    - Systemic diseases of connective tissue (systemic lupus erythematosus, rheumatoid arthritis).

    - Acute adrenal insufficiency.

    - Thyrotoxic crisis.

    - Acute hepatitis, hepatic coma.

    - Reduction of inflammatory phenomena and prevention of cicatricial narrowing (when poisoning with cauterizing fluids).

    - Exacerbation of multiple sclerosis.

    Contraindications:

    - The introduction of the drug intrathecally.

    - Systemic mycosis.

    - Simultaneous use of live and diluted vaccines with immunosuppressive doses of the drug.

    - Breastfeeding period.

    - Hypersensitivity to peanuts or soy. A small amount of soybean oil can theoretically be extracted from the rubber of the bottle, in connection with which the drug is contraindicated in patients with an allergy to peanuts or soy.

    - Idiopathic thrombocytopenic purpura (with intramuscular injection).

    - Epidural introduction methylprednisolone.

    - Edema of the brain of traumatic genesis (due to craniocerebral injury).

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

    In children during growth, the drug Metipred should be used only under absolute indications and under the special supervision of the attending physician.

    The use of Metipred is not recommended in patients with acute and subacute myocardial infarction.

    Carefully:

    - Зabolevaniya gastrointestinal tract - gastric ulcer and duodenal ulcers, esophagitis, gastritis, acute or latent peptic ulcer, recently established intestinal anastomosis, ulcerative colitis, with the threat of perforation or abscess, 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; active or latent tuberculosis. The use in severe infectious diseases is permissible 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 (including the recently transferred myocardial infarction), severe chronic heart failure, hypertension, hyperlipidemia;

    - endocrine diseases - diabetes (including a violation of carbohydrate tolerance), thyrotoxicosis, hypothyroidism, obesity (III-IV item);

    - severe chronic renal and / or liver failure, nefroourolithiasis;

    - hypoalbuminemia and conditions predisposing to its occurrence;

    - systemic osteoporosis, myasthenia gravis gravis, acute psychosis, poliomyelitis (for exclusion of the form of bulbar encephalitis), open and closed angle glaucoma;

    - pregnancy;

    - secondary adrenal failure;

    - convulsive syndrome.

    It is not recommended to use the drug in patients with Isenko-Cushing's disease; in patients with acute and subacute myocardial infarction (possibly spreading the focus of necrosis, slowing the formation of scar tissue and, as a consequence, breaking the heart muscle).

    The use of the drug in chronic heart failure is possible only on absolute indications.

    Pregnancy and lactation:In a number of animal studies, when injecting high doses of methylprednisolone, deformities in the fetus were detected. There have been no relevant studies on the effect on reproductive function of humans. Since it is impossible to rule out the possible harm of using methylprednisolone, taking the drug during pregnancy and in women planning pregnancy is only indicated if the expected therapeutic effect of the mother exceeds the risk of adverse effects on the fetus. Methylprednisolone should be administered during pregnancy only by absolute indications. Methylprednisolone penetrates the placenta. There was an increase in the number of newborns with a delay in intrauterine development, born from mothers who received methylprednisolone, cases of cataract in newborns were also noted. The effect of methylprednisolone on the course and outcome of labor is unknown. Newborns born to mothers who received methylprednisolone during pregnancy, should be carefully screened to identify possible symptoms of adrenal insufficiency.

    Because the methylprednisolone penetrates into breast milk, if it is necessary to use the drug during breastfeeding, breastfeeding should be discontinued.

    Dosing and Administration:

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

    The drug is administered in the form of slow intravenous jet injections or intravenous infusions, as well as intramuscular injections.

    Preparation of the solution. 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 an additional therapy in 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 the disease and / or when standard therapy is ineffective.

    Recommended therapy regimens:

    Rheumatic diseases:

    1 g / day IV for 1-4 days or 1 g / month IV in

    within 6 months

    Systemic lupus erythematosus:

    1 g / day iv in 3 days

    Multiple sclerosis:

    1 g / day IV for 3 or 5 days

    Edematous conditions, for example,

    30 mg / kg IV every other day for 4 days or 1 g / day

    glomerulonephritis, lupus

    IV for 3, 5 or 7 days

    nephritis:

    The above doses should be administered for at least 30 minutes;

    repeat if no improvement has been achieved within a week after the treatment, or if the patient's condition requires it.

    Oncological diseases in the terminal stage - to improve the quality of life: Enter 125 mg / day intravenously daily for up to 8 weeks.

    Prevention of nausea and vomiting associated with chemotherapy for cancer. In chemotherapy characterized by slight or mild vomiting, 250 mg IV is administered for at least 5 minutes 1 hour prior to administration of the chemotherapeutic drug, at the beginning of chemotherapy, and after its termination. In chemotherapy characterized by pronounced emetic action, 250 mg IV is administered for at least 5 minutes in combination with appropriate doses metoclopramide or butirofenone 1 hour prior to the administration of the chemotherapeutic drug, then 250 mg IV at the beginning of chemotherapy and after its completion.

    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 iv or I / m, and the duration of the intervals between administrations depends on the patient's response to therapy and on his clinical condition.

    Side effects:

    Frequency of development and severity side effects depends on duration of application, magnitude the dose used and the possibility of observing the circadian rhythm of prescribing Metipred.

    When applying the drug Metizred can be noted:

    Disorders from the endocrine system: decrease in glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, Itenko-Cushing syndrome (lunar face, pituitary-type obesity, hirsutism,increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae), delayed sexual development in children, inhibition of the synthesis of its own ACTH and cortisol (with prolonged use), pituitary function deficiency, withdrawal syndrome.

    Disorders from the gastrointestinal tract: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding and perforation of the wall of the stomach and intestines, digestive disorders, flatulence, peritonitis, abdominal pain, diarrhea, arrhythmias; development (in predisposed patients) or increased symptoms of chronic heart failure, changes in the electrocardiogram, characteristic of hypokalemia, hypertrophic cardiomyopathy in premature newborns, pulmonary edema. In patients with acute and subacute myocardial infarction - the spread of the focus of necrosis, slowing the formation of scar tissue, which can lead to a rupture heart muscle.

    Vascular disorders: increased blood pressure, lowering blood pressure, hypercoagulation, thrombosis, atherosclerosis, vasculitis, fainting, thromboembolism, thrombophlebitis.

    Violations from the nervous systems: increased intracranial pressure, papillohedral(edema of the optic disc), cramps, headache, dizziness, epidural lipomatosis, paresthesia, neuritis,Neuropathy, Vertigo.

    Disorders of the psyche: Depressed mood, euphoria, mood changes, psychological dependence, suicidal thoughts, psychotic disorders (including mania, delusions, hallucinations, schizophrenia or exacerbation), confusion, nervousness or anxiety, personality changes, pathological behavior, insomnia, delirium, disorientation, manic-depressive psychosis, depression, paranoia, anxiety. In children, most often there are mood changes, behavioral disorders, insomnia, irritability, amnesia, cognitive impairment.

    Disturbances on the part of the organ of sight: 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 (when administered parenterally in the head, neck, nasal turbinate, the scalp may be deposited drug crystals in the blood vessels of the eye), central serous chorioretinopathy, corneal perforation during ocular herpes simplex localization.

    Disorders from the metabolism and nutrition: hypercalciuria, hypocalcemia, increase of body weight, negative nitrogen balance (increased protein breakdown), increased sweating, hypokalemic alkalosis, dyslipidemia, metabolic acidosis, increasing concentrations of urea in the blood, lipomatosis, increasing the need for insulin or oral hypoglycemic agents in patients with diabetes.

    Violations, conditional mineralocorticosteroid activity: sodium and fluid retention (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

    Disorders from the kidneys and urinary tract: the probability of formation of urinary stones and a slight increase in the number of leukocytes and erythrocytes in the urine without obvious damage to the kidneys.

    Disturbances from the liver and bile ducts: hepatitis, hepatomegaly.

    Disturbances from musculoskeletal and connective tissue: Deceleration of growth and ossification processes in children (premature closure epiphyseal growth zones), osteoporosis (very rarely pathological bone fractures, aseptic necrosis of the head of the humerus and femur), bone necrosis, muscle tendon rupture, compression fracture of the spine, steroid myopathy, muscle loss (atrophy), Charcot's disease, arthralgia , myalgia. Disturbances from the skin and subcutaneous tissues: slow healing of wounds, petechiae, ecchymosis, hyper- or hypopigmentation, "steroid" acne, striae, propensity to develop pyoderma and candidiasis, purpura, atrophic skin changes, steroid panniculitis, hematoma, hypertrichosis in women, redness, hives, allergic dermatitis, thinning of hair on the head, "sterile" abscesses, angioedema. Allergic reactions: skin rash, itching, anaphylactic shock, local allergic reactions.

    Violations of the blood and lymphatic system: an increase in the total number of leukocytes, a decrease in the total number of eosinophilic leukocytes, monocytes and lymphocytes, a decrease in the mass of lymphoid tissue.

    Immune system disorders: reactions increased sensitivity to the drug.

    Violations of the genitals and dairy glands: irregular menstruation, increase or decrease in motility of spermatozoa.

    Systemic disorders: insufficiency of adrenal function in long-term treatment.

    Other: development or exacerbation of infections (the occurrence of this side effect is facilitated by co-vaccination), "flushes" of blood to the head, hiccups, increased or decreased appetite.

    Infectious and parasitic diseases: infection, opportunistic infections. Benign, malignant and unspecified neoplasms (including cysts and polyps): corticosteroid-induced tumor lysis syndrome. Laboratory and instrumental data: a decrease in the concentration of potassium in the blood, an increase in the concentration of alanine aminotransferase (ALT), aspartate aminotransferase (ACT), and alkaline phosphatase in the blood; Suppression of skin test reactions.General disorders and disorders at the site of administration: burning, numbness, pain, tingling at the injection site, infections at the injection site, rarely - necrosis of surrounding tissues, scar formation at the injection site; atrophy of the skin and subcutaneous tissue with intramuscular injection (especially dangerous is the introduction to the deltoid muscle).

    In the case of intrathecal or epidural administration of the drug: arachnoiditis, meningitis, paresis / paraplegia, sensory disorders and disorders of the gastrointestinal tract and bladder.

    Overdose:Acute intoxication methylprednisolone is unlikely. With chronic overdose methylprednisolone may symptoms of the syndrome Itenko-Cushing. After chronic overdose due to possible insufficiency of function adrenal glands, should gradually reduce the dose of the drug. There are no specific antidotes of methylprednisolone. Treatment is symptomatic. Methylprednisolone is displayed during dialysis.
    Interaction:

    The compatibility and stability of methylprednisolone solutions with IV administration with other drugs included in the mixtures for IV administration depend on pH, concentration, time, temperature, and also on the solubility of methylprednisolone itself. Methylprednisolone it is recommended, if possible, to be administered separately from other drugs, in the form of intravenous bolus injections, intravenous drip infusion, or via an additional dropper as a second solution.

    Inhibitor inhibitors CYP3A4 - can suppress the metabolism of methylprednisolone, reduce its clearance and increase the concentration in the blood plasma. In this case, in order to avoid overdose phenomena, a dose of methylprednisolone should be titrated.

    Inductors of isoenzyme CYP3A4 - can increase the clearance of methylprednisolone. This is manifested by a decrease in the concentration of methylprednisolone in the blood plasma, which may require increasing the dose of the drug to obtain the desired effect.

    Substrates of the isoenzyme CYP3A4 - in the presence of another isoenzyme substrate CYP3A4 the clearance of methylprednisolone may be delayed or induced, which may require appropriate dose adjustment of methylprednisolone. There is a chance that adverse reactions, manifested when using drugs in the form of monotherapy, can occur more often with the simultaneous use of drugs.

    The following examples of drug interactions may have important clinical implications.

    Class or type of medicinal product

    - drug or substance

    Interaction / effect

    Antibacterial drugs - isoniazid

    Inhibitor of isoenzyme CYP3A4. In addition, there is a probability of methylprednisolone influence on the degree of acetylation and clearance of isoniazid.

    Antibiotic, anti-tuberculosis - rifampicin

    Inductor of isoenzyme CYP3A4.

    Anticoagulants (for oral administration)

    Methylprednisolop has a variety of effects on the effect of indirect anticoagulants. Both enhancement and reduction of the effect of anticoagulants taken simultaneously with methylprednisolone are reported. To maintain the necessary effect of the anticoagulant, constant monitoring of the coagulogram is necessary.

    Antiepileptic drugs - carbamazepine

    Inductor and substrate of the isoenzyme CYP3A4.

    Antiepileptic drugs

    - phenobarbital

    - phenytoin

    Inductors of isoenzyme CYP3A4.

    Anticholinergic drugs

    - neuromuscular blockers

    Methylprednisolone may affect anticholinergic drugs.

    1. Cases of acute myopathy have been reported with simultaneous use of high doses of methylprednicholone and anticholinergic drugs, such as neuromuscular blockers.

    2. Antagonism of the effect of blockade of pancuronium with simultaneous use of methylprednicholone . This effect can be expected with any neuromuscular blocking

    Anticholinesterase inhibitors

    GCS can reduce the effect of inhibitors of anticholinesterase in patients with myasthenia gravis.

    Hypoglycemic drugs

    Since the drug methylprednisolone can increase the concentration of glucose in the blood plasma, should adjust the dose of hypoglycemic drugs.

    Antiemetic drugs

    - aprepitant

    - fosaprepitant

    Inhibitors and substrates of the isoenzyme CYP3A4.

    Antifungal drugs

    - itraconazole

    - ketoconazole

    Inhibitors and substrates of the isoenzyme CYP3A4.

    Antiviral drugs

    - HIV protease inhibitors

    Inhibitors and substrates of the isoenzyme CYP3A4. HIV protease inhibitors, as indinavir and ritonavir, can increase the concentration of methylprednisolone in the blood plasma.

    Aromatase inhibitors

    - aminoglutethimide

    Suppression of the adrenal function induced by aminoglutethimide can inhibit the endocrine changes caused by prolonged therapy with methylprednicholone.

    Calcium channel blockers

    - diltiazem

    Inhibitors and substrates of the isoenzyme CYP3A4.

    Oral contraceptive drugs

    - ethinyl estradiol / noregandron

    Inhibitors and substrates of the isoenzyme CYP3A4.

    Grapefruit juice

    Inhibitor of isoenzyme CYP3A4.

    Immunosuppressive drugs

    - cyclosporine

    Inhibitors and substrates of the isoenzyme CYP3A4.

    1. The simultaneous use of methylprednisolone and cyclosporine causes mutual inhibition of metabolism, which can lead to an increase in the concentration in the blood plasma of one or both drugs. Therefore, it is likely that the side effects associated with the use of each of these drugs as monotherapy, with their joint application may occur more often.

    2. When joint use of these drugs, cases of seizures were noted.

    Immunosuppressive drugs

    - cyclophosphamide

    - tacrolimus

    Substrates of the isoenzyme CYP3A4.

    Antibiotics-macrolides

    - clarithromycin

    - erythromycin

    Inhibitors and substrates of the isoenzyme CYP3A4.

    Non-steroidal

    anti-inflammatory drugs (NSAIDs)

    - high doses of aspirin (acetylsalicylic acid)

    1. Probably increased incidence of gastrointestinal bleeding and ulceration with simultaneous use of methylprednisolone and NSAIDs.

    2. Methylprednisolone can increase the clearance of acetylsalicylic acid, taken in high doses, for a long period, which can lead to a decrease in the level of salicylates in the serum or increase the risk of salicylate toxicity when methylprednisolone is withdrawn. Caution is advised to prescribe acetylsalicylic acid in combination with Pmethylprednisolone.

    Drugs that reduce the concentration of potassium in the blood plasma

    With the simultaneous use of methylprednisolone and drugs that reduce the concentration of potassium in the blood plasma (eg, diuretics, amphotericin B), patients should be carefully monitored for the development of hypokalemia. It should also be taken into account that there is an increased risk of hypokalemia with simultaneous use of methylprednisolone and xanthine or beta2-agonists.

    Incompatibility

    The following drugs are not compatible with methylprednisolone in solution: allopurinol sodium, doxapram hydrochloride, tigecycline, diltiazema hydrochloride, calcium gluconate, vecuronium bromide, rocuronium bromide, cisatracurium besylate, glycopyrrolate, propofol.

    Special instructions:

    Because complications of therapy with Metizred depends on dose and duration values treatment, then in each specific case based on analysis risk / benefit ratios decision on the need for such treatment, as well as determine duration of treatment and frequency of administration.

    In order to better control the patient's condition, the lowest dose of Metipred should be used. When the effect is achieved, if possible, gradually reduce the dose to a maintenance dose or discontinue treatment.

    In view of the risk of arrhythmia, the use of Metipred in high doses should be carried out in a hospital equipped with the necessary equipment (electrocardiograph, defibrillator).

    If long-term spontaneous remission occurs, treatment should be discontinued.

    With prolonged treatment, the patient should go through regular examination (radiography of thoracic organs cells, concentration glucose in blood plasma after 2 hours after eating, general urine analysis, blood pressure, body weight control, it is desirable to conduct a radiographic or endoscopic examination with presence in the anamnesis of ulcerative diseases of the gastrointestinal tract).

    It is necessary to carefully monitor the growth and development of children who are on long-term therapy with Metipred. Growth retardation can be observed in children receiving a long daily divided into several doses of therapy. Daily use of methylprednisolone for a long time in children is possible only on absolute indications. The use of the drug every other day may reduce the risk of developing this side effect or avoid it altogether.

    Children receiving long-term therapy with Metipred are at increased risk for developing intracranial hypertension.

    The drug Metipred should also be administered with great care to patients with confirmed or suspected parasitic infections, such as, strongyloidiasis. Caused methylprednisolone immunosuppression, in such patients leads to strongyloid hyperinfection and dissemination of the process with widespread migration of larvae, often with the development of severe forms of enterocolitis and gram-negative septicemia with possible fatal outcome.Patients receiving drugs that suppress the immune system are more susceptible to infections than healthy individuals. For example, chickenpox and measles can have a more severe course, up to lethal outcome the nonimmunized children or in adults receiving Metipred.

    The efficacy of Metipred in septic shock is questionable. The results of a systematic review of the use of the drug in short courses in high doses do not support the possibility of their use in this mode.

    Patients, which may to be exposed to stress on the background of therapy with Metizred, shows an increase in the dose of the drug before, during and after a stressful situation.

    Due to the fact that it is revealed increased mortality after 2 weeks or 6 months after injury head in patients who received treatment of methylprednisolone sodium succinate, compared with placebo, Metipred should not be used when brain edema caused by head trauma. Causal communication deaths using methylprednisolone sodium succinate not installed. Against the background of drug therapy The meta-map may increase susceptibility to infections, some infections may occur in an erased form, in addition, can develop new infections. Besides addition, the ability organism to localization infectious process. Development infections caused by various pathogenic organisms, such as viruses, bacteria, fungi, protozoa or helminths that are localized in various body systems person, may be due to using Metizred as a as a monotherapy, and in combination with other immunosuppressants, affecting the cellular immunity, humoral immunity or the function of neutrophils. These infections can be mild, however, in some cases, a severe course and even a lethal outcome is possible. Moreover, higher doses of the drug are used, the higher the probability of developing infectious complications.

    Patients receiving treatment with Metiredent in doses that have an immunosuppressive effect are prohibited from administering live or live attenuated vaccines, but it is possible to administer killed or inactivated vaccines, however, the response to the introduction of such vaccines may be reduced or even absent. Patients receiving treatment with Metizred in doses do not providing immunosuppressive action, according to the relevant indications, immunization can be carried out.

    The use of the Metipred preparation with active tuberculosis should be limited to cases of fulminant and disseminated tuberculosis, when Metipred is used for the treatment of the disease in combination with the corresponding antituberculous chemotherapy. If Metizred is prescribed for patients with latent tuberculosis or from positive tuberculin tests, then treatment should be carried out under strict medical supervision, since it is possible to reactivate the disease. During prolonged therapy with the drug, such patients should receive the corresponding preventive treatment. It is reported that patients who received therapy with Metizred, had Kaposi's sarcoma. With the withdrawal of the drug may come a clinical remission. Since in patients receiving parenteral therapy with Metired preparation, in rare cases it is possible to develop skin reactions and anaphylactic / anaphylactoid reactions, before the drug should be administered undertake appropriate preventive measures, especially if a given patient has a history allergic reactions to any medications. In applying metipred drug at therapeutic doses over a long period can develop suppression of the hypothalamic-pituitary-adrenal system (secondary failure bark adrenal glands). Power and duration of insufficiency of adrenal cortex are individual for each patient and depend on dose, frequency of application, time of admission and duration therapy.

    The severity of this effect can be reduced by using the drug every other day or by gradually reducing the dose. This type of relative insufficiency of the adrenal cortex can continue for several months after the end of treatment, therefore, under any stressful situations during this period, Metizred should again be prescribed. Since the secretion of mineralocorticosteroids may be impaired, concomitant the appointment of electrolytes and / or mineralocorticosteroids.Development of acute adrenal insufficiency, leading to lethal outcome, possibly with a sharp cancellation of the drug Metired. The withdrawal syndrome, apparently not related to adrenal insufficiency, can also arise due to the sharp cancellation of the drug Metired. This syndrome includes such symptoms like anorexia, nausea, vomiting, lethargy, headache, fever, joint pain, skin peeling, myalgia, weight loss and lowering of arterial pressure.

    It is assumed that these effects arise in connection with a sharp fluctuation concentrations methylprednisolone in the blood plasma, and not because of a decrease in the concentration of methylprednisolone in the blood plasma.

    In patients with hypothyroidism or cirrhosis of the liver, the effect of Metipred is noted. The use of Metizred can lead to an increase in the concentration of glucose in the blood plasma, worsening of the current diabetes mellitus. Patients receiving long-term therapy with Metizod be predisposed to the development of diabetes.

    On the background of therapy drug Meti perhaps development various mental disorders: from euphoria, insomnia, instability mood, changes in personality and severe depression to acute psychotic manifestations. In addition, they may intensify already the available emotional instability or propensity to psychotic reactions.

    Potentially heavy mental disorders can occur when applying preparation Metizred.

    Symptoms usually appear within a few days or weeks after the start of therapy. Most reactions disappear either after a dose reduction or after the drug is discontinued. Despite this, specific treatment may be required.

    Patients and / or their relatives should be warned that if changes at the psychological status of the patient (especially with the development of a depressive state and suicidal attempts)is necessary turn to behind medical care. Also, patients or their relatives should be warned about the possibility of developing mental disorders during or immediately after lowering the dose of the drug or completely canceling it. Prolonged use of Metizred can lead to the emergence of rear subcapsular cataract and nuclear cataract (especially in children),exophthalmos or glaucoma with possible damage to the optic nerve and provoke the attachment of a secondary ophthalmic fungal or viral infection.

    With the use of Metipred, there is an increase in blood pressure, fluid and salt retention in the body, loss of potassium, hypokalemic alkalosis. These effects are less pronounced when using synthetic derivatives, except for cases when they are used in large doses. It may be necessary limitation needs of salt and products containing sodium.

    Therapy with Metizred can mask the symptoms of peptic ulceration and in this case perforation or bleeding can develop without a significant pain syndrome. Such adverse reactions of Metizred from the side of cardiovascular system, as dyslipidemia, rise arterial pressure, can provoke new patients in predisposed patients in case of high doses of Metipred and long-term treatment. In this regard, Metipred should be used with caution in patients with risk factors for cardiovascular disease.Regular monitoring of heart function is necessary. The use of low doses of Metipred every other day can reduce the severity of these side effects.

    Patients, host glucocorticosteroids, caution should be given to analgesics based on acetylsalicylic acid and nonsteroidal anti-inflammatory drugs. Allergic reactions are possible. AT the fact that patients who received glucocorticosteroids rarely noticed such phenomena as skin irritations and anaphylactic or pseudo-anaphylactic reactions, before appointment glucocorticosteroids should be take the necessary measures, especially if the history of the patient has a history of allergic reactions to medications.

    If during the treatment with Meti-preparation the patient developed adrenocortical insufficiency, it should be tried to eliminate by gradually reducing the dosage. This deficiency occurs in parallel with treatment and can last up to several months after its completion. In order to eliminate this effect, patients experiencing stress after completion of treatment are prescribed hormone therapy.In process of deducing mineralocorticosteroids, concomitant treatment in the form of preparations of salt and (or) mineralocorticosteroids is prescribed.

    Glucocorticosteroids from use caution when possible risk of perforation of an ulcer, abscess or any purulent infection if the patient suffers from ulcerative colitis, diverticulitis, open intestinal anastomosis, or an active (or latent) ulcer. High doses of glucocorticosteroids can cause acute pancreatitis. Therapy high doses glucocorticosteroids can cause acute myopathy; The disease is most likely to affect patients from violations neuromuscular transmission (eg, myasthenia gravis), as well as patients receiving concomitant anticholinergic therapy, eg, blockers neuromuscular transfer. Myopathy of this kind is generalized; it can affect the muscles of the eyes or the respiratory system and even lead to paralysis of all limbs. In addition, the level of creatine kinase may increase. In such cases, clinical recovery may take weeks or even years.

    Osteoporosis is often meeting (but rarely detectable) complication of long-term therapy with high doses of glucocorticosteroids.

    Glucocorticosteroids are cautiously prescribed for prolonged therapy in elderly patients because of the increased risk of osteoporosis and fluid retention in the body, potentially causing an increase in blood pressure. Simultaneous treatment methylprednisolone and fluoroquinolones increases the risk of rupture of tendons, especially in elderly patients.

    High doses of glucocorticosteroids can cause pancreatitis in children.

    After rapid intravenous administration large doses Methylprednisolone (more than 500 mg, administered in less than 10 minutes), there were cases of cardiac arrhythmia, vascular insufficiency, and cardiac arrest. During or after the administration of large doses of methylprednisolone sodium succinate, bradycardia may occur; However, there is no evidence that its occurrence is associated with the speed and duration of the infusion.

    Since the intake of glucocorticosteroids can cause or exacerbate the Itenko-Cushing syndrome, patients, suffering from Isenko-Cushing's disease, is necessary to avoid application of glucocorticosteroids. Patients from renal Insufficiency should be prescribed glucocorticosteroids from caution.

    Patients with chronic heart failure system Glucocorticosteroids are administered with extreme caution and only in critical cases.

    Patients with elevated blood pressure, glucocorticosteroids are also administered with caution.

    Against the background of intravenous pulse therapy high doses of methylprednisolone may develop acute hepatitis. With prolonged therapy with high doses perhaps development epidural lipomatosis.

    With the introduction of methylprednisolone intrathecally or epidurally, severe complications can develop.

    In patients with pheochromocytoma, it is possible to develop sympathetic adrenal crises (including fatal outcome).

    Therapy with methylprednisolone may lead to the development of central serous chorioretinopathy, which in turn can lead to detachment of the retina.

    Required use Methylprednisolone with caution in patients with venous thromboembolism or thromboembolic complications at the present time or having a predisposition to their development, t. cases of thrombosis development are possible.

    With the simultaneous use of methylprednisolone with cyclosporine, it is possible to develop a convulsive syndrome.

    Effect on the ability to drive transp. cf. and fur:

    In connection with the possibility of developing dizziness, visual impairment and weakness in the use of Metipred, caution should be exercised by persons driving vehicles or engaged in activities requiring an increased concentration of attention and speed of motor reactions.

    Form release / dosage:Lyophilized powder for the preparation of solution for intramuscular and intravenous administration of 250 mg
    Packaging:

    1. Lyophilized powder for the preparation of a solution for intramuscular and intravenous administration of 250 mg in vials. 1 bottle together with the instruction for use is placed in a cardboard box.

    2 Lyophilized powder for the preparation of solution for intramuscular and intravenous administration of 250 mg in vials complete with a solvent in ampoules of 4 ml.

    1 bottle and 1 ampoule together with instructions for use are placed in a cardboard box.

    Shelf life:5 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N015709 / 02
    Date of registration:20.02.2009 / 18.01.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:Orion CorporationOrion Corporation Finland
    Manufacturer: & nbsp
    Representation: & nbspORION CORPORATION ORION PHARMA ORION CORPORATION ORION PHARMA Finland
    Information update date: & nbsp09.05.2018
    Illustrated instructions
      Instructions
      Up