Description of the drug METHYLPREDNISOLONE-FS


Pharmacological properties of the drug Methylprednisolone

Synthetic corticosteroids are similar in pharmacological properties to hydrocortisone, but are superior in activity. It has a pronounced anti-inflammatory, antiallergic and immunosuppressive effect. Does not have mineralocorticoid activity. Affects carbohydrate, protein, lipid metabolism. Reduces the number of immunocompetent cells at the site of inflammation, reduces vasodilation, stabilizes lysosomal membranes, and reduces the production of prostaglandins and leukotrienes. Has a catabolic effect. Reduces the absorption of glucose by peripheral tissues, which can lead to hyperglycemia and glucosuria, especially in patients predisposed to diabetes. After oral administration, it is well absorbed in the small intestine. Plasma protein binding is 40–90%. The half-life is 2–4 hours. Metabolized in the liver. It is excreted in the urine, mainly in the form of metabolites (glucuronides, sulfates and unconjugated compounds). The half-life is about 3 hours. The drug penetrates the placental barrier and also into breast milk. After intramuscular administration in the form of a depot suspension at a dose of 40 mg, the maximum concentration in the blood plasma is achieved on average after 7.3 hours and averages 1.48 mcg/100 ml. The half-life is 69.3 hours. The duration of suppression of the hypothalamic-pituitary-adrenal system is 4-8 days. After intra-articular injection of 40 mg depot suspension into each knee joint (total dose 80 mg), the maximum plasma concentration is reached after 4-8 hours and is approximately 21.5 mcg/100 ml. The entry of the active substance into the systemic circulation from the joint cavity persists for approximately 7 days.

CHARACTERISTICS OF INDIVIDUAL DRUGS

Depending on their structure, glucocorticoids differ in duration of action, severity of anti-inflammatory, mineralocorticoid, metabolic and immunosuppressive activity (Table 5). Moreover, there is no direct correlation between their immunosuppressive and anti-inflammatory effects. For example, dexamethasone has a powerful anti-inflammatory effect and relatively low immunosuppressive activity.

CORTISONE

The drug is a natural glucocorticoid, biologically inactive. Activated in the liver, turning into hydrocortisone. Has a short-term effect. Compared to other glucocorticoids, it has more pronounced mineralocorticoid activity, that is, it has a significant effect on water-electrolyte metabolism.

Features of application

Mainly used for replacement therapy

adrenal insufficiency in patients with normal liver function.

Release forms:

  • tablets of 25 and 50 mg (cortisone acetate)
    .

HYDROCORTISONE

A natural glucocorticoid, its glucocorticoid activity is 4 times weaker than prednisolone, but its mineralocorticoid activity is slightly superior. As with cortisone, there is a high risk of edema, sodium retention, and potassium loss.

Features of application

Hydrocortisone, like cortisone, is not recommended for pharmacodynamic therapy

, especially in patients with edema, hypertension, and heart failure.
It is used
mainly
for replacement therapy
for primary and secondary adrenal insufficiency. In acute adrenal insufficiency and other emergency conditions, the drug of choice is hydrocortisone hemisuccinate.

Release forms:

  • hydrocortisone hemisuccinate, dry substance or solution in ampoules and bottles of 100 and 500 mg (hydrocortisone-meva, panukort, solu-cortef)
    ;
  • hydrocortisone acetate, suspension in ampoules and vials of 25 mg/ml.

PREDNISOONE

Synthetic glucocorticoid, most often used in clinical practice for pharmacodynamic therapy

and is considered as a standard drug. In glucocorticoid activity it is 4 times stronger than hydrocortisone, and in mineralocorticoid activity it is inferior to it. Refers to glucocorticoids with an average duration of action.

Release forms:

  • tablets of 5, 10, 20 and 50 mg (ano-prednisone, decortin N, tednisol);
  • prednisolone phosphate, 1 ml ampoules, 30 mg/ml;
  • prednisolone hemisuccinate, powder in ampoules of 10, 25, 50 and 250 mg (decortin salt);
  • prednisolone acetate, suspension in ampoules of 10, 20, 25 and 50 mg ( prednihexol).

PREDNISONE

In terms of activity and other parameters it is close to prednisolone. Initially, prednisone is a metabolically inactive drug (prodrug). Activated in the liver by hydroxylation and conversion to prednisolone. Therefore, it is not recommended to use it for severe liver diseases. The main advantage of prednisone is its lower cost.

Release forms:

  • 5 mg tablets (prednisone).

METHYLPREDNISOLONE

Compared to prednisolone, it has slightly greater (20%) glucocorticoid activity, minimal mineralocorticoid effect, and is less likely to cause undesirable reactions (especially changes in the psyche, appetite, ulcerogenic effect). It has a higher cost than prednisolone.

Features of application

Just like prednisolone, it is used mainly for pharmacodynamic therapy. It is preferable in patients with mental disorders, obesity, peptic ulcer disease, as well as during pulse therapy.

Release forms:

  • tablets of 4 and 16 mg (Medrol, Metypred, Urbazon, Prednol);
  • methylprednisolone succinate, dry substance in ampoules and vials of 8, 20, 40, 125, 250, 500 mg, 1.0 and 2.0 g (metipred, prednol-L, solu-medrol);
  • methylprednisolone acetate, suspension in 40 mg bottles (depo-medrol, metypred);
  • methylprednisolone suleptanate, ampoules of 50 and 100 mg/ml (promedrol).

TRIAMCINOLONE

It is a fluorinated glucocorticoid. It has a stronger (20%) and longer-lasting glucocorticoid effect than prednisolone. Has no mineralocorticoid activity. More often causes undesirable reactions, especially from muscle tissue (“triamcinolone” myopathy) and skin (striae, hemorrhages, hirsutism).

Release forms:

  • tablets of 2, 4 and 8 mg ( berlicort, delficort, kenacort, polcortolone
    );
    triamcinolone acetonide, suspension in ampoules of 40 mg/ml ( kenalog, tricort
    );
  • triamcinolone hexacetonide, suspension in ampoules of 20 mg/ml ( Lederspan
    ).

DEXAMETHASONE

Just like triamcinolone, it is a fluorinated drug. One of the most powerful glucocorticoids: 7 times stronger than prednisolone in glucocorticoid activity. Does not have mineralocorticoid effect. It causes severe depression of the hypothalamic-pituitary-adrenal system, severe disturbances of carbohydrate, fat, calcium metabolism, and a psychostimulating effect, therefore it is not recommended to prescribe it for a long period.

Features of application

The drug has some special indications for use: bacterial meningitis; cerebral edema; in ophthalmology (keratitis, uveitis and others); prevention and treatment of nausea and vomiting during chemotherapy; treatment of severe withdrawal syndrome in alcoholism; prevention of respiratory distress syndrome in premature infants (dexamethasone stimulates the synthesis of surfactant in the alveoli of the lungs); leukemia (replacing prednisolone with dexamethasone in acute lymphoblastic leukemia significantly reduces the incidence of damage to the central nervous system).

Release forms:

  • tablets of 0.5 and 1.5 mg (daxin, dexazone, cortidex);
  • dexamethasone phosphate, ampoules of 1 and 2 ml, 4 mg/ml (daxin, dexabene, dexazone, sondex).

BETAMETHASONE

A fluorinated glucocorticoid, similar in strength and duration of action to dexamethasone. Glucocorticoid activity is 8-10 times higher than that of prednisolone. Does not have mineralocorticoid properties. It has a somewhat weaker effect on carbohydrate metabolism than dexamethasone. The best known drug is betamethasone phosphate/dipropionate, intended for intramuscular, intra-articular and periarticular administration. It consists of two esters, one of which - phosphate - is quickly absorbed from the injection site and gives a quick (within 30 minutes) effect, and the other - dipropionate - is absorbed slowly, but provides a prolonged effect - up to 4 weeks or more. It is a fine-crystalline suspension that cannot be administered intravenously. Water-soluble betamethasone phosphate is administered intravenously and subconjunctivally.

Indications for use of the drug Methylprednisolone

  • endocrine diseases, such as primary or secondary adrenal insufficiency, non-suppurative thyroiditis, hypercalcemia due to tumor disease;
  • rheumatoid arthritis, juvenile rheumatoid arthritis (short-term course as an auxiliary therapy for exacerbation of the process);
  • inflammatory-degenerative and metabolic diseases of the joints, including psoriatic arthritis, ankylosing spondylitis, acute and subacute bursitis, acute and nonspecific tenosynovitis, acute gouty arthritis, post-traumatic osteoarthritis, synovitis in osteoarthritis, epicondylitis (short-term course as an auxiliary therapy for exacerbation of the process) ;
  • rheumatic carditis, polymyalgia rheumatica (mainly during exacerbation);
  • systemic connective tissue diseases, such as systemic lupus erythematosus, dermatomyositis, acute giant cell arthritis (during an exacerbation or as maintenance therapy);
  • skin diseases such as pemphigus, bullous dermatitis herpetiformis, severe erythema multiforme, exfoliative dermatitis, mycosis fungoides, severe psoriasis, severe seborrheic dermatitis;
  • allergic diseases with a severe course that are not amenable to adequate traditional therapy and lead to disability of the patient, for example, seasonal or chronic allergic rhinitis, serum sickness, asthma, drug allergies, contact or atopic dermatitis;
  • eye diseases (severe acute and chronic processes), such as allergic marginal corneal ulcer, herpetic eye lesions, inflammation of the anterior segment of the eye, diffuse posterior uveitis and choroiditis, sympathetic ophthalmia, allergic conjunctivitis, keratitis, chorioretinitis, optic neuritis, iritis and iridocyclitis;
  • respiratory diseases, such as symptomatic sarcoidosis, Loeffler's syndrome, berylliosis, focal or disseminated pulmonary tuberculosis (with simultaneous anti-tuberculosis chemotherapy);
  • hematological diseases such as idiopathic thrombocytopenic purpura in adults, secondary thrombocytopenia in adults, autoimmune hemolytic anemia, erythroblastopenia, congenital hypoplastic anemia;
  • leukemia and lymphoma in adults, acute leukemia in children (as part of complex therapy);
  • nonspecific ulcerative colitis, regional enteritis;
  • multiple sclerosis in the acute phase;
  • trichinosis with damage to the nervous system or myocardium;
  • prevention of rejection after organ transplantation;
  • nephrotic syndrome;
  • cerebral edema due to brain tumor;
  • tuberculous meningitis with a subarachnoid block or with a threat of block development (with simultaneous anti-tuberculosis therapy).

Methylprednisolone-FS tablet 8 mg in container pack No. 10x3

Name

Methylprednisolone-fs t

Release forms

pills

INN

Methylprednisolone

FTG

Glucocorticosteroid

Basic physical and chemical properties

tablets are white or almost white, round, flat-cylindrical, with a notch in the form of a cross.

Compound

active ingredient: methylprednisolone; 1 tablet contains: methylprednisolone 4 mg or 8 mg; excipients: lactose monohydrate, potato starch, sodium starch glycolate (type A), magnesium stearate, colloidal anhydrous silicon dioxide.

Drug classification code

Corticosteroids for systemic use. Glucocorticosteroids. Methylprednisolone. ATX code: N02AB04.

Pharmacological properties
Pharmacodynamics

Methylprednisolone is a synthetic glucocorticosteroid. Glucocorticoids penetrate cell membranes and form complexes with specific cytoplasmic receptors that penetrate the cell nucleus, bind to DNA (chromatin), stimulate mRNA transcription and further synthesis of various enzymes, which explains the effect of systemic use of glucocorticoids. Methylprednisolone is an analogue of prednisolone. It is similar in activity to prednisolone, but has virtually no mineralocorticoid activity, which ensures better tolerability. Glucocorticoids not only have a significant effect on the inflammatory process and the immune response, but also affect carbohydrate, protein and fat metabolism, the cardiovascular system, skeletal muscles and the central nervous system.

Effect on inflammation and immune response

Methylprednisolone has anti-inflammatory, desensitizing and angiallergic effects. It has antishock, antitoxic and immunosuppressive properties. Unlike cytostatics, the immunosuppressive properties of methylprednisolone are not associated with a mitostatic effect, but are the result of suppression of various stages of immunogenesis: migration of bone marrow stem cells, migration of B cells and interaction of T and B lymphocytes. Like other corticosteroids, methylprednisolone inhibits the release of cytokines (interleukins 1 and 2, γ-interferon) from lymphocytes and macrophages, inhibits the release of inflammatory mediators by eosinophils, reduces the metabolism of arachidonic acid, thereby achieving the following therapeutic effects: reducing the number of immunoactive cells near the site of inflammation; decreased vasodilation; stabilization of lysosomal membranes; inhibition of phagocytosis; decreased production of prostaglandins and related compounds. A dose of 4 mg of methylprednisolone has the same glucocorticosteroid (anti-inflammatory) effect as 20 mg of hydrocortisone. Methylprednisolone has only minimal mineralocorticoid effects (200 mg methylprednisolone is equivalent to 1 mg deoxycorticosterone). Effect on protein and carbohydrate metabolism Glucocorticoids exhibit a catabolic effect on proteins: they delay the synthesis and accelerate the breakdown of proteins. By stimulating steroid receptors, they induce the formation of a special class of proteins - lipocortins, which have an anti-edematous effect. The amino acids that are released are converted by the process of gluconeogenesis in the liver into glucose and glycogen. The absorption of glucose in peripheral tissues is reduced, which can lead to hyperglycemia and glycosuria, especially in patients prone to diabetes. Effect on fat metabolism Glucocorticoids have lipolytic activity, which manifests itself primarily in the tissues of the extremities, and lipogenetic activity, which is most pronounced in the chest, neck and head, which leads to the redistribution of fat deposits. In relatively high doses, it inhibits the development of lymphoid and connective tissue, including reticuloendothelium; reduces the number of mast cells, which are the site of formation of hyaluronic acid; inhibits the activity of hyaluronidase and helps reduce capillary permeability. The maximum pharmacological activity of corticosteroids occurs when peak plasma concentrations have already passed, so it is believed that the vast majority of therapeutic effects of drugs are due primarily to modification of enzyme activity, and not to direct action of the drug.

Pharmacokinetics

The pharmacokinetics of methylprednisolone is linear, regardless of the route of administration. Absorption The bioavailability of methylprednisolone in healthy people after oral administration is generally high (82-89%). After oral administration, methylprednisolone is rapidly absorbed and the maximum concentration of methylprednisolone in the blood plasma is achieved within 1.5-2.3 hours (depending on the dose) after taking this drug in healthy people. The level of absorption in the distal region is approximately 50% of the level of absorption in the proximal region. Distribution Methylprednisolone is widely distributed in tissues, penetrates the blood-brain barrier and is excreted into breast milk. Forms weak dissociated bonds with albumin and transcortin. Plasma protein binding of methylprednisolone in humans is approximately 77%. The volume of distribution of methylprednisolone is approximately 1/2 kg. Metabolism Methylprednisolone is metabolized in the liver to inactive metabolites. The main metabolites are 20-α-hydroxymethylprednisolone and 20-β-hydroxymethylprednisolone. Its metabolism in the liver occurs primarily with the participation of the CYP3A4 enzyme (for a list of drug interactions based on metabolism mediated by CYP3A isoenzymes, see the section “Interaction with other drugs and other types of interactions”). Conjugation reactions occur mainly in the liver, and to a lesser extent in the kidneys. Excretion Metabolites are excreted mainly in the urine in the form of glucuronides, sulfates and unconjugated compounds. The half-life of total methylprednisolone is 1.8 to 5.2 hours. The total clearance is about 5-6 ml/min/kg. Methylprednisolone is eliminated by hemodialysis.

Indications for use

Endocrine diseases Primary and secondary adrenal insufficiency (in this case, the first-line drugs are hydrocortisone or cortisone; if necessary, synthetic analogues can be used in combination with mineralocorticoids; simultaneous use of mineralocorticoids is especially important for the treatment of children); congenital adrenal hyperplasia; non-purulent thyroiditis; hypercalcemia in malignant tumors. Non-endocrine diseases Rheumatic diseases As an additional therapy for short-term use (to remove a patient from an acute condition or during an exacerbation of the process) for the following diseases: psoriatic arthritis; rheumatoid arthritis, including juvenile rheumatoid arthritis (in some cases, low-dose maintenance therapy may be required); ankylosing spondylitis; acute and subacute bursitis; acute nonspecific tenosynovitis; acute gouty arthritis; post-traumatic osteoarthritis; synovitis in osteoarthritis; epicondylitis. Collagenoses During the period of exacerbation or in some cases as maintenance therapy for the following diseases: systemic lupus erythematosus; acute rheumatic carditis; systemic dermatomyositis (polymyositis); polymyalgia rheumatica with giant cell arteritis. Skin diseases Pemphigus; bullous dermatitis herpetiformis; severe erythema multiforme (Stevens-Johnson syndrome); mycosis fungoides; severe forms of psoriasis; exfoliative dermatitis; severe seborrheic dermatitis. Allergic diseases Control of severe or allergic conditions for which conventional therapy is ineffective: bronchial asthma; dermatitis (contact, atopic); serum sickness; seasonal or persistent allergic rhinitis; drug allergy. Ophthalmological diseases Severe acute and chronic allergic and inflammatory processes with eye damage, such as: allergic marginal corneal ulcers; eye lesions caused by Herpes zoster, inflammation of the anterior segment of the eye; diffuse posterior uveitis and choroiditis; sympathetic ophthalmia; allergic conjunctivitis; keratitis; chorioretinitis; iritis and iridocyclitis; Optic neuritis. Respiratory diseases Symptomatic sarcoidosis; Lefler's syndrome, refractory to treatment with other methods; berylliosis; focal or disseminated pulmonary tuberculosis (together with appropriate anti-tuberculosis chemotherapy); aspiration pneumonitis. Blood diseases Idiopathic thrombocytopenic purpura in adults; secondary thrombocytopenia in adults; acquired (autoimmune) hemolytic anemia; erythroblastopenia (erythrocyte anemia); congenital (erythroid) hypoplastic anemia. Oncological diseases, as palliative therapy: leukemia and lymphoma in adults; acute leukemia in children. Edema syndrome For induction of diuresis or treatment of proteinuria with nephrotic syndrome without uremia, idiopathic type or caused by systemic lupus erythematosus. Diseases of the digestive tract To remove the patient from a critical condition with the following diseases: ulcerative colitis; Crohn's disease. Diseases of the nervous system: multiple sclerosis in the acute phase; swelling of the brain caused by a brain tumor. Diseases of other organs and systems: tuberculous meningitis with subarachnoid block or with the threat of block development, in combination with appropriate anti-tuberculosis chemotherapy; trichinosis with damage to the nervous system or myocardium. Organ transplantation.

Directions for use and doses

The initial dose for adults can vary from 4 to 48 mg of methylprednisolone per day, depending on the indication. It is necessary to use the lowest dose of corticosteroids to control the course of the disease. For less severe illnesses, low doses are usually sufficient, although individual patients may require higher starting doses. High doses can be used for diseases and conditions such as multiple sclerosis (200 mg per day), cerebral edema (200-1000 mg per day), organ transplantation (up to 7 mg/kg per day). If satisfactory clinical effect is not achieved after an appropriate period of time, therapy with methylprednisolone tablets should be discontinued and the patient should be given alternative therapy. If after long-term therapy the drug needs to be discontinued, it is recommended that this be done gradually rather than suddenly. If a satisfactory effect is achieved as a result of therapy, an individual maintenance dose should be selected for the patient by gradually reducing the initial dose at certain intervals until the lowest dose is found that will maintain the achieved clinical effect. It should be remembered that constant monitoring of the dosage of the drug is necessary. Situations in which it may be necessary to adjust the dose of the drug include: changes in clinical condition due to the onset of remission or exacerbation of the disease; individual patient response to the drug; exposure to stressful situations on the patient are not directly related to the underlying disease that the therapy is aimed at. In the latter case, it may be necessary to increase the dose of methylprednisolone for a certain period of time, depending on the patient's condition. It should be emphasized that the required dose may vary and should be selected individually depending on the nature of the disease and the patient's response to therapy. Alternating therapy (AT) Alternating therapy is a corticosteroid dosing regimen in which a double dose of glucocorticoids should be prescribed every other day, in the morning. The goal of this type of therapy is to provide the patient who requires long-term therapy with the maximum benefits of corticosteroids while minimizing some of the undesirable effects such as pituitary-adrenal suppression, Cushingoid condition, corticosteroid withdrawal syndrome, and growth suppression in children. Diseases Loading dose Maintenance dose Rheumatic diseases - severe rheumatoid arthritis, moderate, mild children - systemic lupus erythematosus - acute rheumatic fever 12-16 mg 8-10 mg 6-8 mg 6-10 mg 20-40 mg 6-12 mg 4-8 mg 2-6 mg2-8 mg8-20 mg 0.5 mg for every 450 g of body weight until serum mucoproteins reach 6 mg% and erythrocyte sedimentation rate remains normal for a week Allergic diseases - severe seasonal asthma - hay fever in severe form - exfoliative dermatitis (erythroderma) - contact dermatitis - asthma - allergic rhinitis not responding to standard therapy - generalized atopic dermatitis - generalized eczema in children 16-40 mg 16-40 mg 16-40 mg 16-40 mg 12-40 mg 12-40 mg 12- 40 mg8-12 mg 4-16 mg4-16 mg4-16 mg Diseases and inflammatory processes of the eye-acute-chronic 12-40 mg12-40 mg 2-12 mg Other diseases-adrenal-genital syndrome-ulcerative colitis-leukemia-nephrotic syndrome 16-60 mg 12-16 mg 20-60 mg (10-14 days or until diuresis appears) 4-12 mg 12-40 mg (3 days a week in a row for 6-12 months)

Adverse reactions

The development of severe adverse reactions depends on the dose and duration of treatment. Adverse reactions usually develop with long-term use of the drug; during a short period of use, the risk of their occurrence is unlikely. The following are adverse reactions associated with methylprednisolone therapy, listed according to organ system class, frequency, and severity. In each group, the frequencies of adverse reactions are indicated in order of decreasing severity. The frequency of adverse reactions is shown as: often (from ≥1/100 to

Contraindications

hypersensitivity to methylprednisolone or other components of the drug; systemic infections in cases where specific antimicrobial therapy is not intended; systemic fungal infections; Administration of live or live attenuated vaccines is contraindicated in patients receiving immunosuppressive doses of corticosteroids.

Overdose

No clinical syndrome of acute corticosteroid overdose has been reported. Case reports of acute toxicity and/or death following corticosteroid overdose are rare. In case of overdose, there is no specific antidote; supportive and symptomatic treatment is provided. Methylprednisolone is eliminated by dialysis.

Precautionary measures

Corticosteroids should be used with caution and under strict medical supervision in patients with arterial hypertension, congestive heart failure, diabetes mellitus (or a family history of diabetes), pancreatitis, and diseases of the digestive tract (peptic ulcer, local ileitis, ulcerative colitis or other inflammatory diseases of the digestive tract or diverticulitis with an increased risk of bleeding and perforation), ocular herpes (as corneal perforation is possible), hypothyroidism, history of corticosteroid-induced myopathy, liver failure, cirrhosis, epilepsy, abscess or other pyogenic infections, glaucoma, prone to thrombophlebitis and with mental disorders disorders. Caution must also be exercised when prescribing the drug to patients who have recently suffered a myocardial infarction, with recent intestinal anastomoses and renal failure. Patients with bleeding disorders should be under medical supervision. Immunosuppressive effects/increased susceptibility to infections Corticosteroids may increase susceptibility to infections and mask some symptoms of infections; In addition, new infections may develop during corticosteroid therapy. When using corticosteroids, resistance to infections may decrease and the body may be unable to localize the infection. There is a risk of developing secondary infections caused by bacteria, fungi, viruses, protozoa or helminths from any location in the body, which may occur during the use of corticosteroids as monotherapy or in combination with other immunosuppressive agents that affect the state of cellular and humoral immunity and neutrophil function . These infections can be mild, but can sometimes be severe and even fatal. As the dose of corticosteroids increases, the incidence of infectious complications increases. Patients taking drugs that suppress the immune system are more susceptible to infections than healthy people. Chickenpox and measles, for example, can have more serious or even fatal outcomes in unimmunized children or adults who take corticosteroids. The use of live or live attenuated vaccines is contraindicated in patients receiving immunosuppressive doses of corticosteroids. Patients receiving immunosuppressive doses of corticosteroids can be vaccinated with killed or inactivated vaccines, but their response to such vaccines may be reduced. These immunization procedures can be performed in patients receiving corticosteroids in doses that do not have an immunosuppressive effect. The use of corticosteroids for active tuberculosis should be prescribed only in cases of fulminant or disseminated tuberculosis, when corticosteroids must be used in combination with appropriate anti-tuberculosis therapy. If corticosteroids are indicated for patients with latent tuberculosis or during the period of tuberculin testing, treatment should be carried out under strict medical supervision, since reactivation of the process is possible. During long-term corticosteroid therapy, such patients should be given appropriate prophylactic treatment. Cases of Kaposi's sarcoma have been reported in patients receiving corticosteroid therapy. In such cases, discontinuation of corticosteroid therapy may result in clinical remission. There is no consensus on the role of corticosteroids in the treatment of patients with septic shock. Previous studies have reported both positive and negative effects of corticosteroid use in this clinical setting. Later studies showed that corticosteroids as adjunctive therapy had a beneficial effect in patients with septic shock due to adrenal insufficiency. However, routine use of these drugs in patients with septic shock is not recommended. A systematic review of the data concluded that there was no benefit from short courses of high-dose corticosteroids in these patients. However, a meta-analysis and one review have shown that longer (5-11 days) courses of low-dose corticosteroids may reduce mortality, especially in patients with vasopressor-dependent septic shock. In addition, corticosteroids should be used with great caution in patients with known or suspected parasitic infections, such as strongyloidiasis (acne infestation). In these patients, corticosteroid-induced immunosuppression can lead to strongyloides hyperinfection and dissemination with widespread larval migration, often accompanied by severe enterocolitis and potentially fatal gram-negative septicemia. Effect on the immune system Allergic reactions (eg, angioedema) may occur. Since skin reactions and anaphylactic/anaphylactoid reactions have been reported in rare cases in patients receiving corticosteroid therapy, appropriate precautions should be taken before use, especially if the patient has a history of allergy to any drug. Effects on the endocrine system In patients receiving corticosteroid therapy and who are exposed to stress, increasing the dose of rapid-acting corticosteroids before, during and after a stressful situation is indicated. Long-term use of glucocorticoids can lead to suppression of the hypothalamic-pituitary-adrenal axis (the development of secondary adrenal insufficiency) and contribute to the exacerbation of diseases and the development of complications in various conditions, for example, during acute injuries, diseases or surgery. The degree and duration of adrenocortical insufficiency varies between patients and depends on the dose, frequency, timing of use, and duration of glucocorticoid therapy. This effect can be minimized by using alternating therapy (see section "Dosage and Administration"). High doses of methylprednisolone significantly reduce the risk of developing these complications. If glucocorticoids are suddenly withdrawn, acute adrenal insufficiency may develop, which can be fatal. Adrenocortical insufficiency caused by the use of the drug can be minimized by gradually reducing the dose. This type of relative deficiency can be recorded for several months after discontinuation of therapy, therefore, if stressful situations arise during this period, hormonal therapy must be reinstated. Since mineralocorticoid secretion may be impaired, electrolytes and/or mineralocorticoids should be administered concomitantly. With long-term use of glucocorticoids, therapy should be discontinued gradually over several weeks to avoid “withdrawal syndrome” and serious complications. This syndrome includes symptoms such as anorexia, nausea, vomiting, lethargy, headache, fever, joint pain, desquamation, myalgia, weight loss and/or hypotension. These effects are thought to result from a sudden change in glucocorticoid concentrations rather than from low corticosteroid levels. Long-term therapy should not be stopped suddenly, also in case of pregnancy. Because corticosteroids may cause or worsen Cushing's syndrome, their use should be avoided in patients with Cushing's disease. Particular attention should be paid to the use of corticosteroids in patients with hypothyroidism, which requires frequent monitoring of their condition. Patients with hypothyroidism or severe liver disease should have their dose reduced due to the increased effect of methylprednisolone. Metabolic and nutritional disorders Corticosteroids, including methylprednisolone, may increase blood glucose, worsen the condition of patients with a history of diabetes mellitus, and also contribute to the development of diabetes mellitus in patients using corticosteroids long-term. Mental disorders When using corticosteroids, various mental disorders are possible: from euphoria, insomnia, mood changes, personality changes to severe depression with the expression of psychotic manifestations. In addition, while taking corticosteroids, existing emotional instability and a tendency to psychotic reactions may increase. Particular attention should be paid to the systemic use of corticosteroids in both patients and their first-degree relatives with pre-existing severe affective mental disorders. These disorders include depressive or manic-depressive illness or pre-existing steroid psychosis. Symptoms usually occur within a few days or weeks of starting therapy. Most reactions disappear after reducing the dose or discontinuing the drug, although special treatment may be necessary. Mental reactions have been observed during corticosteroid withdrawal; their frequency is unknown. Patients and their caregivers should be advised to seek medical attention if the patient develops any mental health problems, especially if the patient is suspected of being depressed or having suicidal thoughts. Patients and their caregivers should be alert to possible psychiatric disorders that may occur during or immediately following tapering or discontinuation of systemic steroids. Nervous system disorders Patients with seizures, as well as myasthenia gravis, should use corticosteroids with caution (see information about myopathy in the “Adverse reactions” section). Although controlled clinical trials have demonstrated the effectiveness of corticosteroids in accelerating the reduction of acute symptoms of exacerbations of multiple sclerosis, they have not demonstrated the effect of corticosteroids on the outcome or natural history of this disease. According to the results of these studies, relatively high doses of corticosteroids must be used to demonstrate a significant effect (see section "Dosage and Administration"). Epidural lipomatosis has been reported in patients taking corticosteroids, usually in high doses over a long period of time. Visual disorders In case of eye damage caused by glaucoma (or if close relatives have this disease) or herpes simplex virus, corticosteroids should be used with caution, as this may cause perforation of the cornea. With long-term use of corticosteroids, posterior subcapsular cataracts and nuclear cataracts (especially in children), proptosis, or increased intraocular pressure may develop, which can lead to glaucoma with possible damage to the optic nerve. Patients taking glucocorticoids are at increased risk of developing secondary eye infections caused by fungi and viruses. Corticosteroid therapy has been associated with the development of retinal detachment. Cardiac disorders The negative effects of glucocorticoids on the cardiovascular system, such as dyslipidemia and hypertension, when used long-term in high doses, may contribute to the occurrence of additional cardiovascular adverse events in patients with pre-existing cardiovascular risk factors. In this regard, corticosteroids should be used rationally in such patients, and also take into account the modification of risk factors and, if necessary, additionally monitor cardiac activity. Low doses and alternating therapy may reduce the incidence of complications during corticosteroid therapy. In patients with congestive heart failure, systemic corticosteroids should be used with caution and only when absolutely necessary. Particular caution is required when using systemic corticosteroids in patients with recent myocardial infarction (myocardial rupture has been reported), and frequent monitoring of the patient's condition is necessary. Caution should be exercised in patients receiving cardioactive drugs such as digoxin due to steroid-induced electrolyte imbalance/potassium loss. Vascular disorders Cases of thrombosis, including thromboembolism, have been reported with the use of corticosteroids. Caution should be exercised when prescribing corticosteroids to patients who have or may be susceptible to thromboembolic disorders. Corticosteroids should be used with caution in patients with hypertension. Gastrointestinal disorders High doses of corticosteroids can cause the development of acute pancreatitis. There is no consensus that corticosteroids themselves cause the development of gastric ulcers during therapy. Corticosteroids may make it difficult to diagnose gastrointestinal complications because they reduce pain and may also mask the symptoms of peptic ulcers. In combination with NSAIDs, the risk of developing gastrointestinal ulcers increases. Therefore, aspirin and nonsteroidal anti-inflammatory drugs should be used with caution in combination with corticosteroids. Corticosteroids should be used with caution in ulcerative colitis if there is a risk of gastrointestinal wall perforation, abscess formation, or other purulent infection; with diverticula; in the case of recently performed intestinal anastomoses; with active or latent peptic ulcer. Hepatobiliary disorders Particular attention should be paid to the use of systemic corticosteroids in patients with cirrhosis and liver failure. Isolated hepatobiliary disorders have been reported, most of which were reversible after discontinuation of the drug. Careful monitoring is required. Musculoskeletal disorders Cases of acute myopathy have been reported with the use of high-dose corticosteroids, most often in patients with disorders of neuromuscular transmission (eg, myasthenia gravis) or in patients receiving therapy with anticholinergic drugs that block neuromuscular transmission ( e.g. pancuronium). This acute myopathy is generalized and can affect the eye and respiratory muscles and lead to tetraparesis. An increase in creatine kinase levels may occur. It may take several weeks to several years for clinical improvement or recovery after discontinuation of corticosteroids. Osteoporosis is one of the adverse reactions that is often observed, but rarely diagnosed, and develops with long-term use of high doses of glucocorticoids. During long-term therapy with methylprednisolone, it is necessary to consider prescribing bisphosphonates in patients with osteoporosis or with risk factors for its development. Risk factors for osteoporosis include age over 65 years, a history or family history of frequent fractures, early menopause (before 45 years), premenopausal amenorrhea, and low body weight. The risk of developing osteoporosis can be minimized by adjusting the dose of methylprednisolone to the lowest therapeutic level. Kidney disorders and

Use of the drug Methylprednisolone

Recommended methods of administration: orally, intramuscularly, intra-articularly, periarticularly, intrabursally, into soft tissues, into a pathological focus, instillation into the rectum. The dose is set individually depending on the nature of the disease and its severity. Orally - at an initial dose of 16–96 mg for 24 hours; for long-term treatment, the minimum possible dose should be prescribed; It is advisable to take every other day in the morning. The maintenance dose for adults is 4–12 mg/day. Parenterally: administered intravenously, intravenously and intramuscularly, usually at a dose of 100–500 mg. To eliminate shock conditions and rejection reactions during organ transplantation for a limited time, the dose can be increased to 30 mg/kg. Methylprednisolone in high doses should be administered as an intravenous drip infusion over at least 10 minutes. To eliminate nausea and vomiting caused by taking cytostatics, 250 mg of methylprednisolone is administered 20 minutes before taking cytostatics and 250 mg 6 hours after taking. When treating young and middle-aged children, the dose should be reduced, but it should be at least 25 mg/day. There are the following regimens for the use of methylprednisolone. Continuous circuit. It is administered taking into account the circadian rhythm of endogenous cortisol secretion. For this purpose, 2/3 of the daily dose is prescribed in the morning, 1/3 in the afternoon. Alternating scheme. Prescribe a double dose of methylprednisolone once in the morning every other day. This regimen of use does not reduce the therapeutic effect, but significantly reduces the incidence of side effects, primarily suppression of the hypothalamic-pituitary-adrenal system, compared to continuous use. On break days, it is advisable to prescribe additional NSAIDs. An alternating regimen of use is especially indicated for use in children, since it does not interfere with the normal growth of the child. In case of moderate severity of the pathological process, alternating therapy can be prescribed from the very beginning of the course of treatment. In severe cases, to eliminate acute manifestations of the disease, continuous treatment is required (usually 4–10 days is sufficient for most allergic diseases and collagenoses). Then there are 2 options: 1) switching to alternative therapy with a gradual reduction in the dose of steroids taken every other day; 2) a gradual reduction in the dose of steroids taken on a continuous basis to a maintenance level, after which a transition to an alternating regimen is made. Theoretically, the first option is more promising. Patients taking GCS for a long time on a continuous basis (rheumatoid arthritis) should try to switch to an alternating dose. However, strong suppression of the hypothalamic-pituitary-adrenal axis complicates the task of transferring to an alternating circuit. Perhaps at the first stage there will be a need to take not double, but triple or even quadruple the dose of methylprednisolone every other day. After achieving control over the course of the disease, the dose can be gradually reduced. Intermittent therapy. Similar to alternating, but the use of methylprednisolone is carried out in short courses of 3-4 days, followed by 4-day intervals between courses. Pulse therapy. A fairly rapid infusion of ultra-high doses of methylprednisolone (500–1000 mg) over 30 minutes is used, the course is 3 days. The maximum concentration in the blood plasma after such an infusion is observed during the first hour, after which the drug is quickly redistributed in the body, and after a day its minimum concentration is determined in the serum. Pulse therapy does not cause sudden changes in the biochemical parameters of blood and urine (the concentration of glucose in the blood may increase, which may persist for several days). Changes in the cardiovascular system occur rarely; the most common complication is increased blood pressure; There are reports of the development of arrhythmia (sinus bradycardia), which can persist for 5 days. When conducting pulse therapy, the following rules are adhered to: a strict selection of candidates for pulse therapy is carried out (severe forms of diseases that are not amenable to conventional treatment with corticosteroids, visceral forms of rheumatic diseases); methylprednisolone infusion at a dose of 1000 mg is carried out over 30–40 minutes; monitor the patient’s general condition, heart rate, blood pressure, respiratory rate once before the infusion and at least 3 times during the day after the infusion; immediately respond to any patient complaints that arise during or after the infusion, repeating the clinical examination; They especially monitor the condition of patients with diseases of the cardiovascular system (hypertension, arterial hypertension, heart block) and diabetes mellitus. Advantages of pulse therapy: quick and effective reduction of symptoms; sustainable therapeutic effect (up to 1 year); reduced risk of side effects, positive dynamics during the course of the disease (especially in the early stages of the pathological process). Local application: for rheumatoid arthritis or osteoarthritis, the dose depends on the size of the joint and the severity of the disease; if necessary, injections can be repeated at intervals of 1–5 weeks or more. 20–80 mg of methylprednisolone is injected into a large joint; average - 10–40 mg; small - 4–10 mg. It is important to introduce the solution into the synovial space. For tendonitis and tenosynovitis, it is injected into the tendon sheath; for tendon sheath cysts, it is injected directly into the cyst. The dose is selected individually; it can range from 4 to 30 mg. Injections can be repeated. For skin diseases, 20–60 mg is injected directly into the lesion. For large lesions, it is possible to distribute the dose (20–40 mg) over several local injections. When a high dose is administered, the affected skin may turn white and peel. The course of treatment is 1–4 injections, intervals are individual. Rectal administration of the suspension is indicated for nonspecific ulcerative colitis. Prescribed as microenemas or rectal drips at a dose of 40–120 mg 3 to 7 times a week for 2 weeks or more. In most cases, 40 mg of methylprednisolone in 30–300 ml of water is sufficient. Depot suspension: IM 40–120 mg, if necessary, every 1–4 weeks. Intra-articular, depending on joint size, 4–80 mg as needed every 1–5 weeks. 4–30 mg is injected into the synovial bursae and tendon sheaths, and 20–60 mg into the area of ​​skin lesions (the drug cannot be administered subcutaneously or intradermally). 40–120 mg is administered rectally as an enema 3–7 times a week.

METIPRED

special instructions

Since complications of therapy with Metipred depend on the dose and duration of treatment, in each specific case, based on an analysis of the risk/benefit ratio, a decision is made on the need for such treatment, and the duration of treatment and frequency of administration are also determined.
In order to better control the patient's condition, the lowest dose of Metypred should be used. When an effect is achieved, if possible, the dose should be gradually reduced to a maintenance dose or treatment should be discontinued.

Due to the danger of developing arrhythmia, the use of the drug Metipred in high doses should be carried out in a hospital environment equipped with the necessary equipment (electrocardiograph, defibrillator).

If prolonged spontaneous remission occurs, treatment should be discontinued.

During long-term treatment, the patient should undergo regular examination (chest x-ray, plasma glucose concentration 2 hours after meals, urinalysis, blood pressure, body weight control, preferably an x-ray or endoscopic examination if there is a history of gastrointestinal ulcers). intestinal tract).

The growth and development of children on long-term therapy with Metipred should be carefully monitored. Growth retardation may occur in children receiving long-term, daily, divided-dose therapy. Daily use of methylprednisolone for a long time in children is possible only for absolute indications. Taking 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 of developing intracranial hypertension.

Metypred should also be prescribed with great caution to patients with confirmed or suspected parasitic infections, such as strongyloidiasis. Immunosuppression caused by methylprednisolone 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 death.

Patients receiving drugs that suppress the immune system are more susceptible to infections than healthy individuals. For example, chickenpox and measles may be more severe and even fatal in unimmunized children or in adults receiving Metypred.

For patients who may be exposed to stress during therapy with Metipred, an increase in the dose of the drug is indicated before, during and after a stressful situation.

During therapy with Metipred, susceptibility to infections may increase, some infections may occur in an erased form, and new infections may develop. In addition, the body’s ability to localize the infectious process is reduced. The development of infections caused by various pathogenic organisms, such as viruses, bacteria, fungi, protozoa or helminths, which are localized in various systems of the human body, may be associated with the use of the drug Metipred, both as monotherapy and in combination with other immunosuppressants that affect on cellular immunity, humoral immunity or neutrophil function. These infections may not be severe, but in some cases they can be severe and even fatal. Moreover, the higher doses of the drug are used, the higher the likelihood of developing infectious complications.

In patients receiving treatment with Metypred in doses that have an immunosuppressive effect, the administration of live or live attenuated vaccines is contraindicated, but killed or inactivated vaccines can be administered, however, the response to the administration of such vaccines may be reduced or even absent. Patients receiving treatment with Metipred in doses that do not have an immunosuppressive effect may be immunized according to appropriate indications. The use of Metypred in active tuberculosis should be limited to cases of fulminant and disseminated tuberculosis, when Metypred is used to treat the disease in combination with appropriate anti-tuberculosis chemotherapy.

If the drug Metypred is prescribed to patients with latent tuberculosis or with positive tuberculin tests, then treatment should be carried out under strict medical supervision, since reactivation of the disease is possible. During long-term drug therapy, such patients should receive appropriate preventive treatment. Kaposi's sarcoma has been reported in patients treated with Metipred. When the drug is discontinued, clinical remission may occur.

When using the drug Metipred in therapeutic doses for a long period, suppression of the hypothalamic-pituitary-adrenal system (secondary adrenal insufficiency) may develop. The degree and duration of adrenal insufficiency is individual for each patient and depends on the dose, frequency of use, time of administration and duration of 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 adrenal insufficiency may continue for several months after the end of treatment, so in case of any stressful situations during this period, Metypred should be re-prescribed. Since the secretion of mineralocorticosteroids may be impaired, concomitant administration of electrolytes and/or mineralocorticosteroids is necessary. The development of acute adrenal insufficiency, leading to death, is possible with abrupt discontinuation of the drug Metipred. Withdrawal syndrome, which does not appear to be related to adrenal insufficiency, can also occur due to abrupt discontinuation of Metypred. This syndrome includes symptoms such as anorexia, nausea, vomiting, lethargy, headache, fever, joint pain, skin peeling, myalgia, weight loss and low blood pressure. It is assumed that these effects occur due to sharp fluctuations in the concentration of methylprednisolone in the blood plasma, and not due to a decrease in the concentration of methylprednisolone in the blood plasma. In patients with hypothyroidism or cirrhosis of the liver, an increased effect of the drug Metypred is observed. The use of the drug Metypred may lead to an increase in glucose concentrations in blood plasma, worsening the course of existing diabetes mellitus. Patients receiving long-term therapy with Metipred may be predisposed to the development of diabetes mellitus. During therapy with Metipred, various mental disorders may develop: from euphoria, insomnia, mood instability, personality changes and severe depression to acute mental manifestations. In addition, existing emotional instability or tendencies to psychotic reactions may intensify. Potentially severe mental disorders may occur when using the drug Metipred. Symptoms usually appear within a few days to weeks after starting therapy. Most reactions disappear either after reducing the dose or after discontinuation of the drug. Despite this, specific treatment may be required. Patients and/or their relatives should be warned that if changes occur in the patient's psychological status (especially with the development of depression and suicidal attempts), it is necessary to seek medical help. Patients or their relatives should also be warned about the possibility of developing mental disorders during or immediately after reducing the dose of the drug or completely discontinuing it. Long-term use of the drug Metypred can lead to the occurrence of posterior subcapsular cataracts and nuclear cataracts (especially in children), exophthalmos or glaucoma with possible damage to the optic nerve and provoke the addition of a secondary ocular fungal or viral infection. When using the drug Metypred, there is an increase in blood pressure, fluid and salt retention in the body, loss of potassium, and hypokalemic alkalosis. These effects are less pronounced when using synthetic derivatives, except when used in large doses. It may be necessary to limit the intake of salt and foods containing sodium. Therapy with Metypred may mask the symptoms of a peptic ulcer, in which case perforation or bleeding may develop without significant pain. Adverse reactions of the drug Metypred from the cardiovascular system, such as dyslipidemia, increased blood pressure, can provoke new reactions in predisposed patients when using high doses of the drug Metypred and long-term treatment. In this regard, Metypred 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 Metypred every other day can reduce the severity of these side effects. Patients taking Metypred should be prescribed acetylsalicylic acid-based analgesics and non-steroidal anti-inflammatory drugs with caution. Allergic reactions are possible. Due to the fact that phenomena such as skin irritation and anaphylactic or pseudoanaphylactic reactions have rarely been observed in patients receiving GCS, the necessary measures should be taken before prescribing GCS, especially if the patient has a history of allergic reactions to drugs. Due to the existing risk of corneal perforation, GCS should be prescribed with caution when treating eye infections caused by the herpes simplex virus (ophthalmoherpes). High doses of GCS can cause acute pancreatitis. Therapy with high doses of GCS can cause acute myopathy; In this case, the disease is most susceptible to patients with disorders of neuromuscular transmission (for example, myasthenia gravis), as well as patients receiving concomitant therapy with anticholinergics, for example, blockers of neuromuscular transmission. This kind of myopathy is generalized; it can affect the muscles of the eyes or respiratory system and even lead to paralysis of all limbs. In addition, creatine kinase levels may increase. In such cases, clinical recovery may take weeks or even years. Osteoporosis is a common (but rarely identified) complication of long-term therapy with high doses of corticosteroids. Corticosteroids are prescribed with caution for long-term therapy in elderly patients due to the increased risk of osteoporosis and fluid retention in body, potentially causing an increase in blood pressure. Concomitant treatment with methylprednisolone and fluoroquinolones increases the risk of tendon rupture, especially in elderly patients. High doses of corticosteroids can cause pancreatitis in children. High doses of methylprednisolone should not be used in cases of brain damage caused by head trauma. Since methylprednisolone can enhance the clinical manifestations of Cushing's syndrome, the use of methylprednisolone should be avoided in patients with Cushing's disease. Careful monitoring of patients receiving systemic corticosteroids and recent history of myocardial infarction. Careful monitoring of patients with a history or current history of thrombosis or thromboembolic complications is necessary.

Side effects of the drug Methylprednisolone

Fluid and electrolyte imbalance: sodium and fluid retention, congestive heart failure (in predisposed patients), potassium loss, hypokalemic alkalosis. From the musculoskeletal system: steroid myopathy, muscle weakness, osteoporosis, pathological fractures, aseptic bone necrosis. From the central nervous system : increased intracranial pressure, pseudotumor of the cerebellum, mental disorders, convulsions. From the endocrine system and metabolic processes: menstrual irregularities, Itsenko-Cushing syndrome, suppression of the pituitary-adrenal axis, decreased tolerance to carbohydrates, steroid diabetes, negative nitrogen balance as a result of protein catabolism, growth retardation in children. From the organs of vision : posterior subcapsular cataract, increased intraocular pressure, exophthalmos. From the digestive tract: pancreatitis, esophagitis, erosive and ulcerative lesions of the digestive tract, including bleeding and perforation. Side effects caused by the immunosuppressive effect of methylprednisolone: ​​decreased body resistance to infections, activation of latent infections, opportunistic infections, deterioration of wound healing. Allergic reactions: skin manifestations, anaphylactic shock. Dermatological reactions: petechiae, ecchymosis, thinning and fragility of the skin. Local reactions: hyper- or hypopigmentation, atrophy of the skin and subcutaneous fat, post-injection exacerbation after intrasynovial use, abscesses. Other: when administered into pathological lesions in the head area, blindness developed in rare cases.

Buy Metypred tablets 4 mg No. 30 in pharmacies

Instructions for use Metipred tab. 4mg No. 30

Dosage forms 4 mg tablets Synonyms Depo-Medrol Medrol Solu-Medrol Group Drugs with glucocorticosteroid activity International nonproprietary name Methylprednisolone Composition Active substance: Methylprednisolone. Manufacturers Orion Corporation (Finland) Pharmacological action Has anti-inflammatory, antiallergic, immunosuppressive effects. Affects all phases of inflammation. By stabilizing the membranes of lysosomes, it reduces the release of lysosomal enzymes, inhibits the synthesis of hyaluronidase, capillary permeability and the formation of inflammatory exudate, improves microcirculation, reduces the production of lymphokines in lymphocytes and macrophages, inhibits the migration of macrophages, the processes of infiltration and granulation, suppresses the release of inflammatory mediators by eosinophils, reduces the production of collagen and mucopolysaccharides, fibroblast activity. Has a pronounced effect on metabolism: reduces synthesis and increases protein breakdown in muscle tissue, increases protein synthesis in the liver, synthesis of higher fatty acids and triglycerides, causes fat redistribution and hyperglycemia, stimulates glyconeogenesis, increases glycogen content in the liver and muscles, disrupts bone mineralization fabrics. When taken orally, it is quickly and completely absorbed. Biotransformation occurs in the liver. Passes through the blood-brain barrier and placenta, penetrates into breast milk. It is excreted in the form of metabolites mainly in the urine. Side effects : Itsenko-Cushing syndrome, atrophy of the adrenal cortex, menstrual irregularities, hirsutism, impotence, growth retardation in children, steroid diabetes, glycosuria, weight gain, negative nitrogen balance, sodium and water retention, edema, potassium loss, hypokalemic alkalosis, decreased tolerance to carbohydrates, peptic ulcers of the stomach and duodenum with possible perforation and bleeding, nausea, vomiting, ulcerative esophagitis, pancreatitis, bloating, headache, dizziness, increased intracranial pressure, cerebellar pseudotumor, mental disorders, convulsions, hypertension, congestive heart disease failure, arrhythmias, hypotension, thrombophilia, decreased resistance to infectious diseases, sterile abscesses, increased intraocular pressure, proptosis, posterior subcapsular cataracts, blindness, muscle weakness, steroid myopathy, decreased muscle mass, osteoporosis (especially in women and children), tendon rupture , vertebral compression fracture, aseptic necrosis of the head of the humerus and femur, pathological fracture of long bones, Charcot-type arthropathy, thinning and atrophy of the epidermis, dermis and subcutaneous tissue, deterioration of regeneration, petechiae, striae, steroid acne, pyoderma, candidiasis, hypo- and hyperpigmentation, ecchymosis, allergic reactions: urticaria, anaphylactic shock, bronchospasm. Indications for use : Primary or secondary adrenocortical insufficiency, Addison's disease, congenital adrenal hyperplasia, non-suppurative thyroiditis, hypercalcemia associated with cancer, shock (anaphylactic, burn, traumatic, cardiogenic), cerebral edema, severe trauma, additional therapy for acute course or exacerbation rheumatic diseases: psoriatic arthritis, rheumatoid arthritis, ankylosing spondylitis, acute or subacute bursitis, acute nonspecific tenosynovitis, acute gouty arthritis, post-traumatic osteoarthritis, synovitis in osteoarthritis, epicondylitis; collagenoses (exacerbation or maintenance therapy): systemic lupus erythematosus, acute rheumatic carditis, systemic dermatomyositis (polymyositis), skin diseases: pemphigus, bullous dermatitis herpetiformis, Stevens-Johnson syndrome, exfoliative dermatitis, mycoses, psoriasis, seborrheic dermatitis; allergic diseases: seasonal and persistent allergic rhinitis, serum sickness, bronchial asthma, allergic reactions caused by drugs, contact dermatitis, atopic dermatitis; anaphylactic and anaphylactoid reactions, urticaria during transfusion, eye diseases, allergic corneal ulcers, herpes zoster ophthalmicus, inflammation of the anterior segment, diffuse uveitis and choroiditis, sympathetic ophthalmia, allergic conjunctivitis, keratitis, chorioretinitis, optic neuritis, iritis and iridocyclitis; diseases of the respiratory tract (with appropriate chemotherapy): symptomatic sarcoidosis, Loeffler's syndrome, berylliosis, pulmonary tuberculosis, aspiration pneumonia; hematological diseases: idiopathic thrombocytopenic purpura in adults, secondary thrombocytopenia in adults, acquired (autoimmune) hemolytic anemia, erythroblastopenia, congenital hypoplastic anemia, agranulocytosis, acute lymphatic and myeloid leukemia; leukemia and lymphomas in adults; myeloma, lung cancer (in combination with cytostatics), gastrointestinal diseases: ulcerative colitis, Crohn's disease, local enteritis, hepatitis; neurological diseases: multiple sclerosis, myasthenia gravis, tuberculous meningitis (with appropriate chemotherapy), trichinosis, suppression of immunological incompatibility during organ transplantation, nausea and vomiting during cytostatic therapy Contraindications Hypersensitivity, acute and chronic bacterial or viral diseases without appropriate chemotherapeutic protection, systemic fungal diseases , active tuberculosis, AIDS, latent tuberculosis, intestinal anastomosis (in immediate history), congestive heart failure or hypertension, severe liver or kidney dysfunction, esophagitis, gastritis, acute or latent peptic ulcer, diabetes mellitus, myasthenia gravis, glaucoma, severe osteoporosis, hypothyroidism, mental disorders, poliomyelitis (except for bulbar-encephalic forms), lymphomas after BCG vaccination, pregnancy, breastfeeding, vaccination period; for intra-articular use - artificial joint, disorders of the blood coagulation system, intra-articular fracture, periarticular infectious process (including a history); for the prevention of respiratory distress syndrome in newborns - amnionitis, uterine bleeding, infectious diseases of the mother, placental insufficiency, premature rupture of the membranes of the fetus. Contraindicated in premature babies. Overdose Symptoms: edema, hypertension, the appearance of protein in the urine, decreased filtration volume, arrhythmias, hypokalemia, cardiopathy. Treatment: antacids, forced diuresis, potassium chloride, for depression and psychosis - dose reduction or discontinuation of the drug and the prescription of phenothiazines or lithium salts (tricyclic antidepressants are not recommended). Interaction Cyclosporine (inhibits metabolism) and ketoconazole (reduces clearance) increase toxicity. Phenobarbital, diphenhydramine, phenytoin, rifampicin and other inducers of liver enzymes increase the rate of elimination and reduce therapeutic effectiveness. Accelerates the release of aspirin, reduces its level in the blood (when methylprednisolone is discontinued, the level of salicylate in the blood increases and the risk of side effects increases). The action is enhanced by ACTH. Antacids (inhibit absorption), salicylates, butadione, indomethacin increase the likelihood of ulceration of the gastric mucosa, potassium-sparing drugs - severe hyperkalemia, amphotericin B and carbonic anhydrase inhibitors - hypokalemia, heart failure, osteoporosis, cardiac glycosides - arrhythmias, sodium-containing drugs - edema and hypertension. Ergocalciferol and parathyroid hormone prevent osteopathy caused by methylprednisolone. High doses of methylprednisolone reduce the effectiveness of somatotropin. Reduces the activity of oral antidiabetic drugs and the effectiveness of vaccines (live vaccines against the background of methylprednisolone can cause the disease). Mitotane and other inhibitors of adrenal function may necessitate an increase in dose. Special instructions With long-term use, it is necessary to monitor the function of the hypothalamic-pituitary-adrenal system, the level of glucose in the blood serum, and conduct ophthalmological examinations. It is not recommended to inject into the deltoid muscle. Intra-articular applications are carried out no more than once every 3 weeks. Intrathecal administration of a suspension of methylprednisolone acetate is contraindicated. May contribute to the spread or occurrence of infection caused by microorganisms and parasites. It should be used with caution in case of nonspecific ulcerative colitis, diverticula, and myasthenia gravis. Long-term use in children may cause growth retardation. The course must be completed by gradually reducing the dose. Withdrawal may be accompanied by abdominal and joint pain, weakness, nausea, headache, dizziness, fever, loss of appetite, and weight loss. With long-term use, you should reduce the calorie content of food, increase potassium intake, and reduce sodium intake. It is better to calculate the dose in children not per kg of body weight, but per square meter of surface. It is not recommended to mix with other injection solutions. Storage conditions List B. In a dark place at a temperature of 15-25 degrees. WITH.

Special instructions for the use of the drug Methylprednisolone

It should be used with caution and only under the strict supervision of a physician in severe forms of hypertension (arterial hypertension) and chronic heart failure, acute endocarditis, Itsenko-Cushing's disease, psychosis, nephritis, osteoporosis, peptic ulcers, syphilis, active forms of tuberculosis, diabetes mellitus. Caution is also necessary in case of herpetic infections (danger of corneal perforation), ulcerative colitis, diverticulitis, peptic ulcers, myasthenia gravis, and the presence of a recent intestinal anastomosis. In case of acute infectious disease, do not apply topically. Injecting the drug into previously infected joints should be avoided. After intra-articular administration, the joint should be unloaded. This is especially important during the period of symptomatic improvement. If there is exudate and hygroma, a puncture must be performed before administration. Intradermal injection should not be deep. An IM injection is performed deep into the gluteal muscle. It is necessary to avoid injection into the deltoid muscle, since in this case there is a high risk of developing atrophy of the subcutaneous fatty tissue. During treatment with methylprednisolone, vaccinations and immunizations should not be carried out due to the possibility of neurological complications and the lack of antibody formation. During treatment with methylprednisolone, it is possible to suppress reactions in tests with skin allergens. During pregnancy and lactation, it is used only when the expected therapeutic effect for the woman exceeds the potential risk to the fetus or child. Experimental studies revealed the embryotoxic effect of methylprednisolone.

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