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Methylprednisolone

Systemic application

The incidence and severity of side effects depend on the duration of use, the size of the dose used and the ability to comply with the circadian rhythm of the prescription.

Endocrine system: decreased glucose tolerance, “steroidal” diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing syndrome (moon-shaped face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia, stretch marks), delay sexual development in children.

Digestive system: nausea, vomiting, pancreatitis, “steroid” ulcer of the stomach and duodenum, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases, increased activity of liver transaminases and alkaline phosphatase.

Cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed individuals) or increased severity of chronic heart failure, changes in the electrocardiogram characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.

Nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor of the cerebellum, headache, convulsions.

Sense organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos.

Metabolism: increased excretion of Ca2+, hypocalcemia, increased body weight, negative nitrogen balance (increased protein breakdown), increased sweating.

Caused by mineralocorticoid activity - fluid and Na+ retention (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

Musculoskeletal system: slower growth and ossification processes in children (premature closure of epiphyseal growth plates), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and femur), rupture of muscle tendons, “steroid” myopathy, decreased muscle mass (atrophy).

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

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

Others: development or exacerbation of infections (the appearance of this side effect is facilitated by simultaneously used immunosuppressants and vaccination), leukocyturia, withdrawal syndrome.

Local for parenteral administration: burning, numbness, pain, paresthesia at the injection site, infection at the injection site, rarely - necrosis of surrounding tissues, scar formation at the injection site; atrophy of the skin and subcutaneous tissue when administered intramuscularly (injection into the deltoid muscle is especially dangerous).

With intravenous administration: arrhythmias, hot flashes, convulsions.

With intracranial administration - nosebleeds.

When administered parenterally in the head, neck, nasal turbinates, scalp, deposition of drug crystals is possible, and sudden loss of vision in the vessels of the eye.

Intra-articular administration - increased pain in the joint.

Local application

“Steroid” acne, purpura, telangiectasia, burning and itching of the skin, irritation and dry skin. With long-term use and/or when applied to large surfaces, systemic side effects are possible.

Application in ophthalmology

With long-term use: increased intraocular pressure, damage to the optic nerve, subcapsular cataracts, impaired visual acuity and narrowing of the visual field (blurred or loss of vision, eye pain, nausea, dizziness).

When the cornea becomes thinner, there is a risk of perforation.

Rarely - the spread of viral or fungal eye diseases.

Contraindications to the use of the drug Methylprednisolone-fs

Hypersensitivity to the drug or its components. Long-term use of Methylprednisolone-FS is contraindicated in acute viral infections (herpes zoster, herpes simplex, chicken pox); with HbsAg-positive active chronic hepatitis; damage to the lymph nodes after vaccination against tuberculosis; mumps; in the period 6 weeks before and up to 2 weeks after preventive vaccinations. The use of Methylprednisolone-FS is not recommended during pregnancy and lactation. If it is necessary to use the drug, the risk to the fetus or child must be carefully weighed against the benefit to the mother.

Pharmacological properties of the drug Methylprednisolone fs

Pharmacodynamics . Methylprednisolone-FS is a synthetic glucocorticosteroid - an analogue of prednisolone. It is close in activity to prednisolone, but has virtually no mineralocorticoid activity, which provides better susceptibility. The drug has anti-inflammatory, desensitizing and antiallergic effects, and also has anti-shock, antitoxic and immunosuppressant properties. Unlike cytostatics, the immunosuppressive properties of methylprednisolone are not associated with a mitostatic effect, but are the result of inhibition of different 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 IL-1 and IL-2 and interferon gamma) from lymphocytes and macrophages, suppresses the release of inflammatory mediators, and reduces the metabolism of arachidonic acid. By stimulating steroid receptors, it induces the formation of a special class of proteins - lipocortins, which exhibit anti-edematous activity. 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 reduces capillary permeability. Delays synthesis and accelerates protein breakdown. Shows lipolytic and lipogenetic activity. Pharmacokinetics. After oral administration, methylprednisolone is rapidly absorbed mainly in the proximal small intestine. Forms weakly dissociating bonds with albumin and transcortin. 40–90% of the drug is in a bound state. The distribution volume is 61 l. The drug is metabolized primarily in the liver. The main metabolites are 20-b-hydroxymethylprednisolone and 6-a-methylprednisolone. Metabolites are excreted mainly in the urine in the form of glucuronides, sulfates and unconjugated compounds. Conjugation reactions occur mainly in the liver, less so in the kidneys. The clearance of methylprednisolone is 383 l/day; half-life - 165 minutes.

Special instructions for the use of the drug Methylprednisolone-fs

Treatment must be carried out under the supervision of a doctor. Methylprednisolone-PS is used in two treatment regimens: in the form of circadian and alternating therapy. In circadian therapy, the drug is taken after meals, mainly after breakfast, without chewing and with the required amount of liquid. In some cases, for example, in the presence of morning and night attacks in patients with obstructive pulmonary diseases, the daily dose can be divided into two doses: 2/3 doses in the morning and 1/3 doses in the evening (between 18:00 and 20:00). With alternating therapy, the drug is taken every second day in a double dose after breakfast (between 6:00 and 8:00), without chewing and with a sufficient amount of liquid.

Drug interactions Methylprednisolone-fs

When used simultaneously with rifampicin, phenytoin, and barbiturates, the effect of methylprednisolone is reduced. Oral contraceptives containing estrogens enhance the effect of methylprednisolone. When using Methylprednisolone-FS simultaneously with NSAIDs, the risk of gastrointestinal bleeding increases. When used simultaneously with Methylprednisolone-FS, the effectiveness of oral hypoglycemic drugs, anticoagulants (coumarin derivatives), and somatotropin decreases. With simultaneous use of Methylprednisolone-FS with praziquantel, the level of praziquantel in the blood may decrease. Concomitant use with chloroquine, hydroxychloroquine, and metloquin increases the risk of developing myopathy and cardiomyopathy. The effect of cardiac glycosides is enhanced when used simultaneously with methylprednisolone. The simultaneous use of Methylprednisolone-FS with saluretics and laxatives increases potassium loss.

Indications for use of the drug Methylprednisolone-fs

Primary or secondary adrenal insufficiency; rheumatic diseases (rheumatoid arthritis, osteoarthritis, bursitis, ankylosing spondylitis, systemic lupus erythematosus); skin diseases: pemphigus, exfoliative dermatitis, severe forms of psoriasis, contact dermatitis, allergic dermatitis; BA; COPD; sarcoidosis; serum sickness; drug allergies; seasonal and common allergic rhinitis; autoimmune hemolytic anemia; idiopathic thrombocytopenic purpura; congenital erythroid hypoplastic anemia; ulcerative colitis; Crohn's disease; palliative treatment of some forms of tumor disease (leukemia and lymphoma).

Use during pregnancy and breastfeeding

The use of corticosteroids during pregnancy is possible if the expected effect of therapy outweighs the potential risk to the fetus (adequate and strictly controlled safety studies have not been conducted). Women of childbearing age should be warned of the potential risk to the fetus (corticosteroids cross the placenta). It is necessary to carefully monitor newborns whose mothers received corticosteroids during pregnancy (adrenal insufficiency may develop in the fetus and newborn). Should not be used frequently, in large doses, over a long period of time.

Category of action on the fetus according to the FDA -

Breastfeeding women are advised to stop either breastfeeding or the use of drugs, especially in high doses (corticosteroids pass into breast milk and can inhibit the production of endogenous corticosteroids, suppress growth and cause undesirable effects in offspring).

Overdose

Symptoms:

edema, the appearance of protein in the urine, decreased filtration volume, arterial hypertension, arrhythmias, cardiopathy, hypokalemia. Repeated frequent use of the drug (daily or several times a week) for a long time can lead to the development of Cushing's syndrome (requiring the need to stop taking the drug).

Treatment:

forced diuresis, potassium chloride, for depression and psychosis - dose reduction or discontinuation of the drug and the prescription of phenothiazine drugs or lithium salts (tricyclic antidepressants are not recommended).

Use of the drug Methylprednisolone-fs

Inside. Doses are selected individually depending on the severity of the disease, the patient's response and the expected duration of treatment. As a rule, it is necessary to take the drug in a high initial dose for several days, which, depending on the disease, can be 4–48 mg/day. In mild cases, low doses are sufficient. High initial doses of the drug may be necessary for multiple sclerosis (200 mg/day), cerebral edema (200–1000 mg/day), organ transplantation (up to 7 mg/kg/day). If there is no clinical effect with adequate treatment, methylprednisolone should be gradually discontinued and other drugs prescribed. After achieving a therapeutic effect, it is necessary to determine an adequate dose of the drug for maintenance treatment. For this purpose, the initial dose is reduced at short intervals to the minimum level at which a satisfactory clinical effect is maintained. As a result (depending on the severity of symptoms), it is necessary to achieve a minimum maintenance dose of 4–12 mg of Methylprednisolone-FS per day. In the treatment of asthma and COPD, methylprednisolone is initially prescribed at a dose of 32–40 mg/day. Then every 4 days the dose is reduced by 8 mg. After 3–4 weeks of treatment, the tablets are stopped or switched to inhaled corticosteroids. In severe forms of asthma, long-term therapy, the minimum dose of Methylprednisolone-FS is 4–8 mg/day. When prescribing a dosage regimen, circadian rhythms should be observed; alternating therapy is impossible in most cases. In the presence of night and morning attacks, the daily dose can be divided into two doses: 2/3 dose in the morning and 1/3 dose in the evening (between 18:00 and 20:00). For acute alveolitis, the initial dose for administration in the 1st week is 32–40 mg/day (in 1–2 doses). Then the dose is gradually reduced to a once daily dose. For pulmonary fibrosis, the initial dose is 24–32 mg/day in combination with azathioprine or penicillamine. Then the dose is gradually reduced to a level that is determined individually: 4–8 mg/day. For sarcoidosis, the initial dose is 32–40 mg/day in 2 doses, then switch to a single dose of the drug and gradually reduce the dose over 4–6 weeks. For hay fever and allergic rhinitis, Methylprednisolone-FS is used in addition to therapy with antihistamines and local antiallergic drugs if they are insufficiently effective and there is a risk of damage to the respiratory tract. In these cases, Methylprednisolone-FS is usually used at an initial dose of 16 mg/day for the first 4 days, then over the next 4 days the dose is reduced to 8 mg/day. The drug is stopped after 8 days. If the achieved effect is insufficient, you can continue taking the drug for up to 2-3 weeks at a daily dose of 4-8 mg. For skin diseases, the initial dose of Methylprednisolone-FS can be 80–160 mg/day, depending on the severity and form of the disease. Subsequently, the dose is quickly reduced so that the total duration of treatment does not exceed 2–4 weeks. Only in some cases, the drug can be extended to several months. When treating autoimmune diseases, depending on the severity and form, the initial dose is 40–60 mg/day. Then the dose is reduced to a maintenance dose, which may be necessary for several years. In case of acute forms, high-dose pulse therapy is possible. For rheumatic joint damage, the initial dose of Methylprednisolone-FS is 16–24 mg/day. For visceral rheumatism - up to 60 mg/day. Then the dose is gradually reduced, reaching a maintenance dose of no more than 8 mg/day. For autoimmune hemolytic anemia, the initial dose of Methylprednisolone-FS is 80–160 mg/day. When the effect is achieved (usually within 2 weeks from the start of administration), the dose is gradually reduced to a maintenance dose. For ulcerative colitis and Crohn's disease, the initial dose of Methylprednisolone-FS is 40–80 mg/day. Then the dose is gradually reduced. For ulcerative colitis, therapy must be completed as quickly as possible. If Crohn's disease requires longer therapy, you should switch to alternative therapy. In the case of replacement therapy for adrenal insufficiency, Methylprednisolone-FS is used at a dose of 4–8 mg/day. If necessary, combine with mineralocorticoid preparations.