Index of drugs

Acute life-threatening conditions, such as anaphylactic shock (after the first injection of adrenaline); cerebral edema (only in the case of intracranial pressure symptoms confirmed in computed tomography) caused by a brain tumor, neurosurgical procedures, brain abscess, bacterial meningitis; persistent shock lung (acute adult respiratory distress syndrome) after the acute phase; severe acute asthma attack; Waterhouse and Friderichsen syndrome; immunological fractures after organ transplantation; toxic pulmonary edema caused by inhalation of irritating gas. In these indications, the drug is used in conjunction with appropriate primary care (e.g., replenishment of fluids, treatment of cardiovascular disorders, administration of antibiotics, pain treatment, etc.). In the therapy of Waterhouse and Friderichsen syndrome, simultaneous administration of mineralocorticosteroids is indicated. The drug can also be used in short-term treatment in MS exacerbations - it can shorten the duration of exacerbations, but does not affect the frequency of their occurrence or the progress of loss of fitness.

One vial of powder contains 33848 mg or 1325.92 mg of methylprednisolone as succinate sodium, equivalent to 250 mg or 1000 mg of methylprednisolone. The medicine contains sodium (a vial of 250 mg contains less than 23 mg of sodium, a vial of 1000 mg contains less than 67.6 mg of sodium).

Nonfluorinated glucocorticosteroid for systemic treatment. Depending on the dose, methylprednisolone has an effect on the metabolism of almost all tissues, which is essential for maintaining the homeostasis of the body at rest and during exercise, as well as in regulating the activity of the immune system. In the case of underdevelopment or adrenocortical insufficiency, methylprednisolone administered in physiological doses can replace endogenous hydrocortisone. In this situation, it affects the metabolism of carbohydrates, proteins and fats in metabolic balance. In terms of dose and effect, 8 mg of methylprednisolone is equivalent to 40 mg of hydrocortisone. Methylprednisolone has practically no mineralocorticotropic activity, therefore in the case of underdevelopment of the adrenal cortex, additionally mineralocorticoid should be administered during substitution treatment. At doses greater than those required for substitution therapy, methylprednisolone has a rapid anti-inflammatory effect (anti-exudative and antiproliferative) and has a delayed immunosuppressive effect. It includes the inhibition of chemotaxis, the activity of cells of the immune system, as well as the release and action of mediators of inflammatory and immune reactions, e.g. lysosomal enzymes, prostaglandins and leukotrienes. After intravenous injection, methylprednisolone is rapidly released from the ester, some of it is immediately available biologically. T_0,5 is 2-3 hours. Regardless of the dose, 77% is bound to proteins, exclusively with albumin. It is metabolised mainly in the liver, metabolites are hormonally inactive and are excreted by the kidneys. The duration of action of methylprednisolone persists longer than the time of presence in the blood serum. In the range of medium doses, it ranges from 12 to 36 hours.

Hypersensitivity to methylprednisolone as sodium succinate, other glucocorticoids or to any of the excipients.

In cases of severe infections, drug administration is indicated only with the simultaneous use of specific antimicrobial therapy. Treatment should only be started after careful benefit and risk analysis and, if necessary, with targeted antimicrobial therapy in the following diseases: acute viral infections (e.g. shingles, herpes, chickenpox, herpetic keratitis); chronic active hepatitis with a positive HBsAg test; about 8 weeks before and up to 2 weeks after vaccination with live vaccines; systemic fungal infections and parasitic infections (eg, amebiosis, nematode infections); Heine-Medina disease; involvement of lymph nodes after vaccination against tuberculosis; acute and chronic bacterial infections; tuberculosis in a history of the drug (the drug may be used only simultaneously with medicines to protect against tuberculosis and under close clinical supervision).In addition, in the following cases, treatment should only be started after a careful benefit and risk analysis and, if necessary, with appropriate treatment: gastric and intestinal ulceration; severe osteoporosis; hypertension difficult to compensate; diabetes difficult to compensate; mental illness (also in an interview); narrow-angle glaucoma and open-angle glaucoma; ulcers and corneal damage. Due to the risk of intestinal perforation with peritonitis, the drug can only be used after careful benefit and risk analysis and under strict control in the following cases: severe ulcerative colitis with the risk of perforation, with abscesses or purulent inflammations; diverticulitis; fistulas between the intestines (immediately after surgery). Patients receiving high-dose glucocorticosteroids may not exhibit signs of peritoneal irritation after gastrointestinal perforation. During treatment, metabolic changes should be regularly monitored in diabetic patients (a higher dose of insulin or oral hypoglycemic agents may be required), blood pressure in hypertensive patients, and the patient's condition in patients with severe heart failure (risk of worsening this condition). Drug therapy may mask the symptoms of a concomitant or developing infection, and thus make recognition difficult. Due to the immunosuppressive effect, treatment with glucocorticosteroids may lead to an increased risk of infection with pathogens that in other circumstances rarely cause infection. In principle, vaccination with inactivated vaccines is possible, however, it should be taken into account that the immune response, and thus the effectiveness of vaccination, can be reduced when using higher doses of corticosteroids. Therefore, vaccination is not indicated in patients receiving maintenance therapy with higher doses (with the exception of substitution treatment). If high doses are administered, sufficient potassium intake and limited sodium intake should be ensured and serum potassium levels monitored. Some viral diseases (chicken pox, measles) can be particularly severe, and in some cases even life-threatening, in patients treated with glucocorticosteroids. The risk applies especially to children with immunosuppression and patients who have not had history of chickenpox and measles. If these patients are in contact with those with measles, chickenpox or shingles during drug therapy, preventive treatment should be given as appropriate. In children, the drug should only be used after careful consideration of the benefit / risk ratio, as methylprednisolone may inhibit growth - the child's growth should be monitored regularly. During long-term treatment with glucocorticosteroids, regular medical check-ups (including eye tests every three months) are recommended. In special stress situations (febrile illness, accident, surgery, childbirth, etc.) during therapy with glucocorticosteroids, a transient dose increase may be required. Depending on the duration and dosage of the drug, an adverse effect on Calcium metabolism can be expected, therefore prevention of osteoporosis is recommended; this applies especially to patients with coexistence of risk factors such as family burden, older age, post menopausal period, insufficient intake of protein and Calcium, smoking, excessive alcohol consumption and lack of physical exercise - prevention includes sufficient intake of calcium and vitamin D, and Physical effort, and in the case of coexistence of osteoporosis, an additional drug should be considered. After the end or long-term treatment, the following risks should be considered: severity or recurrence of the underlying disease, acute adrenal insufficiency (especially in stress situations, eg during infections, after accidents, during severe physical stress), withdrawal syndrome after discontinuation of Cortisone . In cases of hypothyroidism or cirrhosis, relatively small doses may be sufficient or a dose reduction may be necessary; strict medical supervision should be ensured. Pulmonary arrhythmia and / or circulatory collapse and / or cardiac arrest have been reported after initiating pulse therapy with high doses of methylprednisolone (> 500 mg) administered intravenously, even in patients who have not been diagnosed with heart disease - close medical supervision is recommended. treatment and for a few days after the end of therapy. In the short-term treatment of multiple sclerosis exacerbations, infections should be ruled out before commencing infusion administration, and the use of the drug should be carefully evaluated for benefit and risk. The 250 mg dose contains less than 1 mmol (23 mg) sodium per one vial, which means that it is essentially 'sodium-free'.In contrast, the 1,000 mg dose contains 2.9 mmol (67.6 mg) sodium - this should be taken into account in patients who are on a controlled sodium diet.

During pregnancy, especially in the first trimester, treatment should be started after a careful assessment of the risk / benefit ratio. Data regarding the safety of methylprednisolone during pregnancy are insufficient. In animal studies, methylprednisolone caused the cleft of the palate. The possibility of increasing the risk of developing fission in human fetuses due to the administration of glucocorticoids during the first trimester of pregnancy is being considered. In the case of long-term treatment, disturbances of intrauterine growth can not be ruled out. Treatment at the end of pregnancy may lead to adrenal fetal atrophy, which in turn may require substitution treatment with gradual dose reduction in newborns. Glucocorticoids penetrate into human milk in small amounts. Normally, the newborn's exposure corresponds to less than one-hundredth of the systemic circulation in the breast-feeding mother. Greater breast-feeding should be avoided when taking higher doses or long-term treatment.

Depending on the duration of the treatment and the dose, the following side effects may occur: leukocytosis (initially reversible in the course of treatment), lymphopenia, eosinopenia, polycythemia, propensity to thrombocytosis; severe anaphylactic reactions with cardiac collapse, cardiac arrest, cardiac arrhythmias, bronchospasm and / or decrease / increase in blood pressure; weakened immune defenses with an increased risk of infection (some viral diseases such as chickenpox, herpes or - during viraemia - shingles, can have a severe course, even leading to death); masking of infections, revealing latent infections, allergic reactions; suppression of adrenal function and induction of Cushing's syndrome, inhibition of children's growth, sex hormone secretion disorders (amenorrhea, hirsutism, erectile dysfunction), reversible epidermal, epicardial or mediastinal lipopathology; sodium retention accompanied by edema, increased potassium excretion, which may be accompanied by hypokalaemia (attention should be paid to the risk of arrhythmias), decreased Glucose tolerance, diabetes mellitus, hypercholesterolemia and hypertriglyceridemia, increased protein degradation; severe depression, irritability, personality changes, mood changes, euphoria, increased motivation and appetite, psychosis, sleep disorders; alleged brain tumor (especially in children), the appearance of symptoms of hidden epilepsy and increased propensity to convulsions in epilepsy with symptoms, dizziness, headaches; cataract (especially subcapsular posterior cataract), glaucoma, worsening of corneal ulcer symptoms, exacerbation of viral, fungal and bacterial ocular inflammations; arrhythmias, cardiac arrest, worsening lung stagnation in the course of left ventricular failure; vascular collapse, hypertension, increased risk of atherosclerosis and thrombosis, vasculitis (also as a withdrawal syndrome after long-term treatment); stomach and intestinal ulcers with a risk of perforation (for example with peritonitis), bleeding from the stomach or intestines, pancreatitis, epigastric disorders; red stretch marks, atrophy, telangiectasia, increased capillary fragility, ecchymosis, cutaneous bleeding in a certain area, blood haemorrhage, hypertrichosis, steroid acne, delayed wound healing, dermatitis (around the mouth) similar to rosacea, skin pigmentation changes, reactions hypersensitivity such as drug induced rashes; muscle weakness and weakness, in the case of myasthenia, a reversible increase in muscle weakness resulting in myasthenic crisis, induction of acute myopathy in the case of non-depolarising skeletal muscle relaxants, osteoporosis (dose-dependent, also possible during short-term use), in severe cases leading to fracture risk bones, barren bone necks (the head of the humerus and femoral head), rupture of the tendon; too rapid dose reduction after long-term treatment may cause discomfort, such as muscle and joint pain; injection into adipose tissue may cause local loss of body fat; weight gain.

Intravenously.At the beginning of treatment, depending on the indication and the clinical situation, the single dose in the therapy of acute life-threatening conditions is 250-1000 mg of methylprednisolone and above in adults and 4-20 mg / kg. in children. In some indications (eg immunologic breakthroughs of graft rejection), dosages up to 30 mg / kg are recommended. Depending on the condition, the injection interval ranges from 30 minutes to 24 hours.
Anaphylactic shock250-500 mg in combination with the usual primary therapy / medicines used simultaneously.Severe acute asthma attack250-500 mg in combination with the usual primary therapy / medicines used simultaneously.Brain edema (caused by a brain tumor, neurosurgical procedures, brain abscess, bacterial meningitis): in the treatment of acute or severe cerebral edema, 250-500 mg are administered initially, in acute or severe brain edema therapy or mild or chronic cerebral edema, generally administered 32-64 mg 3 times daily for several days; if necessary, gradually reduce the dose and switch to oral treatment.Immune fractures after organ transplantation: inject the dose up to 30 mg / kg, once (in an adult of 60-70 kg, this dose corresponds to 1-2 vials at a dose of 1000 mg), combined with the usual basic therapy, for a few days.Waterhouse and Friderichsen team: initially 30 mg / kg, administration is repeated in 4-6 doses for 24-72 h, in combination with intensive primary treatment.Shocking Lung (Adult Respiratory Distress Syndrome, ARDS): after an acute phase of persistent ARDS, doses of 1-2 mg / kg / day are administered in 4 divided doses up to a dose of 250 mg methylprednisolone every 6 hours, for several days to weeks, with a gradual decrease in dose, depending on the course of diseases.Toxic pulmonary edema caused by inhalation of an irritant gas: Immediately inject 1000 mg intravenously, if necessary, repeat after 6, 12 and 24 h. 32 mg methylprednisolone administered intravenously 3 times a day, in the Next 2 days. Subsequently, 16 mg of methylprednisolone intravenously, 3 times daily are administered for a further 2 days, then the dose is gradually reduced and it is switched to inhaled corticosteroids.Short-term treatment in exacerbations of multiple sclerosis: 1000 mg daily for 3 to a maximum of 5 consecutive days, treatment should begin within 3-5 days after the onset of clinical symptoms and also include gastric protection and antithrombotic prophylaxis; drug administered in the morning to reduce the likelihood of developing sleep disorders; after the end of intravenous therapy, a 14-day period of gradual dose reduction should be implemented, initially using 80 mg of methylprednisolone (or the equivalent dose) administered orally.
The duration of treatment depends on the individual clinical situation and usually lasts only a few days.
It is given by injection into a vein or intravenous infusion. Due to the uncertain conditions of absorption, intramuscular injection should be chosen only exceptionally, in cases where it is not possible to administer intravenously. Intravenous injection should be carried out slowly. Avoid administration together with other medicines mixed in the syringe.