Medomob - instructions for use, doses, side effects, contraindications

Active substance:
prednisolone sodium phosphate in terms of prednisolone phosphate	30 mg
Excipients:
nicotinamide	25.0 mg
phenol	5.0 mg
disodium edetate	0.5 mg
sodium disulfite	0.9 mg
sodium hydroxide	0.25-0.35 mg
water for injections	up to 1.0 ml

Description:

Transparent, colorless or with a yellowish tinge solution.

Pharmacotherapeutic group:Glucocorticosteroid

ATX: & nbsp

H.02.A.B.06 Prednisolone

Pharmacodynamics:

Prednisolone is a synthetic glucocorticosteroid drug, a dehydrated analog of hydrocortisone. Has anti-inflammatory, antiallergic, immunosuppressive, anti-shock effect, increases the sensitivity of beta-adrenoreceptors to endogenous catecholamines.

Interacts with the cytoplasmic receptors of glucocorticosteroids (GCS) to form a complex that induces the formation of proteins (including enzymes that regulate vital processes in cells).

Anti-inflammatory effect is associated with the suppression of the release of eosinophils and mast cells by inflammatory mediators; inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in the permeability of capillaries, stabilization of cell membranes (especially lysosomal) and membranes of organelles. Acts on all stages of the inflammatory process: inhibits the synthesis of prostaglandins at the level of arachidonic acid (lipocortin depresses phospholipase A2_, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, promoting inflammation processes, allergies, etc.), the synthesis of "pro-inflammatory cytokines" (interleukin-1, tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors.

Protein metabolism: reduces the number of globulins in plasma, increases the synthesis of albumin in the liver and kidneys (with increasing albumin / globulin ratio), reduces synthesis and enhances protein catabolism in muscle tissue.

Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (mobilization from the subcutaneous tissue of the extremities and accumulation of fat mainly in the region of the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.

Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract (GIT); increases the activity of glucose-6-phosphatase (increased intake of glucose from the liver into the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); promotes the development of hyperglycemia.

Water-electrolyte exchange: retards sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, causes the calcium to "wash out" of the bones and increases its renal excretion, reduces the mineralization of bone tissue.

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

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

In obstructive airway diseases the effect is mainly due to the inhibition of inflammatory processes, the prevention or reduction of the manifestation of the edema of the bronchial mucous membranes, the decrease in the eosinophilic infiltration of the submucosal layer of the bronchial epithelium and the deposition of circulating immune complexes in the bronchial mucosa, as well as the inhibition of erosion and desquamation of the mucosa. Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchial tubes to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production. It inhibits the synthesis and secretion of adrenocorticotropic hormone (ACTH), and a second synthesis of endogenous corticosteroids. It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

Pharmacokinetics:

With intravenous administration, the maximum concentration is reached after 0.5 hours, the half-life of the drug from the plasma is about 3 hours.

With intramuscular injection, the maximum concentration is reached after 0.5-1 h.

Absorption when injected into the muscles of the thigh is faster than when injected into the gluteal muscles.Up to 90% of the drug binds to plasma proteins: transcortin (corticosteroid-binding globulin) and albumins. Prednisolone metabolized in the liver, partially in the kidneys and other tissues, mainly by conjugation with glucuronic and sulfuric acids. Metabolites are inactive.

It is excreted through the intestine and kidneys by glomerular filtration and is reabsorbed by tubules by 80-90%. 20% of the dose is excreted by the kidneys unchanged.

Indications:

Meдопред® is used for emergency therapy in conditions requiring fastness of increasing the concentration of GCS in the body:

- shock (burn, traumatic, operational, toxic, anaphylactic, hemotransfusion) - with ineffectiveness of vasoconstrictors, plasma-substituting drugs and other symptomatic therapy;

- allergic reactions (acute severe forms): allergy, anaphylactoid reactions, serum sickness;

- respiratory diseases: bronchial asthma (severe form), asthmatic status;

- brain edema (including on the background of a brain tumor or associated with surgery, radiation therapy, or head injury);

- systemic connective tissue diseases: rheumatoid arthritis, systemic lupus erythematosus;

- liver disease: acute hepatitis, hepatic coma;

- endocrine disorders: primary or secondary adrenal insufficiency.

- thyrotoxic crisis;

- Others: reduction of inflammatory phenomena and prevention of cicatricial narrowing (with poisoning with cauterizing fluids).

Contraindications:

Hypersensitivity to prednisolone or the components of the drug. Do not apply during immunization with live vaccine and in cases of eye infection caused by the herpes simplex virus (due to the risk of perforation).

In children during the period of GKO growth, they should be used only under absolute indications under especially careful supervision of the attending physician.

Carefully:

With caution, the drug should be administered in the following conditions and conditions:

- Diseases of the gastrointestinal tract: peptic ulcer of the stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created anastomosis of the intestine, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis;

- parasitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently transferred, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles; amebiasis, stenpyloidosis; systemic mycosis; active or latent tuberculosis.The use in severe infectious diseases is permissible only against the background of specific antimicrobial therapy;

- pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency conditions (including AIDS or HIV infection);

- diseases of the cardiovascular system, incl. recently suffered myocardial infarction (in patients with acute and subacute myocardial infarction, the spread of the necrosis foci, slowing the formation of scar tissue and, consequently, the rupture of the heart muscle), severe chronic heart failure, hypertension, hyperlipidemia;

- Endocrine diseases: diabetes mellitus (including a violation of glucose tolerance, hyperthyroidism, hypothyroidism, Itenko-Cushing's disease, obesity (III-IV st);

- severe chronic renal and / or hepatic insufficiency, nephrourolythiasis. Hypoalbuminemia and conditions predisposing to its occurrence (cirrhosis of the liver, nephrotic syndrome);

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

- Pregnancy.

Pregnancy and lactation:

During pregnancy, the drug is used only if the potential benefit to the mother exceeds the potential risk to the fetus. With prolonged therapy during pregnancy, it is possible to not overgrow the upper palate, impaired fetal growth.

Since GCS penetrates into breast milk, if it is necessary to use the drug during breastfeeding, it is recommended to stop breastfeeding.

Dosing and Administration:

Medopred® is administered intravenously (by drip or jet) or by intramuscular injection. Intravenously, the drug is usually injected first with a stream, then drip. The dose of the drug and the duration of treatment is determined by the doctor individually, depending on the indications and severity of the disease.

In acute adrenal insufficiency a single dose of the drug is 100-200 mg, daily 300-400 mg.

In severe allergic reactions Medopred® is administered in a daily dose of 100-200 mg and for 3-16 days.

With bronchial asthma the drug is administered depending on the severity of the disease and the effectiveness of complex treatment from 75 to 675 mg for a course of treatment from 3 to 16 days; severe cases, the dose can be increased to 1,400 mg per treatment course and more with a gradual dose reduction.

With asthmatic status Medopred® is administered at a dose of 500-1200 mg per day, followed by a decrease to 300 mg per day and transition to maintenance doses.

With thyrotoxic crisis Introduce 100 mg of the drug in a daily dose of 200-300 mg; if necessary, the daily dose can be increased to 1000 mg. The duration of administration depends on the therapeutic effect, usually up to 6 days.

In shock, resistant to standard therapy, Medopred® at the beginning of the therapy is usually injected in a jet, and then they go on to the drip introduction. If the arterial pressure does not increase within 10-20 minutes, repeat the fluid administration of the drug. After excretion from the shock state, drip administration continues until blood pressure stabilizes. Single dose is 50-150 mg (in severe cases - up to 400 mg). Repeated drug is administered after 3-4 hours. The daily dose can be 300 to 1200 mg (with a subsequent dose reduction).

In acute hepatic-renal insufficiency (for acute poisoning, postoperative and postpartum periods, etc.) Medopred® is administered at a dose of 25-75 mg per day; in the presence of indications, the daily dose can be increased to 300-1500 mg per day or more.

With rheumatoid arthritis and systemic lupus erythematosus Medopred® is administered in addition to the systemic administration of the drug at a dose of 75-125 mg per day for not more than 7-10 days.

With acute hepatitis Medopred® is administered at 75-100 mg per day for 7-10 days.

When poisoning with cauterizing liquids with burns of the digestive tract and upper respiratory tract Medopred® is prescribed in a dose of 75-400 mg per day for 3-18 days.

If intravenous administration is not possible, Medopred® is administered intramuscularly in the same doses.

After relief of acute condition is prescribed inside prednisolone in tablets, followed by a gradual decrease in the dose.

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

Side effects:

The frequency of development and severity of side effects depend on the duration of the application, the amount of dose used, and the possibility of observing the circadian rhythm of Medopre®.

When applying Medopred ® can be noted:

From the endocrine system: a decrease in glucose tolerance, "steroid" diabetes mellitus or manifestation of latent diabetes mellitus, oppression of adrenal function,Itenko-Cushing syndrome (lunar face, obesity of the pituitary type, hirsutism, increase of arterial pressure, dysmenorrhea, amenorrhea, muscle weakness, striae), delay in sexual development in children.

From the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding and perforation of the gastrointestinal wall, increase or decrease in appetite, digestive disorders, flatulence, hiccups. In rare cases - increased activity of "liver" transaminases and alkaline phosphatase.

From the side of the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of 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 the focus of necrosis, slowing the formation of scar tissue, which can lead to rupture of the heart muscle.

From the nervous system: delirium, disorientation, euphoria, hallucinations,manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor, cerebral palsy, headache, convulsions.

From the 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 corneal changes, exophthalmos, sudden loss of vision (with parenteral administration in the head, neck, nasal concha, scalp possibly deposition of the crystal in the drug in the vessels of the eye).

From the side of metabolism: increased excretion of calcium, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating.

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

From the side of the musculoskeletal system: slowing growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and thigh bone), rupture of the tendons of the muscles, steroid myopathy, muscle loss (atrophy).

From the skin and mucous membranes: delayed healing of wounds, pecesh, ecchymosis, thinning of the skin, hyper- or hypopigmentation, "steroid" acne, shearing, tendency to develop pyoderma and candidiasis.

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

Local for parenteral administration: burning, numbness, pain, tingling at the injection site, infections at the injection site, rarely - necrosis of surrounding tissues, scar formation at the injection site; atrophy of the skin and subcutaneous tissue with the / m introduction (especially dangerous is the introduction to the deltoid muscle).

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

Overdose:

It is possible to enhance the dose-dependent side effects described above.

Treatment: symptomatic. It is necessary to reduce the dose of Medopred®.

Interaction:

The pharmaceutical incompatibility of prednisolone with other intravenously administered drugs is possible - it is recommended to administer it separately from other drugs (iv bolus, or through another dropper, as a second solution).

When mixing the solution of prednisolone with heparin a precipitate forms.

Prednisolone with prolonged therapy can increase the content of folic acid.

The simultaneous administration of prednisolone with:

- inducers of microsomal liver enzymes (phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration;

- Diuretics (especially "thiazide" and inhibitors of carbonic anhydrase) and amphotericin B can lead to increased excretion of potassium from the body and an increased risk of developing heart failure;

- Sodium-containing drugs can lead to the development of edema and increased blood pressure;

- cardiac glycosides - their tolerance is worsened and the likelihood of developing ventricular extrasystole (due to thehypokalemia);

- indirect anticoagulants - weakens (less intensifies) their effect (dose adjustment is required);

- anticoagulants and thrombolytic - increases the risk of bleeding from gastrointestinal ulcers;

- ethanol and nonsteroidal anti-inflammatory drugs (NSAIDs) - the risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding increases (in combination with NSAIDs in the treatment of arthritis, there may be a decrease in the dose of GCS due to the summation of the therapeutic effect);

- paracetamol - the risk of hepatotoxicity increases (induction of hepatic enzymes and the formation of a toxic metabolite of paracetamol);

- Acetylsalicylic acid - accelerates its elimination and reduces the concentration in the blood (with the withdrawal of prednisolone, the concentration of salicylates in the blood increases and the risk of side effects increases);

- insulin and oral hypoglycemic drugs, hypotensive drugs - their effectiveness decreases;

- vitamin D - its effect on calcium absorption in the intestine decreases;

- a somatotropic hormone - reduces the effectiveness of the latter, and with praziquantel - its concentration in the blood;

- m-holinoblokatorami (including antihistamines and tricyclic antidepressants) and nitrates - promotes increased intraocular pressure;

- Tricyclic antidepressants - may increase the severity of depression caused by taking glucocorticosteroids (not shown for the therapy of these side effects);

- isoniazid and mexlegalom - increases their metabolism (especially in "slow" acetylators), which leads to a decrease in their plasma concentrations.

Inhibitors of carbonic anhydrase and looped diuretics can increase the risk of osteoporosis. Indomethacin, displacing prednisolone from association with albumin, increases the risk of developing its side effects.

ACTH increases the effect of prednisolone.

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

Cyclosporine and ketoconazole, slowing the metabolism of prednisolone, can in some cases increase its toxicity.

Simultaneous appointment of androgens and steroid anabolic drugs with prednisolone promotes the development of peripheral edema and hirsutism, the appearance of acne.

Estrogens and oral estrogen-containing contraceptives reduce the clearance of prednisolone, which may be accompanied by an increase in the severity of its action. With simultaneous use with live antiviral vaccines and against other types of immunization increases the risk of virus activation and the development of infections.

Antipsychotic drugs (antipsychotics) and azathioprine increase the risk of developing cataracts in the appointment of prednisolone.

Simultaneous administration of antacids reduces the absorption of prednisolone.

With simultaneous use with antithyroid drugs is reduced, and with thyroid hormones - increases the clearance of prednisolone. |

Hypokalemia caused by glucocorticosteroids may increase the severity and duration of muscle blockade against the background of muscle relaxants.

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

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

Special instructions:

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

Food should be rich in proteins, vitamins, with a restriction of fat, carbohydrates and table salt.

The effect of the drug is enhanced in patients with hypothyroidism and liver cirrhosis.

The drug may enhance existing emotional instability or psychotic disorders. When referring to a psychosis in an anamnesis, Medopred® in high doses is prescribed under the strict supervision of a physician.

In stressful situations during maintenance treatment (for example, surgical operations, trauma or infectious diseases), a correction of the dose of the drug should be made in response to an increase in the need for GCS.

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

During treatment with Medopred ® should not be vaccinated due to a decrease in its effectiveness (immune response).

When appointing Medopred® with intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously perform antibiotic treatment with bactericidal action.

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

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

Patients with diabetes should monitor blood glucose and, if necessary, correct therapy.

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

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

Medopred increases the content of metabolites of 11-and 17-oxyketocorticosteroids.

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

During treatment, patients are advised to exercise caution when driving vehicles and other potentially dangerous species activities that require increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Solution for intravenous and intramuscular injection, 30 mg / ml.

Packaging:

For 1.0 ml of the solution for intravenous and intramuscular injection into dark glass ampoules (class I) with a fault strip.

5 ampoules per contour cell box made of PVC with PVC coating.

2 contour squares with instructions for use in cardboard pack.

For 20 contour mesh packages with an equal number of instructions for use in cardboard pack (for hospitals).

Storage conditions:Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N012695 / 02

Date of registration:26.03.2012

Expiration Date:Unlimited

The owner of the registration certificate:Medocemi Co., Ltd.Medocemi Co., Ltd. Cyprus

Manufacturer: & nbsp

MEDOCHEMIE, Ltd. Cyprus

Representation: & nbspMEDOKEMI LTD. MEDOKEMI LTD. Cyprus

Information update date: & nbsp26.04.2018

Illustrated instructions

Instructions

Medopred® (Medopred®)