Prednisolone - instructions for use, dose, side effects, contraindications

Excipients: sodium hydrophosphate (sodium hydrophosphate anhydrous) 0.5 mg, sodium dihydrogen phosphate dihydrate 0.35 mg, propylene glycol 150 mg, water for injection up to 1 ml.

Description:

Transparent or slightly opalescent colorless or slightly colored liquid.

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, desensitizing, anti-shock, antitoxic and immunosuppressive action.

Suppresses the release of pituitary beta-lipotropin, but does not reduce the concentration of circulating beta-endorphin. Oppressing the secretion of thyroid-stimulating hormone (TSH) and follicle-stimulating hormone (FSH). Increases the excitability of the central nervous system (CNS), reduces the number of lymphocytes and eosinophils, increases erythrocytes (stimulates the production of erythropoietins).

Interacts with the cytoplasmic receptors of glucocorticosteroids (GSK) and forms a complex penetrating into the nucleus of the cell, and stimulates the synthesis of mRNA; the latter induces the formation of proteins, including lipocortin, that mediate cellular effects. Lipocortin depresses phospholipase A2, inhibits the release of arachidonic acid, and inhibits the synthesis of endoperoxides, prostaglandins (Pg), leukotrienes, contributing to the processes of inflammation, allergies and more.

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

Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat occurs mainly in the area of the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.

Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract; increases the activity of glucose-6-phosphatase (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 ions and water in the body, stimulates the excretion of potassium ions (mineralocorticoid activity), reduces the absorption of calcium ions from the gastrointestinal tract, reduces the mineralization of bone tissue.

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.

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, 2, gamma-interferon) from lymphocytes and macrophages and a decrease the formation of antibodies.

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

In obstructive airway diseases the effect is mainly due to the inhibition of inflammatory processes, the prevention or reduction of the degree of edema of the 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.

Suppresses the synthesis and secretion of adrenocorticotropic hormone and, secondarily, the synthesis of endogenous glucocorticosteroids.

Anti-shock and antitoxic action is associated with an increase in blood pressure (by increasing the concentration of circulating catecholamines and restoring the sensitivity of adrenoreceptors to them, as well as vasoconstriction), a decrease in the permeability of the vascular wall, membrane-protective properties, activation of liver enzymes involved in the metabolism of endo- and xenobiotics.

It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

Pharmacokinetics:

Up to 90% of prednisolone binds to plasma proteins: transcortin (corticosteroid-binding globulin) and albumins.

Prednisolone is 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 80-90% reabsorbed by tubules, 20% of the dose is excreted by the kidneys unchanged. The half-life from the plasma after intravenous administration is 2-3 hours.

Indications:

Prednisolone is swallowed for emergency therapy in conditions requiring a rapid increase in the concentration of glucocorticosteroids in the body:

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

- allergic reaction (acute severe), transfusion shock, anaphylactic shock, anaphylactoid reactions;

- cerebral edema (including on the background of a brain tumor or associated with surgical intervention, radiation therapy or head trauma);

- bronchial asthma (severe form), astatic status;

- systemic connective tissue diseases (systemic lupus erythematosus, rheumatoid arthritis);

- acute adrenal insufficiency;

- thyrotoxic crisis;

- acute hepatitis, hepatic coma;

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

Contraindications:

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

In children during growth, glucocorticosteroids should be used only in absolute indications and under the close supervision of the treating physician.

Carefully:

The drug should be prescribed in the following diseases and conditions:

- diseases of the gastrointestinal tract - peptic ulcer of the stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with perforation or abscessing, diverticulitis;

- parasitic and infectious diseases of viral,fungal or bacterial (currently or recently transferred, including recent contact with the patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles; amebiasis, strongyloidiasis; 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 states (including acquired immunodeficiency syndrome (AIDS) or human immunodeficiency virus (HIV infection);

- diseases of the cardiovascular system (including the recently transferred

myocardial infarction - in patients with acute and subacute myocardial infarction it is possible to spread the focus of necrosis, slow the formation of scar tissue and, as a result, break the heart muscle), decompensated chronic heart failure, arterial hypertension,

hyperlipidemia);

- endocrine diseases - diabetes mellitus (including impaired tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease,obesity III-IY stage);

- severe chronic renal and / or hepatic insufficiency,

nefroourolithiasis;

- hypoalbuminemia and conditions predisposing to its occurrence;

- 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.

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

Dosing and Administration:

Intravenously, the drug is usually injected first with a jet, repeated injections are performed by 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 adrenocortical insufficiency single dose of the drug is 100-200 mg, daily - 300-400 mg.

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

With bronchial asthma the drug is administered at a dose of 75 mg to 675 mg for a course of treatment of 3 to 16 days; in severe cases, the dose may be increased to 1,400 mg per treatment course and more with a gradual dose reduction.

With asthmatic status prednisolone injected at a dose of 500-1200 mg per day, followed by a decrease to 300 mg per day and the transition to maintenance doses.

With thyrotoxic crisis 100 mg of the drug are administered 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, prednisolone At the beginning of therapy, injections are usually given, after which they pass to a 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 300-1200 mg (with a subsequent dose reduction).

In acute liver-kidney failure (acute poisoning, postoperative and postpartum periods, etc.) prednisolone administered at 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 prednisolone In addition to the systemic administration of the drug in a dose of 75-125 mg per day, not more than 7-10 days.

With acute hepatitis prednisolone Enter 75-100 mg per day for 7-10 days. When poisoning with cauterizing liquids with burns of the digestive tract and upper respiratory tract - prescribe a dose of 75-400 mg per day for 3-18 days.

If intravenous injection is not possible prednisolone 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!

Children from 2 to 12 months - 2-3 mg / kg, from 1 to 14 years - 1-2 mg / kg intramuscularly; intravenously injected slowly (within 3 minutes). If necessary, this dose can be repeated after 20-30 minutes.

Side effects:

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

From the endocrine system: 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 in blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae), delay 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, increased or decreased appetite, digestive disorders, flatulence, hiccups. In rare cases - increased activity of "liver" transaminases and alkaline phosphatase.

From 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, tendency to develop secondary bacterial, fungal or viral eye infections, trophic corneal changes, exophthalmos, sudden loss of vision.

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

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

From the musculoskeletal system: slowing the growth and processes of ossification 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 muscle tendons, steroid myopathy, muscle loss (atrophy).

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

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

Local reactions with 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 intramuscular injection (especially dangerous is the introduction to the deltoid muscle).

With intravenous administration: arrhythmias, "tides" of blood to the face, seizures.

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 increase dose-dependent side effects. It is necessary to reduce the dose of prednisolone.

Treatment: symptomatic.

Interaction:

Possible pharmaceutical incompatibility of prednisolone with other intravenously administered drugs - it is recommended to inject it separately from other drugs (intravenously bolus, or through another dropper, as a second solution). When mixing the solution of prednisolone with heparin a precipitate forms.

Prednisolone increases the toxicity of cardiac glycosides (because of the resulting hypokalemia, the risk of arrhythmias increases).

Accelerates the removal of acetylsalicylic acid, reduces its concentration in the blood (with the abolition of prednisolone, the concentration of salicylates in the blood increases and the risk of side effects increases).

With simultaneous use with live antiviral vaccines and against other types of immunizations, increases the risk of virus activation and the development of infections.

Increases the metabolism of isoniazid, mexiletine (especially in "fast acetylators"), which leads to a decrease in their plasma concentrations.

Increases the risk of hepatotoxic reactions of paracetamol (induction of "hepatic" enzymes and the formation of a toxic metabolite of paracetamol).

Increases (with prolonged therapy) the content of folic acid. Hypokalemia caused by glucocorticosteroids may increase the severity and duration of muscle blockade against the background of muscle relaxants.

In high doses reduces the effect of somatropin.

Prednisolone reduces the effect of hypoglycemic drugs; enhances the anticoagulant effect of coumarin derivatives.

Weaken the influence of vitamin D on the absorption of calcium ions in the lumen of the intestine.

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

Reduces the concentration of praziquantel in the blood.

Cyclosporine (inhibits metabolism) and ketoconazole (reduces clearance) increase toxicity.

Thiazide diuretics, carbonic anhydrase inhibitors, other glucocorticosteroids and amphotericin B increase the risk of hypokalemia,sodium-containing medicines-edema and increased blood pressure.

Non-steroidal anti-inflammatory drugs (NSAIDs) and ethanol increase the risk of ulceration of the gastrointestinal tract (GI) mucosa and bleeding, in combination with non-steroidal anti-inflammatory drugs (NSAIDs), a reduction in the dose of glucocorticosteroids due to the summation of the therapeutic effect is possible for the treatment of arthritis.

Indomethacin, displacing prednisolone from association with albumin, increases the risk of developing its side effects.

Amphotericin B and carbonic anhydrase inhibitors increase the risk of osteoporosis.

The therapeutic effect of glucocorticosteroids decreases under the influence of phenytoin, barbiturates, ephedrine, theophylline, rifampicin, and other inductors of microsomal liver enzymes (an increase in metabolic rate).

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

The clearance of glucocorticosteroids rises against the background of thyroid hormones.

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

Estrogens (including oral estrogen-containing contraceptives) reduce the clearance of glucocorticosteroids, prolong the half-life and their therapeutic and toxic effects.

The emergence of hirsutism and acne is facilitated by the simultaneous use of other steroid hormonal drugs - androgens, estrogens, anabolic, oral contraceptives.

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

The risk of developing cataracts increases with other glucocorticosteroids, antipsychotic drugs (neuroleptics), carbutamide and azathioprine.

Simultaneous administration with m-holinoblokatorami (including antihistamines, tricyclic antidepressants with m-holinoblokiruyuschey activity), nitrates contributes to the development of increased intraocular pressure.

Special instructions:

During treatment with prednisolone (especially long-term) it is necessary to observe the oculist, control blood pressure, condition of water-electrolyte balance, as well as pictures of peripheral blood and blood glucose level.

In order to reduce side effects, it is possible to prescribe antacids, and also to increase the intake of potassium ions into the body (diet, potassium preparations). 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 prednisolone in high doses prescribed under the strict supervision of a doctor.

With caution should be used in acute and subacute myocardial infarction - possibly spreading the focus of necrosis, slowing the formation of scar tissue and rupture of the heart muscle.

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 connection with an increase in the need for glucocorticosteroids.

In case of sudden cancellation, especially in case of prior application of high doses, it is possible to develop the "withdrawal" syndrome (anorexia, nausea, block, generalized musculoskeletal pain, general weakness), as well as an exacerbation of the disease for which it was prescribed prednisolone. During treatment with prednisolone, vaccination should not be given due to a decrease in its effectiveness (immune response). Assigning prednisolone with intercurrent infections, septic states and tuberculosis, it is necessary to simultaneously perform antibiotic treatment of bactericidal action.

In children during growth, glucocorticosteroids should be used only in absolute indications and under the close supervision of the treating physician. Children who were in contact with sick measles or chickenpox during the treatment period prophylactically prescribe specific immunoglobulins.

Due to a weak mineralocorticoid effect for replacement therapy with adrenal insufficiency prednisolone 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.

Prednisolone in patients with latent infectious diseases of the kidneys and urinary tract can cause leukocyturia, which can have diagnostic value.

Prednisolone increases the metabolites of 11- and 17-oxyketocorticosteroids.

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

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection, 30 mg / ml.

Packaging:

1 ml of solution in neutral glass ampoules.

For 10 ampoules with instruction for use and a knife for opening ampoules or a scarifier ampullum is placed in a box of cardboard.

5 or 10 ampoules are placed in a contoured cell pack of a polyvinylchloride film or polyethylene terephthalate tape and aluminum foil or paper with a polyethylene coating or without a foil, or without paper.

For 1 or 2 contour packs with instructions for use and a knife for opening ampoules or a scarifier ampullum is placed in a pack of cardboard.

When you pack the ampoules with a break ring or break point, the ampoule opener or ampoule scapper is not put in.

Storage conditions:

In the dark place at a temperature of no higher than 15 ° C.

Keep out of the reach of children.

Shelf life:

1 year.

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

Terms of leave from pharmacies:On prescription

Registration number:LS-001789

Date of registration:22.12.2011

The owner of the registration certificate:NOVOSIBHIMFARM, OJSC NOVOSIBHIMFARM, OJSC Russia

Manufacturer: & nbsp

NOVOSIBHIMFARM, OJSC Russia

Representation: & nbspNOVOSIBHIMFARM, OJSCNOVOSIBHIMFARM, OJSC

Information update date: & nbsp28.08.2015

Illustrated instructions

Instructions

Prednisolone (Prednisolon)