Prednisolone application features. How to reduce the side effects of prednisolone. Special patient groups

Catad_pgroup Systemic corticosteroids

Prednisolone Nycomed - instructions for use

INSTRUCTIONS
on the medical use of the drug

(PREDNISOLONY NYCOMED)

Registration number

Tradename: Prednisolone Nycomed

International non-proprietary name:

Prednisolone

Chemical Name:(6 alpha, 11 beta)-11,17,21-Trihydroxypregna-1,4-diene-3,20-dione

Dosage form
Tablets; solution for intravenous and intramuscular administration.

Compound

1 tablet contains:
active substance- prednisolone 5 mg,
Excipients: magnesium stearate, talc, corn starch, lactose monohydrate.

1 ml of solution contains:
active substance- prednisolone 25 mg,
Excipients: glycerol formal, butanol, sodium chloride, water for injection.

Description
Tablets white, round, flat on both sides, with beveled edges, x notch for graduation on one side and engraving "PD" above the notch and "5.0" below the notch.
Solution- transparent colorless.

Pharmacotherapeutic group:

Glucocorticosteroid.

ATC Code: H02AB06.

Pharmacological properties
Pharmacodynamics.
Prednisolone Nycomed is a synthetic glucocorticosteroid drug, a dehydrated analogue of hydrocortisone. It has anti-inflammatory, anti-allergic, immunosuppressive effects, increases the sensitivity of beta-adrenergic receptors to endogenous catecholamines.
Interacts with specific cytoplasmic receptors (glucocorticosteroid (GCS) receptors are found in all tissues, especially in the liver) to form a complex that induces the formation of proteins (including enzymes that regulate vital processes in cells.)
Protein metabolism: reduces the amount of globulins in plasma, increases albumin synthesis in the liver and kidneys (with an increase in the 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 (accumulation of fat occurs mainly in 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); contributes to the development of hyperglycemia.
Water-electrolyte metabolism: retains sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, reduces the mineralization of bone tissue.
The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils and mast cells; inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes (especially lysosomal) and organelle membranes. It acts on all stages of the inflammatory process: it inhibits the synthesis of prostaglandins at the level of arachidonic acid (lipocortin inhibits phospholipase A2, inhibits the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, which contribute to inflammation, 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.
The immunosuppressive effect is caused by the involution of lymphoid tissue, inhibition of the proliferation of lymphocytes (especially T-lymphocytes), suppression of B-cell migration and the interaction of T- and B-lymphocytes, inhibition of the release of cytokines (interleukin-1, 2; interferon gamma) from lymphocytes and macrophages and decreased antibody production.
The antiallergic effect develops as a result of a decrease in the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, 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 allergy mediators, inhibition of antibody production, changes in the body's immune response.
In obstructive diseases of the respiratory tract, the action is mainly due to the inhibition of inflammatory processes, the prevention or decrease in the severity of edema of the mucous membranes, the decrease in eosinophilic infiltration of the submucosal layer of the bronchial epithelium and the deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucosa. Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.
Suppresses the synthesis and secretion of ACTH and secondarily - the synthesis of endogenous corticosteroids.
It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

Pharmacokinetics.
When taken orally, prednisolone is well absorbed from the gastrointestinal tract. The maximum concentration in the blood is reached 1-1.5 hours after oral administration. Up to 90% of the drug binds to plasma proteins: transcortin (cortisol-binding globulin) and albumin. Prednisolone is metabolized in the liver, partly in the kidneys and other tissues, mainly by conjugation with glucuronic and sulfuric acids. Metabolites are inactive.
It is excreted in bile and urine by glomerular filtration and is reabsorbed by tubules by 80-90%. 20% of the dose is excreted by the kidneys unchanged.
The plasma half-life after oral administration is 2-4 hours, after intravenous administration 2-3.5 hours.

Compound

active substance: 1 ml of the solution contains prednisototkg for prednisolone - 30 mg;

Excipients: sodium hydrogen phosphate anhydrous, sodium dihydrogen phosphate dihydrate, propylene glycol, water for injection.

Basic physical and chemical properties: clear colorless or almost colorless solution.

Pharmacotherapeutic group

Corticosteroids for systemic use. Glucocorticoids. ATX code H02A B06.

Pharmacological properties .

Pharmacodynamics.

It has anti-inflammatory, anti-allergic, immunosuppressive, anti-shock and anti-toxic effects.

In relatively large doses, it inhibits the activity of fibroblasts, the synthesis of collagen, reticuloendothelium and connective tissue (inhibition of the proliferative phase of inflammation), delays synthesis and accelerates protein catabolism in muscle tissue, but increases its synthesis in the liver.

The antiallergic and immunosuppressive properties of the drug are due to the inhibition of the development of lymphoid tissue with its involution during long-term use, a decrease in the number of circulating T- and B-lymphocytes, inhibition of mast cell degranulation, and suppression of antibody production.

The anti-shock effect of the drug is due to an increase in the vascular response to endo- and exogenous vasoconstrictor substances, with the restoration of the sensitivity of vascular receptors to catecholamines and an increase in their hypertensive effect, as well as a delay in the excretion of sodium and water from the body.

The antitoxic effect of the drug is associated with stimulation of protein synthesis processes in the liver and acceleration of the inactivation of endogenous toxic metabolites and xenobiotics in it, as well as with an increase in the stability of cell membranes, incl. hepatocytes. It enhances the deposition of glycogen in the liver and the synthesis of glucose from the products of protein metabolism. An increase in blood glucose levels activates the secretion of insulin. It inhibits the uptake of glucose by fat cells, which leads to the activation of lipolysis. However, due to the increase in insulin secretion, lipogenesis is stimulated, which contributes to the accumulation of fat.

Reduces calcium absorption in the intestines, increases its leaching from bones and excretion by the kidneys. It suppresses the release of adrenocorticotropic hormone and β-lipotropin by the pituitary gland, and therefore, with prolonged use, the drug may contribute to the development of functional insufficiency of the adrenal cortex.

The main factors limiting long-term therapy with prednisolone are osteoporosis and Itsenko-Cushing's syndrome. Prednisolone inhibits the secretion of thyroid-stimulating and follicle-stimulating hormones.

In high doses, it can increase the excitability of brain tissue and help lower the seizure threshold.

Stimulates excess secretion of hydrochloric acid and pepsin in the stomach, and therefore may contribute to the development of peptic ulcers.

Pharmacokinetics

When administered intramuscularly, it is absorbed into the blood quickly, however, compared with reaching the maximum level in the blood, the pharmacological effect of the drug is significantly delayed and develops in 2-8 hours. In blood plasma, most prednisolone binds to transcortin (cortisol-binding globulin), and when the process is saturated, to albumin. With a decrease in protein synthesis, a decrease in the binding capacity of albumins is observed, which can cause an increase in the free fraction of prednisolone and, as a result, the manifestation of its toxic effect when using conventional therapeutic doses. The half-life in adults is 2-4 hours, in children it is shorter. Biotransformed by oxidation mainly in the liver, as well as in the kidneys, small intestine, bronchi. Oxidized forms are glucuronized or sulfated and excreted in the form of conjugates by the kidneys. About 20% of prednisolone is excreted from the body by the kidneys unchanged; a small part is excreted in the bile.

In liver diseases, the metabolism of prednisolone slows down and the degree of its binding to blood plasma proteins decreases, which leads to an increase in the half-life of the drug.

Clinical Characteristics

Indications.

Intramuscular, intravenous administration: systemic connective tissue diseases: systemic lupus erythematosus, dermatomyositis, scleroderma, periarteritis nodosa, ankylosing spondylitis;

hematological diseases: acute hemolytic anemia, lymphogranulomatosis, granulocytopenia, thrombocytopenic purpura, agranulocytosis, various forms of leukemia;

skin diseases: common eczema, erythema multiforme exudative, pemphigus vulgaris, erythroderma, exfoliative dermatitis, seborrheic dermatitis, psoriasis, alopecia, adrenogenital syndrome;

replacement therapy: Addison's crisis;

emergency conditions: severe forms of non-specific ulcerative colitis and Crohn's disease, shock (burn, traumatic, surgical, anaphylactic, toxic, transfusion), status asthmaticus, acute adrenal insufficiency, hepatic coma, severe allergic and anaphylactic reactions, hypoglycemic reactions;

Intra-articular administration: chronic polyarthritis, osteoarthritis of large joints, rheumatoid arthritis, post-traumatic arthritis, arthrosis;

Contraindications

Hypersensitivity to the components of the drug; peptic ulcer of the stomach and duodenum, osteoporosis, Itsenko-Cushing's disease, tendency to thromboembolism, renal failure, arterial hypertension, viral infections (including viral lesions of the eyes and skin), decompensated diabetes mellitus, vaccination period (at least 14 days before and after preventive immunization), lymphadenitis after BCG vaccination, active tuberculosis, glaucoma, cataracts, productive symptoms in mental illness, psychosis, depression; systemic mycosis, herpetic diseases, syphilis, severe myopathy (with the exception of myasthenia gravis), poliomyelitis (with the exception of the bulbar-encephalitic form), pregnancy and lactation.

For intra-articular injections - infections at the injection site.

Interaction with other medicinal products and other forms of interaction

Anticoagulants: when used simultaneously with glucocorticoids, the effect of anticoagulants may increase or decrease. Parenteral administration of prednisolone causes the thrombolytic effect of vitamin K antagonists (fluindione, acenocoumarol).

Salicylates and other non-steroidalanti-inflammatorydrugs: the simultaneous use of salicylates, indomethacin and other non-steroidal anti-inflammatory drugs may increase the likelihood of ulceration of the gastric mucosa. Prednisolone reduces the level of salicylates in the blood serum, increasing their renal clearance. Caution is required when reducing the dose of prednisolone with prolonged simultaneous use.

Hypoglycemic drugs: Prednisolone partially inhibits the hypoglycemic effect of oral hypoglycemic agents and insulin.

liver enzyme inducers, for example, barbiturates, phenytoin, pyryramidone, carbamazepine and rimfampicin increase the systemic clearance of prednisolone, thus reducing the effect of prednisolone by almost 2 times.

InhibitorsCYP3 A4, for example, erythromycin, clarithromycin, ketoconazole, diltiazem, aprepitant, itraconazole, and oleandomycin increase the elimination and plasma levels of prednisolone, which enhances the therapeutic and side effects of prednisolone.

Estrogen may potentiate the effect of prednisolone by slowing down its metabolism. It is not recommended to adjust the dose of prednisolone in women using oral contraceptives, which contribute not only to an increase in the half-life, but also to the development of an atypical immunosuppressive effect of prednisolone.

Fluoroquinolones: simultaneous use can lead to damage to the tendons. Amphotericin, diuretics and laxatives: prednisolone may increase the excretion of potassium from the body in patients who receive these drugs at the same time. Immunosuppressants: Prednisolone has active immunosuppressive properties, which may cause an increase in therapeutic effects or the risk of various adverse reactions when used simultaneously with other immunosuppressants. Only some of them can be explained by pharmacokinetic interactions. Glucocorticoids increase the antiemetic efficacy of antiemetic drugs that are used concomitantly in therapy with anticancer drugs that cause vomiting.

Corticosteroids can increase the concentration of tacrolimus in the blood plasma when they are used simultaneously; when they are canceled, the concentration of tacrolimus in the blood plasma decreases.

Immunization: glucocorticoids may reduce the effectiveness of immunization and increase the risk of neurological complications. The use of therapeutic (immunosuppressive) doses of glucocorticoids with live virus vaccines may increase the risk of developing viral diseases. During therapy with the drug, emergency-type vaccines can be used.

Anticholinesterase agents: in patients with myasthenia gravis, the use of glucocorticoids and anticholinesterase agents can cause muscle weakness, especially in patients with myasthenia gravis.

cardiac glycosides: increases the risk of developing glycoside intoxication.

Other: Two serious cases of acute myopathy have been reported in elderly patients treated with doxocarium chloride and high doses of prednisone. With long-term therapy, glucocorticoids may reduce the effect of somatotropin.

Cases of acute myopathy have been described with the use of corticosteroids in patients who are simultaneously treated with neuromuscular blockers (eg, pancuronium).

With the simultaneous use of prednisolone and cyclosporine, cases of seizures have been noted. Since the simultaneous administration of these drugs causes mutual inhibition of metabolism, it is likely that convulsions and other side effects associated with the use of each of these drugs as monotherapy may occur more often when they are used simultaneously. Simultaneous use may cause an increase in the concentration of other drugs in the blood plasma.

Antihistamine drugs reduce the effect of prednisone.

With the simultaneous use of prednisolone with antihypertensive drugs, the effectiveness of the latter may decrease.

Application features

In infectious diseases and latent forms of tuberculosis, the drug should be prescribed only in combination with antibiotics and anti-tuberculosis drugs. If it is necessary to use prednisolone while taking oral hypoglycemic drugs or anticoagulants, it is necessary to adjust the dosing regimen of the latter. In patients with thrombocytopenic purpura, the drug should be used only intravenously.

After discontinuation of treatment, withdrawal syndrome, adrenal insufficiency, as well as an exacerbation of the disease, in connection with which prednisolone was prescribed, may occur. If functional adrenal insufficiency is observed after the end of treatment with prednisolone, the use of the drug should be resumed immediately, and the dose reduction should be carried out very slowly and with caution (for example, the daily dose should be reduced by 2-3 mg for 7-10 days). Because of the risk of developing hypercortisolism, a new course of cortisone treatment after a previous long-term treatment with prednisolone for several months should always be started with low initial doses (except in acute life-threatening conditions).

The electrolyte balance should be especially carefully monitored when prednisone is used in combination with diuretics. With long-term treatment with prednisone, in order to prevent hypokalemia, it is necessary to prescribe potassium supplements and an appropriate diet due to a possible increase in intraocular pressure and the risk of developing subcapsular cataracts.

During treatment, especially long-term treatment, an ophthalmologist's supervision is necessary. When indicating a history of psoriasis, prednisolone in high doses should be used with extreme caution.

If there is a history of psychosis, convulsions, prednisolone should be used only in the minimum effective doses.

Prednisolone should be used with extreme caution in children.

With extreme caution, prescribe in immunodeficiency states (including AIDS). or HIV infection). Also, use with caution after a recent myocardial infarction (in patients with acute, subacute myocardial infarction, it is possible to expand the focus of necrosis, slow down the formation of scar tissue, and rupture the heart muscle).

With special caution, it is prescribed for liver failure, conditions that cause the occurrence of hypoalbuminemia, obesity of III-IV degree.

Women during menopause need to undergo research regarding the possible occurrence of osteoporosis.

In the liver with glucocorticoids for a long time, it is recommended to regularly monitor blood pressure, determine the level of glucose in the urine and blood, conduct an analysis of feces for occult blood, analyzes of blood coagulation indicators, X-ray control of the spine. Before starting treatment with glucocorticoids, a thorough examination of the gastrointestinal tract should be carried out to exclude peptic ulcer of the stomach and duodenum.

Application during pregnancypregnancy or breastfeeding

During pregnancy, the drug should not be used.

If necessary, the use of the drug during lactation is recommended to stop breastfeeding.

The ability to influence the reaction rate when driving or dother mechanisms

Patients treated with prednisolone should refrain from potentially hazardous activities that require increased attention to the speed of mental and motor reactions.

Special patient groups

Elderly age

With prolonged therapy, muscle atrophy, muscle pain or weakness, delayed wound healing, atrophy of the bone protein matrix leading to osteoporosis, vertebral compression fractures, aseptic necrosis of the femoral head or humeral head, pathological fractures of long tubular bones can be observed. Particularly serious complications may occur in elderly and debilitated patients.

Before starting glucocorticoid therapy in postmenopausal women, it should be taken into account that such patients are particularly prone to osteoporosis.

Use with caution in patients with osteoporosis.

Liver dysfunction

In patients with cirrhosis, an increase in the effect of glucocorticoids is observed.

Violations of the function by check.

Apply with caution.

Method of applicationvalues and doses

The dose of the drug and the duration of treatment is set by the doctor individually, depending on the indications and severity of the disease.

Prednisolone is administered intravenously (drip or jet) or intramuscularly. Intravenously, the drug is usually administered first by jet, then by drip.

In acute adrenal insufficiency, a 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.

In bronchial asthma, the drug is administered depending on the severity of the disease and the effectiveness of complex treatment from 75 mg to 675 mg for a course of treatment from 3 to 16 days; in severe cases, the dose may be increased to 1400 mg per course of treatment or more with a gradual dose reduction.

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

With a thyrotoxic crisis, 100 mg of the drug is administered at 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 is usually administered by bolus at the beginning of therapy, after which it is switched to drip administration. If within 10-20 minutes the blood pressure does not increase, repeat the jet administration of the drug. After removing from the state of shock, drip administration is continued until blood pressure stabilizes. A single dose is 50-150 mg (in severe cases, up to 400 mg). The drug is re-administered after 3-4 hours. The daily dose can be 300-1200 mg (with subsequent dose reduction).

In acute hepatic and renal insufficiency (with acute poisoning, in the postoperative and postpartum periods, etc.), Prednisolone is administered at a dose of 25-75 mg / day; if indicated, the daily dose can be increased to 300-1500 mg / day and above.

In rheumatoid arthritis and systemic lupus erythematosus, Prednisolone is administered in addition to the systemic intake of the drug at a dose of 75-125 mg per day for no more than 7-10 days.

In acute hepatitis, Prednisolone is administered at a dose of 75-100 mg / day for 7-10 days.

In case of poisoning with caustic fluids with burns of the digestive tract and upper respiratory tract, Prednisolone is prescribed at a dose of 75-400 mg / day for 3-18 days.

If intravenous administration is not possible, Prednisolone is administered intramuscularly in the same doses. After stopping the acute condition, Prednisolone is prescribed orally 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 should not be stopped abruptly!

Children

Use in children over 6 years of age only as directed and under medical supervision. The doctor determines the doses and duration of therapy individually, depending on the age and severity of the course of the disease. With prolonged use in children, growth retardation is possible, therefore, it is necessary to limit the use of minimal doses for certain indications for the shortest possible time. The benefit of treatment should outweigh the potential risk of adverse reactions.

Overdose

In case of an overdose, nausea, vomiting, bradycardia, arrhythmia, increased symptoms of heart failure, cardiac arrest are possible; hypokalemia, increased blood pressure, muscle cramps, hyperglycemia, thromboembolism, acute psychosis, dizziness, headache, hypercortisolism symptoms may develop: weight gain, edema development, arterial hypertension, glucosuria, hypokalemia. In children with an overdose, inhibition of the hypothalamic-pituitary-adrenal system, Itsenko-Cushing's syndrome, decreased excretion of growth hormone, and increased intracranial pressure are possible.

There is no specific antidote.

Treatment: discontinuation of the drug, symptomatic therapy, if necessary, correction of the electrolyte balance.

Adverse reactions

The development of severe adverse reactions depends on the dose and duration of treatment. Adverse reactions usually develop with prolonged treatment with the drug. Over a short period, the risk of their occurrence is unlikely.

Infections and infestations: hypersensitivity to bacterial, viral, fungal infections, their severity with symptom masking, opportunistic infections.

From the blood and lymphatic system: an increase in the total number of leukocytes with a decrease in the number of eosinophils, monocytes and lymphocytes. The mass of lymphoid tissue decreases. Blood coagulation may increase, which leads to thrombosis, thromboembolism.

From the endocrine system and metabolism: depression of the hypothalamic-pituitary-adrenal system, growth retardation in children and adolescents, menstrual irregularities, impaired secretion of sex hormones (amenorrhea), postmenopausal bleeding, cushingoid face, hirsutism, weight gain, decreased carbohydrate tolerance, increased need for insulin and oral hypoglycemic drugs, hyperlipidemia, negative balance of nitrogen and calcium, increased appetite, impaired mineral metabolism and electrolyte balance, hypokalemic alkalosis, hypokalemia, fluid and sodium retention in the body is possible.

Mental disorders: irritability, euphobia, depression, suicidal tendencies, insomnia, labile mood, increased concentration, psychological dependence, mania, hallucinations, exacerbation of schizophrenia, dementia, psychosis, anxiety, sleep disturbance, epileptic seizures, cognitive dysfunction (including amnesia and impaired consciousness), increased intracranial pressure, which is accompanied by nausea and swelling of the optic nerve head in children.

From the nervous system: increased intracranial pressure, epileptic seizures, peripheral neuropathy, paresthesia, dizziness, headache, autonomic disorders.

From the side of the organs of vision: increased intraocular pressure, glaucoma, swelling of the optic nerve, cataracts, thinning of the cornea and sclera, exacerbation of eye viral and fungal infections, exophthalmos.

From the side of the cardiovascular system: myocardial rupture due to myocardial infarction, arterial hypo- or hypertension, bradycardia, combined ventricular arrhythmia, asystole (due to rapid administration of the drug), atherosclerosis, thrombosis, vasculitis, heart failure, peripheral edema.

In patients with acute myocardial infarction - the spread of necrosis, slowing down the formation of the scar.

From the immune system: allergic reactions that cause fatal anaphylactic shock, angioedema, allergic dermatitis, changes in reaction to skin tests, relapse of tuberculosis, immunosuppression, hypersensitivity reactions, including rash, skin itching.

From the gastrointestinal tract: nausea, bloating, bad taste in the mouth, dyspepsia, peptic ulcers with perforation and bleeding, esophageal ulcer, esophageal candidiasis, pancreatitis, gallbladder perforation, gastric bleeding, local ileitis and ulcerative colitis.

During the use of the drug, there may be an increase in ALT, AST and alkaline phosphatase, which is usually not significant and is reversible after discontinuation of the drug.

From the side of the skin: delayed regeneration, skin atrophy, formation of hematomas and atrophic skin streaks (striae), telangiectasia, acne, acne, hirsutism, microhemorrhages, ecchymosis, purpura, hypo- or hyperpigmentation, post-steroid panniculitis, which is characterized by the appearance of erythematosis, hot subcutaneous thickening for 2 weeks after discontinuation of the drug, Kaposi's sarcoma.

From the musculoskeletal system: proximal myopathy, osteoporosis, tendon rupture, muscle weakness, atrophy, myopathy, fractures of the spine and long bones, aseptic osteonecrosis.

From the urinary system: increased risk of urolith formation and the content of leukocytes and erythrocytes in the urine without obvious damage to the kidneys.

General: malaise, persistent hiccups when using the drug in high doses, adrenal insufficiency, which leads to arterial hypotension, hypoglycemia and death in stressful situations, such as surgery, trauma or infection, if the dose of prednisolone is not increased.

With a sharp withdrawal of the drug, withdrawal syndrome is possible, the severity of symptoms depends on the degree of adrenal atrophy, headache, nausea, abdominal pain, dizziness, anorexia, weakness, mood changes, lethargy, fever, myalgia, arthralgia, rhinitis, conjunctivitis, skin pain syndrome, weight loss. In more severe cases - severe mental disorders and increased intracranial pressure, steroid pseudo-rheumatism in patients with rheumatism, death.

Reactions at the injection site: pain, burning, pigmentation changes (depigmentation, leukoderma), skin atrophy, sterile abscesses, rarely lipoatrophy.

1 ml of the drug in 1 ml glass ampoules with a break ring. 5 ampoules of the drug are put into a blister from a polyvinyl chloride film, which is covered

a pack of cardboard box (chrome-ersatz).

On prescription.

Manufacturer

PJSC "BIOPHARMA", Ukraine; OOO FZ BIOPHARMA, Ukraine.

Manufacturer's location and address

Ukraine, 03680, Kyiv, st. N. Amosova, 9;

Ukraine, 09100, Kyiv region, Belaya Tserkov, st. Kyiv, 37.

Injections Prednisolone is a drug that makes up a group of glucocorticosteroid hormones. It is permissible to use it only after consulting with your doctor, as injections have a large number of contraindications and side effects. Most often, they are prescribed in cases where the use of non-steroidal anti-inflammatory drugs is not acceptable or has not shown proper effectiveness.

Mechanism of action

Prednisolone is an injection solution that has powerful anti-inflammatory, anti-shock, analgesic and immunosuppressive effects. Once in the body, the drug forms a glucocorticoid receptor. It rapidly penetrates the cell nucleus, where it interacts with genes. Because of this, there are serious changes in the production of proteins and RNA. Prednisolone is valued for its high anti-inflammatory effect, which is due to the following factors:

The active ingredients increase the production of lipocortin, which prevents the further production of phospholipase. Because of this, damaged tissues can no longer produce arachidonic acid. All this leads to the impossibility of the synthesis of prostaglandins.
The active substances interfere with the exchange of COX-2 genes, which also reduces the production of prostaglandins.
Prednisolone stops the metabolic processes between molecules in the blood vessels, so that neutrophils and monocytes do not penetrate into the focus of inflammation.

Prednisolone is a drug with powerful anti-inflammatory, analgesic and immunosuppressive effects.

Indications for use

Prednisolone is a powerful medicine that should only be used after consulting a doctor. Usually experts prescribe it:

With postoperative, traumatic, toxic and burn shocks.
In acute and severe forms of allergies.
With anaphylactic or blood transfusion shock.
With swelling of the brain caused by radiation therapy, head trauma or tumor.
With a severe form of bronchial asthma.
With serious skin lesions: psoriasis, dermatitis, bullous dermatitis, seborrhea, Stevens-Jones syndrome.
With allergic conjunctivitis.
With serious disorders and congenital anomalies of the adrenal glands.
With severe uveitis, optic neuritis.
With hepatic coma.
With thyrotoxic crisis.
With acute hepatitis.
With serious diseases of the blood and circulatory system.
With Leffler's syndrome, berylliosis.
With multiple sclerosis.
With hypercalcemia caused by malignant neoplasms.
As a preventive measure to reject a transplanted organ.
To reduce inflammation.
For the prevention of cicatricial narrowing.

Mode of application

Instructions for the use of Prednisolone injections states that it is permissible to use the medicine only after consultation with a qualified attending physician. This medicine has a high impact on the body, therefore, due to improperly selected therapy, there is a high risk of side effects. Prednisolone in the form of injections must be administered inside the muscles, joints, or in the form of impregnation of tissues. It is very important to treat the skin with alcohol before the procedure in order to kill all pathogenic microorganisms.

To stop the soreness of the joints, it is necessary to inject 25-50 mg into large ones, 10 mg into small ones. With a pronounced syndrome, the procedure can be repeated several times. It is very important to evaluate the therapeutic effect after such therapy in order to either increase the dose of the active substance, or change the medicine, if necessary. In order for the drug to be properly distributed over the joint, after administration it must be repeatedly bent and unbent. Lotions from the solution will also help reduce pain - they treat small areas of the affected surfaces.

To cope with various types of conjunctivitis, injections or instillation of the drug into the eyes will help. Do this 1-3 drops three times a day for 2 weeks. In order for the therapy not to bring any complications or side effects, it is necessary to regularly measure the level of blood pressure and administer anabolic drugs. Also, the doctor should send you once every two weeks for a blood, feces and urine test. At the time of therapy, it is necessary to monitor the water balance in the body, if necessary, take diuretics.

It should be borne in mind that with prolonged use, Prednisolone can cause a decrease in the level of potassium in the blood. To prevent this, it is recommended to follow a special diet and take this macronutrient in the form of tablets. Otherwise, there is a high risk of osteoporosis - damage to bone tissue, due to which it becomes extremely fragile.

Therapeutic dosage

Keep in mind that only the attending physician can prescribe a therapeutic dose of Prednisolone, as well as the duration of its use. He must familiarize himself with the results of diagnostic studies, and only after that prescribe treatment. Injections can be injected into the body by drip or jet, however, in practice, two of these methods are used at once in one procedure.

Disease	Dosage	Duration
Acute adrenal insufficiency	100-200 mg	3 days to 2 weeks
Bronchial asthma	75-675 mg	3 days to 2 weeks
asthmatic crisis	150-1200 mg	Once
Thyrotoxic crisis	200-300 mg	Week 1
Toxin poisoning	75-400 mg	1-2 weeks
Burns of the respiratory tract and gastrointestinal tract	120-350 mg	Week 1
All kinds of shocks	300-1200 mg	Week 1
Acute kidney and liver failure	300-1500 mg	Week 1
Rheumatoid arthritis	75-100 mg	Week 1
Acute hepatitis	75-100 mg	10 days

In cases where it is not possible to inject Prednisolone into the bloodstream, it is permissible to administer it intramuscularly. To stop acute conditions, doctors prescribe the tablet form of this medication. To avoid the withdrawal syndrome, the end of treatment is accompanied by a decrease in the therapeutic dose. It is strictly forbidden to abruptly stop the use of this medication - the risk of serious complications is high.

Despite the generally accepted dosages, only the attending physician should prescribe treatment with Prednisolone based on advanced diagnostic data.

withdrawal syndrome

With prolonged use of the solution for injection of Prednisolone, the body begins to get used to the components. In addition, the drug affects and changes the functioning of the adrenal glands. With a sharp refusal of therapy with this drug, a person may experience malaise, fatigue, high body temperature. Such conditions disappear without additional therapy in a few days. However, if high doses of Prednisolone were abruptly discontinued, there is a risk of a hypoadrenaline crisis. You can recognize it by increasing convulsions, vomiting and collapse. If medical care is not provided to a person in a timely manner, cardiac arrest is possible due to acute cardiovascular insufficiency.

Contraindications

To reduce the risk of complications due to taking Prednisolone, you must always remember about the presence of contraindications. Even in emergency cases, it is forbidden to administer this injection if there is an increased sensitivity to the components of the drug. It should also be borne in mind that lactose is present in the composition of the drug, to which some people have persistent intolerance. With extreme caution, treatment with Prednisolone is permissible in the following cases:

Prednisolone is a drug that has a large number of side effects. To prevent their occurrence, it is necessary to strictly adhere to all the recommendations of the attending physician. The most dangerous are the following:

Decreased glucose tolerance is especially dangerous for people with diabetes. Substances entering the body slow down the work of the liver, which disrupts the production of insulin.
Inhibition of adrenal function - this leads to hormonal imbalance. It also slows down the removal of toxins from the body.
Itsenko-Cushing's syndrome is a condition that occurs with a powerful change in hormonal levels.
The appearance of nausea, vomiting, pain in the abdomen.
The formation of bleeding inside the gastrointestinal tract: erosive gastritis, perforation of the intestinal walls, ulcers.
Violation of digestion in the form of changes in appetite, constipation and diarrhea, flatulence.
Exacerbation of cardiovascular pathologies.
The appearance of prolonged hiccups.
Changes in the nervous system: TIR, depression, euphoria, paranoia, disorientation.
Frequent seizures, especially at night.
Headaches and dizziness.
Significant increase in pressure inside the eyes.
Increased intraocular pressure, trophic changes in the structure of the cornea.
Hyperhidrosis, the appearance of a specific body odor.
Weight loss, muscle atrophy.
Prolonged wound healing.
The formation of acne and striae on the body.
Local allergic reactions.

Synthetic glucocorticosteroid drug, dehydrated analogue of hydrocortisone. It has anti-inflammatory, anti-allergic, immunosuppressive effects, increases the sensitivity of beta-adrenergic receptors to endogenous catecholamines.

Protein metabolism: reduces the amount of globulins in plasma, increases albumin synthesis in the liver and kidneys (with an increase in the 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 (accumulation of fat occurs mainly in 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); contributes to the development of hyperglycemia.

Water-electrolyte metabolism: retains sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, reduces the mineralization of bone tissue.

Important: Description of the drug Prednisolone is not intended for prescribing treatment without the participation of a physician.

Instructions for use:

Pharmacological properties

Pharmacodynamics

It has anti-inflammatory, anti-allergic, immunosuppressive, anti-shock and anti-toxic effects. In relatively large doses, it inhibits the activity of fibroblasts, the synthesis of collagen, reticuloendothelium and connective tissue (inhibition of the proliferative phase of inflammation), delays synthesis and accelerates protein catabolism in muscle tissue, but increases its synthesis in the liver.

It enhances the deposition of glycogen in the liver and the synthesis of glucose from the products of protein metabolism. An increase in blood glucose levels activates the secretion of insulin. It inhibits the uptake of glucose by fat cells, which leads to the activation of lipolysis.

However, due to the increase in insulin secretion, lipogenesis is stimulated, which contributes to the accumulation of fat. Reduces calcium absorption in the intestines, increases its leaching from bones and excretion by the kidneys.

It suppresses the release of adrenocorticotropic hormone and b-lipotropin by the pituitary gland, and therefore, with prolonged use, the drug may contribute to the development of functional insufficiency of the adrenal cortex.

In high doses, it can increase the excitability of brain tissue and help lower the seizure threshold. Stimulates excess secretion of hydrochloric acid and pepsin in the stomach, and therefore may contribute to the development of peptic ulcers.

Pharmacokinetics

In plasma, most prednisolone binds to transcortin (cortisol-binding globulin), and when the process is saturated, to albumin. With a decrease in protein synthesis, a decrease in the binding capacity of albumins is observed, which can cause an increase in the free fraction of prednisolone and, as a result, the manifestation of its toxic effect when using conventional therapeutic doses.

The half-life in adults is 2-4 hours, in children it is shorter. Biotransformed by oxidation mainly in the liver, as well as in the kidneys, small intestine, bronchi. Oxidized forms are glucuronized or sulfated and excreted in the form of conjugates by the kidneys.

About 20% of prednisolone is excreted from the body by the kidneys unchanged; a small part is excreted in bile. In liver diseases, the metabolism of prednisolone slows down and the degree of its binding to plasma proteins decreases, which leads to an increase in the half-life of the drug.

Indications for the use of Prednisolone

Intramuscular, intravenous administration

Systemic connective tissue diseases

systemic lupus erythematosus,
dermatomyositis,
scleroderma,
nodular periarteritis,
ankylosing spondylitis.

Hematological diseases

acute hemolytic anemia,
lymphogranulomatosis,
granulocytopenia,
thrombocytopenic purpura,
agranulocytosis,
various forms of leukemia.

Skin diseases

common eczema,
erythema multiforme exudative,
vesicle normal,
erythroderma,
exfoliative dermatitis,
seborrheic dermatitis,
psoriasis,
alopecia,
adrenogenital syndrome.

Replacement therapy

Addisonian crisis.

Emergency conditions

severe forms of non-specific ulcerative colitis and Crohn's disease,
shock (burn, traumatic, surgical, anaphylactic, toxic, transfusion),
status asthmaticus,
acute insufficiency of the adrenal cortex,
hepatic coma,
severe allergic and anaphylactic reactions,
hypoglycemic reactions.

Intra-articular injection

chronic polyarthritis,
osteoarthritis of large joints,
rheumatoid arthritis,
post-traumatic arthritis,
arthrosis.

Dosage and administration

Mixing and simultaneous use of prednisolone with other drugs in the same infusion system or syringe is not allowed! The drug is prescribed for intravenous, intramuscular or intraarticular administration. The dose of prednisolone depends on the severity of the disease.

For the treatment of adults, the daily dose is 4-60 mg intravenously or intramuscularly. For children, the drug is prescribed intramuscularly (deep into the gluteal muscle) strictly according to indications and under the supervision of a doctor: children aged 6-12 years - 25 mg / day, over 12 years old - 25-50 mg / day.

The duration of use and the number of injections of the drug is determined individually. In Addison's disease, the daily dose for adults is 4-60 mg intravenously or intramuscularly.

In severe form of ulcerative colitis, 8-12 ml / day (240-360 mg Prednisolone) for 5-6 days, in severe form of Crohn's disease - 10-13 ml / day (300-390 mg Prednisolone) for 5 -7 days.

In emergencies, prednisolone is administered intravenously, slowly (over about 3 minutes) or drip, at a dose of 30-60 mg.

If intravenous infusion is difficult, the drug is administered intramuscularly, deeply. With this method of administration, the effect develops more slowly. If necessary, the drug is administered repeatedly intravenously or intramuscularly at a dose of 30-60 mg every 20-30 minutes. In some cases, an increase in the indicated dose is allowed, which the doctor decides individually in each case.

The adult dose of intra-articular prednisolone is 30 mg for large joints, 10-25 mg for medium-sized joints, and 5-10 mg for small joints. The drug is administered every 3 days. The course of treatment is up to 3 weeks.

Application features

In patients with thrombocytopenic purpura, the drug is used only intravenously. After discontinuation of treatment, withdrawal syndrome, adrenal insufficiency, as well as an exacerbation of the disease, in connection with which prednisolone was prescribed, may occur.

If functional adrenal insufficiency is observed after the end of treatment with prednisolone, the use of the drug should be resumed immediately, and the dose reduction should be carried out very slowly and with caution (for example, the daily dose should be reduced by 2-3 mg for 7-10 days).

Because of the risk of developing hypercortisolism, a new course of cortisone treatment after a previous long-term treatment with prednisolone for several months should always be started with low initial doses (except in acute life-threatening conditions).

During treatment, especially long-term treatment, an ophthalmologist's supervision is necessary. When indicating a history of psoriasis, prednisolone in high doses is used with extreme caution. If there is a history of psychosis, convulsions, prednisolone should be used only in the minimum effective doses.

It is also prescribed with caution after a recent myocardial infarction (in patients with acute, subacute myocardial infarction, it is possible to expand the focus of necrosis, slow the formation of scar tissue, and rupture the heart muscle).

With special caution, it is prescribed for liver failure, conditions that cause the occurrence of hypoalbuminemia, obesity III - IV degrees. Women during menopause need to undergo research regarding the possible occurrence of osteoporosis.

When treated with glucocorticoids for a long time, it is recommended to regularly monitor blood pressure, determine the level of glucose in urine and blood, conduct an analysis of feces for occult blood, analyzes of blood coagulation indicators, and X-ray control of the spine.

Before starting treatment with glucocorticoids, a thorough examination of the gastrointestinal tract should be carried out to exclude peptic ulcer of the stomach and duodenum.

Side effects

Infections and infestations

Hypersensitivity to bacterial, viral, fungal infections, their severity with symptom masking, opportunistic infections.

Blood system and lymphatic system

An increase in the total number of leukocytes with a decrease in the number of eosinophils, monocytes and lymphocytes. The mass of lymphoid tissue decreases. Blood coagulation may increase, which leads to thrombosis, thromboembolism.

Endocrine system and metabolism

Inhibition of the hypothalamic-pituitary-adrenal system, growth retardation in children and adolescents, menstrual irregularities, impaired secretion of sex hormones (amenorrhea), postmenopausal bleeding, cushingoid face, hirsutism, weight gain, decreased carbohydrate tolerance, increased need for insulin and oral sugar-lowering drugs, hyperlipidemia, negative balance of nitrogen and calcium, increased appetite, impaired mineral metabolism and electrolyte balance, hypokalemic alkalosis, hypokalemia, fluid and sodium retention in the body is possible.

Mental disorders

Irritability, euphobia, depression, suicidal tendencies, insomnia, labile mood, increased concentration, psychological dependence, mania, hallucinations, exacerbation of schizophrenia, dementia, psychosis, anxiety, sleep disturbance, epileptic seizures, cognitive dysfunction (including amnesia and impaired consciousness), increased intracranial pressure, which is accompanied by nausea and swelling of the optic nerve head in children.

Nervous system

Increased intracranial pressure, epileptic seizures, peripheral neuropathy, paresthesia, dizziness, headache, autonomic disorders.

organs of vision

Increased intraocular pressure, glaucoma, swelling of the optic nerve, cataracts, thinning of the cornea and sclera, exacerbation of eye viral and fungal infections, exophthalmos.

The cardiovascular system

Myocardial rupture due to myocardial infarction, arterial hypo- or hypertension, bradycardia, combined ventricular arrhythmia, asystole (due to rapid administration of the drug), atherosclerosis, thrombosis, vasculitis, heart failure, peripheral edema.

The immune system

Allergic reactions that cause fatal anaphylactic shock, angioedema, allergic dermatitis, changes in reaction to skin tests, relapse of tuberculosis, immunosuppression.

Gastrointestinal tract

Nausea, bloating, bad taste in the mouth, dyspepsia, peptic ulcers with perforation and bleeding, esophageal ulcer, esophageal candidiasis, pancreatitis, gallbladder perforation, gastric bleeding, local ileitis and ulcerative colitis. During the use of the drug, an increase in ALT, AST and alkaline phosphatase may be observed, which is usually not important and is reversible after drug withdrawal.

Leather

Delayed regeneration, skin atrophy, formation of hematomas and atrophic skin streaks (striae), telangiectasia, acne, acne, hirsutism, microhemorrhages, ecchymosis, purpura, hypo- or hyperpigmentation, post-steroid panniculitis, which is characterized by the appearance of erythematosis, hot subcutaneous thickening for 2 weeks after discontinuation of the drug, Kaposi's sarcoma.

Musculoskeletal system

Proximal myopathy, osteoporosis, tendon rupture, muscle weakness, atrophy, myopathy, fractures of the spine and long bones, aseptic osteonecrosis. Urinary system: increased risk of urolith formation and Instructions for use: leukocytes and erythrocytes in the urine without obvious damage to the kidneys.

General

Malaise, persistent hiccups when using the drug in high doses, adrenal insufficiency, which leads to arterial hypotension, hypoglycemia and death in stressful situations, such as surgery, trauma or infection, if the dose of prednisolone is not increased.

In more severe cases - severe mental disorders and increased intracranial pressure, steroid pseudorheumatism in patients with rheumatism, death. Reactions at the injection site: pain, burning, pigmentation changes (depigmentation, leukoderma), skin atrophy, sterile abscesses, rarely - lipoatrophy.

Interaction with other drugs

Anticoagulants: when used simultaneously with glucocorticoids, the effect of anticoagulants may increase or decrease. Parenteral administration of prednisolone causes the thrombolytic effect of vitamin K antagonists (fluindione, acenocoumarol).

Salicylates and other non-steroidal anti-inflammatory drugs: the simultaneous use of salicylates, indomethacin and other non-steroidal anti-inflammatory drugs may increase the likelihood of gastric ulcers. Prednisolone reduces the level of salicylates in the blood serum, increasing their renal clearance.

Caution is required when reducing the dose of prednisolone with prolonged simultaneous use. Hypoglycemic drugs: prednisolone partially inhibits the hypoglycemic effect of oral hypoglycemic agents and insulin. Liver enzyme inducers, such as barbiturates, phenytoin, pyryramidone, carbamazepine and rimfampicin, increase the systemic clearance of prednisolone, thus reducing the effect of prednisolone by almost 2 times.

CYP3A4 inhibitors such as erythromycin, clarithromycin, ketoconazole, diltiazem, aprepitant, itraconazole, and oleandomycin increase the elimination and plasma levels of prednisolone, which enhances the therapeutic and side effects of prednisolone.

Estrogen can potentiate the effect of prednisone by slowing down its metabolism. It is not recommended to adjust the dose of prednisolone in women using oral contraceptives, which contribute not only to an increase in the half-life, but also to the development of an atypical immunosuppressive effect of prednisolone.

Fluoroquinolones: Concomitant use may lead to tendon damage. Amphotericin, diuretics and laxatives: Prednisone may increase the excretion of potassium from the body in patients who receive these drugs at the same time.

Immunosuppressants: Prednisolone has active immunosuppressive properties, which may cause an increase in therapeutic effects or the risk of various adverse reactions when used simultaneously with other immunosuppressants.

Only some of them can be explained by pharmacokinetic interactions. Glucocorticoids increase the antiemetic efficacy of antiemetic drugs that are used concomitantly in therapy with anticancer drugs that cause vomiting.

Corticosteroids can increase the plasma concentration of tacrolimus when they are used simultaneously; when they are canceled, the plasma concentration of tacrolimus decreases. Immunization: Glucocorticoids may reduce the effectiveness of immunization and increase the risk of neurological complications.

The use of therapeutic (immunosuppressive) doses of glucocorticoids with live virus vaccines may increase the risk of developing viral diseases. During therapy with the drug, emergency-type vaccines can be used.

Anticholinesterase agents: In patients with myasthenia gravis, the use of glucocorticoids and anticholinesterase agents can cause muscle weakness, especially in patients with myasthenia gravis.

Others: Two serious cases of acute myopathy have been reported in elderly patients treated with doxocarium chloride and high doses of prednisolone. With long-term therapy, glucocorticoids may reduce the effect of somatotropin.

Cases of acute myopathy have been described with the use of corticosteroids in patients who are simultaneously treated with neuromuscular blockers (eg, pancuronium).

Simultaneous use may cause an increase in plasma concentrations of other drugs. Antihistamine drugs reduce the effect of prednisone. With the simultaneous use of prednisolone with antihypertensive drugs, the effectiveness of the latter may decrease.

Contraindications

Overdose

Symptoms

In children with an overdose, inhibition of the hypothalamic-pituitary-adrenal system, Itsenko-Cushing's syndrome, decreased excretion of growth hormone, and increased intracranial pressure are possible. There is no specific antidote.

Treatment

Discontinuation of the drug, symptomatic therapy, if necessary - correction of the electrolyte balance.

Questions and answers about the drug "Prednisolone"

Question:Hello, our daughter is 5 years old. We got to the hematology department with a diagnosis of hemorrhagic vasculitis in the mildest form (only a rash on the legs). In the hospital, they were dripped, pierced with heparin. Thank God the spots are almost gone. When discharged, prednisone was prescribed 3.5 tablets per day for 2 weeks, followed by a decrease. After 10 days, we abruptly stopped giving, as the child began to gain weight. We haven't had a drink for 3 days now. The child feels fine. We were scared that there could be consequences due to a sharp refusal. Please tell me, if the child has been feeling fine for 3 days, should we be afraid of anything?

Answer: The dangerous consequences arising after the termination of therapy with Prednisolone include: the return of the symptoms of the pathology, including the pain syndrome; headache; sharp fluctuations in body weight; deterioration in mood; digestive disorders. In this case, it is recommended to resume taking the drug, and then, under the supervision of a doctor, gradually reduce single and daily dosages. Monitor the condition of the child, if it worsens, contact your doctor.

Question:Hello. Red rashes appeared on the skin with white dots, as from nettles. What can from the raspberries eaten last evening, but it happens on a nervous basis. We were prescribed to drink zodak at home, drink enterosgel and diet. And there, in the hospital, an injection - with prastin with prednisolone. That's actually the question, suprastin is understandable, but why prednisolone?

Answer: Hello. Prednisolone is used to relieve shock, a severe allergic reaction.

Question:Hello! My baby is 7 months old. fell ill with the flu, or acute respiratory infections (during the flu epidemic) with all the symptoms. In the children's polyclinic, they told me that in order to alleviate the condition and relieve the spasm of the larynx, it is necessary to prick a no-shpu. Together with no-shpa, we were given an injection of prednisolone. I didn’t know then what kind of drug it was, because. did not encounter him. The nurse said it was an anti-inflammatory, not an antibiotic - and I agreed. In the evening, the child had a stomach ache, cramping pains and foamy diarrhea. Now there is no diarrhea, but the poop is still not like before. The smell is sour and the consistency of feces is rarer than before. I read on the Internet and prednisolone and now I'm afraid - maybe it's increased acidity of the stomach. Tell me how dangerous this injection is for my child and how I can minimize its consequences. Of course, I’m not going to wave my fists after a fight, especially since it’s my own fault - I didn’t know what prednisolone was and gave me an injection of a medicine unknown to me. The child was not at risk. We were then prescribed the antibiotic agumetin, it seems, but we did not drink it, we got better without it.

Answer: The doctors did everything right. Prednisolone injection, single injection, does not give any side effects. Moreover, the child had indications for its introduction. Violation of the stool and abdominal pain are associated with the disease itself and are not a side effect of the drug administration. Now you need to make a coprocytogram and take a probiotic, for example, acipol (1 capsule 2 times a day - 10 days) to normalize the stool.

Question:Hello. Tell me please, I have such a problem: after giving birth, problems with the joints in my arms began, they became inflamed and hurt. I went through a bunch of tests and never got a diagnosis. I even took tests for Le cells, they were not confirmed. Prescribed to take prednisolone 2 tablets a day. The pains disappeared and the swelling from the joints subsided, periodically in the spring and autumn the joints on the hands become inflamed, but after a week everything goes away. Can I replace prednisolone with a lighter drug? And how to gradually stop taking it altogether?

Answer: Prednisone should be discontinued gradually. Start doing it like this: On even days, continue to take 2 tablets, on odd days, 1.5 tablets. And so for 3 weeks. Then another 3 weeks: on even days, continue to take 2 tablets, on odd days - 1 tablet. Next 3 weeks: even - 2 tablets. Odd: 1/2 tablet. Next 3 weeks: even - 2 tablets. Odd: do not accept. Next 3 weeks: even - 1.5 tablets. Odd: do not accept. Next 3 weeks: even - 1 tablet. Odd: do not accept. In the future, do not drink prednisolone, but take licorice root infusion for 3 weeks (licorice root is sold in a pharmacy), take it according to the instructions on the package. At this time, you can also start taking Wobenzym - 3 tablets 3 times a day for 2 months.

13541 0

Prednisolone
Glucocorticoid agents

Release form

Ointment 0.5%
Since. liof. d / in. 25 mg
Solution d / in. 25 mg, 30 mg, 40 mg
Susp. d / in. 25 mg
Tab. 1 mg, 5 mg, 10 mg

Mechanism of action

Prednisolone is a synthetic analogue of hydrocortisone. The main molecular mechanism is the regulation of the expression of a number of genes at the transcriptional and post-transcriptional levels, incl. their effect on transcriptional activation of the cytoplasmic inhibitor of NF-kB, IkBa. By inducing the biosynthesis of lipocortins in leukocytes, it inhibits phospholipase A and reduces the production of prostanoids, leukotrians and platelet activating factor.

Stabilizes cell membranes, inhibits the formation of oxygen free radicals and lipid peroxides, constricts blood vessels in the focus of inflammation and reduces their permeability, inhibits exudation, reduces the synthesis of mucopolysaccharides and proteins, inhibits the processes of lymphopoiesis, reduces the number and activity of T-lymphocytes circulating in the blood, reduces the number and activity of circulating basophils, reduces the release of immediate-type allergy mediators from sensitized cells (histamine, heparin, serotonin, etc.), affects water-salt metabolism and increases the sensitivity of vessels to catecholamines. Depending on the dose, the effects of corticosteroids can be realized at different levels.

Main Effects
■ Anti-inflammatory.
■ Antiallergic.
■ Antishock.
■ Desensitizing.
■ Immunosuppressive.
■ Antitoxic.
■ Antimetabolic.

Pharmacokinetics

After oral administration, it is well absorbed from the gastrointestinal tract. Cmax when taken orally - 1-1.5 hours. In plasma, most (90%) of prednisolone binds to transcortin (cortisol-binding globulin) and albumin.

Metabolized by oxidation mainly in the liver, partly in the kidneys, small intestine, bronchi. The oxidized forms are glucuronidated or sulfated. T1 / 2 - 2-4 hours. Excreted by the kidneys - 20% unchanged.
With intravenous administration, Cmax is reached after 0.5 hours.
T1 / 2 - 2-3 hours.

Indications

Local application:
■ arthritis and arthrosis of the temporomandibular joint;
■ keloid scars;
■ in endodontics - to relieve the inflammatory process in the pulp and periapical tissues: pulpitis, periodontitis.

Systemic therapy:
■ angioedema;
■ systemic lupus erythematosus, bullous pemphigoid, lichen planus, erythema multiforme exudative, Stevens-Johnson syndrome (in combination therapy);
■ emergency care for shock (burn, traumatic, surgical, toxic, cardiogenic) with the ineffectiveness of other therapy;
■ status asthmaticus;
■ allergic diseases (hypersensitivity, including to drugs and chemicals, serum sickness, urticaria, allergic rhinitis, Quincke's edema).

Parenteral administration:
■ burn shock;
■ traumatic shock;
■ operational or resulting from poisoning shock;
■ shock in myocardial infarction;
■ allergic reactions (severe forms);
■ anaphylactic shock;
■ transfusion shock;
■ status asthmaticus;
■ intoxication against the background of infectious diseases (with long-term treatment, prednisolone is combined with an appropriate antibiotic);
■ acute adrenal insufficiency;
■ hepatic coma;
■ in pediatrics - all types of anaphylaxis, allergies, laryngotracheobronchitis, laryngitis, bronchial asthma (severe form), shock.

Dosage and administration

In / in (slowly) and / m (deep into the muscles) 5-30 mg 1 r / day, if necessary, increase the dose to 150-300 mg. Children - 1-2 mg / kg / day.

Outwardly: the ointment is applied to the affected areas of the skin or mucous membranes with a thin layer 1-3 r / day. The course of treatment is 7-14 days.

Contraindications

Intra-articular injection in dentistry is not used.

For systemic use:
■ hypersensitivity;
■ generalized mycosis, herpetic diseases;
■ infectious lesions of the joints and periarticular soft tissues;
■ obesity (III-IV degree);
■ diverticulitis, recently created intestinal anastomosis, peptic ulcer of the stomach and duodenum;
■ chronic renal failure;
■ systemic osteoporosis;
■ myasthenia gravis;
■ arterial hypertension;
■ decompensated diabetes mellitus;
■ mental illness;
■ glaucoma;
■ hypoalbuminemia;
■ Itsenko-Cushing's syndrome;
■ tuberculosis (active form).

For topical use:
■ hypersensitivity;
■ tuberculosis;
■ syphilis;
■ bacterial, viral, fungal skin lesions;
■ skin tumors;
■ pregnancy;
■ acne vulgaris and rosacea (exacerbation of the disease is possible).

Precautions, therapy control

Before starting treatment, the patient should be examined for possible contraindications.

Clinical examination should include examination of the cardiovascular system, x-ray examination of the lungs, examination of the stomach and duodenum, urinary system, organs of vision.

During treatment, you should:
■ monitor complete blood count, blood and urine glucose, plasma electrolytes;
■ for intercurrent infections, septic conditions and tuberculosis to carry out antibiotic therapy;
■ exclude immunization;
■ children who during the period of treatment were in contact with patients with measles or chicken pox, prophylactically prescribe specific immunoglobulins;
■ use anabolic steroids to reduce side effects and increase dietary K+ intake;
■ in Addison's disease, exclude the simultaneous appointment of barbiturates - the risk of developing acute adrenal insufficiency (addisonian crisis);
■ when applied topically, the course of treatment should not exceed 14 days.

With sudden withdrawal, especially in the case of previous use of high doses, a “withdrawal” syndrome is possible - anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness.

After cancellation for several months, it must be taken into account that relative insufficiency of the adrenal cortex remains: if stressful situations arise during this period, GCS is prescribed (according to indications), if necessary, in combination with mineralocorticosteroids.

Use during pregnancy in the first trimester and when breastfeeding: prescribed taking into account the expected therapeutic effect and the negative impact on the fetus and child. With long-term therapy during pregnancy, fetal growth may be impaired, in the third trimester of pregnancy - the risk of atrophy of the adrenal cortex in the fetus (replacement therapy in a newborn is possible).

In extreme conditions, the absolute contraindications listed above can be considered as relative.

Side effects

From the digestive system:
■ nausea, vomiting;
■ steroid ulcers in the gastrointestinal tract;
■ bleeding from ulcers;
■ perforation of the intestinal wall;
■ pancreatitis;
■ hepatomegaly.

From the side of the central and peripheral nervous system:
■ epilepsy;
■ convulsions;
■ craniocerebral hypertension;
■ increased fatigue;
■ mood disorders;
■ psychoses;
■ dizziness;
■ headache.

From the side of the cardiovascular system:
■ bradycardia;
■ increased blood pressure;
■ arrhythmias;
■ cardiac arrest;
■ aggravation of the phenomena of heart failure;
■ myocardial dystrophy;
■ steroid vasculitis;
■ hypercoagulation;
■ thromboembolism.

From the endocrine system:
■ dysmenorrhea;
■ Itsenko-Cushing's syndrome;
■ growth retardation in children;
■ atrophy of the adrenal cortex;
■ hyperlipoproteinemia;
■ hyperglycemia;
■ steroid diabetes;
■ hirsutism;
■ adrenal insufficiency, especially during times of stress (in case of trauma, surgery, concomitant diseases).

From the side of metabolism:
■ violation of nitrogen metabolism;
■ catabolic action;
■ bulimia;
■ weight gain;
■ fluid retention, sodium;
■ hypokalemia.

From the musculoskeletal system:
■ muscle weakness;
■ steroid myopathy;
■ decrease in muscle mass;
■ osteoporotic fractures;
■ aseptic necrosis of the femoral head.

From the skin and its derivatives:
■ delayed wound healing;
■ thinning of the skin;
■ sweating;
■ flushing of the skin of the face;
■ petechiae;
■ ecchymosis;
■ striae;
■ allergic dermatitis;
■ acne.

From the side of the organ of vision:
■ development of subcapsular cataract;
■ increased intraocular pressure with possible damage to the optic nerve;
■ development of secondary viral and fungal eye diseases;
■ steroid exophthalmos. Other effects:
■ immunosuppression;
■ more frequent occurrence of infections and aggravation of the severity of their course.

When using ointments and / or creams:
■ steroid acne;
■ purpura;
■ telangiectasia;
■ burning;
■ itching;
■ irritation;
■ dry skin.

With prolonged use and / or when applied to large surfaces, systemic side effects are possible.

Interaction

Synonyms

Medopred (Cyprus), Prednisol (India), Prednisolone (Russia, Poland, Hungary, India), Prednisolone 5 mg Jenafarm (Germany), Prednisolone Nycomed (Austria), Prednisolone-AKOS (Russia), Prednisolone hemisuccinate (Russia), Prednisolone sodium phosphate (France), Prednisolone ointment (Russia)

G.M. Barer, E.V. Zoryan