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

active substance:
prednisolone sodium phosphate	40.32 mg
(in terms of prednisolone)	30 mg
Excipients:
disodium edetate dihydrate (Trilon B)	0.5 mg
sodium hydrophosphate (sodium phosphate disubstituted)	2.3 mg
sodium dihydrogen phosphate dihydrate (sodium phosphate monosubstituted 2-water)	0.34 mg
propylene glycol	0.25 ml
water for injections	up to 1 ml

Description:

Transparent, colorless or slightly colored solution, practically odorless.

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, immuno-depressant effect, increases the sensitivity of beta-adrenoreceptors to endogenous catecholamines:

It interacts with cytoplasmic receptors of glucocorticosteroids (GCS) (there are GGC receptors in all tissues, especially in the liver), with the formation of a complex inducing the formation of proteins (including enzymes that regulate vital processes in cells).

Protein metabolism: reduces the number of globulins in plasma, increases the synthesis of albumin in the liver and kidneys (fromyourthe coefficient of albumin / globulin in 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: delays sodium ions (Na⁺) and water in the body, stimulates the excretion of potassium ions (K⁺) (mineralocorticoid activity), reduces the absorption of calcium ions (Ca²⁺) 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. It works on all stages of the inflammatory process: it inhibits the synthesis of prostaglandins at the level of arachidonic acid (lipocortin oppresses phospholipase, A2,suppresses the release of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, promoting inflammation processes, allergies, etc.), the synthesis of "pro-inflammatory cytokines" (interleukin-1, tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors.

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 (ACTH) and again - the synthesis of endogenous glucocorticosteroids.

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 with bile and urine by glomerular filtration and is reabsorbed by tubules by 80-90%. 20% of the dose is excreted by the kidneys unchanged. Half-life from the plasma after intravenous administration is 2-3 hours.

Indications:

Prednisolone is used 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 reactions (acute severe forms), hemotransfusion shock, anaphylactic shock, anaphylactoid reactions;

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

- bronchial asthma (severe form), asthmatic status;

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

acute adrenocortical insufficiency;

- thyrotoxic crisis;

acute hepatitis, hepatic coma;

- Reduction of inflammatory phenomena and prevention of cicatricial narrowing (when poisoning with 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:

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

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

- parasitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently transferred, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles; amebiasis, 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 AIDS or HIV infection).

- diseases of the cardiovascular system (including 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 a violation of carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease, obesity (III-IV century);

- severe chronic renal and / or hepatic insufficiency, nephrourolythiasis;

- hypoalbuminemia and conditions predisposing to its occurrence;

- systemic osteoporosis, myasthenia 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.

Dosing and Administration:

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. Prednisolone buffus is administered intravenously (by drip or jet) or by intramuscular injection. Intravenously, the drug is usually injected first with a stream, then drip.

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

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

With bronchial asthma and asthmatic status, the drug is administered from 75 to 675 mg for a course of treatment from 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 bufus is administered at a dose of 500-1200 mg per day, followed by a decrease to 300 mg per day and transition to maintenance doses.

In thyrotoxic crisis, 100 mg of the drug are 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 the case of shock resistant to standard therapy, prednisolone bufus is usually injected at the beginning of therapy, repeated injections are performed by drip.If within 10-20 minutes the arterial pressure does not increase, repeat, the jet injection of the drug. After excretion from the shock state, drip administration continues until blood pressure stabilizes. Single dose is 50-150 mg (in severe cases - up to 400 mg). Repeated drug is administered after 3-4 hours. The daily dose can be 300 to 1200 mg (with a subsequent dose reduction).

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

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

When poisoning with cauterizing liquids with burns of the digestive tract and upper respiratory tract prednisolone bufus appoint a dose of 75-400 mg per day for 3-18 days.

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

If intravenous administration is not possible, prednisolone boufus is administered intramuscularly in the same doses. After relief of acute condition is prescribed inside Prednisolone in tablets, followed by a gradual decrease in the dose.With prolonged use of the drug, the daily dose should be reduced gradually. Long-term therapy can not be stopped suddenly!

Side effects:

When applying Prednisolone, bufus may be noted:

From the endocrine system: depression of glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal cortex function, Itenko-Cushing syndrome (lunar face, pituitary obesity, hirsutism, increased 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 and hiccough. 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 foci of necrosis, slowing down, 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 infections of the eyes, trophic corneal changes, exophthalmos, sudden loss of vision (local reactions during parenteral administration in the head, neck, scalp may be deposited crystals of the drug in the vessels of the eye).

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

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

From the side of the musculoskeletal system: growth retardation and ossification processes, in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely pathological bone fractures, aseptic necrosis of the head of the humerus and thigh bone), rupture of 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, a tendency to develop pyoderma and candidiasis.

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

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

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

Overdose:It is possible to increase dose-dependent side effects. It is necessary to reduce the dose of prednisolone boufus.

Treatment: symptomatic.

Interaction:

The pharmaceutical incompatibility of prednisolone with other intravenously administered drugs is possible. It is recommended that it be administered separately from other drugs (intravenously bolus or via another drip as a second solution). When mixing the solution of prednisolone with heparin a precipitate forms.

The simultaneous administration of prednisolone with:

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

- diuretics (especially "thiazide" and inhibitors carbonic anhydrase) and amphotericin B - can lead to increased elimination from the body of potassium ions (K +) and an increased risk of developing heart failure;

- with sodium-containing preparations - to the development of edema and increased blood pressure;

- cardiac glycosides their tolerability worsens and the likelihood of developing ventricular extrasitolia increases (due to induced hypokalemia);

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

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

- ethanol and non-steroidal anti-inflammatory drugs (NSAIDs) - the risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding increases (in combination with NSAIDs, a reduction in the dose of glucocorticosteroids due to the summation of the therapeutic effect is possible in the treatment of arthritis);

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

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

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

- vitamin D - its effect on the absorption of calcium ions decreases (Ca²⁺) in the intestine;

- Growth hormone - It reduces the effectiveness of the latter, and with praziquantel - its concentration;

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

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

Inhibitors of carbonic anhydrase and looped diuretics can increase the risk of osteoporosis.

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

Adrenocorticotropic hormone enhances the effect of prednisolone.

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

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

Simultaneous use of androgens and steroid anabolic drugs with prednisolone promotes the development of peripheral edema and hirsutism, the appearance of acne.Estrogens and oral estrogen-containing contraceptives reduce the clearance of prednisolone, which may be accompanied by an increase in the severity of its action.

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

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

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

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

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

Immunosuppressants increase the risk of developing injections and lymphomas or other lymphoproliferative disorders caused by the Epstein-Barr virus.

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

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, antacids can be prescribed, as well as increased intake of K⁺ in 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 Prednisolone should not be vaccinated 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 prolonged treatment with prednisolone, careful monitoring of the dynamics of growth and development is necessary. 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 in adrenocortical 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 content of 11- and 17-oxyketocorticosteroids.

Before using, it is necessary to read the information on the opening of polymer ampoules (see thematic pictures on the drug package):

1. Separate the plastic ampoule.

2. Turn the valve and open the plastic ampoule.

3. Insert the cannula of the syringe without the needle into the opening of the ampoule.

4. Type the contents of the ampoule into the syringe.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions, due to side effects when the drug is used, namely, the drug may cause dizziness.

Form release / dosage:

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

Packaging:

1 ml per ampoule polymer from polyethylene or polypropylene.

By 3, 5, 10, 100 ampoules of polymer with instructions for use are put in a cardboard pack.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-000945

Date of registration:18.10.2011

The owner of the registration certificate:UPDATE OF PFC, CJSC UPDATE OF PFC, CJSC Russia

Manufacturer: & nbsp

UPDATE, PFC CJSC Russia

Representation: & nbspUPDATE OF PFC, CJSCUPDATE OF PFC, CJSC

Information update date: & nbsp28.08.2015

Illustrated instructions

Instructions

Prednisolone bufus (Prednisolon bufus)