Prednisolone - instructions for use, reviews, analogs and formulations (1 mg and 5 mg tablets, injections for injections, eye drops, 0.5% ointment) for the treatment of shock conditions in adults, children and pregnancy
In this article, you can read the instructions for the use of a medicinal hormone drug Prednisolone. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Prednisolone in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of prednisolone in the presence of existing structural analogues.Use for the treatment of shock and urgent conditions, allergic reactions, inflammatory manifestations in adults, children, as well as during pregnancy and lactation.
Prednisolone - a synthetic glucocorticoid drug, a dehydrated analog of hydrocortisone. Has anti-inflammatory, antiallergic, immunosuppressive action, increases the sensitivity of beta-adrenoreceptors to endogenous catecholamines.
Interacts with specific cytoplasmic receptors (receptors for GCS are present 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 the plasma, increases the synthesis of albumins in the liver and kidneys (with increasing albumin / globulin ratio), reduces synthesis and enhances protein catabolism in muscle tissue.
Lipid metabolism: increases 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 digestive 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 metabolism: retards sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces absorption of calcium from the digestive tract, reduces the mineralization of bone tissue.
The 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. Effects on all stages of the inflammatory process: inhibits the synthesis of prostaglandins at the level of arachidonic acid (lipocortin depresses phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endopersides, leukotrienes,inflammatory cytokines "(interleukin 1, tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors.
Immunosuppressive effect is caused by induced lymphoid tissue involution, suppression of lymphocyte proliferation (especially T-lymphocytes), suppression of B-cell 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 in the formation of antibodies.
The 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,prevention or reduction of the degree of edema of the mucous membranes, a 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 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 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
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%.
Indications
- shock conditions (burn, traumatic, operational, toxic, cardiogenic) - with ineffectiveness of vasoconstrictors, plasmal replacement drugs and other symptomatic therapy;
- allergic reaction (acute severe), transfusion shock, anaphylactic shock, anaphylactoid reactions;
- brain edema (including on the background of a brain tumor or associated with surgery, radiation therapy, or head injury);
- bronchial asthma (severe form), asthmatic status;
- systemic connective tissue disease (systemic lupus erythematosus, scleroderma, polyarteritis nodosa, dermatomyositis, rheumatoid arthritis);
- acute and chronic inflammatory diseases of the joints - gouty and psoriatic arthritis, osteoarthritis (including post-traumatic), polyarthritis, humeropathy periarthritis, ankylosing spondylitis (Bechterew's disease), juvenile arthritis, Still's syndrome in adults, bursitis, nonspecific tenosynovitis, synovitis and epicondylitis ;
- skin diseases - pemphigus, psoriasis, eczema, atopic dermatitis (common atopic dermatitis), contact dermatitis (affecting a large skin surfaces), drug reaction, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), bullous herpetiformis dermatitis, Stevens-Johnson syndrome ;
- allergic eye diseases: allergic forms of conjunctivitis;
- inflammatory diseases of the eyes - sympathetic ophthalmia, severe sluggish anterior and posterior uveitis, optic neuritis;
- congenital adrenal hyperplasia;
- blood diseases and hematopoiesis system - agranulocytosis, panmyelopathy, autoimmune hemolytic anemia, acute lympho- and myeloid leukemia, lymphogranulomatosis, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocyte anemia), congenital (erythroid) hypoplastic anemia;
- berylliosis, Leffler's syndrome (not susceptible to other therapy); lung cancer (in combination with cytostatics);
- multiple sclerosis;
- prevention of graft rejection during organ transplantation;
- hypercalcemia on the background of cancer, nausea and vomiting during cytostatic therapy;
- myeloma;
- thyrotoxic crisis;
- acute hepatitis, hepatic coma;
- Reduction of inflammatory phenomena and prevention of cicatricial narrowing (with poisoning by cauterizing fluids).
Forms of release
Tablets 1 mg and 5 mg.
Solution for intravenous and intramuscular injection (injections in ampoules for injection) 30 mg / ml.
Eye drops 0.5%.
Ointment for external use 0,5%.
Instructions for use and dosage
Injections
The dose of Prednisolone and the duration of treatment are set by the doctor individually, depending on the indications and severity of the disease.
Prednisolone is administered intravenously (by drip or jet) in droppers or intramuscularly. In / in the preparation is usually injected first with a stream, then drip.
In acute adrenal insufficiency, a single 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 to 675 mg for a course of treatment of 3 to 16 days; in severe cases, the dose may be increased to 1,400 mg per treatment course and more with a gradual dose reduction.
With asthmatic status Prednisolone 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 is usually injected at the start of the therapy, after which it is switched to a drop introduction.If the BP does not increase within 10-20 minutes, repeat the fluid administration of the drug. After excretion from the shock state, the drip administration continues until the BP stabilizes. Single dose is 50-150 mg (in severe cases - up to 400 mg). Repeated drug is administered after 3-4 hours. The daily dose can be 300-1200 mg (with a subsequent dose reduction).
In acute hepatic-renal failure (acute poisoning, postoperative and postpartum periods, etc.), prednisolone is administered at 25-75 mg per day; in the presence of indications, the daily dose can be increased to 300-1500 mg per day or more.
In rheumatoid arthritis and systemic lupus erythematosus Prednisolone 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.
In acute hepatitis Prednisolone 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 is prescribed in a dose of 75-400 mg per day for 3-18 days.
If it is impossible to / in the introduction of prednisolone is administered in / m in the same doses. After relief of acute condition, Prednisolone is given intravenously in tablets, followed by a gradual decrease in dose.
With prolonged use of the drug, the daily dose should be reduced gradually. Long-term therapy can not be stopped suddenly!
Pills
The entire daily dose of the drug is recommended to take a single or double daily dose every other day, taking into account the circadian rhythm of the endogenous secretion of glucocorticosteroids in the interval from 6 to 8 am. A high daily dose can be divided into 2-4 doses, with a large dose taken in the morning. Tablets should be taken orally during or immediately after meals, with a small amount of liquid.
In acute conditions and as a replacement therapy, adults are prescribed in an initial dose of 20-30 mg per day, the maintenance dose is 5-10 mg per day. If necessary, the initial dose can be 15-100 mg per day, supporting - 5-15 mg per day.
For children, the initial dose is 1-2 mg / kg of body weight per day in 4-6 receptions, supporting - 300-600 mcg / kg per day.
When the therapeutic effect is obtained, the dose is gradually reduced by 5 mg, then by 2.5 mg at intervals of 3-5 days, canceling at a later time. With prolonged use of the drug, the daily dose should be reduced gradually.Long-term therapy can not be stopped suddenly! The withdrawal of the maintenance dose is slower the longer the glucocorticosteroid therapy is used.
In case of stressful influences (infection, allergic reaction, trauma, surgery, mental overload), the dose of prednisolone should be temporarily increased (in 1.5-3, and in severe cases - 5-10 times) in order to avoid exacerbation of the underlying disease.
Side effect
- decreased glucose tolerance;
- Steroid diabetes mellitus or manifestation of latent diabetes mellitus;
- oppression of adrenal function;
- Isenko-Cushing syndrome (lunar face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae);
- delay in sexual development in children;
- nausea, vomiting;
- steroid ulcer of the stomach and duodenum;
- erosive esophagitis;
- gastrointestinal bleeding and perforation of the gastrointestinal wall;
- increased or decreased appetite;
- indigestion;
- flatulence;
- hiccough;
- arrhythmias;
- bradycardia (up to cardiac arrest);
- ECG changes characteristic of hypokalemia;
- increased blood pressure;
- disorientation;
- euphoria;
- hallucinations;
- affective insanity;
- depression;
- paranoia;
- increased intracranial pressure;
- nervousness or anxiety;
- insomnia;
- dizziness;
- headache;
- convulsions;
- increased intraocular pressure with possible damage to the optic nerve;
- propensity to develop secondary bacterial, fungal or, viral infections of the eyes;
- trophic changes of the cornea;
- increased excretion of calcium;
- weight gain;
- increased sweating;
- fluid and sodium retention in the body (peripheral edema);
- hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue);
- slowing growth and ossification processes in children (premature closure of epiphyseal growth zones);
- osteoporosis (very rare - pathological bone fractures, aseptic necrosis of the head of the humerus and femur);
- rupture of muscle tendons;
- decrease in muscle mass (atrophy);
- delayed healing of wounds;
- acne;
- stria;
- skin rash;
- itching;
- anaphylactic shock;
- development or exacerbation of infections (the emergence of this side effect is facilitated by jointly used immunosuppressants and vaccination);
- withdrawal syndrome.
Contraindications
For short-term use according to vital indications, the only contraindication is hypersensitivity to prednisolone or the components of the drug.
The preparation contains lactose. Patients with rare hereditary diseases, such as lactose intolerance, Lappease lactase deficiency or glucose-galactose malabsorption, should not take the drug.
With caution, the drug should be administered in the following conditions and conditions:
- gastrointestinal diseases - peptic ulcer of stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with perforation or abscessing threat, diverticulitis;
- parasitic and infectious diseases of a viral, fungal or bacterial nature (ongoing or recent, including recent contact with a patient)
- herpes simplex, herpes zoster (viremic phase), chicken pox, measles; amebiasis, strongyloidiasis; systemic mycosis; active and latent tuberculosis.The use in severe infectious diseases is permissible only against the background of specific therapy;
- pre-and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency conditions (including AIDS or HIV infection);
- diseases of the cardiovascular system, incl. the recently transferred myocardial infarction (in patients with acute and subacute myocardial infarction it is possible to spread the focus of necrosis, slow the formation of scar tissue and, as a result, break the heart muscle), decompensated chronic heart failure, hypertension, hyperlipidemia;
- endocrine diseases - diabetes mellitus (including a violation of carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease, obesity (3-4 items);
- severe chronic renal and / or hepatic insufficiency, nephrourolythiasis;
- hypoalbuminemia and conditions predisposing to its occurrence (cirrhosis of the liver, nephrotic syndrome);
- systemic osteoporosis, myasthenia gravis, acute psychosis, poliomyelitis (except for the form of bulbar encephalitis), open and closed angle glaucoma;
- pregnancy;
- in children during growth, glucocorticosteroids should be used only in absolute indications and under the close supervision of the treating physician.
Application in pregnancy and lactation
At pregnancy (especially in 1 trimester) apply only on vital indications.
Since glucocorticosteroids pass into breast milk, if it is necessary to use the drug during breastfeeding, it is recommended to stop breastfeeding.
special instructions
Before the beginning of treatment (if it is impossible due to the urgency of the condition - during the treatment), the patient should be examined for possible contraindications. Clinical examination should include the examination of the cardiovascular system, radiographic examination of the lungs, examination of the stomach and duodenum, urinary system, vision; the control of the formula of blood, the content of glucose and electrolytes in the blood plasma. During treatment with prednisolone (especially prolonged), it is necessary to observe the oculist, control the blood pressure, the state of the water-electrolyte balance, as well as the patterns of peripheral blood and blood glucose levels.
In order to reduce side effects, it is possible to prescribe antacids, and also to increase the intake of potassium 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 is prescribed under the strict supervision of a physician.
In stressful situations during maintenance treatment (for example, surgical operations, trauma or infectious diseases), a correction of the dose of the drug should be made in connection with an increase in the need for glucocorticosteroids.
Patients should be carefully observed during the year after the end of long-term therapy with prednisolone in connection with the possible development of a relative insufficiency of the adrenal cortex in stressful situations.
With sudden cancellation, especially in the case of previous use of high doses, it is possible to develop withdrawal syndrome (anorexia, nausea, blocking, gyneralized musculoskeletal pain, general weakness), as well as an exacerbation of the disease for which prednisolone was prescribed.
During treatment with prednisolone, vaccination should not be given due to a decrease in its effectiveness (immune response).
When prescribing prednisolone in intercurrent infections, septic states and tuberculosis, it is necessary to simultaneously perform antibiotic treatment with bactericidal action.
Children during prolonged treatment with prednisolone should carefully monitor the dynamics of growth. Children who were in contact with sick measles or chickenpox during the treatment period prophylactically prescribe specific immunoglobulins.
Due to the weak mineralocorticoid effect for substitution therapy for adrenal insufficiency, prednisolone is used in combination with mineralocorticoids.
Patients with diabetes should monitor blood glucose and, if necessary, correct therapy.
An x-ray control of the osteoarticular system (images of the spine, hands) is shown.
Prednisolone in patients with latent infectious diseases of the kidneys and urinary tract can cause leukocyturia, which can have diagnostic value.
In Addison's disease, simultaneous administration of barbiturates should be avoided - the risk of acute adrenal insufficiency (addisonic crisis).
Drug Interactions
Simultaneous appointment of prednisolone with inducers of hepatic microsomal enzymes (phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration.
Simultaneous prescription of prednisolone with diuretics (especially thiazide and inhibitors of carbonic anhydrase) and amphotericin B can lead to increased excretion of potassium from the body.
Simultaneous prescription of prednisolone with sodium-containing drugs leads to the development of edema and increased blood pressure.
The simultaneous administration of prednisolone with amphotericin B increases the risk of developing heart failure.
Simultaneous prescription of prednisolone with cardiac glycosides worsens their tolerability and increases the likelihood of developing ventricular extrasystole (due to induced hypokalemia).
Simultaneous prescription of prednisolone with indirect anticoagulants - prednisolone enhances the anticoagulant effect of coumarin derivatives.
Simultaneous prescription of prednisolone with anticoagulants and thrombolytics increases the risk of bleeding from ulcers in the gastrointestinal tract.
Simultaneous prescription of prednisolone with ethanol (alcohol) and non-steroidal anti-inflammatory drugs increases the risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding (in combination with NSAIDs in the treatment of arthritis, a decrease in the dose of glucocorticosteroids due to the summation of the therapeutic effect) is possible.
Simultaneous prescription of prednisolone with Paracetamol increases the risk of hepatotoxicity (induction of hepatic enzymes and the formation of a toxic metabolite of paracetamol).
Simultaneous prescription of prednisolone with Acetylsalicylic acid accelerates its excretion 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).
Simultaneous prescription of prednisolone with insulin and oral hypoglycemic drugs, hypotensive drugs reduces their effectiveness.
Simultaneous prescription of prednisolone with vitamin D reduces its effect on the absorption of Ca in the intestine.
Simultaneous prescription of prednisolone with a somatotropic hormone reduces the effectiveness of the latter, and with praziquantel - its concentration.
Simultaneous prescription of prednisolone with m-holinoblokatorami (including antihistamines and tricyclic antidepressants) and nitrates contributes to increased intraocular pressure.
Simultaneous prescription of prednisolone with Isoniazid and mexiletine increases the metabolism of isoniazid, mexiletine (especially in "fast" acetylators), which leads to a decrease in their plasma concentrations.
Simultaneous prescription of prednisolone with inhibitors of carbonic anhydrase and amphotericin B increases the risk of osteoporosis.
Simultaneous prescription of prednisolone with Indomethacin - displacing prednisolone from bond with albumin, increases the risk of its side effects.
Simultaneous prescription of prednisolone with ACTH increases the effect of prednisolone.
The simultaneous administration of prednisolone with ergocalciferol and parathyroid hormone interferes with the development of osteopathy caused by prednisolone.
Simultaneous prescription of prednisolone with cyclosporine and Ketoconazole - cyclosparin (inhibits metabolism) and ketoconazole (lowers clearance) increases toxicity.
The emergence of hirsutism and acne is facilitated by the simultaneous use of other steroid hormonal drugs (androgens, estrogens, anabolic, oral contraceptives).
The simultaneous administration of prednisolone with estrogens and oral estrogen-containing contraceptives reduces the clearance of prednisolone, which may be accompanied by an increase in the severity of its therapeutic and toxic effects.
The simultaneous administration of prednisolone with 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 immunization increases the risk of virus activation and the development of infections.
With simultaneous use of prednisolone with antipsychotic drugs (neuroleptics) and azathioprine, the risk of developing cataracts increases.
Simultaneous administration of antacids reduces the absorption of prednisolone.
With simultaneous use with antithyroid drugs is reduced, and with thyroid hormones, the clearance of prednisolone increases.
When used simultaneously with immunosuppressants, the risk of infection and lymphoma or other lymphoproliferative disorders associated with the Epstein-Barr virus increases.
Tricyclic antidepressants can increase the severity of depression caused by taking glucocorticosteroids (not shown for the therapy of these side effects).
Increases (with prolonged therapy) the content of folic acid.
Hypokalemia caused by glucocorticosteroids may increase the severity and duration of muscle blockade against the background of muscle relaxants.
In high doses reduces the effect of somatropin.
Analogues of the drug Prednisolone
Structural analogs for the active substance:
- Decortin H20;
- Decortin H5;
- Decortin H50;
- Medomobred;
- Prednisol;
- Prednisolone 5 mg of Jenafarm;
- Prednisolone buff;
- Prednisolone hemisuccinate;
- Prednisolone Nycomed;
- Prednisolone-Ferein;
- Prednisolone sodium phosphate;
- Sol-Decortin H25;
- Solu-Decortin H250;
- Sol-Decortin H50.
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