Description
Latin name
Prednisolon
Release form
Solution for injection
Packing
3 pcs
Pharmacological action
Prednisone – glucocorticoid, anti-allergic, anti-inflammatory.
Pharmacodynamics
Synthetic corticosteroids with a pronounced anti-inflammatory effect (action of 5 mg of prednisolone is equivalent to 4 mg of methylprednisolone, 4 mg of triamcinolone, 0.75 mg of dexamethasone, 0.6 mg of betamethasone, 20 mg of hydrocortisone). Its mineralocorticoid effect accounts for about 60% of the activity of hydrocortisone. It inhibits the development of symptoms of inflammation. It inhibits the accumulation of macrophages, white blood cells and other cells in the area of inflammation. It inhibits phagocytosis, the release of lysosomal enzymes, as well as the synthesis and release of inflammatory mediators. Causes a decrease in capillary permeability, inhibition of white blood cell migration. It enhances the synthesis of lipomodulin, an phospholipase A2 inhibitor that releases arachidonic acid from phospholipid membranes, while inhibiting its synthesis.
Immunosuppressive effect. The mechanism is not fully understood. Prednisolone is known to reduce the number of T-lymphocytes, monocytes and acidophilic granulocytes. Reduces the binding of immunoglobulins to receptors on the cell surface and inhibits the synthesis or release of interleukins by reducing the blastogenesis of T-lymphocytes and reducing the early immunological response. It inhibits the penetration of immunological complexes through membranes and reduces the concentration of components, complement and immunoglobulins.
Effect on water-electrolyte balance. It acts on the distal part of the renal tubules, enhancing the reverse absorption of sodium and water, as well as increasing the excretion of potassium and hydrogen ions.
Other effects. It inhibits the secretion of ACTH by the pituitary gland, which leads to a decrease in the production of corticosteroids and androgens by the adrenal cortex. After prolonged use of large doses, adrenal function can recover within about a year, and in some patients there is a persistent suppression of their function.
Enhances protein catabolism and induces enzymes involved in amino acid metabolism. It inhibits the synthesis and enhances protein catabolism in the lymphatic, connective, muscle and skin tissue. With prolonged use, atrophy of these tissues may develop.
Increases blood glucose concentration by inducing gluconeogenesis enzymes in the liver, stimulating protein catabolism (which increases the number of amino acids for gluconeogenesis) and reducing glucose uptake in peripheral tissues. This leads to the accumulation of glycogen in the liver, an increase in the concentration of glucose in the blood and an increase in insulin resistance. Enhances lipolysis and mobilizes fatty acids from adipose tissue, which increases the concentration of fatty acids in serum. With prolonged treatment, redistribution of adipose tissue is possible. It inhibits the formation of bone tissue and enhances its resorption, reducing the concentration of calcium in the blood serum, which leads to secondary hyperfunction of the parathyroid glands, simultaneous stimulation of osteoclasts and inhibition of osteoblasts. These effects, together with a secondary decrease in the amount of protein components as a result of protein catabolism, can lead to inhibition of bone growth in children and adolescents and the development of osteoporosis in patients of all ages.
Enhances the action of endo- and exogenous catecholamines.
Indications for
endocrine diseases: primary adrenal cortex insufficiency (Addison’s disease) and secondary, acute adrenal cortex insufficiency, adrenogenital syndrome (congenital, adrenal cortical dysfunction), before surgery and in severe diseases and injuries in patients with acute adrenal insufficiency
severe allergic diseases resistant to other methods of treatment: contact and atopic dermatitis, serum sickness, hypersensitivity reactions lnosti drug, permanent or seasonal allergic rhinitis, anaphylaxis, angioedema
rheumatic diseases: rheumatoid arthritis, juvenile rheumatoid arthritis resistant to other therapies, psoriatic arthritis, ankylosing spondylitis, acute gouty arthritis, acute rheumatic fever, rheumatic or non-rheumatic myocarditis, dermatomyositis, systemic lupus erythematosus, giant granulomatous mesarteritis, systemic scleroderma, periarteritis nodosa, recurrent polychymrhythmitis disease, systemic dermatitis, rheumatoid disease, seborrheic dermatitis, herpetiform bullous dermatitis, severe erythema multiforme (Stevens-D syndrome Onsong), mycosis fungoides, pemphigus, severe psoriasis, severe eczema, pemphigoid
hematologic diseases: acquired autoimmune hemolytic anemia, congenital aplastic anemia, idiopathic thrombocytopenic purpura (thrombocytopenic purpura disease) in adults, anemia due to selective bone marrow hypoplasia, secondary thrombocytopenia in adults, hemolysis of
liver disease: alcoholic hepatitis with encephalopathy, chronic active hepatitis
hypercalcemia in malignant neoplasms or sarcoidosis
inflammatory diseases of the joint, acute and acute myocardial hypertrophy oncological diseases: acute and chronic leukemia, lymphomas, breast cancer, multiple myeloma, prostate cancer lezy
neurological diseases: tuberculous meningitis with subarachnoid block, multiple sclerosis in exacerbation, myasthenia
eye diseases (severe acute and chronic allergic and inflammatory processes): flaccid anterior and posterior uveitis, optic neuritis, sympathetic ophthalmia
pericarditis
respiratory diseases: bronchial asthma, berylliosis, Leffler’s syndrome, symptomatic sarcoidosis, fulminant or disseminated pulmonary tuberculosis (in combination with anti-tuberculosis chemotherapy), chronic pulmonary emphysema or and tissues for the prevention and treatment of transplant rejection in combination with other immunosuppressive drugs.
Contraindications
Hypersensitivity to prednisone and other systemic fungal infections.
Use during pregnancy and lactation
During pregnancy (especially in the first trimester), it is used only for health reasons. With prolonged therapy during pregnancy, the possibility of impaired fetal growth is not ruled out. If used in the third trimester of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.
Since corticosteroids pass into breast milk, if it is necessary to use the drug during breastfeeding, breastfeeding is recommended to be discontinued.
Composition
1 ml of the solution contains:
Active ingredient: prednisone sodium phosphate (calculated as prednisolone) 30 mg
Excipients: sodium nicotinamide disodium sodium metabisulfite edetate sodium hydroxide water for injection.
Dosage and administration of
The dose of prednisone and the duration of treatment are determined by the doctor individually depending on the indications and severity of the disease.
Prednisolone is administered in / in (drip or stream) or in / m. In / in the drug is usually administered first in a jet, 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 the complex treatment from 75 to 675 mg per treatment course from 3 to 16 days in severe cases, the dose can be increased to 1400 mg per treatment course or more with a gradual decrease in dose.
With asthmatic status, prednisone is administered at a dose of 500-1200 mg / day, followed by a decrease to 300 mg / day and a transition to maintenance doses.
With thyrotoxic crisis, 100 mg of the drug is administered in a daily dose of 200-300 mg, if necessary, the daily dose can be increased to 1000 mg. The duration of administration depends on the therapeutic effect, usually up to 6 days.
In shock resistant to standard therapy, prednisolone is usually injected at the beginning of therapy in a jet manner, after which they switch to drip. If within 10-20 minutes the blood pressure does not increase, repeat the injection of the drug. After removal from the shock state, 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 administered again after 3-4 hours. The daily dose may be 300-1200 mg (with subsequent dose reduction).
In acute hepatic-renal failure (in acute poisoning, in the postoperative and postpartum periods, etc.), Prednisolone is administered at 25-75 mg / day, if indicated, the daily dose can be increased to 300-1500 mg / day and above.
With rheumatoid arthritis and systemic lupus erythematosus, prednisolone is administered in addition to systemic administration of the drug at a dose of 75-125 mg / day for no more than 7-10 days.
In acute hepatitis, prednisone is administered at 75-100 mg / day for 7-10 days.
For poisoning by cauterizing fluids with burns to 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 IM in the same doses. After the relief of an acute condition, Prednisoloneum is prescribed inside tablets, followed by a gradual decrease in dose.
With prolonged use of the drug, the daily dose should be reduced gradually. Long-term therapy should not be stopped suddenly!
Side effects of the
From the endocrine system: decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, inhibition of adrenal gland function, Itsenko-Cushing’s syndrome (moon-shaped face, obesity of the pituitary type, hypertension, dysmenorrhea, dysmenorrhea, muscle weakness, striae), delayed 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 wall of the gastrointestinal tract, increased or decreased appetite, digestive disorders, flatulence, hiccups. In rare cases, an increase in the activity of hepatic transaminases and alkaline phosphatase.
From the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest) development (in predisposed patients) or increased severity of heart failure, changes in the electrocardiogram characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction – the spread of the focus of necrosis, slowing the formation of scar tissue, which can lead to rupture of the heart muscle.
From the nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, cerebellar pseudotumor, headache, convulsions.
From the sensory organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral infections of the eyes, trophic changes in the cornea, exophthalmos, sudden loss of vision (with parenteral administration in the head, neck, nasal concha, scalp may deposit crystals of the drug in the vessels of the eye).
From the side of metabolism: increased excretion of calcium, hypocalcemia, increased body weight, negative nitrogen balance (increased protein breakdown), increased sweating.
Caused by mineralocorticoid activity: fluid and sodium retention (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 the pineal gland), osteoporosis (very rarely pathological bone fractures, aseptic necrosis of the head of the humerus and femur), rupture of tendons of the muscles, steroid myopathy, decreased muscle masses (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 reactions.
Local for parenteral administration: burning, numbness, pain, tingling at the injection site, infection at the injection site, rarely – necrosis of surrounding tissues, scarring at the injection site, atrophy of the skin and subcutaneous tissue with i / m administration (introduction into the deltoid muscle is especially dangerous )
Other: the development or exacerbation of infections (the combined immunosuppressants and vaccination contribute to this side effect), leukocyturia, withdrawal syndrome.
Drug Interaction
Cardiac glycosides: increased risk of cardiac arrhythmias and glycoside toxicity associated with hypokalemia.
Barbiturates, antiepileptic drugs (phenytoin, carbamazepine), rifampicin, glutethimide accelerate the metabolism of GCS (by induction of microsomal enzymes), attenuate their action.
Antihistamines weaken the action of prednisolone.
Amphotericin B, carbonic anhydrase inhibitors: hypokalemia, left ventricular myocardial hypertrophy, circulatory insufficiency.
Paracetamol: hypernatremia, peripheral edema, increased calcium excretion, risk of hypocalcemia and osteoporosis. Increased risk of hepatotoxicity of paracetamol.
Anabolic steroids, androgens: increase the risk of developing peripheral edema, use acne with caution, especially in the case of liver and heart disease.
Oral contraceptives containing estrogens: increase in concentration of globulins binding glucocorticosteroids in serum, slowing of metabolism, increase of T1 / 2, increase of action of prednisolone.
Cholin blockers (basically, atropine) – increase in intraocular pressure.
Anticoagulants (coumarin derivatives, indandion, heparin), streptokinase, urokinase: reduction, and in some patients the increase in the efficacy of the dose should be determined on the basis of PV increasing the risk of ulceration and bleeding from the gastrointestinal tract.
Tricyclic antidepressants can increase the mental disorders associated with prednisolone intake. They should not be prescribed to treat these disorders.
Oral antidiabetic drugs, insulin: hypoglycemic action, increased blood glucose. Dose adjustment for anti-diabetic drugs is possible.
Antithyroid drugs, thyroid hormones – change in thyroid function (dose adjustment of these drugs or discontinuation of their administration is possible).
Diuretics: weakening of action of diuretics (potassium-sparing), hypokalemia.
Laxatives: attenuation, hypokalemia.
Ephedrine can accelerate the metabolism of ACS (prednisolone dose adjustment is possible).
Immunosuppressive drugs: increased risk of infection, lymphoma and other lymphoproliferative diseases.
Isoniazid: decreased plasma isoniazid concentration, mainly in individuals with rapid acetylation (dose change is possible).
Mexiletine: accelerate the metabolism of mexiletine and decrease its serum concentration.
Drugs that block neuromuscular conduction (depolarizing muscle relaxants): Hypocalcaemia associated with the use of prednisolone may increase the blockage of synapses, leading to an increase in the duration of neuromuscular blockade.
NSAIDs, acetylsalicylic acid, alcohol: weakening of the action, increasing the risk of developing peptic ulcer and bleeding from the gastrointestinal tract.
Sodium-containing preparations and foods: peripheral edema, arterial hypertension (it may be necessary to reduce the intake of sodium from foods and high-sodium medicines, sometimes with the use of ACS requiring additional sodium administration).
Vaccines containing live viruses: During the use of immunosuppressive doses of ACS, replication of viruses and the development of viral diseases may reduce the production of antibodies (simultaneous use is not recommended).
Other vaccines: increased risk of neurological complications and decreased antibody production.
Folic acid: increasing the need for this drug.
Overdose
The side effects described above may increase.
It is necessary to reduce the dose of Prednisolone. Treatment is symptomatic.
Storage conditions
At temperatures below 25 ° C.
Shelf suitability
3 Year
Deystvuyuschee substances
prednisone
Adzhio Farmatsevtikalz Ltd., India
