Prednisolone, solution for injection. Side effects and use of the drug Prednisolone Prednisolone side effects
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The site provides reference information for informational purposes only. Diagnosis and treatment of diseases should be carried out under the supervision of a specialist. All drugs have contraindications. Expert advice is required!
Prednisolone is a synthetic glucocorticoid hormone(glucocorticosteroid), similar in spectrum of therapeutic activity to those that are normally produced in the human body by the adrenal glands. Glucocorticosteroids, including Prednisolone, are administered orally in the form of tablets, systemically in the form of injections, and locally - the ointment is applied to the skin and eyes.Prednisolone has anti-inflammatory, anti-allergic, anti-shock, anti-exudative, anti-proliferative, antipruritic and immunosuppressive effects. These effects are very powerful and pronounced, so Prednisolone is used only for severe diseases and conditions that occur with severe inflammation, muscle spasm (for example, bronchial tubes, etc.) and profuse exudation, which are potentially life-threatening.
This drug is used only as part of complex therapy to relieve severe inflammation, edema, itching, exudation and proliferation in vasculitis, rheumatism, arthritis, myocarditis, pericarditis, dermatomyositis, scleroderma, periarteritis, bronchial asthma, Quincke's edema, Bechterew's disease, drug allergies, shock, eczema, dermatitis, hepatitis, glomerulonephritis, multiple sclerosis, pemphigus, psoriasis, systemic lupus erythematosus, leukemia, lymphogranulomatosis, tumors, inflammatory pathologies of the eye and adrenal insufficiency.
Varieties, names, forms of release and composition of Prednisolone
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Currently, doctors, pharmacists and patients under the name "Prednisolone" mean the entire set of drugs containing prednisolone as the active substance. These drugs are sold under different commercial names, many of which have been registered in the CIS countries over the past 20 years, since before that there was a practice of producing drugs containing the same active substance by various pharmaceutical plants in the cities and republics of the USSR under the same the same name. That is, for example, a drug containing prednisolone was produced at the pharmaceutical plant in Nizhny Novgorod, Samara, Tomsk and other cities, but was always sold in pharmacies under the same name "Prednisolone".
Today, many pharmaceutical factories, wanting to protect the drug they produce, register it under a different name, for example, Prednisol, Medopred, etc. This is done so that people, doctors and pharmacists can quickly find out which "prednisolone" is produced by one plant or another. This is convenient, because some drugs, for some subjective reasons, people may like more than others. Knowing the commercial name of such a "good" prednisolone, you can immediately purchase it, and not look for "Prednisolone" produced by a certain plant in pharmacies.
Today, medicines containing prednisolone are produced and sold under the following commercial names:
- Decortin H20, Decortin H5 and Decortin H50;
- Medopred;
- Prednisol;
- Prednisolone;
- prednisolone bufus;
- Prednisolone-Nycomed;
- Prednisolone-Ferein;
- prednisolone hemisuccinate;
- Prednisolone sodium metasulfobenzoate;
- Prednisolone sodium phosphate;
- Prednisolone ointment;
- Solyu-Decortin H25, Solyu-Decortin H50 and Solyu-Decortin H250.
Prednisolone preparations are available in five dosage forms:
- Tablets for oral administration;
- Solution for intravenous and intramuscular injections;
- Powder for solution for injection;
- Ointment for external use;
- Drops or suspension for the eyes.
Prednisolone - prescription
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Rep.: Tab. Prednisoloni 0.001 (or 0.005)
D.t. d. N 50 tablets
S. 1 tablet 3 times a day.
The prescription for Prednisolone ointment is as follows:
Rp.: Ung. Prednisoloni 0.5%
D.S. Apply to affected areas 1 to 2 times a day.
The prescription for Prednisolone eye drops is as follows:
Rp.: Sol. Prednisoloni 0.5%
D. S. Introduce into the conjunctival sac 1-2 drops 2-3 times a day.
The prescription for a solution for injection of Prednisolone is as follows:
Rp.: Sol. Prednisoloni 3% (30 mg/ml)
D.t. d. N 10 inamp.
S. Administer intravenously 1 to 2 times a day.
In all recipes after the letters "Rp." the name of the dosage form of the drug is indicated (Sol - solution, Ung - ointment, Tab - tablets) and the name of the drug is written in Latin (Prednisoloni). After the name of the drug, the concentration of the active substance is indicated, that is, the dosage. On the next line, after the letters "D. t." it is indicated how much the drug needs to be given to a person (for example, No. 50 intablet means that a person needs to release 50 tablets, etc.). After the letter "S" indicates how to use the drug. This prescription line is for the person who will use Prednisone.
Effects of Prednisolone (therapeutic action)
Prednisolone with systemic (tablets and injections), local (eye drops) and external use (ointment) has the following therapeutic effects:- Anti-inflammatory action, which consists in the rapid and effective relief of the inflammatory process of any localization and intensity;
- Anti-allergic effect, which consists in the rapid cessation of the development of an allergic reaction and its manifestations, such as spasm, swelling, skin rashes, etc.;
- Anti-shock action, which consists in stopping shock in order to prevent death;
- Anti-exudative action, which consists in suppressing the active process of exudation (exudation of inflammatory fluid from tissues);
- Antiproliferative action, which consists in suppressing the active reproduction of cells in the area of damage, which prevents the formation of cicatricial thickening of the walls of organs;
- Antipruritic action, which consists in eliminating the sensation of itching provoked by allergic or inflammatory reactions;
- Immunosuppressive action, which consists in suppressing the immune system and creating artificial immunodeficiency.
Since Prednisolone has a very powerful effect, it is used only in severe cases, when other drugs (for example, non-steroidal anti-inflammatory drugs, antihistamines, etc.) do not have the desired effect. If it is possible to maintain a normal state and prevent the worsening of the disease not with Prednisolone, but with other, "weaker" drugs, then this should be done in this way. The use of Prednisolone should be resorted to only in cases where other means are ineffective or a life-threatening condition has arisen (for example, Quincke's edema, anaphylactic shock, bronchospasm, etc.), which must be removed very quickly.
In addition to the listed therapeutic effects, Prednisolone is able to have the following pharmacological effects:
- Increases protein breakdown, reducing its concentration in blood plasma and tissues;
- Increases protein synthesis in the liver;
- Suppresses active growth in children by increasing the breakdown of proteins;
- Leads to the redistribution of fat, increasing its deposition on the face and upper body;
- Increases blood glucose levels;
- Retains water and sodium in the body, which contributes to the formation of edema;
- Removes potassium from the body and reduces its absorption in the intestine;
- Increases the excitability of the brain;
- Reduces the threshold of convulsive readiness, as a result of which convulsions can develop in a person more often when exposed to stimuli of relatively low strength;
- Inhibits the synthesis of own glucocorticosteroids by the adrenal glands;
- Inhibits the synthesis of thyroid-stimulating and follicle-stimulating hormone (TSH and FSH).
Indications for use
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Prednisolone in any form is intended only for relief of symptoms, therefore, it should be used as part of complex therapy aimed at curing the disease or achieving stable remission. Consider the indications for the use of each dosage form.
Indications for intravenous and intramuscular administration of Prednisolone solution
Indications for intravenous and intramuscular administration of a solution of Prednisolone are as follows:- Acute allergic reactions with severe swelling, spasm and infiltration (for example, Quincke's edema, bronchospasm, swelling and inflammation after an insect or snake bite, a large, itchy and painful skin rash, etc.);
- Asthmatic status;
- Bronchial asthma (severe form);
- Prevention and treatment of thyrotoxicosis and thyrotoxic crisis;
- Shock (burn, traumatic, surgical, toxic, cardiogenic, anaphylactic, blood transfusion);
- Anaphylactoid reactions;
- Cerebral edema caused by any cause;
- Acute adrenal insufficiency;
- Acute hepatitis;
- Acute liver failure or hepatic coma;
- Poisoning by cauterizing liquids (for example, vinegar essence, alkalis, etc.).
Indications for intra-articular administration of Prednisolone solution
Indications for intra-articular administration of a solution of Prednisolone are as follows:- Polyarthritis;
- Post-traumatic arthritis;
- Osteoarthritis of large joints (femoral, shoulder, knee, elbow, etc.);
- Arthrosis.
Indications for the use of Prednisolone tablets and intramuscular injection of the solution
Indications for the use of Prednisolone tablets and intramuscular injection of the solution are as follows:- Systemic connective tissue diseases (eg, systemic lupus erythematosus, dermatomyositis, rheumatoid arthritis, etc.);
- Acute and chronic inflammatory joint pathologies (arthritis, including psoriatic and gouty arthritis, polyarthritis, juvenile arthritis, osteoarthritis, humeroscapular periarthritis, ankylosing spondylitis, bursitis, synovitis, epicondylitis, tendosynovitis, Still's syndrome in adults);
- rheumatic fever;
- Acute rheumatic heart disease;
- Severe degrees of bronchial asthma;
- Asthmatic status;
- Acute and chronic allergic diseases (allergy to drugs and products, serum sickness, urticaria, rhinitis, angioedema, exanthema, hay fever);
- Inflammatory skin diseases (pemphigus, psoriasis, eczema, atopic, contact, exfoliative and herpetiform dermatitis, pruritus, neurodermatitis, toxidermia, seborrheic dermatitis, toxic epidermal necrolysis, Stevens-Johnson syndrome);
- swelling of the brain;
- Allergic ulceration of the cornea of the eye;
- allergic conjunctivitis;
- Inflammatory eye diseases (sympathetic ophthalmia, sluggish uveitis, optic neuritis);
- Adrenal insufficiency, including after removal of the organ;
- Congenital adrenal hyperplasia;
- Autoimmune kidney diseases (acute glomerulonephritis, nephrotic syndrome, etc.);
- Subacute thyroiditis;
- Diseases of the blood system (autoimmune hemolytic anemia, panmyelopathy, agranulocytosis, leukemia, lymphogranulomatosis, thrombocytopenic purpura, thrombocytopenia in adults, erythroblastopenia, congenital hypoplastic anemia);
- Lung diseases (acute alveolitis, fibrosis, sarcoidosis II-III degree);
- Tuberculous meningitis;
- Pulmonary tuberculosis;
- Aspiration pneumonia (provoked by the ingestion of foreign bodies, sputum, water, tissue decay products, etc. into the lungs);
- Beryllium;
- Loeffler's syndrome;
- Lung cancer;
- Chorea;
- Hepatitis;
- Pathology of the digestive tract (ulcerative colitis, Crohn's disease, enteritis);
- Prevention of rejection of organs and tissues after transplantation;
- Increased blood calcium levels in oncological diseases;
- Nausea and vomiting while taking cytostatics;
- multiple myeloma;
- Addison-Birmer disease;
- Androgenital syndrome.
Indications for the use of Prednisolone ointment
Ointment Prednisolone is indicated for use in the following diseases:- Hives;
- Atopic, seborrheic, simple and allergic dermatitis;
- Simple chronic lichen;
- Eczema;
- discoid lupus erythematosus;
- Toxidermia;
- erythroderma;
- Psoriasis;
- epicondylitis;
- tendovaginitis;
- Bursitis;
- Shoulder-shoulder periarthritis;
- Keloid scars;
- Dupuytren's contracture.
Indications for the use of eye drops Prednisolone
Eye drops Prednisolone are indicated for use in the following diseases:- Non-infectious inflammatory diseases of various parts of the eye (iritis, iridocyclitis, uveitis, episcleritis, scleritis, conjunctivitis, keratitis, blepharoconjunctivitis, blepharitis);
- allergic conjunctivitis;
- Inflammatory process in the eye caused by injuries and surgical interventions;
- Sympathetic ophthalmia.
Instructions for use
With regard to the use of any form of Prednisolone, the following simple and immutable rule should be used - use the drug at the lowest effective dose and for the shortest possible period, which is sufficient to relieve an acute condition. Remember that Prednisolone is an "acute condition" drug, and it is not intended for long-term course use due to numerous, very dangerous and severe side effects. Therefore, after stopping the acute condition with Prednisolone, you should switch to taking other drugs intended for course use.Consider the rules for using various dosage forms of Prednisolone separately.
Tablets Prednisolone - instructions for use
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At the beginning of therapy for acute and severe conditions, 50-75 mg (10-15 tablets) per day should be taken, and for chronic diseases, 20-30 mg per day (4-6 tablets). After normalization of the condition, the dosage of Prednisolone is reduced to 5-15 mg per day and the tablets continue to be taken. The duration of treatment is determined by the doctor, and depends on the general condition of the person and the effectiveness of therapy.
For children, the dosage is calculated individually by body weight, based on the ratio of 1-2 mg per 1 kg of weight to start treatment, and 0.25-0.5 mg / kg for a maintenance dose.
Prednisolone ampoules - instructions for use
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The optimal way to administer a solution of Prednisolone is intravenous injection. This means that for various diseases and conditions, the method of choice for administering the solution is intravenous. Intramuscular administration of Prednisolone should be carried out only if it is impossible to perform an intravenous injection. Intra-articular administration of Prednisolone is indicated exclusively for diseases and conditions in which tissues inside the joint are affected.
When swelling, inflammation and exudation into the joint subside, Prednisolone injections can be replaced with tablets, which should be taken until a stable remission develops.
Since normally in the human body the adrenal glands release glucocorticoid hormones into the blood between 6-00 and 8-00 in the morning, injections should be made at the same time. That is, the optimal time for the injection of the solution is the interval between 6-00 and 8-00 in the morning. It is recommended to administer the entire dosage of the hormone at a time in the morning. If for some reason it is impossible to administer the entire daily dose of Prednisolone at a time, then most of it (at least 2/3) should be administered in the morning, and the remaining amount in the afternoon (12-00).
In case of shock, 50-150 mg of Prednisolone is administered at a time (2-5 ml of a 3% (30 mg / ml) solution). Re-introduce the same amount of solution every 3-4 hours during the first day. After that, the doctor determines whether there is a need to continue injections of Prednisolone or whether they can be stopped. In acute insufficiency of the adrenal glands and liver, as well as in case of allergic reactions, 100-200 mg of Prednisolone is administered every 8 hours. In case of asthmatic status, 500-1200 mg of Prednisolone is administered once, on the second day the dosage is reduced to 300 mg, on the third day - up to 150 mg and on the fourth day - up to 100 mg. On the 5th - 6th day, Prednisolone can be canceled if the status asthmaticus has not recurred.
For children, the daily dosage is calculated individually, depending on age and body weight:
- Children 2 - 12 months - 2 - 3 mg per 1 kg of weight;
- Children 1 - 14 years old - 1 - 2 mg per 1 kg.
The dosage of Prednisolone for intra-articular administration is determined by the size of the joint:
- In large joints - 25 - 50 mg;
- In the joints of medium size - 10 - 25 mg;
- Small joints - 5 - 10 mg.
How to properly inject Prednisolone
Intravenous injection of Prednisolone is made in two ways - by jet and drip ("dropper"). Moreover, in the first hours after the development of an acute condition, Prednisolone is injected in a jet, that is, a vein is pierced, a needle is inserted into it and the solution is released from the syringe. This jetting of the solution is continued until a very rapid effect is required. After partial normalization of a person's condition, they switch to the drip administration of Prednisolone ("droppers"). To do this, the required amount of Prednisolone solution is mixed with saline in a volume of 250-500 ml and injected at a rate of 15-25 drops per minute.Intramuscular injection is made according to the general rules. That is, the solution is injected into the outer-lateral upper part of the thigh, the upper third of the shoulder, or into the stomach if the person is slender. Before injection, the injection area is wiped with an antiseptic, after which the solution is drawn into the syringe, and the needle is inserted deep into the tissues perpendicular to the skin. By pressing on the piston, the solution is released into the muscle, the needle is removed, and the skin is again wiped with an antiseptic.
Dosages of prednisolone for various diseases
The dosages of Prednisolone for various diseases in the form of a solution for injection are as follows:- Acute adrenal insufficiency - a single dose of 100 - 200 mg, daily - 300 - 400 mg;
- Severe allergic reactions - 100 - 200 mg per day for 3 - 16 days;
- Bronchial asthma - 25 - 35 mg per day for 3 - 16 days (in case of severe disease and no improvement within 2 days, the dosage can be increased to 50 - 70 mg per day);
- Asthmatic status - 500 - 1200 mg per day;
- Thyrotoxic crisis - 200 - 300 mg per day (if necessary, increase the dosage to 1000 mg) for 2 - 6 days;
- Shock - 50 - 150 mg every 4 hours for 1 - 2 days;
- Acute renal or hepatic failure - 25 - 75 mg per day;
- Rheumatoid arthritis and systemic lupus erythematosus - 75 - 125 mg per day for 7 - 10 days;
- Acute hepatitis - 75 - 100 mg per day for 7 - 10 days;
- Poisoning with caustic fluids, burns of the gastrointestinal tract and respiratory system - 75-400 mg per day for 3-18 days.
Start of reception
Start taking Prednisolone in any form (tablets and solution) for various diseases, with the exception of life-threatening conditions, should be taken from the lowest possible dosages, which, if there is no effect, increase by 25-50% daily. In case of danger to life, Prednisolone is administered immediately in the required dose.Cancellation of the drug
If the drug was taken for more than 5 days, then it should be canceled gradually so as not to provoke a withdrawal syndrome. Usually the dosage is reduced by 3 - 5 mg every 2 - 3 days, bringing it to 1 - 5 mg per day. After that, the drug is taken for another 2 to 3 days and canceled completely.Ointment Prednisolone - instructions for use
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Rules for the use of eye drops Prednisolone
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Application during pregnancy
Prednisolone during pregnancy can be used only if there is a threat to the life of the mother, since Prednisolone has a teratogenic effect. In experiments on rats and mice, the development of a cleft palate was shown in cubs born to a mother who received Prednisolone during pregnancy.When breastfeeding, Prednisolone should also not be used, since the hormone penetrates into milk and can affect the baby's body. Therefore, if it is necessary to use Prednisolone in nursing mothers, the child should be transferred to artificial mixtures.
special instructions
Prednisolone in tablets and solution is optimally administered from 6 to 8 in the morning, and during these hours you should take all or most of the daily dose (at least 2/3). If a stressful situation occurs in a person taking glucocorticoids, Prednisolone should be administered until this effect of stress has passed.If a person has suffered from psychosis in the past, then high dosages of Prednisolone should be taken only under medical supervision.
During the entire course of therapy with Prednisolone, one should undergo an examination by an ophthalmologist once a week and donate blood to determine the concentration of potassium, sodium, calcium, chlorine and glucose in plasma, as well as a complete blood count. The level of pressure should be monitored daily, and in children, the dynamics of growth and development should be additionally monitored.
When using drops, intraocular pressure and the condition of the cornea should be monitored. And Prednisolone ointment is recommended to be used simultaneously with antifungal and antibacterial agents in order to prevent infectious diseases of the skin.
Cancel Prednisolone, which was taken for more than 5 days, should always be gradual.
Against the background of therapy with Prednisolone, a person's resistance to infections decreases, therefore, if signs of the disease appear, you should consult a doctor and take the necessary antibiotics, antiviral and antifungal drugs.
Anabolic steroids, antacids and potassium preparations can be taken to reduce the severity of the side effects of Prednisolone.
Interaction with other drugs
Interaction with other drugs was noted only for tablets and solution. Ointment and eye drops do not interact with other drugs so pronounced that it is of clinical importance. So, Prednisolone in combination with other drugs has the following effects:- Cardiac glycosides, diuretics (non-potassium-sparing) - increases the excretion of potassium;
- Antidiabetic drugs - reducing the effect of lowering glucose levels;
- Coumarin - a decrease in the anticoagulant effect;
- Rifampicin - a decrease in the activity of Prednisolone;
- Acetylsalicylic acid - increases the risk of bleeding from the digestive tract.
Overdose
An overdose of Prednisolone is possible and is manifested by increased pressure, edema and increased side effects. For the treatment of acute overdose, gastric lavage is performed and sorbents are taken. For the treatment of chronic overdose, reduce the dose of prednisolone.Prednisone for children
In children, Prednisolone is used only when absolutely necessary, when there is a threat to life or a serious illness that cannot be treated with other drugs. When using tablets and a solution of Prednisolone in children under 14 years of age, an intermittent regimen should be used, which consists in taking the drug for 3 days, after which there is a break for 4 days, etc. This intermittent regimen reduces the risk of stopping the growth and development of the child. When using the ointment, it is impossible to additionally carry out activities that enhance the absorption of the drug into the blood (for example, warming up, tight bandages, etc.). Otherwise, the rules for use and precautions for children are the same as for adults.The dosage of ointment and eye drops Prednisolone for children is the same as for adults. And the dosage of tablets and solution is calculated individually depending on body weight and age. The initial dosage of tablets, which the child takes for 1-2 days to relieve an acute condition, is calculated by the ratio of 1-2 mg per 1 kg of body weight. This dosage is divided into 4 - 6 doses per day. After the acute condition returns to normal, the child is transferred to a maintenance dosage of Prednisolone, which is calculated by the ratio of 0.3-0.6 mg per 1 kg of body weight per day.
The daily dosage of the solution is calculated individually depending on the age and body weight:
- Children 2 - 12 months - 2 - 3 mg per 1 kg of weight;
- Children 1 - 14 years old - 1 - 2 mg per 1 kg;
- Over 14 years old - adult dosages.
After Prednisolone (edema, overweight)
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With sufficient perseverance in visiting the gym and regular training, many people note that even during the course of using Prednisolone, they do not gain weight. The only thing that cannot be controlled is the deposition of fat on the face with the formation of a moon-shaped shape. However, it is really almost impossible to stop the deposition of fat on the face, so you have to put up with it. Some time after stopping the use of Prednisolone, the fat from the face will go away on its own.
As for edema, they are possible only during therapy with Prednisolone. After completing the course of treatment, swelling of a person should not be disturbed if there is no disease that can provoke them. However, the deposition of fat on the face during the course of using Prednisolone leads to an increase in the amount of subcutaneous tissue in the cheeks, orbits and other parts, which fills with blood during sleep, as a result of which its mass and volume slightly increase. And it is this increased volume of the soft tissues of the face that people take for edema.
During the day, blood flows from the adipose tissue of the face under the influence of gravity, and this "edema" disappears by lunch or dinner. Many people are concerned about this "swelling", because they think that this is a symptom of some kind of trouble in the body. However, this is not true, and such behavior of the subcutaneous fatty tissue on the face is the price for life-saving treatment. With regular training and proper nutrition, a general weight loss will occur within a few months, and the amount of fatty tissue will decrease in all parts of the body, including the face. And only after that "edema" will begin to pass.
prednisone for allergies
Prednisolone for allergies is used only in cases where a person's reaction to an allergen is strong, life-threatening or the normal functioning of organs and systems, for example, bronchospasm, swelling of the airways (Quincke's edema), an excessive increase in vascular permeability, anaphylactic shock, etc. In these situations, Prednisolone should be taken in tablets or administered intravenously for 1-2 times 100-200 mg (3-6 ampoules or 20-40 tablets). After normalization of the condition and the cessation of the progression of the allergic reaction, you should switch to taking other antiallergic drugs, such as antihistamines (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 free oxygen 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 complex 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 cancellation, 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 the 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.
Application 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
Formula: C21H28O5, chemical name: (11beta)-11,17,21-Trihydroxypregna-1,4-diene-3,20-dione.
Pharmacological group: hormones and their antagonists/corticosteroids/glucocorticoids.
Pharmachologic effect: anti-inflammatory, glucocorticoid, anti-allergic, immunosuppressive, anti-shock.
Pharmacological properties
Prednisolone, interacting in the cytoplasm of the cell with specific receptors, forms a complex that penetrates into the cell nucleus, binds to DNA and causes depression or mRNA expression. All this leads to a change in the synthesis of proteins on the ribosomes that mediate cellular effects.
Prednisolone increases the formation of lipocortin, which inhibits phospholipase A2, blocks the release of arachidonic acid and the biosynthesis of prostaglandins, endoperoxide, leukotrienes (which contribute to inflammation, allergies and other pathological processes).
Prednisolone stabilizes lysosomal membranes, reduces the formation of lymphokines, and inhibits the production of hyaluronidase.
It affects the exudative and alternative phases of inflammation, preventing its spread. A decrease in the transition of monocytes to the focus of inflammation and a slowdown in the maturation of fibroblasts determine the antiproliferative effect.
Prednisolone inhibits the production of mucopolysaccharides, thereby limiting the binding of plasma proteins and water in the focus of the rheumatic inflammatory process.
Prednisolone reduces the activity of collagenase, which prevents the destruction of bones and cartilage in rheumatoid arthritis.
The antiallergic properties of prednisolone are due to a decrease in the number of basophils, direct inhibition of the release and production of mediators of an immediate allergic reaction. Prednisolone causes involution of lymphoid tissue and lymphopenia, this is due to the immunosuppressive effect. Reduces the level of T-lymphocytes in the blood, their effect on B-lymphocytes and the formation of immunoglobulins. Prednisolone reduces the production and increases the destruction of the components of the complement system, inhibits the functions of macrophages and leukocytes, and blocks the Fc receptors of immunoglobulins. Increases the number of receptors and increases (restores) their sensitivity to physiologically active substances, including catecholamines.
Prednisolone reduces plasma protein levels and the formation of a protein that binds calcium, increases protein catabolism in muscles. Promotes the synthesis of enzymes in the liver, erythropoietin, fibrinogen, lipomodulin, surfactant, triglycerides and higher fatty acids, redistribution of fat (increases the breakdown of fat in the limbs and its deposition in the upper half of the body and on the face). Prednisolone increases the resorption of carbohydrates in the gastrointestinal tract, the activity of phosphoenolpyruvate kinase and glucose-6-phosphatase, these processes lead to the release of glucose into the bloodstream and enhance gluconeogenesis. Prednisolone retains water and sodium and promotes potassium excretion due to the mineralocorticoid action. Prednisolone reduces intestinal absorption of calcium, increases its leaching from bones and excretion by the kidneys. Prednisolone has an anti-shock effect, stimulates the formation of certain cells in the bone marrow, increases the number of platelets and erythrocytes in the blood, reduces lymphocytes, monocytes, eosinophils, basophils.
When taken orally, prednisolone is well and rapidly absorbed from the gastrointestinal tract. In plasma, 70-90% of prednisolone is bound to albumin and transcortin. Tmax of prednisolone after oral administration is 1-1.5 hours. Prednisolone is oxidized mainly in the liver, to a lesser extent in the kidneys, bronchi, and small intestine. Oxidized forms of prednisolone are sulfated or glucuronidated. The half-life of prednisolone from plasma is 2-4 hours, from tissues - 18-36 hours. Prednisolone crosses the placental barrier, is excreted (less than 1% of the dose) in breast milk. Prednisolone is excreted by the kidneys, unchanged - 20%.
Indications
For parenteral administration: acute allergic reactions; status asthmaticus and bronchial asthma; therapy or prevention of thyrotoxic crisis and thyrotoxic reaction; shock (including those resistant to other treatment); acute adrenal insufficiency; myocardial infarction; acute hepatitis, cirrhosis of the liver, acute renal and hepatic failure; poisoning with caustic fluids (to reduce inflammatory reactions and prevent cicatricial constrictions). For intra-articular administration: rheumatoid arthritis, post-traumatic arthritis, spondyloarthritis, osteoarthritis (in the presence of synovitis, pronounced signs of joint inflammation). For oral administration (tablets): chronic and acute inflammatory diseases of the joints: psoriatic and gouty arthritis, polyarthritis, osteoarthritis (including post-traumatic), ankylosing spondylitis, humeroscapular periarthritis, juvenile arthritis, bursitis, Still's syndrome in adults, nonspecific tendosynovitis, epicondylitis and synovitis ; systemic connective tissue diseases (nodular periarteritis, scleroderma, systemic lupus erythematosus, rheumatoid arthritis, dermatomyositis); acute rheumatic heart disease, rheumatic fever; chronic and acute allergic diseases: allergic reactions to food and drugs, serum sickness, allergic rhinitis, urticaria, angioedema, hay fever, drug exanthema; bronchial asthma; skin diseases: psoriasis, pemphigus, eczema, diffuse neurodermatitis, atopic dermatitis, contact dermatitis (with lesions of a large skin surface), seborrheic dermatitis, toxidermia, exfoliative dermatitis, bullous dermatitis herpetiformis, toxic epidermal necrolysis, malignant exudative erythema; primary or secondary adrenal insufficiency (including conditions after removal of the adrenal glands); congenital adrenal hyperplasia; cerebral edema (including with brain tumors or associated with radiation therapy, surgery or head trauma) after prior parenteral use; subacute thyroiditis; nephrotic syndrome, kidney disease of autoimmune origin (including acute glomerulonephritis); diseases of the hematopoietic organs: panmyelopathy, agranulocytosis, congenital (erythroid) hypoplastic anemia, autoimmune hemolytic anemia, lymphogranulomatosis, acute lympho- and myeloid leukemia, myeloma, secondary thrombocytopenia in adults, thrombocytopenic purpura, erythroblastopenia; berylliosis, Leffler's syndrome (not amenable to other therapy); multiple sclerosis; lung diseases: pulmonary fibrosis, acute alveolitis, stage 3-3 sarcoidosis; pulmonary tuberculosis, tuberculous meningitis, aspiration pneumonia (together with specific chemotherapy); lung cancer (in combination with cytostatics); hepatitis; diseases of the gastrointestinal tract (to remove the patient from a critical condition): Crohn's disease, ulcerative colitis, local enteritis; nausea and vomiting in the treatment of cytostatics; hypercalcemia in cancer; inflammatory eye diseases: severe sluggish posterior and anterior uveitis, sympathetic ophthalmia, optic neuritis; allergic eye diseases: allergic forms of conjunctivitis, allergic corneal ulcers; prevention of graft rejection. For external use (ointment): atopic dermatitis, urticaria, diffuse neurodermatitis, seborrheic dermatitis, eczema, limited neurodermatitis, chronic lichen simplex, discoid lupus erythematosus, allergic and simple dermatitis, erythroderma, alopecia, toxidermia, psoriasis, epicondylitis, bursitis, tendosynovitis, humeroscapular periarthritis, sciatica, keloid scars. For eye drops: non-infectious inflammatory diseases of the anterior segment of the eye - iridocyclitis, iritis, uveitis, scleritis, episcleritis, conjunctivitis, discoid and parenchymal keratitis without damage to the corneal epithelium, blepharoconjunctivitis, allergic conjunctivitis, blepharitis, sympathetic ophthalmia, inflammatory processes after surgery and eye injuries .
Method of administration of prednisolone and doses
Prednisolone is used orally, intraarticularly, parenterally (intramuscularly and intravenously), externally. The dosage regimen and method of administration are set individually depending on the severity and nature of the disease, the patient's condition and the response to therapy. Inside (regardless of food intake, the entire dose or the main part is taken in the morning). Replacement therapy: the initial dose is 20-30 mg / day, the maintenance dose is 5-10 mg / day. Perhaps the use of prednisolone, if necessary, in higher doses. Therapy with prednisolone should be stopped under the supervision of a physician slowly, gradually lowering the dose. Children: the initial dose is 1–2 mg/kg of body weight per day for 4–6 doses, the maintenance dose is 0.3–0.6 mg/kg/day. Intravenously (usually at first in a stream, then drip), intramuscularly administered in the same doses if it is impossible to administer intravenously. Shock: single dose is 0.05-0.15 g (up to 0.4 g in severe cases), re-administered after 3-4 hours, the daily dose is 0.3-1.2 g. Acute adrenal insufficiency: single dose is 0.1–0.2 g, the daily allowance is 0.3–0.4 g. Severe allergic reactions: administered at a dose of 0.1–0.2 g / day. Asthmatic status: administered at 0.5-1.2 g / day with a further decrease in dose to 0.3-0.15-0.1 g / day. For tissue infiltration, 5 to 50 mg is injected, with Dupuytren's contracture, it is injected into the lesion. 5–10 mg is injected into small joints, 10–25 mg into medium-sized joints, and 25–50 mg into large joints. Eye drops are instilled into the conjunctival sac: 1-2 drops 3 times a day, in acute situations, instillations are made every 2-4 hours. After surgery on the eyes, prednisolone is used only on the 3-5th day after the operation. Outwardly: the ointment is applied with a thin layer 1-3 times a day on the affected skin. The duration of therapy depends on the effectiveness of treatment and the nature of the disease and is usually 6-14 days. To enhance the effect on limited foci, it is possible to use occlusive dressings.
It is necessary to use glucocorticoids for the minimum length of time needed to achieve a therapeutic effect, and in the smallest dosages. When using prednisolone, it is necessary to take into account the daily circadian rhythm of endogenous release of glucocorticoids: at 6–8 o'clock in the morning, all or the main part of the dose is prescribed. With the development of stressful situations, patients who are on treatment with corticosteroids are shown to administer parenteral corticosteroids before, during and after a stressful situation. If the patient has a history of psychosis, high doses of prednisolone are used only under the strict supervision of a physician. During therapy, especially long-term, it is necessary to carefully monitor the dynamics of development and growth in children, it is necessary to observe an oculist, control blood pressure, blood glucose levels, water and electrolyte balance, and regular analyzes of peripheral blood for cellular composition. Abrupt withdrawal of prednisolone can cause the development of acute adrenal insufficiency; with prolonged use, the drug cannot be suddenly canceled, the dose should be reduced gradually, under the supervision of a physician.
With sudden withdrawal after prolonged use, a withdrawal syndrome may develop, which is manifested by hyperthermia, arthralgia and myalgia, and malaise. These symptoms may appear even when adrenal insufficiency is not noted. Prednisolone can hide the manifestations of infectious diseases, reduce resistance to infection. When treating with eye drops, it is necessary to control the condition of the cornea and intraocular pressure. When using ointment in children from 1 year and older, it is necessary to limit the total duration of therapy and exclude activities that lead to increased absorption and resorption of prednisolone (fixing, warming and occlusive dressings). To prevent infectious skin lesions, prednisolone ointment should be used together with antifungal and antibacterial agents.
Contraindications for use
Application restrictions
No data.
Use during pregnancy and lactation
The use of corticosteroids during pregnancy is possible if the expected effects of treatment outweigh the possible risk to the fetus (there are no strictly controlled and adequate safety studies of the use of prednisolone in women during pregnancy). Women of childbearing age should be warned about the possible risk to the fetus. For newborns, mothers who took corticosteroids during pregnancy, strict control is necessary (the development of adrenal insufficiency in the newborn and fetus is possible). In many animal species that received prednisolone at doses equivalent to human doses, teratogenicity of prednisolone has been shown. During studies in pregnant rats, mice and rabbits, an increase in the incidence of development of the cleft palate in the offspring was found. Breastfeeding women should either stop breastfeeding or use prednisone (corticosteroids are excreted in breast milk and can suppress growth, endogenous corticosteroid production and cause unwanted effects in the newborn).
Side effects of prednisone
The severity and frequency of development of adverse reactions depend on the duration and method of application, the possibility of maintaining the circadian rhythm and the dose of prednisolone used.
System effects - metabolism: fluid and sodium retention in the body, hypokalemic alkalosis, hypokalemia, hyperglycemia, negative nitrogen balance due to protein catabolism, glycosuria, weight gain;
endocrine system: secondary hypothalamic-pituitary and adrenal insufficiency (especially during stressful situations such as trauma, illness, surgery), growth suppression in children, Cushing's syndrome, menstrual irregularities, manifestation of latent diabetes mellitus, decreased carbohydrate tolerance, increased need for oral antidiabetic agents or insulin in patients with diabetes mellitus;
blood and circulatory system: increase in blood pressure, increased severity or development of chronic heart failure, thrombosis, hypercoagulability, ECG changes that are characteristic of hypokalemia; in patients with subacute and acute myocardial infarction - a slowdown in the formation of scar tissue with a possible rupture of the heart muscle, the spread of a focus of necrosis, obliterating endarteritis;
support and movement system: muscle weakness, loss of muscle mass, steroid myopathy, osteoporosis, aseptic necrosis of the head of the humerus and femur, compression fracture of the spine, pathological fractures of long tubular bones;
digestive system: steroid ulcer with possible bleeding and perforation, pancreatitis, ulcerative esophagitis, flatulence, digestive disorders, nausea, increased appetite, vomiting;
skin covers: hypo - or hyperpigmentation, skin and subcutaneous atrophy, atrophic streaks, abscess, acne, thinning of the skin, delayed wound healing, ecchymosis, petechiae, increased sweating, erythema;
sense organs and nervous system: delirium, euphoria, disorientation, depression, hallucinations, increased intracranial pressure, congestive optic nerve papilla syndrome, headache, sleep disturbances, vertigo, dizziness, sudden loss of vision (when administered parenterally in the neck, head, scalp, turbinates), the formation of posterior subcapsular cataracts, glaucoma, increased intraocular pressure with possible damage to the optic nerve, steroid exophthalmos; allergic reactions: local and generalized (urticaria, allergic dermatitis, anaphylactic shock);
others: general weakness, fainting, concealment of symptoms of infectious diseases, withdrawal syndrome.
When used on the skin: steroid acne, telangiectasia, purpura, itching and burning of the skin, dryness and irritation of the skin; when applied to large surfaces and / and with prolonged use of prednisolone, systemic adverse reactions and the development of hypercortisolism are possible (in these cases, the use of the ointment is canceled); with prolonged use of the ointment, the appearance of atrophic changes, secondary infectious skin lesions, hypertrichosis is also possible.
For eye drops: with prolonged use - damage to the optic nerve, increased intraocular pressure, formation of a posterior subcapsular cataract, narrowing of the field and impaired visual acuity (loss of vision or blurring, pain in the eyes, dizziness, nausea), with thinning of the cornea there is a danger of perforation; rarely - the spread of fungal or viral eye diseases.
Interaction of prednisolone with other substances
With the combined use of prednisolone with cardiac glycosides, the risk of cardiac arrhythmias increases due to the resulting hypokalemia. Antiepileptic drugs (carbamazepine, phenytoin), barbiturates, rifampicin accelerate metabolism and, thereby, weaken the effect of glucocorticoids. The action of prednisolone is weakened by antihistamines. Thiazide diuretics, carbonic anhydrase inhibitors, amphotericin B increase the possibility of developing severe hypokalemia, sodium-containing drugs - arterial hypertension and edema. When using prednisolone with paracetamol, the risk of hepatotoxicity increases. Oral contraceptives that contain estrogens can alter the metabolism of prednisolone and its protein binding, increasing the half-life and decreasing clearance, thus enhancing the toxic and therapeutic effects of prednisolone. With the combined use of prednisolone and anticoagulants (derivatives of indandione, coumarin, heparin), it is possible to reduce the anticoagulant effect of the latter. Tricyclic antidepressants can exacerbate mental disorders that are associated with taking prednisolone. Prednisolone reduces the hypoglycemic effects of insulin and oral antidiabetic drugs. Immunosuppressants increase the possibility of developing lymphoma and other lymphoproliferative diseases, infectious diseases. Non-steroidal anti-inflammatory drugs, alcohol increase the possibility of developing peptic ulcer and bleeding from the gastrointestinal tract. During the period of use of vaccines that contain live viruses and immunosuppressive doses of glucocorticoids, a decrease in antibody production, viral replication and the development of viral diseases are possible. When using prednisolone with other vaccines, it is possible to reduce the production of antibodies and increase the risk of neurological complications. With prolonged use, prednisolone increases the content of folic acid. Prednisolone increases the possibility of electrolyte disturbances when taken together with diuretics.
Overdose
The possibility of an overdose of prednisolone increases with prolonged use, especially at high doses. With an overdose of prednisolone, peripheral edema appears, blood pressure rises, and other side effects of prednisolone increase. In case of acute overdose, it is necessary: immediate induction of vomiting or gastric lavage, symptomatic therapy; there is no specific antidote. In case of chronic overdose of prednisolone, it is necessary to reduce the dose of the drug.
GKS. Suppresses the functions of leukocytes and tissue macrophages.
drug: prednisolone
The active substance of the drug:
prednisolone
ATX encoding: S01BA04
KFG: GCS for topical use in ophthalmology
Registration number: P No. 015942/01
Date of registration: 05.05.06
The owner of the reg. honor.: WARSAW PHARMACEUTICAL WORK POLFA S.A. (Poland)
Release form Prednisolone, drug packaging and composition.
Eye drops in the form of a white suspension.
1 ml
prednisolone acetate
5 mg
5 ml - colorless glass dropper bottles (1) - packs of cardboard.
DESCRIPTION OF THE ACTIVE SUBSTANCE.
All the information provided is provided only for familiarization with the drug, you should consult a doctor about the possibility of using it.
Pharmacological action Prednisolone
GKS. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of inflammation. Violates the ability of macrophages to phagocytosis, as well as to the formation of interleukin-1. Contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of inflammation. Reduces capillary permeability due to the release of histamine. Suppresses the activity of fibroblasts and the formation of collagen.
Inhibits the activity of phospholipase A2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce the production of prostaglandins.
Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed into the lymphoid tissue; inhibits the formation of antibodies.
Prednisolone inhibits the release of pituitary ACTH and β-lipotropin, but does not reduce the level of circulating α-endorphin. Inhibits the secretion of TSH and FSH.
When applied directly to the vessels, it has a vasoconstrictor effect.
Prednisolone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys, and increases the activity of gluconeogenesis enzymes. In the liver, prednisolone enhances the deposition of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from protein metabolism products. An increase in blood glucose stimulates the secretion of insulin.
Prednisolone inhibits the uptake of glucose by fat cells, which leads to the activation of lipolysis. However, due to an increase in insulin secretion, lipogenesis is stimulated, which contributes to the accumulation of fat.
It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone, it affects the processes of water-electrolyte metabolism: it promotes the excretion of potassium and calcium ions, the retention of sodium and water ions in the body. Osteoporosis and Itsenko-Cushing's syndrome are the main factors limiting long-term therapy with corticosteroids. As a result of the catabolic action, growth suppression in children is possible.
In high doses, prednisolone can increase the excitability of brain tissue and help lower the seizure threshold. Stimulates excess production of hydrochloric acid and pepsin in the stomach, which leads to the development of peptic ulcers.
With systemic use, the therapeutic activity of prednisolone is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.
With external and local application, the therapeutic activity of prednisolone is due to anti-inflammatory, anti-allergic and anti-exudative (due to the vasoconstrictor effect) action.
Compared with hydrocortisone, the anti-inflammatory activity of prednisolone is 4 times greater, and the mineralocorticoid activity is 0.6 times less.
Pharmacokinetics of the drug.
When taken orally, it is well absorbed from the gastrointestinal tract. Cmax in plasma is observed after 90 minutes. In plasma, most prednisolone binds to transcortin (cortisol-binding globulin). It is metabolized mainly in the liver.
T1 / 2 is about 200 minutes. Excreted by the kidneys unchanged - 20%.
Indications for use:
For oral and parenteral use: rheumatism; rheumatoid arthritis, dermatomyositis, periarteritis nodosa, scleroderma, Bechterew's disease, bronchial asthma, status asthmaticus, acute and chronic allergic diseases, anaphylactic shock, Addison's disease, acute adrenal insufficiency, adrenogenital syndrome; hepatitis, hepatic coma, hypoglycemic conditions, lipoid nephrosis; agranulocytosis, various forms of leukemia, lymphogranulomatosis, thrombocytopenic purpura, hemolytic anemia; chorea; pemphigus, eczema, itching, exfoliative dermatitis, psoriasis, pruritus, seborrheic dermatitis, lupus erythematosus, erythroderma, alopecia.
For intra-articular administration: chronic polyarthritis, post-traumatic arthritis, osteoarthritis of large joints, rheumatic lesions of individual joints, arthrosis.
For infiltration introduction into tissues: epicondylitis, tendovaginitis, bursitis, humeroscapular periarthritis, keloids, sciatica, Dupuytren's contracture, rheumatic and similar lesions of the joints and various tissues.
For use in ophthalmology: allergic, chronic and atypical conjunctivitis and blepharitis; inflammation of the cornea with intact mucosa; acute and chronic inflammation of the anterior segment of the choroid, sclera and episclera; sympathetic inflammation of the eyeball; after injuries and operations with prolonged irritation of the eyeballs.
Dosage and method of application of the drug.
When taken orally for replacement therapy in adults, the initial dose is 20-30 mg / day, the maintenance dose is 5-10 mg / day. If necessary, the initial dose can be 15-100 mg / day, maintenance - 5-15 mg / day. The daily dose should be reduced gradually. For children, the initial dose is 1-2 mg / kg / day in 4-6 doses, the maintenance dose is 300-600 mcg / kg / day.
When administered intramuscularly or intravenously, the dose, frequency and duration of use are determined individually.
With intra-articular injection into large joints, a dose of 25-50 mg is used, for joints of medium size - 10-25 mg, for small joints - 5-10 mg. For infiltration administration into tissues, depending on the severity of the disease and the size of the affected area, doses from 5 to 50 mg are used.
Locally in ophthalmology, they are used 3 times / day, the course of treatment is no more than 14 days; in dermatology - 1-3 times / day.
Side effects of prednisone:
From the endocrine system: menstrual disorders, suppression of adrenal function, Itsenko-Cushing's syndrome, suppression of the function of the pituitary-adrenal system, decreased carbohydrate tolerance, steroid diabetes or the manifestation of latent diabetes mellitus, growth retardation in children, delayed sexual development in children.
From the digestive system: nausea, vomiting, steroid ulcer of the stomach and duodenum, pancreatitis, esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases, an increase in the activity of hepatic transaminases and alkaline phosphatase.
From the side of metabolism: negative nitrogen balance due to protein catabolism, increased excretion of calcium from the body, hypocalcemia, weight gain, increased sweating.
From the side of the cardiovascular system: loss of potassium, hypokalemic alkalosis, arrhythmia, bradycardia (up to cardiac arrest); steroid myopathy, heart failure (development or worsening of symptoms), ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.
From the musculoskeletal system: growth retardation and ossification processes in children (premature closure of the epiphyseal growth zones), osteoporosis (very rarely, pathological fractures, aseptic necrosis of the head of the humerus and femur), rupture of muscle tendons, muscle weakness, steroid myopathy, reduction muscle mass (atrophy).
From the side of the central nervous system: headache, increased intracranial pressure, delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, nervousness or anxiety, insomnia, dizziness, vertigo, cerebellar pseudotumor, convulsive seizures.
On the part of the organ of vision: posterior subcapsular cataract, increased intraocular pressure (with possible damage to the optic nerve), trophic changes in the cornea, exophthalmos, a tendency to develop a secondary infection (bacterial, fungal, viral).
Dermatological reactions: petechiae, ecchymosis, thinning and fragility of the skin, hyper- or hypopigmentation, acne, striae, a tendency to develop pyoderma and candidiasis.
Reactions due to immunosuppressive action: slowing down regeneration processes, reducing resistance to infections.
With parenteral administration: in isolated cases, anaphylactic and allergic reactions, hyper- or hypopigmentation, atrophy of the skin and subcutaneous tissue, exacerbation after intrasynovial use, Charcot-type arthropathy, sterile abscesses, when injected into lesions on the head - blindness.
Contraindications to the drug:
For short-term use for health reasons - hypersensitivity to prednisone.
For intra-articular injection and injection directly into the lesion: previous arthroplasty, pathological bleeding (endogenous or caused by the use of anticoagulants), intra-articular bone fracture, infectious (septic) inflammatory process in the joint and periarticular infections (including history), as well as common infectious disease, severe periarticular osteoporosis, no signs of inflammation in the joint (“dry” joint, for example, in osteoarthritis without synovitis), severe bone destruction and joint deformity (sharp narrowing of the joint space, ankylosis), joint instability as an outcome of arthritis, aseptic necrosis of the joint joint of the epiphyses of bones.
For external use: bacterial, viral, fungal skin diseases, skin tuberculosis, skin manifestations of syphilis, skin tumors, post-vaccination period, violation of the integrity of the skin (ulcers, wounds), children's age (up to 2 years, with itching in the anus - up to 12 years), rosacea, acne vulgaris, perioral dermatitis.
For use in ophthalmology: bacterial, viral, fungal eye diseases, eye tuberculosis, trachoma, violation of the integrity of the eye epithelium.
Use during pregnancy and lactation.
During pregnancy (especially in the first trimester), they are used only for health reasons. If necessary, use during lactation should carefully weigh the expected benefits of treatment for the mother and the risk to the child.
Special instructions for the use of Prednisolone.
Use with caution for 8 weeks before and 2 weeks after vaccination, with lymphadenitis after BCG vaccination, with immunodeficiency states (including AIDS or HIV infection).
Use with caution in diseases of the gastrointestinal tract: peptic ulcer of the stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis.
Use with caution in diseases of the cardiovascular system, incl. after a recent myocardial infarction (in patients with acute and subacute myocardial infarction, the focus of necrosis may spread, slowing down the formation of scar tissue and, as a result, rupture of the heart muscle), with decompensated chronic heart failure, arterial hypertension, hyperlipidemia), with endocrine diseases - diabetes mellitus ( including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, with severe chronic renal and / or hepatic insufficiency, nephrourolithiasis, with hypoalbuminemia and conditions predisposing to its occurrence, with systemic osteoporosis, myasthenia gravis, acute psychosis , obesity (III-IV degree), with poliomyelitis (with the exception of the form of bulbar encephalitis), open- and angle-closure glaucoma.
If necessary, intra-articular administration should be used with caution in patients with a general severe condition, ineffectiveness (or short duration) of the action of 2 previous injections (taking into account the individual properties of the GCS used).
During treatment (especially long-term), it is necessary to observe an ophthalmologist, control blood pressure and water and electrolyte balance, as well as pictures of peripheral blood, blood glucose; in order to reduce side effects, you can prescribe anabolic steroids, antibiotics, and also increase the intake of potassium in the body (diet, potassium supplements). It is recommended to clarify the need for the introduction of ACTH after a course of treatment with prednisolone (after a skin test!).
In Addison's disease, simultaneous use with barbiturates should be avoided.
After discontinuation of treatment, withdrawal syndrome, adrenal insufficiency, as well as an exacerbation of the disease, for which prednisolone was prescribed, may occur.
With intercurrent infections, septic conditions and tuberculosis, simultaneous antibiotic therapy is necessary.
In children during the period of growth, GCS should be used only according to absolute indications and under the close supervision of a physician.
Outwardly should not be used for more than 14 days. In the case of use in acne vulgaris or rosacea, an exacerbation of the disease is possible.
Interaction of Prednisolone with other drugs.
With the simultaneous use of prednisolone with anticoagulants, it is possible to increase the anticoagulant effect of the latter.
With simultaneous use with salicylates, the likelihood of bleeding increases.
With simultaneous use with diuretics, aggravation of electrolyte disturbances is possible.
With simultaneous use with hypoglycemic drugs, the rate of decrease in blood glucose levels decreases.
With simultaneous use with cardiac glycosides, the risk of developing glycoside intoxication increases.
With simultaneous use with rifampicin, a weakening of the therapeutic effect of rifampicin is possible.
With the simultaneous use of antihypertensive drugs, their effectiveness may decrease.
With the simultaneous use of coumarin derivatives, the anticoagulant effect may be weakened.
With the simultaneous use of rifampicin, phenytoin, barbiturates, the effect of prednisolone may be weakened.
With the simultaneous use of hormonal contraceptives - increased action of prednisolone.
With the simultaneous use of acetylsalicylic acid - a decrease in the content of salicylates in the blood.
With the simultaneous use of praziquantel, a decrease in its concentration in the blood is possible.
The appearance of hirsutism and acne contributes to the simultaneous use of other corticosteroids, androgens, estrogens, oral contraceptives and anabolic steroids. The risk of developing cataracts increases with the use of antipsychotics, carbutamide and azathioprine against the background of GCS.
Simultaneous administration with m-anticholinergics (including antihistamines, tricyclic antidepressants), nitrates contributes to the development of an increase in intraocular pressure.
Dosage form:  solution for intravenous and intramuscular administration Compound:1 ml of the drug contains:
active substance:
prednisolone sodium phosphate (in terms of prednisolone) 30 mg;Excipients: sodium hydrogen phosphate (anhydrous sodium hydrogen phosphate) 0.5 mg, sodium dihydrogen phosphate dihydrate 0.35 mg, propylene glycol 150 mg, water for injection up to 1 ml.
Description:Clear or slightly opalescent, colorless or slightly colored liquid.
Pharmacotherapeutic group:glucocorticosteroid ATX:  H.02.A.B.06 Prednisolone
Pharmacodynamics:Prednisolone is a synthetic glucocorticosteroid drug, a dehydrated analogue of hydrocortisone. It has anti-inflammatory, anti-allergic, desensitizing, anti-shock, anti-toxic and immunosuppressive effects.
Suppresses the release of pituitary beta-lipotropin, but does not reduce the concentration of circulating beta-endorphin. It inhibits the secretion of thyroid-stimulating hormone (TSH) and follicle-stimulating hormone (FSH). Increases the excitability of the central nervous system (CNS), reduces the number of lymphocytes and eosinophils, increases - erythrocytes (stimulates the production of erythropoietins).
Interacts with cytoplasmic glucocorticosteroid (GSC) receptors and forms a complex that penetrates the cell nucleus and stimulates mRNA synthesis; the latter induces the formation of proteins, including lipocortin, mediating cellular effects. Lipocortin inhibits phospholipase A2, inhibits the release of arachidonic acid and inhibits the synthesis of endoperoxides, prostaglandins (Pg), leukotrienes, which promote inflammation, allergies, and more.
Protein metabolism: reduces the amount of globulins in plasma, increases the synthesis of albumin in the liver and kidneys (with an increase in the albumin / globulin ratio in blood plasma), reduces the 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); contributes to the development of hyperglycemia.
Water-electrolyte exchange: retains sodium ions and water in the body, stimulates the excretion of potassium ions (mineralocorticoid activity), reduces the absorption of calcium ions from the gastrointestinal tract, reduces the mineralization of bone tissue.
Anti-inflammatory effect 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.
Immunosuppressive effect caused by the involution of lymphoid tissue, inhibition of the proliferation of lymphocytes (especially T-lymphocytes), suppression of B-lymphocyte 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 a decrease in antibody formation.
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 formation, changes in the body's immune response.
For obstructive airways disease 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 mucous membrane. 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 adrenocorticotropic hormone and secondarily - the synthesis of endogenous glucocorticosteroids.
Antishock and antitoxic action associated with an increase in blood pressure (due to an increase in the concentration of circulating catecholamines and the restoration of adrenoreceptor sensitivity to them, as well as vasoconstriction), a decrease in the permeability of the vascular wall, membrane-protective properties, and activation of liver enzymes involved in the metabolism of endo- and xenobiotics.
It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
Pharmacokinetics:Up to 90% of prednisolone binds to plasma proteins: transcortin (corticosteroid-binding globulin) and 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. Excreted through the intestines and kidneys by glomerular filtration and 80-90% reabsorbed by the tubules, 20% of the dose is excreted by the kidneys unchanged. The plasma half-life after intravenous administration is 2-3 hours.
Indications:Prednisolone is taken for emergency therapy in conditions requiring a rapid increase in the concentration of glucocorticosteroids in the body:
Shock (burn, traumatic, surgical, toxic, cardiogenic) - with the ineffectiveness of vasoconstrictors, plasma-substituting drugs and other symptomatic therapy;
Allergic reactions (acute severe forms), hemotransfusion shock, anaphylactic shock, anaphylactoid reactions;
Cerebral edema (including against the background of a brain tumor or associated with surgery, radiation therapy, or head trauma);
Bronchial asthma (severe form), astatic status;
Systemic connective tissue diseases (systemic lupus erythematosus, rheumatoid arthritis);
Acute adrenal insufficiency;
thyrotoxic crisis;
Acute hepatitis, hepatic coma;
Reducing inflammation and preventing cicatricial narrowing (in case of poisoning with caustic fluids).
Contraindications:For short-term use for health reasons, the only contraindication is hypersensitivity to prednisolone or the components of the drug.
In children during the period of growth, glucocorticosteroids should be used only according to absolute indications and under the most careful supervision of the attending physician.
Carefully:The drug should be prescribed for the following diseases and conditions:
Diseases of the gastrointestinal tract - peptic ulcer of the stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis;
Pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination;
Immunodeficiency states (including acquired immunodeficiency syndrome (AIDS) or human immunodeficiency virus (HIV infection);
Diseases of the cardiovascular system (including recent
myocardial infarction - in patients with acute and subacute myocardial infarction, a focus of necrosis may spread, a slowdown in the formation of scar tissue and, as a result, a rupture of the heart muscle), decompensated chronic heart failure, arterial hypertension,
hyperlipidemia);
Endocrine diseases - diabetes mellitus (including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, stage III-IY obesity);
Severe chronic renal and / or liver failure,
nephrourolithiasis;
Hypoalbuminemia and conditions predisposing to its occurrence;
Systemic osteoporosis, myasthenia gravis, acute psychosis, poliomyelitis (with the exception of the form of bulbar encephalitis), open and angle-closure glaucoma;
Pregnancy.
Pregnancy and lactation:During pregnancy, the drug is used only in cases where the potential benefit to the mother outweighs the potential risk to the fetus.
Since glucocorticosteroids pass into breast milk, if it is necessary to use the drug during breastfeeding, it is recommended to stop breastfeeding.
Dosage and administration:Intravenously, the drug is usually administered first by jet, repeated injections are carried out by drip.
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.
In acute adrenal insufficiency a single dose of the drug is 100-200 mg, daily - 300-400 mg.
For severe allergic reactions prednisolone is administered at a daily dose of 100-200 mg for 3-16 days.
With bronchial asthma the drug is administered at a dose of 75 mg to 675 mg for a course of treatment 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.
For status asthmaticus administered at a dose of 500-1200 mg per day, followed by a decrease to 300 mg per day and the transition to maintenance doses.
With thyrotoxic crisis 100 mg of the drug 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.
For shock refractory to standard therapy, at the beginning of therapy, they are usually injected in a jet, after which they switch 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). Repeatedly the drug is administered after 3-4 hours. The daily dose can be 300-1200 mg (with subsequent dose reduction).
In acute hepatic-renal failure (with acute poisoning, in the postoperative and postpartum periods, etc.) enter 25-75 mg per day; if indicated, the daily dose can be increased to 300-1500 mg per day and above.
For rheumatoid arthritis and systemic lupus erythematosus administered in addition to the systemic administration of the drug at a dose of 75-125 mg per day for no more than 7-10 days.
For acute hepatitis administered at 75-100 mg per day for 7-10 days. In case of poisoning with caustic fluids with burns of the digestive tract and upper respiratory tract, it is prescribed at a dose of 75-400 mg per day for 3-18 days.
If intravenous administration is not possible administered intramuscularly in the same doses. After stopping the acute condition, it 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 from 2 to 12 months - 2-3 mg / kg, from 1 to 14 years - 1-2 mg / kg intramuscularly; administered intravenously slowly (within 3 minutes). If necessary, this dose can be repeated after 20-30 minutes.
Side effects:The frequency of development and severity of side effects depends on the duration of use, the size of the dose used and the possibility of observing the circadian rhythm of prednisone administration.
From the endocrine system: decreased glucose tolerance, "steroidal" diabetes mellitus or manifestation of latent diabetes mellitus, adrenal suppression, Itsenko-Cushing's syndrome (moon face, pituitary-type 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 wall of the gastrointestinal tract, increased or decreased appetite, indigestion, flatulence, hiccups. In rare cases, an increase in the activity of "liver" transaminases and alkaline phosphatase.
From the side of 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, hypercoagulability, thrombosis. In patients with acute and subacute myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.From the side of 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 sense organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos, sudden loss of vision.
From the side of metabolism: increased excretion of calcium, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating.
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 musculoskeletal system: growth retardation and ossification processes in children (premature closure of the epiphyseal growth zones), osteoporosis (very rarely, pathological bone fractures, aseptic necrosis of the head of the humerus and femur), muscle tendon rupture, "steroid" myopathy, decreased muscle mass (atrophy).
From the skin and mucous membranes: delayed wound healing, 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 reactions with 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 intramuscular injection (especially dangerous is the introduction into the deltoid muscle).
When administered intravenously: arrhythmias, flushes of blood to the face, convulsions.
Others: development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination), leukocyturia, "withdrawal" syndrome.
Overdose:May increase dose-dependent side effects. It is necessary to reduce the dose of prednisolone.
Treatment: symptomatic.
Interaction:Pharmaceutical incompatibility of prednisolone with other intravenously administered drugs is possible - it is recommended to administer it separately from other drugs (intravenous bolus, or through another dropper, as a second solution). When mixing a solution of prednisolone with heparin, a precipitate forms.
Prednisolone increases the toxicity of cardiac glycosides (due to the resulting hypokalemia, the risk of developing arrhythmias increases).
Accelerates the excretion of acetylsalicylic acid, reduces its concentration in the blood (with the abolition of prednisolone, the concentration of salicylates in the blood increases and the risk of side effects increases).
When used simultaneously with live antiviral vaccines and against the background of other types of immunizations, it increases the risk of virus activation and the development of infections.
Increases the metabolism of isoniazid, mexiletine (especially in "fast acetylators"), which leads to a decrease in their plasma concentrations.
Increases the risk of developing hepatotoxic reactions of paracetamol (induction of "liver" enzymes and the formation of a toxic metabolite of paracetamol).
Increases (with prolonged therapy) the content of folic acid. Hypokalemia caused by glucocorticosteroids can increase the severity and duration of muscle blockade against the background of muscle relaxants.
In high doses, it reduces the effect of somatropin.
Prednisolone reduces the effect of hypoglycemic drugs; enhances the anticoagulant effect of coumarin derivatives.
Weakens the effect of vitamin D on the absorption of calcium ions in the intestinal lumen.
Ergocalciferol and parathyroid hormone prevent the development of osteopathy caused by glucocorticosteroids.
Reduces the concentration of praziquantel in the blood.
Cyclosporine (inhibits metabolism) and (reduces clearance) increase toxicity.
Thiazide diuretics, carbonic anhydrase inhibitors, other glucocorticosteroids and amphotericin B increase the risk of hypokalemia, sodium-containing drugs - edema and increased blood pressure.
Non-steroidal anti-inflammatory drugs (NSAIDs) and increase the risk of ulceration of the mucous membrane of the gastrointestinal tract (GIT) and bleeding, in combination with non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment of arthritis, it is possible to reduce the dose of glucocorticosteroids due to the summation of the therapeutic effect.
Indomethacin, displacing from the connection with albumin, increases the risk of its side effects.
Amphotericin B and carbonic anhydrase inhibitors increase the risk of osteoporosis.
The therapeutic effect of glucocorticosteroids is reduced under the influence of phenytoin, barbiturates, ephedrine, theophylline, rifampicin and other inducers of microsomal liver enzymes (increased metabolic rate).
Mitotan and other inhibitors of adrenal function may necessitate an increase in the dose of glucocorticosteroids.
The clearance of glucocorticosteroids increases against the background of thyroid hormones.
Immunosuppressants increase the risk of developing infections and lymphoma or other lymphoproliferative disorders caused by the Epstein-Barr virus.
Estrogens (including oral estrogen-containing contraceptives) reduce the clearance of glucocorticosteroids, prolong the half-life and their therapeutic and toxic effects.
The appearance of hirsutism and acne is facilitated by the simultaneous use of other steroid hormonal drugs - androgens, estrogens, anabolics, oral contraceptives.
Tricyclic antidepressants may increase the severity of depression caused by taking glucocorticosteroids (not indicated for the treatment of these side effects).
The risk of developing cataracts increases when used in combination with other glucocorticosteroids, antipsychotic drugs (neuroleptics), carbutamide and azathioprine.
Simultaneous administration with m-anticholinergics (including antihistamines, tricyclic antidepressants with m-anticholinergic activity), nitrates contributes to the development of an increase in intraocular pressure.
Special instructions:During treatment with prednisolone (especially long-term), it is necessary to observe an ophthalmologist, control blood pressure, the state of water and electrolyte balance, as well as pictures of peripheral blood and blood glucose levels.
In order to reduce side effects, you can prescribe antacids, as well as increase the intake of potassium ions in the body (diet, potassium preparations). Food should be rich in proteins, vitamins, with limited content of fats, carbohydrates and salt.
The effect of the drug is enhanced in patients with hypothyroidism and cirrhosis of the liver. The drug may increase existing emotional instability or psychotic disorders. When indicating a history of psychosis, high doses are prescribed under the strict supervision of a physician.
Caution should be used in acute and subacute myocardial infarction - it is possible to spread the focus of necrosis, slow the formation of scar tissue and rupture the heart muscle.
In stressful situations during maintenance treatment (for example, surgery, trauma or infectious diseases), the dose of the drug should be adjusted due to an increase in the need for glucocorticosteroids.
With sudden cancellation, especially in the case of previous use of high doses, the development of a "withdrawal" syndrome (anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness) is possible, as well as an exacerbation of the disease for which it was prescribed. During treatment with prednisolone, vaccination should not be carried out due to a decrease in its effectiveness (immune response). When prescribing for intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously treat with bactericidal antibiotics.
In children during the period of growth, glucocorticosteroids should be used only according to absolute indications and under the most careful supervision of the attending physician. Children who during the period of treatment were in contact with patients with measles or chickenpox are prescribed specific immunoglobulins prophylactically.
Due to the weak mineralocorticoid effect for replacement therapy in adrenal insufficiency, it is used in combination with mineralocorticoids.
In patients with diabetes mellitus, blood glucose levels should be monitored and, if necessary, therapy should be adjusted.
X-ray control of the osteoarticular system (spine, hand) is shown.
Prednisolone in patients with latent infectious diseases of the kidneys and urinary tract can cause leukocyturia, which may be of diagnostic value.
Prednisolone increases the content of 11- and 17-hydroxyketocorticosteroid metabolites.
Influence on the ability to drive transport. cf. and fur.:During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.
Release form / dosage:Solution for intravenous and intramuscular administration, 30 mg/ml.
Package:1 ml solution in neutral glass ampoules.
10 ampoules with instructions for use and a knife for opening ampoules or an ampoule scarifier are placed in a cardboard box.
5 or 10 ampoules are placed in a blisters of polyvinyl chloride film or polyethylene terephthalate tape and aluminum foil or polyethylene-coated paper or without foil or without paper.
1 or 2 blister packs with instructions for use and a knife for opening ampoules or an ampoule scarifier are placed in a pack of cardboard.
When packing ampoules with a break ring or a break point, a knife for opening ampoules or an ampoule scarifier is not included.
Storage conditions:In a place protected from light at a temperature not exceeding 15 ° C.
Keep out of the reach of children.
Best before date: Do not use after the expiry date stated on the packaging. Conditions for dispensing from pharmacies: On prescription Registration number: Close Instructions