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From what the drug prednisolone 5 mg. Instructions for use of prednisolone

"Prednisolone" is a universal medicine of hormonal origin, which helps in cases where other medicines are ineffective. It is prescribed to many patients with the most various pathologies However, the use of the drug without the permission of a doctor is strictly prohibited.

The hormonal drug has several forms of release and is always selected on an individual basis.

  1. Pills. This is an oral tablet. They act systemically, are included in the metabolism inside the body. The active substance is absorbed into the bloodstream through digestive tract, previously passing through the capillaries of the villi of the small intestine.
  2. Solution. This is liquid "Prednisolone" in ampoules, which is necessary for injections. The drug works by analogy with tablets, acting systemically. The main difference, which will serve as an advantage, is the fastest possible absorption into the blood.
  3. Ointment. This form is intended for local effects on the focus of inflammation. This is the safest version of the drug, since the internal blood flow is practically not involved in the distribution and excretion of the drug.
  4. Drops. Another option for local use, which is prescribed to patients in the treatment of organs of vision.

Regardless of the form, the active substance is always the same. It is the hormone prednisolone, which provides an anti-inflammatory effect.

Additional ingredients may vary. So, tablets necessarily contain a base - silicon dioxide, starch, lactose. The composition of the ointment, along with the hormone, will include paraffin, glycerin, emulsifiers and parabens. Solution for injection is a mixture hormonal substance and additional ingredients sterile water, sodium hydroxide, sodium metabisulphite and nicotinamide.

Pharmacological action, pharmacodynamics and pharmacokinetics

To understand what hormonal drugs are used for, you need to consider their mechanism of action. It does not matter how exactly the active substance will enter the body. The drug always works on the same principle.

The hormone begins to interact with receptors inside cells (mainly in liver tissues). As a result, the synthesis of specific proteins is initiated. Then the targeted suppression of inflammatory processes begins at any stage of their development.

Prednisolone has a positive effect on the patient's condition, since during its use it is observed:

  • increasing the resistance of cell membranes to damage;
  • normalization of the exchange of water and dissolved electrolytes;
  • suppression of histamine synthesis;
  • reduction in the number of mast cells;
  • decrease in the number of antibodies.

As a result hormonal drug suppresses inflammation in any part of the body. By analogy, local means also work. They are applied to the affected area and block the formation of histamine, which leads to the rapid suppression of allergic manifestations.

What is Prednisolone used for?

The hormonal drug can rightly be called multifunctional and universal. It is used when various pathologies even in advanced forms.

The list of indications includes:

  • rheumatic fever;
  • any inflammation of the joint space;
  • multiple sclerosis;
  • pneumonia;
  • tuberculosis;
  • meningitis;
  • adrenal hyperplasia;
  • nephrotic syndrome;
  • inflammation of the digestive tract;
  • leukemia;
  • hypoglycemia;
  • swelling of the brain.

These pathologies require the use of a systemic drug. The doctor prescribes injections or tablets in the dosage appropriate for the age and severity of the disease.

Ointment "Prednisolone" has a slightly different list of indications. It helps with allergic reactions and other skin lesions, in particular with psoriasis or eczema. Doctors advise using the drug if dermatitis is diagnosed, which manifests itself as severe itching, turning into a burning sensation, the appearance of a rash, redness, swelling of tissues.

Instructions for use and dosage

The drug is prescription, so it will not be possible to purchase it without a doctor's prescription.

The regimen is also discussed with the doctor in advance in order to avoid addiction and, as a result, a decrease in the effectiveness of the drug. Each form of release has its own nuances, which will certainly be taken into account by a specialist.

Tablets Prednisolone 1 mg and 5 mg

The remedy in the form of tablets is taken orally strictly according to the scheme proposed by the doctor. The volume of the dose will depend primarily on the age of the patient. So, adults should receive 23 - 30 mg of the hormone daily. If we are talking about maintenance therapy, then the amount is reduced to 5-10 mg per day.

The amount of medicine for children is significantly reduced. The daily dose is 1-2 mg of the drug for every kilogram of the child's body. You can divide the amount received into 5-6 receptions.

Solution for intravenous and intramuscular administration

Injections "Prednisolone" are given not only intramuscularly, but also intraarticularly. Intravenous administration of a hormonal drug is also provided if a quick positive effect is required. This method is necessary when severe conditions. The patient is drip-injected 1-2 g of the hormone every day for 3-5 days. Average duration one procedure - 30 minutes.

In all other cases, the drug is injected into the muscle or directly into the area of ​​the affected joint. The dose for children is 1-3 mg/kg. Adult patients receive 30-1200 mg per day, depending on the severity of the pathology.

Important. The hormone prednisolone is best administered in morning time(from 6 to 8 hours). It is during this period that cortisol, the lack of which is covered by prednisolone, is produced especially actively.

Eye drops 0.5%

When using drops, there should be no difficulties. The patient must carry out instillations. Do this three times a day, burying liquid solution(1 or 2 drops) under the lower eyelid. After the procedure, it is recommended to sit with your eyes closed for a short time. An increase in the number of eye treatments is possible after an ophthalmic operation.

Ointment for external use 0.5%

The agent in the format of an ointment is applied directly to the affected area with a thin layer. Repeat the treatment is allowed up to three times a day. Fixation with a gauze bandage is possible.

During pregnancy and breastfeeding

The drug belongs to the group of teratogenic. This means that when using it, the risk of developing abnormalities in the development of the fetus increases. This fact becomes the basis for the prohibition of treatment with "Prednisolone" during the bearing of the baby. Exception is a vital necessity.

Worth refraining from hormonal medication and while breastfeeding. Lactation during therapy is canceled, and the child is transferred to the mixture selected by the pediatrician. About being able to resume breastfeeding the doctor will tell.

drug interaction

Prescribing a medication is always done by a doctor, and the specialist should be aware of whether any other medications are being taken, since their interaction with the hormone can lead to a worsening of the patient's condition.

  1. When combined with non-steroidal anti-inflammatory drugs, the risk of negative impact on the mucous membranes of the gastrointestinal tract - the patient may develop gastritis or an ulcer may worsen.
  2. At simultaneous reception with paracetamol, the load on the liver increases. Perhaps the partial destruction of its cells.
  3. When combined with immunosuppressants, suffers natural defense organism, and it becomes exposed to pathogenic microbes.
  4. Using oral contraceptives increased toxicity of "Prednisolone".
  5. When used in conjunction with diuretics, an electrolyte imbalance develops.

You can avoid negative consequences if you warn the doctor in a timely manner about the use of any medications.

Alcohol compatibility

"Prednisolone" for allergies or inflammatory processes is a fast-working and highly effective remedy, however, if the patient takes alcohol, positive result will not be.

In addition, it has been proven that when the active substance interacts with ethyl alcohol the toxic effect on the organs involved in the excretion of the spent drug is enhanced, in particular, on the kidneys and liver. These structures of the body undergo negative changes, some of their cells die, after which they cannot cope with the functions assigned to them in full.

Doctors provide information that alcohol can enhance side effects from taking a hormonal agent, therefore, for the period of therapy, it is best to refuse to drink any alcohol-containing drinks, even in small quantities.

Contraindications, side effects and overdose

Doctors call a number of conditions in which the use of drugs based on prednisolone is strictly prohibited.

This list includes:

  • myocardial infarction;
  • peptic ulcer;
  • infectious diseases of a bacterial or fungal nature;
  • hyperlipidemia;
  • pathology of the endocrine system;
  • urolithiasis disease;
  • glaucoma;
  • acute psychosis;
  • insufficiency of the liver and kidneys;
  • obesity;
  • lactation and pregnancy.

In all these cases, the drug can be prescribed, provided that it is necessary to maintain life.

Side effects from hormone treatment usually occur when using systemic forms of action - tablets or injection solution.

The list of unwanted manifestations includes:

At long-term use overdose is possible with increased volumes of the drug. She manifests characteristic symptoms- increased pressure, edema and the development of pronounced side effects.

Drug analogues

Hormonal preparations are not always used to treat allergies or inflammatory processes in tissues. In some cases, it is appropriate to use funds from the NSAID group. These are powerful but safe non-steroidal drugs.

The list of the most famous includes:

  • "Diclofenac";
  • "Ibuprofen";
  • "Naproxen";
  • "Indomethacin".

If none of the listed remedies helps to improve the condition, then doctors prescribe analogues of Prednisolone, which contain hormones.

The list of effective ones includes:

  • "Hydrocortisone";
  • "Dexamed";
  • "Medrol";
  • "Betamethasone";
  • "Metipred".

The decision to use any hormonal drug is always made by the doctor, taking into account the intended benefit to the patient and his initial condition. This is the only way to quickly achieve a positive effect.

In case of allergic reactions, inflammation of the joints or tissues, doctors prescribe Prednisolone - the instructions for use include the information necessary for the patient. The drug is available in four different forms: tablets, ointments, solution for intravenous administration, ophthalmic suspension. Familiarize yourself with the procedure for using a glucocorticoid medication.

What is prednisolone

According to pharmacological classification, Prednisolone belongs to the group synthetic glucocorticoids. It is used topically or internally. Prednisolone - instructions for use indicate its indications, which differ a wide range, contraindications, possible side effects. A medication is used to treat inflammation, the effects of allergies.

Composition and form of release

Prednisolone is available in four popular forms, each with a different composition. Only the active active ingredient, prednisolone sodium phosphate, remains unchanged. The instruction indicates its amount in terms of prednisone. Detailed composition medicines:

Release form

Pills

Injection

Ocular suspension

For 1 pc. 5 mg

0.5 g per 100 g

Per 1 ml 30 mg

5 mg per 1 ml

Excipients

Sucrose, glucose, lactose monohydrate, gelatin, calcium stearate monohydrate, potato starch

Distilled glycerin, medical vaseline, stearic acid, emulsifier, nipagin, nipazole, water

Nicotinamide, sodium metabisulphite, disodium edetate, sodium hydroxide, water

Purified water

Package

10, 20, 30, 50 or 60 pcs. in blisters or jars

Tube 15 ml

3 ampoules in plastic trays and cardboard boxes, 1 ml in one ampoule

Transparent glass bottles 5 ml with a dropper dispenser

Description

White flat cylindrical shape

Ointment texture

Transparent, colorless

white suspension

Pharmacodynamics and pharmacokinetics

Prednisolone - instructions for its use indicate that the composition includes synthetic hormones cortisone and hydrocortisone secreted by the adrenal cortex. The drug does not cause fluid and salt retention, slightly increases the excretion of potassium. Hydrocortisone analogue has the following actions:

  1. Shows anti-inflammatory activity - the components of the drug penetrate into the nucleus of cells, enhance the synthesis of lipocortin inhibitors infectious diseases and reduce the synthesis of prostaglandins - sources of inflammation, have an immunosuppressive effect.
  2. Antiproliferative action - inhibits DNA synthesis inside the cells of the basal layer and fibroblasts of the dermis.
  3. Antiallergic effect - reduces the number of basophils, inhibits the synthesis and production of biologically active substances.
  4. Antishock, antiexudative, antitoxic effects, affects antibodies.

When taken orally, the active ingredients are well absorbed by the gastrointestinal tract, the maximum concentration in the blood is reached 1.5 hours after consumption. 90% of the absorption of prednisolone occurs in plasma. Biotransformation of the hydrocortisone analog occurs by oxidation within the liver. Metabolic products are excreted in urine or feces. An immunosuppressive drug with an anti-inflammatory effect is able to penetrate the placental barrier.

Indications for use

Instructions for use indicate the following indications of use medicinal product- a synthetic analog of the hormone of the adrenal cortex:

Method of application and dosage

Depending on the chosen format of the drug, the method of administration and dosage is set. Tablets and solution are applied orally, ointment - topically, eye drops are used only to treat eye diseases. The doctor prescribes an analogue of the adrenal hormone individually, depending on the characteristics of the patient, the severity of the course of the disease. The course is also set individually.

Tablets Prednisolone

On the recommendation of a doctor, it is necessary to drink Prednisolone tablets in a single or double daily dose every other day, taking into account the rhythm of the production of glucocorticosteroids in the range of 6-8 hours. The daily dose can be divided into 2-4 doses, a small dosage is prescribed in the morning. Tablets are taken during or after meals. Treatment should not be stopped suddenly. In stressful conditions, the dosage can be increased by 1.5-3 times or 5-10 times per day. severe cases.

At acute currents diseases and in substitution treatment, adults take 20-30 mg / day, the maintenance dose is 5-10 mg / day. Your doctor may prescribe 15-100 mg/day as an initial dose or 5-15 mg/day as a maintenance dose. hormone therapy. Children from three years of age are shown 1-2 mg per kg of body weight per day, divided into 4-6 doses. The maintenance dose for children is 0.3-0.6 mg/kg. After obtaining the effect, the dose is reduced to 5 mg, then 2.5 mg at intervals of 3-5 days.

Ointment

The cream version is applied externally for itchy skin, allergic rashes. Apply the cream in a thin layer 2-3 times a day. The ointment can be used in gynecology - with combined treatment with antibiotics and antifungal agents. The course of treatment lasts about 6-14 days, maintenance therapy involves applying the ointment once a day.

Prednisolone solution

A common form of release of the drug is a solution for injection. Prednisolone is administered intravenously, intraarticularly or intramuscularly under strict sterile conditions. Intra-articular injections involve the introduction of 10 mg of hydrocortisone in small joints, 25 mg in medium and 50 mg in large. It can be repeated multiple times. After that, the doctor evaluates the severity of the effect. With its deficiency, the issue of increasing the dose is decided.

In shock, Prednisolone is administered intravenously slowly or dropwise in an amount of 30-90 mg. In other cases, the dose ranges from 30-45 mg. If the introduction into the vein is difficult, the hormonal drug is administered intramuscularly. The repeated dose is 30-69 mg. For children, the calculation of the dose of glucocorticosteroids depends on age: 2-12 months - 2-3 mg / kg, 1-14 years - 1-2 mg / kg intravenously (slowly, at least three minutes). The drug is re-introduced after 20-30 minutes, with an assessment of metabolism.

Eye drops

According to the instructions, shake the solution for instillation into the eyes before use. The eye suspension is instilled into the cavity between the posterior surface of the eyelid and the anterior surface of the eyeball (it is called the conjunctival sac), 1-2 drops three times a day. The course of treatment for infection lasts no more than 14 days. After opening a new vial, it can be stored for longer than a month.

special instructions

In the instructions for the drug there is a section special instructions describing the use of the drug. Pay attention to these points:

  • prolonged therapy requires the appointment of potassium supplements and diet to avoid the development of hypokalemia;
  • after the end of long-term therapy, doctors observe patients for another year to exclude the risk of developing adrenal insufficiency of the cortex;
  • sudden withdrawal of glucocorticosteroids leads to anorexia, nausea, weakness, muscle pain and exacerbation of the disease;
  • during therapy with Prednisolone, vaccines are not administered;
  • during the treatment period, it is worth refraining from driving cars and dangerous mechanisms.

Prednisone for children

According to the instructions, the drug is contraindicated under the age of three years in the form of tablets. A solution for parenteral administration can be prescribed according to strict indications and after consultation with a doctor. The dosage is set individually, depending on age and body weight. During the treatment of children in the growth period, the attending physician regularly checks the development of the child in order to exclude Negative influence medication and eliminate indications of infections.

drug interaction

According to the instructions for use, Prednisolone is not combined with all drugs:

  • taking medication against the background of weak insulin secretion, the use of antidepressants and anticoagulants requires adjustment of their dose;
  • patients with Addison's syndrome should be careful when combined with barbiturates;
  • corticosteroid increases the risk of bleeding when combined with salicylates;
  • increases the possibility of electrolyte imbalance with diuretics;
  • sodium-containing drugs lead to peripheral edema;
  • Amphotericin B increases the risk of underperformance heart rate;
  • ethanol increases metabolism, can lead to adrenal insufficiency;
  • accelerates the elimination of aspirin, so you can not prescribe acetylsalicylic acid during therapy with hydrocortisone;
  • reduces the effectiveness of the introduction of insulin, somatotropic hormone;
  • adrenocorticotropic hormone enhances the anti-inflammatory effect of prednisolone;
  • Cyclosporine and Ketoconazole increase the toxicity of synthetic glucocorticosteroids;
  • androgens and steroid anabolic hormonal agents increase puffiness, lead to the appearance of acne;
  • estrogens and contraceptives reduce the clearance of prednisolone, and he himself lowers the effect of insulin.

Side effects of prednisolone

Instructions for use of the drug warns of the development of such possible side effects:

  • obesity, hirsutism, acne;
  • failure of the menstrual cycle;
  • osteoporosis, Itsenko-Cushing complex;
  • ulceration of the esophagus, stomach ulcers;
  • hemorrhagic pancreatitis;
  • hyperglycemia;
  • weakening of immunoglobulins, increased blood clotting;
  • psychical deviations.

Overdose

According to studies and guidelines, cases of overdose are rare, as are the manifestations of acute toxic effects or death from the fact that the doses of the drug were overestimated. Likely symptoms overdose are increased infection and signs of side effects. In this case, treatment with specific antidotes is not carried out, since they are not available. Doctors eliminate the symptoms of infection themselves.

Contraindications

Instructions for use states that if there is the following contraindications the drug is not allowed to be used for its intended purpose:

  • severe form of hypertension, diabetes mellitus, steroid diabetes;
  • circulatory failure;
  • first trimester of pregnancy;
  • acute endocarditis;
  • psychosis, nephritis, osteoporosis;
  • kidney disease;
  • stomach or duodenal ulcer;
  • syphilis;
  • tuberculosis treatment;
  • old age;
  • for infections, it is prescribed only with antibiotics.

Terms of sale and storage

The drug is dispensed from pharmacies by prescription. Keep away from children and protected from light at temperatures up to 25 degrees. Shelf life is two years for tablets and ointment, three years for solution and eye drops.

Analogues

By active active ingredient or pharmacological action allocate synthetic analogues of Prednisolone in ampoules, tablets and ointments of domestic or foreign production:

  • Medopred;
  • prednisolone bufus;
  • Prednisolone-AKOS;
  • Decortin;
  • Inflanefran;
  • Novo-Prednisolone;
  • Prednihexal;
  • Prednisolone acetate or hemisuccinate, sodium phosphate;
  • Salt-Decortin.

Price of Prednisolone

You can buy the drug through pharmacies or the Internet, having a prescription on hand. The cost will depend on the form of release, the manufacturer and the number of tablets / ampoules inside the package. Approximate prices.

Prednisolone is an anti-inflammatory, anti-allergic, anti-toxic and anti-shock drug. And in order to know exactly what Prednisolone should be taken from, you should read our article. This medicinal product is synthetic analogue hormones cortisone and hydrocortisone, which are secreted by the adrenal cortex. When taken orally, it is more effective than cortisone by 4-5 times and about 3 times than hydrocortisone. Prednisolone slightly increases potassium excretion and practically does not cause sodium and water retention in the human body. When taking Prednisolone tablets orally, its maximum accumulation in plasma is noted after 1.5 hours. The drug is well absorbed from gastrointestinal tract. Biotransformed through oxidation mostly in the liver. The drug is excreted from the body in the form of metabolites with urine and feces. Prednisolone affects protein, water-electrolyte, carbohydrate and fat metabolism in the human body.

What does prednisone help with?

  • inflammation of the cornea of ​​\u200b\u200bthe eye with intact mucosa; blepharitis (inflammation of the edges of the eyelids);
  • allergic and chronic conjunctivitis (inflammation of the mucous membrane of the eye);
  • sympathetic ophthalmia (inflammation of the membrane of the eye due to injury to the other eye);
  • after eye surgery;
  • multiple sclerosis;
  • bronchial asthma;
  • hepatitis; chronic and acute allergies (atopic dermatitis, urticaria, food and drug allergy, Quincke's edema, toxicoderma, hay fever);
  • rheumatic fever;
  • rheumatic carditis;
  • chronic and acute illnesses joints (polyarthritis, osteoarthritis, bursitis, synovitis, rheumatoid arthritis, psoriatic and gouty arthritis, humeroscapular periarthritis, Still's syndrome in adults);
  • inflammatory diseases of the gastrointestinal tract (local enteritis, nonspecific ulcerative colitis);
  • infectious mononucleosis (an infectious disease in which the palatine lymph nodes, liver increase and heat body);
  • connective tissue diseases (dermatomyositis, scleroderma, lupus erythematosus, periarteritis nodosa);
  • autoimmune diseases;
  • acute pancreatitis (nonspecific inflammation of the pancreas);
  • hemolytic anemia;
  • glomerulonephritis (kidney disease).

Prednisolone tablets from what else can you take:

  • shock during surgical interventions;
  • prevention of rejection in tissue and organ transplantation.

Mode of application:

The dose of the drug for each person is set individually. To correctly prescribe the dose of Prednisolone, you need to take into account the daily secretory rhythm of glucocorticoids. Tablets are taken orally with a small amount of liquid. Usually, a large dose is prescribed in the morning, an average dose in the afternoon, and a small dose in the evening. As a rule, the introductory dose of the drug is 20-30 mg over 24 hours (4-6 tablets). Gradually, the transition to a maintenance dose is carried out, which is 5-10 mg (1-2 tablets). In certain diseases (certain rheumatic diseases, nephrosis), the daily introductory dose may be 15-100 mg. To complete treatment with prednisolone, daily dose gradually decreases. For children, the initial dose of the drug is prescribed at the rate of 1-2 mg / kg of body weight and distributed into 4-6 doses per day. The maintenance dose of the drug is 300-600 mcg / kg of the child's body weight. When treating with Prednisolone, you should check arterial pressure, to do urine tests and to determine the level of sugar in the blood.

Contraindications:

  • individual susceptibility to the components of the drug;
  • post-vaccination period; diabetes;
  • acute endocarditis;
  • pregnancy;
  • ulcer duodenum and stomach;
  • gastritis; acute peptic ulcer;
  • persistent rise in blood pressure;
  • active form of tuberculosis;
  • syphilis;
  • nephritis (inflammation of the kidneys);
  • acute psychosis;
  • polio;
  • recent myocardial infarction;
  • chronic heart failure.

Side effects:

Emergence adverse reactions depends on the duration of treatment with Prednisolone and the size of the dose taken. Possible development of such side effects:

  • mental disorders;
  • increase in blood sugar levels;
  • violation of the menstrual cycle;
  • obesity;
  • decreased resistance to infections;
  • hirsutism (excess hair growth in women);
  • convulsions;
  • dizziness;
  • osteoporosis;
  • growth retardation in children;
  • depression;
  • insomnia;
  • hallucinations;
  • decrease muscle mass.

We hope that this article has helped you understand what Prednisolone is for, and how to calculate its dose.

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 physiological 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 on 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 bone marrow the formation of some cells, 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, 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) with 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 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 joint inflammation). For oral administration (tablets): chronic and acute inflammatory diseases 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 diseases connective tissue (nodular periarteritis, scleroderma, systemic lupus erythematosus, rheumatoid arthritis, dermatomyositis); acute rheumatic heart disease, rheumatic fever; chronic and acute allergic diseases: allergic reactions to food products And medications, 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 large surface skin), 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 hyperplasia adrenal glands; cerebral edema (including in brain tumors or associated with radiation therapy, surgical intervention 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, multiple 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 with oncological diseases; inflammatory eye diseases: severe sluggish posterior and anterior uveitis, sympathetic ophthalmia, neuritis optic nerve; allergic eye diseases: allergic forms 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 surgical interventions 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: a single dose of 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 deficiency adrenal glands: a single dose is 0.1-0.2 g, the daily dose 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). For prevention infectious lesions skin, prednisone 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 need to be warned childbearing age O possible risk for 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 may suppress growth, endogenous corticosteroid production and lead to unwanted effects in a 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 in 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 infarction myocardium - slowing down 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 possible bleeding and perforation, pancreatitis, ulcerative esophagitis, flatulence, digestive disorders, nausea, increased appetite, vomiting;
skin covers: hypo- or hyperpigmentation, cutaneous and subcutaneous atrophy, atrophic streaks, abscess, acne, thinning of the skin, delayed wound healing, ecchymosis, petechiae, excessive sweating, erythema;
sense organs and nervous system: delirium, euphoria, disorientation, depression, hallucinations, increased intracranial pressure, congestive optic papilla syndrome, headache, sleep disturbances, vertigo, dizziness, sudden loss of vision (when administered parenterally in the neck, head, scalp, turbinates), posterior subcapsular cataract formation, 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.
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 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, which contain estrogens, can change the metabolism of prednisolone and its protein binding, increasing the half-life and reducing 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 folic acid. Prednisolone increases the possibility of electrolyte disturbances in joint admission 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. At chronic overdose prednisolone, the dose of the drug should be reduced.

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