Prednisolone dilution. Types, names, forms of release and composition of Prednisolone

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Prednisolone for injection belongs to the group of glucocorticosteroids, the drug is intended for a fairly wide range of applications and a fairly wide range of diseases. It is used both to treat asthma and to relieve anaphylactic shock or an allergy attack from an unidentified irritant. This is first aid to a person if anaphylactic shock occurs and an opportunity to save his life. The drug is also used during radiotherapy courses and is considered a good anti-inflammatory agent.

The range of uses of the medicine is very wide; it is used and prescribed by doctors for the treatment of asthmatic diseases and allergic reactions.

About the drug

The drug three main pharmacological actions:

Anti-inflammatory;
Immunosuppressive;
Antiallergic;
Antishock;
Antipruritic;

Prednisolone is a synthetic hormone, absolutely similar to the hormone produced by the human adrenal glands.

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Irina Martynova. Graduated from Voronezh State Medical University named after. N.N. Burdenko. Clinical resident and neurologist of the BUZ VO \"Moscow Polyclinic\".

When the adrenal glands malfunction, the hormone becomes smaller or stops being produced altogether. A lack of the hormone in the body can lead to quite sad consequences, and the drug has very strong pharmacological effects, therefore it is used in the treatment of really serious diseases or serious situations that threaten human life (anaphylactic shock, exacerbation of bronchial asthma). Use it only as part of complex therapy.

The drug is produced in India.

Release forms

There are several forms of release:

. The cost of the ointment is only about 50 rubles. The main component is prednisolone, additional components: medical white paraffin, glycerin and stearic acid.
Pills. The cost of the tablets is about 68 rubles. The main component is also prednisolone, additional components: milk sugar, potato starch, calcium stearate. Used to treat diseases of the musculoskeletal system.
Prednisolone injections, which cost from 46 to 130 rubles. Main component: prednisolone sodium phosphate, additional components: water for injection, nicotinamide, sodium hydroxide.

Dosages and regimen of use

Dosage and application regimen differs depending on the pharmacological form of release and the disease:

Prednisolone in ampoules can be prescribed as droppers. In this case, the dosage and continuation of treatment is determined by the attending physician. Typically, droppers with the drug are prescribed to seriously ill patients, people with severe allergies or anaphylactic shock.
For acute adrenal insufficiency, 300-400 mg per day is prescribed. (injections)
For a severe allergic reaction, 100-200 mg per day is prescribed. Treatment time ranges from 10 to 16 days.
For bronchial asthma, the course of treatment ranges from three to 16 days, the dosage is prescribed by the doctor. Self-medication is not recommended.
For rheumatoid arthritis, an ointment may be prescribed in addition to the main medications.
For skin allergic reactions, 1-2 tablets per day may be prescribed.

Injections can be administered intramuscularly and can make a solution for IVs.

Solution lasts for about a day, depending on the susceptibility of the human body and the disease. One injection may be enough intramuscularly for several days, especially when treating allergic reactions and various diseases of the musculoskeletal system. The solution administered intramuscularly contains a fairly high dose of prednisolone, which has strong pharmacological properties. Injecting the solution is quite painful, but after a couple of hours (half an hour - two hours) relief comes.

Indications for use

Instructions for use indicate that the drug can be used to treat shock, accompanied by a decrease in blood pressure, acute adrenal failure, cerebral edema, asthma and rheumatoid arthritis. The drug is also used for allergies; severe allergic (anaphylactic) shock can also be treated with injections. The drug also treats hepatic coma.

The fact is that the adrenal glands stop producing the hormone in full, so the body needs an influx of synthesized hormone for normal functioning. The drug increases the synthesis of peptide inhibitors and reduces the level of PG, stabilizes lysosome membranes.

Due to this, many diseases quickly decrease with successful complex therapy and correct dosage selection.

Contraindications

In shock conditions the drug is administered without taking into account contraindications(emergency situations such as anaphylactic shock, traumatic shock, severe allergic reaction). For longer treatment, the following must be taken into account:

Presence of a stomach ulcer;
Osteoporosis;
Cushing's syndrome;
Psychoses;
Severe arterial hypertension;

The drug should not be used for smallpox, herpes, or herpes zoster; it is not recommended for active tuberculosis.

For acute renal failure and liver problems, Before taking it, you must consult a medical specialist.

Pregnant women in the first trimester and breastfeeding women are not recommended to take the drug. The drug is not recommended for children under 18 years of age, but in emergency situations it is likely to be used. However, when used for longer treatment, examination and consultation of several medical specialists are necessary.

Overdose and side effects

As side effects:

Weight gain;
Hypokalemia;
Cushing's syndrome;
Increased blood pressure;
Nausea;
Vomit;
Diarrhea;
Depression and hallucinations;

The occurrence of side effects is not necessary; their occurrence varies depending on the physical characteristics of the person.

In general, there are very few reported cases of side effects; the drug is well tolerated by patients even with long-term treatment. If the dosage is exceeded and an overdose occurs, nausea, vomiting, weakness, drowsiness, disturbances in the gastrointestinal tract, depression, hallucinations, a sharp increase in blood pressure, and edema are possible. To reduce an overdose, it is necessary to urgently rinse the stomach and seek medical help in an ambulance. There is little information about the toxicity of the drug.

Interaction with substances

Interaction of the drug with alcohol and other drugs was noted for tablets and solution. Solution in combination with diuretics increases potassium excretion, and in combination with antidiabetic agents reduces glucose levels. Interaction with alcohol and alcohol-containing substances is extremely negative and can lead to uncontrollable side effects.

When combined with acetylsalicylic acid, the risk of bleeding in the stomach increases.

Storage

The medicine is stored for two years and is sold in pharmacies only with a prescription. You can use them as analogues (from 300 rubles), other analogues differ much more in composition and you should consult your doctor about them.

FAQ

Does it hurt to give an injection?? Painful sensations are present, but during the injection itself and the administration of the medicine there is practically no pain, painful sensations appear after a couple of hours, pain in the gluteal muscle increases, but is quite tolerable. When inserting and puncturing the skin, pain is practically not felt, unlike B vitamins, magnesium and other drugs.

How long does it last?? In cases of shock, anaphylactic shock, or severe allergies, the injection acts almost instantly, and its effect lasts for a really long time. Sometimes just one injection is enough to completely get rid of all the consequences, and sometimes it is necessary to inject a full course for relief to occur. In general, the medicine lasts for about a couple of days.

Prednisolone is very often used by emergency physicians as a fast-acting, long-acting drug.

Reviews

Reviews from experts about prednisolone indicate that the drug is really effective in stressful and shock situations and effectively brings a person out of anaphylactic shock. This drug perfectly blocks the state of shock, literally returning a person from the other world. However, we should not forget about the many side effects of the drug and the danger of overdose. It is necessary to use the medicine wisely, not exceeding the prescribed dose, and do not use it if there are contraindications or hypersensitivity to one of the components.

On special forums, a lot of different reviews about the drug have been collected, both positive and negative.

Most patients note the extreme effectiveness of prednisolone, especially in stressful or shock situations. Many people note painful sensations some time after the injection in that area, itching, burning.

Many patients noted a significant improvement in their well-being after use for rheumatoid arthritis and diseases of the musculoskeletal system. They reduce pain, relieve most of the inflammation, and lower body temperature. On forums dedicated to children and their illnesses, mothers also note the effectiveness of the drug when administered intravenously to children.

In general, the reviews are positive, proving the effectiveness of the drug. There are not so many negative reviews, mostly either the dosage is exceeded or individual intolerance is revealed.

For allergic reactions and anaphylactic shock, it has established itself as a reliable and effective remedy that has a good targeted effect, especially if anaphylactic shock is caused by an unknown irritant and urgent medical care is necessary.

According to reviews, “Prednisolone” is the name of a drug that belongs to synthetic glucocorticoids (in other words, it is a hormonal drug). It is an analogue of "water-deprived" hydrocortisone. In medical activities, Prednisolone is used externally, orally in the form of tablets, eye drops, or for intravenous (sometimes intramuscular) administration.

Characteristics of the active substance

Prednisolone is a crystalline powder, odorless and white in color (sometimes with a slight tint of yellow). Almost insoluble in water. But it is slightly soluble in alcohol, dioxane, chloroform and methanol. Its molecular weight is 360.444 g/mol.

pharmachologic effect

According to reviews, Prednisolone has anti-inflammatory, immunosuppressive, antiallergic, glucocortioid and anti-shock effects.

The substance interacts in the cytoplasm of the cell with special receptors and forms a specific complex that penetrates into the nucleus, binding to DNA and causing the expression of mRNA. Changes the formation of proteins on ribosomes that express the effects of cells. Accelerates the synthesis of lipocortin, which inhibits phospholipase A2, inhibits the biosynthesis of endoperoxide and the liberation of archidonic acid, essential for the body, as well as prostaglandins, leukotreins (promote the progression of inflammation, allergies and other processes of a pathological nature).

Stabilizes the membrane membrane of lysosomes, inhibits the synthesis of hyaluronidase (an enzyme that breaks down hyaluronic acid in a special way), reduces the production of lymphokines produced by lymphocytes. Affects the processes of alteration and exudation during inflammation, delays the spread of the inflammatory process.

Inhibits the migration of monocytes in areas of inflammation and limits the proliferation of connective tissue cells, which has an antiproliferative effect. Inhibits the process of formation of mucopolysaccharides, thereby preventing water from combining with plasma proteins in the rheumatic focus of inflammation.

Inhibits the intensity of destruction of peptide bonds, preventing the destruction of tissue and cartilage in rheumatoid arthritis.

In what cases is Prednisolone prescribed to children? Reviews confirm that the antiallergic effect of the drug is due to a decrease in the number of basophils, a decrease in the synthesis and secretion of mediators of an immediate allergic reaction. Promotes the development of lymphopenia and involution of lymphoid tissue, thereby causing immunosuppression.

Reduces the concentration of T-lymphocytes in the blood plasma and the production of immunoglobulins. Increases the breakdown and reduces the production of components of a complex of complex proteins, inhibits Fc receptors of immunoglobulins, inhibits the functions of macrophages and leukocytes. Increases the number of receptors and normalizes their sensitivity to a variety of physiologically active substances in the body. This is confirmed by the instructions for use and reviews for Prednisolone ointment.

Reduces protein synthesis and its amount in the blood plasma, but at the same time accelerates its energy metabolism in muscle tissue. Promotes the production of fibrinogen, surfactant, erythropoietin, lipomodulin and enzyme proteins in the liver. It also promotes the redistribution of fat, the production of triglycerides and IVH. Increases the absorption of carbohydrates from the gastrointestinal tract, the activity of phosphoenolpyruvate kinase and glucose-6-phosphatase, which enhances gluconeogenesis and mobilizes glucose in the bloodstream.

Retains water and sodium, and also accelerates the excretion of potassium. Reduces the absorption of calcium in the intestines, while increasing excretion by the kidneys and leaching it from the bones.

Pharmacokinetics

“Prednisolone,” according to reviews, has an anti-shock effect, activates the production of certain cells in the bone marrow, increases the number of red blood cells and platelets in the blood, and also reduces the number of monocytes, lymphocytes, basophils and eosinophils.

When taken orally, the medicine is well and quickly absorbed from the gastrointestinal tract. 70-90% of the substance is found in plasma in bound form: with albumin and transcortin. After oral administration, the maximum concentration of the substance in the blood plasma is observed after an hour and a half.

Metabolized in the liver by oxidation. The half-life of the substance from plasma is 120-240 minutes, from tissues - in the range from 20 to 34 hours. Less than 1% of the dose of the substance passes into the milk of a nursing woman. 20% of the substance is excreted unchanged by the kidneys.

Indications for use

According to reviews, Prednisolone is administered by intravenous or intramuscular infusion for:

acute allergic reaction;
bronchial asthma and status asthmaticus;
for the prevention and treatment of thyrotoxic reactions and thyrotoxic shock;
myocardial infarction;
acute adrenal insufficiency;
liver cirrhosis;
acute hepatitis;
poisoning with cauterizing liquids.

Prednisolone is administered by intra-articular injection for:

rheumatoid arthritis;
spondyloarthritis;
post-traumatic arthritis;
osteoarthritis.

Pills

In the form of Prednisolone tablets, according to reviews, it is prescribed for:

systemic connective tissue diseases;
chronic and acute inflammatory diseases of the joints: psoriatic and gouty arthritis, osteoarthritis, polyarthritis, juvenile arthritis, glenohumeral periarthritis, Still's syndrome in adults, synovitis and epicondylitis;
rheumatic fever and acute rheumatic carditis;
bronchial asthma;

acute and chronic allergies;
allergic reactions to food and drugs, angioedema, serum sickness, urticaria, allergic rhinitis, drug exanthema, hay fever;
skin diseases;
pemphigus, psoriasis, eczema, atopic dermatitis, diffuse neurodermatitis, contact dermatitis, toxicerma, seborrheic dermatitis, exfoliative dermatitis, malignant exudative erythema (Stevens-Johnson syndrome), cerebral edema after preliminary use in the form of intravenous or intramuscular injections;
adrenal insufficiency;
kidney diseases of autoimmune origin, nephrotic syndrome;
diseases of the hematopoietic organs: agranulocytosis, panmyelopathy, autoimmune hemolytic anemia, lymphogranulomatosis, myeloma, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia;
lung diseases: acute alveolitis, pulmonary fibrosis, stage II-III sarcoidosis;
pulmonary tuberculosis, tuberculous meningitis, aspiration pneumonia;
berylliosis, Loeffler's syndrome;
lung cancer;
multiple sclerosis;
diseases of the gastrointestinal tract;
hepatitis;
prevention of transplant rejection reactions;
hypercalcemia due to cancer;
nausea and vomiting during cytostatic therapy;
allergic eye diseases;
inflammatory eye diseases.

This is confirmed by the instructions for use and reviews for Prednisolone. The price will be presented below.

Ointment

Prednisolone in ointment form is used for:

urticaria, atopic dermatitis, diffuse neurodermatitis, lichen simplex chronicus, eczema, seborrheic dermatitis, discoid lupus erythematosus, simple and allergic dermatitis, toxicerma, erythroderma, psoriasis, alopecia;
epicondelitis, tenosynovitis, bursitis, humeroscapular periarthritis, colloid scars, sciatica.

Drops

"Prednisolone" in the form of eye drops is prescribed for non-infectious inflammatory diseases of the anterior segment of the eye - iritis, uveitis, episcleritis, scleritis, conjunctivitis, parenchymal and discoid keratitis without damage to the corneal epithelium, allergic conjunctivitis, blepharoconjunctivitis, blepharitis, inflammatory processes after eye injuries and surgery , sympathetic ophthalmia.

The price and reviews of Prednisolone are of interest to many. We will talk about them below.

Contraindications for use

Contraindications for systemic use are:

This is confirmed by the instructions for use and reviews for Prednisolone.

Contraindications to intra-articular injections are:

infectious and inflammatory processes in the joint;
general infectious diseases;
“dry” joint;
pregnancy;
joint instability as an outcome of arthritis.

Contraindications for use on the skin are:

viral, bacterial and fungal skin diseases;
skin manifestations of syphilis;
lupus;
skin tumors;
acne vulgaris;
pregnancy.

Contraindications to the use of Prednisolone, according to reviews, in the form of eye drops may be:

fungal and viral eye diseases;
purulent corneal ulcer;
acute purulent conjunctivitis;
glaucoma;
trachoma.

Adverse reactions

The severity and frequency of adverse reactions depend on the duration and method of use of the drug. Basically, the following side effects may develop when using Prednisolone:

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

This is confirmed by the instructions and reviews for Prednisolone.

Dosage and method of administration

The dosage is set depending on the method of use of the drug.

IN In the form of Prednisolone tablets, doctors recommend taking it once a day or a double dose every other day from 6 to 8 am. The total daily dose can be divided into several doses, and in the morning you should take the drug in a larger dosage. Prednisolone in tablet form should be taken during or after meals. Sudden termination of treatment can lead to negative consequences, so this should not be done. The dosage of the drug should be increased by 1.5-3 times in acute stressful conditions. If the case is severe, then the dosage is increased by 5-10 times.

In acute cases of the disease, adults are prescribed 4-6 tablets (20-30 mg) per day. The dose that maintains the therapeutic effect is 1-2 tablets (5-10 mg) per day. For some diseases, an initial dose of 5-100 mg/day may be prescribed or 5-15 mg/day as hormonal maintenance therapy.

As a rule, for children over three years of age, a dose of 1-2 mg per 1 kg of body weight per day, divided into several doses, is prescribed. The dose that maintains the therapeutic effect for children is about 0.5 mg per 1 kg of body weight. After achieving the effect, the dose should be reduced to 5 mg and then to 2.5 mg per day with a break of 3-5 days.

In the form of an ointment, the hormonal drug Prednisolone is used externally for allergic rashes and itching of the skin. The cream is applied several times a day in a thin layer. Also, Prednisolone ointment can be used in gynecology, but only in combination with antifungals and antibiotics. As a rule, the course of treatment with Prednisolone ointment ranges from 6 to 14 days. To maintain the therapeutic effect, the ointment is applied once a day.

In the form of an injection solution, the drug is administered intraarticularly, intravenously or intramuscularly under strict sterile conditions. For intra-articular administration of the drug, the recommended dose is 10 mg in small joints, and 25-50 mg in large joints. This injection can be repeated several times. If the therapeutic effect is insufficient, it is necessary to consider increasing the dose with your doctor.

For intravenous administration of the drug, the recommended dose is 25 mg for small affected parts of the body, and 50 mg for larger parts of the body.

In the form of eye drops, apply 1-2 drops three times a day into the conjunctival sac. As a rule, the course of treatment with these eye drops is no more than two weeks.

special instructions

with long-term therapy, it is necessary to prescribe potassium supplements and diet in order to avoid the development of hypokalemia;
after the end of long-term therapy, doctors should monitor the patient for another year so that adrenal insufficiency does not develop;
Do not suddenly stop using the drug, because this can lead to anorexia, weakness, nausea, exacerbation of the disease and muscle pain;
It is prohibited to administer any vaccines during Prednisolone therapy;
It is not recommended to drive complex machinery and vehicles during treatment with Prednisolone.

Price

Ampoules cost about 30 rubles, ointment - 70 rubles, tablets - about 100 rubles, drops - 100-200 rubles. It all depends on the city and the specific pharmacy.

Indications for use:
Collagenoses (a general name for diseases characterized by diffuse damage to connective tissue and blood vessels), rheumatism, infectious nonspecific polyarthritis (inflammation of several joints), bronchial asthma, acute lymphoblastic and myeloblastic leukemia (malignant blood tumor arising from hematopoietic cells of the bone marrow), infectious mononucleosis ( acute infectious disease occurring with increased temperature, enlargement of the palatine lymph nodes, liver), neurodermatitis (skin disease caused by dysfunction of the central nervous disease), eczema (neuroallergic skin disease, characterized by weeping, itchy inflammation) and other skin diseases, various allergic diseases , Addison's disease (decreased adrenal function), acute adrenal insufficiency, hemolytic anemia (decreased hemoglobin in the blood due to increased breakdown of red blood cells), glomerulonephritis (kidney disease), acute pancreatitis (inflammation of the pancreas); shock and collapse (sharp drop in blood pressure) during surgical interventions; to suppress the rejection reaction during homotransplantation (transplantation from one person to another) of organs and tissues.
Allergic, chronic and atypical conjunctivitis (inflammation of the outer membrane of the eye) and blepharitis (inflammation of the edges of the eyelids); inflammation of the cornea with intact mucosa; acute and chronic inflammation of the anterior segment of the choroid, sclera (the opaque part of the fibrous membrane of the eyeball) and episclera (the outer loose layer of the sclera in which blood vessels pass); sympathetic inflammation of the eyeball (inflammation of the anterior part of the choroid due to penetrating injury to the other eye); after injuries and operations with prolonged irritation of the eyeballs.

Pharmachologic effect:
Prednisolone is a synthetic analogue of the hormones cortisone and hydrocortisone secreted by the adrenal cortex. Prednisolone is 4-5 times more active than cortisone and 3-4 times more active than hydrocortisone when used orally. Unlike cortisone and hydrocortisone, prednisolone does not cause noticeable sodium and water retention and only slightly increases potassium excretion.
The drug has a pronounced anti-inflammatory, anti-allergic, anti-exudative, anti-shock, anti-toxic effect.
The anti-inflammatory effect of prednisolone is achieved mainly with the participation of cytosolic glucocorticosteroid receptors. The hormone-receptor complex, penetrating into the nucleus of the skin target cells (keratinocytes, fibroblasts, lymphocytes), enhances the expression of genes encoding the synthesis of lipocortins, which inhibit phospholipase A2 and reduce the synthesis of arachidonic acid metabolic products, cyclic endoperoxides, prostaglandins and thromboxane. The antiproliferative effect of prednisolone is associated with inhibition of the synthesis of nucleic acids (primarily DNA) in the cells of the basal layer of the epidermis and fibroblasts of the dermis. The antiallergic effect of the product is due to a decrease in the number of basophils, direct inhibition of the synthesis and secretion of biologically active substances.

Pharmacokinetics.
When taken orally, it is well absorbed from the gastrointestinal tract. The maximum concentration in blood plasma is reached after 90 minutes. after reception. In plasma, 90% of prednisolone is in bound form (with transcortin and albumin). Biotransformed by oxidation mainly in the liver; oxidized forms are glucuronidated or sulfated. It is excreted in urine and feces in the form of metabolites, partly unchanged. Penetrates the placental barrier and is found in small quantities in breast milk.

Prednisolone route of administration and dosage:
The dose is set individually. In acute conditions and as an introductory dose, 20-30 mg per day (4-6 tablets) is usually used. The maintenance dose is 5-10 mg per day (1-2 tablets). For some diseases (nephrosis, a kidney disease characterized by damage to the renal tubules with the development of edema and the appearance of protein in the urine), some rheumatic diseases, it is prescribed in higher doses. Treatment is stopped slowly, gradually reducing the dose. If there are indications of psychosis in the anamnesis (medical history), large doses are prescribed under the strict supervision of a physician. The dose for children is usually 1-2 mg per kg of body weight per day in 4-6 divided doses. When prescribing prednisolone, the daily secretory rhythm of glucocorticoids (the rhythm of the release of hormones from the adrenal cortex) must be taken into account: large doses are prescribed in the morning, medium doses in the afternoon, small doses in the evening.
For shock, 30-90 mg of prednisolone is administered intravenously slowly or by drip.
For other indications, prednisolone is prescribed at a dose of 30-45 mg intravenously slowly. If intravenous infusion is difficult, the product can be injected deep into the muscle. According to indications, prednisolone is administered repeatedly at a dose of 30-60 mg, intravenously or intramuscularly. After relief (removal) of the acute condition, prednisolone is prescribed orally in tablets, gradually reducing the dose.
In children, prednisolone is used at the following rate: at the age of 2-12 months - 2-3 mg/kg; 1-14 years - 1-2 mg/kg intravenously slowly (over 3 minutes). If necessary, the product can be reintroduced after 20-30 minutes.
The drug in the form of an injection suspension and solution for injection is intended for intra-articular, intramuscular and infiltration (impregnation of tissues) administration with strict adherence to asepsis (sterility). For intra-articular injection, it is recommended to administer 10 mg to small joints, 25 mg or 50 mg to large joints. The injection can be repeated more than once. After several injections, the severity of the therapeutic effect should be assessed. If the intensity is insufficient, decide on increasing the dose. After removing the needle from the joint, the patient must move the joint several times, bending and unbending it, for better distribution of the hormone. When infiltrated into small affected parts of the body - 25 mg, into larger ones - 50 mg.
The eye suspension is instilled into the conjunctival sac (the cavity between the back surface of the eyelids and the front surface of the eyeball) 1-2 drops 3 times every day. The course of treatment is no more than 14 days.
It is recommended to regularly monitor blood pressure, conduct urine and stool tests, measure blood sugar levels, administer anabolic hormonal products, and antibiotics. You should especially carefully monitor the electrolyte (ionic) balance when using prednisolone in combination with diuretics. During long-term treatment with prednisolone, potassium products and an appropriate diet should be prescribed to prevent hypokalemia (low potassium levels in the blood). To reduce the risk of catabolism (tissue breakdown) and osteoporosis (malnutrition of bone tissue, accompanied by an increase in its fragility), methandrostenolone is used.

Prednisolone contraindications:
Severe forms of hypertension (persistent rise in blood pressure), diabetes mellitus and Itsenko-Cushing's disease; pregnancy, circulatory failure stage III, acute endocarditis (inflammation of the internal cavities of the heart), psychosis, nephritis (inflammation of the kidneys), osteoporosis, peptic ulcer of the stomach and duodenum, recent operations, syphilis, active form of tuberculosis, old age.
Prednisolone is prescribed for diabetes mellitus with caution and only for absolute indications or for the treatment of insulin resistance (lack of response and insulin administration) associated with an increased titer of anti-insulin antibodies. For infectious diseases and tuberculosis, the product should only be used in combination with antibiotics or drugs for the treatment of tuberculosis.

Drug interactions:
If prednisolone is prescribed against the background of antidiabetic or anticoagulant drugs, then their dose must be adjusted.
Caution should be exercised when prednisolone and barbiturates are used together in patients suffering from Addison's disease.
During pregnancy, especially in the first trimester, prednisolone should be prescribed with extreme caution.

Overdose:
Reports of acute toxic effects or death from glucocorticoid overdose are rare. In cases of overdose, there are no specific antidotes. Symptomatic therapy is carried out.

Prednisolone side effects:
With prolonged use, obesity, hirsutism (excessive hair growth in women, manifested by the growth of a beard, mustache, etc.), acne, menstrual irregularities, osteoporosis, Itsenko-Cushing symptom complex (obesity, accompanied by decreased sexual function, increased bone fragility due to increased secretion of adrenocorticotropic hormone from the pituitary gland), ulceration of the digestive tract, perforation of an unrecognized ulcer (the appearance of a through defect in the wall of the stomach or intestine at the site of the ulcer), hemorrhagic pancreatitis (inflammation of the pancreas, occurring with hemorrhage into its body), hyperglycemia (increased blood sugar levels) , decreased resistance to infections, increased blood clotting, mental disorders. When treatment is stopped, especially long-term, withdrawal syndrome (sharp deterioration of the patient’s condition after stopping the drug product), adrenal insufficiency, and exacerbation of the disease for which prednisolone was prescribed may occur.

Release form:
Tablets containing 0.001; 0.005; 0.02 or 0.05 g of prednisolone in a pack of 100 pieces. Ampoules of 25 and 30 mg in 1 ml in a pack of 3 pcs. Ampoules with 1 ml of injection suspension containing prednisolone 25 or 50 mg, in a pack of 5, 10, 50, 100 and 1000 pcs. 0.5% ointment in tubes of 10 g. 0.5% ophthalmic suspension in a pack of 10 ml.

Synonyms:
Antisolone, Codelkorton, Cordex, Dacortin, Decortin N, Dihydrocortisol, Delta-Cortef, Deltacortil, Deltastab, Deltidrozol, Deltisilone, Gostacortin N, Guideltra, Hydrocortancil, Mecortolone, Metacortalone, Metacortandrolone, Melicortelone, Nisolone, Paracortol, Precortalone, Prednelan, Prenolon , Steran, Sgerolon, Ultracorten N, Tednisol, Sherizolon, Prednisolone-Darnitsa.

Storage conditions:
List B. In a place protected from light.
Dispensing conditions: by prescription.

Prednisolone composition:
International and chemical names: Prednisolonum; (pregnadiene-1,4-triol-11,17,21-dione-3,20 (or -dehydrocortisone);
basic physical and chemical properties: white tablets;
composition: 1 tablet contains 0.005 g of prednisolone;
excipients: milk sugar, potato starch, calcium stearate.

Additionally:
Manufacturers:
CJSC "Pharmaceutical Firm "Darnitsa", Kyiv, Ukraine;
RUE BelMedPreparaty, Minsk, Belarus;
Gedeon Richter, Hungary.

Attention!
Before using the medication "Prednisolone" You should consult your doctor.
The instructions are provided for informational purposes only. Prednisolone».

Analogues

These are drugs belonging to the same pharmaceutical group, which contain different active substances (INN), differ in name, but are used to treat the same diseases.

- Suspension for intramuscular and intraarticular administration 25 mg/ml
- Suspension for injection 40 mg/ml
- Tablets 4 mg

Indications for use of the drug Prednisolone

Endocrinological diseases:

Adrenal cortex insufficiency: primary (Addison's disease) and secondary;

Adrenogenital syndrome (congenital adrenal hyperplasia);

Acute adrenal insufficiency;

Before surgical interventions and in case of severe illnesses and injuries in patients with adrenal insufficiency;

Subacute thyroiditis.

Severe allergic diseases resistant to other therapy:

Contact dermatitis;

Atopic dermatitis;

Serum sickness;

Hypersensitivity reactions to drugs;

Permanent or seasonal allergic rhinitis;

Anaphylactic reactions;

Angioedema.

Rheumatic diseases:

Rheumatoid arthritis, juvenile rheumatoid arthritis (in cases resistant to other treatment methods);

Psoriatic arthritis;

Ankylosing spondylitis;

Acute gouty arthritis;

Acute rheumatic fever;

Myocarditis (including rheumatic);

Dermatomyositis;

Systemic lupus erythematosus;

Granulomatous giant cell mesoarteritis;

Systemic scleroderma;

Periarteritis nodosa;

Relapsing polychondritis;

Polymyalgia rheumatica (Horton's disease);

Systemic vasculitis.

Dermatological diseases:

Exfoliative dermatitis;

Bullous dermatitis herpetiformis;

Severe seborrheic dermatitis;

Severe erythema multiforme (Stevens-Johnson syndrome);

Mycosis fungoides;

Pemphigus;

Severe psoriasis;

Severe forms of eczema;

Pemphigoid.

Hematological diseases:

Acquired autoimmune hemolytic anemia;

Congenital aplastic anemia;

Idiopathic thrombocytopenic purpura (Werlhof's disease) in adults;

Hemolysis.

Liver diseases:

Alcoholic hepatitis with encephalopathy;

Chronic active hepatitis.

Hypercalcemia in malignancy or sarcoidosis.

Inflammatory joint diseases:

Acute and subacute bursitis;

Epicondylitis;

Acute tenosynovitis;

Post-traumatic osteoarthritis.

Oncological diseases:

Acute and chronic leukemia;

Lymphomas;

Mammary cancer;

Prostate cancer;

Multiple myeloma.

Neurological diseases:

Tuberculous meningitis with subarachnoid block;

Multiple sclerosis in the acute phase;

Myasthenia.

Eye diseases (severe acute and chronic allergic and inflammatory processes):

Severe sluggish anterior and posterior uveitis;

Optic neuritis;

Sympathetic ophthalmia.

Pericarditis.

Respiratory diseases:

Bronchial asthma;

Beryllium;

Loeffler's syndrome;

Symptomatic sarcoidosis;

Fulminant or disseminated pulmonary tuberculosis (in combination with anti-tuberculosis chemotherapy);

Chronic pulmonary emphysema (resistant to treatment with aminophylline and beta-agonists).

During organ and tissue transplantation to prevent and treat graft rejection (in combination with other immunosuppressive drugs).

Release form of the drug Prednisolone

tablets 5 mg; polypropylene bottle (bottle) 100 cardboard pack 1;

Tablets 5 mg; bottle (bottle) 30 cardboard pack 1;

Tablets 5 mg; plastic bag (bag) 100 plastic bottle (bottle) 1;

Tablets 5 mg; contour packaging 10 cardboard pack 1;

Tablets 5 mg; contour packaging 10 cardboard pack 10;

Pharmacodynamics of the drug Prednisolone

The mechanism of the immunosuppressive effect of prednisolone is not fully understood. The drug reduces the number of T-lymphocytes, monocytes and acidophilic granulocytes, as well as the binding of immunoglobulins to receptors on the surface of cells, inhibits the synthesis or release of interleukins by reducing the blastogenesis of T-lymphocytes; reduces the early immunological response. It also inhibits the penetration of immunological complexes through membranes and reduces the concentration of complement components and immunoglobulins.

Prednisolone acts on the distal part of the renal tubules, increasing the reabsorption of sodium and water, as well as increasing the excretion of potassium and hydrogen ions.

Prednisolone inhibits the secretion of ACTH by the pituitary gland, which leads to a decrease in the production of corticosteroids and androgens by the adrenal cortex. After long-term use of the drug in high doses, adrenal function can be restored within a year, and in some cases, persistent suppression of their function develops. Prednisolone enhances protein catabolism and induces enzymes involved in amino acid metabolism. Inhibits the synthesis and enhances the catabolism of proteins in lymphatic, connective, and muscle tissue. With prolonged use, atrophy of these tissues (as well as the skin) may develop.

Increases blood glucose concentrations by inducing gluconeogenesis enzymes in the liver, stimulating protein catabolism (which increases the amount of amino acids for gluconeogenesis) and reducing glucose consumption in peripheral tissues. This leads to the accumulation of glycogen in the liver, increasing blood glucose concentrations and increasing insulin resistance.

With prolonged use of the drug, redistribution of adipose tissue is possible.

Inhibits the formation of bone tissue and enhances its resorption, reducing the concentration of calcium in the blood serum, which leads to secondary hyperfunction of the parathyroid glands and simultaneous stimulation of osteoclasts and inhibition of osteoblasts.

These effects, together with a secondary reduction in the amount of protein components as a result of protein catabolism, can lead to suppression of bone growth in children and adolescents and to the development of osteoporosis in children of all ages.

Enhances the effect of endo- and exogenous catecholamines.

Use of Prednisolone during pregnancy

With extreme caution, especially in the first trimester of pregnancy; When breastfeeding, caution should be exercised if the baby has hyperbilirubinemia.

Contraindications to the use of the drug Prednisolone

Peptic ulcer of the stomach and duodenum, Cushing's syndrome, osteoporosis, predisposition to thromboembolism, renal failure, severe arterial hypertension, chickenpox, herpes simplex and herpes zoster, vaccination period.

Side effects of the drug Prednisolone

With short-term use of prednisolone (as well as other corticosteroids), side effects are rarely observed. When using prednisolone for a long time, the following side effects may develop.

From the side of the central nervous system and peripheral nervous system: increased intracranial pressure with optic nerve congestion syndrome (occurs most often in children, after too rapid dose reduction, symptoms - headache, deterioration of visual acuity, double vision); convulsions, dizziness, headache, sleep disturbances.

From the endocrine status: secondary adrenal and hypothalamic-pituitary insufficiency (especially during stressful situations: illness, injury, surgery); Cushing's syndrome, growth suppression in children, menstrual irregularities, hyperglycemia, glycosuria, decreased tolerance to carbohydrates, manifestation of latent diabetes mellitus and increased need for insulin or oral hypoglycemic drugs in patients with diabetes mellitus, hirsutism.

From the organ of vision: posterior subcapsular cataract, increased intraocular pressure, glaucoma, exophthalmos.

From the mental sphere: most often appear during the first 2 weeks of therapy, symptoms can imitate schizophrenia, mania, delirium; Women and patients with systemic lupus erythematosus are most susceptible to developing mental disorders.

Metabolism: negative nitrogen balance (as a result of protein catabolism).

From laboratory parameters: an increase in the number of leukocytes (20,000/μl), a decrease in the number of lymphocytes and monocytes, an increase or decrease in the number of platelets, an increase in the concentration of calcium in the blood and urine, an increase in the level of total cholesterol, LDL, triglycerides in the blood serum, an increase in the concentration 17-hydroxycorticosteroids and 17-ketosteroids in the urine, decreased uptake of labeled technetium into bone tissue and brain tumor tissue, decreased uptake of labeled iodine into the thyroid gland; weakening of the reaction in skin allergy tests and tuberculin test.

Other: anaphylactic reactions, hypersensitivity reactions; obliterating arteritis, weight gain, fainting.

Method of administration and dosage of the drug Prednisolone

Orally, without chewing and with a small amount of liquid. The dose is selected individually. When prescribing, the circadian secretory rhythm of GCS should be taken into account: most of the dose (2/3 of the dose) or the entire dose should be taken in the morning (about 8 a.m.), and 1/3 in the evening. Treatment is stopped slowly, gradually reducing the dose.

Adults: for acute conditions and as replacement therapy, the initial daily dose is 20–30 mg, the maintenance daily dose is 5–10 mg. If necessary, the initial daily dose can be 15–100 mg, maintenance - 5–15 mg/day.

Children: the initial daily dose is 1–2 mg/kg body weight and is divided into 4–6 doses, the maintenance daily dose is 300–600 mcg/kg.

Overdose of Prednisolone

The risk of overdose increases with long-term use of prednisolone, especially in high doses.

Symptoms: increased blood pressure, peripheral edema; In addition, increased side effects are possible.

Treatment: temporarily stop taking the drug or reduce the dose.

Interactions of Prednisolone with other drugs

When used together with cardiac glycosides, the risk of developing cardiac arrhythmias and glycoside toxicity associated with hypokalemia increases. Barbiturates, anticonvulsants (phenytoin, carbamazepine), rifampicin, glutethimide accelerate the metabolism of GCS (by inducing microsomal enzymes) and weaken their effect.

When used together, histamine H1 receptor blockers weaken the effect of prednisolone.

When prednisolone is used together with amphotericin B, carbonic anhydrase inhibitors, hypokalemia, left ventricular myocardial hypertrophy, and circulatory failure may develop.

When used together with paracetamol, it is possible to develop hypernatremia, peripheral edema, increase calcium excretion, and increase the risk of hypocalcemia and osteoporosis, as well as hepatotoxic reactions associated with paracetamol.

When used together with anabolic steroids and androgens, the risk of developing peripheral edema and acne increases (this combination requires caution, especially in the case of concomitant heart and liver diseases).

When used simultaneously with oral contraceptives containing estrogens, it is possible to increase the concentration of steroid-binding globulins in the blood serum, slow down metabolism, increase T1/2 and enhance the effect of prednisolone.

When used together with anticholinergics (atropine), intraocular pressure may increase.

When used together with anticoagulants (coumarin derivatives, indadione, heparin), streptokinase, urokinase, a decrease (in some patients - an increase) of effectiveness is possible, and the formation of ulcers and bleeding from the gastrointestinal tract is possible; the dose should be determined based on prothrombin time.

When used together with tricyclic antidepressants, it is possible to increase mental disorders associated with taking prednisolone (the use of tricyclic antidepressants for the correction of mental disorders while taking corticosteroids is not recommended).

When used together with prednisolone, the hypoglycemic effect of insulin and oral hypoglycemic agents may be weakened, and glucose levels may increase (which may require dose adjustment of antidiabetic drugs).

When used together with prednisolone, dose adjustment or discontinuation of antithyroid drugs or thyroid hormones may be required, because changes in thyroid function indicators are possible.

When used together with prednisolone, the effect of potassium-sparing diuretics and hypokalemia may be weakened.

When used together with prednisolone, the effect of laxatives and the development of hypokalemia may be weakened.

When used together, ephedrine may accelerate the metabolism of corticosteroids (prednisolone dose adjustment may be required).

When prednisolone is used together with other immunosuppressive drugs, the likelihood of developing infections, lymphomas and other lymphoproliferative diseases increases.

When used simultaneously with prednisolone, a decrease in the concentration of isoniazid in the blood plasma is possible (mainly in individuals with rapid acetylation); a dose adjustment of prednisolone may be required.

When used simultaneously with prednisolone, an accelerated metabolism of mexiletine and a decrease in its concentration in plasma are observed.

When used together with depolarizing muscle relaxants, it should be noted that hypocalcemia associated with the use of prednisolone may enhance synaptic blockade, leading to an increase in the duration of neuromuscular blockade.

Acetylsalicylic acid and other NSAIDs, ethanol weaken the effect of prednisolone, increase the risk of developing peptic ulcers and bleeding from the gastrointestinal tract.

Drugs and foods containing sodium, when used simultaneously with prednisone, increase the likelihood of developing arterial hypertension and peripheral edema.

The use of corticosteroids increases the need for folic acid.

Precautions when taking Prednisolone

Glucocorticoids should be prescribed in the smallest dosages and for the minimum duration necessary to achieve the desired therapeutic effect. When prescribing, the daily circadian rhythm of endogenous secretion of glucocorticoids should be taken into account: at 6–8 a.m., most (or all) of the dose is prescribed.

In the event of stressful situations, patients on corticosteroid therapy are advised to administer parenteral corticosteroids before, during and after the stressful situation.

If there is a history of psychosis, high doses are prescribed under the strict supervision of a physician.

During treatment, especially with long-term use, the dynamics of growth and development in children should be carefully monitored; observation by an ophthalmologist, monitoring of blood pressure, water and electrolyte balance, blood glucose levels, and regular analyzes of the cellular composition of peripheral blood are necessary.

Sudden cessation of treatment may cause the development of acute adrenal insufficiency; with long-term use, the drug should not be suddenly discontinued; the dose should be reduced gradually. With sudden withdrawal after long-term use, withdrawal syndrome may develop, manifested by increased body temperature, myalgia and arthralgia, and malaise. These symptoms can appear even in cases where there is no adrenal insufficiency.

Special instructions when taking Prednisolone

Prednisolone is contraindicated in patients with systemic fungal infections due to the risk of worsening the infection. The drug is in some cases used in the treatment of fungal infections with amphotericin B to reduce the side effects of the antifungal drug, but this combination can lead to the development of circulatory failure and left ventricular myocardial hypertrophy, as well as severe hypokalemia.

In case of stressful situations, patients receiving Prednisolone are recommended to administer parenteral corticosteroids.

Sudden withdrawal of GCS can cause the development of acute adrenal insufficiency, so the dose of Prednisolone should be reduced gradually.

Prednisolone can mask the symptoms of infection, reduce the body's resistance to infections, and also reduce the body's ability to localize the infectious process.

With the use of the drug, clinical manifestations of latent amoebiasis are possible.

In persons arriving from tropical countries or in patients with dysentery of unknown etiology, dysenteric amoebiasis should be excluded before using Prednisolone. Long-term use of Prednisolone increases the risk of developing secondary fungal or viral infections.

Long-term use of corticosteroids may lead to the development of cataracts and glaucoma (including damage to the optic nerve).

When using Prednisolone in high doses, you should monitor blood pressure (possible development of arterial hypertension), body weight of patients (possible occurrence of peripheral edema).

Serum electrolyte concentrations should be monitored periodically. In some cases, you may need to limit your sodium intake and increase your potassium intake.

Prednisolone also causes an increase in calcium excretion.

Patients receiving GCS should not be vaccinated with live viral vaccines (due to possible viral replication and development of viral diseases), and there may be a decrease in antibody production. Administration of an inactivated viral or bacterial vaccine may not produce the expected increase in antibodies. Patients who receive corticosteroids as replacement therapy, for example, for Addison's disease, can be vaccinated. In addition, patients taking GCS have an increased risk of developing neurological complications.

Prescribing GCS to patients with an active form of tuberculosis is possible only in cases of disseminated or fulminant tuberculosis and only in combination with anti-tuberculosis therapy. Patients with latent tuberculosis or a positive tuberculin test taking Prednisolone should be monitored due to the high risk of activation of the tuberculosis process. With long-term use of GCS, this category of patients should receive chemoprophylaxis.

The use of the drug may mask the symptoms of infectious diseases.

With sudden withdrawal of Prednisolone (especially after long-term use), withdrawal syndrome may develop (manifested by anorexia, fever, myalgia and arthralgia, general weakness). Symptoms can occur even in cases where there is no adrenal insufficiency.

In patients with hypothyroidism or liver cirrhosis, the effect of Prednisolone is enhanced.

When using Prednisolone, the development of mental disorders (euphoria, insomnia, sudden mood changes, personality changes, severe depression, symptoms of psychosis) is possible. Pre-existing emotional instability or psychotic tendencies may increase during GCS therapy.

When using GCS in patients with hypoprothrombinemia, acetylsalicylic acid should be prescribed with caution.

The drug is prescribed with caution for nonspecific ulcerative colitis due to the risk of developing intestinal perforation, abscess or other purulent infections; with intestinal diverticulosis, fresh intestinal anastomoses, erosive and ulcerative lesions of the gastrointestinal tract, with renal failure, arterial hypertension, osteoporosis, myasthenia gravis, diabetes mellitus, liver dysfunction, glaucoma, viral infections, hyperlipidemia, hypoalbuminemia.

With the development of gastrointestinal perforation during the use of corticosteroids, the symptoms of peritonitis may be slightly expressed or absent altogether.

In some patients, during GCS therapy, the number and motility of sperm changes.

Taking the drug with food may reduce the likelihood of developing gastrointestinal side effects. The effectiveness of antacid medications in preventing the formation of ulcers, gastrointestinal bleeding, or intestinal perforation has not been confirmed.

With the development of steroid myopathy and the impossibility of discontinuing GCS therapy, replacing prednisolone with another GCS can alleviate the symptoms.

The risk of developing osteoporosis associated with long-term use of corticosteroids can be reduced by taking vitamin D and calcium supplements or, if the patient's condition allows, by performing appropriate physical exercise.

If psychosis or depression occurs, reduce the dose or stop taking the drug if possible. If necessary, phenothiazine or lithium preparations can be used. The use of tricyclic antidepressants is contraindicated.

In order to mitigate some of the symptoms of withdrawal syndrome, it is possible to prescribe acetylsalicylic acid or other NSAIDs.

Use in pediatrics

When prescribing the drug to children, monitoring of their growth and development is necessary.

Prednisolone is a synthetic dehydrogenated analogue of the glucocorticosteroid hormone hydrocortisone. The drug suppresses inflammatory processes, prevents the development of allergic reactions, has an immunosuppressive and anti-shock effect, increases the reactivity of beta-adrenergic receptors to adrenaline and norepinephrine synthesized in the body. The effect of prednisolone one way or another covers almost the entire body, because specific cytoplasmic glucocorticosteroid receptors are found in many organs and tissues. By interacting with them, the drug becomes part of a complex that enhances protein synthesis, including enzymes that control vital processes. The anti-inflammatory effect of prednisolone is due to the suppression of the release of inflammatory mediators by eosinophils and mastocytes; inducing the reproduction of lipomodulins and reducing the number of mast cells that synthesize hyaluronic acid; decreased permeability of capillary walls; stabilization of lysosomal membranes and organelle membranes. Prednisolone acts on all parts of inflammation: it suppresses the formation of inflammatory mediators prostaglandins at the level of arachidonic acid, inhibits the production of pro-inflammatory cytokines, and increases the resistance of cell membranes to adverse factors. The “hand” of prednisolone can be clearly seen in the ongoing changes in the metabolism of proteins, carbohydrates, and lipids. Thus, at the level of protein metabolism, the drug reduces the amount of globulins in the blood, stimulates the synthesis of albumins in the kidneys and liver, suppresses the synthesis and promotes the breakdown of proteins in muscle tissue. As part of fat metabolism, prednisolone stimulates the formation of triglycerides and higher fatty acids, redistributes areas of fat accumulation in favor of the abdomen, shoulder girdle and face, and causes hypercholesterolemia. The effect of the drug on carbohydrate metabolism is expressed in increased absorption of carbohydrates from the gastrointestinal tract, activation of glucose-6-phosphatase (as a result of which glucose flows more intensively from the liver into the blood), activation of gluconeogenesis, and promotion of the development of hyperglycemia.

As for water-electrolyte metabolism, here prednisolone manifests itself by delaying sodium and water in the body, increasing the elimination of potassium, reducing the absorption of calcium in the gastrointestinal tract, “washing out” calcium from bone tissue and increasing its excretion by the kidneys, reducing bone mineral density . The immunosuppressive effect of the drug is associated with the regression of lymphoid tissue it causes, suppression of differentiation and proliferation of lymphocytes, inhibition of the migration of B cells and the interaction of B and T lymphocytes, inhibition of the release of cytokines, and suppression of antibody synthesis. The antiallergic effect of prednisolone is due to the suppression of the synthesis and release of allergy mediators, inhibition of histamine secretion by mastocytes and basophils, a decrease in the number of free basophils, inhibition of the proliferation of lymphoid and connective tissue, a decrease in the number of T and B lymphocytes, desensitization of effector cells in relation to allergy mediators, suppression of antibody formation .

Prednisolone is available in the form of tablets, injection solution, and ointment for external use. The dosage regimen of the drug and the duration of the drug course are established by the doctor individually, based on the indications and severity of the disease. The daily dose is recommended to be taken at a time, taking into account the intensity of secretion of endogenous glucocorticosteroids in the time interval from 6 to 8 am. A high daily dose can be divided into several doses, taking most of the drug in the morning. Before starting pharmacotherapy, the patient should be examined to identify contraindications. This examination should include a cardiac examination, chest x-ray, examination of the gastrointestinal and urogenital tract, visual organs, blood picture, glucose and electrolyte levels in the blood.

Pharmacology

Prednisolone is a synthetic glucocorticosteroid drug, a dehydrated analogue of hydrocortisone. It has anti-inflammatory, anti-allergic, immunosuppressive, anti-shock effects, increases the sensitivity of beta-adrenergic receptors to endogenous catecholamines.

Interacts with specific cytoplasmic receptors (receptors for glucocorticosteroids are found in all tissues, especially in the liver) to form a complex that induces the formation of proteins (including enzymes that regulate vital processes in cells).

The anti-inflammatory effect is 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. Acts on all stages of the inflammatory process: inhibits the synthesis of prostaglandins (Pg) at the level of arachidonic acid (lipocortin inhibits phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, which contribute to inflammation, allergies, etc.), the synthesis of pro-inflammatory cytokines (interleukin- 1, tumor necrosis factor alpha); increases the resistance of the cell membrane to the action of various damaging factors.

Protein metabolism: reduces the amount of globulins in plasma, increases albumin synthesis in the liver and kidneys (with an increase in the albumin/globulin ratio), reduces synthesis and increases protein catabolism in muscle tissue.

Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (fat accumulation occurs mainly in 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 (increasing the flow of glucose from the liver into the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); promotes the development of hyperglycemia.

Water-electrolyte metabolism: retains sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, causes “leaching” of calcium from the bones and increases its renal excretion, reduces the mineralization of bone tissue.

The immunosuppressive effect is caused by the involution of lymphoid tissue, inhibition of the proliferation of lymphocytes (especially T-lymphocytes), suppression of the migration of B cells and the interaction of T and B lymphocytes, inhibition of the release of cytokines (interleukin-1, 2; γ-interferon) from lymphocytes and macrophages and decreased antibody formation.

The 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, suppression of the development of lymphoid and connective tissue, a decrease in the number of T- and B-lymphocytes, mast cells , reducing the sensitivity of effector cells to allergy mediators, suppressing antibody formation, changing the body’s immune response.

In obstructive diseases of the respiratory tract, the effect is mainly due to inhibition of inflammatory processes, prevention or reduction of the severity of swelling of the mucous membranes, reduction of eosinophilic infiltration of the submucosal layer of the bronchial epithelium and deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucosa. Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.

Suppresses the synthesis and secretion of adrenocorticotropic hormone (ACTH) and secondarily the synthesis of endogenous glucocorticosteroids.

Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

Pharmacokinetics

When taken orally, prednisolone is well absorbed from the gastrointestinal tract. Cmax in the blood is reached 1-1.5 hours after oral administration. Up to 90% of the drug binds to plasma proteins: transcortin (cortisol-binding globulin) and albumin. Prednisolone is metabolized in the liver, partially in the kidneys and other tissues, mainly by conjugation with glucuronic and sulfuric acids. Metabolites are inactive.

It is excreted in the bile and kidneys by glomerular filtration and is 80-90% reabsorbed by the tubules. 20% of the dose is excreted unchanged by the kidneys. T1/2 from plasma after oral administration is 2-4 hours.

Release form

30 pcs. - bottles (1) - cardboard packs.

Dosage

The dose of the drug and the duration of treatment are determined by the doctor individually depending on the indications and severity of the disease.

It is recommended to take the entire daily dose of the drug once or twice the daily dose every other day, taking into account the circadian rhythm of endogenous secretion of glucocorticosteroids in the interval from 6 to 8 am. A high daily dose can be divided into 2-4 doses, with a larger dose taken in the morning. The tablets should be taken orally during or immediately after meals with a small amount of liquid.

In acute conditions and as replacement therapy for adults, an initial dose of 20-30 mg/day is prescribed, the maintenance dose is 5-10 mg/day. If necessary, the initial dose can be 15-100 mg/day, maintenance - 5-15 mg/day.

For children, the initial dose is 1-2 mg/kg body weight/day in 4-6 divided doses, maintenance dose is 300-600 mcg/kg/day.

When a therapeutic effect is obtained, the dose is gradually reduced - 5 mg, then 2.5 mg at intervals of 3-5 days, first canceling later doses. With long-term use of the drug, the daily dose should be reduced gradually. Long-term therapy should not be stopped suddenly! The maintenance dose is discontinued more slowly the longer the glucocorticosteroid therapy is used.

In case of stressful effects (infection, allergic reaction, trauma, surgery, mental overload), in order to avoid exacerbation of the underlying disease, the dose of prednisolone should be temporarily increased (by 1.5-3, and in severe cases - by 5-10 times).

Overdose

The side effects described above may increase. It is necessary to reduce the dose of prednisolone. Treatment is symptomatic.

Interaction

The simultaneous administration of prednisolone with inducers of hepatic microsomal enzymes (phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration.

Co-administration of prednisolone with diuretics (especially thiazide and carbonic anhydrase inhibitors) and amphotericin B may lead to increased excretion of potassium from the body.

The simultaneous administration of prednisolone with sodium-containing drugs leads to the development of edema and increased blood pressure.

Co-administration of prednisolone with amphotericin B increases the risk of developing heart failure.

The simultaneous administration of prednisolone with cardiac glycosides worsens their tolerability and increases the likelihood of developing ventricular extrasystole (due to hypokalemia).

Simultaneous administration of prednisolone with indirect anticoagulants - prednisolone enhances the anticoagulant effect of coumarin derivatives.

The simultaneous administration of prednisolone with anticoagulants and thrombolytics increases the risk of bleeding from ulcers in the gastrointestinal tract.

The simultaneous administration of prednisolone with ethanol and NSAIDs increases the risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding (in combination with NSAIDs in the treatment of arthritis, it is possible to reduce the dose of glucocorticosteroids due to the summation of the therapeutic effect).

The simultaneous administration of prednisolone with paracetamol increases the risk of hepatotoxicity (induction of liver enzymes and the formation of a toxic metabolite of paracetamol).

The simultaneous administration of prednisolone with acetylsalicylic acid accelerates its elimination and reduces its concentration in the blood (when prednisolone is discontinued, the level of salicylates in the blood increases and the risk of side effects increases).

The simultaneous administration of prednisolone with insulin and oral hypoglycemic drugs and antihypertensive drugs reduces their effectiveness.

The simultaneous administration of prednisolone with vitamin D reduces its effect on the absorption of Ca 2+ in the intestine.

The simultaneous administration of prednisolone with growth hormone reduces the effectiveness of the latter, and with praziquantel - its concentration.

The simultaneous administration of prednisolone with m-anticholinergics (including antihistamines and tricyclic antidepressants) and nitrates increases intraocular pressure.

The simultaneous administration of prednisolone with isoniazid and mexiletine increases the metabolism of isoniazid and mexiletine (especially in “fast” acetylators), which leads to a decrease in their plasma concentrations.

Co-administration of prednisolone with carbonic anhydrase inhibitors and amphotericin B increases the risk of developing osteoporosis.

The simultaneous administration of prednisolone with indomethacin - displacing prednisolone from its connection with albumin, increases the risk of developing its side effects.

The simultaneous administration of prednisolone with ACTH enhances the effect of prednisolone.

The simultaneous administration of prednisolone with ergocalciferol and parathyroid hormone prevents the development of osteopathy caused by prednisolone.

The simultaneous administration of prednisolone with cyclosporine and ketoconazole - cyclosparine (inhibits metabolism) and ketoconazole (reduces clearance) increases toxicity.

The appearance of hirsutism and acne is facilitated by the simultaneous use of other steroid hormonal drugs (androgens, estrogens, anabolic steroids, oral contraceptives).

The simultaneous administration of prednisolone with estrogens and oral estrogen-containing contraceptives reduces the clearance of prednisolone, which may be accompanied by an increase in the severity of its therapeutic and toxic effects.

Concomitant administration of prednisolone with mitotane and other inhibitors of adrenal function may necessitate an increase in the dose of prednisolone.

When used simultaneously with live antiviral vaccines and against the background of other types of immunization, it increases the risk of viral activation and the development of infections.

With simultaneous use of prednisolone with antipsychotics (neuroleptics) and azathioprine, the risk of developing cataracts increases.

The simultaneous administration of antacids reduces the absorption of prednisolone.

When used simultaneously with antithyroid drugs, the clearance of prednisolone decreases and with thyroid hormones increases.

When used concomitantly with immunosuppressants, the risk of developing infections and lymphoma or other lymphoproliferative disorders associated with the Epstein-Barr virus increases.

Tricyclic antidepressants may increase the severity of depression caused by taking glucocorticosteroids (not indicated for the treatment of these side effects).

Increases (with long-term therapy) the content of folic acid.

Hypokalemia caused by glucocorticosteroids can increase the severity and duration of muscle blockade due to muscle relaxants.

In high doses, it reduces the effect of somatropin.

Side effects

The incidence and severity of side effects depends on the duration of use, the size of the dose used and the ability to comply with the circadian rhythm of prednisolone administration. When using prednisolone, the following may occur:

From the endocrine system: decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing syndrome (moon-shaped face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, stretch marks), delayed sexual development in children.

From the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding and perforation of the gastrointestinal tract wall, increased or decreased appetite, indigestion, flatulence, hiccups. In rare cases, increased activity of liver transaminases and alkaline phosphatase.

From the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of heart failure, ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction, the necrosis focus spreads, the formation of scar tissue slows down, which can lead to rupture of the heart muscle.

From the nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive, psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor of the cerebellum, headache, convulsions.

From the senses: 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.

From the metabolic side: increased excretion of calcium, hypocalcemia, increased body weight, negative nitrogen balance (increased breakdown of proteins), increased sweating.

Caused by mineralocorticoid activity: fluid and sodium retention in the body (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

From the musculoskeletal system: slower growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoparosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and femur), rupture of muscle tendons, steroid myopathy, decreased muscle mass (atrophy).

From the skin and mucous membranes: delayed wound healing, petechiae, ecchymoses, thinning of the skin, hyper- or hypopigmentation, acne, stretch marks, tendency to develop pyoderma and candidiasis.

Allergic reactions: skin rash, itching, anaphylactic shock.

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

Indications

systemic connective tissue diseases (systemic lupus erythematosus, scleroderma, periarteritis nodosa, dermatomyositis, rheumatoid arthritis);
acute and chronic inflammatory diseases of the joints - gouty and psoriatic arthritis, osteoarthritis (including post-traumatic), polyarthritis, glenohumeral periarthritis, ankylosing spondylitis (Bechterew's disease), juvenile arthritis, Still's syndrome in adults, bursitis, nonspecific tenosynovitis, synovitis and epicondylitis ;
acute rheumatic fever, rheumatic carditis;
bronchial asthma (severe form), status asthmaticus;
acute and chronic allergic diseases - incl. allergic reactions to drugs and foods, serum sickness, urticaria, allergic rhinitis, Quincke's edema, drug exanthema, hay fever;
skin diseases - pemphigus, psoriasis, eczema, atopic dermatitis (common neurodermatitis), contact dermatitis (affecting a large surface of the skin), toxicerma, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), bullous dermatitis herpetiformis, Stevens-Johnson syndrome ;
cerebral edema (including due to a brain tumor or associated with surgery, radiation therapy or head injury) after prior parenteral use;
allergic eye diseases: allergic forms of conjunctivitis;
inflammatory eye diseases - sympathetic ophthalmia, severe sluggish anterior and posterior uveitis, optic neuritis;
primary or secondary adrenal insufficiency (including the condition after removal of the adrenal glands);
congenital adrenal hyperplasia;
kidney diseases of autoimmune origin (including acute glomerulonephritis); nephrotic syndrome (including against the background of lipoid nephrosis);
subacute thyroiditis;
diseases of the blood and hematopoietic system - agranulocytosis, panmyelopathy, autoimmune hemolytic anemia, acute lympho- and myeloid leukemia, lymphogranulomatosis, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocyte anemia), congenital (erythroid) hypoplastic anemia;
interstitial lung diseases - acute alveolitis, pulmonary fibrosis, stage II-III sarcoidosis;
tuberculous meningitis, pulmonary tuberculosis, aspiration pneumonia (in combination with specific chemotherapy);
berylliosis, Loeffler's syndrome (unresponsive to other therapy); lung cancer (in combination with cytostatics);
multiple sclerosis;
gastrointestinal diseases - ulcerative colitis, Crohn's disease, local enteritis;
hepatitis;
prevention of graft rejection during organ transplantation;
hypercalcemia due to cancer, nausea and vomiting during cytostatic therapy;
multiple myeloma.

Contraindications

For short-term use for health reasons, the only contraindication is hypersensitivity to prednisolone or the components of the drug.

The drug contains lactose. Patients with rare hereditary diseases such as lactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not take the drug.

Features of application

Use during pregnancy and breastfeeding

During pregnancy (especially in the first trimester) it is used only for health reasons.

Since glucocorticosteroids pass into breast milk, if it is necessary to use the drug during breastfeeding, it is recommended to stop breastfeeding.

Use for liver dysfunction

Carefully

severe chronic liver failure.

Use for renal impairment

Carefully

severe chronic renal disease, nephrourolithiasis.

Use in children

special instructions

Before starting treatment (if impossible due to the urgency of the condition, during treatment), the patient should be examined to identify 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, and visual organs; control of blood formula, glucose and electrolytes in blood plasma. During treatment with prednisolone (especially long-term), observation by an ophthalmologist, monitoring of blood pressure, water and electrolyte balance, as well as peripheral blood patterns and blood glucose levels are necessary.

In order to reduce side effects, antacids can be prescribed, as well as increasing the intake of potassium in the body (diet, potassium supplements). Food should be rich in proteins, vitamins, and limit the content of fats, carbohydrates and table salt.

The effect of the drug is enhanced in patients with hypothyroidism and liver cirrhosis.

The drug may worsen existing emotional instability or psychotic disorders. If a history of psychosis is indicated, prednisolone in high doses is prescribed under the strict supervision of a physician.

In stressful situations during maintenance treatment (for example, surgery, trauma or infectious diseases), the dose of the drug should be adjusted due to an increased need for glucocorticosteroids.

Patients should be carefully monitored for a year after the end of long-term therapy with prednisolone due to the possible development of relative insufficiency of the adrenal cortex in stressful situations.

With sudden withdrawal, especially in the case of previous use of high doses, withdrawal syndrome may develop (anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness), as well as an exacerbation of the disease for which prednisolone was prescribed.

During treatment with prednisolone, vaccination should not be carried out due to a decrease in its effectiveness (immune response).

When prescribing prednisolone for intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously treat with bactericidal antibiotics.

In children during long-term treatment with prednisolone, careful monitoring of growth dynamics is necessary. Children who during the treatment period were in contact with patients with measles or chickenpox are prescribed specific immunoglobulins prophylactically.

Due to the weak mineralocorticoid effect, prednisolone is used in combination with mineralocorticoids for replacement therapy for adrenal insufficiency.

In patients with diabetes mellitus, blood glucose levels should be monitored and therapy adjusted if necessary.

X-ray monitoring of the osteoarticular system (images of the spine, hand) is indicated.

Prednisolone in patients with latent infectious diseases of the kidneys and urinary tract can cause leukocyturia, which may have diagnostic value.

Prednisolone increases the content of 11- and 17-oxyketocorti metabolites. In Addison's disease, simultaneous administration of barbiturates should be avoided - there is a risk of developing acute adrenal insufficiency (Addisonian crisis).