Less toxic analogues of prednisolone are better. Prednisolone is an effective drug for injections in emergency situations. Terms and conditions of storage


GCS for injections

Active substance

Release form, composition and packaging

Injection transparent, colorless or slightly yellowish or greenish-yellowish.

Excipients: nicotinamide, sodium metabisulphite, disodium edetate, sodium hydroxide, water for injections.

1 ml - ampoules (3) - plastic trays (1) - cardboard boxes.

pharmachologic effect

Synthetic glucocorticoid drug, dehydrated analogue. It has anti-inflammatory, anti-allergic, immunosuppressive effects, increases the sensitivity of beta-adrenergic receptors to endogenous catecholamines.

Interacts with specific cytoplasmic receptors (there are receptors for corticosteroids 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.)

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

Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat occurs mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.

Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract; increases the activity of glucose-6-phosphatase (increased intake from the liver into the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); contributes to the development of hyperglycemia.

Water-electrolyte metabolism: retains Na + and water in the body, stimulates the excretion of K + (mineralocorticoid activity), reduces the absorption of Ca 2+ from the gastrointestinal tract, reduces the mineralization of bone tissue.

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. It acts on all stages of the inflammatory process: it inhibits the synthesis of prostaglandins at the level of arachidonic acid (lipocortin inhibits phospholipase A2, inhibits 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, etc.); increases the resistance of the cell membrane to the action of various damaging factors.

The immunosuppressive effect is due to the involution of lymphoid tissue, inhibition of the proliferation of lymphocytes (especially T-lymphocytes), suppression of B-cell migration and the interaction of T- and B-lymphocytes, inhibition of the release of cytokines (interleukin-1, 2; interferon gamma) from lymphocytes and macrophages and decreased antibody production.

Prednisolone is metabolized in the liver, partly in the kidneys and other tissues, mainly by conjugation with glucuronic and sulfuric acids. Metabolites are inactive.

Excreted in the bile and urine by glomerular filtration and 80-90% reabsorbed by the tubules. 20% of the dose is excreted by the kidneys unchanged. T 1/2 from plasma after intravenous administration of 2-3 hours.

Indications

Prednisolone is used for emergency therapy in conditions requiring a rapid increase in the concentration of corticosteroids in the body:

- shock conditions (burn, traumatic, surgical, toxic, cardiogenic) - with the ineffectiveness of vasoconstrictors, plasma-substituting drugs and other symptomatic therapy;

- allergic reactions (acute severe forms), hemotransfusion shock, anaphylactic shock, anaphylactoid reactions;

- cerebral edema (including against the background of a brain tumor or associated with surgery, radiation therapy or head trauma);

- bronchial asthma (severe form), status asthmaticus;

- systemic connective tissue diseases (systemic lupus erythematosus, rheumatoid arthritis);

- acute adrenal insufficiency;

- thyrotoxic crisis;

- acute hepatitis, hepatic coma;

- reduction of inflammation and prevention of cicatricial narrowing (in case of poisoning with caustic fluids).

Contraindications

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

In children during the period of growth, corticosteroids should be used only according to absolute indications and under the most careful supervision of the attending physician.

FROM caution the drug should be prescribed for the following diseases and conditions:

- diseases of the gastrointestinal tract - peptic ulcer of the stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis;

- pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination;

- immunodeficiency states (including AIDS or HIV infection);

- diseases of the cardiovascular system (including a recent myocardial infarction - in patients with acute and subacute myocardial infarction, the focus of necrosis may spread, slowing down the formation of scar tissue and, as a result, rupture of the heart muscle), severe chronic heart failure, arterial hypertension, hyperlipidemia);

- endocrine diseases - diabetes mellitus (including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, obesity (III - IV stage);

- severe chronic renal and / or liver failure, nephrourolithiasis;

- hypoalbuminemia and conditions predisposing to its occurrence;

- systemic osteoporosis, myasthenia gravis, acute psychosis, poliomyelitis (with the exception of the form of bulbar encephalitis), open and angle-closure glaucoma;

- pregnancy.

Dosage

The dose of Prednisolone and the duration of treatment are set by the doctor individually, depending on the indications and the severity of the disease.

Prednisolone is administered intravenously (drip or jet) or intramuscularly. In / in the drug is usually administered first in a jet, then drip.

At acute adrenal insufficiency a single dose of 100-200 mg for 3-16 days.

At bronchial asthma the drug is administered depending on the severity of the disease and the effectiveness of complex treatment from 75 to 675 mg per course of treatment from 3 to 16 days; in severe cases, the dose may be increased to 1400 mg per course of treatment or more with a gradual dose reduction.

At status asthmaticus Prednisolone is administered at a dose of 500-1200 mg/day, followed by a decrease to 300 mg/day and switching to maintenance doses.

At thyrotoxic crisis administer 100 mg of the drug in a daily dose of 200-300 mg; if necessary, the daily dose can be increased to 1000 mg. The duration of administration depends on the therapeutic effect, usually up to 6 days.

At shock resistant to standard therapy, Prednisolone at the beginning of therapy is usually administered by jet, after which they switch to drip administration. If blood pressure does not increase within 10-20 minutes, repeat the jet administration of the drug. After removing from the state of shock, continue drip administration until blood pressure stabilizes. A single dose is 50-150 mg (in severe cases, up to 400 mg). The drug is re-administered after 3-4 hours. The daily dose can be 300-1200 mg (with subsequent dose reduction).

At acute hepatic-renal failure(for acute poisoning, in the postoperative and postpartum periods, etc.), Prednisolone is administered at 25-75 mg / day; if indicated, the daily dose can be increased to 300-1500 mg / day and above.

At rheumatoid arthritis and systemic lupus erythematosus Prednisolone is administered in addition to the systemic administration of the drug at a dose of 75-125 mg / day for no more than 7-10 days.

At acute hepatitis Prednisolone is administered at 75-100 mg/day for 7-10 days.

At poisoning with caustic fluids with burns of the digestive tract and upper respiratory tract Prednisolone is prescribed at a dose of 75-400 mg / day for 3-18 days.

If intravenous administration is not possible, Prednisolone is administered intramuscularly in the same doses. After stopping the acute condition, Prednisolone is prescribed orally in tablets, followed by a gradual decrease in the dose.

With prolonged use of the drug, the daily dose should be reduced gradually. Long-term therapy should not be stopped abruptly!

Side effects

The frequency of development and severity of side effects depends on the duration of use, the size of the dose used and the possibility of observing the circadian rhythm of prednisolone administration.

When using Prednisolone, you may experience:

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

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

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

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

From the sense organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos, sudden loss of vision (with parenteral administration in the head, neck, turbinates, scalp, it is possible deposition of crystals of the drug in the vessels of the eye).

From the side of metabolism: increased excretion of calcium, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating.

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

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

From the skin and mucous membranes: delayed wound healing, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, steroid acne, striae, a tendency to develop pyoderma and candidiasis.

Allergic reactions: skin rash, itching, anaphylactic shock, local allergic reactions.

Local for parenteral administration: burning, numbness, pain, tingling at the injection site, infection at the injection site, rarely - necrosis of surrounding tissues, scarring at the injection site; atrophy of the skin and subcutaneous tissue with intramuscular injection (especially dangerous is the introduction into the deltoid muscle).

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

Overdose

It is possible to increase the side effects described above.

It is necessary to reduce the dose of prednisolone. Treatment is symptomatic.

drug interaction

Pharmaceutical incompatibility of Prednisolone with other intravenously administered drugs is possible - it is recommended to administer it separately from other drugs (in / in a bolus, or through another dropper, as a second solution). When mixing a solution of prednisolone with heparin, a precipitate forms.

Co-administration of prednisolone with:

inducers of hepatic microsomal enzymes(phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration;

diuretics(especially "thiazide" and carbonic anhydrase inhibitors) and amphotericin B may lead to increased excretion of K + from the body and an increase in the risk of developing heart failure;

with sodium preparations- to the development of edema and increased blood pressure;

cardiac glycosides- their tolerance worsens and the likelihood of developing ventricular extrasitolia increases (due to the hypokalemia caused);

indirect anticoagulants- weakens (rarely enhances) their effect (dose adjustment is required);

anticoagulants and thrombolytics- increased risk of bleeding from ulcers in the gastrointestinal tract;

ethanol and NSAIDs- the risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding increases (in combination with NSAIDs in the treatment of arthritis, it is possible to reduce the dose of GCS due to the summation of the therapeutic effect);

paracetamol - the risk of developing hepatotoxicity (induction of liver enzymes and the formation of a toxic metabolite of paracetamol) increases;

- accelerates its excretion and reduces the concentration in the blood (with the abolition of prednisolone, the level of salicylates in the blood increases and the risk of side effects increases);

insulin and oral hypoglycemic drugs, antihypertensive drugs - their effectiveness decreases;

vitamin D - its effect on the absorption of Ca 2+ in the intestine decreases;

somatotropic hormone - reduces the effectiveness of the latter, and with praziquantel - its concentration;

M-anticholinergics(including antihistamines and tricyclic antidepressants) and nitrates- promotes increase in intraocular pressure;

isoniazid and mexiletin- increases their metabolism (especially in "slow" acetylators), which leads to a decrease in their plasma concentrations.

Carbonic anhydrase inhibitors and loop diuretics may increase the risk of osteoporosis.

Indomethacin, displacing prednisone from its association with albumin, increases the risk of its side effects.

ACTH enhances the action of prednisone.

Ergocalciferol and parathyroid hormone prevent the development of osteopathy caused by prednisone.

Cyclosporine and ketoconazole, by slowing down the metabolism of prednisolone, can in some cases increase its toxicity.

Simultaneous administration of androgens and steroid anabolic drugs with prednisolone contributes to the development of peripheral edema and hirsutism, the appearance of acne.

Estrogens and oral estrogen-containing contraceptives reduce the clearance of prednisolone, which may be accompanied by an increase in the severity of its action.

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 virus activation and the development of infections.

Antipsychotics (neuroleptics) and azathioprine increase the risk of developing cataracts when prednisolone is prescribed.

With simultaneous use with antithyroid drugs, it decreases, and with thyroid hormones, the clearance of prednisolone increases.

special instructions

During treatment with Prednisolone (especially long-term), it is necessary to observe an ophthalmologist, control blood pressure, the state of water and electrolyte balance, as well as pictures of peripheral blood and blood glucose levels.

In order to reduce side effects, you can prescribe antacids, as well as increase the intake of K + in the body (diet, potassium preparations). Food should be rich in proteins, vitamins, with limited content of fats, carbohydrates and salt.

The effect of the drug is enhanced in patients with hypothyroidism and cirrhosis of the liver. The drug may increase existing emotional instability or psychotic disorders. When indicating a history of psychosis, prednisolone in high doses is prescribed under the strict supervision of a physician.

Caution should be used in acute and subacute myocardial infarction - it is possible to spread the focus of necrosis, slow the formation of scar tissue and rupture the heart muscle.

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

With sudden cancellation, especially in the case of previous use of high doses, the development of a withdrawal syndrome (anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness) is possible, as well as an exacerbation of the disease, for which 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 the dynamics of growth and development is necessary. Children who during the period of treatment were in contact with patients with measles or chickenpox are prescribed specific immunoglobulins prophylactically.

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

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

X-ray control of the osteoarticular system (spine, hand) is shown.

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

Prednisolone increases the content of 11- and 17-hydroxyketocorticosteroid metabolites.

Pregnancy and lactation

During pregnancy (especially in the first trimester), they are used only for health reasons. With prolonged therapy during pregnancy, the possibility of impaired fetal growth is not ruled out. In the case of use in the III trimester of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

List B. The drug should be stored at a temperature not exceeding 25 ° C, out of the reach of children. Shelf life - 3 years. Do not use after the expiry date stated on the packaging.

Prednisolone ointment is an anti-allergic, anti-inflammatory drug with an immunosuppressive effect. This is a synthetic glucocoricoid (hormone), during the treatment of which the accumulation of immune cells is inhibited in the damaged area of ​​the body, which reduces the signs of inflammatory processes. We will learn in more detail what the composition of the ointment is, what it is used for, the treatment regimen and possible side effects.

How to replace Prednisolone ointment: analogues

  1. Fusimet. The ointment is prescribed for the treatment of purulent-inflammatory processes of the skin: furunculosis, impetigo, folliculitis, superficial abrasions and wounds. The drug is effective in the treatment of stage burns.
  2. Petroleum. Non-steroidal substitute for Prednisolone, prepared from refined oil according to homeopathic rules. Indicated for chronic skin diseases: eczema, neurodermatitis. Shows good results in the treatment of rheumatism, joint sprains, skin cracks, pathologically unpleasant smell of sweat.
  3. Decortin. It is effective in systemic diseases: rheumatoid arthritis, dermatomyositis, periarteritis nodosa. It is prescribed for use in Bechterew's disease, bursitis, rheumatic fever.

Release form and composition of the ointment Prednisolone

Prednisolone is produced in the form of a topical ointment in tubes of 10, 15 g, packed in cardboard boxes, each of which contains an annotation.

The active ingredient of the hormonal drug is the component of the same name prednisone. Auxiliary substances in the composition of the ointment are:

  • emulsifier 1;
  • stearic acid;
  • petrolatum;
  • propylparaben;
  • methylparaben;
  • purified water.

pharmachologic effect

Prednisolone is a hormone of the adrenal cortex that inhibits the functional activity of tissue macrophages and leukocytes, limiting their migration to the focus of inflammation. The substance has the ability to reduce the permeability of blood capillaries due to the release of histamine. This inhibits collagen formation and fibroblast activity. Prednisolone in liver cells enhances the synthesis of glucose from protein metabolism and the activity of glycogen synthetase.

High absorbability is noted 90 minutes after applying the ointment. The drug is excreted unchanged by the kidneys. In high doses, prednisolone increases the excitability of brain tissue.

What ointment helps from: indications for use

According to the instructions for use, Prednisolone ointment (international name of the drug: Prednisolone) is prescribed for non-infectious skin lesions, characterized by weeping, itching, rash:

  • Hives.
  • Seborrheic, atopic dermatitis.
  • Lupus erythematosus.
  • Limited, diffuse neurodermatitis.
  • Psoriasis.
  • Fissures of the rectum, hemorrhoids.
  • Toxidermia.
  • Edema of the subcutaneous tissue.
  • Skin manifestations of allergy.
  • Eczema.
  • Complete or partial alopecia.
  • Inflammatory diseases of the eyes.
  • allergic rhinitis.

Method of application and dosage

Treatment with Prednisolone is carried out externally.

The ointment is applied in a thin layer to the affected area once a day. The course of treatment with the drug will be prescribed by the doctor individually. According to the instructions, the average duration of therapy is weeks. The frequency of application of Prednisolone ointment at the end of the course should be halved so that an overdose does not occur. In chronic pathology, long-term therapy is allowed under the supervision of a doctor, and it needs to be continued for several more days after all symptoms have been eliminated to prevent a possible relapse.

It is allowed to use an ointment under the bandage to improve the therapeutic effect.

Contraindications and side effects

Do not forget that the ointment is hormonal, so the consequences of using the drug Prednisolone may be accompanied by unpleasant side reactions of the body. Among them, excessive hair on the skin, impaired immunity, viral diseases, stretch marks due to the destruction of collagen, excessive pigmentation, dry skin, steroid acne, folliculitis, erythema.

Do not use Prednisolone ointment for skin tuberculosis or syphilitic lesions. Absolute contraindications of the drug also include skin tumors, bacterial infections, viral pathologies caused by skin lesions, peptic ulcer of the digestive system, intolerance to ointment substances.

If the patient suffers from any of the above diseases, the doctor should replace Prednisolone with another drug.

Application for children and pregnant women

Prednisolone during pregnancy in any form is prohibited. The gynecologist in extreme cases can make an exception if the benefit to the woman outweighs the risks of the negative effects of the steroid on fetal development. The active substance of the ointment is very quickly absorbed through the placenta, and then excreted along with mother's milk, so during lactation, feeding the baby should be stopped. Prednisolone ointment for children is prescribed from one year.

But hormone therapy with the drug is carried out under the supervision of a pediatrician. Uncontrolled use of the hormone should not be allowed, the total duration of which should not be more than 7 days.

special instructions

Judging by the opinions of experts, it is undesirable to combine the use of Prednisolone ointment with salicylates in order to avoid the risk of bleeding, diuretics, in order to avoid electrolyte disturbances, cardiac glycosides, in order to exclude the hypoglycemic effect and with anticoagulants, so that there is no increase in the anticoagulant effect. Alcoholic drinks do not affect the work of the ointment.

Reviews

Elena, 31 years old : In a pharmacy, I read the indications for the use of Prednisolone ointment and decided to buy an inexpensive drug for dermatitis on the skin of the face. The ointment in a matter of days helped to get rid of the rash on the cheeks and redness on the wings of the nose. Judging by the description, the drug is also effective for neurodermatitis, eczema, itching, and costs only a little more than 50 rubles.

Alexander, 34 years old : This is the best remedy for dry eczema, which has been tormenting me for several years.

In the spring-winter period, my skin begins to peel off on various parts of the body, and then the symptoms turn into pain, bleeding, itching, burning. After I started using Prednisolone ointment, after 2 days I felt better, and after 2 weeks the eczema disappeared. Before that, he suffered from this sore from September to April.

Prednisolone (in Latin INN Prednisolonum) is a unique drug that is a synthetic analogue of the adrenal cortex.

It has an anti-inflammatory and antiallergic effect. Pharmacological group Glucocorticosteroids.

It also reduces the amount of protein in the plasma and performs the synthesis of the protein that binds calcium. It acts as an auxiliary substance and stimulates the formation of cells in the bone marrow, retains water, phosphate and sodium, enhances receptor sensitivity, reduces the number of immunosuppressive diseases by reducing them.

Another function is increased gluconeogenesis.

What is prescribed, indications for use

It is prescribed for a whole list of diseases: collagenosis, rheumatoid arthritis, polyarthritis, asthma, leukemia, mononucleosis, neurodermatitis, eczema, allergies, adrenal insufficiency, anemia, pancreatitis, collapse and shock, conjunctivitis, blepharitis, inflammation of different parts of the eye, as well as after eye injuries.

Analogues are cheaper

There is no single answer to the question of which is better. Everything is decided by the price. But at the same time, all drugs are good enough and cope with the functions assigned to them. Consult with your doctor before taking, and he will individually prescribe one of these drugs.

Methylprednisolone and prednisolone difference

The main difference and differences between these largely similar drugs are side effects.

Because some people tolerate prednisone better than others methylprednisolone. Another important difference is cost. Here, plus it is worth putting prednisolone.

Prednisolone instructions for use

The instruction is individual for each person. The form of the tablet or ampoule also plays an important role.

Tablets

In an acute condition, you need to drink 4 to 6 tablets per day, the exact dose is individual. maintenance dose of the tablet. With nephrosis and rheumatism, the doses are higher, after which they are gradually reduced.

In ampoules intramuscularly

It can also be administered intravenously into the blood or intramuscularly, including through the introduction of droppers into the blood.

In this case, the infusion should be done as deeply as possible. In shock, the dose is a milligram, with repeated administration of mg.

During pregnancy

Pregnancy is included in the list of contraindications, so prednisolone is prescribed in exceptional cases and is used during pregnancy with extreme caution.

For kids

The calculation for children is the following on the order of milligrams per kilogram of weight per day. The dose is stretched over receptions.

Medicines containing prednisolone

Decortin

International name: Prednisolone (Prednisolone)

Dosage form: tablets

Pharmachologic effect:

Indications:

Dermozolon

International name: Prednisolone + Clioquinol (Prednisolone + Clioquinol)

Dosage form:

Pharmachologic effect: Dermozolon is a combined preparation for topical application, it has anti-inflammatory, anti-allergic, antimicrobial and fungicidal effects.

Indications: Dyshidrosis, dermatitis of various etiologies, complicated by a bacterial or fungal infection, bacterial secondarily infected eczema, interdigital mycosis, itching, anogenital eczema, superficial skin infections.

Inflanefran

International name: Prednisolone (Prednisolone)

Dosage form: eye drops

Pharmachologic effect: GCS, a dehydrated analogue of hydrocortisone, has a pronounced anti-inflammatory, anti-allergic and anti-exudative effect.

Interacting

Indications: Non-infectious inflammatory diseases of the anterior segment of the eye - iritis, iridocyclitis, uveitis, episcleritis, scleritis, conjunctivitis, parenchymal

Novo-Prednisolone

International name: Prednisolone (Prednisolone)

Dosage form: tablets

Pharmachologic effect: GCS is a dehydrated analogue of hydrocortisone that inhibits the release of interleukin1, interleukin2, interferon gamma from lymphocytes and macrophages.

Indications: Systemic connective tissue diseases (SLE, scleroderma, periarteritis nodosa, dermatomyositis, rheumatoid arthritis). Acute and chronic

Prednihexal

International name: Prednisolone (Prednisolone)

Dosage form:

Pharmachologic effect: GCS is a dehydrated analogue of hydrocortisone that inhibits the release of interleukin1, interleukin2, interferon gamma from lymphocytes and macrophages.

Indications:

Prednisolone 5 mg Jenafarm

International name: Prednisolone (Prednisolone)

Dosage form: tablets

Pharmachologic effect: GCS is a dehydrated analogue of hydrocortisone that inhibits the release of interleukin1, interleukin2, interferon gamma from lymphocytes and macrophages.

Indications: Systemic connective tissue diseases (SLE, scleroderma, periarteritis nodosa, dermatomyositis, rheumatoid arthritis).

Acute and chronic

prednisolone acetate

International name: Prednisolone (Prednisolone)

Dosage form: lyophilisate for solution for intravenous and intramuscular injection, solution for intravenous and intramuscular injection, suspension for intramuscular injection

Pharmachologic effect: GCS is a dehydrated analogue of hydrocortisone that inhibits the release of interleukin1, interleukin2, interferon gamma from lymphocytes and macrophages.

Indications: Shock (burn, traumatic, surgical, toxic, cardiogenic) with the ineffectiveness of others.

therapy. Allergic reactions (acute, severe

Prednisolone hemisuccinate

International name: Prednisolone (Prednisolone)

Dosage form: lyophilisate for solution for intravenous and intramuscular injection, solution for intravenous and intramuscular injection, suspension for intramuscular injection

Pharmachologic effect: GCS is a dehydrated analogue of hydrocortisone that inhibits the release of interleukin1, interleukin2, interferon gamma from lymphocytes and macrophages.

Indications: Shock (burn, traumatic, surgical, toxic, cardiogenic) with the ineffectiveness of other therapy. Allergic reactions (acute, severe

Prednisolone-AKOS

International name: Prednisolone (Prednisolone)

Dosage form: ointment for external use

Pharmachologic effect: Dehydrated analog of hydrocortisone. When applied externally, it has anti-inflammatory, anti-allergic, antipruritic and anti-exudative

Indications: Urticaria, atopic dermatitis, diffuse neurodermatitis, lichen simplex chronicus (limited neurodermatitis), eczema, seborrheic dermatitis, discoid

Elderly people over 65 years of age should make an appointment with a doctor while taking the drug. In such people, side effects are detected in 90% of cases. Therefore, if it is possible to replace the drug with another drug, then it is recommended to refuse the use of Prednisolone.

How to take the drug for children?

The dosage of tablets is calculated depending on body weight. For one kilogram of weight it is necessary to give a milligram of the drug. As a maintenance dose, 0.5 milligrams per kilogram of body weight is prescribed.
The dosage of injections for children under one year old is calculated based on weight.

One milligram of solution must be injected per kilogram. Adolescents from one to fourteen years of age are injected with a milligram of the drug per kilogram of weight.

Prednisolone during pregnancy should be used if there is a real threat to the life of the expectant mother, since the drug has a teratogenic effect. Results in rodents have shown that when the drug is used during pregnancy, there is a risk of giving birth to premature babies. A child may be born with a cleft palate. The fetus may have an increased pulse, which leads to an unwanted miscarriage.

During breastfeeding, the use of the drug is strictly prohibited.

The hormone is able to penetrate into breast milk and adversely affect the health of the child.

After taking the drug by the mother, the baby must be transferred to artificial mixtures.

Table of analogues

Many patients think about how to replace the medicine. To date, there are a large number of cheap analogues, as well as new generation medicines.

Preparations Description Contraindications
PrednisonePrednisone is a similar drug that replaces Prednisolone.Prednisone is not recommended for patients with gastric and colonic ulcers.
MethylprednisoloneEasily relieves inflammation.

Has an anti-shock effect.

Contraindicated in people with eye damage and tuberculosis.
DexamethasoneDexamethasone is a drug containing sodium phosphate in its composition.Dexamethasone is not recommended for hypersensitive patients.
MetipredAvailable in the form of tablets and lyophilisate.Contraindicated in people with ulcerative lesions.
FormoterolIt is a bronchodilator drug.Contraindicated for allergy sufferers.
Prednisolone HemisuccinateBefore using the remedy, the pulse should be even and calm.

The drug inhibits the function of leukocytes.

Contraindicated in people with a tumor
TriamcinoloneSuppresses the performance of tissue macrophages.Contraindicated in patients with a history of acute psychosis.

Interaction with other drugs

  • When taken simultaneously with salicylates, the risk of bleeding increases;
  • Diuretics disrupt electrolyte balance;
  • Hypoglycemic drugs reduce the amount of glucose;
  • Glycosides cause intoxication;
  • Hypotensins cause a weakening of the effect of the drug;
  • Somatropins cause a decrease in absorption;
  • If you combine oral contraceptives containing estrogen, then an increase in the effectiveness of the drug may occur;
  • Carbutamide and azathioprine are at risk of developing cataracts;
  • Nitrates and M-anticholinergics increase intraocular pressure;

pharmachologic effect

GKS. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of ​​inflammation. Violates the ability of macrophages to phagocytosis, as well as to the formation of interleukin-1. Contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of ​​inflammation. Reduces capillary permeability due to the release of histamine. Suppresses the activity of fibroblasts and the formation of collagen.
Inhibits the activity of phospholipase A 2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce the production of prostaglandins.
Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed into the lymphoid tissue; inhibits the formation of antibodies.
Prednisolone inhibits the release of pituitary ACTH and b-lipotropin, but does not reduce the level of circulating b-endorphin. Inhibits the secretion of TSH and FSH.
When applied directly to the vessels, it has a vasoconstrictor effect.
Prednisolone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys, and increases the activity of gluconeogenesis enzymes. In the liver, prednisolone enhances the deposition of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from protein metabolism products. An increase in blood glucose stimulates the secretion of insulin.
Prednisolone inhibits the uptake of glucose by fat cells, which leads to the activation of lipolysis. However, due to an increase in insulin secretion, lipogenesis is stimulated, which contributes to the accumulation of fat.
It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone, it affects the processes of water-electrolyte metabolism: it promotes the excretion of potassium and calcium ions, the retention of sodium and water ions in the body. Osteoporosis and Itsenko-Cushing's syndrome are the main factors limiting long-term therapy with corticosteroids. As a result of the catabolic action, growth suppression in children is possible.
In high doses, prednisolone can increase the excitability of brain tissue and help lower the seizure threshold. Stimulates excess production of hydrochloric acid and pepsin in the stomach, which leads to the development of peptic ulcers.
With systemic use, the therapeutic activity of prednisolone is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.
With external and local application, the therapeutic activity of prednisolone is due to anti-inflammatory, anti-allergic and anti-exudative (due to the vasoconstrictor effect) action.
Compared with hydrocortisone, the anti-inflammatory activity of prednisolone is 4 times greater, and the mineralocorticoid activity is 0.6 times less.

Pharmacokinetics

When taken orally, it is well absorbed from the gastrointestinal tract. The maximum plasma concentration is observed after 90 minutes. In plasma, most prednisolone binds to transcortin (cortisol-binding globulin). It is metabolized mainly in the liver.
The half-life is about 200 minutes. Excreted by the kidneys unchanged - 20%.

Indications

For oral and / m: rheumatism; rheumatoid arthritis; dermatomyositis; nodular periarteritis; scleroderma; ankylosing spondylitis; bronchial asthma, status asthmaticus; acute and chronic allergic diseases; Addison's disease, acute adrenal insufficiency, adrenogenital syndrome; hepatitis, hepatic coma, hypoglycemic conditions, lipoid nephrosis; agranulocytosis, various forms of leukemia, lymphogranulomatosis, thrombocytopenic purpura, hemolytic anemia; chorea; pemphigus, eczema, itching, exfoliative dermatitis, psoriasis, pruritus, eczema, seborrheic dermatitis, lupus erythematosus, erythroderma, psoriasis, alopecia.
For use in ophthalmology: allergic, chronic and atypical conjunctivitis and blepharitis; inflammation of the cornea with intact mucosa; acute and chronic inflammation of the anterior segment of the choroid, sclera and episclera; sympathetic inflammation of the eyeball; after injuries and operations with prolonged irritation of the eyeballs.
For intra-articular administration: chronic polyarthritis, post-traumatic arthritis, osteoarthritis of large joints, rheumatic lesions of individual joints, arthrosis.
For infiltration introduction into tissues: epicondylitis, tendovaginitis, bursitis, humeroscapular periarthritis, keloids, sciatica, Dupuytren's contracture, rheumatic and similar lesions of the joints and various tissues.

Dosing regimen

When taken orally for replacement therapy in adults, the initial dose is 20-30 mg / day, the maintenance dose is 5-10 mg / day. If necessary, the initial dose can be 15-100 mg / day, maintenance - 5-15 mg / day. The daily dose should be reduced gradually. For children, the initial dose is 1-2 mg / kg / day in 4-6 doses, the maintenance dose is 300-600 mcg / kg / day.
With the / m administration, the dose, frequency and duration of use are determined individually. With intra-articular injection into large joints, a dose of 25-50 mg is used, for joints of medium size - 10-25 mg, for small joints - 5-10 mg. For infiltration administration into tissues, depending on the severity of the disease and the size of the affected area, doses from 5 to 50 mg are used.
Locally used in ophthalmology 3 times / day, the course of treatment is no more than 14 days; in dermatology - 1-3 times / day.

Side effect

From the endocrine system: Itsenko-Cushing's syndrome, weight gain. Hyperglycemia up to the development of steroid diabetes, depletion (up to atrophy) of the function of the adrenal cortex.
On the part of the digestive system: increased acidity of gastric juice, ulcerogenic effect on the gastrointestinal tract.
From the side of metabolism: increased excretion of potassium, sodium retention in the body with the formation of edema, negative nitrogen balance.
From the side of the cardiovascular system: arterial hypertension.
From the blood coagulation system: increased blood clotting.
From the musculoskeletal system: osteoporosis, aseptic necrosis of bones.
On the part of the organ of vision: steroid cataract, provoking latent glaucoma.
From the side of the central nervous system: mental disorders.
Effects due to immunosuppressive action: reduced resistance to infections, delayed wound healing.
When applied externally: steroid acne, purpura, telangiectasias may appear, as well as burning, itching, irritation, dry skin; with prolonged use and / or when applied to large surfaces of the skin, a resorptive effect may develop.
When applied topically: a slight burning sensation is possible.

Contraindications

Peptic ulcer of the stomach and duodenum, osteoporosis, Itsenko-Cushing's syndrome, tendency to thromboembolism, renal failure, severe arterial hypertension, systemic mycoses, viral infections, vaccination period, active form of tuberculosis, glaucoma, productive symptoms in mental illness. Hypersensitivity to prednisolone.
Infiltration introduction into the lesions of the skin and tissues with chicken pox, specific infections, mycoses, with a local reaction to vaccination.
In ophthalmology - viral and bacterial eye diseases, primary glaucoma, corneal diseases with damage to the epithelium. In dermatology - bacterial, viral, fungal skin lesions, tuberculosis, syphilis, skin tumors.

Pregnancy and lactation

During pregnancy (especially in the first trimester), they are used only for health reasons. If necessary, use during lactation should carefully weigh the expected benefits of treatment for the mother and the risk to the child.

special instructions

Not intended for intravenous administration. During the day, it is recommended to use taking into account the circadian rhythm of endogenous secretion of corticosteroids in the range from 6 to 8 in the morning.
Use with caution in patients with a history of psychosis; nonspecific infections with simultaneous chemotherapy or antibiotic therapy. In diabetes mellitus, the use is possible only with absolute indications or to prevent suspected insulin resistance. With latent forms of tuberculosis, prednisolone can only be used in combination with anti-tuberculosis drugs.
During treatment (especially long-term), it is necessary to observe an ophthalmologist, control blood pressure and water and electrolyte balance, as well as pictures of peripheral blood and blood sugar levels; in order to reduce side effects, you can prescribe anabolic steroids, antibiotics, as well as increase the intake of potassium in the body (diet, potassium supplements). It is recommended to clarify the need for the introduction of ACTH after a course of treatment with prednisolone (after a skin test!). In Addison's disease, simultaneous use with barbiturates should be avoided.
After discontinuation of treatment, withdrawal syndrome, adrenal insufficiency, as well as an exacerbation of the disease, for which prednisolone was prescribed, may occur.
Outwardly should not be used for more than 14 days. In the case of use in acne vulgaris or rosacea, an exacerbation of the disease is possible.

Prednisolone in the form of tablets, injection solution, dry substance for injection, eye drops, ointment is included in the Vital and Essential Drugs List.

drug interaction

With the simultaneous use of prednisolone with anticoagulants, it is possible to increase the anticoagulant effect of the latter; with salicylates - the likelihood of bleeding increases; with diuretics - aggravation of electrolyte disturbances is possible; with antidiabetic drugs - the rate of decrease in blood sugar decreases; with cardiac glycosides - the risk of developing glycoside intoxication increases; with rifampicin - a weakening of the therapeutic effect of rifampicin.

pharmachologic effect

Synthetic glucocorticosteroid (GCS), a dehydrated analog of hydrocortisone. It has anti-inflammatory, immunosuppressive and antiallergic effects.

Having easily penetrated into the target cells, it enters into contact with GCS receptors in the cytoplasm. Free receptors are usually associated with the so-called. heat shock protein (HSP90). After attaching to GCS receptors, the structure of HSP90 changes and it leaves the receptor. The latter moves to the nucleus of the cell. The multilateral action of steroids is due to the presence of the so-called. elements of the glucocorticoid response (CRE) in the promoter zones of several genes, some of which are "turned off" as a result of the attachment of receptors to their CRE, while others are in an active state. A key role in this complex process is played by the ubiquitous so-called. intracellular transcription factor Nf-kB. Various inflammatory mediators activate Nf-kB to trigger cytokine production. GCS also cause transcription of the IkB protein, which captures the activated Nf-kB and forms an inactive cytoplasmic complex with it. In addition, steroids activate lipocortins, which are representatives of another family of proteins, enhance the transcription of β 2 receptor genes. The essence of the action of lipocortins is to inhibit the chain of reactions leading to the formation of prostaglandins, leukotrienes and platelet activating factor. These mediators typically increase vascular permeability leading to tissue edema, leukocyte migration, and fibrin deposits.

Prednisolone has an effect on all stages inflammatory process, among which the inhibition of phospholipase A 2 and the blockade of the formation of arachidonic acid by stimulating the synthesis of an inhibitor polypeptide, the so-called. lipocortin-1 with subsequent suppression of the biosynthesis of inflammatory mediators, the so-called. pleiotropic cytokines of the reaction of the acute phase of inflammation: interleukin-1, TNF-α, as well as interleukins-4 and 5. In addition, it blocks the transcription of genes for such inflammatory enzymes as NO-synthetase and cyclooxygenase. Suppresses the functions of neutrophils and macrophages, incl. release of chemical mediators and their effects on capillaries. Prednisolone stabilizes cell and organelle membranes (especially liposomal ones) and increases their resistance to various damaging factors. By blocking inflammatory reactions in the connective tissue, it prevents the formation of scar tissue.

It suppresses the inflammatory process, regardless of its etiology, with an excessive or "useless" inflammatory reaction, it has a beneficial effect, but it is dangerous in infections due to the suppression of the protective inflammatory process.

The immunosuppressive effect is due to the action of prednisolone on numerous targets, among which the suppression of cytokine secretion is especially important. Prednisolone inhibits the proliferation of lymphocytes, incl. leukemia lymphocytes, expression of MHC II on macrophages and adhesive molecules of endothelial cells, causes eosinopenia and prevents degranulation of eosinophils and adhesion of neutrophils, prevents the release of cytokines (mainly interleukin-2 and γ-interferon) and secretion and release of prostaglandin E, and also blocks fibroblast collagen synthesis. Large doses of glucocorticosteroids suppress antibody production.

hinders development allergic reactions. Reduces the number of circulating eosinophils, basophils and the release of immediate allergy mediators. The interaction of allergens with antibodies remains unchanged, but there are no damaging effects of inflammation.

The drug affects various types of metabolism in the human body.

carbohydrate metabolism: prednisolone activates gluconeogenesis (increased absorption of carbohydrates from the gastrointestinal tract, increased activity of glucose-6-phosphatase and phosphoenol-pyruvate kinase with an increase in the flow of glucose from the liver into the blood), while peripheral glucose utilization (transport of glucose through the cell membrane) may decrease, leading to hyperglycemia and sometimes glycosuria. Latent diabetes manifests itself, this effect can be used as a test to identify the pre-diabetic stage of the disease.

Protein metabolism: anabolism decreases (a decrease in the amount of globulins, an increase in the synthesis of albumins in the liver and kidneys, an increase in the albumin / globulin ratio) with a constant or even increased intensity of catabolic processes, which leads to a negative nitrogen balance with atrophy of muscle tissue. Osteoporosis is possible due to a decrease in the protein matrix of bone tissue, growth retardation in children, skin atrophy, which, with increased capillary fragility, leads to increased skin vulnerability and the formation of striae. The healing of wounds and peptic ulcers slows down and occurs with the formation of fibrous tissue.

Fat metabolism: the synthesis of higher fatty acids and triglycerides is enhanced with the deposition of fat in the shoulder girdle, on the face and abdomen and its mobilization from the subcutaneous fatty tissue of the extremities, followed by hypercholesterolemia.

Water-electrolyte metabolism (mineralocorticoid effects): sodium retention in the renal tubules increases, potassium excretion increases along with urine. Prednisolone reduces hypercalcemia with excessive absorption of calcium from the gastrointestinal tract (sarcoidosis, vitamin D intoxication), increases urinary calcium excretion with possible formation of stones.

Suppresses feedback hypothalamic-pituitary-adrenocorticoid system with prolonged use (with subsequent slow recovery), which, with a sharp cessation of treatment, leads to the development of a state of adrenocorticoid insufficiency in the patient: it inhibits the synthesis and secretion of ACTH by the pituitary gland, thereby inhibiting the synthesis of endogenous glucocorticoid (and androgenic) hormones by the adrenal glands.

Pharmacokinetics

When taken orally, it is well absorbed from the gastrointestinal tract. Cmax in plasma is achieved within 1-2 hours. Bioavailability 82±13%. Communication with blood proteins reaches 90-95%, while most of prednisolone binds to transcortin (cortisol-binding globulin) and albumin.

Metabolism is carried out mainly in the liver and partly in the kidneys, small intestine, bronchi. The oxidized forms are glucuronidated or sulfated. Excreted by the kidneys 20% unchanged, the rest - in the form of free and conjugated metabolites. T 1/2 is 2-3 hours (2.2±0.5).

Prednisolone crosses the placental barrier and is excreted in small amounts in breast milk.

Indications

- rheumatic fever, rheumatic carditis, chorea minor;

- systemic connective tissue diseases (systemic lupus erythematosus, scleroderma, periarteritis nodosa, dermatomyositis);

- multiple sclerosis;

- acute and chronic inflammatory diseases of the joints (rheumatoid arthritis, juvenile arthritis, ankylosing spondylitis, gouty and psoriatic arthritis, polyarthritis, humeroscapular periarthritis, osteoarthritis (including post-traumatic), Still's syndrome in adults, bursitis, nonspecific tendosynovitis, synovitis, epicondylitis );

- bronchial asthma, status asthmaticus;

- interstitial lung diseases (acute alveolitis, pulmonary fibrosis, sarcoidosis stage II-III);

- lung cancer (in combination with cytostatics);

- berylliosis, aspiration pneumonia (in combination with specific therapy), Leffler's eosinophilic pneumonia;

- tuberculosis (pulmonary tuberculosis, tuberculous meningitis) - in combination with specific therapy;

- primary and secondary adrenal insufficiency (including conditions after removal of the adrenal glands);

- congenital adrenal hyperplasia;

- adrenogenital syndrome;

- subacute thyroiditis;

- acute and chronic allergic diseases (drug and food allergies, serum sickness, hay fever, atopic dermatitis, contact dermatitis involving a large body surface, urticaria, allergic rhinitis, Quincke's edema, Stevens-Johnson syndrome, toxicoderma);

- hepatitis;

- hypoglycemic conditions;

- autoimmune diseases (including acute glomerulonephritis);

- nephrotic syndrome;

- inflammatory diseases of the gastrointestinal tract (ulcerative colitis, Crohn's disease, local enteritis);

- diseases of the blood and hematopoietic organs (agranulocytosis, panmyelopathy, myeloma, acute lympho- and myeloid leukemia, lymphogranulomatosis, thrombocytopenic purpura, secondary thrombocytopenia in adults, autoimmune hemolytic anemia, erythroblastopenia, congenital erythroid hypoplastic anemia);

- autoimmune and other skin diseases (eczema, seborrheic dermatitis, psoriasis, Lyell's syndrome, bullous dermatitis herpetiformis, pemphigus, exfoliative dermatitis);

- cerebral edema postoperative, post-radiation, post-traumatic, with a brain tumor (used after parenteral glucocorticosteroids);

– eye diseases, incl. allergic and autoimmune (sympathetic ophthalmia, allergic forms of conjunctivitis, allergic corneal ulcers, non-purulent keratitis, iridocyclitis, iritis, severe sluggish anterior and posterior uveitis, choroiditis, optic nerve neuritis);

— prevention of graft rejection reactions;

- hypercalcemia against the background of oncological diseases;

- for the prevention and relief of nausea, vomiting during cytostatic therapy.

Dosing regimen

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

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

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

Side effect

The frequency of development and severity of side effects depend on the duration of treatment, the dose of the drug and taking into account the daily rhythm of GCS synthesis.

From the digestive system: increased acidity of gastric juice, nausea, vomiting, hiccups, flatulence, indigestion, decreased or increased appetite, steroid ulcers in the gastrointestinal tract, erosive esophagitis, perforation of the wall of the stomach or intestines, bleeding from ulcers, pancreatitis, hepatomegaly, in rare cases - increased activity hepatic transaminases and alkaline phosphatase.

From the side of the cardiovascular system: arterial hypertension, bradycardia, cardiac arrest, arrhythmia, ECG changes characteristic of hypokalemia, aggravation or development of heart failure (in patients predisposed to it), myocardial dystrophy, in acute and subacute myocardial infarction, the spread of necrosis, slowing down the formation of scar tissue and a tendency to myocardial rupture.

From the blood coagulation system: increased blood clotting, thrombosis, thromboembolism.

From the side of metabolism: negative nitrogen balance (catabolic effect), bulimia, weight gain.

From the side of water-electrolyte balance: increased excretion of potassium, hypokalemic syndrome (hypokalemia, myalgia, muscle spasm, unusual weakness), sodium and water retention in the body with the formation of peripheral edema, hypernatremia, increased excretion of calcium, hypocalcemia.

From the musculoskeletal system: decrease in muscle mass (atrophy), muscle weakness, steroid myopathy, osteoporosis, very rarely - compression fractures of the vertebrae, pathological fractures of tubular bones, aseptic necrosis of the head of the humerus and femur, rupture of muscle tendons, slowing down of growth and ossification processes in children (premature closure epiphyseal growth zones).

Dermatological reactions: ecchymosis, thinning of the skin, hyper- or hypopigmentation, flushing of the skin of the face, allergic dermatitis, steroid acne, petechiae, excessive sweating.

From the CNS: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, nervousness, anxiety, insomnia, convulsions, epilepsy, craniocerebral hypertension, dizziness, headache, cerebellar pseudotumor.

From the endocrine system: dysmenorrhea, amenorrhea, slowing of sexual development in children, hyperlipoproteinemia, hirsutism, Itsenko-Cushing's syndrome, adrenal insufficiency up to atrophy of the adrenal cortex, especially affecting during stress: with trauma, surgery, concomitant diseases, decreased glucose tolerance, manifestation of latent diabetes mellitus, hyperglycemia up to steroid diabetes, "withdrawal" syndrome, increased activity of the renin-angiotensin-aldosterone system.

From the organ of vision: development of secondary bacterial, viral and fungal eye diseases, posterior subcapsular steroid cataract, manifestation of latent glaucoma with possible damage to the optic nerve, trophic changes in the cornea, exophthalmos.

From the side of the immune system: increased fatigue, decreased resistance to infections, exacerbation of infections (which is facilitated by the simultaneous use of immunosuppressants and vaccines), delayed wound healing, generalized or local allergic skin rash, itching, steroid vasculitis, anaphylactic shock.

Contraindications for use

In the case of short-term use of the drug for health reasons, the only contraindication is hypersensitivity to the components of the drug.

With caution, the drug should be prescribed for the following diseases and conditions:

- peptic ulcer of the stomach and duodenum;

- acute or latent peptic ulcer;

- esophagitis;

- gastritis;

- diverticulitis;

- newly created intestinal anastomosis;

- non-specific ulcerative colitis with the threat of perforation or abscess formation;

- predisposition to thromboembolism;

- acute and subacute myocardial infarction;

- severe chronic heart failure;

- arterial hypertension;

- systemic mycoses;

- bacterial and fungal infections (actively occurring or recently transferred, including contact with the patient);

- active and latent forms of tuberculosis;

- pervaccinal period (8 weeks before vaccination and within 2 weeks after it);

- lymphadenitis after BCG vaccination;

- immunodeficiency states (including infection with HIV and AIDS);

- diabetes mellitus (including reduced glucose tolerance);

- Itsenko-Cushing's disease;

- hypothyroidism;

- hyperthyroidism;

- mental disorders (for example, acute psychosis);

- poliomyelitis (with the exception of bulbar encephalitis);

- severe myasthenia gravis;

- obesity stage III-IV;

- severe chronic renal and / or liver failure;

- nephrolithiasis;

- hypoalbuminemia and conditions predisposing to its occurrence;

- glaucoma;

- systemic osteoporosis.

Use during pregnancy and lactation

It has an adverse effect on pregnancy in animals.

During pregnancy (especially in the first trimester), prednisolone is used only for health reasons. In cases where the use of corticosteroids is indispensable, women with a normal pregnancy can receive treatment similar to that prescribed for non-pregnant women. Long-term therapy with prednisolone during pregnancy may be associated with a small risk of developing gothic palate and intrauterine growth retardation. Taking the drug in the third trimester of pregnancy can lead to atrophy of the adrenal cortex of the fetus, which leads to the need for replacement therapy in the newborn.

During breastfeeding, glucocorticosteroids are taken with caution, as they pass into breast milk in small amounts. In order to detect signs of possible adrenal suppression, the condition of children whose mothers take pharmacological doses of steroids should be carefully monitored.

Use in children

Children with bronchial asthma are contraindicated in the use of prednisolone simultaneously with sympathomimetic aerosols.

Overdose

Symptoms: increased side effects.

drug interaction

Children with bronchial asthma are contraindicated in the use of Prednisolone simultaneously with sympathomimetic aerosols.

With the simultaneous appointment of Prednisolone and indirect anticoagulants, the anticoagulant effect of the latter may be weakened, less often - increased. Dose adjustment required.

The combination of Prednisolone with anticoagulants and thrombolytics increases the risk of developing ulcerative bleeding from the gastrointestinal tract.

Simultaneous use of Prednisolone with salicylates increases the likelihood of gastrointestinal bleeding.

Simultaneous administration with acetylsalicylic acid is accompanied by an acceleration of excretion and a decrease in its concentration in the blood, and with the abolition of Prednisolone, an increase in the content of salicylates in the blood with the likelihood of side effects.

The combination of Prednisolone with diuretics, especially thiazide derivatives and carbonic anhydrase inhibitors, amphotericin B can aggravate electrolyte disturbances, incl. increase potassium excretion (when administered with amphotericin B, the risk of heart failure may also increase).

The combination of Prednisolone with sodium-containing drugs leads to edema and increased blood pressure.

The simultaneous use of Prednisolone with antihypertensive drugs, antidiabetic drugs and insulin reduces their effectiveness, with cardiac glycosides - increases the risk of developing glycoside intoxication with the development of ventricular extrasystole as a result of hypokalemia.

Hormonal contraceptives enhance the action of Prednisolone.

The simultaneous use of Prednisolone and ethanol or NSAIDs increases the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract (dose reduction may be required).

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

Simultaneous use with hormonal contraceptives is accompanied by an increase in the action of Prednisolone due to a decrease in the clearance of the latter.

The risk of developing cataracts increases with the simultaneous use of Prednisolone with antipsychotics, carbutamide and azathioprine.

Simultaneous use with inducers of microsomal liver enzymes (phenytoin and barbiturates, ephedrine, rifampicin, theophylline) leads to a decrease in the concentration and weakening of the effect of Prednisolone.

Simultaneous use of Prednisolone with M-anticholinergics, incl. antihistamines, tricyclic antidepressants and nitrates contributes to an increase in intraocular pressure.

Taking Prednisolone with a pasiqualator leads to a decrease in the concentration of the latter.

Simultaneous administration with paracetamol increases the hepatotoxic effect as a result of the induction of hepatic enzymes and the formation of a toxic metabolite of paracetamol.

Simultaneous intake with vitamin D reduces the effect of the latter on calcium absorption in the intestine.

When taken simultaneously with somatotropic hormone, the effectiveness of the latter is reduced.

Metabolism increases and the concentration of isoniazid and mexelitin in the blood decreases while taking them with Prednisolone, especially in slow acetylators.

Carbonic anhydrase inhibitors and loop diuretics, when co-administered with prednisolone, may contribute to the development of osteoporosis.

Indomethacin displaces prednisone from its association with albumin and promotes the development of osteoporosis.

Ergocalciferol and parathyroid hormone prevent the development of prednisolone osteopathy.

ACTH enhances the action of Prednisolone.

Cyclosporine and ketoconazole, slowing down the metabolism of Prednisolone, in some cases increase its toxicity.

When taken simultaneously with mitotane and other inhibitors of adrenal cortex function, an increase in the dose of Prednisolone may be required.

Simultaneous use with live antiviral vaccines and other types of immunization contributes to the activation of viruses with the development of infectious diseases.

Antacids reduce the absorption of prednisolone.

Antithyroid drugs reduce and thyroid hormones increase the clearance of prednisolone.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

Storage conditions

List B.

Store at a temperature of 15 to 30 ° C, protected from light and out of the reach of children.

Best before date:

Do not use after the expiry date stated on the packaging.

Application for violations of liver function

Use with caution in severe liver failure.

The drug has a more pronounced effect in the case of cirrhosis of the liver.

Application for violations of kidney function

Use with caution in severe renal failure.

Use in elderly patients

There are no data on the use of the drug in elderly patients.

special instructions

Before starting treatment, the patient should be carefully examined to identify possible contraindications. In the future, during treatment, especially long-term, it is necessary to periodically repeat the examination with a study of the state of the cardiovascular system and water-electrolyte metabolism, x-ray examination of the lungs, examination of the stomach and duodenum, urinary system, as well as pictures of peripheral blood and blood sugar levels and urine, the organ of vision.

Treatment of children with glucocorticosteroids during the period of growth is possible only according to absolute indications and with careful supervision of the attending physician.

Children receiving prednisolone therapy and who have been in contact with patients with measles or chickenpox are prescribed specific immunoglobulins prophylactically.

During treatment with Prednisolone, immunizations should be avoided.

With indications of a history of psychosis, high doses of Prednisolone should be prescribed under the indispensable strict medical supervision.

In diabetes mellitus, Prednisolone is prescribed only according to absolute indications. In order to reduce side effects, you can prescribe anabolic steroids, increase the intake of potassium in the body (diet, potassium supplements).

In severe infectious diseases, the use of Prednisolone is permissible only against the background of the use of specific therapy.

In the case of intercurrent infections, septic conditions and tuberculosis, simultaneous chemotherapy or antibiotic therapy is necessary.

The drug has a more pronounced effect in the case of hypothyroidism and cirrhosis of the liver.

In Addison's disease, the simultaneous use of prednisolone and barbiturates should be avoided, since this combination can provoke acute adrenal insufficiency (addisonian crisis).

With a sharp cessation of treatment with Prednisolone, especially after the use of high doses of the drug, it is possible to develop a withdrawal syndrome or exacerbate the underlying disease, for the treatment of which Prednisolone was used. To avoid the development of a withdrawal syndrome (loss of appetite, nausea, lethargy, generalized musculoskeletal pain, general weakness), the drug is withdrawn for several days, gradually reducing the dose.

After discontinuation of the drug, a state of relative insufficiency of the adrenal cortex persists for several months, so monitoring of the patient should be continued. In the event of stressful situations during the period of withdrawal of prednisolone, glucocorticoid drugs are prescribed temporarily and according to indications, if necessary, in combination with mineralocorticosteroids.

Due to the mild mineralocorticoid effect in adrenal insufficiency, prednisolone is used in combination with mineralocorticoids.

With latent infections of the kidneys and urinary tract, Prednisolone provokes leukocyturia, which may be of diagnostic value.

Prednisolone increases the content of 11- and 17-hydroxyketocorticosteroid metabolites.

Injections Prednisolone is a drug that makes up a group of glucocorticosteroid hormones. It is permissible to use it only after consulting with your doctor, as injections have a large number of contraindications and side effects. Most often, they are prescribed in cases where the use of non-steroidal anti-inflammatory drugs is not acceptable or has not shown proper effectiveness.

Mechanism of action

Prednisolone is an injection solution that has powerful anti-inflammatory, anti-shock, analgesic and immunosuppressive effects. Once in the body, the drug forms a glucocorticoid receptor. It rapidly penetrates the cell nucleus, where it interacts with genes. Because of this, there are serious changes in the production of proteins and RNA. Prednisolone is valued for its high anti-inflammatory effect, which is due to the following factors:

  • The active ingredients increase the production of lipocortin, which prevents the further production of phospholipase. Because of this, damaged tissues can no longer produce arachidonic acid. All this leads to the impossibility of the synthesis of prostaglandins.
  • The active substances interfere with the exchange of COX-2 genes, which also reduces the production of prostaglandins.
  • Prednisolone stops the metabolic processes between molecules in the blood vessels, so that neutrophils and monocytes do not penetrate into the focus of inflammation.

Prednisolone is a drug with powerful anti-inflammatory, analgesic and immunosuppressive effects.

Indications for use

Prednisolone is a powerful medicine that should only be used after consulting a doctor. Usually experts prescribe it:

  • With postoperative, traumatic, toxic and burn shocks.
  • In acute and severe forms of allergies.
  • With anaphylactic or blood transfusion shock.
  • With swelling of the brain caused by radiation therapy, head trauma or tumor.
  • With a severe form of bronchial asthma.
  • With serious skin lesions: psoriasis, dermatitis, bullous dermatitis, seborrhea, Stevens-Jones syndrome.
  • With allergic conjunctivitis.
  • With serious disorders and congenital anomalies of the adrenal glands.
  • With severe uveitis, optic neuritis.
  • With hepatic coma.
  • With thyrotoxic crisis.
  • With acute hepatitis.
  • With serious diseases of the blood and circulatory system.
  • With Leffler's syndrome, berylliosis.
  • With multiple sclerosis.
  • With hypercalcemia caused by malignant neoplasms.
  • As a preventive measure to reject a transplanted organ.
  • To reduce inflammation.
  • For the prevention of cicatricial narrowing.

Mode of application

Instructions for the use of Prednisolone injections states that it is permissible to use the medicine only after consultation with a qualified attending physician. This medicine has a high impact on the body, therefore, due to improperly selected therapy, there is a high risk of side effects. Prednisolone in the form of injections must be administered inside the muscles, joints, or in the form of impregnation of tissues. It is very important to treat the skin with alcohol before the procedure in order to kill all pathogenic microorganisms.

To stop the soreness of the joints, it is necessary to inject 25-50 mg into large ones, 10 mg into small ones. With a pronounced syndrome, the procedure can be repeated several times. It is very important to evaluate the therapeutic effect after such therapy in order to either increase the dose of the active substance, or change the medicine, if necessary. In order for the drug to be properly distributed over the joint, after administration it must be repeatedly bent and unbent. Lotions from the solution will also help reduce pain - they treat small areas of the affected surfaces.

To cope with various types of conjunctivitis, injections or instillation of the drug into the eyes will help. This should be done 1-3 drops three times a day for 2 weeks. In order for the therapy not to bring any complications or side effects, it is necessary to regularly measure the level of blood pressure and administer anabolic drugs. Also, the doctor should send you once every two weeks for a blood, feces and urine test. At the time of therapy, it is necessary to monitor the water balance in the body, if necessary, take diuretics.

It should be borne in mind that with prolonged use, Prednisolone can cause a decrease in the level of potassium in the blood. To prevent this, it is recommended to follow a special diet and take this macronutrient in the form of tablets. Otherwise, there is a high risk of osteoporosis - damage to bone tissue, due to which it becomes extremely fragile.

Therapeutic dosage

Keep in mind that only the attending physician can prescribe a therapeutic dose of Prednisolone, as well as the duration of its use. He must familiarize himself with the results of diagnostic studies, and only after that prescribe treatment. Injections can be injected into the body by drip or jet, however, in practice, two of these methods are used in one procedure at once.

DiseaseDosageDuration
Acute adrenal insufficiency100-200 mg
3 days to 2 weeks
Bronchial asthma75-675 mg
3 days to 2 weeks
asthmatic crisis150-1200 mg
Once
Thyrotoxic crisis200-300 mgWeek 1
Toxin poisoning75-400 mg1-2 weeks
Burns of the respiratory tract and gastrointestinal tract120-350 mgWeek 1
All kinds of shocks300-1200 mgWeek 1
Acute kidney and liver failure300-1500 mgWeek 1
Rheumatoid arthritis75-100 mgWeek 1
Acute hepatitis75-100 mg10 days

In cases where it is not possible to inject Prednisolone into the bloodstream, it is permissible to administer it intramuscularly. To stop acute conditions, doctors prescribe the tablet form of this medication. To avoid the withdrawal syndrome, the end of treatment is accompanied by a decrease in the therapeutic dose. It is strictly forbidden to abruptly stop the use of this medication - the risk of serious complications is high.

Despite the generally accepted dosages, only the attending physician should prescribe treatment with Prednisolone based on advanced diagnostic data.

withdrawal syndrome

With prolonged use of the solution for injection of Prednisolone, the body begins to get used to the components. In addition, the drug affects and changes the functioning of the adrenal glands. With a sharp refusal of therapy with this drug, a person may experience malaise, fatigue, high body temperature. Such conditions disappear without additional therapy in a few days. However, if high doses of Prednisolone were abruptly discontinued, there is a risk of a hypoadrenaline crisis. You can recognize it by increasing convulsions, vomiting and collapse. If medical assistance is not provided to a person in a timely manner, cardiac arrest is possible due to acute cardiovascular insufficiency.

Contraindications

To reduce the risk of complications due to taking Prednisolone, you must always remember about the presence of contraindications. Even in emergency cases, it is forbidden to administer this injection if there is an increased sensitivity to the components of the drug. It should also be borne in mind that lactose is present in the composition of the drug, to which some people have persistent intolerance. With extreme caution, treatment with Prednisolone is permissible in the following cases:

Prednisolone is a drug that has a large number of side effects. To prevent their occurrence, it is necessary to strictly adhere to all the recommendations of the attending physician. The most dangerous are the following:

  • Decreased glucose tolerance is especially dangerous for people with diabetes. Substances entering the body slow down the work of the liver, which disrupts the production of insulin.
  • Inhibition of adrenal function - this leads to hormonal imbalance. It also slows down the removal of toxins from the body.
  • Itsenko-Cushing's syndrome is a condition that occurs with a powerful change in hormonal levels.
  • The appearance of nausea, vomiting, pain in the abdomen.
  • The formation of bleeding inside the gastrointestinal tract: erosive gastritis, perforation of the intestinal walls, ulcers.
  • Violation of digestion in the form of changes in appetite, constipation and diarrhea, flatulence.
  • Exacerbation of cardiovascular pathologies.
  • The appearance of prolonged hiccups.
  • Changes in the nervous system: TIR, depression, euphoria, paranoia, disorientation.
  • Frequent seizures, especially at night.
  • Headaches and dizziness.
  • Significant increase in pressure inside the eyes.
  • Increased intraocular pressure, trophic changes in the structure of the cornea.
  • Hyperhidrosis, the appearance of a specific body odor.
  • Weight loss, muscle atrophy.
  • Prolonged wound healing.
  • The formation of acne and striae on the body.
  • Local allergic reactions.