Gks - glucocorticosteroids: use of drugs in medicine

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Content

  • 1Gks - what is this in medicine? effects and effects of glucocorticosteroid preparations
    • 1.1General information on GCS. What is this in medicine?
    • 1.2Mechanism of action of GCS
    • 1.3Main effects of GCS
    • 1.4Pharmacokinetics
  • 2Preparations of glucocorticosteroids - indications, contraindications
    • 2.1Effect of glucocorticosteroids on the body
    • 2.2The main effects of glucocorticosteroids
    • 2.3Treatment with glucocorticosteroids
    • 2.4Contraindications to glucocorticosteroids
  • 3Glucocorticosteroids
  • 4Glucocorticosteroid - instructions for use, analogues, price, reviews
    • 4.1Preparations that include
    • 4.2Indications for use
    • 4.3Contraindications
    • 4.4Instructions for use Glucocorticosteroid (method and dosage)
    • 4.5Substitution therapy GCS
    • 4.6Suppressive therapy GCS
    • 4.7Pharmacodynamic therapy
    • 4.8Side effects
    • 4.9Overdose
    • 4.10Analogues
    • 4.11pharmachologic effect
    • 4.12special instructions
    • 4.13At pregnancy and thoracal feeding
    • 4.14In childhood
    • 4.15In old age
    • 4.16Drug Interactions
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    • 4.17Conditions of leave from pharmacies
    • 4.18Terms and conditions of storage
    • 4.19Price in pharmacies

Gks - what is this in medicine? effects and effects of glucocorticosteroid preparations

Surely you have ever heard of steroid hormones. Our body continuously develops them for regulating vital processes.

In this article we will consider glucocorticoids - steroid hormones, which are formed in the adrenal cortex. Although most of all we are interested in their synthetic analogues - GCS.

What is this in medicine? What are they used for and what harm do they do? Let's see.

General information on GCS. What is this in medicine?

Our body synthesizes such steroid hormones as glucocorticoids. They are produced by the adrenal cortex, and their use is mainly associated with the treatment of adrenal insufficiency.

Nowadays, not only natural glucocorticoids, but also their synthetic analogues - GCS, are used.

What is this in medicine? For mankind, these analogues have a lot to do, since they exert anti-inflammatory, immunosuppressive, anti-shock, anti-allergic action on the body.

Glucocorticoids began to be used as medicines (further in the article - drugs) in the 40s of the XX century.

By the end of the 30s of the XX century, scientists discovered steroid hormonal compounds in the adrenal cortex of a person, and already in 1937 a mineralocorticoid deoxycorticosterone was isolated. In the early 40-ies, glucocorticoids hydrocortisone and cortisone were also excreted.

The pharmacological effects of cortisone and hydrocortisone were so diverse that it was decided to use them as a drug. After a while, scientists made their synthesis.

The most active glucocorticoid in the human body - cortisol (analog - hydrocortisone, the price of which is 100-150 rubles), it is considered the main one. It is also possible to identify less active: corticosterone, cortisone, 11-deoxycortisol, 11-dehydrocorticosterone.

Of all the natural glucocorticoids, only hydrocortisone and cortisone have been used as a drug.

However, the latter causes side effects more often than any other hormone, because of which currently its use in medicine is limited.

For today from glucocorticoids only hydrocortisone or its ethers (hydrocortisone hemisuccinate and hydrocortisone acetate) is used.

As for glucocorticosteroids (synthetic glucocorticoids), a number of such agents have been synthesized in our time, among which we can distinguish fluorinated (flumethasone, triamcinolone, betamethasone, dexamethasone, etc.) and non-fluorinated (methylprednisolone, prednisolone, prednisone) glucocorticoids.

Such funds are more active than their natural counterparts, and smaller doses are required for treatment.

Mechanism of action of GCS

The effect of glucocorticosteroids at the molecular level has not been clarified to the end. Scientists believe that these drugs act on cells at the level of regulation of gene transcription.

Glucocorticosteroids interact with glucocorticoid intracellular receptors, which are present in virtually every cell of the human body.

In the absence of this hormone, the receptors (they are cytosolic proteins) are simply inactive.

In the inactive state, they are part of heterocomplexes, which also include immunophilin, heat shock proteins, and so on.

When glucocorticosteroids penetrate inside the cell (through the membrane), they bind to the receptors and activate the "glucocorticoid + receptor" complex, after which it penetrates into the nucleus of the cell and interacts with regions of DNA that are located in the promoter fragment of the steroid-responsive gene (they are also called glucocorticoid-responsive elements).

The complex "glucocorticoid + receptor" is able to regulate (suppress or, conversely, activate) the process of transcription of some genes. This is what leads to suppression or stimulation of mRNA formation, as well as to the modification of the synthesis of various regulatory enzymes and proteins that mediate cellular effects.

Various studies show that the "glucocorticoid + receptor" complex interacts with different transcription factors, for example, such as the nuclear factor kappa B (NF-kB) or transcriptional activator protein (AP-1), which regulate genes involved in the immune response and inflammation (adhesion molecules, cytokine, proteinase and etc.).

Main effects of GCS

Effects of glucocorticosteroids on the human body are numerous. These hormones have antitoxic, anti-shock, immunodepressive, anti-allergic, desensitizing and anti-inflammatory actions. Let's take a closer look at how the GCS works.

  • Anti-inflammatory effect of SCS. Due to the suppression of the activity of phospholipase A2. When this enzyme is suppressed in the human body, suppression of the liberation (liberation) of the arachidonic acid and inhibition of the formation of certain inflammatory mediators (such as prostaglandins, leukotrienes, troboxane and etc.). Moreover, the intake of glucocorticosteroids leads to a decrease in fluid exudation, vasoconstriction (narrowing) of the capillaries, and improvement of microcirculation in the inflammatory focus.
  • Antiallergic effect of GCS. It occurs as a result of a decrease in the secretion and synthesis of mediators of allergy, a decrease in circulating basophils, inhibition of the release of histamine from basophils and sensitized mast cells, reducing the number of B- and T-lymphocytes, reducing the sensitivity of cells to mediators of allergies, changes in the immune response of the body, as well as inhibition antibody formation.
  • Immunosuppressive activity of SCS. What is this in medicine? This means that drugs inhibit immunogenesis, suppress the production of antibodies. Glucocorticosteroids inhibit the migration of bone marrow stem cells, inhibit the activity of B- and T-lymphocytes, inhibit the release of cytokines from macrophages and leukocytes.
  • Antitoxic and anti-shock effects of SCS. This effect of hormones is due to increased blood pressure in humans, as well as activation of liver enzymes that participate in the metabolism of xeno- and endobiotics.
  • Mineralocorticoid activity. Glucocorticosteroids have the ability to retard sodium and water in the human body, stimulate the excretion of potassium. In this synthetic substitutes are not as good as natural hormones, but they still have such an effect on the body.

Pharmacokinetics

By the duration of action, systemic glucocorticosteroids can be divided into:

  1. Glucocorticosteroids with a short action (for example, hydrocortisone, the price of which varies from 100 to 150 rubles).
  2. Glucocorticosteroids with an average duration of action (prednisolone (reviews of which are not very good), methylprednisolone).
  3. Glucocorticosteroids with prolonged action (triamcinolone acetonide, dexamethasone, betamethasone).

But not only the duration of the action can determine glucocorticosteroids. Their classification can also be according to the mode of administration:

  • oral;
  • intranasal;
  • inhaled glucocorticosteroids.

This classification, however, applies only to systemic glucocorticosteroids.

Also there are some preparations in the form of ointments and creams (local SCS). For example, "Afloderm". Reviews about such drugs are good.

Let's look at the types of system GCSs separately.

Oral glucocorticosteroids are perfectly absorbed into the digestive tract without causing problems. Actively bind to proteins in the plasma (transcortin, albumin).

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The maximum concentration of oral glucocorticosteroids in the blood is reached after one hour after administration.

They undergo biotransformation in the liver, kidneys (partially) and in other tissues by conjugation with sulfate or glucuronide.

Approximately 70% of conjugated GCS is excreted in the urine, another 20% will be excreted later with feces, and the remainder - with other biological fluids (for example, afterwards). Half-life is from 2 to 4 hours.

A source: http://.ru/article/168116/gkschto-eto-v-meditsine-deystvie-i-effektyi-preparatov-glyukokortikosteroidov

Preparations of glucocorticosteroids - indications, contraindications

Glucocorticosteroid is a substance of natural or synthetic origin from the subclass of hormones of the adrenal cortex.

Effect of glucocorticosteroids on the body

In their chemical nature, these substances are steroids. In the human body and animals, the main place of their formation is the adrenal cortex.

Glucocorticosteroids generally increase the body's resistance to stress, this is the biological significance of these hormonal substances.

Glucocorticosteroids have an effect on the metabolism in the body, mainly on carbohydrate, mineral, protein and water.

Artificially created drugs glucocorticosteroids act as anti-inflammatory, desensitizing, immunosuppressive, antitoxic and anti-shock drugs.

The main effects of glucocorticosteroids

The effect of glucocorticosteroids is realized, penetrating diffusely through the cell membranes into the cytoplasm.

There they bind to special intracellular receptors, through which they affect protein synthesis.

It is also known about the inhibitory effect of these hormones on phospholipase A2 and hyaluronidase, which are inflammatory enzymes.

Substances of this group stabilize cell membranes, due to which inhibit the release of biologically active substances (histamine, leukotrienes, thromboxane) from mast cells. They slow down the formation of pro-inflammatory cytokines from arachidonic acid.

The immunosuppressive effect of glucocorticosteroid hormones is used in medicine to suppress the excessive aggression of the immune system directed at one's own organism.

This is required for organ transplants (for example, kidneys, bone marrow), with malignant tumors, autoimmune diseases.

The positive effect of treatment with glucocorticosteroids is achieved by suppressing the migration of stem cells and lymphocytes, as well as the interaction of different groups of lymphocytes with each other.

The ability of glucocorticosteroids to increase blood pressure is realized by increasing the release of adrenaline and restoration of sensitivity to adrenaline receptors, narrowing of the lumen of blood vessels and reducing their permeability. This is their property allows you to deal with shock states in critical situations.

Glucocorticosteroids increase the formation of glucose in the liver and the breakdown of proteins, thereby increasing the content of free amino acids and glucose in the blood. In this case, the body receives a sufficient amount of high-energy substances.

Treatment with glucocorticosteroids

In medicine, preparations of glucocorticosteroids are divided into 3 groups according to the duration of the action: short, medium duration and long-term action.

Short-acting glucocorticosteroids include hydrocortisone. This is an analog of its own hydrocortisone organism, in comparison with other drugs, it has a minimal effect on water-salt metabolism.

Preparations of glucocorticosteroids of medium duration - methylprednisolone and prednisolone.

Long-acting glucocorticosteroids include betamethasone and dexamethasone.

In the treatment of glucocorticosteroids use forms of drugs for oral administration, inhalation, intranasal and parenteral.

Preparations for oral intake are well absorbed from the digestive tract, in the blood they bind to plasma proteins.

They are used to treat congenital dysfunction of the adrenal cortex, primary and secondary adrenal insufficiency, subacute thyroiditis, Crohn's disease, interstitial lung diseases and COPD in stage exacerbation.

Of inhaled glucocorticosteroids most commonly used are budesonide, triamcinolone acetonide, beclomethasone dipropionate, mometasone furoate, fluticasone propionate. They are well suited for the basic treatment of bronchial asthma and COPD, allergic rhinitis.

Intranasal glucocorticosteroids are prescribed for polyposis of the nose, allergic and idiopathic rhinitis. The peculiarity of their introduction suggests that part of the drug will fall on the nasal mucosa and the respiratory tract, and part will be swallowed and enter the digestive tract.

Contraindications to glucocorticosteroids

They are used with caution in case of Izenko-Cushing's disease, diabetes mellitus, thromboembolism, ulcerative disease, high blood pressure, severe renal failure, herpes and systemic mycosis.

Also contraindications to glucocorticosteroids will be active forms of syphilis and tuberculosis, pustular processes on the skin, viral eyes, corneal lesions with epithelial defects, glaucoma, the period of the breast feeding.

Intranasal glucocorticosteroids can not be administered with repeated nasal bleeding, hemorrhagic diathesis, individual intolerance.

During treatment with glucocorticosteroids, measles and chicken pox are harder to treat.

A source: http://www.neboleem.net/gljukokortikosteroidy.php

Glucocorticosteroids

Currently, the GCS includes both the natural hormones of the adrenal cortex and their synthetic analogues:• with predominantly glucocorticoid function - cortisone and hydrocortisone (cortisol) • their synthesized analogues - prednisone, prednisolone, methylprednisolone and others. • including halogenated (fluorinated) derivatives - triamcinolone, dexamethasone, betamethasone, etc.

A wide range of physiological and pharmacological effects of glucocorticoids:

• adaptogenic • anti-inflammatory • analgesic • antipyretic • nonspecific membrane-stabilizing • anti-edematous • antiallergic • immunosuppressive • hematological • hemodynamic • anti-shock • antitoxic • antiemetic and other

makes these drugs almost universal medicines, and today it is difficult to find such a pathological condition, in which they would not be shown at this or that stage of development.

Among the indications in the first place can be identified so-called rheumatic diseases, kidney disease, blood, allergic diseases, transplants, urgent states.

Depending on the purpose, there are three variants of SCS therapy; while any of them can be either urgent or planned.

Because of the abundance of side effects, GCS therapy is mainly aimed at achieving maximum effect in prescribing minimal doses, the magnitude of which is determined by the disease and does not depend on body weight and age; the dose is adjusted in accordance with the individual reaction.

Two principally different schemes for assigning GCSs were adopted:

• starting with the lowest possible dose, increase it with insufficient effect until optimal; at There is a danger of increasing the duration of treatment, loss of efficacy and development of actions;
• starting from the maximum daily doses, they are reduced after obtaining a clinical effect; at the same time, an early effect is achieved, the duration of treatment and the total dose of GCS are reduced.

Depending on the daily dose (in terms of prednisolone) and the duration of application of GCS, it is customary to allocate several types of therapy with different indications:

• in situations that directly threaten life, intensive therapy is administered with ultra-high (up to 500-4000 mg intravenously) or medium / high (25-150 mg oral) doses (the oral dose of prednisolone is equivalent to about 1/6 of intravenous) - this therapy can be carried out for several days and does not require a gradual cancellation;

• with severe exacerbations or with chronic course of severe diseases (leukemia, some collagenoses, hemolytic anemia, thrombocytopenia) is performed limited therapy, limited to weeks when administered in high doses (80-200 mg) and weeks or months in the case of medium doses (25-60 mg);

the maximum doses prescribed at the beginning, as the condition improves, decrease step-by-step with the subsequent transition to supportive ones; • for several chronic diseases (bronchial asthma, rheumatoid arthritis), long-term therapy with low doses (up to 10 mg), but doses less than 5 mg most likely are only substitutive and give a clinical effect only with atrophy of the adrenal cortex induced by prolonged glucocorticoid therapy.

With all daily schemes, the GCS should be administered in the early morning hours (between 6 and 8 hours); if One-time administration is not possible due to the dose, 2/3 of the dose is given at 8 hours and 1/3 by the day (about midday).In any dosing regimen, upon reaching the planned effect, the dose gradually decreases to a supporting dose or the drug is canceled altogether.

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The ratio of therapeutic and side effects allows us to state that currently the drug of choice for long-term and lifelong therapy is methylprednisolone.

Currently, methylprednisolone is widely used in the treatment of autoimmune diseases, in transplantology and intensive care.

The variety of forms of release allows to use the drug in all age categories in optimal dosages.

The second most effective drug remains in most cases prednisolone.

In many urgent situations, fluorinated compounds have certain advantages: dexamethasone (dexazone, dexona) and betamethasone (celeston, diprospan).

However, in the case of emergency therapy, in which the anti-inflammatory effect does not play a leading role, a comparative evaluation of the efficacy and safety of various drugs is very difficult at least for two reasons: • the effectiveness and safety of different drugs can be related only on the basis of their equivalent doses.

Meanwhile, if for various side effects of individual GCS there are characteristics of relative activity, of all therapeutic effects only Anti-inflammatory, according to which the equivalent dose is calculated; • the ratio of doses for oral and parenteral use of specific there is no unambiguous data even when it comes to the anti-inflammatory effect, not to mention other therapeutic or side effects.

In connection with the above difficulties, a conditional equivalent unit (EEA) was proposed, for which the minimum effective doses are taken. It is shown that maximum daily effective doses of fluorinated GCS (dexamethasone and betamethasone) expressed in EEE are five times less than that of non-halogenated drugs.

This provides not only a higher effectiveness and safety of this group of drugs prescribed in certain situations, but also their pharmacoeconomic benefits.

Methods for controlling undesirable reactions with the use of GCS

1. Observing the dynamics of body weight.

2. Control of blood pressure.

3. Investigation of blood sugar and urine.

4. Controlling the electrolyte composition of the plasma.

To prevent hypokalemia, the risk of which increases with the concomitant use of diuretics, prescribe potassium preparations.

5. Control over the state of the gastrointestinal tract. In patients with dyspeptic symptoms, antacids are prescribed to prevent ulceration, but their protective effect is not firmly established.

6. Control over the condition of the musculoskeletal system. Long-term use of glucocorticoids in a dose of g., 5 mg / day according to prednisolone leads to the development of osteoporosis of long tubular bones. The most pronounced changes are noted in the first 6 months, and the administration of the drugs every other day (alternating scheme) does not weaken the bone lesions.

For prevention and treatment, calcium, vitamin D, thiazide diuretics with a simultaneous limitation of sodium intake, bisphosphonates, sex hormones are recommended. Particular caution should be exercised in relation to the most dangerous complication - aseptic necrosis of bones. It is necessary to warn patients about the possibility of its development. At occurrence of any "new" pains, especially in humeral, hip and knee joints, it is necessary to exclude aseptic necrosis of bone. 7.Ophthalmological examination. Measurement of intraocular pressure and examination with a slit lamp to detect cataracts. 8. Control over the development of infectious complications.

SECONDARY ADRENAL METAL INSUFFICIENCY

The most severe complications of glucocorticoid therapy, potentially life-threatening, include secondary adrenal insufficiency, which is consequence of oppression of the hypothalamic-pituitary-adrenal system with long-term use of glucocorticoids, especially if the principles of their prolonged use destination.

Clinic of the syndrome of "cancellation" of glucocorticoids

The severity of the "cancellation" syndrome depends on the degree of preservation of the function of the adrenal cortex.

In mild cases, patients after the abolition of glucocorticoids have weakness, malaise, fast fatigue, loss of appetite, muscle pain, exacerbation of the underlying disease, increased temperature.

In severe cases, especially with large stresses, a classic Addisonian crisis can develop, accompanied by vomiting, collapse, convulsions.

Without the introduction of glucocorticoids, patients quickly die of acute cardiovascular insufficiency.

Prevention of secondary adrenal insufficiency

1. With the exception of urgent conditions and special indications, use glucocorticoids in accordance with the circadian rhythm.

2. Maximally use alternating therapy.

3. In the course of treatment for more than 10 days, the elimination of glucocorticoids should be performed with a gradual decrease in their dose. The cancellation mode depends on the duration of glucocorticoid intake.

At a course of several weeks to several months, a reduction in the dose of -5 mg of prednisolone (or an equivalent amount of another drug) every 3-5 days is permissible.

With more prolonged use, it is necessary to lower the dose more slowly, by, mg every 1-3 weeks. Particular care should be taken when the daily dose is less than 10 mg (prednisolone).

4. After the abolition of glucocorticoids, which were used for 2 weeks or more, for a period of -2 years to monitor the patient's condition under stressful situations. If necessary, carry out protective therapy with glucocorticoids.

Contraindications for the appointment of glucocorticoids are only relative and should be taken into account when planning long-term therapy. In urgent situations, glucocorticoids are administered without taking into account contraindications.

Relative contraindications for the appointment of glcocorticoids:

  1. • Diabetes mellitus (especially dangerous fluorinated glucocorticoids)
  2. • Mental diseases, epilepsy • Peptic ulcer of stomach and duodenum
  3. • Severe osteoporosis
  4. • Severe arterial hypertension
  5. • Severe heart failure

A source: http://doctorspb.ru/articles.ph? rticle_id = 592

Glucocorticosteroid - instructions for use, analogues, price, reviews

Glucocorticosteroid is a substance of synthetic or natural origin, which belongs to the subclass of hormones of the adrenal cortex.

Has an effect on water, protein, mineral and carbohydrate metabolism.

Artificially created drugs act as immunosuppressive, desensitizing, anti-shock, antitoxic and anti-inflammatory drugs.

Preparations that include

Drugs that include glucocorticosteroids:

  • Alclomethasone (Afloderm).
  • Betamethasone (Acriderm, Beloderm, Belosalik, Belogent, Diprosalik, Diprospan, Garazon, Nasobek, Triderm, Flucicort, Celeston, Celestoderm-B).
  • Beclomethasone dipropionate (Aldecin, Bezlason Eco, Beclodget, Bekotid, Clenil, Rinochenyl).
  • Budesonide (Benocort, Pulmicort, Symbicort Turbuhaler, Tafen Nazal). Flumethasone (Lorinden C, Seretide).
  • Hydrocortisone (Hydrocortisone, Cortef, Laticort, Oxycourt).
  • Dexamethasone (Ambien, Dexa-Gentamicin, Maxidex, Maxitrol, Polydex, Tevodex).
  • Methylprednisolone (Advantan, Metipred, Solu-Medrol).
  • Mometasone furoate (Momat, Nazonex, Elokom).
  • Prednisolone (Aurobin, Dermozolone, Prednisolone).
  • Triamcinolone acetonide (Kenalog, Polcortolone, Fluorocort).
  • Fluticasone propionate (Fliksonase, Fliksotid).
  • Flukortolon (Ultraproject).

Preparations containing glucocorticosteroids are divided into 3 groups:

  • Short-acting medicines.
  • Medications of average duration of action - Methylprednisolone and Prednisolone.
  • Long-acting medicines - Betamethasone and Dexamethasone.

Inhaled glucocorticosteroids: Triamcinolone acetonide, budesonide, mometasone furoate, beclomethasone dipropionate, fluticasone propionate.

Indications for use

Indications for use of glucocorticosteroids:

  • Adrenal insufficiency (primary, secondary chronic and acute).
  • Congenital dysfunction of the adrenal cortex.
  • Bronchial asthma.
  • Severe form of pneumonia.
  • Rheumatism.
  • Subacute thyroiditis.
  • Exacerbation of chronic obstructive pulmonary disease.
  • Acute respiratory distress syndrome.
  • Crohn's disease.
  • Nonspecific ulcerative colitis.
  • Interstitial lung diseases.
  • Acute lymphoblastic and myeloblastic leukemia.
  • Infectious mononucleosis.
  • Eczema and other skin diseases.
  • Allergic diseases.
  • Transplantation of internal organs.
  • Autoimmune diseases.
  • Malignant neoplasms.

Intrasolutely glucocorticosteroids are used in the following cases:

  • Seasonal or all-the-year-round rhinitis.
  • Polyposis of the nose.
  • Rhinitis is not allergic with eosinophilia.
  • Idiopathic rhinitis.

Inhalations with glucocorticosteroids are used to treat chronic obstructive pulmonary disease and bronchial asthma.

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Glucocorticosteroids are used to treat arthritis in the following cases:

  • Lesion of several joints at the same time.
  • Disturbance of mobility of joints due to severe pain.
  • Inability to use other drugs for any reason.

Contraindications

With special care, preparations of glucocorticosteroids are taken by people suffering from diabetes mellitus, Itenko-Cushing's disease, thromboembolism, increased blood pressure (hypertension), peptic ulcer disease, viral eye lesions, systemic mycoses, severe renal insufficiency, and herpes.

The main contraindications to the drugs are the following pathological conditions:

  • syphilis;
  • tuberculosis;
  • glaucoma;
  • pustular processes on the skin;
  • damage to the cornea of ​​the eye with epithelial defects;
  • the period of breastfeeding.

If we talk about intranasal glucocorticosteroids, they can not be administered with hemorrhagic diathesis, repeated nosebleeds, and also, with individual intolerance.

During the period of therapy with the aforementioned agents, chicken pox and measles are more severe.

Before using this medication, it is absolutely necessary to consult a physician and thoroughly study the instructions for use.

Instructions for use Glucocorticosteroid (method and dosage)

Glucocorticosteroids can be administered parenterally, intra- and periarticularly, by inhalation, intranasally, retro- and parabulbarno, in the form of eye and ear drops, externally in the form of ointments, creams, lotions, orally or in the form of injections. Dosage and duration of treatment is determined by the doctor in each case.

Injection is performed in the joint after preliminary evacuation of excess fluid. If necessary, articular fluid can be sent to the laboratory for further study.

Substitution therapy GCS

Substitution therapy is prescribed for adrenal insufficiency. Physiological doses of glucocorticosteroids are used.

If it is necessary to conduct surgical intervention and acute disease, the total recommended dosage can be increased 2-5 times.

Rules of use: at 6-8 am the maximum dose of the drug is prescribed, and then the rest is introduced later. With chronic insufficiency of the adrenal cortex, SCS is administered for life.

Suppressive therapy GCS

Conducted with congenital dysfunction of the adrenal cortex in childhood in supraphysiological doses. Most of the dose is given in the evening.

Pharmacodynamic therapy

It is used for the treatment of allergic and inflammatory diseases.

There are several types of pharmacodynamic therapy:

  • Intensive is prescribed for acute conditions that threaten life. The drug is administered intravenously, starting with the maximum dosage (5 mg per kilogram of body weight). After relief of acute condition, GCS is abruptly abolished.
  • Limiting is prescribed for chronic and subacute conditions (systemic scleroderma, bronchial asthma, systemic lupus erythematosus, hemolytic anemia, leukemia, etc.). The duration of treatment is several months, and the recommended dosage is 2-5 mg per kilogram of body weight per day.

It is acceptable to use SCS using one of the following schemes:

  • Alternative therapy. Medications with short or medium duration of action are administered once in the morning.
  • Intermittent scheme involves the use of GCS short courses in 3-4 days with interruptions of 4 days between them.
  • Pulse therapy consists in the rapid administration of intravenously a large dose of the drug from 1g for emergency care.

Side effects

The use of glucocorticosteroids can cause the following side effects:

  • From the central nervous system: euphoria, psychosis, depression, insomnia, increased excitability.
  • From the cardiovascular system: increased blood pressure, deep vein thrombosis, myocardial dystrophy, thromboembolism.
  • From the digestive system: pancreatitis, fatty liver, bleeding in the organs of the gastrointestinal tract, steroid ulcers of the intestine and stomach.
  • From the sense organs: glaucoma, posterior subcapsular cataract.
  • On the part of the endocrine system: diabetes, obesity, atrophy of the adrenal cortex, Cushing's syndrome.
  • From the skin: striae, alopecia, thinning of the skin.
  • From the musculoskeletal system: osteoporosis, growth retardation in children, fractures and aseptic necrosis of tissues, muscle hypotrophy, myopathy.
  • On the part of the reproductive system: violation of the menstrual cycle, decreased libido, hirsutism, delay in sexual development.
  • Hypokalemia, hyperglycemia, hyperlipidemia, hypercholesterolemia, neutrophilic leukocytosis.
  • Others: puffiness, water and sodium retention.

Local side effects of inhaled glucocorticosteroids: cough, dysphonia, candidiasis of the oral cavity.

Side effects of intranasal drugs: sneezing, nosebleeds, perforation of the nasal septum, itching in the nose, dryness and burning in the nose and nose.

Overdose

Continuous use of GCS or excess of the recommended dose leads to suppression of the functions of the adrenal cortex and the suppression of natural hormone production.

Analogues

Analogs for ATX code: none.

Medicines with a similar mechanism of action (coincidence of the ATC code of the 4th level): no data.

Do not make the decision to replace the drug yourself, consult a doctor.

pharmachologic effect

Glucocorticosteroids are steroids that are synthesized by the adrenal cortex. Their main role is to increase the stress-resistance of the organism, normalize protein, water, carbohydrate and mineral metabolism in the body.

Artificially synthesized steroids have anti-inflammatory, immunosuppressive, anti-shock and antitoxic effects.

Glucocorticosteroids penetrate the cytoplasm of the cell, where they interact with intracellular steroid receptors.

special instructions

Patients with cirrhosis of the liver, hypoalbuminemia, hypothyroidism and elderly people need a dosage adjustment.

Patients taking SCS are more likely to suffer such infectious diseases as measles and chicken pox.

During the application of GCS, the administration of live vaccines is prohibited.

With prolonged use of glucocorticosteroids, the risk of developing osteoporosis increases.

Steroid ulcers that develop on the background of SCS can be asymptomatic or malosymptomatic, accompanied by bleeding or perforation. Therefore, patients are recommended to periodically take a blood test for latent blood and carry out fibroesophagogastroduodenoscopy.

In the treatment of inflammatory or autoimmune diseases (rheumatoid arthritis, systemic lupus erythematosus and intestinal diseases), cases of steroid resistance may be observed.

The elimination of glucocorticosteroids is gradual due to the high risk of withdrawal syndrome. Abrupt cancellation is permissible in exceptional cases, in the main there is a gradual decrease in the dosage of the drug.

At pregnancy and thoracal feeding

The use of glucocorticosteroids during pregnancy is possible only if the benefit to the mother exceeds the potential harm to the fetus.

In childhood

Application in childhood is acceptable on strict indications (for example, stunting or sexual development).

In old age

With special care is used to treat people of advanced age.

Drug Interactions

Inductors of microsomal liver enzymes increase the therapeutic and toxic effect of GCS, and their reduction is promoted by contraceptives and estrogens.

Glycosides of digitalis, diuretics, amphotericin B, inhibitors of carbonic anhydrase increase the risk of hypokalemia and arrhythmia.

Nonsteroidal anti-inflammatory drugs and ethanol increase the likelihood of bleeding and ulcerative lesions of the gastrointestinal tract.

GCS reduces the hypoglycemic effect of antidiabetic drugs and insulin; diuretic and natriuretic effect of diuretics; anticoagulant and fibrinolytic - derivatives of coumarin and indandione, heparin, streptokinase and urokinase, the activity of vaccines, reduce the concentration in the blood of salicylates, mexiletine.

Mitotan, Metarapon, Ketoconazole, Triloston and Aminoklutetimid suppress the secretion of corticosteroids by the adrenal cortex

Conditions of leave from pharmacies

Information is absent.

Terms and conditions of storage

Conditions and periods of storage depend on the form of the drug.

Price in pharmacies

Price Glucocorticosteroid for 1 package from 148 rubles.

A source: http://dolgojit.net/gliukokortikosteroid.php

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