home Audience 1 Characteristics and list of glucocorticosteroid drugs: rules for the use of hormonal drugs for renal diseases. Glucocorticosteroids for the treatment of joint diseases GCS mechanism of action

Characteristics and list of glucocorticosteroid drugs: rules for the use of hormonal drugs for renal diseases. Glucocorticosteroids for the treatment of joint diseases GCS mechanism of action

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The site provides reference information for informational purposes only. Diagnosis and treatment of diseases must be carried out under the supervision of a specialist. All drugs have contraindications. Consultation with a specialist is required!

Introduction (characteristics of drugs)

Natural corticosteroids

Corticosteroids- common name hormones adrenal cortex, which includes glucocorticoids and mineralocorticoids. The main glucocorticoids produced in the human adrenal cortex are cortisone and hydrocortisone, and the mineralocorticoid is aldosterone.

Corticosteroids perform many very important functions in the body.

Glucocorticoids refer to steroids, which have an anti-inflammatory effect, they are involved in the regulation of the metabolism of carbohydrates, fats and proteins, control puberty, kidney function, the body's response to stress, and contribute to the normal course of pregnancy. Corticosteroids are inactivated in the liver and excreted in the urine.

Aldosterone regulates the metabolism of sodium and potassium. Thus, under the influence mineralocorticoids Na+ is retained in the body and the excretion of K+ ions from the body increases.

Synthetic corticosteroids

Synthetic corticosteroids, which have the same properties as natural ones, have found practical application in medical practice. They are capable of temporarily suppressing the inflammatory process, but they have no effect on the infectious origin or pathogens of the disease. After the corticosteroid drug wears off, the infection returns.

Corticosteroids cause tension and stress in the body, and this leads to a decrease in immunity, since immunity is provided at a sufficient level only in a relaxed state. Considering the above, we can say that the use of corticosteroids contributes to the protracted course of the disease and blocks the regeneration process.

In addition, synthetic corticosteroids suppress the function of natural corticosteroid hormones, which leads to dysfunction of the adrenal glands in general. Corticosteroids affect the functioning of other endocrine glands and disrupt the hormonal balance of the body.

Corticosteroid drugs, eliminating inflammation, also have an analgesic effect. Synthetic corticosteroid drugs include Dexamethasone, Prednisolone, Sinalar, Triamcinolone and others. These drugs are more active and cause fewer side effects than natural ones.

Forms of release of corticosteroids

Corticosteroids are produced in the form of tablets, capsules, solutions in ampoules, ointments, liniments, and creams. (Prednisolone, Dexamethasone, Budenofalm, Cortisone, Cortinef, Medrol).

Preparations for internal use (in tablets and capsules)

Preparations for injections

Preparations for local use (topical)

Topical corticosteroids are divided into more and less active ones.
Weakly active agents: Prednisolone, Hydrocortisone, Cortade, Lokoid;
Moderately active: Afloderm, Laticort, Dermovate, Fluorocort, Lorinden;
Highly active: Akriderm, Advantan, Kuterid, Apulein, Cutivate, Sinaflan, Sinalar, Sinoderm, Flucinar.
Very highly active: Clobetasol.

Corticosteroids for inhalation

Beclamethasone in the form of metered aerosols (Becotide, Aldecim, Beclomet, Beclocort); in the form of becodisks (powder in a single dose, inhaled using a diskhaler); in the form of a dosed aerosol for inhalation through the nose (Beclomethasone-nasal, Beconase, Aldecim);
Flunisolide in the form of metered aerosols with a spacer (Ingacort), for nasal use (Sintaris);
Budesonide – dosed aerosol (Pulmicort), for nasal use – Rhinocort;
Fluticasone in the form of Flixotide and Flixonase aerosols;
Triamcinolone - metered-dose aerosol with a spacer (Azmacort), for nasal use - Nazacort.

Indications for use

Corticosteroids are used to suppress inflammation in many branches of medicine and for many diseases.

Indications for the use of glucocorticoids

Rheumatism;
rheumatoid and other types of arthritis;
collagenoses, autoimmune diseases (scleroderma, systemic lupus erythematosus, periarteritis nodosa, dermatomyositis);
blood diseases (myeloblastic and lymphoblastic leukemia);
some types of malignant neoplasms;
skin diseases (neurodermatitis, psoriasis, eczema, seborrheic dermatitis, discoid lupus erythematosus, atopic dermatitis, erythroderma, lichen planus);
bronchial asthma;
allergic diseases;
pneumonia and bronchitis, fibrosing alveolitis;
ulcerative colitis and Crohn's disease;
acute pancreatitis;
hemolytic anemia;
viral diseases (infectious mononucleosis, viral hepatitis and others);
external otitis (acute and chronic);
treatment and prevention of shock;
in ophthalmology (for non-infectious diseases: iritis, keratitis, iridocyclitis, scleritis, uveitis);
neurological diseases (multiple sclerosis, acute spinal cord injury, optic neuritis;
during organ transplantation (to suppress rejection).

Indications for the use of mineralocorticoids

Addison's disease (chronic deficiency of adrenal hormones);
myasthenia gravis (an autoimmune disease manifested by muscle weakness);
disorders of mineral metabolism;
adynamia and muscle weakness.

Contraindications

Contraindications for the use of glucocorticoids:

hypersensitivity to the drug;
severe infections (except tuberculous meningitis and septic shock);
immunization with live vaccine.

Carefully Glucocorticosteroids should be used for diabetes mellitus, hypothyroidism, gastric and duodenal ulcers, ulcerative colitis, high blood pressure, liver cirrhosis, cardiovascular failure in the stage of decompensation, increased thrombus formation, tuberculosis, cataracts and glaucoma, mental illness.

Contraindications for the use of mineralocorticoids:

high blood pressure;
diabetes;
low potassium levels in the blood;
renal and hepatic failure.

Adverse reactions and precautions

Corticosteroids can cause a wide variety of side effects. When using weakly or moderately active drugs, adverse reactions are less pronounced and occur rarely. High doses of drugs and the use of highly active corticosteroids, their long-term use can cause the following side effects:

the appearance of edema due to sodium and water retention in the body;
increased blood pressure;
increased blood sugar levels (even the development of steroid diabetes mellitus is possible);
osteoporosis due to increased calcium secretion;
aseptic necrosis of bone tissue;
exacerbation or occurrence of gastric ulcer; gastrointestinal bleeding;
increased thrombus formation;
weight gain;
the occurrence of bacterial and fungal infections due to decreased immunity (secondary immunodeficiency);
menstrual irregularities;
neurological disorders;
development of glaucoma and cataracts;
skin atrophy;
increased sweating;
the appearance of acne;
suppression of the tissue regeneration process (slow wound healing);
excess facial hair growth;
suppression of adrenal function;
mood instability, depression.

Long courses of corticosteroids can lead to changes in the patient's appearance (Cushing's syndrome):

excess fat deposition in certain areas of the body: on the face (the so-called “moon face”), on the neck (“bull neck”), chest, and abdomen;
the muscles of the limbs are atrophied;
bruising on the skin and stretch marks (stretch marks) on the abdomen.

With this syndrome, there is also growth retardation, disturbances in the formation of sex hormones (menstrual irregularities and male hair growth in women, and signs of feminization in men).

To reduce the risk of adverse reactions, it is important to respond promptly to their occurrence, adjust doses (use small doses whenever possible), control body weight and calorie content of foods consumed, and limit the consumption of table salt and liquid.

How to use corticosteroids?

Glucocorticosteroids can be used systemically (in the form of tablets and injections), locally (intra-articular, rectal administration), topically (ointments, drops, aerosols, creams).

The dosage regimen is prescribed by the doctor. The tableted drug should be taken from 6 a.m. (first dose) and no later than 2 p.m. for subsequent doses. Such conditions of administration are necessary to approach the physiological entry of glucocorticoids into the blood when they are produced by the adrenal cortex.

In some cases, with large doses and depending on the nature of the disease, the dose is distributed by the doctor to be distributed evenly throughout the day in 3-4 doses.

The tablets should be taken with meals or immediately after meals with a small amount of water.

Treatment with corticosteroids

There are the following types of corticosteroid therapy:

intense;
limiting;
alternating;
intermittent;
pulse therapy.

At intensive care(in the case of an acute, life-threatening pathology), the drugs are administered intravenously and, when the effect is achieved, are canceled at once.

Limiting therapy used for long-term, chronic processes - as a rule, tablet forms are used for several months or even years.

To reduce the inhibitory effect on the function of the endocrine glands, intermittent drug dosing regimens are used:

alternating therapy – use glucocorticoids with short and medium duration of action (Prednisolone, Methylprednisolone) once from 6 to 8 am every 48 hours;
intermittent therapy – short, 3-4-day courses of taking the drug with 4-day breaks between them;
pulse therapy– rapid intravenous administration of a large dose (at least 1 g) of the drug for emergency care. The drug of choice for such treatment is Methylprednisolone (it is more accessible for administration to the affected areas and has fewer side effects).

Daily doses of drugs(in terms of Prednisolone):

Low – less than 7.5 mg;
Medium – 7.5 -30 mg;
High – 30-100 mg;
Very high – above 100 mg;
Pulse therapy – above 250 mg.

Treatment with corticosteroids should be accompanied by the prescription of calcium and vitamin D supplements for the prevention of osteoporosis. The patient's diet should be rich in proteins, calcium and include a limited amount of carbohydrates and table salt (up to 5 g per day), liquid (up to 1.5 l per day).

For prevention If there is an undesirable effect of corticosteroids on the gastrointestinal tract, before taking the tablets, you can recommend using Almagel, jelly. It is recommended to exclude smoking and alcohol abuse; moderate exercise.

Corticosteroids for children

Systemic glucocorticoids are prescribed to children exclusively for absolute indications. For bronchial obstruction syndrome that threatens the life of a child, intravenous prednisolone is used at a dose of 2-4 mg per 1 kg of the child’s body weight (depending on the severity of the disease), and if there is no effect, the dose is increased by 20-50% every 2-4 hours until getting the effect. After this, the drug is discontinued immediately, without gradually reducing the dosage.

Children with hormonal dependence (with bronchial asthma, for example), after intravenous administration of the drug, are gradually transferred to a maintenance dose of prednisolone. For frequent relapses of asthma, Beclamethasone dipropionate is used in the form of inhalations - the dose is selected individually. After obtaining the effect, the dose is gradually reduced to a maintenance dose (selected individually).

Topical glucocorticoids(creams, ointments, lotions) are used in pediatric practice, but children have a higher predisposition to the systemic effects of drugs than adult patients (delayed development and growth, Itsenko-Cushing syndrome, inhibition of the function of the endocrine glands). This is because children have a larger body surface area to body weight ratio than adults.

For this reason, topical glucocorticoids should be used in children only in limited areas and for a short course. This is especially true for newborns. For children in the first year of life, you can only use ointments containing no more than 1% hydrocortisone or a fourth-generation drug - Prednicarbate (Dermatol), and for children under 5 years of age - Hydrocortisone 17-butyrate or ointments with medium strength drugs.

For the treatment of children over 2 years old, Mometasone can be used as prescribed by a doctor (ointment, has a prolonged effect, applied once a day).

There are other drugs for the treatment of atopic dermatitis in children, with a less pronounced systemic effect, for example, Advantan. It can be used for up to 4 weeks, but its use is limited due to the possibility of local adverse reactions (dryness and thinning of the skin). In any case, the choice of drug to treat the child remains with the doctor.

Corticosteroids during pregnancy and lactation

The use of glucocorticoids, even short-term, can “program” for decades to come the work of many organs and systems in the unborn child (blood pressure control, metabolic processes, behavior formation). The synthetic hormone imitates the stress signal for the fetus from the mother and thereby causes the fetus to speed up the use of reserves.

This negative effect of glucocorticoids is enhanced by the fact that modern long-acting drugs (Metypred, Dexamethasone) are not deactivated by placental enzymes and have a long-lasting effect on the fetus. Glucocorticoids, by suppressing the immune system, help reduce a pregnant woman's resistance to bacterial and viral infections, which can also negatively affect the fetus.

Glucocorticoid drugs can be prescribed to a pregnant woman only if the result of their use significantly outweighs the risk of possible negative consequences for the fetus.

Such indications may be:
1. Threat of premature birth (a short course of hormones improves the readiness of the premature fetus for birth); the use of surfactant for the child after birth has allowed us to minimize the use of hormones for this indication.
2. Rheumatism and autoimmune diseases in the active phase.
3. Hereditary (intrauterine) hyperplasia of the fetal adrenal cortex is a difficult disease to diagnose.

Previously, there was a practice of prescribing glucocorticoids to maintain pregnancy. But no convincing data on the effectiveness of this technique have been obtained, so it is not currently used.

In obstetric practice Metypred, Prednisolone and Dexamethasone are more often used. They penetrate the placenta in different ways: Prednisolone is destroyed by enzymes in the placenta to a greater extent, and Dexamethasone and Metipred - by only 50%. Therefore, if hormonal drugs are used to treat a pregnant woman, it is preferable to prescribe Prednisolone, and if to treat the fetus, it is preferable to prescribe Dexamethasone or Metypred. In this regard, Prednisolone causes adverse reactions in the fetus less often.

For severe allergies, glucocorticoids are prescribed both systemically (injections or tablets) and local (ointments, gels, drops, inhalations). They have a powerful antiallergic effect. The following drugs are mainly used: Hydrocortisone, Prednisolone, Dexamethasone, Betamethasone, Beclomethasone.

Of the topical glucocorticoids (for local treatment), intranasal aerosols are used in most cases: for hay fever, allergic rhinitis, nasal congestion (sneezing). They usually have a good effect. Fluticasone, Dipropionate, Propionate and others have found widespread use.

In allergic conjunctivitis, due to the higher risk of side effects, glucocorticoids are rarely used. In any case, in case of allergic manifestations, hormonal medications cannot be used independently in order to avoid undesirable consequences.

Corticosteroids for psoriasis

Glucocorticoids for psoriasis should be used mainly in the form of ointments and creams. Systemic (injections or tablets) hormonal drugs can contribute to the development of a more severe form of psoriasis (pustular or pustular), so their use is not recommended.

Glucocorticoids for local use (ointments, creams) are usually used 2 times a day. per day: creams during the day without dressings, and at night together with coal tar or anthralin using an occlusive dressing. For extensive lesions, approximately 30 g of the drug is used to treat the entire body.

The choice of glucocorticoid drug according to the degree of activity for topical use depends on the severity of psoriasis and its prevalence. As the psoriasis lesions decrease during treatment, the drug should be changed to a less active one (or used less frequently) to minimize the occurrence of side effects. When the effect is obtained after about 3 weeks, it is better to replace the hormonal drug with an emollient for 1-2 weeks.

The use of glucocorticoids over large areas over a long period can aggravate the process. Relapse of psoriasis after stopping the use of the drug occurs earlier than with treatment without the use of glucocorticoids.
, Coaxil, Imipramine and others) in combination with glucocorticoids can cause an increase in intraocular pressure.

Glucocorticoids (with long-term use) enhance the effectiveness of adrenomimetics (Adrenaline, Dopamine, Norepinephrine).

Theophylline in combination with glucocorticoids contributes to the appearance of a cardiotoxic effect; enhances the anti-inflammatory effect of glucocorticoids.

Amphotericin and diuretics in combination with corticosteroids increase the risk of hypokalemia (low potassium levels in the blood) and increased diuretic effects (and sometimes sodium retention).

The combined use of mineralocorticoids and glucocorticoids increases hypokalemia and hypernatremia. With hypokalemia, side effects of cardiac glycosides may occur. Laxatives may potentiate hypokalemia.

Indirect anticoagulants, Butadione, Ethacrynic acid, Ibuprofen in combination with glucocorticoids can cause hemorrhagic manifestations (bleeding), and salicylates and Indomethacin can cause the formation of ulcers in the digestive organs.

Glucocorticoids enhance the toxic effect on the liver of paracetamol.

Retinol preparations reduce the anti-inflammatory effect of glucocorticoids and improve wound healing.

The use of hormones together with Azathioprine, Methandrostenolone and Chingamin increases the risk of developing cataracts and other adverse reactions.

Glucocorticoids reduce the effect of Cyclophosphamide, the antiviral effect of Idoxuridine, and the effectiveness of glucose-lowering drugs.

Estrogens enhance the effect of glucocorticoids, which may make it possible to reduce their dosage.

Androgens (male sex hormones) and iron supplements enhance erythropoiesis (the formation of red blood cells) when combined with glucocorticoids; reduce the process of hormone elimination, contribute to the appearance of side effects (increased blood clotting, sodium retention, menstrual irregularities).

The initial stage of anesthesia when using glucocorticoids is lengthened and the duration of anesthesia is reduced; Fentanyl doses are reduced.

Rules for withdrawing corticosteroids

With long-term use of glucocorticoids, drug withdrawal should be gradual. Glucocorticoids suppress the function of the adrenal cortex, so if the drug is stopped quickly or suddenly, adrenal insufficiency may develop. There is no standardized regimen for discontinuing corticosteroids. The mode of withdrawal and dose reduction depends on the duration of the previous course of treatment.

If the duration of the glucocorticoid course is up to several months, then you can reduce the dose of Prednisolone by 2.5 mg (0.5 tablets) every 3-5 days. With a longer course duration, the dose is reduced more slowly - by 2.5 mg every 1-3 weeks. With great caution, reduce the dose below 10 mg - 0.25 tablets every 3-5-7 days.

If the initial dose of Prednisolone was high, then at first the reduction is carried out more intensively: by 5-10 mg every 3 days. Upon reaching the daily dose equal to 1/3 of the original dose, reduce by 1.25 mg (1/4 tablet) every 2-3 weeks. As a result of this reduction, the patient receives maintenance doses for a year or more.

The drug reduction regimen is prescribed by the doctor, and violation of this regimen can lead to an exacerbation of the disease - treatment will have to be started again with a higher dose.

Prices for corticosteroids

Since there are so many corticosteroids available in different forms, prices for just a few are listed here:

Hydrocortisone – suspension – 1 bottle 88 rubles; eye ointment 3 g – 108 rubles;
Prednisolone – 100 tablets of 5 mg – 96 rubles;
Metypred – 30 tablets of 4 mg – 194 rubles;
Metypred – 250 mg 1 bottle – 397 rubles;
Triderm - ointment 15 g - 613 rubles;
Triderm – cream 15 g – 520 rubles;
Dexamed – 100 ampoules of 2 ml (8 mg) – 1377 rubles;
Dexamethasone – 50 tablets of 0.5 mg – 29 rubles;
Dexamethasone – 10 ampoules of 1 ml (4 mg) – 63 rubles;
Oftan Dexamethasone – eye drops 5 ml – 107 rubles;
Medrol – 50 tablets of 16 mg – 1083 rubles;
Flixotide – aerosol 60 doses – 603 rubles;
Pulmicort – aerosol 100 doses – 942 rubles;
Benacort – aerosol 200 doses – 393 rubles;
Symbicort - aerosol with a dispenser of 60 doses - 1313 rubles;
Beclazon - aerosol 200 doses - 475 rubles.

Before use, you should consult a specialist.

I. G. Bereznyakov

Glucocorticoids in clinical practice

Kharkov Institute for Advanced Medical Studies

Introduction

Cells of the zona fasciculata of the adrenal cortex under physiological conditions secrete two main glucocorticoids into the blood - cortisone and cortisol (hydrocortisone). The secretion of these hormones is regulated by corticotropin of the adenohypophysis (formerly called adrenocorticotropic hormone). An increase in the level of cortisol in the blood, through a feedback mechanism, inhibits the secretion of corticotropin in the hypothalamus and corticotropin in the pituitary gland.

The intensity of glucocorticoid secretion into the blood changes significantly during the day. The maximum content of hormones in the blood is observed in the early morning hours (6-8 hours), the minimum in the evening and at night.

The physiological effects of glucocorticoids are largely opposite to those caused by insulin. Hormones have catabolic (i.e., they promote the breakdown of complex protein molecules into simple substances) and anti-anabolic (i.e., they interfere with the biosynthesis of protein molecules) effects on protein metabolism. As a result, protein breakdown in the body increases and the excretion of nitrogenous products increases. Protein breakdown occurs in muscle, connective and bone tissues. The level of albumin in the blood decreases.

Glucocorticoids stimulate triglyceride catabolism and inhibit fat synthesis from carbohydrates. At the same time, a decrease in adipose tissue in the extremities is often combined with an increase in fat deposition on the abdominal wall and between the shoulder blades. Hyperglycemia under the influence of hormones occurs due to increased formation of glucose in the liver from amino acids (gluconeogenesis) and suppression of its utilization by tissues; the glycogen content in the liver also increases. Glucocorticoids reduce tissue sensitivity to insulin and the synthesis of nucleic acids.

Hormones increase the sensitivity of adrenergic receptors to catecholamines, enhance the pressor effects of angiotensin II, reduce capillary permeability, and take part in maintaining normal arteriolar tone and myocardial contractility. Under the influence of glucocorticoids, the content of lymphocytes, monocytes, eosinophils and basophils in the blood decreases, the release of neutrophils from the bone marrow is stimulated and their number in the peripheral blood increases. Hormones retain sodium and water in the body against the background of potassium loss, inhibit the absorption of calcium in the intestines, and promote the release of the latter from bone tissue and its excretion in the urine. Glucocorticoids increase sensory sensitivity and excitability of the nervous system, participate in stress reactions, and affect the human psyche.

Natural glucocorticoids and their synthetic analogues are widely used in the clinic mainly because they have several more valuable qualities: they have anti-inflammatory, immunosuppressive, anti-allergic and anti-shock effects. The final results of therapy depend on many factors, including the duration of treatment, the dose of drugs, the method and mode of their administration, the immunological and immunogenetic characteristics of the diseases themselves, etc. In addition, various glucocorticoids have varying degrees of immunosuppressive and anti-inflammatory effects, among which there is no direct relationship. Thus, dexamethasone has powerful anti-inflammatory and relatively low immunosuppressive activity.

Comparative characteristics of glucocorticoids

Natural glucocorticoids (cortisone and hydrocortisone) and their semisynthetic derivatives are used in clinical practice. The latter, in turn, are divided into non-fluorinated (prednisone, prednisolone, methylprednisolone) and fluorinated (triamcinolone, dexamethasone and betamethasone).

When taken orally, glucocorticoids are rapidly and almost completely absorbed in the upper jejunum. Eating does not affect the degree of absorption of hormones, although the rate of this process slows down somewhat.

The peculiarities of the use of injectable forms are determined both by the properties of the glucocorticoid itself and the ester associated with it. For example, succinates, hemisuccinates and phosphates dissolve in water and, when administered parenterally, have a rapid but relatively short-term effect. On the contrary, acetates and acetonides are fine-crystalline suspensions and are insoluble in water. Their action develops slowly, over several hours, but lasts for a long time (weeks). Water-soluble glucocorticoid esters can be used intravenously, fine-crystalline suspensions cannot.

Depending on the duration of the therapeutic effect, all glucocorticoids are divided into 3 groups (Table 1). Knowledge of equivalent dosages of corticosteroids allows, if necessary, to replace one drug with another. The previously existing principle - “pill for tablet” (that is, if it is necessary to transfer the patient to another glucocorticoid, he was prescribed the same number of tablets of the new drug as he received before the change) - is not currently valid. This is explained by the introduction into clinical practice of dosage forms of glucocorticoids with different contents of the active principle.

Table 1

Glucocorticoid hormones

Duration of action	Drug name	Equivalent dosage (mg)
Short acting	Hydrocortisone	20
	Cortisone	25
	Prednisone	5
	Prednisolone	5
	Methylprednisolone	4
	Triamcinolone	4
	Paramethasone	2
Long-lasting	Dexamethasone	0,75
Long-lasting	Betamethasone	0,6

Natural glucocorticoids have mineralocorticoid activity, although weaker than true mineralocorticoids. Non-fluorinated semisynthetic glucocorticoids also have mineralocorticoid effects (the severity of which, in turn, is inferior to the effects of natural glucocorticoids). Fluorinated drugs do not have mineralocorticoid activity (Table 2). The glucocorticoid activity of semisynthetic drugs is higher than that of cortisone and hydrocortisone, which is explained by lower protein binding compared to natural glucocorticoids. A feature of fluoridated drugs is their slower metabolism in the body, which entails an increase in the duration of action of the drugs.

table 2

Comparative characteristics of glucocorticoids for systemic use

Duration of action	Drug name	Gluco- corticoid activity	Mineral corticoid activity
Short acting	Hydrocortisone	1	1
	Cortisone	0,8	1
	Prednisone	4	0,8
	Prednisolone	4	0,8
	Methylprednisolone	5	0,5
Average duration of action	Triamcinolone	5	-
Long-lasting	Dexamethasone	30	-
Long-lasting	Betamethasone	30	-

The terms widely used in the medical literature are: “low” doses of glucocorticoids, “high”, etc. “Low” doses of corticosteroids are spoken of if the daily dose does not exceed 15 mg (3 tablets) of prednisolone (or an equivalent dose any other drug). Such doses are usually prescribed for maintenance treatment. If the daily dose of prednisolone is 20-40 mg (4-8 tablets), they speak of “medium” doses of glucocorticoids, and more than 40 mg/day are “high”. Values close to those given are also obtained when calculating the daily dose of corticosteroids per 1 kg of patient body weight. The conventional boundary between “medium” and “high” doses is 0.5 mg of prednisolone per 1 kg of patient body weight per day.

Over the past 20 years, the clinic has also used intravenous administration of very large doses of glucocorticoids (at least 1 g of methylprednisolone per day) for several days. This treatment method is called “pulse therapy”.

The dose of glucocorticoids prescribed at the beginning of treatment for a particular disease depends mainly on the nosological form and severity of the disease. The dose size is also affected by the age of the patient; presence or absence of concomitant diseases; concomitant use of other medications and other factors.

The main clinical uses of glucocorticoids can be summarized as follows:

local application:

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	external - skin, eyes, ears (in the form of ointments, drops, creams, lotions, aerosols);
	inhalation - into the lungs or nasal cavity;
	intrathecal (epidural);
	intradermal - into scars;
	intracavitary - into the pleural cavity, intrapericardial, etc.;
	intra-articular and periarticular;
	systemic use:
	inside;
	in suppositories (suppositories);
	parenterally (mainly intramuscularly and intravenously).

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In terms of durability and severity of the therapeutic anti-inflammatory effect, as well as tolerability, prednisolone and methylprednisolone are the best.

Prednisolone is considered as a standard drug for pharmacodynamic therapy. The ratio of glucocorticoid and mineralocorticoid activity of prednisolone is 300:1.

Methylprednisolone Compared to prednisolone, it has slightly greater glucocorticoid activity (20%) and has a weak mineralocorticoid effect. The advantage of the drug is its very moderate stimulation of the psyche and appetite, which justifies its use in patients with an unstable psyche and excess body weight.

Prednisone is hydroxylated in the liver (where it is converted to prednisolone), and is therefore not recommended for severe liver disease. Cheaper than prednisolone, but used less frequently in clinical practice.

Triamcinolone- a fluorinated glucocorticoid devoid of mineralocorticoid activity. Hence, the ability to retain sodium and water is lower compared to other drugs. Compared to prednisolone, it has a more pronounced (20%) and longer-lasting glucocorticoid effect. On the other hand, it more often causes undesirable reactions from muscle tissue (“triamcinolone” myopathy) and skin. Therefore, long-term use of this medication is undesirable.

Dexamethasone Its glucocorticoid activity is 7 times greater than that of prednisolone. It is a fluorinated glucocorticoid and does not have a mineralocorticoid effect. Compared to other drugs, it suppresses the function of the adrenal cortex to a greater extent. Long-term use is not recommended due to the risk of serious side effects (primarily inhibition of the hypothalamic-pituitary-adrenal axis, metabolic disorders, psychostimulating effects).

Betamethasone- a fluorinated glucocorticoid, which is similar in strength and duration of action to dexamethasone. It is slightly superior to the latter in glucocorticoid activity (8-10 times higher than prednisolone) and has a lesser effect on carbohydrate metabolism. Betamethasone phosphate is water-soluble and can be administered intravenously and subconjunctivally. For intramuscular, intra-articular and periarticular administration, a mixture of two betamethasone esters is used - phosphate (absorbed quickly) and dipropionate (absorbed slowly). This mixture is a fine-crystalline suspension that cannot be administered intravenously. Phosphate provides a quick effect (within 30 minutes), and diproprionate has a long-lasting effect, up to 4 weeks or more.

Cortisone Currently, it is practically not used due to lower efficiency and poorer tolerability. Together with hydrocortisone, it has the most pronounced mineralocorticoid activity among all glucocorticoids. The main area of application is replacement therapy for adrenal insufficiency in patients with normal liver function (since cortisone is converted to hydrocortisone in the liver, in case of severe damage to this organ, the use of the drug is not recommended).

Hydrocortisone is perhaps the only glucocorticoid that could be used for long-term parenteral treatment, but it is significantly inferior to modern drugs in terms of tolerability. It is weaker than prednisolone in glucocorticoid activity (4 times), but superior to it in the severity of mineralocorticoid action. Hydrocortisone is commonly used for physiological replacement and stress relief in patients with hypothalamic-pituitary-adrenal axis deficiency. In acute adrenal insufficiency and other emergency conditions, hydrocortisone hemisuccinate is the drug of choice.

Beclomethasone, flunisolide, budesonide, triamcinolone acetonide and fluticasone administered by inhalation. Beclomethasone (beclomet, becotide, etc.) is most often prescribed for long-term maintenance therapy for bronchial asthma. It has a slight systemic effect, although in large doses (1000-2000 mcg/day) it causes osteoporosis and other side effects. The use of flunisolide (Ingacort) compared to beclomethasone leads to the development of oral candidiasis somewhat less frequently. Budesonide (Pulmicort) when administered by inhalation is slightly more effective and has less effect on renal function than beclomethasone. Fluticasone (flixotide, flixonase) has an affinity for glucocorticoid receptors that is 30 times greater than prednisolone and 2 times greater than budesonide. It has a 2 times stronger local anti-inflammatory effect than beclomethasone.

Indications and contraindications

The scope of glucocorticoids is so wide that even a cursory listing of diseases and pathological conditions for which they can be used as therapeutic agents would take up a lot of space. On the other hand, navigating such a list is also not easy. Therefore, below are the general indications for use and the scope of use of glucocorticoids.

In general, glucocorticosteroids can be used as agents:

replacement therapy for adrenal insufficiency;
suppressive therapy for adrenogenital syndrome;
pharmacodynamic therapy (i.e., as a means of symptomatic or pathogenetic treatment due to their inherent anti-inflammatory, antiallergic, immunosuppressive and other properties).

For replacement therapy of adrenal insufficiency, physiological doses of glucocorticoids are used. In patients with chronic adrenal insufficiency, drugs are used for life. Natural remedies (cortisone and hydrocortisone) are administered taking into account the rhythm of secretion of natural glucocorticoids (2/3 of the daily dose in the morning and 1/3 in the evening), synthetic derivatives are prescribed once a day in the morning.

In adrenogenital syndrome, to suppress the secretion of corticotropin (and subsequent reduction of hypersecretion of androgens by the adrenal cortex), glucocorticoids are used in therapeutic (i.e., supraphysiological) doses. According to the goal, the rhythm of hormone administration also changes. Glucocorticoids (cortisone or hydrocortisone) are taken either in equal doses 3 times a day, or 1/3 of the daily dose is prescribed in the morning, and 2/3 in the evening.

Pharmacodynamic therapy is the most common clinical use of glucocorticoids. An indispensable condition for treatment is taking into account the physiological rhythm of hormone secretion, which makes it possible to reduce the frequency and severity of undesirable effects.

The scope of application of corticosteroids can be outlined as follows.

Glucocorticoids are indicated for:

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	diffuse connective tissue diseases (systemic lupus erythematosus, severe rheumatoid arthritis, polyarteritis nodosa, etc.);
	allergic reactions (Quincke's edema, hay fever, urticaria, anaphylactic shock, etc.);
	kidney diseases (rapidly progressive glomerulonephritis, etc.);
	diseases of the adrenal glands (Addison's disease);
	blood diseases (autoimmune hemolytic anemia, thrombocytopenic purpura, etc.);
	lung diseases (bronchial asthma);
	diseases of the gastrointestinal tract (for example, Crohn's disease, certain forms of liver cirrhosis, etc.);
	diseases of the nervous system (some types of seizures);
	eye diseases (allergic keratitis, conjunctivitis, etc.);
	skin diseases (including erythema nodosum, eczema, etc.);
	malignant tumors (primarily leukemia and lymphoproliferative diseases);
	cerebral edema of various origins;
	some infectious diseases (tuberculous pericarditis, Pneumocystis pneumonia, etc.);
	severe shock states.

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Since glucocorticoids are natural hormones or their synthetic analogs, they have no absolute contraindications for use. In emergency cases, hormones are used without regard to contraindications at all. Relative contraindications are:

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	peptic ulcer of the stomach and duodenum in the acute stage;
	(severe) arterial hypertension;
	tuberculosis (except tuberculous pericarditis);
	acute viral infections (herpes, chicken pox, etc.);
	vaccination period;
	pregnancy;
	severe renal and heart failure;
	tendency to thromboembolic complications;
	severe osteoporosis;
	Itsenko-Cushing's disease and syndrome;
	diabetes mellitus (fluorinated glucocorticoids are the most dangerous);
	psychosis, epilepsy.

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Systemic use of glucocorticoids

To this day, discussions continue regarding the choice of adequate doses and optimal dosage forms of drugs, routes of administration, duration of therapy, and side effects. In general, the decision to use topical corticosteroids usually does not cause significant difficulty for clinicians. Therefore, in the following presentation the main attention will be focused on the systemic use of hormones.

If systemic administration of glucocorticoids is necessary, preference is given to oral administration. If it is not possible to administer these drugs orally, they can be used in suppositories; the dose in this case increases by 25-50%. Glucocorticoids existing in injection forms, when administered intramuscularly and, in particular, intravenously, are quickly metabolized in the body, and therefore their effect is short-lived and in most cases is not sufficient for long-term treatment. To obtain an equivalent therapeutic effect compared to oral administration, doses 2-4 times larger would have to be administered parenterally and frequent injections would have to be used. Existing long-acting drugs for parenteral use (for example, triamcinolone acetonide, or Kenalog) are not used for active “suppressive” treatment, but mostly as maintenance or local (for example, intra-articular) therapy.

In the morning hours, the hypothalamic-pituitary-adrenal axis is least sensitive to the inhibitory effects of exogenous corticosteroids. When dividing the daily dose of glucocorticoids into 3-4 parts and taking them at equal intervals, the risk of suppressing the hypothalamic-pituitary-adrenal axis increases. Therefore, in most cases, hormones are prescribed in the form of one morning dose (primarily long-acting drugs), or 2/3-3/4 of the daily dose is taken in the morning, and the rest - around noon. This regimen of use reduces the risk of suppression of the hypothalamic-pituitary-adrenal axis and reduces the risk of developing osteoporosis.

The therapeutic effectiveness of glucocorticoids increases with increasing dose and frequency of administration, but the severity of complications also increases equally. With alternating (every other day) use of hormones, the number of adverse reactions is less, but in many cases this regimen is not effective enough (for example, for blood diseases, (nonspecific) ulcerative colitis, malignant tumors, as well as for severe diseases). Alternative therapy is usually used after suppression of inflammatory and immunological activity by reducing the dose of glucocorticoids and switching to maintenance treatment. With an alternating dosing regimen, the dose of hormones required for a 48-hour period is administered every second day in the morning at a time. This approach makes it possible to reduce the inhibitory effect of exogenous glucocorticoids on the function of the patient’s adrenal cortex and, therefore, prevent its atrophy. In addition, with alternating use of glucocorticoids, the risk of infectious complications is reduced, and growth retardation in children is not as pronounced as with daily use of hormones.

Only in rare cases (for example, with nephrotic syndrome in children) is alternating therapy prescribed from the first days of treatment. Typically, this regimen of hormone administration is reserved for patients whose condition has been stabilized with daily use of glucocorticoids. Below is an example of transferring a patient to alternating therapy, whose initial dose of prednisolone was 50 mg.

When alternating treatment, only corticosteroids of intermediate duration of action (prednisone, prednisolone, methylprednisolone) are used. After taking one dose of these drugs, the hypothalamic-pituitary-adrenal axis is suppressed for 12-36 hours. When prescribing long-acting glucocorticoids (triamcinolone, dexamethasone, betamethasone) every other day, there remains a risk of suppression of the hypothalamic-pituitary-adrenal axis, and therefore it is irrational to use them for alternating treatment. The scope of use of natural hormones (cortisone and hydrocortisone) is currently limited to replacement therapy for adrenal insufficiency and suppressive treatment for adrenogenital syndrome.

If the symptoms of the disease worsen on the second (“hormonal-free”) day, it is recommended to increase the dose of the drug on the first day, or take a small additional dose on the second day.

High doses (for example, 0.6-1.0 mg of prednisolone per 1 kg of body weight per day), or doses divided into several doses throughout the day, are indicated in the early phases of the most aggressive diseases. It is necessary to strive to transfer the patient within 1-2 weeks to a single morning dose of the entire daily dose. Further reduction to the minimum effective maintenance dose (alternating dosage is preferred) is determined by specific clinical circumstances. Too gradual a decrease is combined with an increase in the number and severity of side effects of glucocorticoid treatment, and too rapid a decrease predisposes to exacerbation of the disease.

In order to reduce side effects, the possibility of “steroid sparing” should be considered. In rheumatology, for example, this is achieved through the use of non-steroidal anti-inflammatory drugs or basic therapy (immunosuppressants, antimalarial drugs, etc.). Alternation is another option to reduce complications of steroid therapy.

Therapy with high doses of glucocorticoids may be unsatisfactory due to lack of effectiveness and/or the occurrence of severe complications. In such cases, the possibility of pulse therapy, i.e. intravenous administration of very large doses of hormones over a short period of time, should be considered. Although there is still no clear definition of pulse therapy, this term usually refers to the rapid (within 30-60 minutes) intravenous administration of large doses of glucocorticoids (at least 1 g) once a day for 3 days. In a more general form, pulse therapy can be represented as intravenous administration of methylprednisolone (this is the drug used most often than others) at a dose of up to 1 g/m2. meter of body surface for 1-5 days. Currently, pulse therapy with steroid hormones is often used at the beginning of treatment for a number of rapidly progressive immunologically mediated diseases. The usefulness of this method for long-term maintenance therapy appears to be limited.

In general, topical steroid use produces fewer toxic effects than systemic use. The greatest number of adverse events with systemic use of hormones occurs if the daily dose is divided into several doses. When the daily dose is taken in one dose, the number of adverse effects is fewer and the alternating dosage regimen is least toxic.

When taken daily, synthetic glucocorticoid analogues with long half-lives (eg, dexamethasone) are more likely to cause side effects than drugs with short and intermediate half-lives. Prescribing higher doses of steroids is relatively safe if the duration of their use does not exceed one week; with longer administration of such doses, clinically significant side and toxic effects can be predicted.

The use of natural and non-fluorinated glucocorticoids during pregnancy is generally safe for the fetus. With long-term use of fluoridated drugs, the development of undesirable effects in the fetus, including deformities, is possible. If the woman in labor has been taking glucocorticoids for the previous 1.5-2 years, hydrocortisone hemisuccinate 100 mg is additionally administered every 6 hours to prevent acute adrenal insufficiency.

When breastfeeding, low doses of hormones equivalent to 5 mg of prednisolone do not pose a danger to the baby. Higher doses of drugs can cause growth retardation and suppression of the hypothalamic-pituitary-adrenal axis in the baby. Therefore, women taking moderate and high doses of glucocorticoids are not recommended to breastfeed.

To prevent respiratory distress syndrome in premature infants, long-acting drugs (most often dexamethasone) are used. It is recommended that intramuscular administration of dexamethasone to a woman in labor is up to 34 weeks of pregnancy, 24-48 hours before the expected birth. Repeated administration of the drug is possible if premature birth does not occur within the next 7 days.

Table 3

Scheme of transfer to alternating therapy followed by gradual withdrawal of glucocorticoids

Transfer to alternative therapy		Reducing the dose of glucocorticoids
Day	Prednisolone, mg	Day	Prednisolone, mg	Day	Prednisolone, mg
1	60	11	90	21	85
2	40	12	5	22	5
3	70	13	90	23	80
4	30	14	5	24	5
5	80	15	90	25	80
6	20	16	5	26	5
7	90	17	85	27	80
8	10	18	5	28	5
9	95	19	85	29	80
10	5	20	5	30	0

Patient education

The patient should be aware of the possible clinical consequences of insufficiency of the hypothalamic-pituitary-adrenal axis, which can occur as a result of systemic use of glucocorticoids. The patient should be warned against stopping treatment on their own or quickly reducing the dose of hormones without appropriate medical advice. The response of the hypothalamic-pituitary-adrenal axis to stress may be reduced even after taking glucocorticoids daily for 7 days. If regular oral hormonal treatment is interrupted for more than 24 hours, the patient may develop circulatory collapse in response to physiological stress, trauma, infection, or surgery, which often requires parenteral administration of glucocorticoids to eliminate. It is impossible to reliably predict the occurrence of insufficiency of the hypothalamic-pituitary-adrenal axis either by the dose of hormones, or by the duration of treatment, or by the level of fasting plasma cortisol (although insufficiency more often develops when high doses of glucocorticoids are prescribed).

The patient's attention should be drawn to the fact that hormone treatment stimulates appetite and causes weight gain and the importance of diet should be emphasized before treatment is started. The doctor should describe to the patient the symptoms of diabetes, steroid myopathy, neuropsychiatric, infectious and other complications of glucocorticoid therapy.

Complications of glucocorticoid therapy

Currently, side effects cannot be completely avoided during hormone therapy (Table 4).

Table 4

Interaction with other medications

Some medications can affect the concentration of glucocorticoids in the blood. Thus, phenobarbital and rifampicin intensify the metabolism of hormones in the liver and thereby reduce their therapeutic effect. The combined use of steroids and thiazide diuretics significantly increases the risk of hyperglycemia and hypokalemia. The simultaneous administration of glucocorticoids and acetylsalicylic acid reduces the level of the latter in the blood so much that its concentration is below therapeutic.

Conclusion

Glucocorticoid hormones occupy a worthy place in the medical arsenal. In many cases, timely and adequate use of these drugs saves the lives of patients, allows one to prevent (delay) the onset of disability or mitigate its manifestations. At the same time, in society, including among doctors, the fear of “hormones” is very common. The key to demythologizing glucocorticoids is their rational use in clinical practice.

Literature.

Belousov Yu. B., Omelyanovsky V. V. Clinical pharmacology of respiratory diseases. - M.: Universum Publishing, 1996. - P. 119-130.
Bereznyakov I. G. Glucocorticosteroids: clinical use (manual for doctors). - Kharkov, 1995. - 42 p.
Fundamentals of human physiology (edited by B.I. Tkachenko). - St. Petersburg: International Foundation for the History of Science. - T. 1. - P. 178-183.
Sigidin Ya. A., Guseva N. G., Ivanova M. M. Diffuse diseases of connective tissue. - M.: Medicine, 1994. - 544 p.
Strachunsky L. S., Kozlov S. N. Glucocorticoid drugs. - Smolensk, 1997. - 64 p.
Therapeutic Handbook of the University of Washington (edited by M. Woodley, A. Whelan). - M.: Praktika, 1995. - 832 p.
Boumpas D. T., Chrousos G. P., Wilder R. L., Cupps T. R. Glucocorticoid therapy for immune-mediated diseases: basic and clinical correlates. - Annals of internal medicine. - 1993. - Vol. 119, No. 12. - P. 1198-1208.

Often a person finds the optimal solution to any problem within himself. Where, for example, does the body get the strength to fight disease?

As scientific research conducted in the mid-twentieth century showed, glucocorticoid hormones play an important role in this matter.

They are produced by the adrenal glands for almost all cells of the human body, and it is these hormones that help fight various inflammatory processes.

Synthesized analogues of the hormone are now successfully used in medicine.

Glucocorticosteroids (GCS) - what is it in medicine

Glucocorticoids and glucocorticosteroids are the same thing, synonymous words that denote hormones produced by the adrenal cortex, both natural and synthetic, sometimes the abbreviation GCS is used for brevity.

Together with mineralocorticoids, GCS make up a large group of corticosteroids, but it is GCS that are especially in demand as medications. You can read about what kind of drugs these are - corticosteroids.

They provide the doctor with great opportunities for treating serious diseases, “extinguish” foci of inflammation, can enhance the effect of other medicinal drugs, relieve swelling, and dull the feeling of pain.

By artificially increasing the amount of GCS in the patient’s body, doctors solve problems that previously seemed impossible.

Medical science has also achieved that GKS today can be used “targetedly”- act exclusively on the problem area, without disturbing other healthy ones.

As a result of such local application, the risk of side effects is reduced.

The scope of application of glucocorticoid drugs is quite wide. These tools are used:

In addition, GCS is used in the treatment of injuries ( they have an effective anti-shock effect), and also to restore body functions after complex operations, radiation and chemotherapy.

The regimen for taking GCS takes into account the possible withdrawal syndrome of glucocorticoids, that is, the risk of a deterioration in the patient’s well-being after stopping taking these drugs.

The patient may even develop so-called glucocorticoid deficiency.

To prevent this from happening, Treatment with glucocorticoids is usually completed smoothly, carefully reducing the dose of medication at the end of the treatment course.

All the most important systemic processes take place under the influence of GCS at the cellular, including genetic level.

It means that Only specialists can work with medicinal drugs of this kind, self-medication is strictly prohibited, as it can cause various kinds of complications.

The mechanism of action of glucocorticoids on the body has not yet been fully studied. GCS, as scientists managed to find out, are formed according to the “command” of the pituitary gland: it releases a substance called “corticotropin” into the blood, which already sends its own signal - about how much GCS should be released by the adrenal glands.

One of their main products is an active glucocorticoid called cortisol, also called the “stress hormone.”

Such hormones are produced for various reasons; their analysis helps doctors identify disorders in the endocrine system, serious pathologies and select medications (including corticosteroids) and treatment methods that will be most effective in each specific situation.

Glucocorticoids affect the body in several directions at once. One of the most important is their anti-inflammatory effect.

GCS are able to reduce the activity of enzymes that destroy body tissue, isolating the affected areas from healthy ones.

GCS affect cell membranes, making them rougher, and therefore complicating metabolism; as a result, infections are not given a chance to spread throughout the body, putting it in a “rigid framework.”

Among other ways that GCS influences the human body:

immunoregulatory effect– under different circumstances, immunity increases slightly or, on the contrary, immunity is suppressed (medics use this property of GCS during tissue transplants from donors);
antiallergic;
anti-shock - effective, for example, in anaphylactic shock, when the medication should provide lightning-fast results to save the patient.

GCS can influence the production of insulin (this helps patients with hypoglycemia), accelerate the production of a substance such as erythropoietin in the body (with its participation in the blood, the hemoglobin content increases), can raise blood pressure, and affect protein metabolism.

When prescribing drugs, doctors have to take into account many nuances, including the so-called resorptive effect, when the drug, after absorption, enters the general bloodstream, and from there into the tissues. Many types of GCS allow the use of drugs more locally.

Unfortunately, not all “activities” of glucocorticoids are 100% beneficial to humans.

Excess corticosteroids as a result of long-term use of the drug leads, for example, to changes in internal biochemistry - calcium is washed out, bones become brittle, and osteoporosis develops.

Glucocorticoids are differentiated by how long they work inside the body.

Short-acting drugs remain in the patient’s blood from two hours to half a day (examples - Hydrocortisone, Cyclesonide, Mometasone). You can read the instructions for using Hydrocortisone.

Medium-acting GCS– up to one and a half days (Prednisolone, Methylprednisolone), long-acting – 36-52 hours (Dexamethasone, Beclomethasone).

There is a classification according to the method of drug administration:

Fluorinated glucocorticoids have a particularly powerful effect on the patient’s body. These funds also have their own classification.

Depending on the amount of fluorine they contain, they are monofluorinated, di- and trifluorinated.

The variety of drugs using GCS gives doctors the opportunity to select a drug of the desired form (tablets, cream, gel, ointment, inhaler, patch, nasal drops) and the appropriate “content” in order to obtain exactly those pharmacological effects that are necessary, and in no case do not aggravate the patient’s condition by causing any side effects in the body.

Pharmacology is the domain of specialists; only a doctor understands all the intricacies of what effect a particular drug can have on the body, when and according to what scheme it is used.

As an example, here are the names of glucocorticoid drugs:

Treatment methods

Various types of treatment methods using GCS have been developed:

replacement – used if the adrenal glands cannot independently produce the amount of hormones required by the body;
suppressive – for children with congenital abnormalities in the functioning of the adrenal cortex;
pharmacodynamic(it includes intensive, limiting and long-term treatment) - in antiallergic and anti-inflammatory therapy.

In each case, certain doses of the drug taken and the frequency of their use are prescribed.

Thus, alternating therapy involves taking glucocorticoids once every two days, pulse therapy means the prompt administration of at least 1 g of medication for urgent assistance to the patient.

How dangerous are glucocorticoids for the body? They change his hormonal balance and sometimes cause the most unexpected reactions., especially if for some reason an overdose of the drug occurs.

Diseases provoked by GCS include, for example, hyperfunction of the adrenal cortex.

The fact is that using a drug that helps the adrenal glands perform their intended functions gives them the opportunity to “relax.” If you stop taking the drug abruptly, the adrenal glands can no longer engage in full work.

What other troubles can await after taking GCS?? This:

If the danger is noticed in time, almost all problems that arise can be safely resolved. The main thing is not to aggravate them with self-medication, but act exclusively in accordance with the doctor’s recommendations.

Contraindications

Standards of treatment with glucocorticoids suggest only one absolute contraindication for the use of GCS once - this is the individual intolerance of the drug by the patient.

If long-term treatment is required, the list of contraindications becomes wider.

These are diseases and conditions such as:

pregnancy;
diabetes;
diseases of the gastrointestinal tract, kidneys, liver;
tuberculosis;
syphilis;
mental disorders.

Pediatric glucocorticoid therapy provided only in very rare cases.

Thank you

General information

Glucocorticoids are called steroid hormones secreted by the adrenal cortex, as well as their artificial analogues used in medicine.
The first samples of these drugs date back to the 40s of the twentieth century and the first hormones used were hydrocortisone and cortisone.

In total, five hormones of this group have been studied to date ( presented by the degree of impact on processes in the body in descending order):

Hydrocortisone
Cortisone
Corticosterone
11-deoxycortisol
11-dehydrocorticosterone.

The function of hormone production is regulated by the brain, more precisely by the pituitary gland. The maximum level of these hormones is produced in a person at the age of 30, and subsequently it gradually decreases.

Classification of drugs

All drugs in this group are divided into:

natural ( hydrocortisone and cortisone),
synthetic.

Synthetic ones, in turn, are divided into:

halogenated ( beclomethasone, dexamethasone, fluticasone),
non-halogenated ( prednisolone, budesonide, clobetasol).

Most synthetic drugs are more powerful, so smaller dosages are used. The most promising are fluorinated glucocorticoids, which act effectively, while they practically do not disturb the water-salt balance and provoke fewer side effects.

According to the duration of exposure, all drugs can be divided into:

short acting ( cortisone, hydrocortisone),
medium duration action ( prednisolone, methylprednisolone),
long-acting ( dexamethasone, betamethasone, triamcinolone).

Action

Scientists have not yet fully figured out the mechanism of action of these hormones on the body. Entering the cell through the cell membrane, the hormone acts on receptors sensitive to steroid substances, is sent along with the receptor to the cell nucleus and participates in the production of special protein components involved in the inflammatory process.

Hormones influence the following processes occurring in the body:

Indications

Adrenal insufficiency of any origin,
Shock therapy,
Rheumatism,
Acute lymphoblastic and myeloblastic leukemia,
Infectious mononucleosis ,
Asthmatic status,
Allergies complicated by collagenosis, dermatoses, asthma,
Inflammations of various localizations,
Hemolytic anemia,
Acute pancreatitis,
Viral hepatitis,
Organ and tissue transplantation,
Autoimmune diseases.

The dosage regimen is prescribed by the attending physician. It should be borne in mind that in most cases, drugs significantly alleviate the patient’s condition, but do not in any way affect the cause of the disease.

Contraindications

Absolute:

Fungal diseases
Viral infections,
Individual intolerance.

Relative:

Relative contraindications are taken into account in cases where long-term treatment is involved.
If we are talking about urgently saving the patient’s life, the drugs are used in any case.

More information about essential drugs

Cortisone
Used for replacement therapy in patients with adrenal insufficiency. Produced in tablets. Used only when the liver is functioning normally. Affects the exchange of water and salts.

Hydrocortisone
Prescribed for adrenal insufficiency. Not recommended for edema, cardiac dysfunction, hypertension, as it contributes to sodium retention in the body and potassium excretion. Produced in the form of liquid for injection, suspension.

Prednisolone
Quite a frequently prescribed drug. It is produced in the form of tablets, liquid and suspension for injection, powder in ampoules.

Methylprednisolone
Stronger than prednisolone, it causes fewer side effects and is more expensive. Indicated for patients suffering from obesity, stomach ulcers, and mental illness. Available in the form of tablets, suspensions, dry substances in bottles.

Dexamethasone
This is one of the most powerful drugs in this group. Since the drug has many side effects, it is not used in long courses. Prescribed, among other things, to alleviate the patient’s condition during chemotherapy, as well as to prevent breathing problems in premature infants. Available in the form of tablets and liquid for injection in ampoules.

Betamethasone
It is similar in power to dexamethasone and has fewer side effects. Most often used in the form of liquid for injection, including intra-articular and periarticular. The duration of action of such injections can reach a month due to the special chemical composition of the drug.
Produced in the form of tablets, liquid in ampoules, suspensions.

Inhalation medications

Beclomethasone– the drug is used in the treatment of bronchial asthma, relieves inflammation and relieves allergies. When used as inhalation, it is practically not absorbed into the blood and does not act systemically.

Contraindications:

acute bronchospasm,
intolerance,
status asthmaticus,
bacterial bronchitis.

The drug may cause some side effects, including bronchospasm and sore throat.

Budesonide– the main therapy for bronchial asthma, chronic obstructive pulmonary disease.
Contraindications: individual intolerance. Liquid for inhalation is prohibited for use in the treatment of children under 16 years of age, suspension is prohibited for use in the treatment of children under 3 months of age, and powder for children under 6 years of age.

pregnancy, breastfeeding, fungal, viral and bacterial diseases of the respiratory system, tuberculosis.

The drug can provoke a coughing attack, drying of the oral mucosa, migraine-like pain, stomatitis, nausea, and hyperactivity.
The drug should not come into contact with the eyes.

Fluticasone– the drug is prescribed for bronchial asthma and chronic obstructive pulmonary disease as the main treatment.
Contraindications:

non-asthmatic bronchitis,
intolerance,
acute bronchospasm,
asthmatic status.

Relative contraindications:

osteoporosis,
common infections,
lactation,
pregnancy.

The drug is used only in the form of inhalation. It can provoke candidiasis of the oral mucosa, changes in voice timbre, and bronchospasm. If used for a long time in large quantities, it causes systemic side effects. To prevent oral candidiasis, rinse your mouth after inhalation.
This drug is not used to relieve asthma attacks.

Preparations for systemic use

Drugs have been created for systemic use prednisone, cortisone.
There are quite a lot of drugs that are used both locally and systemically. These include: betamethasone, dexamethasone, triamcinolone, fludrocortisone, mazipredone, methylprednisolone, prednisolone.
Such drugs are used both in the form of tablets for oral use and in injections.

Ointments, creams, lotions

Glucocorticoids for external use are available in the form of ointments, gels, creams, and lotions. Prescribed for certain dermatological diseases of a non-infectious nature.

Indications:

contact dermatitis,
seborrheic dermatitis,
lichen planus,
erythroderma,
discoid lupus erythematosus.

These remedies relieve inflammation, itching, allergic reactions, redness and swelling of tissues.

How to choose the right dosage form of the drug?
Ointments They begin to act more slowly and their consistency is greasy. They are prescribed for dry skin prone to flaking and weeping processes.

Creams may cause irritation or dryness if there are wounds on the skin. They are prescribed for intertriginous phenomena. This form does not leave greasy stains and is quickly absorbed.

Lotions indicated for wet conditions, very convenient for treating the scalp.

All glucocorticosteroids used in dermatology are divided into four groups according to the power of their effect:

Very powerful: chalcinonide, clobetasol propionate.
Powerful: budesonide, dexamethasone, flumethasone, triaminolone.
Medium strength: prednisolone.
Weak: hydrocortisone.

It should be borne in mind that drugs of medium strength and weak ones have a less pronounced effect, and the number of side effects is higher than that of more powerful drugs.

Side effects

Glucocorticosteroid drugs really very quickly relieve many unwanted symptoms of diseases. However, they cause quite a lot of side effects. Therefore, they are prescribed only in cases where no others are able to help.
Particularly many side effects are observed with the systemic use of these drugs. Several new methods have been developed for using these drugs, which slightly reduce the likelihood of unwanted effects. But treatment with these drugs in any case requires constant monitoring of the patient’s general health.

When using steroid hormonal drugs, the following side effects are likely to develop:

From the motion apparatus side: osteoporosis, compression

Receptors for steroids are located in the cytoplasm of cells. However, their density in different cells is not the same: from 10 to 100 steroid-sensitive receptors, which may cause different sensitivity tissues to GCS. In addition, GCS may have different tropism to GKR. Quantity glucocorticosteroid receptors (GCR) can vary significantly and change during GCS therapy.

Recent studies have shown that the effect of glucocorticosteroid hormones on the biosynthesis of messenger RNA (mRNA) is the main step in the implementation of the biological effects of GCS in the cells of target organs.

GCS can have both a specific stimulating effect and an inhibitory effect on the synthesis of various RNAs. Multidirectional effects can manifest themselves in the same organ and, perhaps, the final response of the cell to a hormonal signal depends on their ratio. GCS also affect the activity of RNA polymerase.

Pharmacodynamic effects of glucocorticosteroids

1. The anti-inflammatory effect of GCS manifests itself in the form of antiexudative and stabilization of cellular and subcellular membranes (mitochondria and lysosomes);

decreased permeability of the vascular wall, in particular capillaries;

vasoconstriction at the site of inflammation;

reducing the release of biologically active amines (histamine, serotonin, kinins and prostaglandins) from mast cells;

reduction in the intensity of energy formation processes in the focus of inflammation;

inhibition of migration of neutrophils and macrophages to the site of inflammation, disruption of their functional activity (chemotactic and phagocytic), peripheral leukocytosis;

suppression of monocyte migration, slowing down the release of mature monocytes from the bone marrow and reducing their functional activity;

inducing the synthesis of lipomodulin, which blocks phospholipase A of cell membranes, disrupts the release of phospholipid-bound arachidonic acid and the formation of pro-inflammatory prostaglandins, leukotrienes and thromboxane A2;

inhibition of the formation of leukotrienes (leukotriene B4 reduces the chemotaxis of leukocytes, and leukotrienes C4 and D4 (slowly reacting substance) reduce the contractile ability of smooth muscles, vascular permeability and mucus secretion in the airways);

suppression of the synthesis of some pro-inflammatory cytokines and blockade of the synthesis of cytokine receptor proteins in tissues.

antiproliferative effects. suppression of nucleic acid synthesis;

impaired differentiation of fibrocytes from fibroblasts;

decrease in the functional activity of fibrocytes

2. Immunosuppressive effect: a decrease in the number of lymphocytes in the peripheral blood (lymphopenia), due to the transition of circulating lymphocytes (mainly T cells) into lymphoid tissue, possibly accumulating them in the bone marrow;

increased apoptosis of immature or activated T- and B-lymphocytes;

suppression of T cell proliferation;

decreased function of T-helpers, T-suppressors, cytotoxic T-lymphocytes;

inhibition of the activity of the complement system;

inhibition of the formation of fixed immune complexes;

decrease in the level of immunoglobulins (high doses of glucocorticoids);

inhibition of delayed type hypersensitivity reactions (type IV allergic reactions), in particular the tuberculin test;

violation of cooperation between T - and B - lymphocytes;

disruption of the synthesis of immunoglobulins and antibodies, including autoantibodies;

decrease in the number of monocytes in the vascular bed.