What is the difference between prednisolone and prednisolone. Detailed instructions for the use of prednisolone

The hormonal medical drug Prednisolone has a pronounced anti-inflammatory effect. Belongs to the category of drugs of medium duration of exposure. A good therapeutic effect of the drug is due to its ability to inhibit the activity of leukocytes and macrophages, and also prevent their movement to the inflamed area in the body.

In addition, Prednisolone does not allow the immune system to absorb cells and accentuate interleukin. The impact on metabolic processes in adipose tissues does not allow cells to capture glucose and stimulates the breakdown of fats. However, due to its increased amount in the body, increased production of insulin occurs, which leads to the accumulation of fat.

The difference between Prednisolone and Dexamethasone is that it changes the water-salt balance more strongly: it removes potassium and calcium, but contributes to the retention of fluids and sodium. The antiallergic effect of a more powerful analogue of natural hydrocortisone (4 times more powerful) is due to the ability to minimize the number of basophils and reduce the production of biologically active components.

Dexamethasone

Dexamethasone acts in much the same way, but the biomechanism of its action is slightly different. It is a long-acting drug, so it is not prescribed in long-term regimens. This analogue of Prednisolone provokes an increase in the volume of triglycerides, fatty acids and cholesterol in the blood. In addition, this medicine can cause hyperglycemia.

The drug practically does not change the water-salt balance and does not affect the amount of electrolytes. Dexamethasone is considered ten times superior to natural cortisone. Inflammatory processes in the body are localized by acting on eosinophils and mast cells, and also increases the stability of membranes.

Similarity of drugs

It is often difficult to immediately say that Dexamethasone or Prednisolone is better, since both of these drugs belong to the same category of drugs - glucocorticosteroids, i.e. natural substances produced by the adrenal cortex.

They have a number of similar characteristics:

Unlike natural hormones, both Dexamethasone and Prednisolone are more active at lower doses;
They have an equally good anti-inflammatory effect on the body;
Well relieve allergic manifestations due to the ability to release histamine from mast cells;
Have an antitoxic effect;
The immunosuppressive properties of both drugs are equally effective in reducing disturbances in the body's immune system;
Used in anti-shock therapy, as they greatly increase blood pressure;
They are used for the same indications.

Dexamethasone and Prednisolone are widely used both in emergency care and in the fight against systemic diseases.

What is the difference between Dexamethasone and Prednisolone

Despite the fact that these drugs belong to the same drug, they have differences:

Duration of action. The activity of Prednisolone in the body is approximately hours, while Dexamethasone can act up to hours;
Impact power. Prednisolone is much weaker than its analogue;
The difference between Dexamethasone and Prednisolone also lies in the mechanism of action, therefore, different processes occur in the body, often bringing a negative result in certain situations;
They affect the water-salt balance in the body in different ways.

With long-term treatment regimens, as well as during pregnancy, it is more advisable to replace Dexamethasone with Prednisolone, since this will reduce the risk of side effects. Therefore, it is impossible to assume that these drugs are full-fledged analogues of each other.

Which drug is better

When choosing which is better Dexamethasone or Prednisolone, you must follow the doctor's recommendations. This is due to the fact that each of these drugs has a different dosage of the main substance. It is known that various preparations, which include natural hormones, act on the body in different ways. So, for example, hydrocortisone is 4 times weaker, and metipred or triamcinolone is 20% stronger than Prednisolone. At the same time, Prednisolone is 7 times weaker than Dexamethasone and 10 times weaker than Betamethasone.

When choosing one or another hormonal remedy, the doctor will definitely take into account the degree of the disease and the general physical condition of the patient. Of course, for each specific case, the doctor will choose the appropriate medicine, but he will never recommend taking Prednisolone along with Dexamethasone.

When is this group of drugs used?

Preparations made on the basis of the hormone of the adrenal cortex are used in therapy:

replacement (necessary when reducing your own glucocorticosteroids in the body);
suppressive (needed to stop the production of other hormones);
pharmacodynamic (symptomatic effect).

In the treatment of certain diseases, doctors prefer Prednisolone or try to replace Dexamethasone with an analogue in cases of injuries and changes in blood vessels and tissues, with fevers of various etiologies, certain types of anemia, infectious mononucleosis, exacerbation of pancreatitis, or shock conditions.

An analogue of Prednisolone - Dexamethasone is used for manifestations of severe inflammatory conditions, sepsis, peritonitis, anaphylactic shock, asthma or multiple sclerosis.

Application methods

The dose of the drug (Prednisolone or Dexamethasone) can only be selected by a specialist. We must not forget that glucocorticosteroid drugs are powerful drugs that can cause serious harm to the body.

These medications should be taken under medical supervision. The daily dosage of Prednisolone during acute conditions is usually mg, and this rate is divided into several doses within 24 hours. As the condition stabilizes, the amount of the drug is gradually reduced to 5-10 mg per day. In exceptional cases, a one-time increase in Prednisolone domg is allowed. In such situations, the drug is administered intravenously. The maximum dose for a child is 1 mg per kilogram of body weight.

Sometimes it is more expedient to use an analogue of Prednisolone - Dexamethasone. In critical situations, you can also use a large amount of the drug, but then the dosage is gradually reduced.

In the process of prolonged use of glucocorticosteroid drugs, it is necessary to carefully monitor the water-salt balance in the body and the level of glucose in the blood. To exclude the occurrence of hypokalemia, along with taking Prednisolone, Dexamethasone or their analogues, potassium preparations are usually prescribed.

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Choice of glucocorticoid drug - Glucocorticoid therapy in clinical practice

We do not have convincing evidence that any of the currently used glucocorticoid drugs has a more specific effect on the pathological processes that develop in rheumatic and other diseases.

The severity of the immunosuppressive effect of various glucocorticoids does not always correlate with the anti-inflammatory effect. The most powerful immunosuppressive effect in vitro is demonstrated by methylprednisolone (Medrol®) and betamethasone, the intermediate effect is dexamethasone, prednisolone, hydrocortisone, and the smallest is prednisone.

Some features of the mechanism of action, pharmacokinetics and frequency of side effects allow us to recommend a certain differential approach to the choice of the drug and the nature of its administration. Thus, hydrocortisone should be avoided in severe kidney and heart disease because of its potential for sodium and water retention. The introduction of synthetic fluorine glucocorticoids (triamcinolone, dexamethasone, betamethasone) into the molecule caused not only an increase in anti-inflammatory activity, but also a deterioration in their tolerance due to a number of side effects. The most common side effects of triamcinolone are amyotrophy, cushingoid and mental disorders, but it has the least appetite.

stimulating effect. Dexamethasone has the greatest appetite-stimulating effect. Dexamethasone and betamethasone, to a greater extent than other glucocorticoids, contribute to an increase in body weight, an increase in blood pressure, the development of osteoporosis, peptic ulcers and skin complications (ecchymosis, striae, acne, hirsutism). Dexamethasone has a more pronounced inhibitory effect on the function of neutrophilic granulocytes, and therefore its use is hardly acceptable in patients with an increased risk of developing ingercurrent infections. In general, among the used glucocorticoids, methylprednisolone (Medrol®) has the best tolerance, which is clearly shown in Table 4.

Table 4. The total number of side effects of various

The amount of side effects

The sum of side effects when using methylprednisolone was 8, being significantly lower than that of other glucocorticoids. When using Medrol®, the frequency and severity of such side effects as pituitary suppression, loss of K +, Na + retention, development of arterial hypertension, diabetogenic effect, stimulation of appetite, weight gain, effects on the psyche, the development of cushingoid, osteoporosis and muscle atrophy in general were lower than those of other glucocorticoids, as shown in Table 5. In this regard, Medrol® is the drug of choice for patients with unstable mentality, arterial hypertension, overweight, insulin resistance, with a risk of developing ulcerative lesions of the gastrointestinal tract and sugar diabetes.

In 1976 E.S. Cathcart et al. reported the positive effect of intravenous infusions of ultra-high doses of methylperdnisolone (Solu-Medrol®), designated as "pulse therapy", in 7 patients with lupus glomerulonephritis, occurring with a rapid deterioration in renal function. Subsequently, quite a few reports appeared on the use of this method of treatment in patients with high activity and involvement in the pathological process of vital organs and systems in many rheumatic diseases, vasculitis, primary and secondary glomerulonephritis.

Table 5. Comparative evaluation of the activity and side effects of glucocorticoids

Weight gain

Impact on the gastrointestinal tract

Impact on the psyche

"Pulse therapy" with methylprednisolone (Solu-Medrol®) involves intravenous drip injection of about 1.0 g (10-30 mg/kg body weight) of the drug per day for 2-3 days. Such courses are held 1-2 times a month and, depending on the clinical situation, can last for 6 months or more.

The introduction of ultra-high doses of methylprednisolone to healthy people causes severe lymphocytopenia in combination with neutrophilia, which lasts for 1-2 days. Leukocytopenia is due primarily to a decrease in recirculating T cells. In addition, a significant suppression of the response of peripheral lymphocytes to stimulation with various mitogens is observed within hours. With “pulse therapy” with methylprednisolone, a pronounced and prolonged depression of NK cells is observed. Under the influence of ultra-high doses of methylprednisolone, the adhesive abilities of polymorphonuclear leukocytes and their other functions are significantly impaired (short-term - up to 24 hours), the generation of free radicals and degranulation change insignificantly. In addition, there is a slowdown in the secretion of lactoferrin by polymorphonuclear leukocytes, as well as a violation of the destruction and digestion of bacteria. The latter may contribute to an increased risk of developing intercurrent infections in patients receiving "pulse therapy" with methylprednisolone.

In many reports on uncontrolled studies of the effectiveness of "pulse therapy" with methylprednisolone in acute severe clinical manifestations of rheumatic diseases and vasculitis, there is a favorable dynamics of the clinical picture under the influence of such a treatment regimen. Along with this, there is also a normalization or a clear positive dynamics of laboratory (including serological) parameters.

In a few controlled studies that included a small number of patients, there were no particular advantages (or the advantage was short-lived) compared with traditional oral glucocorticoid therapy.

Excessive optimism, observed at the initial stages of the use of "pulse therapy" with methylprednisolone, today has given way to a sober assessment of the possibilities of the considered variant of glucocorticoid therapy and indications for its use. The use of “pulse therapy” with methyltoelnisolone is clearly justified in

various diseases and pathological conditions, where glucocorticoid therapy is indicated for the rapid elimination (or reduction) of life-threatening manifestations.

Unreasonable prescription of "pulse therapy", violation of the method of its application (excessively rapid administration of the drug), as well as the lack of adequate monitoring of the patient during the administration of the drug and after the procedure, can cause quite serious complications, including: arrhythmias, cardiac arrest, severe intercurrent infections and more.

In connection with the foregoing, it is necessary to conduct large controlled studies to evaluate both the immediate and long-term results of "pulse therapy" with methylpredizolone in diseases with different course activity and involvement of various organs in the pathological process and varying severity of their damage.

Along with oral and intravenous use of glucocorticoids, pharmacological forms of glucocorticoids intended for intramuscular administration to achieve prolonged anti-inflammatory, immunosuppressive and antiallergic effects occupy an important place in clinical practice. Moreover, these forms of glucocorticoids make it possible to achieve a systemic effect, and are also used in situ, primarily intra-articularly, for the purpose of a local (local) effect.

One of the representatives of this form of glucocorticoids is Depomedrol®, the active ingredient of which is methylprednisolone acetate (40 mg in 1 ml of suspension). The latter has the same pharmacological properties and clinical effects as methylprednisolone (Medrol®), but it dissolves worse and is less actively metabolized, which is the reason for its longer clinical effect.

Depo-Medrol® undergoes hydrolysis under the influence of serum cholinesterases with the formation of active metabolites. About 40-90% of methylprednisolone binds to albumin and transcortin.

The duration of the anti-inflammatory activity of glucocorticoids is associated with the duration of their inhibition of the hypothalamic-pituitary-adrenal axis. After a single intramuscular injection of Depomedrol® (40 mg / ml), its maximum concentration in the blood is reached after 7-8 hours, and the duration of inhibition of the hypothalamic-pituitary-adrenal axis is 4-8 days.

The dosage of Depo-Medrol®, administered intramuscularly once a week, is determined by the characteristics of the disease. At the same time, the necessary

the weekly dosage, when compared with the required oral dose, should be the daily value of the latter multiplied by 7.

Intramuscular and intraarticular administration of glucocorticoids is considered as adjuvant therapy and is usually (with the exception of gout, bursitis, tendinitis) performed against the background of basic (disease-modifying) therapy. Table 6 below shows the indications for intra-articular use of glucocorticoids.

Table 6. Indications for intra-articular use of glucocorticoids

Rheumatoid arthritis
Osteoarthritis
Gout and pseudogout
SLE and other systemic connective tissue diseases
Ankylosing spondylitis
Reiter's disease
Arthritis in patients with psoriasis
Tietz syndrome
Acute traumatic arthritis

For intramuscular and intraarticular use, preparations of various glucocorticoids are used, which are presented in table 7.

Table 7. Glucocorticoids for intramuscular and intraarticular administration and their prednisolone equivalents

Dexamethasone sodium phosphate 4 mg/ml (Dexadron®)

Hydrocortisone acetate 25 mg/ml (Hydrocorton®)

Methylprednisolone acetate 20.40, 80 mg/ml (Depo-medrol®)

Prednisolone tebutate 20 mg/ml

Triamcinolone acetonide 10 and 40 mg / ml (Kenalog® - 10 and Kenalog® - 40)

Note: one equivalent is equal to 5 mg of prednisone

Depo-medrol® dosages used in rheumatoid arthritis and osteoarthritis (in the presence of synovitis) are determined by the size

tt/%"%l"

large joints (knee, ankle, shoulder) is mg; in the middle joints (elbow, wrist) mg; and in small (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular) mg.

honey problem

Dexamethasone is 7 times more glucocorticoid than prednisolone. The difference in drugs is also that Prednisone is considered a more proven drug. Just like triamcinolone, it is a fluorinated drug.

25 and 50 mg (cortisone acetate). In acute adrenal insufficiency and other emergency conditions, the drug of choice is hydrocortisone hemisuccinate. According to glucocorticoid activity, it is 4 times stronger than hydrocortisone, and inferior to it in mineralocorticoid activity. Refers to glucocorticoids with an average duration of action.

"Prednisone" and "Prednisolone": differences

It is activated in the liver by hydroxylation and conversion to prednisolone. It has a stronger (20%) and longer glucocorticoid effect than prednisolone. Medicines may differ in composition, mechanism of action, cost and have different characteristics. The differences and instructions for their use will be presented to your attention. The annotation states that the active substance of the drug is the compound of the same name: prednisolone.

Indications and contraindications

The composition of the drug "Prednisolone" is 5 mg of the active compound. It would seem that since the same substance is present in the composition of medicines, then their purpose should be the same. Prednisolone tablets are prescribed for endocrine disorders, adrenal pathologies, severe allergies, rheumatic diseases, hematological diseases and liver malfunctions.

Prednisone is not used for viral and fungal diseases, hypertension, during the period of vaccination, exacerbation of stomach ulcers, during mental illness. There are different reviews about the drugs "Prednisone" and "Prednisolone", including negative ones. That is why before using the product, it is necessary to read the instructions and pay attention to contraindications. If you have hypersensitivity to the components, then those and other tablets will provoke an allergy.

About the drugs "Prednisolone" and "Prednisone" reviews of doctors report that the medicines are quite effective in their use. Medicines also to some extent eliminate intoxication, enhance the effect of other drugs used to treat diseases of the spine. But its plus and another difference is the form of release. If you have to take Prednisolone tablets 10 or more pieces per day, then a similar medication can be used in a smaller amount, which is very convenient.

Composition and cost: two main differences

It would seem that they are identical and do not differ in anything. In order for the effect of the treatment to be expected, follow the doctor's recommendations and purchase only the medicines prescribed for you. The cells of the fascicular zone of the adrenal cortex under physiological conditions secrete two main glucocorticoids into the blood - cortisone and cortisol (hydrocortisone). An increase in the level of cortisol in the blood by a feedback mechanism inhibits the secretion of corticoliberin in the hypothalamus and corticotropin in the pituitary gland.

As a result, the breakdown of protein in the body increases and the excretion of nitrogenous products increases. Protein breakdown occurs in muscle, connective and bone tissues. Glucocorticoids stimulate the catabolism of triglycerides and inhibit the synthesis of fat from carbohydrates. At the same time, a decrease in the adipose tissue of the extremities is often combined with an increase in the deposition of fat on the abdominal wall and between the shoulder blades.

Application features

In clinical practice, natural glucocorticoids (cortisone and hydrocortisone) and their semi-synthetic derivatives are used. The latter, in turn, are divided into non-fluorinated (prednisone, prednisolone, methylprednisolone) and fluorinated (triamcinolone, dexamethasone and betamethasone). Natural glucocorticoids have mineralocorticoid activity, although weaker than true mineralocorticoids.

A feature of fluorinated drugs is a slower metabolism in the body, which leads to an increase in the duration of the drug action. Values close to those given are also obtained when calculating the daily dose of corticosteroids per 1 kg of the patient's body weight. The dose of glucocorticoids prescribed at the beginning of the treatment of a particular disease depends mainly on the nosological form and severity of the disease.

According to the persistence and severity of the therapeutic anti-inflammatory effect, as well as tolerability, prednisolone and methylprednisolone are the best. Compared to prednisolone, methylprednisolone has a slightly higher glucocorticoid activity (by 20%) and has a weak mineralocorticoid effect.

It is a fluorinated glucocorticoid and does not have a mineralocorticoid effect. For example, dexamethasone has a potent anti-inflammatory effect and relatively low immunosuppressive activity. Just like prednisolone, it is mainly used for pharmacodynamic therapy. In today's article we will talk about the drugs "Prednisone" and "Prednisolone". Synthetic glucocorticoid, most often used in clinical practice for pharmacodynamic therapy and is considered as a standard drug.

HYDROCORTISONE is the only glucocorticoid that meets all the requirements that apply to drugs used for chronic chronic renal failure replacement therapy. Hydrocortisone is 4 times weaker than prednisolone in glucocorticoid activity, but surpasses it in the severity of mineralocorticoid action. In CNN, as well as in acute adrenal insufficiency and other emergency conditions, hydrocortisone preparations are the drugs of choice.

Currently, the only hydrocortisone drug registered in Russia for per os use is CORTEF (PHARMACIA & UPJON), which is available in tablets of 5, 10 and 20 mg (Table 7).

For parenteral administration, SOLU-CORTEF (PHARMACIA & UPJON) is used - a dry substance for injection in a vial containing 100 mg of sodium hydrocortisone succinate with a solvent of 2 ml in an ampoule; SOPOLCORT N (ELFA) - solution for injection 1 ml in an ampoule containing hydrocortisone hemisuccinate 25 mg and 50 mg; HYDROCORTISONE (GEDEON RICHTER) - suspension for injection, 5 ml in a vial containing 125 mg of microcrystalline hydrocortisone acetate (only for deep intramuscular injections); HYDROCORTISONE (HEMOFARM) is a lyophilized powder for injection in a vial containing 500 mg of hydrocortisone acetate, complete with a solvent in ampoules.

Dose equivalence of glucocorticoid drugs

Equivalent dosage (mg)

Average duration of action

Comparative characteristics of gluco- and mineralocorticoids

Biological half-life, min

Protein binding, %

Cortisone, like hydrocortisone, has a pronounced mineralocorticoid activity, but is inferior to hydrocortisone in both gluco- and mineralocorticoid activity. It is used in patients with chronic renal failure only with normal liver function, since cortisone is converted to hydrocortisone in the liver and in case of severe damage to this organ, the use of the drug is not recommended.

In clinical practice, CORTISONE ACETATE (AKRIKHIN) is used, produced in tablets of 25 mg.

PREDNISOLONE is widely used for HNN replacement therapy. Currently, it is believed that prednisolone is less preferable for chronic chronic renal failure replacement therapy, since, like all synthetic drugs, it differs from hydrocortisone in the intensity of binding to proteins, receptors, and the ratio of various biological effects. The ratio of glucocorticoid and mineralocorticoid activity of prednisolone is 300:1.

PREDNISOLONE (DECORTIN, MEDOPRED) for HNN replacement therapy is available in 5 mg tablets. PREDNISOLONE for injection (GEDEON RICHTER) - solution for injection, 1 ml of which contains 30 mg mazipredone hydrochloride; SOLU-DECORTIN N (MERCK) - powder for the preparation of an injection solution in ampoules containing prednisolone (in the form of sodium hemisuccinate) 10.25, 50 and 250 mg, complete with a solvent; PREDNISOLONE (SANAVITA) - suspension for injection in 1 ml ampoules containing prednisolone acetate 25 mg; PREDNISOLONE HAFSLUND NIKOMED (NYCOMED AUSTRIA) - solution for injection, 1 ml containing 25 mg of prednisolone; PREDNISOLONE ACETATE (ASTRAPIN) - suspension for injection, in 1 ml of prednisolone acetate 25 mg.

Methylprednisolone compared with prednisolone has a slightly higher glucocorticoid activity (by 20%) and has a weak mineralocorticoid effect. The advantage of the drug is a very moderate stimulation of the psyche and appetite, which justifies its appointment to patients with an unstable psyche and overweight. MEDROL (PHARMACIA&UPJON), METIPRED (ORION PHARMA INTERNATIONAL) - methylprednisolone 4 mg per tablet; SOLU-MEDROL (PHARMACIA & UPJON) - methylprednisolone sodium succinate 40 mg in 1 ml, 125 mg in 2 ml and vials containing 250,500 and 1000 mg, METIPRED dry substance for injection - 4 ml ampoules containing methylprednisolone sodium succinate 250 mg; METIPRED depot injection - 2 ml in an ampoule containing methylprednisolone acetate 80 mg (is a drug for parenteral administration of long-acting slow absorption - after intramuscular administration of 80 mg of the drug, its effect lasts for 12 hours after injection, and systemic effects are observed within 17 days); DEPO-MEDROL (PHARMACIA&UPJON) - 40 mg of methylprednisolone in 1 ml.

DEXAMETHASONE in glucocorticoid activity is 7 times superior to prednisolone. It is a fluorinated glucocorticoid and does not have a mineralocorticoid effect. Compared to other drugs, it inhibits the function of the pituitary gland 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, psychostimulant action). DEXAMETHASONE (DEXAZONE, DEXAMED) is available in tablets of 0.5 mg; DEXAMETHASONE solution for injection containing 4 mg of dexamethasone phosphate.

Question #13 - Prednisolone or Hydrocortisone

The doctor prescribed a choice of prednisolone or hydrocortisone, which is better to use for allergies?

Answer from our expert

Both substances (both prednisolone and hydrocortisone) belong to the group of glucocorticoids - stress hormones synthesized by the adrenal cortex. Preparations based on them have a powerful anti-inflammatory effect.

The therapeutic properties of prednisolone and hydrocortisone in allergic reactions are due to the ability to have an immunosuppressive effect. That is, when they enter the body, they block the reaction of immune cells to a substance alien from their point of view.

Hydrocortisone is a natural analogue of the steroid hormone produced in the human body. It is produced under the control of the pituitary gland and the central nervous system. The pituitary gland synthesizes corticotropin, which has a stimulating effect on the adrenal cortex.

Long-term use of hydrocortisone leads to inhibition and atrophy of the adrenal cortex. At the same time, the production of corticotropin and thyrotropin, which is a stimulant of the thyroid gland, is significantly reduced.

Prednisolone is a synthetic substance belonging to the group of glucocorticoids. It has more activity than the natural analogue of cortisol. Although the action of synthetic and natural hormones is similar, it is more pronounced.

It has been proven that a synthetic analogue of cortisol is 30 times more effective than natural. When applied topically, prednisolone is poorly absorbed into the blood, which means that it has a slight side effect on the internal organs.

Despite the temptation associated with the naturalness of hydrocortisone, the use of its synthetic analogues is considered the most preferable. They are more efficient and last longer. At the same time, synthetic hormonal preparations practically do not affect the metabolic processes in the body.

Video: Doping without cuts Prednisolone

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Glucocorticoids are a double-edged sword

General information

The first samples of these drugs date back to the 40s of the twentieth century and the first hormones used were hydrocortisone and cortisone.

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, subsequently it gradually decreases.

Classification of drugs

Synthetic, in turn, are divided into:

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

Synthetic preparations for the most part act more strongly, therefore, 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.

short action ( cortisone, hydrocortisone),
actions of medium duration ( prednisolone, methylprednisolone),
long term ( dexamethasone, betamethasone, triamcinolone).

Action

The exchange of carbohydrates. The processing of sugar in the body worsens, sometimes taking drugs causes diabetes.
Protein exchange. Suppresses protein production in bones, muscles and skin. Therefore, the patient taking these drugs loses weight, he has stretch marks on the skin, hemorrhages, cuts and scratches are poorly scarred, muscles atrophy. Osteoporosis often develops.
lipid metabolism. There is an increase in the amount of subcutaneous fatty tissue in the face, neck, chest and a decrease in volume in the arms and legs.
calcium exchange. Hormones of this class inhibit the absorption of calcium by the intestines and accelerate its leaching from the bones. Therefore, there is a possibility of developing a lack of calcium.
The work of the heart and blood vessels. Under the influence of these hormones, the permeability of small blood vessels worsens. Hormones tone blood vessels and the contractility of the heart muscle.
Inflammatory process. Any inflammatory manifestations are suppressed, since glucocorticoids reduce the permeability of cell membranes for certain substances involved in the inflammatory process. In addition, the walls of blood vessels are strengthened, which inhibits the movement of immune cells in the focus.
regulation of the immune system. These hormones suppress the local immune response, so they are used in tissue transplantation. They suppress the activity of certain immune bodies ( lymphocytes and "anti-inflammatory" cytokines) involved in the development of diseases such as meningitis and rheumatism.
Blood formation. Under the influence of these hormones, the production of lymphocytes, eosinophils, monocytes simultaneously decreases and the production of red blood cells and platelets increases. Even a single dose of the drug for a day changes the blood picture. If the treatment was long, it takes from 7 to 30 days to restore the normal picture.
The work of the endocrine glands. The connection between the hypothalamus, pituitary gland and adrenal glands is suppressed. This violation becomes noticeable with long courses of taking drugs. The production of sex hormones also decreases, which leads to the development of osteoporosis.

Indications

Adrenal insufficiency of any origin,
Shock therapy,
Rheumatism,
Rheumatoid arthritis,
Acute lymphoblastic and myeloid leukemia,
Infectious mononucleosis,
status asthmaticus,
Allergy complicated by collagenoses, dermatoses, asthma,
Inflammations of different localization,
hemolytic anemia,
acute pancreatitis,
viral hepatitis,
Glomerulonephritis,
Transplantation of organs and tissues,
Autoimmune diseases.

The regimen is prescribed by the attending physician. It should be borne in mind that in most cases, drugs greatly alleviate the patient's condition, but in no way affect the cause of the disease.

Contraindications

Relative contraindications are taken into account when it comes to long-term treatment.

If we are talking about urgently saving the patient's life, drugs are used in any case.

More about the main drugs

It is used in replacement therapy in patients with adrenal insufficiency. Produced in tablets. It is used only during normal liver function. Affects the exchange of water and salts.

It is prescribed for adrenal insufficiency. It is not recommended for edema, heart failure, hypertension, as it contributes to sodium retention in the body and potassium excretion. Produced in the form of liquid for injection, suspension.

A fairly commonly prescribed drug. Produced in the form of tablets, liquids and suspensions for injection, powder in ampoules.

Stronger than prednisolone, less side effects, more expensive. Indicated for patients suffering from obesity, stomach ulcers, mental illness. Produced in the form of tablets, suspensions, dry substance in vials.

This is one of the most powerful drugs in this group. Since the drug has many side effects, it is not used for long courses. It is prescribed, among other things, to alleviate the patient's condition during chemotherapy, as well as to prevent respiratory failure in premature babies. Available in the form of tablets and liquid for injection in ampoules.

It is similar in power to dexamethasone and has fewer side effects. It is most often used as a 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.

Preparations in the form of inhalation

The drug can provoke the appearance of some side effects, including bronchospasm and discomfort in the throat.

Contraindications: individual intolerance. Liquid for inhalation is forbidden to be used in the treatment of children under 16 years of age, suspension is forbidden to be used in the treatment of children under 3 months of age, powder - for children under 6 years of age.

Do not allow the drug to get into the eyes.

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

The drug is used only in the form of inhalation. It can provoke candidiasis of the oral mucosa, a change in the timbre of the voice, bronchospasm. If used for a long time in large quantities, it causes systemic side effects. To prevent candidiasis of the oral cavity after inhalation, rinse your mouth.

This drug is not used to treat asthma attacks.

Preparations for systemic use

There are 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

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

Ointments begin to act more slowly, their consistency is greasy. They are prescribed for dry skin, prone to peeling, with weeping processes.

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

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

Side effects

Especially many side effects are observed with the systemic use of these drugs. Several new methods have been developed for the use of these drugs, which slightly reduce the likelihood of unwanted effects. But treatment with these drugs in any case requires constant monitoring of the general health of the patient.

From the side of the movement apparatus: osteoporosis, compression fractures of the spine, myopathy, pathological fractures, necrosis of the femoral head,
From the side of the skin: acne, stretch marks, hemorrhages, atrophy, thinning of the dermis, worsening of scarring of wounds,
From the side of the brain: psychosis, emotional instability, brain pseudoneogenesis syndrome,
From the side of the organs of vision: exophthalmos, glaucoma, cataract,
From the side of metabolism: gluttony, hyperglycemia, hyperlipidemia, Cushing's syndrome,
From the digestive tract: inflammation of the pancreas, esophagitis, indigestion, stomach ulcers, gastric and intestinal bleeding,
From the endocrine system: inhibition of puberty and growth, amenorrhea, diabetes, adrenal suppression,
From the side of the heart and blood vessels: increase in blood pressure
From the immune system: manifestations of infectious diseases intensify, the picture of diseases becomes implicit,
Violation of the ratio of water and salts in the tissues, swelling, lack of potassium in the body are observed.

The first side effects that appear during treatment are sleep disturbances, gluttony, mood swings, and weight gain.

Application during pregnancy

Hyperandrogenism ( overproduction of male sex hormones),
The threat of premature resolution from the burden in the third trimester,
Congenital intrauterine hyperplasia of the adrenal cortex in the fetus.

A woman who has been using glucocorticoids for the past year and a half is prescribed during childbirth hydrocortisone hemisuccinate by injection every six hours. This will prevent the development of acute adrenal insufficiency.

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hydrocortisone and prednisone differences

Kharkov Institute of Postgraduate Medical Education

Introduction

The cells of the fascicular zone 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 adenohypophysis corticotropin (formerly known as adrenocorticotropic hormone). An increase in the level of cortisol in the blood by a feedback mechanism inhibits the secretion of corticoliberin in the hypothalamus and corticotropin in the pituitary gland.

The intensity of secretion of glucocorticoids into the blood during the day varies significantly. 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 for the most part opposite to those induced by insulin. Hormones have catabolic (i.e., they contribute to the breakdown of complex protein molecules into simple substances) and anti-anabolic (i.e., they prevent the biosynthesis of protein molecules) effects on protein metabolism. As a result, the breakdown of protein in the body increases and the excretion of nitrogenous products increases. Protein breakdown occurs in muscle, connective and bone tissues. The content of albumin in the blood decreases.

Glucocorticoids stimulate the catabolism of triglycerides and inhibit the synthesis of fat from carbohydrates. At the same time, a decrease in the adipose tissue of the extremities is often combined with an increase in the deposition of fat 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 are involved in maintaining normal arteriole 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 and an increase in their number in the peripheral blood are stimulated. Hormones retain sodium and water in the body against the background of potassium loss, inhibit calcium absorption in the intestines, promote the release of the latter from the bone tissue and its excretion in the urine. Glucocorticoids increase sensory sensitivity and excitability of the nervous system, participate in the implementation of stress reactions, affect the human psyche.

Natural glucocorticoids and their synthetic analogs are widely used in the clinic mainly because they have several other valuable properties: 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 features of the diseases themselves, etc. In addition, various glucocorticoids have varying degrees of immunosuppressive and anti-inflammatory effects, between which there is no direct relationship. So, dexamethasone has a powerful anti-inflammatory and relatively low immunosuppressive activity.

Comparative characteristics of glucocorticoids

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.

Features of the use of injectable forms are due to both the properties of the glucocorticoid itself and the ester associated with it. For example, succinates, hemisuccinates and phosphates are soluble in water and, when administered parenterally, have a rapid but relatively short-term effect. On the contrary, acetates and acetonides are finely crystalline suspensions and are insoluble in water. Their action develops slowly, over several hours, but lasts for a long time (weeks). Water-soluble ethers of glucocorticoids can be used intravenously, fine-grained suspensions - no.

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 a tablet" (that is, if it was 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 replacement) - is currently not valid. This is due to the introduction into clinical practice of dosage forms of glucocorticoids with different content of the active principle.

Natural glucocorticoids have mineralocorticoid activity, although weaker than true mineralocorticoids. Non-fluorinated semi-synthetic glucocorticoids also have mineralocorticoid effects (the severity of which, in turn, is inferior to the effects of natural glucocorticoids). Fluorinated preparations have no mineralocorticoid activity (Table 2). The glucocorticoid activity of semi-synthetic drugs is higher than that of cortisone and hydrocortisone, which is explained by lower protein binding compared to natural glucocorticoids. A feature of fluorinated drugs is a slower metabolism in the body, which leads to an increase in the duration of the drug action.

In the medical literature, the terms are widespread: “low” doses of glucocorticoids, “high”, etc. They say about “low” doses of corticosteroids 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 - "high". Values close to those given are also obtained when calculating the daily dose of corticosteroids per 1 kg of the patient's body weight. The conditional boundary between "medium" and "high" doses is 0.5 mg of prednisolone per 1 kg of the patient's 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 method of treatment is called "pulse therapy".

The dose of glucocorticoids prescribed at the beginning of the treatment of a particular disease depends mainly on the nosological form and severity of the disease. The age of the patient also influences the dose; the presence or absence of comorbidities; concomitant use of other drugs and other factors.

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

According to the persistence 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.

Compared to prednisolone, methylprednisolone has a slightly higher glucocorticoid activity (by 20%) and has a weak mineralocorticoid effect. The advantage of the drug is a very moderate stimulation of the psyche and appetite, which justifies its appointment to patients with an unstable psyche and overweight.

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

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

Dexamethasone is 7 times more glucocorticoid than prednisolone. It is a fluorinated glucocorticoid and does not have a mineralocorticoid effect. Compared with 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, psychostimulant action).

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

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

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. Weaker than prednisolone in glucocorticoid activity (4 times), but surpasses it in the severity of mineralocorticoid action. Hydrocortisone is commonly used for physiological replacement and "stress" cover in patients with hypothalamic-pituitary-adrenal axis insufficiency. In acute adrenal insufficiency and other emergencies, hydrocortisone hemisuccinate is the drug of choice.

Beclomethasone, flunisolide, budesonide, triamcinolone acetonide, and fluticasone are administered by inhalation. Beclomethasone (beclomet, becotide, etc.) is most often prescribed for long-term maintenance therapy for bronchial asthma. It has an insignificant systemic effect, although in high doses (1000-2000 mcg / day) it causes osteoporosis and other side effects. The use of flunisolide (ingacort) in comparison with beclomethasone leads to the development of oral candidiasis somewhat less frequently. Budesonide (pulmicort) when administered by inhalation is somewhat superior in efficacy and has less effect on kidney function than beclomethasone. Fluticasone (flixotide, flixonase) is 30 times more affinity for glucocorticoid receptors than prednisolone and 2 times budesonide. It has 2 times stronger local anti-inflammatory effect than beclomethasone.

Indications and contraindications

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

In general, glucocorticosteroids can be used as agents:

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

For the 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 1 time per day in the morning.

In adrenogenital syndrome, glucocorticoids are used in therapeutic (i.e., supraphysiological) doses to suppress the secretion of corticotropin (and subsequently reduce the hypersecretion of androgens by the adrenal cortex). 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 represents the most common clinical use of glucocorticoids. An indispensable condition for treatment is to take into account the physiological rhythm of hormone secretion, which makes it possible to reduce the frequency and severity of undesirable effects.

The scope of corticosteroids can be outlined as follows.

Glucocorticoids are indicated for:

Since glucocorticoids are natural hormones or their synthetic analogues, they have no absolute contraindications to the appointment. In urgent cases, hormones are used without contraindications at all. Relative contraindications are:

Systemic use of glucocorticoids

To date, 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 difficulties for physicians. Therefore, in the following presentation, the main attention will be focused on the systemic use of hormones.

If systemic administration of glucocorticoids is necessary, oral administration is preferred. If it is not possible to administer these drugs by mouth, they can be used in suppositories; the dose in this case increases by 25-50%. Existing injectable forms of glucocorticoids, when administered intramuscularly and, especially, intravenously, are rapidly metabolized in the body, and therefore their action is short-term and in most cases insufficient for long-term treatment. To obtain an equivalent, compared with oral administration, therapeutic effect, parenteral doses would have to be administered 2-4 times larger and frequent injections would have to be used. Existing long-acting parenteral preparations (eg, triamcinolone acetonide, or kenalog) are not used for active "suppressive" treatment, but mostly as maintenance or topical (eg, intra-articular) therapy.

In the morning, the hypothalamic-pituitary-adrenal axis is the least sensitive to the inhibitory effects of exogenous corticosteroids. When dividing the daily dose of glucocorticoids into 3-4 parts and taking them at regular intervals, the risk of suppressing the hypothalamic-pituitary-adrenal axis increases. Therefore, in most cases, hormones are prescribed in the form of a single 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 scheme of application can reduce the risk of inhibition of the hypothalamic-pituitary-adrenal axis and reduce the risk of osteoporosis.

The therapeutic efficacy 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, in blood diseases, (nonspecific) ulcerative colitis, malignant tumors, and also in severe diseases). Alternative therapy is usually used after the suppression of inflammatory and immunological activity with a decrease in the dose of glucocorticoids and the transition to maintenance treatment. With an alternating regimen, the dose of hormones required for a 48-hour period of time 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 the alternating use of glucocorticoids, the risk of infectious complications is reduced, and growth retardation in children is not as pronounced as with daily hormones.

Only in rare cases (for example, with nephrotic syndrome in children) is alternative therapy prescribed from the first days of treatment. Typically, this regimen of hormone administration is reserved for patients who have managed to achieve stabilization with the help of daily use of glucocorticoids. Below is an example of switching a patient to alternating therapy, in which the initial dose of prednisolone was 50 mg.

In alternative treatment, only intermediate-acting corticosteroids (prednisone, prednisolone, methylprednisolone) are used. After taking a single dose of these drugs, the hypothalamic-pituitary-adrenal axis is suppressed for 12-36 hours. When prescribing long-acting glucocorticoids every other day (triamcinolone, dexamethasone, betamethasone), the risk of inhibition of the hypothalamic-pituitary-adrenal axis remains, and therefore it is irrational to use them for alternating treatment. The field of application 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 ("hormone-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 (eg, 0.6-1.0 mg 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 intake of the entire daily dose. Further reduction to the minimum effective maintenance dose (an alternating dose is preferred) is determined by the specific clinical circumstances. Too gradual reduction is combined with an increase in the number and severity of side effects of glucocorticoid treatment, and too rapid - predisposes to an exacerbation of the disease.

In order to reduce side effects, the possibility of "saving steroids" 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 the complications of steroid therapy.

Therapy with high doses of glucocorticoids may be unsatisfactory due to lack of efficacy and / or the appearance of severe complications. In such cases, one should consider the possibility of pulse therapy, i.e. intravenous administration of very large doses of hormones for a short time. Although there is still no clear definition of pulse therapy, this term is usually understood as 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 drug is used more often than others) at a dose of up to 1 g / sq. meter of body surface for 1-5 days. Currently, pulse therapy with steroid hormones is often used at the beginning of the treatment of a number of rapidly progressive immunologically mediated diseases. The usefulness of this method for long-term maintenance therapy appears to be limited.

In general, less toxic effects develop with topical steroids than with systemic use. The greatest number of adverse events in the systemic use of hormones occurs if the daily dose is divided into several doses. When the daily dose is taken as a single dose, the number of adverse effects is less, and the alternating regimen is the least toxic.

Synthetic glucocorticoid analogs with a long half-life (eg, dexamethasone) are more likely to cause side effects when taken daily than drugs with a short and intermediate half-life. The appointment of higher doses of steroids is relatively safe if the duration of their use does not exceed one week; with a longer intake 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 prolonged use of fluorinated drugs, the development of undesirable effects in the fetus, including deformities, is possible. If a woman in labor has taken glucocorticoids for the previous 1.5-2 years, hydrocortisone hemisuccinate 100 mg every 6 hours is additionally administered to prevent acute adrenal insufficiency.

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

For the prevention of respiratory distress syndrome in premature infants, long-acting drugs (most often dexamethasone) are used. Recommended intramuscular administration of dexamethasone to a woman in labor at a gestational age of up to 34 weeks 24-48 hours before the expected birth. Re-introduction of the drug is possible if preterm labor has not occurred within the next 7 days.

Patient education

The patient should be aware of the possible clinical consequences of insufficiency of the hypothalamic-pituitary-adrenal axis, which may result from the systemic use of glucocorticoids. The patient should be warned about the inadmissibility of self-cessation of treatment or a rapid reduction in the dose of hormones without appropriate medical recommendations. The response of the hypothalamic-pituitary-adrenal axis to stress may be reduced even after daily administration of glucocorticoids for 7 days. If regular oral hormone treatment is interrupted for more than 24 hours, then the patient may develop circulatory collapse in response to physiological stress, trauma, infection, surgery, which often requires parenteral administration of glucocorticoids to eliminate it. 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 develops more often with the appointment of high doses of glucocorticoids).

The patient's attention should be drawn to the fact that hormonal treatment stimulates appetite and causes weight gain and the importance of diet should be emphasized even 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, it is impossible to completely avoid side effects during hormone therapy (Table 4).

Interaction with other medicines

Some drugs 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 lowers the level of the latter in the blood so much that its concentration is below the therapeutic one.

Conclusion

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

Belousov Yu. B., Omelyanovsky V. V. Clinical pharmacology of respiratory diseases.- M.: Universum Publishing, 1996.- S. 119-130.
Bereznyakov I.G. Glucocorticosteroids: clinical application (manual for physicians).- Kharkov, 1995.- 42 p.
Fundamentals of human physiology (under the editorship of B. I. Tkachenko). - St. Petersburg: International Fund for the History of Science. - T. 1. - S. 178-183.
Sigidin Ya. A., Guseva N. G., Ivanova M. M. Diffuse diseases of the connective tissue.- M .: Medicine, 1994.- 544 p.
Strachunsky L. S., Kozlov S. N. Glucocorticoid preparations.- Smolensk, 1997.- 64 p.
Therapeutic handbook of the University of Washington (under the editorship of M. Woodley, A. Whelan) .- M .: Practice, 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.

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Prednisolone Nycomed is an effective drug that treats inflammatory diseases of the joints, asthma, diseases of the lungs, blood, and skin. Its pharmacological group: glucocorticosteroids. It is a hormonal drug. It has anti-allergic and immunosuppressive effects. Easily relieves fatigue and eliminates inflammation. This medicine is for oral use.

Instructions for use Prednisolone suggests the use of this drug in acute or chronic asthma, dermatitis and various manifestations of allergies.

Prednisolone Nycomed is able to virus-duncate the synthesis of annexin, which inhibits the active action of A2 phospholipases;
With an anti-inflammatory effect, the effectiveness of glucocorticoids is activated to stop the performance of the COX-2 complex;
The drug is able to stop the active movement of chromosomes in the blood vessels;
With immunosuppressive performance, a reduction in T-lymphocytes occurs. There is an increased production of ummunoglobulins;
With the action directed against allergies, suppression of the synthesis of mediators that cause an unpleasant condition can be formed;

Mechanism of action

A drug can be used for all sorts of systemic pathologies that are inherently associated with the autoimmune process. After taking the drug, steroid hormones, together with receptors, move to the cell nucleus. Once in the nucleus itself, hormones begin to interact with effector elements that are located on the acceptor sites of chromatin. At this point, the interaction of the drug begins. Short-term therapy with Prednisolone has a beneficial effect on the body.

Prevents the development of various diseases.

Ask your question to a neurologist for free

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

Release form and packaging

Medicines containing prednisolone are produced under various brand names. The drug has several analogues, synonymous drugs and new generation drugs. These funds are produced in five different dosage forms:

Tablets that need to be washed down with a small amount of distilled water;
Snow-white crystalline powder for the manufacture of suspension for injection;
Liquids for injections and injections intramuscularly or intravenously;
Medicinal ointment intended for external use;
Ophthalmic drops;

Price

Tablets of a snow-white shade, roundish. They have a small chamfer with an engraved trademark, weighing five milligrams. The cost of tablets depends on the cheating dealers. The price for one pack of medicine in the amount of one hundred pieces is 101 rubles and more.
The crystalline powder is available in a sealed package weighing 10 grams. The cost of this form of the drug is 75 rubles or more.
The solution for intravenous injection is produced in the amount of three ampoules, weighing 25 milligrams-1 milliliter. The price of the dosage form is 42 rubles and more.
The ointment is available in a tube weighing 15 grams. Contains in its composition 0.5% of the active ingredient. The cost of this dosage form is 28 rubles and more.
Eye drops are produced in glass bottles in the amount of one milliliter with a dropper. The cost of the drug is 60 rubles or more.

Compound

The main active ingredient of the drug is prednisolone.

In tablets that are intended for oral use, there are 5 or 1 milligrams of the substance;
The powder contains 30 milligrams of the substance;
The solution contains 15 or 30 milligrams of the component per milliliter;
The ointment contains 0.5% of the component;
The eye drops contain 0.5% of the active ingredient;

Auxiliary components of tablets:

Potato polysaccharide;
Milk sugar;
E 572;
Gelatin is used as a thickener;

Additional components of the solution:

Glycerolum Formal;
Butyl alcohol C4H9OH;
Sodium salt of hydrochloric acid;
Distilled water;

Indications for use

Definition of ARF, rheumatic carditis, Sydenham's chorea;

Rheumatic diseases:

Libman-Sachs disease;
Autoimmune disease Scleroderma;
Nodular polyarteritis;
Wagner's disease;
Multiple sclerosing encephalomyelitis;

Joint diseases that cause inflammation and are acute or chronic:

Rheumatoid Arthritis;
Juvenile arthritis, which occurs only in children and adolescents under 16 years of age;
Bechterew's disease;
Gouty and psoriatic arthritis;
Polyarthritis;
Shoulder-shoulder periarthritis, which causes inflammation of the periarticular tissues;
Osteoarthritis Cartilage;
Inflammatory disease Still's syndrome;
Inflammation of mucous bags Bursitis;
Tenosynovitis;
synovitis;
epicondylitis;
Asthma, Status asthmaticus;

Diseases of the lung tissue ILD:

inflammation of the alveoli;
Education in the lungs of scar tissue;
Besnier-Beck-Schaumann disease of the second and third degree;
1. Bronchogenic cancer;
2. Inflammation of the connective tissue Beryllium;
3. Pneumonia;
4. Eosinophilic pneumonia of Loeffler;
5. Tuberculosis;

Consumption;
Tuberculous meningitis, causing inflammation of the meninges;

Postoperative syndrome after removal of the adrenal glands, as well as insufficiency and malfunction of the organ;
Congenital adrenal hyperplasia;
Congenital dysfunction of adrenogenital syndrome;
Thyroiditis de Quervain;

Allergy, manifested in acute and chronic form:

Allergic reactions that form after drug therapy or consumption of food containing dyes;
Serum sickness caused by immune sera therapy;
Allergic rhinoconjunctivitis;
Diffuse neurodermatitis;
contact dermatitis;
Urticaria;
Hay fever;
Angioedema;
Malignant exudative erythema;
Toxic-allergic dermatitis;

Liver disease:

Alcoholic hepatitis with encephalopathy;
Chronic active hepatitis CAH;
Hypoglycemic coma with SD. hypoglycemia;
1. Autoimmune kidney diseases, including an acute form of bilateral organ damage);
2. nephrotic syndrome;
3. Inflammation of the gastrointestinal tract:

Diffuse ulcerative inflammation of NUC;
Chronic disease Crohn's disease;
Polyetiological disease Local enteritis;

Diseases of the blood and hematopoietic organs:

Pathological condition Agranulocytosis;
panmyelopathia;
Rusticki-Kahler disease;
Acute form of AML;
Tumor disease Lymphogranulomatosis;
Werlhof disease;
Secondary thrombocytopenia in adults;
Autoimmune hemolytic anemia;
Erythroblastopenia;
Congenital erythroid hypoplastic anemia;

Autoimmune and other diseases affecting the skin:

Eczema;
Seborrheic dermatitis;
Psoriasis vulgaris;
Toxic epidermal necrolysis;
bullous dermatitis herpetiformis;
Pemphigus;
Ritter's exfoliative dermatitis;
swelling of the brain;

Ophthalmic diseases:

Damage to the choroid;
Conjunctivitis;
Allergic ulcers of the cornea;
Keratitis, manifested in the form of pus;
Anterior uveitis;
Iritis;
Uveitis;
choroiditis;
Neuritis of the optic nerve;

Prophylactic use in transplant rejection.
Hypercalcemia, which is formed after oncological diseases.
For preventive measures and to eliminate the feeling of intoxication, manifested in the form of vomiting and nausea during the cytostatic course of treatment.

Contraindications

Prednisolone Nycomed in most cases it is used to eliminate severe pathologies. Therefore, the list of contraindications is small:

The drug is not recommended for use in systemic fungal infections;
The medicine is contraindicated in hypersensitive patients and allergy sufferers;

Before use, you should consult with a professional specialist. Self-medication can adversely affect the health of the patient.

Side effects

Negative effects after a short application are extremely rare. Basically, the consequences that affect human health are manifested in people prone to various allergic reactions. Long-term treatment can provoke a deterioration in health and irreversible consequences. With prolonged use of the drug may occur:

In the digestive system: development of stomach and colon ulcers, bleeding, nausea, gag reflex, increased appetite. The development of pancreatitis, esophagitis, increased gas formation may be observed.
Side effects in the nervous system: there is an increase in intracranial pressure, which provokes stagnation of the optic nerve head. Some patients experience insomnia, migraine, dizziness, increased heart rate, convulsions, fainting, severe headache.
In the endocrine system: impaired performance of the adrenal cortex, growth retardation in adolescents, increased blood sugar. Girls may experience a failure of the cycle of critical days, an increase in hair growth on the skin.
There may be a delay of salts and water in the body, which provokes a violation of pressure and a malfunction in the work of hematopoiesis.
Patients may feel weakness, brittle bones, pain in the muscles, increased fractures, shifts of the vertebrae.
On the skin, wound healing worsens, the formation of erythema. There may be increased sweating. Adolescents develop acne, rash, dermatitis.
Side effects in ophthalmology in patients develops cataracts, increases intraocular pressure. In especially severe cases, exophthalmos and glaucoma develop.
A disturbance of nervous activity is formed. Patients have psychosis, depression, fear, irritation.
A negative nitrogen balance may occur, which provokes the destruction of proteins. This interaction can lead to weight gain.
There is a decrease in the number of leukocytes and platelets. At the same time, there is an increase in the level of calcium and cholesterol.
Side effects in the development of allergies. Allergic reactions are formed, the development of anaphylactic shock, an increase in heart rate. People develop skin rashes, hives, blistering.

withdrawal syndrome

There are four types of withdrawal syndrome:

There is a violation of the hypothalamic-pituitary-adrenal work capacity. Therefore, it is necessary to prescribe cortisol therapy.
With a rapid decrease in the dose of the drug, there is: malaise, weakness, fatigue, depression, irritability, arthralgia.
At this stage, the development of glucocorticoid dependence occurs.
At this stage, there are no clinical manifestations, but there is laboratory evidence in which there is a failure in the performance of the adrenal function. In this case, experts prescribe cortisol therapy.

In order to neutralize the side effects, need to see a specialist. The doctor will prescribe the necessary therapy, reduce dosages or advise you to stop taking Prednisolone Nycomed.

Recipe

Recommended prescription for taking medicine in tablets: Tab. Prednisoloni 50 or 100 pieces per pack. One little thing three times a day;
Recommended prescription for injection fluid: Sol. Prednisoloni 3%. Administer intravenously once or twice a day;
Recommended prescription for gel: Ung. Prednisoloni 0.5%. It is necessary to impose on burns and other defects of the skin once or twice a day;
Recommended prescription for ophthalmic drops: Sol. Prednisoloni 0.5%. Bury eyes one or two drops two or three times a day;

The tablets should be taken with distilled water. They are swallowed completely. Chew this medicine or make it into a crystalline powder Not recommended. Required time of taking 6-8 o'clock in the morning. At least 2/3 of the daily dose should be taken early in the morning. It is at this time that the effect of the drug increases.

For serious diseases in severe form, patients should take at least 50-75 milligrams of the drug. This dose is identical to taking 10-15 pieces per day.
In chronic diseases, it is recommended to take 20-30 milligrams, which is equal to 4-6 tablets.
After the body returns to normal, the dosage of the drug should be reduced to 5-15 milligrams per day.

The duration of therapy may vary. It inherently depends on the state of health of the patient and is appointed by a specialist.

Diluted powder for the preparation of an intravenous solution, as well as a ready-made solution, can be used for both adults and children. The required dose, course of therapy and the option of administering the drug to the body are prescribed by a specialist. Injections must be made from 6 to 8 in the morning. Injections must be made early in the morning.

The ointment is applied in a thin layer on the skin with light massaging movements one to three times a day. The duration of treatment is from 6 to 14 days. As soon as improvement occurs, the use of the drug should be discontinued. It is forbidden to apply a bandage on top of the gel. Otherwise, a large amount of the drug can be absorbed into the bloodstream and cause the formation of side effects. It is not recommended to use the medicine for more than two weeks.

Eye drops should be instilled one to two drops three times a day. In acute diseases, it is necessary to instill every 2-4 hours. After surgical interventions, the drug can be used only on the fifth day after the operation.

After improvement of a condition therapy needs to be stopped.

Special indications

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

How to take the drug for children. The dosage of tablets is calculated depending on body weight. For one kilogram of weight, it is necessary to give 1-2 milligrams of the drug. As a maintenance dose, 0.25-0.5 milligrams per kilogram of weight is prescribed.
The dosage of injections for children under one year old is calculated based on weight. For one kilogram it is necessary to inject 2-3 milligrams of the solution. Adolescents from one to fourteen years old are injected with 1-2 milligrams of the drug per kilogram of weight.

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

During breastfeeding, the use of the drug is strictly prohibited. The hormone is able to penetrate into breast milk and adversely affect the health of the child.

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

Storage, dispensing from pharmacies

The drug is sold in pharmacies strictly by prescription. It is necessary to store medicine in the dark dry place at a temperature not above 18-25 °C. The shelf life of the drug is five years.

Analogues

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

Preparations	Description	Contraindications	Cost, rub
Prednisone	Prednisone is a similar drug that replaces Prednisolone.	Prednisone is not recommended for patients with gastric and colonic ulcers.	The cost of Prednisone is 250 rubles and more.
Methylprednisolone	Easily relieves inflammation. Has an anti-shock effect.	Contraindicated in people with eye damage and tuberculosis.	From 100
	Dexamethasone is a drug containing sodium phosphate in its composition.	Dexamethasone is not recommended for hypersensitive patients.	The cost of Dexamethasone is from 152
	Available in the form of tablets and lyophilisate.	Contraindicated in people with ulcerative lesions.	From 198
Formoterol	It is a bronchodilator drug.	Contraindicated for allergy sufferers.	From 414
Prednisolone Hemisuccinate	Before using the remedy, the pulse should be even and calm. The drug inhibits the function of leukocytes.	Contraindicated in people with skin tumors and intra-articular fractures.	From 100
	Suppresses the performance of tissue macrophages.	Contraindicated in patients with a history of acute psychosis.	The cost of Triamcinolone is 100 rubles and more.

Interaction with other drugs

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

17,21-Dihydroxypregna-1,4-diene-3,11,20-trione

Chemical properties

This substance is steroid which is normally produced in the body adrenal cortex .

Prednisone belongs to a group of synthetic non-fluorinated glucocorticosteroids . Compounds of this kind are more active than natural substances. They are used in smaller dosages. The influence of this group of substances on water-salt metabolism in the body is minimized, side reactions are rare.

pharmachologic effect

Anti-inflammatory, glucocorticosteroid, antiallergic.

Pharmacodynamics and pharmacokinetics

The substance contributes to stabilization processes lysosomal membranes , reduces the output intensity proteolytic enzymes from lysosome cells , inhibits enzyme production phospholipases A2 And arachidonic acid . The result is inhibition of synthesis hydroxy acids , leukotrienes and inflammatory mediators. Prednisone reduces capillary permeability, inhibits the phase exudation And proliferation .

The tool has anti-allergic properties due to its ability to lead to mast cell degranulation , inhibit the synthesis process leukotrienes And specific antibodies .

Anti-shock properties due to an increase in the body's response to vasoconstrictor substances, stimulation of the cardiovascular system and a delay in the tissues of water and sodium. The substance stimulates the work of the central nervous system, also thanks to the synthetic GKS the process of excretion of toxic substances from the liver is accelerated, the permeability of cell membranes decreases.

After oral administration, the substance is absorbed in the usual way. Its maximum concentration, reaching within 60-120 minutes. Prednisone has a high bioavailability, about 90%. Undergoes metabolic reactions in the liver.

The pharmacokinetic parameters of the drug have a linear dependence on the dosage.

The drug is excreted through the kidneys.

Indications for use

Prednisone preparations are prescribed:

with , patients suffering from acute adrenal insufficiency , androgenital syndrome ;
for treatment, nodular periarthritis ;
at , scleroderma And ;
for the treatment of various Addison's disease ;
at hepatic coma , hypoglycemia , ;
as a therapeutic and prophylactic agent for shocked ;
in various forms, hemolytic anemia ;
patients with thrombocytopenic purpura ;
for treatment, itching on the skin,;
at pruritus ,erythroderma ;
at false croup in childhood.

Contraindications

Tablets are not prescribed:

if the patient has synthetic corticosteroids or active substance;
during exacerbation;
sick;
at Itsenko-Cushing's disease ;
if the patient has a tendency to;
with severe kidney disease, increased HELL or ;
persons with viral infections, mental disorders.

Side effects

During treatment with Prednisone, the following adverse reactions may develop:

promotion blood pressure ;
Itsenko-Cushing's syndrome , severe exhaustion adrenal cortex ;
imbalance of nitrogen in the blood, weight gain of the patient, hyperglycemia ;
mental problems;
an increase in the content of acids in gastrointestinal tract and as a result, an aggravation or stomach ulcers ;
swelling caused by sodium retention and excess excretion of potassium from the body;
bone necrosis , ;
increase in blood coagulability;
, (latent);
decrease, slowdown in the healing of wounds and cuts.

Prednisone, instructions for use (Method and dosage)

Dosage and mode of administration are individual.

Most often, adults are prescribed 20-30 mg per day. As a maintenance dose, 5-10 mg is used.
If necessary, the initial dosage may be 100 mg, maintaining up to 15 mg.

Reducing the daily dosage should be carried out smoothly.

The maximum amount of a substance that can be given to an adult at a time is 15 mg, per day - 100 mg.

To eliminate shock and other emergencies, large doses of the substance can be administered to the victim for a short period of time.

Overdose

An increase in the frequency and severity of side effects is expected.

Interaction

In combination with the drug promotes the development hypoprothrombinemia .

When combined with and cardiac glycosides increased likelihood of developing hypokalemia .

Gross formula

C 21 H 26 O 5

Pharmacological group of the substance Prednisone

Nosological classification (ICD-10)

CAS code

53-03-2

Pharmacology

pharmachologic effect- anti-inflammatory, antiallergic, glucocorticoid.

Stabilizes cell membranes, incl. lysosomal, reduces the release of proteolytic enzymes from lysosomes (inhibition of the alteration phase and limitation of the focus of inflammation), inhibits phospholipase A 2, disrupts the liberation of arachidonic acid and, as a result, inhibits the synthesis of PG, hydroxy acids and leukotrienes, inhibits the activity of hyaluronidase and reduces capillary permeability (phase inhibition exudation), fibroblast activity (inhibition of the proliferation phase). Antiallergic properties are due to a violation of mast cell degranulation, a decrease in the synthesis of leukotrienes and suppression of antibody production, anti-shock properties are due to sodium and water retention, an increase in the vascular response to endo- and exogenous vasoconstrictor substances and a stimulating effect on cardiac activity, antitoxic properties are due to an acceleration of the inactivation of toxic substances in the liver, a decrease in permeability of cell membranes.

When taken orally, it is easily absorbed, Cmax in blood plasma is observed after 1-2 hours. Bioavailability exceeds 90%. Undergoes biotransformation, mainly in the liver, excreted mainly by the kidneys. With an increase in dose, T 1/2, total clearance, volume of distribution and degree of protein binding increase. Affects carbohydrate, protein, fat and water-salt metabolism. Increases blood glucose levels, promotes the accumulation of glycogen in the liver, enhancing gluconeogenesis. Activates the processes of catabolism, slows down regeneration, controls the deamination of amino acids in the liver, promotes the redistribution of adipose tissue, retains sodium and water in the body, enhances the excretion of potassium; stimulates the cardiovascular system, increases the tone of arterioles and myocardial contractility, increases stroke and minute volume, excites the central nervous system, has antitoxic and immunosuppressive effects, causes an increase in the secretion of the gastric mucosa and acidity of gastric juice.

The use of prednisone

Rheumatism, rheumatoid arthritis, dermatomyositis, periarteritis nodosa, scleroderma, Bechterew's disease, bronchial asthma, allergic diseases, Addison's disease, acute adrenal insufficiency, adrenogenital syndrome, hepatitis, hepatic coma, hypoglycemic conditions, lipoid nephrosis, agranulocytosis, various forms of leukemia, lymphogranulomatosis , thrombocytopenic purpura, hemolytic anemia, infectious mononucleosis, acute pancreatitis, pemphigus, eczema, pruritus, exfoliative dermatitis, psoriasis, pruritus, seborrheic dermatitis, lupus erythematosus, erythroderma, alopecia; prevention and treatment of shock.

Contraindications

Hypersensitivity, peptic ulcer of the stomach and duodenum in the acute phase, osteoporosis, Itsenko-Cushing's disease, tendency to thromboembolism, renal failure, severe arterial hypertension, systemic mycoses, viral infections, vaccination period, active form of tuberculosis, productive symptoms in mental illness.

Application restrictions

Diabetes mellitus, nonspecific infections, latent forms of tuberculosis, pregnancy (especially the first trimester).

Side effects of prednisone

Reduced resistance to infection, hyperglycemia up to the development of steroid diabetes, negative nitrogen balance, osteoporosis, aseptic bone necrosis, increased acidity of gastric juice, ulcerogenic effect on the gastrointestinal tract, hypokalemia, sodium and water retention, edema, arterial hypertension, increased blood clotting, Itsenko's syndrome - Cushing's, weight gain, "moon" face, steroid cataract, latent glaucoma, menstrual disorders in women, insomnia, muscle weakness; withdrawal syndrome associated with inhibition of function or atrophy of the adrenal cortex.

Glucocorticosteroid drug. Drugs used in rheumatoid arthritis, spondylitis, rheumatism of unspecified origin, arthritis, traumatic shock, infectious diseases.

Release form and composition

Tablets containing the active substance - prednisone 1, 5, 20 and 50 mg in each tablet. Tablets with a concentration of 1 mg - one hundred pieces in a polymer jar. Tablets with a concentration of 5, 20 and 50 mg - ten pieces in a polymer blister, two blisters in a carton.

Pharmacological properties

Anti-inflammatory, glucocorticoid and antiallergic drug. Stabilizes the state of cell membranes, inhibits the production of prostaglandins, which are responsible for the severity of pain in pathologies of the musculoskeletal system.

It reduces capillary permeability, anti-allergic properties are due to a decrease in the production of specific antibodies, anti-shock properties are due to a vasoconstrictor effect and stimulation of the cardiovascular system.

Rapidly absorbed when taken orally, peak blood concentrations are reached after two hours. Transformed in the liver, excreted by the kidneys.

Influences lipid, carbohydrate and protein metabolism. Promotes the accumulation of glycogen glycogen in the liver and increase blood glucose levels. The drug is able to retain water and sodium in the body, stimulate the cardiovascular system and increase the tone of arterioles, the ability of the heart muscle to contract.

Regarding the central nervous system, it acts as a causative agent, exhibits antitoxic and immunosuppressive effects. Increases the acidity of gastric juice and the secretion of the gastric membrane.

Indications for use

In the practice of treating diseases of the musculoskeletal system and muscles, it is used for rheumatism, rheumatoid arthritis, periarteritis, scleroderma, dermatomyositis.

It is used in the treatment of allergic diseases, Addison's disease, with acute adrenal insufficiency, androgenital syndrome and hepatitis, hepatic coma, hypoglycemia.

It is used in the treatment of lipoid nephrosis, agranulocytosis, leukemia of any etiology, lymphogranulomatosis, thrombocytopenic purpura, hemolytic anemia.

As part of complex therapy for infectious mononucleosis, acute pancreatitis, pemphigus, itching of unknown etiology, eczema, dermatitis, psoriasis, seborrheic dermatitis, lupus erythematosus, erythroderma. It is used as a prophylactic for shock conditions.

Prednisone is contraindicated in cases of known hypersensitivity to the active substance or any other ingredient in the formulation. It is not used for peptic ulcer of the duodenum and stomach, especially in the acute phase. It is not applicable for osteoporosis, Itsenko-Cushing's disease, and also in cases where the patient is prone to thromboembolism.

The use of the drug is contraindicated in case of renal insufficiency, severe arterial hypertension and hypertension, generalized fungal infections (mycosis, including candidiasis), with a viral infection in the acute or chronic phase.

It is forbidden to take this drug during the vaccination period, with an active form of tuberculosis, symptoms of mental pathologies.

Carefully

Caution should be exercised when prescribing Prednisone to patients with any form of diabetes mellitus, as well as for non-specific infections, including carriage of staphylococcus, streptococcus.

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Caution requires prescribing the drug to patients with latent forms of tuberculosis, as well as pregnancy, especially the first trimester.

Only a specialist should deal with the appointment of the drug - it is forbidden to take the drug on your own without consulting a doctor.

How to use

The official instructions for the use of the drug Prednisone indicate that the dosage and frequency of administration are set individually by the attending physician, depending on the severity of the pain syndrome and the inflammatory process.

Maintenance dosages should be prescribed after the desired therapeutic effect is achieved. The calculation of the maintenance dosage depends on the prescribed dosage during the period of active treatment - the maintenance dosage should be three times less than the therapeutic one.

If necessary and at the discretion of the attending physician, the initial dosage during treatment may be 0.1 g, the maintenance dose may be 0.015 g. It is necessary to gradually reduce the daily concentration of the drug.

The dosage for use in childhood is calculated based on body weight. The calculated amount of the drug should be divided into five doses.

Single maximum dosage - no more than 15 mg, daily - no more than 100 mg. In the event of life-threatening emergencies, as well as in shock conditions, the administration of large amounts of the drug is allowed under the supervision of a physician.

Side effects

Treatment with the drug can lead to such undesirable effects as low resistance of the body to infectious and viral diseases, the development of hyperglycemia, sometimes up to steroid diabetes.

Possible side effects such as necrosis of bone tissue, increased acidity of the stomach and, as a result, pain, hypokalemia, water and sodium retention in the body with swelling of the face and extremities as a result.

There may be the development of Itsenko-Cushing's syndrome, weight gain without other objective reasons, steroid cataracts, latent glaucoma, menstrual irregularities in women.

On the part of the central nervous system, such an undesirable consequence of taking Prednisone is also noted, such as sleep disturbance, insomnia, muscle weakness, hand tremor.

With a sharp cessation of treatment with Prednisone, a withdrawal syndrome may develop, associated with a decrease in the function of the adrenal cortex and their atrophy.

Side effects can be avoided and the likelihood of their manifestation can be minimized by carefully calculating the individual dosage.

Interaction with other drugs

The rate of processing of Prednisone by the liver is increased by phenobarbital, difenin, ephedrine and diphenhydramine. Prednisone accelerates the breakdown of digitoxin, penicillin, barbiturate-based drugs and chloramphenicol.

Concomitant use of cardiac glycosides and / or amphotercin increases the risk of hypokalemia. The combination of the drug with aspirin increases the risk of hypoprothrombinemia.

Cost and analogues

The price of a package of one hundred tablets of Prednisone costs from 1417 to 1685 rubles. Drug analogues:

Prednisolone

Prednisone and Prednisolone are often confused as there are enough differences between them. However, they are. Both drugs belong to the same pharmacological group and are produced on the basis of glucocorticosteroids.

Prednisone is credited with a structural similarity to Prednisolone, but the latter also has such forms of release as ointment and injections, while Prednisone is available only in tablet form. In addition, Prednisolone is much cheaper - up to 148 rubles per hundred tablets. Reviews of Prednisone indicate that the drug is difficult to access in pharmacy chains, unlike Prednasolone.

Active ingredient Fepranona has a psychostimulating effect.

The mechanism of action is based on the excitation of the center of saturation and the oppression of the center of hunger. Fepranon according to the instructions, stimulating the cerebral cortex, has practically no peripheral adrenostimulating effect.

In addition, Fepranon improves metabolism and promotes weight loss in obesity.

The pharmacodynamic effect develops one hour after taking the dragee, the duration of the effect is at least eight hours.

Release form Fepranon

The drug Fepranon is produced in the form of a 25 mg dragee containing the active ingredient - amfepramone.

Fepranon's analogs

Fepranon's analogues for the active substance are not released.

The closest analogues of Fepranon in terms of the mechanism of action are the drugs Goldline, Meridia, Reduxin, Lindax and Slimia.

Indications for the use of Fepranon

According to the instructions, Fepranon is prescribed for the treatment of obesity of alimentary origin.

In addition, Fepranone can be taken as part of combination therapy in the treatment of adiposogenital syndrome and hypothyroidism.

Fepranon according to the instructions is contraindicated for use in:

arterial hypertension;
atherosclerosis;
Pheochromocytoma;
myocardial infarction;
Diabetes;
pituitary adenoma;
epilepsy;
psychosis;
Glaucoma;
thyrotoxicosis;
Hypersensitivity to the active or auxiliary components of Fepranon.

Fepranon is approved for use in pediatrics from the age of twelve.

How to use Fepranon

Dragee Fepranon is recommended to be taken before meals (half an hour) along with a low-calorie diet. A single dosage is 1 tablet, the frequency of administration is up to three times a day. With insufficient effect from the therapy carried out by Fepranon, the daily dosage can be increased to four tablets.

The average duration of treatment with Fepranon is six to ten weeks. You can repeat the course of treatment after three months.

Children over 12 years old are usually prescribed half the adult dosage.

Side effects of Fepranon

The drug Fepranon reviews can cause the following undesirable side effects:

Weakness;
dry mouth;
Tachycardia;
Skin itching;
Insomnia;
Conjunctivitis;
Rhinitis;
Headache;
constipation or diarrhea;
Euphoria;
Increased blood pressure;
Deterioration of mood;
Irritability;
Nausea;
Rash;
Vomit;
swelling of the eyelids;
myalgia;
polyuria;
Dysuria.

With a long The use of Fepranon according to reviews may cause a decrease in potency, alopecia, in some cases - drug dependence.

When taken in high doses, Fepranon can lead to the development of:

hyperreflexia;
Tremor;
confusion;
tachypnea;
collapse;
hallucinations;
Convulsions (on the background of epilepsy).

forced diuresis;
Gastric lavage;
inducing vomiting;
Taking psychoactive drugs (with the development of severe mental disorders) and beta-blockers (with tachycardia);
Artificial ventilation of the lungs (if symptoms of respiratory failure appear).

drug interaction

Fepranone can weaken the hypoglycemic effect of insulin and the hypotensive effect of guanethidine.

The risk of developing a hypertensive crisis increases with the simultaneous use of Fepranone with MAO inhibitors.

Glucocorticosteroid. Dehydrated analog of hydrocortisone, inhibits the release of interleukin1, interleukin2, interferon gamma from lymphocytes and macrophages. It has anti-inflammatory, anti-allergic, desensitizing, anti-shock, anti-toxic and immunosuppressive effects.

It suppresses the release of adrenocorticotropic hormones and beta-lipotropin by the pituitary gland, while not reducing the concentration of circulating beta-endorphin. It inhibits the secretion of thyroid-stimulating hormones and follicle-stimulating hormones.

Increases the excitability of the central nervous system, reduces the number of lymphocytes and eosinophils, increases the number of red blood cells (stimulates the production of erythropoietins).

Interacts with specific cytoplasmic receptors and forms a complex that penetrates the cell nucleus and stimulates the synthesis of matrix ribonucleic acid; which, in turn, induces the formation of proteins, including lipocortin, mediating cellular effects.

Lipocortin inhibits phospholipase A2, inhibits the release of arachidonic acid and inhibits the synthesis of endoperoxides, Pg, leukotrienes, which contribute to inflammation, allergies and other similar processes.

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

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

Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract; increases the activity of glucose-6-phosphatase, which leads to an increase in the flow of glucose from the liver into the blood; increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases, which lead to the activation of gluconeogenesis.

Water-electrolyte metabolism: reduces the absorption of Ca2+ from the gastrointestinal tract, "washes" Ca2+ from the bones, increases the excretion of Ca2+ by the kidneys, retains Na+ and water in the body, stimulates the excretion of K+ (MKS activity).

The anti-inflammatory effect is based on the inhibition of the release of inflammatory mediators by eosinophils; inducing the formation of lipocortin and reducing the number of mast cells that produce hyaluronic acid; as well as a decrease in capillary permeability; stabilization of cell membranes and organelle membranes (especially lysosomal).

The antiallergic effect develops due to suppression of the development of lymphoid and connective tissue, suppression of the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, changes in the body's immune response, a decrease in the number of circulating basophils, and a decrease in the amount of T- and B- lymphocytes, mast cells, reducing the sensitivity of effector cells to allergy mediators, inhibition of antibody production.

In chronic obstructive pulmonary disease, the effect of the drug is mainly based on inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium, inhibition of inflammatory processes, inhibition of development or prevention of mucosal edema, deposition of circulating immune complexes in the bronchial mucosa, and inhibition of erosion and desquamation of the mucous membrane. The drug reduces the viscosity of mucus by inhibiting or reducing its production, increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchi to endogenous catecholamines and exogenous sympathomimetics.

The anti-shock and antitoxic effect is associated with an increase in blood pressure (due to an increase in the concentration of circulating catecholamines and the restoration of adrenoreceptor sensitivity to them, as well as vasoconstriction), with a decrease in the permeability of the vascular wall, membrane-protective properties, and activation of liver enzymes involved in the metabolism of endo- and xenobiotics.

The immunosuppressive effect of the drug is due to inhibition of the release of cytokines (interleukin1, interleukin2; interferon gamma) from lymphocytes and macrophages.

The drug inhibits the synthesis and secretion of adrenocorticotropic hormones and, secondarily, the synthesis of endogenous glucocorticosteroids, and also inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

Indications

Systemic connective tissue diseases (dermatomyositis, rheumatoid arthritis, systemic lupus erythematosus, periarteritis nodosa, scleroderma).

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

Rheumatic fever, acute rheumatic fever.

Asthmatic status, bronchial asthma.

Acute and chronic allergic diseases: hay fever, allergic rhinitis, urticaria, allergic reactions to food and drugs, serum sickness, angioedema, drug exanthema.

Skin diseases: toxidermia, seborrheic dermatitis, exfoliative dermatitis, eczema, psoriasis, pemphigus, atopic dermatitis, diffuse neurodermatitis, contact dermatitis (with damage to a large surface of the skin), toxic epidermal necrolysis (Lyell's syndrome), malignant exudative erythema (Stevens-Johnson syndrome) , bullous dermatitis herpetiformis.

Cerebral edema (including on the background of a brain tumor or associated with surgery, radiation therapy or head trauma) after prior parenteral use.

Allergic eye diseases: allergic forms of conjunctivitis, allergic corneal ulcers.
Inflammatory eye diseases: optic neuritis, sympathetic ophthalmia, severe indolent anterior and posterior uveitis.

Primary or secondary adrenal insufficiency (including the condition after removal of the adrenal glands).

Congenital adrenal hyperplasia.

Kidney diseases of autoimmune origin (including acute glomerulonephritis); nephrotic syndrome.
Subacute thyroiditis.

Diseases of the hematopoietic organs: acute lympho- and myeloid leukemia, lymphogranulomatosis, agranulocytosis, panmyelopathy, autoimmune hemolytic anemia, congenital (erythroid) hypoplastic anemia, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocytic anemia).

Pulmonary diseases: sarcoidosis of the second or third stage, acute alveolitis, pulmonary fibrosis.
Tuberculous meningitis, pulmonary tuberculosis, aspiration pneumonia (in combination with specific chemotherapy).

Beryllium, Loeffler's syndrome (not amenable to other therapy).

Malignant tumor of the lung (in combination with cytostatics).

Multiple sclerosis.

Diseases of the gastrointestinal tract: Crohn's disease, ulcerative colitis, local enteritis.

Prevention of graft rejection.

Hypercalcemia against the background of oncological diseases, nausea and vomiting during cytostatic therapy.

Myeloma.

In the case of using the drug for "vital" indications for a short period of time, the only contraindication is hypersensitivity to prednisolone or the components of the drug.

Apply with caution:

Post-vaccination period (a period of eight weeks before and two weeks after vaccination), lymphadenitis after vaccination against tuberculosis (BCG).

Immunodeficiency states (including AIDS or HIV infection).

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

Diseases of the cardiovascular system, including recent myocardial infarction (in patients with acute and subacute myocardial infarction, a focus of necrosis may spread against the background of a slowdown in the formation of scar tissue, which can lead to rupture of the heart muscle), decompensated chronic heart failure, hyperlipidemia, arterial hypertension.
Endocrine diseases: hypothyroidism, diabetes mellitus (including impaired carbohydrate tolerance), Itsenko-Cushing's disease, thyrotoxicosis.

Severe chronic renal and / or liver failure, nephrourolithiasis.
Hypoalbuminemia and conditions predisposing to its occurrence.

And also: during pregnancy and lactation, with acute psychosis, systemic osteoporosis, myasthenia gravis, against the background of obesity (third or fourth stage), with poliomyelitis (with the exception of the form of bulbar encephalitis), open- and closed-angle glaucoma.

Not only the severity of side effects, but also the frequency of their development depends on the duration of use, the size of the dose used and the possibility of observing the circadian rhythm of prescribing the drug.

endocrine system: Itsenko-Cushing's syndrome (dysmenorrhea, amenorrhea, moon-shaped face, hirsutism, pituitary-type obesity, increased blood pressure, myasthenia gravis, striae), decreased glucose tolerance, "steroidal" diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, delayed sexual development in pediatric patients;
digestive system: "steroid" ulcer of the stomach and duodenum 12, pancreatitis, vomiting, nausea, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, hiccups, flatulence, increased or decreased appetite. In rare cases, an increase in the activity of "liver" transaminases and alkaline phosphatase;
cardiovascular system: increased blood pressure, development (in predisposed patients) or increased severity of chronic heart failure, arrhythmias, bradycardia (up to cardiac arrest); ECG changes characteristic of hypokalemia, thrombosis, hypercoagulability. In patients with acute and subacute myocardial infarction, there is a risk of spreading the focus of necrosis against the background of slowing down the formation of scar tissue, as a result of which rupture of the heart muscle is possible;
nervous system: insomnia, nervousness or anxiety, delirium, hallucinations, disorientation, euphoria, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, cerebellar pseudotumor, headache, dizziness, convulsions, vertigo;
sensory organs: increased intraocular pressure with possible damage to the optic nerve, posterior subcapsular cataract, a tendency to develop secondary bacterial, fungal or viral eye infections, exophthalmos, trophic changes in the cornea;
metabolism: weight gain, increased sweating, increased excretion of Ca2 +, hypocalcemia, negative nitrogen balance (increased protein breakdown);
caused by ISS activity: hypernatremia, fluid retention and Na + (peripheral edema), hypokalemic syndrome (unusual weakness and fatigue, hypokalemia, arrhythmia, myalgia or muscle spasm);
musculoskeletal system: osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and femur), retardation of growth and ossification processes in children (premature closure of epiphyseal growth zones), rupture of muscle tendons, decrease in muscle mass (atrophy), " steroid myopathy;
skin and mucous membranes: hyper- or hypopigmentation, acne, striae, delayed wound healing, thinning of the skin, a tendency to develop pyoderma and candidiasis, ecchymosis, petechiae;
allergic reactions: local allergic reactions, generalized allergic reactions (skin itching, anaphylactic shock, skin rash);
others: the development or exacerbation of infections (the appearance of this side effect is possible with the combined use of the drug with immunosuppressants and vaccination), "withdrawal" syndrome, leukocyturia.

Application and dosage

With substitution therapy, the drug is prescribed at a dose of 20-30 milligrams per day.

The maintenance dose is 5-10 milligrams per day.

In the case of certain diseases (nephrotic syndrome, some rheumatic diseases), the drug is prescribed in higher doses. Treatment should be stopped slowly, gradually reducing the dose.

If patients have a history of psychosis, then high doses of the drug are prescribed under the strict supervision of a physician.

Doses for pediatric patients: the initial dose is 1-2 milligrams per kilogram of body weight per day, for four to six doses, the maintenance dose is 0.3-0.6 milligrams per kilogram of body weight per day.

Most or all of the dose should be given in the morning. This is due to the daily secretory rhythm of glucocorticosteroids.

special instructions

Before starting treatment, it is necessary to examine the patient to identify possible contraindications.

The clinical examination should include:

study of the cardiovascular system;
x-ray examination of the lungs;
examination of the stomach and duodenum;
study of the urinary system;
study of the organs of vision.

Before starting and during steroid therapy, it is necessary to control the complete blood count, the concentration of glucose in the blood and urine, and the plasma concentration of electrolytes.
With intercurrent infections, septic conditions and tuberculosis, simultaneous antibiotic therapy is necessary.

Immunization should not be carried out during the treatment period.

The syndrome of "cancellation" of glucocorticosteroids occurs when the drug is suddenly discontinued (especially in the case of previous use of high doses). This syndrome is expressed by nausea, decreased appetite, asthenia, lethargy, generalized musculoskeletal pain.

After discontinuation of the drug, relative insufficiency of the adrenal cortex persists for several months. If stressful situations arise during this period, glucocorticosteroids can be prescribed (according to indications) for a while, if necessary, in combination with the ISS.

Patients of childhood who during the period of treatment were in contact with patients with measles or chicken pox should be given specific Ig for prophylaxis.

To reduce side effects, the appointment of anabolic steroids, an increase in the intake of K + with food, is justified.

In the case of Addison's disease, the simultaneous administration of barbiturates should be avoided, since in this case there is a risk of developing acute adrenal insufficiency (Addisonian crisis).
Use during pregnancy in the first trimester and during lactation, the drug is prescribed based on the expected therapeutic effect and the negative impact on the fetus and child.

With prolonged therapy during pregnancy, there is a risk of impaired fetal growth. When treated with the drug in the third trimester of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

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

Sources

http://ArtrozamNet.ru/prednizon/
http://www.neboleem.net/fepranon.php
http://opuholi.org/lekarstva/prednizolon.html

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