Glucocorticoid hormones — what it is, list of drugs

General information

 

Cortical substance of the adrenal glands produces 3 types of hormones:

  • controlling potassium-sodium exchange (mineralocorticoid);
  • responsible for the reproductive function (sex steroids);
  • corticosteroids, which is responsible for the regulation of intermediate metabolism.

Production of corticosteroids is controlled by the pituitary and hypothalamus, but is carried out in a pair of endocrine organs located above the kidneys, for which he received its name.

For the first time, these hormones were applied as medicines in 40 years of the last century, they got their name, due to its ability to regulate glucose metabolism. Further clinical studies showed that hormones do not only affect lipid, carbohydrate, protein metabolism, and regulate the activity of the circulatory system, kidneys, immune system, participate in development and exchange of bone tissue, a considerable impact on the Central nervous system.

The use of hormones in a natural way, despite the significant effectiveness has been limited due to the large amount of negative side effects.

Structural and functional analogs

Glucocorticoids are structural and functional analogs of those hormones that are synthesized in the adrenal cortex, in its beam area. Drugs in this group are divided into:

  • glucocorticoids are of natural origin (cortisone is a prodrug that forms an active metabolite, hydrocortisone);
  • synthetic drugs, derived from hydrocortisone (cortisol) by attaching to the molecule of different chemical compounds.

They also determine the difference in the applied areas, significant change in the properties that gives the attached chemical.

Fludrocortisone formed by adding a fluorine atom to the eye, at 12 times the glucocorticoid activity and 125 times the mineralocorticoid cortisone.

Dexamethasone, added to the molecule of fludrocortisone 16-methyl group, retains glucocorticoid activity but insignificant mineralocorticoid has.

Methylprednisolone, to which was added 1 radical, exceeds the prodrug 5 times according to the degree of glucocorticoid activity.

Artificial pharmaceutical analogues of the hormones of the adrenal cortex, used in medicine, in severe cases, when drug benefits are greater than the harm from their side-effects. Sometimes, due to the extreme condition, or concomitant severity of other way except the use of hormonal therapy, no. Preparations of corticosteroids are used to provide:

  • anti-inflammatory;
  • desensitizing agents;
  • antitoxic;
  • antishock;
  • immunosuppressive action.

It’s not all medicinal effects that can be obtained at the calculated dose, and an individual approach to the appointment. In diseases of the spine glucocorticoid drugs are used and because of their ability to greatly increase the effect of medicines used in complex therapy simultaneously.

The main principle of prescribing GK – achievement of the maximum effect at the lowest possible doses. For this purpose, and the development of synthetic analogs having a much more pronounced effect, which allows to reduce the dosage, and the duration of the designated course.

Classification and division of the drugs

Generally accepted classification of drugs, with the use of adrenal hormones, are still not developed. Practitioners are divided into CC on the place and method of application. According to this, it is highly conditional division into subgroups, there are the following types of drugs:

  • injectable;
  • preformed;
  • means of the local application in the form of ointments, creams, gels and suspensions.

The second principle of allocation categories is to split by the main active substance in the drug. Medications differenciate according to dominant component:

  • the prednisolone;
  • to methylprednisolone;
  • the betamethasone;
  • dexamethasone, etc.

There is a clinical difference of hormonal drugs on the duration of exposure, which is established through scientific research. Glucocorticoids are divided into funds:

  • a short exposure;
  • the average duration;
  • long (prolonged) actions.

Funds short exposure to apply hydrocortisone, which is a synthetic analogue of the hormone. Due to the relative invariability of its composition, it has virtually no effect on water-salt metabolic balance, and do not interferes with cellular metabolism.

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Betamethasone and dexamethasone, changed the structure, is able to exert long-term effect, whereas prednisolone and methylprednisolone treat drug expectancy effects.

In medicine, there is another unit glucocorticoids, which distinguishes between them by using the basic substance, and involves the allocation:

  • endogenous (natural) compounds;
  • synthetic analogues (oily);
  • synthetic analogues (fluorinated).

None of the existing grades, because of the wide use of various forms of GK, does not include the full features of hormonal preparation and is used in professional terminology specific qualification of the scientific community.

Hormones internal exposure

Drugs internal actions are also divided into:

  • intranasal (through the nose used);
  • parenteral;
  • orally (swallowed when taken);
  • inhalation.

This division of drugs provides a clear gradation of diseases, in imposing forms of the drug. Intranasal is usually used to treat:

  • allergic rhinitis;
  • idiopathic inflammation of the nasal mucosa;
  • when polyps in the nose.

Parenterally applicable in diseases of the adrenal, some diseases of the thyroid gland, and other complex pathologies.

Inhalation drugs are specificity effects, and are prescribed for complex dysfunctions of the respiratory system. Bronchial asthma, COPD, allergic rhinitis being treated by these means, as a basic therapy. Of the most widely used inhaled medicines include:

  • triamcinolone acetonide;
  • beclomethasone dipropionate;
  • mometasone furoate;
  • budesonide;
  • fluticasone propionate.

Cases of serious respiratory diseases made to undertake clinical trials of new inhaled drugs for the treatment of asthma during pregnancy. They showed that the treatment of the drug in pairs at the place of pathology not only increased the incidence of children with endocrine diseases, but also gave the opportunity to celebrate their appearance in children who were born to mothers who suffered from asthma, and has not used inhalers to alleviate his condition.

The emergence of intranasal and inhaled forms of release of drugs have saved patients from some of the risks common with parenteral drugs using GC.

With the development of therapeutic forms and new synthetic analogues become less dangerous the use of glucocorticoid hormones, which are used without effects on the internal organs and systems of exchange.

Pharmacodynamics and mechanism of action

Natural link hormones produced by the adrenal glands koordiniruyutsya by the pituitary and hypothalamus, and is carried out with complementary matching the specific code of the hormone receptor cells. The match between BCS can be implemented in a cellular membrane, and outside if the hormone cannot diffuse into the cell. GK contact special glucocorticoid receptors inside the cell membrane than is caused by the emergence of RNA and the concomitant synthesis of regulatory proteins.

There are cytostatic mechanism that can suspend the effects of hormones and enzymes and chemicals that speed up the process of interaction.

Main effects achieved by the use of corticosteroids in the human body include the following:

  • violation of the synthesis of inflammation mediators (prostaglandins and leukotrienes) by blocking and oppression of the enzyme phospholipase;
  • in a different dosage providing immunosuppressive and immunostimulatory effects, the inhibition of the production of antibodies, production of lymphokines and cytokines;
  • obstacle the conclusion of histamine, stabilize the membranes of fat cells;
  • impact on the metabolism of proteins, carbohydrates, calcium, fats, water and electrolyte metabolism;
  • an increased sensitivity of blood vessels and cardiac muscle to noradrenaline and adrenaline;
  • stimulation of the formation of red blood cells and platelets;
  • inhibition of production of white blood cells, basophils and eosinophils;
  • effects on other hormones, including the sex, luteinizing, thyroid hormones.

If ingestion is rapidly absorbed in the small intestine, reaching maximum concentration in less than an hour. The parenteral introduction of variable, and provides the features of the drug. Are excreted through the kidneys in the blood bind to proteins partially gestructureerde liver. Method of administration depends on the nature of the product and the characteristics of the disease. In the treatment of musculoskeletal system are used intra-articular injections.

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The list of hormonal drugs

The list of drugs of the group of glucocorticoid hormones quite extensive, but in clinical practice the most common are:

  • Cortisone;
  • Prednisone;
  • Methylprednisolone;
  • Triamcinolone;
  • Dexamethasone;
  • Betamethasone.

Analogues of the drugs under commercial names, or specific species with a modified form, are less common, and require learning to use the application, with a clear description of the contraindications and indications structure chemical formula and characteristics of destination.

Hormones belong to list B, require certain storage conditions. Before independent use of such drugs should consult with your doctor to pay special attention to the possibility, or protivopokazannosti medicines in use for newborns, children, pregnant women.

All preparations of glucocorticoid hormones described in the Anatomic-therapeutic-chemical classification (ATC), which has a hierarchical structure and facilitates the search for the desired medication. Any drug of this group is indispensable clinical testing, and is described by specialists.

Indications for use

Today has been well studied not only the adverse and therapeutic effects, but also the interaction of GK with many medications, the dosage, the developed scheme of complex therapy. This made possible the use of drugs in many branches of medicine, as basic and auxiliary drugs.

Pathological condition in which there are undoubted benefits Ledger will be an incredibly long list of chronic, systemic and acute pathologies. In rheumatology, they are used to treat:

  • systemic lupus erythematosus;
  • ankylosing spondylitis;
  • systemic sclerosis;
  • polymyalgia rheumatica.

The glucocorticoids used in the treatment of vasculitis, and pyelonephritis, in endocrinology they treat:

  • the adrenal insufficiency;
  • hyperthyroidism, and ACTH deficiency.

In gastroenterology:

  • ulcerative colitis;
  • severe forms of hepatitis;
  • Crohn’s disease in the acute stage.

But the scope of hormonotherapy drugs is not limited. Cardiology uses:

  • some types of pericarditis;
  • postirochnaja and leukocyte nonspecific myocarditis.

In chest diseases:

  • bronchial asthma;
  • eosinophilic pneumonia;
  • alveolitis and bronchiolitis;
  • sarcoidosis of the lungs.

In Hematology hormonal therapy to treat thrombocytopenia and anaemia.

GK – essential drugs of choice in acute conditions and in transplantation. Despite the contraindications, and side effects, glucocorticoids are widely used, and sometimes indispensable tool, in severe lesions and acute conditions. In the treatment of diseases of the spine are used for the treatment of:

  • degenerative disc disease;
  • pain;
  • non-infectious arthritis;
  • ankylosing spondylitis;
  • injuries of the spine and its membranes.

The creation of synthetic products has accelerated and increased the impact of this group of drugs than further expanded the scope of their activities.

Contraindications to the use of hormonal drugs

There are certain contraindications to the administration of drugs in a specific form. Forbidden intra-articular injections of hormones with:

  • diseases affecting blood clotting;
  • severe osteoporosis;
  • significant infectious process, systemic, or local character.

An obstacle to the holding of such injections can be articular fracture, or severe destruction of the joint. Conditionally recommended GK (this is called relative contraindications), when:

  • diabetes;
  • ulcer of stomach and duodenum;
  • hypertension;
  • heart failure;
  • mental disorders;
  • epilepsy.

The recommended use of glucocorticoids in severe threatening conditions, as an effective method of exposure, has led to the fact that, most often, relative contraindications in critical situations are not considered. However, the purpose of hormonotherapy drugs in situations less severe emergency, doctors have to consider some General parameters of the physical and pathological condition of man.

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By far the GK application not recommended for:

  • tuberculosis;
  • syphilis;
  • viral lesions of the eye and glaucoma;
  • herpes, and systemic mycosis.

Intranasal drug may not be recommended if there are repeated nosebleeds, hypersensitivity to drugs, or bleeding diathesis.

Any use of preparations containing adrenal hormones or their synthetic analogues, should be made only on medical advice, and under strict medical supervision.

Side effects the use of hormonal therapy

One of the discoverers of the therapeutic effects of glucocorticoids hormones, said they should be used only if the expected healing the result will exceed the negative impact.

The emergence of synthetic analogues acting much faster, reduced side effects from the use of glucocorticoids, but did not rule out the possibility of their development. To prevent pronounced negative effects of the use of GK, a prophylactic prescription of necessary medications.

As manifestations of the adverse effects of drugs with analogues of natural hormones of the adrenal cortex, may occur:

  • violation of lipid volume and a significant increase of body weight;
  • increases susceptibility to infections and noted their prolonged flow;
  • develops pancreatitis;
  • amenorrhea;
  • violations of linear growth and puberty in children;
  • steroid diabetes and steroid ulcers of the digestive system;
  • osteoporosis and compression fractures, the treatment of diseases of the musculoskeletal system.

Emotional state, especially in women, is much worse, there is aggressiveness, excitability and drowsiness at the same time expressed the mood swings. Hormonal disturbances caused by significant doses of drugs that can cause infertility, loss of libido, sleep disorders. Some side effects are well known to modern medicine, but their appearance at the present day can neither prevent nor correct.

So, when intra-articular injection of drugs, may occur damage of the nerve trunks, the calcination of the joint, or atrophy, destruction (steroid arthropathy), tendon rupture. This inevitably leads to disability and limitation, but it saves lives. This is due to careful application hormonotherapy drugs, and their replacement in cases of moderate severity, non-steroidal anti-inflammatory drugs which also have side effects, but less pronounced.

Especially therapeutic use of hormones and precautions

Corticosteroids, because of their wide use in various branches of medicine, for the treatment of various diseases. Almost all known States of the developed therapeutic schemes and the Protocol in the States of varying severity.

The duration of action of the drug, the degree of rekomendovano, the duration of treatment, short duration, or prolongation, and even a certain dosage, for everything is in the competence of the doctor who knows how to deal with a specific medication.

That is why so much has been said about the non-appointment of the synthetic hormone drugs, on purely caution of their application, careful and thoughtful treatment of drugs of this group. Any, the remedy, in case of incorrect assignment, and excessive intake can bring significant harm to the human body. Therefore, to produce treatment needs only a doctor familiar with all the subtleties of the impact of a specific preparation.

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