What is dexamethasone used for? Medicinal reference book geotar

Dexamethasone is a hormonal drug, which in modern medicine is considered as one of the vital pharmaceuticals belonging to the group of synthetic glucocorticosteroids. Dexamethasone is able to penetrate the tissues of all organs and systems, including the brain and nervous system, and affect the entire body. In severe conditions - shock, acute systemic allergies, severe inflammation, pathological immune reactions, the medicine can save a life.

For treatment different type diseases Dexamethasone is produced in 4 dosage forms, the therapeutic basis of which is dexamethasone sodium phosphate.

This substance is a synthetic analogue of the natural steroid hormone, which is produced in the body by the adrenal glands.

Basic forms:

  1. Tablets of 0.5 mg (0.5 mg of the active ingredient) in a pack of 10 units.
  2. Injection solution (0.4%) in 1 ml ampoules containing 4 mg of active ingredient (5 or 25 units per pack). It is used for injection into a muscle, vein (stream or drip), inside the joint, into the soft tissues surrounding it, into the fiber of the eyeball.
  3. Dexamethasone eye drops (ear) 10 ml with an active substance concentration of 0.1% (1 mg in 1 ml).
  4. Eye ointment - tube 2.5 g.

All forms of the drug contain as auxiliary components substances that are necessary for stabilizing, shaping and transporting dexamethasone to the painful focus, as well as preservatives and additives that facilitate the absorption of the drug.

Each treatment form has its own purposefulness in application, certain indications and contraindications, so you should not treat yourself - only a specialist is able to develop desired scheme therapy, calculate the dose and frequency of use.

The drug is dispensed by prescription, where the name of the drug in Latin is denoted as Dexamethasoni.

Pharmacological properties and pharmacokinetics

Medicinal properties

The mechanism of the therapeutic action of the drug is based on its ability to create a high concentration of the component in the blood and foci of inflammation, penetrate into all tissues and act at the cellular level.

This allows the active substance to work in the brain and nerve tissues, relieve swelling of the brain, lungs in case of hemorrhage, poisoning, trauma, tumors, removing the patient from a life-threatening state of shock, slow down the course of cancer processes, and eliminate the manifestations of acute allergies.

Glucocorticosteroid activates a series of processes that lead to a decrease in the permeability of the walls of blood vessels, strengthening the protection of cell membranes and blocking inflammation at any stage of development.

By suppressing the acute reaction of the immune system to allergens, the drug stops the development of an allergic reaction, including anaphylactic shock, reduces the degree of swelling of the mucous membrane of the respiratory organs, bronchi, restoring the flow of air during laryngeal edema or an asthmatic attack.

At the same time, the drug inhibits the production of histamine, stopping the pathological manifestations of allergies.

Slows down the formation of cicatricial changes in the tissues of various organs.

Absorption and elimination from the body

The corticosteroid is actively and almost completely absorbed not only after injection, but also after internal administration. Bioavailability or the amount of a therapeutic substance reaching the focus of exposure is 77 - 79%, due to which the therapeutic effect of the drug is maximum.

In the blood, 65 - 70% of dexamethasone binds to the transport protein transcortin, which provides a high concentration of the drug in the blood. With the blood flow, the protein delivers dexamethasone throughout the body, penetrating into the intracellular spaces of tissues.

The largest amount of the active substance in the blood, providing the maximum therapeutic effect, is observed in the range from 40 to 90 minutes, depending on the method of application.

The active substance is processed by liver enzymes to inactive intermediates. It is removed from the body along with urine and in small amounts (about 10%) is excreted by the intestines. A small amount of dexamethasone passes into women's milk, which should be taken into account when prescribing the drug to a nursing mother.

Why is the drug prescribed

The action of the drug is used in many diseases of internal organs, systemic, autoimmune pathologies, in diseases of the joints, eyes, skin and in many other areas of medicine.

The list of pathological conditions that require Dexamethasone injections or tablets include:

  • life-threatening shock conditions of all forms, including pain shock, toxic, cardiogenic, allergic, postoperative, blood transfusion (after blood transfusions);
  • swelling of brain tissues (with hemorrhage, meningitis, tumors, encephalitis, trauma, surgery);
  • an attack of bronchial asthma or long-term asthmatic status;
  • lung pathology: berylliosis, tuberculosis, alveolitis, pneumonia, Leffler's syndrome (resistant to other medicines);
  • allergic reactions: urticaria, Quincke's edema, hay fever, allergy to drugs and products, serum sickness;
  • endocrine disorders - adrenal insufficiency, diseases thyroid gland, thyrotoxic crisis, thyroiditis, adrenogenital syndrome;
  • autoimmune diseases - rheumatic heart disease, multiple sclerosis, systemic lupus erythematosus, pemphigus, scleroderma, systemic vasculitis;
  • pain with inflammation of the reproductive organs, including prostatitis; various types of myositis;
  • intractable skin diseases - eczema, various types of dermatitis, psoriasis, toxidermia, Lyell and Stevens-Johnson syndromes, discoid lupus erythematosus, keloid scars (topical application);
  • allergic and inflammatory eye lesions: scleritis, corneal ulcer, different types conjunctivitis (except purulent), uveitis, keratitis, blepharitis, inflammation of the optic nerve, ophthalmopathy against the background of diabetes mellitus;
  • swelling of the larynx and glottis with acute croup;
  • inflammation of the joints of different course: arthritis different forms, osteoarthritis, polyarthritis, ankylosing spondylitis, bursitis, tendosynovitis and others;
  • hematopoietic disorders: Addison's disease, lymphoma, agranulocytosis, anemia of various origins, thrombocytopenia;
  • critical conditions in case of damage to the gastrointestinal system: enteritis, including granulomatous, hepatitis and hepatic coma, ulcerative colitis;
  • allergic-toxic reaction with massive helminthic aggression;
  • lesions of the esophagus and stomach in case of poisoning with alkalis, acids to suppress inflammation and prevent cicatricial narrowing;
  • acute renal pathologies - glomerulonephritis, nephrotic syndrome;
  • malignant processes in the lungs, leukemia, lymphocytic leukemia, multiple myeloma;
  • nausea and vomiting while taking cytostatics.

Application instruction of Dexamethasone

The treatment regimen with Dexamethasone and the dosage regimen are established only by the attending physician in order to obtain the maximum therapeutic effect with a minimum risk of unwanted side reactions.

Tablets

Usually prescribed for the chronic course of the pathology or after the removal of an acute condition.

The dose is determined for each patient separately, taking into account the nature and severity of the disease, the planned duration of the course, age, drug tolerance and the patient's response.

The usual minimum effective dose for adults per day is 0.5-9 mg. A small dose is taken at a time, a large dose is divided into 3-4 doses. The largest amount of dexamethasone per day should not exceed 10-15 mg.

The average maintenance dose per day is 0.5 - 3 mg.

With long-term use of the drug in a large dose, the drug is combined with food. In this case, between meals, it is desirable to use means that reduce gastric acidity (antacids).

After the patient's condition improves, the dose should be gradually reduced - every 3 days by 0.5 mg to a maintenance dose.

The duration of the course of application ranges from 3 - 5 days to several months.

It is unacceptable to abruptly stop treatment with Dexamethasone, so as not to cause a withdrawal syndrome,

which is expressed in an exacerbation of the underlying disease and painful manifestations of the withdrawal syndrome (weakness, weight loss, vomiting, diarrhea, drop in blood sugar and pressure, muscle pain, fever).

Dosing for children

Juvenile patients are prescribed in accordance with body weight or body area, age and severity of the pathological process.

The approximate children's dose per day is 0.0833 - 0.333 mg per 1 kilogram of the child's body weight. Thus, according to the calculation, a child weighing 25 kg can receive a maximum of 0.333 x 25 = 8.36 mg of the drug per day, divided into 3-4 doses. The minimum dose that will give a therapeutic effect for a small patient with such a weight is 0.0833 x 25 = 2.08 mg.

More precisely, the children's dose is calculated by the surface area of ​​the child's body at the rate of 0.0025 - 0.0001 mg per 1 square meter per day in 3 - 4 doses, depending on age.

Injections

Dexamethasone injections for systemic diseases are given into the muscle, or administered intravenously, which is preferable in life-threatening situations when the risk to the patient's life is high. The solution immediately enters the bloodstream, providing a rapid therapeutic effect.

For emergency short-term or single use of the drug, only intolerance to any of the substances in the composition of Dexamethasone is considered a contraindication. In critical situations, the side effects of the drug are neglected.

Adults in acute and emergency conditions per day can enter 3-4 times 4-20 mg. In the acute phase of the pathology, as well as at the beginning of therapy, higher doses of corticosteroid are used. The highest dose is 80 mg, but in critical cases it is higher.

Children's doses for intramuscular injection are calculated according to the weight of the child at the rate of 0.02776 - 0.16665 mg per kilogram of body weight after 12 - 24 hours.

The duration of injection with a gradual decrease in dose usually does not exceed 3-4 days, after which the patient is transferred to taking tablets at a maintenance dose.

Drops eye and ear

In acute inflammation, patients over 12 years of age for 48 hours 4-5 times a day drip an ophthalmic solution over the lower eyelid, 1-2 drops. When the degree of inflammation decreases, the treatment is continued for another 4-6 days, reducing the frequency of instillation to 3 times a day.

In chronic processes, the remedy is used twice a day for no longer than 20-40 days.

In case of allergic eye damage, similar doses are used up to 5 times a day for 48 hours, then they gradually reduce the frequency of instillation to 2 times a day and stop treatment for 7 to 12 days.

For patients 6-12 years old, to eliminate inflammatory and allergic phenomena, 1 drop is administered per eyelid up to 4 times a day for no longer than 10 days.

The solution is used from the 8th day after the operation to eliminate cataracts, retinal detachment, strabismus up to 4 times a day for 2 to 4 weeks.

In case of inflammation of the ear (otitis) of a non-viral nature, 3-4 drops are instilled into the sore ear in a warm form (children 1-2) three times a day.

The lenses are removed before instillation. You can put them on only after 15 minutes.

Dexamethasone eye ointment

It is used for the same indications as ophthalmic drops in patients from 6 years of age. A strip of ointment 10-15 mm long is carefully placed behind the lower eyelid 3 times a day. The maximum duration of treatment is not more than 20 days.

Use during pregnancy and lactation

In a study on small mammals, it was found that Dexamethasone, like many other hormonal agents, penetrates through the placenta into the tissues of the embryo and can lead to the death of the embryo at an early stage and fetal deformities. The class of action of the drug on the fetus is C (according to the FDA).

Therefore, Dexamethasone is used during pregnancy only if there is a threat to the life of the mother.

If the pregnant woman received Dexamethasone, after childbirth, monitoring of the health of the baby is necessary - since the child may be diagnosed with adrenal dysfunction, which requires immediate intensive treatment.

Since the drug passes into women's milk, breastfeeding mothers need to switch to artificial feeding or refuse the drug.

With long-term use of ointment or drops, partial absorption of the drug into the blood occurs. Therefore, these dosage forms are allowed to be used by expectant mothers only after 12 weeks of gestation, in very short courses up to 3 days and in minimal doses.

During lactation, treatment with ointment and drops is acceptable for no longer than 7 to 10 days.

Can I drink alcohol while taking the drug

Treatment with Dexamethasone is incompatible with the use of alcohol, otherwise the consequences of parallel use will be very serious.

There is a high probability of such severe manifestations as:

  • indomitable diarrhea;
  • partial loss of vision;
  • abdominal pain, vomiting;
  • acute pain at the injection site;
  • redness of the skin on the chest, urticaria, acne rash on the face;
  • ulceration of the mucous membrane of the digestive organs;
  • internal bleeding.

If the patient has a serious alcohol dependence and is not able to give up alcohol for the duration of therapy, other drugs are required.

Drug interactions with other drugs

The combination of Dexamethasone and non-hormonal anti-inflammatory drugs (Aspirin, Paracetamol) increases the likelihood of formation or deepening of ulcers of the digestive organs.

The action of the corticosteroid is reduced with concomitant use:

  • antacids that reduce the absorption of the treating substance in the stomach;
  • growth hormone;
  • drugs from a series of inducers of the CYP3A4 isoenzyme (for example, phenobarbital, phenobarbital, rifabutin, rifampicin, carbamazepine);
  • aminoglutethimide and ephedrine.

With parallel use, Dexamethasone is capable of:

  • reduce the therapeutic effect of insulin, hypoglycemic drugs, high blood pressure drugs, Praziquantel and natriuretic diuretics;
  • enhance the effect of Heparin, Albendazole.
  • increase the excretion of potassium when combined with diuretics; influence the action of anticoagulants based on coumarin;

Ketoconazole-based antifungals, birth control pills, and macrolide antibiotics can prolong the urinary excretion of dexamethasone and increase the frequency and severity of adverse reactions.

The combination of a medication with Thalidomide can provoke the development of Lyell's syndrome, with anticholinergics - glaucoma, with antipsychotics and Azathioprine - cataracts; with cardiac glycosides - arrhythmias.

The combination with anabolic steroids, androgens, contraceptives, estrogens can cause increased facial hair, chest, edema, acne.

The use of antiviral vaccines in parallel with Dexamethasone therapy increases viral aggressiveness against the background of a decrease in immunity.

Contraindications, side effects and overdose

Contraindications

If Dexamethasone is urgently required to save a life, all contraindications (except drug intolerance) and possible adverse reactions are ignored.

For any severe infections, it is permissible to prescribe Dexamethasone injections and tablets only with the simultaneous specific treatment of these diseases.

Contraindications for intra-articular injections:

  • tendency to bleeding;
  • intra-articular fracture of the bone;
  • infection, osteoporosis, instability, joint deformity, bone destruction, ankylosis;
  • surgery (arthroplasty);
  • necrosis of the articular bone;
  • low efficiency after 2 previous injections.

Contraindications for local forms (ointment, drops):

  • eye damage with a tubercle bacillus, fungus, viruses, including herpes;
  • glaucoma;
  • acute suppuration of the structures of the eye (if antibiotic treatment is not carried out);
  • injury and ulcer of the cornea, the period after the removal of a foreign object;
  • hole in the eardrum.

Important! Ointment and drops Dexamethasone can reduce the severity of manifestations in the development of bacterial and fungal infections of the ears and eyes.

Therefore, after clarifying the diagnosis and identifying the infection, the drug should be used with appropriate antimicrobial treatment.

Side effects

A hormonal agent has a profound effect on all body systems. The task of the attending physician is to minimize the risk, frequency and severity of adverse reactions with a high therapeutic effect of the drug.

Undesirable manifestations depend on the duration of the course, dosages, age and condition of the patient.

Basic side effects:

  • allergic rashes, pruritus, urticaria, swelling on the face, respiratory disorders, bronchospasm, anaphylactic shock;
  • restlessness, disorientation, depressive, paranoid states or euphoria;
  • double vision, visual disturbances, pain in the head due to an increase in intracranial pressure, characteristic of a rapid decrease in dose;
  • insomnia, dizziness;
  • persistent increase in blood pressure;
  • weakening of the myocardium, arrhythmias;
  • potassium deficiency and cardiac disorders associated with hypokalemia;
  • decrease in adrenal function, the development of diabetes mellitus, Itsenko-Cushing's syndrome, excessive hair growth, menstrual cycle disorder, developmental delay in children;
  • a sharp increase in blood viscosity and thrombosis;
  • nausea, bouts of vomiting, ulceration of the digestive organs, gastritis, pancreatitis, colitis;
  • frequent infections against the background of immunosuppression;
  • osteoporosis, abnormal fractures, joint and muscle pain, femoral head necrosis, tendon rupture;
  • acne, sweating, dry skin, slow healing of lesions;
  • swelling of the limbs, weight gain;
  • a sharp deterioration in vision (with injections in the area of ​​the face, neck and head);
  • increased pain when injected into the joint;
  • burning, itching of the mucosa and skin (ointment and drops), with treatment longer than 20 days, allergies, glaucoma and cataracts may develop, and visual function may decrease.

Drivers of transport and workers who require increased concentration should be careful when treating with Dexamethasone, as concentration is disturbed when it is taken.

Overdose

Excessive doses of corticosteroid or long-term treatment can lead to overdose, which manifests itself in an increase in unwanted side reactions.

The drug is immediately canceled and the symptoms of an overdose are eliminated with the help of drugs that can relieve certain manifestations.

With long-term therapy, constant monitoring of the development of children, periodic examination of the organs of vision, control of intraocular, intracranial pressure, sugar and blood coagulability, functions of the adrenal glands and the hypothalamic-pituitary system are required.

Dexamethasone analogs

Synonyms - drugs with the same active ingredient as Dexamethasone and a similar therapeutic effect: Dexamethasone-Vial, Dexamethasone-Ferein, eye drops - Dexamethasone Long, Maxidex, Oftan Dexamethasone, Ozurdex.

Analogues with a similar action, but a different composition:

  • drops with Dexamethasone and other active ingredients: Sofradex, Dexon;
  • Prednisolone is a corticosteroid drug with a similar but weaker therapeutic effect.

We should pay tribute to modern pharmacology, which has been able to achieve unprecedented success in the use of hormonal drugs for the treatment of both acute and chronic ailments. The basis of such drugs are synthesized analogues of the body's own hormones. Inflammatory diseases are treated by the use of hormonal drugs, which are more analogous to the secretion of the adrenal cortex. Such drugs allow you to quickly and effectively remove inflammatory processes, which is important to take into account in the development of allergic reactions and in diseases of the joints.

One such drug is a drug called Dexamethasone. This drug belongs to glucocorticosteroids, and has a number of beneficial effects. Why Dexamethasone is so useful, let's find out in more detail.

Features of the drug

Dexamethasone is a synthetic type of glucocorticosteroid (hormonal) substances, which is a derivative of fluoroprednisolone. The drug has anti-allergic, anti-inflammatory, immunosuppressive effects, and also allows you to increase the sensitivity of adrenergic receptors. Presented as a solution for injection in ampoules of 1 and 2 ml. The package contains 25 ampoules, and the cost of the drug is about 200 rubles. The solution for injection is a clear or yellowish liquid, depending on the release series. One 1 ml ampoule contains the following components:

  • dexamethasone sodium phosphate 4 mg;
  • sodium chloride;
  • disodium edatate;
  • sodium hydrogen phosphate dodecahydrate;
  • water.

The effectiveness of the drug is determined by the mechanism of its action. This mechanism is associated with several fundamental effects, which are:

  1. After the active substances of the drug enter the human body, their reaction with the receptor protein is observed. After entering the reaction, the active substances penetrate directly into the nucleus of membrane cells.
  2. A number of metabolic processes are activated by inhibiting the phospholipase enzyme.
  3. There is a blocking of the extraction of mediators of inflammatory reactions from the immune system.
  4. Inhibition of the functioning of enzymes that are responsible for the breakdown of proteins. This action has a positive effect on the process of metabolism of cartilage and bone tissue.
  5. Blocking proteins that are involved in the process of inflammatory processes.
  6. Reducing the permeability of small vessels, which contributes to inhibition of the excretion of inflammatory cells.
  7. Decrease in the intensity of production of leukocytes.

Through all of the above factors, it can be noted that the drug Dexamethasone has the following properties:

  • anti-inflammatory;
  • immunosuppressive;
  • antiallergic;
  • anti-shock.

It's important to know! Dexamethasone has an immediate effect on intravenous administration, and with intramuscular injection after 8 hours.

Like any other drug, Dexamethasone has negative properties, through which the human body has an adverse effect.

The negative effect of the drug

Dexamethasone has a number of negative factors, which include:

  • a depressant effect on the immune system, thereby increasing the likelihood of severe infectious diseases and the formation of tumors;
  • an interfering effect on the formation of bone tissue, which becomes possible through an inhibitory effect on calcium absorption;
  • performs the redistribution of fat cells on the body, as a result of which the main amount of adipose tissue is deposited in the body area;
  • retention of water and sodium ions in the kidneys, which prevents the excretion of adrenocorticotropic hormone.

Such negative reactions medicinal product allow you to understand what side effects can be. It is possible to avoid the development of side effects by using the drug in the lowest possible doses, which will reduce Negative influence on the body.

Indications for use

Dexamethasone is popular in many areas of medicine. The drug is used to treat diseases of the joints, as well as to relieve allergic manifestations. Indications for the use of Dexamethasone are the following diseases and pathologies:

  1. Shock conditions of the patient.
  2. Puffiness of the brain, caused by the following symptoms: tumors, craniocerebral injuries, neurosurgical types of interventions, meningitis, hemorrhages, encephalitis and radiation injuries.
  3. With the development of acute insufficiency of the adrenal cortex.
  4. Acute types of hemolytic anemia, thrombocytopenia, agranulocytosis, as well as severe infectious diseases.
  5. Acute laryngotracheitis in children.
  6. Rheumatic diseases.
  7. Skin diseases: psoriasis, eczema, dermatitis.
  8. Multiple sclerosis.
  9. Intestinal diseases with unexplained genesis.
  10. Shoulder-scapular periarthritis, bursitis, osteochondrosis, osteoarthritis and others.

Solution for injection Dexamethasone is used in the development of acute and urgent conditions, when a person's life depends on the speed of exposure to the drug. The drug is intended primarily for short-term use in connection with vital indications.

How to apply

Dexamethasone is indicated for use not only for adults, but also for children from the first year of life. Instructions for use of the drug Dexamethasone in the form of injections informs that the drug can be used not only for intramuscular injection, but also intravenously by jet or drip. The dosage of the drug depends on such factors as the severity and form of the disease, the age of the patient and the presence of negative reactions. For intravenous administration by drip infusion, a solution must first be prepared. For preparation, it is necessary to dilute the drug with saline or glucose solution. Let us consider in more detail the features of the use of Dexamethasone for adults and children.

For adults, Dexamethasone is used both intramuscularly and intravenously in an amount of 4 to 20 mg. The maximum dosage per day should not exceed 80 ml, so the drug can be administered 3-4 times a day. If there are acute dangerous cases in which a fatal outcome may occur, then on an individual basis, as directed by a doctor, the daily dose may be increased. The duration of parenteral use of the drug is no more than 3-4 days. If it is necessary to continue treatment, then the oral form of the drug in the form of tablets is used. In the event of a positive effect, the dosage is reduced until a maintenance dose is identified. The decision to stop taking the drug is made by the attending physician.

It is unacceptable to use Dexamethasone in the form of intravenous administration in large doses. fast way. This can lead to the development of cardiac complications, so the drug should be administered slowly. Intramuscularly, the drug should also be administered slowly. With the development of cerebral edema, the initial dosage of the drug should not exceed 16 mg. The subsequent dosage is 5 mg intravenously or intramuscularly every 6 hours until a positive result is achieved. If surgical interventions were performed in the brain area, then such dosages may be required for several more days. Continuous use of the drug can significantly affect the reduction of increased intracranial pressure, which occurs due to the presence of a tumor in the brain.

For children, Dexamethasone injections are prescribed in the form of intramuscular injection. Children's dosage depends on the weight of the child and is 0.2-0.4 mg / kg of body weight per day. Treatment should not be prolonged, and dosages for children should be kept to a minimum, depending on the nature of the disease.

Features of use in articular diseases

Treatment of joint diseases with Dexamethasone is a necessary measure when non-steroidal types of drugs are not able to provide the necessary therapeutic effect. The main indications for the use of Dexamethasone in articular diseases are:

  • Bechterew's disease.
  • Rheumatoid arthritis.
  • Articular syndrome in the development of psoriasis.
  • Lupus and scleroderma with articular involvement.
  • Bursitis.
  • Still's disease.
  • Polyarthritis.
  • synovitis.

In such diseases, Dexamethasone is supposed to be used for both local and general treatment.

It's important to know! The drug is injected into the joint area only in an amount of not more than 1 time. Re-injection of Dexamethasone into the joint area is allowed after 3-4 months. In a year, the number of injections for the joint should not exceed 3-4 times. If the norm is exceeded, then this threatens the development of damage to cartilage tissues.

The dosage for intra-articular use is from 0.4 to 4 mg. The dose is influenced by such features as the age of the patient, the size of the shoulder joint, as well as weight. The dosage should be prescribed by the attending physician after a preliminary examination of the patient. Below is a table that shows the approximate doses for the treatment of articular diseases.

Type of introductionDosage
Intra-articular (general)0.4-4 mg
Introduction to Large Joints2-4 mg
Introduction to small joints0.8-1 mg
Introduction to the bursa2-3 mg
Insertion into the tendon sheath0.4-1 mg
Introduction to the tendon1-2 mg
Local administration (into the affected area)0.4-4 mg
Introduction to Soft Tissues2-6 mg

The data in the table are indicative, so it is very important not to prescribe dosages yourself.

It's important to know! Prolonged intra-articular administration of the drug is unacceptable, as this can lead to tendon ruptures.

Application for allergic diseases

Allergic reactions of various forms are treated with antihistamines. If the inflammatory processes are very strong, then antihistamines do not cope with the task. Dexamethasone comes to the rescue, which is a derivative of prednisolone. Active substances act on mast cells, reducing allergic symptoms, resulting in the disappearance of symptoms.

Dexamethasone is used to eliminate allergic manifestations. It is effective for the following allergic abnormalities:

  1. Allergic skin conditions such as dermatitis and eczema.
  2. Quincke's edema.
  3. Hives.
  4. Anaphylactic shock.
  5. The development of inflammatory reactions in the nasal mucosa.
  6. Angioedema, manifested on the face and neck.

With the development of allergic reactions, you should immediately contact an allergist who will select the necessary dosage of the drug and will be able to provide timely and correct assistance to the patient.

Features of use during pregnancy

The period of pregnancy and lactation in the life of every woman is a very important stage. During pregnancy, a woman's body is more susceptible to negative factors, due to a decrease in the immune system.

The main feature of Dexamethasone is the fact that its active and metabolic forms of the drug have the ability to penetrate through any barriers. It follows from this that during pregnancy it is necessary to use the drug with extreme caution. When carrying a child, the need to use Dexamethasone is taken by the doctor in each individual case.

An international organization has assigned class C status to Dexamethasone. This means that the drug is capable of causing negative impact on the fetus, but if there is a risk to the health of the mother, then its use is possible.

Mothers who feed their babies with natural milk should know that it is forbidden to use the medicine in any form during this period. If it is impossible to do without the use of Dexamethasone to cure the disease, then the child should be transferred to artificial feeding. When using Dexamethasone during pregnancy and breastfeeding, the following complications may develop in the fetus and already born child:

  • insufficiency of the adrenal cortex;
  • the formation of congenital malformations;
  • abnormal development of the head and limbs;
  • deterioration in growth and development.

When prescribing Dexamethasone during pregnancy and breastfeeding, the doctor assumes responsibility.

Presence of contraindications

With the development of serious severe complications, such as angioedema or anaphylactic shock, the main contraindication to the use of the drug is the presence of signs of individual intolerance. In all other cases, Dexamethasone will save a life by resuscitating the patient.

If the drug is prescribed as a prophylaxis for chronic ailments, then it is important to take into account some types of contraindications. In the presence of such contraindications, the use of the drug can be harmful, so it is very important to take this seriously. The main types of contraindications are:

  1. In the presence of active types of infectious diseases: viral, bacterial and fungal.
  2. With the development of immunodeficiency, which can be both congenital and acquired.
  3. Tuberculosis in the active form of the disease.
  4. Severe osteoporosis.
  5. In the presence of a peptic ulcer of the gastrointestinal tract.
  6. Esophagitis.
  7. With myocardial infarction.
  8. With diabetes.
  9. Mental types of disorders.
  10. Joint fractures.
  11. Internal bleeding.

The main contraindication is intolerance to any component of the drug. All these contraindications should be considered in each individual case. If you use the drug in the presence of contraindications, then this will lead to a deterioration in the condition and the development of side effects. What are the side effects, find out further.

Adverse symptoms

With improper use of Dexamethasone, the following adverse reactions may occur:

  1. Urticaria, allergic dermatitis, rash and angioedema.
  2. Arterial hypertension and encephalopathy.
  3. Heart failure, cardiac arrest or rupture.
  4. Decrease in the number of lymphocytes and monocytes, as well as thrombocytopenia.
  5. Swelling of the optic disc. The development of neurological side effects, as well as convulsions, dizziness and sleep disturbances, is not excluded.
  6. Mental disorders, insomnia, depressive psychosis, hallucinations, paranoia, schizophrenia.
  7. Adrenal atrophy, growth problems in children, disorders menstrual cycle, increased appetite and weight, hypocalcemia.
  8. Nausea, vomiting, hiccups, stomach ulcers, internal bleeding in the gastrointestinal tract, pancreatitis and gallbladder perforation.
  9. Muscle weakness, osteoporosis, articular cartilage damage and bone necrosis, tendon rupture.
  10. Delayed wound healing, itching, bruising, erythema, excessive sweating.
  11. Excessive intraocular pressure, glaucoma, cataract, exacerbation of bacterial and viral infections eye.
  12. development of impotence.
  13. Pain at the injection site. Atrophy of the skin, scarring at the injection site.

The development of nosebleeds, as well as increased pain in the joints, is not excluded. The development of side effects in patients who, after undergoing a course of therapy, abruptly completed treatment, is not excluded. These side effects include the following ailments: adrenal insufficiency, arterial hypotension, and death.

It's important to know! With the development of side symptoms, as well as with complications and ailments, you must immediately inform your doctor about this. The course of treatment should be stopped immediately if the patient's condition worsens.

Dexamethasone is available from several manufacturers. In addition, it should be noted that the drug has analogues:

  • Dexaven;
  • Dexamed;
  • Dexon;
  • Decadron;
  • Dexafar.

Advantages and disadvantages

What are the advantages and disadvantages of Dexamethasone? Having received an answer to this question, we can conclude that the use of the drug is appropriate. But when it comes to life, the doctor does not think about the presence of contraindications and side effects, and prescribes the medicine urgently. Another thing is when systemic long-term treatment is planned, then in this case it is important to weigh all the pros and cons.

The main advantages of Dexamethasone are:

  1. Speedy and pronounced positive effect after drug administration.
  2. Wide range of influences.
  3. The possibility of using the drug in various convenient forms. The injectable has the fastest effect.
  4. The low cost of the drug, since the packaging will cost 200 rubles.
  5. The possibility of using the drug both in a single dosage and with maintenance.

It is also important to take into account the disadvantages of the drug, which are not so few:

  1. Large list of adverse reactions.
  2. Limited possibility of prescribing the drug during breastfeeding and pregnancy.
  3. The need to choose the lowest possible dosage of the drug.
  4. The need to control the intake of the drug.
  5. The absence of dosage forms in the form of ointments and gels, which would be useful in case of articular pathologies.
  6. Glucose during pregnancy: intravenous administration for the correction of physiological processes Injection with Mydocalm: instructions for use

Catad_pgroup Systemic corticosteroids

Catad_pgroup Preparations for ophthalmology

Dexamethasone for injection - instructions for use

INSTRUCTIONS for the medical use of the drug

Name of the medicinal product:

Trade name of the drug:

Dexamethasone

International non-proprietary name:

dexamethasone

Dosage form:

injection

Compound

Active substance:
Dexamethasone sodium phosphate (dexamethasone phosphate disodium salt) in terms of 100% substance - 4.0 mg

Excipients:
glycerol (distilled glycerin) - 22.5 mg
disodium edetate (trilon B) - 0.1 mg
sodium hydrogen phosphate dodecahydrate (sodium phosphate disubstituted 12-water) - 0.8 mg
water for injection - up to 1 ml

Pharmacotherapeutic group:

glucocorticosteroid

ATC code:

H02AB02

Description:

clear colorless or light yellow liquid.

pharmachologic effect

Synthetic glucocorticosteroid is a methylated derivative of fluoroprednisolone. It has anti-inflammatory, anti-allergic, desensitizing, anti-shock, anti-toxic and immunosuppressive effects.

Interacts with specific cytoplasmic receptors and forms a complex that penetrates the cell nucleus and stimulates mRNA synthesis; the latter induces the formation of proteins, incl. lipocortin mediating cellular effects. Lipocortin inhibits phospholipase A2, inhibits the release of arachidonic acid and inhibits the biosynthesis of endoperoxides, prostaglandins, leukotrienes, which promote inflammation, allergies, and others.

Protein metabolism: reduces the amount of protein in plasma (due to globulins) with an increase in the albumin / globulin ratio, increases 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 (accumulation of fat 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, leading to the activation of gluconeogenesis.

Antagonistic action in relation to vitamin D: "washing out" of calcium from the bones and increasing its renal excretion.

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

The antiallergic effect is due to a decrease in the number of circulating eosinophils, which leads to a decrease in the release of immediate allergy mediators; reduces the effect of allergy mediators on effector cells.

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

Suppresses the synthesis and secretion of adrenocorticotropic hormone and secondarily - the synthesis of endogenous glucocorticosteroids. The peculiarity of the action is a significant inhibition of the function of the pituitary gland and the almost complete absence of mineralocorticosteroid activity.

Doses of 1-1.5 mg / day inhibit the function of the adrenal cortex; the biological half-life is 32-72 hours (the duration of the inhibition of the hypothalamus-pituitary-adrenal cortex system).

According to the strength of glucocorticosteroid activity, 0.5 mg of dexamethasone corresponds to approximately 3.5 mg of prednisone (or prednisolone), 15 mg of hydrocortisone, or 17.5 mg of cortisone.

Pharmacokinetics
In the blood, it binds (60-70%) to a specific protein - the carrier - transcortin. Easily passes through histohematic barriers (including through the blood-brain barrier and placental). It is excreted in a small amount from breast milk. Metabolized in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites. Excreted by the kidneys.

Indications for use:

The drug is used for diseases requiring the introduction of a fast-acting glucocorticosteroid, as well as in cases where oral administration of the drug is not possible:

Endocrine diseases (acute insufficiency of the adrenal cortex, primary or secondary insufficiency of the adrenal cortex, congenital hyperplasia of the adrenal cortex, subacute thyroiditis);
- shock resistant to standard therapy; anaphylactic shock;
- cerebral edema (with a brain tumor, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury);
- status asthmaticus; severe bronchospasm (exacerbation of bronchial asthma, chronic obstructive bronchitis);
- severe allergic reactions;
- rheumatic diseases;
- systemic connective tissue diseases;
- acute severe dermatoses;
- malignant diseases (palliative treatment of leukemia and lymphoma in adult patients; acute leukemia in children; hypercalcemia in patients suffering from malignant tumors when oral treatment is not possible);
- diagnostic study of hyperfunction of the adrenal glands;
- blood diseases (acute hemolytic anemia, agranulocytosis, idiopathic thrombocytopenic purpura in adults);
- severe infectious diseases (in combination with antibiotics);
- intra-articular and intra-synovial administration: arthritis of various etiologies, osteoarthritis, acute and subacute bursitis, acute tendovaginitis, epicondylitis, synovitis;
- local application (in the area of ​​pathological formation): keloids, discoid lupus erythematosus, granuloma annulare.

Contraindications for use:

For short-term use according to "vital" indications, the only contraindication is hypersensitivity.

For intra-articular administration: previous arthroplasty, pathological bleeding (endogenous or caused by the use of anticoagulants), intra-articular bone fracture, infectious (septic) inflammatory process in the joint and periarticular infections (including history), as well as a general infectious disease, severe periarticular osteoporosis, lack of signs of inflammation in the joint (the so-called "dry" joint, for example, in osteoarthritis without synovitis), severe bone destruction and joint deformity (sharp narrowing of the joint space, ankylosis), joint instability as an outcome of arthritis, aseptic necrosis of the epiphyses of the bones forming the joint.

Post-vaccination period (period lasting 8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency states (including AIDS or HIV infection).

Diseases of the gastrointestinal tract (gastric ulcer and 12 duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis).

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

Endocrine diseases - diabetes mellitus (including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease.

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

Systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (III-IV stage), poliomyelitis (except for the form of bulbar encephalitis), open and angle-closure glaucoma, pregnancy, lactation.

For intra-articular administration: the general serious condition of the patient, the inefficiency (or short duration) of the action of 2 previous injections (taking into account the individual properties of the glucocorticosteroids used).

Dosage and administration:

Intra-articular, in the lesion - 0.2-6 mg, repeated 1 time in 3 days or 3 weeks.

Intramuscularly or intravenously - 0.5-9 mg / day.

For the treatment of cerebral edema - 10 mg in the first injection, then 4 mg intramuscularly every 6 hours until the symptoms disappear. The dose can be reduced after 2-4 days with a gradual withdrawal in the period of 5-7 days after the elimination of cerebral edema. Maintenance dose - 2 mg 3 times / day.

For the treatment of shock, 20 mg intravenously at the first injection, then 3 mg/kg for 24 hours as an intravenous infusion or intravenous bolus - from 2 to 6 mg/kg as a single injection or 40 mg as a single injection given every 2- 6 h; possible intravenous administration of 1 mg / kg once. Shock therapy should be canceled as soon as the patient's condition stabilizes, the usual duration is no more than 2-3 days.

Allergic diseases - intramuscularly in the first injection of 4-8 mg. Further treatment is carried out with oral dosage forms.

With nausea and vomiting, during chemotherapy - intravenously 8-20 mg 5-15 minutes before a chemotherapy session. Further chemotherapy should be carried out using oral dosage forms.

For the treatment of respiratory distress syndrome in newborns - intramuscularly 4 injections of 5 mg every 12 hours for two days.

The maximum daily dose is 80 mg.

For children: for the treatment of adrenal insufficiency - intramuscularly at 23 mcg / kg (0.67 mg / sq. M) every 3 days, or 7.8-12 mcg / kg (0.23-0.34 mg / sq. m.). m / day), or 28-170 mcg / kg (0.83-5 mg / sq. m) every 12-24 hours.

Precautions for use

Children who are in contact with patients with measles or chicken pox during the treatment period are prescribed special immunoglobulins prophylactically.
In children during the period of growth, glucocorticosteroids should be used only according to absolute indications and under the most careful supervision of a physician.
It should be borne in mind that in patients with hypothyroidism, the clearance of glucocorticosteroids decreases, and in patients with thyrotoxicosis it increases.

Overdose

Symptoms: increased blood pressure, edema, peptic ulcer, hyperglycemia, impaired consciousness.
Treatment: symptomatic, there is no specific antidote.

Side effect

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

From the side of metabolism: sodium and water retention in the body; hypokalemia; hypokalemic alkalosis; negative nitrogen balance caused by increased protein catabolism, increased appetite, weight gain.

From the side of the cardiovascular system: higher risk of thrombosis (especially in immobilized patients), arrhythmias, increased blood pressure, development or aggravation of chronic heart failure, myocardial dystrophy, steroid vasculitis.

From the musculoskeletal system: muscle weakness, steroid myopathy, decreased muscle mass, osteoporosis, vertebral compression fractures, aseptic necrosis of the femoral head and humerus, pathological fractures of long bones.

From the digestive system: nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract (which can cause perforations and bleeding), hepatomegaly, pancreatitis, ulcerative esophagitis.

Dermatological reactions: thinning and vulnerability of the skin, petechiae and subcutaneous hemorrhages, ecchymosis, striae, steroid acne, delayed wound healing, increased sweating.

From the side of the central nervous system: fatigue, dizziness, headache, mental disorders, convulsions and false symptoms of a brain tumor (increased intracranial pressure with congestive optic disc).

From the endocrine system: decreased glucose tolerance, "steroidal" diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing's syndrome (moon face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis, striae), delayed sexual development in children.

From the side of the organs of vision: posterior subcapsular cataract, increased intraocular pressure, exophthalmos.

Side effects associated with immunosuppressive action: more frequent occurrence of infections and aggravation of the severity of their course.

Others: allergic reactions.

Local reactions (at the injection site): hyperpigmentation and leukoderma, atrophy of subcutaneous tissue and skin, aseptic abscess, hyperemia at the injection site, arthropathy.

Interaction with other drugs

Simultaneous use with phenobarbital, rifampicin, phenytoin or ephedrine can accelerate the biotransformation of dexamethasone, thereby weakening its effect. Hormonal contraceptives enhance the effect of dexamethasone.

Simultaneous use with diuretics (especially "loop") can lead to increased excretion of potassium from the body.

With simultaneous appointment with cardiac glycosides, the possibility of cardiac arrhythmias increases.

Dexamethasone weakens (rarely enhances) the effect of coumarin derivatives, which requires dose adjustment.

Dexamethasone enhances the side effects of non-steroidal anti-inflammatory drugs, especially their effect on the gastrointestinal tract (increased risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract). In addition, it reduces the concentration of non-steroidal anti-inflammatory drugs in the blood serum and thereby their effectiveness.

Carbonic anhydrase inhibitors: increase the risk of hypernatremia, edema, hypokalemia, osteoporosis.

Reduces the effectiveness of insulin and oral hypoglycemic drugs, antihypertensive drugs.

Antacids weaken the effect of dexamethasone.

In combination with paracetamol leads to an increased risk of hepatotoxicity, due to the induction of liver enzymes and the formation of a toxic metabolite of paracetamol.

The simultaneous use of androgens, steroid anabolics contributes to the appearance of edema, hirsutism and acne; estrogen, oral contraceptives - leads to a decrease in clearance, an increase in the toxic effects of dexamethasone.

The risk of developing cataracts increases with the use of antipsychotics (neuroleptics) and azathioprine in combination with dexamethasone.

Simultaneous administration with M-anticholinergics (including antihistamines, tricyclic antidepressants) and nitrates contributes to the development of glaucoma.

When used simultaneously with live antiviral vaccines and against the background of other types of immunizations, it increases the risk of virus activation and the development of infections.

Amphotericin B increases the risk of developing heart failure.

In combination with anticoagulants and thrombolytics, the risk of developing gastrointestinal ulcers and bleeding increases.

Reduces the plasma concentration of salicylates (increases the excretion of salicylates).

Increases the metabolism of mexiletine, reducing its plasma concentration.

Possibilities and features of the use of the drug during pregnancy

(especially in the first trimester), the drug can be used only when the expected therapeutic effect outweighs the potential risk to the fetus. With prolonged therapy during pregnancy, the possibility of impaired fetal growth is not ruled out. In the case of use at the end of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

If it is necessary to carry out drug treatment during breastfeeding then breastfeeding should be discontinued.

The effect of the drug on the ability to drive vehicles, mechanisms

During treatment, driving is not recommended, as well as engaging in activities that require quick psychomotor reactions and precise movements.

Release form:

Solution for injections 4 mg/ml.

1 ml in neutral glass ampoules.

10 ampoules, together with instructions for use and a knife for opening ampoules or an ampoule scarifier, are placed in a cardboard box.

5 ampoules in a blister pack made of polyvinyl chloride film.

1 or 2 blister packs, together with instructions for use and a knife for opening ampoules or an ampoule scarifier, are placed in a pack of cardboard.

When using ampoules with notches, rings and break points, an ampoule scarifier or a knife for opening ampoules may not be inserted.

Best before date:

2 years. Do not use after the expiry date stated on the package.

Storage conditions:

In a place protected from light at a temperature of 5 to 25 ° C.
Keep out of the reach of children.

Conditions for dispensing from pharmacies:

Released by prescription.

Name, address of the manufacturer and address of the place of manufacture of the medicinal product / organization accepting claims

JSC DALHIMFARM, 680001, Russian Federation, Khabarovsk Territory, Khabarovsk, st. Tashkentskaya, 22.

Other dosage forms: eye ointment, tablets.

Ampoules "Dexamethasone" produces several manufacturers, in addition, there are synonyms:

  • Decadron;
  • Dexaven;
  • Dexazon;
  • Dexamed;
  • Dexafar;
  • Dexon.

Price

Average price online* 197 rub. (pack of 25 ampoules)

Where could I buy:

Instructions for use

"Dexamethasone" is a drug that is used as an anti-inflammatory agent, and also relieves attacks of allergies and itchy skin. The drug belongs to the group of glucocorticoids, therefore it is used only as prescribed by the attending physician.

Description and properties

Dexamethasone is a broad-spectrum hormonal agent. The drug has the following properties:

  • effectively relieves inflammation;
  • eliminates allergic reactions;
  • has an anti-shock effect;
  • normalizes water balance;
  • participates in the synthesis of glycogen;
  • maintains glucose homeostasis;
  • helps to establish the exchange of sodium and potassium;
  • exhibits immunosuppressive activity;
  • relieves itching (on the skin and mucous membranes).

The main component of the drug is dexamethasone, which has a powerful effect on the epicenter of the lesion, allowing you to quickly cope even with high-intensity inflammatory processes.

"Dexamethasone" for injection is available as a solution in 1 and 2 ml ampoules (25 ampoules per pack).

The therapeutic effect comes:

  • with intravenous administration - instantly (within 5-15 minutes);
  • with intramuscular injection - after 8 hours.

The drug has a long-term effect, which reaches from 3 to 4 weeks (when injected into the muscle) and from 3 days to 3 weeks when used topically (injection of the substance into the affected area).

Indications

"Dexamethasone" in the form of injections is usually used for severe inflammatory processes, as well as allergic reactions to external stimuli (usually in an emergency).

Indications for the use of Dexamethasone injections are:

  • brain tumors, accompanied by the formation of edema;
  • swelling of the brain resulting from a traumatic brain injury or surgery;
  • bronchial asthma (in the acute stage);
  • acute bronchitis;
  • dysfunction (acute insufficiency) of the adrenal cortex;
  • state of shock (including anaphylactic shock);
  • therapy of lymphoma and leukemia in patients over 18 years of age;
  • leukemia (acute) in pediatric patients;
  • hypercalcemia against the background of oncological diseases (if oral use is not possible);
  • the need for a diagnostic study of the adrenal cortex;
  • conjunctivitis and other eye diseases (if there is a risk of loss of vision or its significant deterioration);
  • fibrous-compacted folliculitis;
  • annular granuloma;
  • sarcoidosis;
  • severe allergy attacks (extreme);
  • joint damage, accompanied by inflammation of a non-infectious nature.

Dosage and administration

Dexamethasone is a prescription hormonal drug, the injection form must be prescribed and administered by a specialist. Self-medication is fraught with consequences.

"Dexamethasone" before use can be diluted with saline or glucose, while it is strictly forbidden to mix the drug with other drugs (in the same syringe or dropper bottle).

The initial dosage for adult patients is 0.5-0.9 mg (administered intravenously or intramuscularly), after which the dosage regimen can be adjusted if necessary.

In allergic diseases, the drug is administered intramuscularly in the first injection of 4-8 mg. Further treatment is preferably carried out with tablets.

Intravenous injection through a syringe is performed when emergency assistance is needed. Even in this case, the administration of the drug should last several minutes.

It is preferable to administer intravenously by infusion method (dropper). For infusion, isotonic sodium chloride solution or 5% dextrose solution is used.

For shock, 20 mg IV at first injection, then 3 mg/kg over 24 hours as an IV infusion or IV bolus—2 to 6 mg/kg as a single injection or 40 mg as a single dose injections given every 2-6 hours; possible in / in the introduction of 1 mg / kg once. Shock therapy should be canceled as soon as the patient's condition stabilizes, the usual duration is no more than 2-3 days.

For oncology:

With nausea and vomiting during chemotherapy, an intravenous injection of 8-20 mg is prescribed 5-15 minutes before a chemotherapy session.

Dosing of the drug for other routes of administration:

Important!

The drug is injected into the joint area only once, subsequent administration is allowed after 3-4 months. The total number of injections per year (in one joint) should not exceed 3-4 times, otherwise there is a risk of cartilage damage.

Dosing of the drug when used in children (only intramuscularly)

Indications Dosage Multiplicity of application
Insufficiency of the adrenal cortex 23.3 µg/kg 3 injections (put once every three days)
7.76-11.65 mcg/kg 1 knock every day
Other indications 27.76-166.65 mcg/kg Every 12-24 hours

Contraindications

"Dexamethasone" in injections is used in short courses, however, there are certain restrictions on its use, for example:

  • osteoporosis;
  • fungal and viral lesions of the organs of vision, purulent eye infections, trachoma, glaucoma, corneal pathology (for use in ophthalmology);
  • infectious diseases in the absence of treatment (viral, fungal and bacterial);
  • lactation;
  • Cushing's syndrome;
  • idiopathic thrombocytopenic purpura (for injection into the muscle);
  • intolerance to the components of the drug.

Dexamethasone should be used with caution in persons with the following diagnoses:

  • cirrhosis of the liver;
  • hepatitis;
  • impaired renal function;
  • psychosis.

Use during pregnancy and breastfeeding

Use during pregnancy is possible only for health reasons. The drug crosses the placenta, the FDA fetal category is C (animal studies have shown negative impact on the fetus, there have been no adequate studies in pregnant women).

Unfortunately, sometimes there is a situation of threat to the life of the patient, in this case there are no alternatives. All glucocorticoids are classified as category C.

Side effects

When administering Dexamethasone injections, the following undesirable consequences were diagnosed:

  • redness of the skin in the face and neck;
  • convulsions;
  • heart rhythm failures;
  • nervous excitability;
  • feeling of anxiety;
  • disorientation in space;
  • euphoria, hallucinations;
  • cataract;
  • glaucoma;
  • increased intraocular pressure;
  • local reactions (with local administration);
  • burning and numbness at the injection site;
  • vision loss.

Important! With prolonged intra-articular administration, there is a risk of tendon rupture.

Other

The drug is sold by prescription. Shelf life - 2 years from the date of production. Store in the refrigerator or at room temperature (not higher than 25 degrees).

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Compound

1 ml of the drug contains

active substance- dexamethasone sodium phosphate 4 mg in terms of dexamethasone phosphate 100% substance

Excipients: sodium chloride, sodium hydrogen phosphate dodecahydrate, disodium edetate, water for injection

PharmacotherapeuticGroup

Corticosteroids for systemic use. Glucocorticosteroids. Dexamethasone

ATX code H02A B02

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Pharmacological properties

Pharmacokinetics

After intravenous administration, the maximum concentration of dexamethasone phosphate in blood plasma is reached in just 5 minutes, and after intramuscular administration - after 1 hour. When applied topically in the form of injections into the joints or soft tissues, absorption is slower. The action of drugs begins quickly after intravenous administration. When administered intramuscularly, the clinical effect is observed 8 hours after administration. The drug acts for a long time: from 17 to 28 days after intramuscular injection and from 3 days to 3 weeks after topical application. The biological half-life of dexamethasone is 24-72 hours. In plasma and synovial fluid, dexamethasone phosphate is rapidly converted to dexamethasone.

In plasma, approximately 77% of dexamethasone is protein bound, predominantly to albumin. Only a small amount of dexamethasone binds to other plasma proteins. Dexamethasone is a fat-soluble substance, so it penetrates into the inter- and intracellular space. It has its effect in the central nervous system (hypothalamus, pituitary gland) by binding to membrane receptors. In peripheral tissues, it binds and acts through cytoplasmic receptors. Dexamethasone breaks down at the site of its action, i.e. in a cage. Dexamethasone is metabolized primarily in the liver. A small amount of dexamethasone is metabolized in the kidneys and other tissues. The main route of excretion is by the kidneys.

Pharmacodynamics

Dexamethasone is a synthetic hormone of the adrenal cortex (corticosteroid) that has a glucocorticoid effect. It has anti-inflammatory and immunosuppressive effects, and also affects energy metabolism, glucose metabolism and (due to negative feedback) on the secretion of the hypothalamic activating factor and the trophic hormone of the adenohypophysis.

The mechanism of action of glucocorticoids is still not fully understood. There are now a sufficient number of reports on the mechanism of action of glucocorticoids to confirm that they act at the cellular level. There are two well-defined receptor systems in the cytoplasm of cells. By binding to glucocorticoid receptors, corticoids exert anti-inflammatory and immunosuppressive effects and regulate glucose metabolism, and by binding to mineralocorticoid receptors, they regulate sodium, potassium, and fluid and electrolyte balance.

Glucocorticoids dissolve in lipids and easily penetrate the target cells through the cell membrane. Binding of the hormone to the receptor leads to a change in the conformation of the receptor, which increases its affinity for DNA. The hormone/receptor complex enters the nucleus of the cell and binds to the regulatory center of the DNA molecule, also called the glucocorticoid response element (GRE). An activated receptor associated with GRE or with specific genes regulates mRNA transcription, which can be increased or decreased. The newly formed mRNA is transported to the ribosome, after which the formation of new proteins occurs. Depending on the target cells and the processes that take place in the cells, protein synthesis can be increased (for example, the formation of tyrosine transaminase in liver cells) or reduced (for example, the formation of IL-2 in lymphocytes). Since glucocorticoid receptors are found in all types of tissues, glucocorticoids can be considered to act on most cells in the body.

Indications for use

  • shock of various origins
  • cerebral edema (with brain tumors, traumatic brain injury, neurosurgical operations, cerebral hemorrhage, meningitis, encephalitis, radiation injuries)
  • bronchial asthma, status asthmaticus, severe allergic reactions (angioedema, bronchospasm, dermatosis, acute anaphylactic reaction to drugs, administration of serum and antibiotics), pyrogenic reactions
  • acute hemolytic anemia, thrombocytopenia, acute lymphoblastic leukemia, agranulocytosis, severe infectious diseases (in combination with antibiotics)
  • acute adrenal insufficiency
  • acute stenosing laryngotracheitis in children
  • humeroscapular periarthritis, epicondylitis, bursitis, tendovaginitis, osteochondrosis, arthritis of various etiologies, osteoarthritis
  • rheumatic diseases, collagenoses

Dexamethasone, solution for injection, 4 mg/ml, is used in acute and emergency conditions in which parenteral administration is vital. The drug is intended for short-term use according to vital indications.

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Dosage and administration

Assign to adults and children from birth.

The dosage regimen is individual and depends on the indications, the severity of the disease and the patient's response to therapy. The drug is administered intramuscularly, intravenously slowly in a stream or drip, it is also possible periarticular or intraarticular administration. In order to prepare a solution for intravenous drip infusion, isotonic sodium chloride solution, 5% glucose solution or Ringer's solution should be used.

Adults intravenously, intramuscularly administered from 4 to 20 mg 3-4 times / day. The maximum daily dose is 80 mg. In acute life-threatening situations, high dosages may be necessary. The duration of parenteral use is 3-4 days, then they switch to maintenance therapy with the oral form of the drug. When the effect is achieved, the dose is reduced over several days until a maintenance dose is reached (on average 3-6 mg / day, depending on the severity of the disease) or until treatment is stopped with continuous monitoring of the patient. Rapid intravenous administration of massive doses of glucocorticoids can cause cardiovascular collapse: the injection is performed slowly, over several minutes.

Cerebral edema (adults): an initial dose of 8-16 mg intravenously, followed by 5 mg intravenously or intramuscularly every 6 hours until a satisfactory result is achieved. In brain surgery, these dosages may be needed for several days after the operation. After that, the dosage should be gradually reduced. Continuous treatment may counteract the increase in intracranial pressure associated with a brain tumor.

children prescribe dexamethasone injections intramuscularly. The dose of the drug is usually from 0.2 mg / kg to 0.4 mg / kg per day. Treatment should be reduced to the minimum dose for the shortest possible period of time.

At intra-articular injection the dose depends on the degree of inflammation, the size and location of the affected area. The drug is administered once every 3-5 days (for the synovial bag) and once every 2-3 weeks (for the joint).

Inject no more than 3-4 times into the same joint and no more than 2 joints at the same time. More frequent administration of dexamethasone can damage articular cartilage. Intra-articular injections must be carried out under strictly sterile conditions.

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Side effects

  • thromboembolism, a decrease in the number of monocytes and / or lymphocytes, leukocytosis, eosinophilia (as with other glucocorticoids), thrombocytopenia and non-thrombocytopenic purpura
  • hypersensitivity reactions, rash, allergic dermatitis, urticaria, angioedema, bronchospasm and anaphylactic reactions, decreased immune response and increased susceptibility to infections
  • polytopic ventricular extrasystole, paroxysmal bradycardia, heart failure, cardiac arrest, cardiac rupture in patients with recent myocardial infarction
  • arterial hypertension, hypertensive encephalopathy
  • after treatment, optic nerve edema and increased intracranial pressure (pseudotumor) may occur. There may also be neurological side effects such as dizziness (vertigo), convulsions and headache, sleep disturbances, confusion, nervousness, restlessness.
  • changes in personality and behavior, which most often manifest as euphoria; the following side effects have also been reported: insomnia, irritability, hyperkinesia, depression and psychoses, as well as manic-depressive psychosis, delirium, disorientation, hallucinations, paranoia, mood lability, suicidal thoughts, worsening of schizophrenia, amnesia, worsening of epilepsy
  • depression of function and atrophy of the adrenal glands (decrease in response to stress), Cushing's syndrome, growth retardation in children and adolescents, menstrual irregularities, amenorrhea, hirsutism, the transition of latent diabetes to a clinically active form, a decrease in carbohydrate tolerance, an increase in appetite and an increase in body weight, hypertriglyceridemia, obesity, increased need for insulin or oral antidiabetic agents in diabetic patients, negative nitrogen balance due to protein catabolism, hypokalemic alkalosis, sodium and water retention, increased potassium loss, hypocalcemia
  • esophagitis, dyspepsia, nausea, vomiting, hiccups, peptic ulcers of the stomach and duodenum, ulcerative perforations and bleeding in the digestive tract (vomiting blood, melena), pancreatitis and perforation of the gallbladder and intestines (especially in patients with chronic intestinal inflammation) are also possible )
  • muscle weakness, steroid myopathy (muscle weakness causes muscle catabolism), osteoporosis (increased calcium excretion) and compression fractures of the spine, fractures of long bones, aseptic osteonecrosis (more often - aseptic necrosis of the heads of the bones of the thighs and shoulders), tendon ruptures (especially with parallel some quinolones), articular cartilage damage and bone necrosis (due to intra-articular infection), premature closure of epiphyseal growth plates
  • delayed wound healing, itching, thinning and sensitization of the skin, striae, petechiae and bruising, acne, telangiectasia, erythema, increased sweating, depressed reaction to skin tests
  • increased intraocular pressure, glaucoma, cataract or exophthalmos, thinning of the cornea, exacerbation of bacterial, fungal or viral eye infections
  • development of opportunistic infections, recurrence of inactive tuberculosis
  • impotence
  • edema, hyper- or hypopigmentation of the skin, atrophy of the skin or subcutaneous layer, sterile abscess and redness of the skin, transient burning and stinging sensation in the perineum when administered intravenously or when administered at high doses
  • with intramuscular injection, changes at the injection site, including swelling, burning, numbness, pain, paresthesia and infection at the injection site, rarely necrosis of surrounding tissues, scarring at the injection site, atrophy of the skin and subcutaneous tissue, with intramuscular injection (introduction into the deltoid is especially dangerous muscle)

With intravenous administration: arrhythmias, flushing of the face, convulsions.

With intracranial administration - nosebleeds.

With intra-articular injection - increased pain in the joint.

Signs of glucocorticoid withdrawal syndrome

In patients who have been treated with dexamethasone for a long time, withdrawal syndrome and cases of adrenal insufficiency, arterial hypotension or death may occur during a rapid dose reduction.

In some cases, withdrawal symptoms may be similar to those of worsening or relapse of the disease for which the patient was being treated.

If severe adverse reactions occur, treatment should be discontinued.

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Contraindications

  • hypersensitivity to dexamethasone or to any other ingredient of the drug
  • acute viral, bacterial or systemic fungal infections (unless appropriate therapy is used)
  • Cushing's syndrome
  • vaccination with a live vaccine
  • intramuscular administration is contraindicated in patients with severe bleeding disorders
  • peptic ulcer of the stomach and duodenum
  • osteoporosis
  • pregnancy and lactation
  • acute psychoses
  • viral and fungal eye diseases, corneal diseases combined with epithelial defects
  • trachoma, glaucoma
  • active tuberculosis
  • kidney failure
  • cirrhosis of the liver and chronic hepatitis
  • epilepsy
  • topical administration is contraindicated in bacteremia, systemic fungal infections, in patients with unstable joints, infections at the site of application, including septic arthritis due to gonorrhea or tuberculosis.

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Drug Interactions

Concurrent use of dexamethasone and non-steroidal anti-inflammatory drugs increases the risk of gastrointestinal bleeding and ulceration.

The effectiveness of dexamethasone is reduced if rifampicin, rifambutin, carbamazepine, phenobarbitone, phenytoin (diphenylhydantoin), primidone, ephedrine or aminoglutethimide are taken concomitantly, so the dose of dexamethasone in such combinations should be increased.

Interactions between dexamethasone and all of the above drugs may interfere with the dexamethasone inhibition test. This must be taken into account when evaluating test results.

Injections Dexamethasone reduces the therapeutic effect of anticholinesterase drugs used in myasthenia gravis.

The combined use of dexamethasone and drugs that inhibit CYP 3A4 enzyme activity, such as ketoconazole, macrolide antibiotics, may cause an increase in the concentration of dexamethasone in serum and plasma. Dexamethasone is a moderate inducer of CYP 3A4. Co-administration with drugs that are metabolized by CYP3A4, such as indinavir, erythromycin, may increase their clearance, causing a decrease in serum concentrations.

Ketoconazole can inhibit the adrenal synthesis of glucocorticoids, thus, due to a decrease in the concentration of dexamethasone, adrenal insufficiency may develop.

Dexamethasone reduces the therapeutic effect of drugs for the treatment of diabetes mellitus, arterial hypertension, coumarin anticoagulants, praziquantel and natriuretics (therefore, the dose of these drugs must be increased); it increases the activity of heparin, albendazole and kaliuretics (the dose of these drugs should be reduced if necessary).

Dexamethasone can change the effect of coumarin anticoagulants, so when using this combination of drugs, you need to check the prothrombin time more often.

The concomitant use of dexamethasone and high doses of other glucocorticoids or β2-adrenergic agonists increases the risk of hypokalemia. In patients with hypokalemia, cardiac glycosides contribute more to rhythm disturbance and have greater toxicity.

Antacids reduce the absorption of dexamethasone from the stomach. The effect of dexamethasone when taken with food and alcohol has not been studied, but the simultaneous use of drugs and food with a high sodium content is not recommended. Smoking does not affect the pharmacokinetics of dexamethasone.

Glucocorticoids increase the renal clearance of salicylate, so it is sometimes difficult to obtain therapeutic serum concentrations of salicylates. Caution should be exercised in patients who gradually reduce the dose of corticosteroid, since this may lead to an increase in the concentration of salicylate in the blood serum and intoxication.

If oral contraceptives are used in parallel, the half-life of glucocorticoids may increase, which enhances their biological effect and may increase the risk of side effects.

Simultaneous use of ritodrine and dexamethasone is contraindicated during childbirth, as this can lead to pulmonary edema. A maternal death has been reported due to the development of this condition.

The simultaneous use of dexamethasone and thalidomide can cause toxic epidermal necrolysis.

Types of interaction that have therapeutic benefits: concomitant administration of dexamethasone and metoclopramide, diphenhydramide, prochlorperazine, or 5-HT3 receptor antagonists (serotonin or 5-hydroxytryptamine type 3 receptors, such as ondansetron or granisetron) is effective in preventing nausea and vomiting caused by chemotherapy with cisplatin, cyclophosphamide, methotrexate, fluorouracil.

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special instructions

During parenteral treatment with corticoids, hypersensitivity reactions can rarely be observed, therefore, it is necessary to take appropriate measures before starting treatment with dexamethasone, taking into account the possibility of allergic reactions (especially in patients with a history of allergic reactions to any other drugs).

Patients treated with dexamethasone for a long time may experience a withdrawal syndrome (also without visible signs of adrenal insufficiency) upon discontinuation of treatment (fever, runny nose, conjunctival redness, headache, dizziness, drowsiness or irritability, muscle and joint pain, vomiting , weight loss, weakness, often also convulsions). Therefore, the dose of dexamethasone should be reduced gradually. Sudden discontinuation of treatment can be fatal.

If the patient is under severe stress (due to trauma, surgery, or serious illness) during therapy, the dose of dexamethasone should be increased, and if this occurs during the cessation of treatment, hydrocortisone or cortisone should be used.

Patients who have been treated with dexamethasone for a long time and who experience severe stress after discontinuation of therapy should be reinstated on dexamethasone, as the resulting adrenal insufficiency may last for several months after discontinuation of treatment.

Treatment with dexamethasone or natural glucocorticoids may mask symptoms of an existing or new infection, as well as symptoms of intestinal perforation. Dexamethasone can exacerbate systemic fungal infection, latent amoebiasis, and pulmonary tuberculosis.

Caution and medical supervision are recommended in patients with osteoporosis, arterial hypertension, heart failure, tuberculosis, glaucoma, hepatic or renal insufficiency, diabetes mellitus, active peptic ulcer, recent intestinal anastomosis, ulcerative colitis and epilepsy. Special care is required for patients during the first weeks after myocardial infarction, patients with thromboembolism, myasthenia gravis, hypothyroidism, psychosis or psychoneurosis, as well as elderly patients .

During treatment, an exacerbation of diabetes mellitus or a transition from a latent phase to clinical manifestations of diabetes mellitus may occur.

With prolonged treatment, it is necessary to control the level of potassium in the blood serum.

Vaccination with a live vaccine is contraindicated during treatment with dexamethasone. Vaccination with an inactivated viral or bacterial vaccine does not lead to the expected antibody synthesis and does not have the expected protective effect. Dexamethasone phosphate is usually not prescribed 8 weeks before vaccination and is not started earlier than 2 weeks after vaccination.

Patients who have been treated with high doses of dexamethasone for a long time and have never had measles should avoid contact with infected individuals; in case of accidental contact, prophylactic treatment with immunoglobulin is recommended.

The action of glucocorticoids is enhanced in patients with cirrhosis of the liver or hypothyroidism.

Severe mental reactions may accompany the systemic use of corticosteroids. Usually, symptoms appear a few days or weeks after the start of treatment. The risk of developing these symptoms increases with high doses. Most reactions resolve with dose reduction or drug withdrawal. It is necessary to observe and timely detect changes in the mental state, especially depressive mood, suicidal thoughts and intentions. With particular caution, corticosteroids should be used in patients with affective disorders present or in history, as well as in close relatives. The occurrence of undesirable effects can be prevented by using the minimum effective dose for the shortest period or by using the required daily dose of the drug 1 time in the morning.

Intra-articular use of dexamethasone can lead to systemic effects.

Frequent use may cause cartilage damage or bone necrosis.

Before intra-articular injection, synovial fluid must be removed from the joint and examined (check for infection). Injection of corticoids into infected joints should be avoided. If a joint infection develops after the injection, appropriate antibiotic therapy should be started.

Patients should be advised to avoid exertion on the affected joints until the inflammation has resolved.

Avoid injecting the drug into unstable joints.

Corticoids can interfere with the results of skin allergy tests.

Special precautions regarding excipients. The drug contains 1 mmol (23 mg) sodium per dose, which is a very small amount.

Incompatibility. The drug should not be mixed with other drugs, except for the following: 0.9% sodium chloride solution or 5% glucose solution.

When mixing dexamethasone with chlorpromazine, diphenhydramine, doxapram, doxorubicin, daunorubicin, idarubicin, hydromorphone, ondansetron, prochlorperazine, potassium nitrate and vancomycin, a precipitate forms.

Approximately 16% dexamethasone dissolves in 2.5% glucose solution and 0.9% sodium chloride solution with amikacin.

Some medicines, such as lorazepam, should be mixed with dexamethasone in glass vials rather than plastic bags (Lorazepam concentrations drop below 90% after 3-4 hours of storage in PVC bags at room temperature).

Some drugs, such as metapaminol, have a so-called "incompatibility that develops slowly" - it develops within a day when mixed with dexamethasone.

Dexamethasone with glycopyrolate: The pH of the final solution is 6.4, which is outside the stability range.

Use during pregnancy or lactation

The drug is contraindicated during pregnancy or during lactation

Application in pediatrics . Use in children from birth only if absolutely necessary. During treatment with dexamethasone, careful monitoring of the growth and development of children is necessary.

Features of the effect of the drug on the ability to drive vehicles or potentially dangerous mechanisms

Considering that in sensitive patients, when using the drug, adverse reactions may occur (dizziness, confusion, etc.), for the period of using the drug, you should refrain from driving vehicles and performing other work that requires concentration.

Solution for injection 4 mg/ml 1 ml

Shelf life

Do not use the drug after the expiration date indicated on the package.

Terms of dispensing from pharmacies

On prescription

Manufacturer

PJSC "Farmak", Ukraine, 04080, Kyiv, st. Frunze, 63.

Registration certificate holder

PJSC Farmak, Ukraine