Compound
Composition of Dexamethasone in ampoules: dexamethasone sodium phosphate (4 mg/ml), glycerin, propylene glycol, disodium edetate, phosphate buffer solution (7.5 pH), methyl and propyl parahydroxybenzoate, water for injection.
Dexamethasone tablets contain 0.5 mg of the active substance dexamethasone sodium phosphate , as well as lactose in the form of monohydrate, MCC, colloidal anhydrous silicon dioxide, magnesium stearate, croscarmellose sodium.
Dexamethasone eye drops: dexamethasone sodium phosphate (1 mg/ml), boric acid, benzalkonium chloride (preservative), sodium tetraborate, Trilon B, water d/i.
Pharmacodynamics and pharmacokinetics
Dexamethasone is a synthetic corticosteroid (adrenal cortex hormone). Wikipedia and the Vidal reference book indicate that the substance, when interacting with cytoplasmic receptors, forms complexes that penetrate the cell nucleus and stimulate the synthesis of m-RNA.
m-RNA, in turn, induces the biosynthesis of proteins (including enzymes that regulate vital processes in cells), which inhibit phospholipase A2, the release of arachidonic acid, the biosynthesis of endoperoxides, LT and PG, which are mediators of allergies, inflammation, pain, etc. .
Inhibits the activity of proteases, collagenase, hyaluronidase, as well as the release of inflammatory mediators from eosinophils, promotes:
- normalization of the function of the intercellular matrix of bone and cartilage tissue;
- decreased capillary permeability;
- stabilization of membranes (including lysosomal) cells;
- inhibition of the release of cytokines from macrophages and lymphocytes (gamma interferon and IL);
- involution of lymphoid tissue;
- acceleration of protein catabolism;
- decreased glucose utilization;
- increased gluconeogenesis in the liver;
- decreased absorption and increased excretion of Ca;
- Na and water retention;
- delayed ACTH secretion.
After oral administration, the substance is almost completely absorbed. The bioavailability of the drug in tablet form is up to 80%. Cmax and the maximum effect of use are observed after one to two hours. The effect after taking a single dose lasts for 2.75 days.
Binding to plasma proteins (mainly albumin ) is approximately 77%.
The substance is fat-soluble, therefore it is able to penetrate both inside the cell and into the intracellular space. The action manifests itself in the central nervous system ( pituitary gland , hypothalamus ), which is due to the ability of dexamethasone to bind to cell membrane receptors.
In peripheral tissues it binds and acts through cytoplasmic receptors. Dexamethasone breaks down in the cell (at the site of its action). Metabolization occurs primarily in the liver and, partly, in the kidneys and other tissues. The main route of elimination is through the kidneys.
Dexason
Dexamethasone is a synthetic hormone of the adrenal cortex, a glucocorticosteroid (GCS), a methylated derivative of fluoroprednisolone. It has anti-inflammatory, antiallergic, desensitizing, antishock, antitoxic and immunosuppressive effects.
Interacts with specific cytoplasmic GCS receptors to form a complex that penetrates the cell nucleus and stimulates the synthesis of matrix ribonucleic acid, the latter induces the formation of proteins, including lipocortin, that mediate cellular effects. Lipocortin inhibits phospholipase A2, suppresses the release of arachidonic acid and suppresses the synthesis of endoperoxides, prostaglandins, leukotrienes, which contribute to inflammation, allergies, etc.
Effect on protein metabolism: reduces the amount of protein in plasma (due to globulins) with an increase in the albumin/globulin ratio, increases albumin synthesis in the liver and kidneys; enhances protein catabolism in muscle tissue.
Effect on lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (fat accumulation occurs mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.
Effect on carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract (GIT); increases the activity of glucose-6-phosphatase, which leads to an increase in the flow of glucose from the liver into the blood; increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases, which leads to the activation of gluconeogenesis.
Effect on water-electrolyte metabolism: retains sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract (GIT), “washes” calcium from the bones, increases the excretion of calcium by the kidneys.
The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils; inducing the formation of lipocortin and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes and organelle membranes (especially lysosomal ones).
The antiallergic effect develops as a result of suppression of the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, a decrease in the number of circulating basophils, suppression of the development of lymphoid and connective tissue, a decrease in the number of T- and B-lymphocytes, mast cells , reducing the sensitivity of effector cells to allergy mediators, suppressing antibody formation, changing the body’s immune response.
In chronic obstructive pulmonary disease, the effect is based mainly on inhibition of inflammatory processes, inhibition of the development or prevention of edema of the mucous membranes, inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium, deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucous membrane. Increases the sensitivity of beta-adrenergic receptors of small and medium-caliber bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of bronchial secretions due to inhibition or reduction of its production.
Antishock and antitoxic effects are associated with an increase in blood pressure (BP) (due to an increase in the concentration of circulating catecholamines and restoration of the sensitivity of adrenoreceptors to them, as well as vasoconstriction), a decrease in the permeability of the vascular wall, membrane protective properties, activation of liver enzymes involved in the metabolism of endo- and xenobiotics .
The immunosuppressive effect is due to inhibition of the release of cytokines (interleukin-1 and interleukin-2, interferon gamma) from lymphocytes and macrophages. Dexamethasone has a 30 times more pronounced effect than endogenous cortisol. Therefore, it is a more potent inhibitor of the secretion of corticotropin-releasing hormone and adrenocorticotropic hormone (ACTH). In pharmacological doses, it inhibits the hypothalamic-pituitary-adrenal system and promotes the development of secondary adrenal insufficiency. Suppresses the synthesis and release of ACTH by the pituitary gland and, secondarily, the synthesis of endogenous corticosteroids. Inhibits the secretion of thyroid-stimulating hormone and follicle-stimulating hormone. Suppresses the release of beta-lipotropin, but does not reduce circulating beta-endorphin.
Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
Increases the excitability of the central nervous system. Reduces the number of lymphocytes and eosinophils, increases the number of red blood cells (by stimulating the production of erythropoietins).
The peculiarity of the action is significant inhibition of pituitary function and the almost complete absence of mineralocorticoid activity.
Indications for use
Why is Dexamethasone prescribed in injections and tablets?
Diseases amenable to systemic treatment are indicated for the use of Dexamethasone (if necessary, the drug can be used as an addition to the main therapy). The solution is administered intravenously and intramuscularly in cases where oral administration or local treatment is ineffective or impossible.
The drug Dexamethasone (injections and tablets) is indicated for rheumatic and allergic diseases, cerebral edema , shock of various origins, certain kidney diseases, autoimmune disorders, respiratory tract diseases, blood diseases, acute severe dermatoses, IBD, during HRT (for example, in case of insufficiency adenohypophysis/adrenal glands).
Why is Dexamethasone eye drops prescribed?
In ophthalmological practice, the use of the drug is advisable for allergic and non-purulent conjunctivitis, iridocyclitis , iritis , keratitis , keratoconjunctivitis without damaging the integrity of the corneal epithelium, blepharoconjunctivitis , scleritis , blepharitis , episcleritis , sympathetic ophthalmia , as well as for relieving inflammation after surgery or eye injury.
What is instillation of the drug into the ear indicated for?
The drug is instilled into the canal of the external ear for inflammatory and allergic diseases of the ear.
Dexamethasone for coronavirus COVID-19
Based on the results of clinical trials (not yet published), it can be assumed that Dexamethasone is most effective in treating severe cases of coronavirus. ventilators decreased by a third compared to the control group. Mortality decreased by 20% in patients receiving oxygen therapy without mechanical ventilation. No effect was observed in the treatment of mild forms of coronavirus.
Dexamethasone 4 mg/ml 1 ml 25 pcs. injection
pharmachologic effect
Glucocorticosteroid.
Composition and release form Dexamethasone 4 mg/ml 1 ml 25 pcs. injection
Solution - 1 ml:
- active ingredient: dexamethasone sodium phosphate 4.4 mg (which corresponds to 4.0 mg of dexamethasone phosphate);
- excipients: methyl parahydroxybenzoate 1.5 mg, propyl parahydroxybenzoate 0.2 mg, sodium disulfite 1.0 mg, disodium edetate 1.0 mg, sodium hydroxide to pH 7.0-8.5, water for injection up to 1.0 ml.
1.0 ml of the drug in dark glass ampoules. 25 ampoules in a mesh cardboard lattice, 1 lattice along with instructions for use in a cardboard box.
5 ampoules in a plastic tray, 5 pallets along with instructions for use in a cardboard box.
Description of the dosage form
Transparent, colorless to light yellow solution.
Directions for use and doses
The dosage regimen is individual and depends on the indications, the patient’s condition and his response to therapy.
The drug is administered intravenously (IV) slowly in a stream or drip (in acute and emergency conditions); intramuscularly (i.m.); local (into the pathological formation) and subconjunctival, retrobulbar or parabulbar administration is also possible.
To prepare a solution for intravenous infusion, use an isotonic sodium chloride solution or a 5% glucose (dextrose) solution.
The drug is administered intravenously and intramuscularly at a dose of 0.5-24 mg/day in 2 doses (equivalent to 1/3-1/2 oral dose) in the shortest possible course at the minimum effective dose, treatment is discontinued gradually. Long-term treatment should be carried out at a dose not exceeding 0.5 mg/day. No more than 2 ml of solution is injected intramuscularly into the same place.
In case of shock, administer strictly intravenously as a bolus at a dose of 2-6 mg/kg. If necessary, repeated doses are administered every 2 to 6 hours or as a long-term intravenous infusion at a dose of 3 mg/kg/day. Treatment with dexamethasone should be carried out as part of complex therapy for shock. The use of pharmacological doses is permissible only in life-threatening conditions, and, as a rule, this time does not exceed 48 - 72 hours.
For cerebral edema, an initial dose of 10 mg is administered intravenously, then 4 mg every 6 hours until symptoms subside (usually within 12-24 hours). After 2-4 days, the dose is reduced and the use of the drug is gradually stopped over 5-7 days. Patients with malignant neoplasms may require maintenance treatment - 2 mg IM or IV 2-3 times a day.
In case of acute cerebral edema, short-term intensive therapy is carried out: for adults, the loading dose is 50 mg IV, then on days 1-3, 8 mg is administered every 2 hours, on the 4th day - 4 mg every 2 hours, on days 5-8 day - 4 mg every 4 hours, then the daily dose is reduced by 4 mg/day until it is completely discontinued. For children weighing more than 35 kg, the loading dose is 25 mg IV, then 4 mg every 2 hours on days 1-3, 4 mg every 4 hours on days 4, 4 mg every 4 hours on days 5-8. mg every 6 hours, then the daily dose is reduced by 2 mg/day until it is completely discontinued. For children weighing less than 35 kg, the loading dose is 20 mg IV, then on days 1-3, 4 mg every 3 hours, on the 4th day - 4 mg every 6 hours, on days 5-8 - 2 mg every 6 hours, then the daily dose is reduced by 1 mg/day until it is completely discontinued.
For acute self-limiting allergic reactions or exacerbation of chronic allergic diseases, parenteral and oral administration of dexamethasone is combined: day 1 - iv 4-8 mg, day 2-3 - orally 1 mg 2 times a day, day 4-5 - orally 0 .5 mg 2 times a day, 6-7 days - 0.5 mg orally once. On the 8th day, the effectiveness of therapy is assessed.
In emergency situations, higher doses are used: the initial dose is 4-20 mg, which is repeated until the desired effect is achieved, the total daily dose rarely exceeds 80 mg. After achieving a therapeutic effect, Dexamethasone is administered in doses of 2-4 mg as needed, followed by gradual withdrawal of the drug. To maintain a long-term effect, the drug is administered every 3-4 hours or as a long-term drip infusion. After relief of acute conditions, the patient is transferred to taking the drug Dexamethasone orally.
Doses of the drug for children (i.m.):
The dose of the drug during replacement therapy (for adrenal insufficiency) is 0.0233 mg/kg body weight or 0.67 mg/m2 body surface area, divided into 3 doses, every 3rd day or 0.00776-0.01165 mg/kg body weight or 0.233-0.335 mg/m2 body surface area daily.
For other indications, the recommended dose is 0.02776 to 0.16665 mg/kg body weight or 0.833 to 5 mg/m2 body surface area every 12 to 24 hours.
Long-term use of high doses of the drug requires a gradual dose reduction in order to prevent the development of acute adrenal insufficiency.
Pharmacodynamics
Dexamethasone is a synthetic hormone of the adrenal cortex, a glucocorticosteroid (GCS), a methylated derivative of fluoroprednisolone. It has anti-inflammatory, antiallergic, desensitizing, antishock, antitoxic and immunosuppressive effects.
It interacts with specific cytoplasmic glucocorticosteroid receptors to form a complex that penetrates the cell nucleus and stimulates the synthesis of matrix ribonucleic acid, the latter inducing the formation of proteins, including lipocortin, that mediate cellular effects. Lipocortin inhibits phospholipase A2, suppresses the release of arachidonic acid and suppresses the synthesis of endoperoxides, prostaglandins, leukotrienes, which contribute to inflammation, allergies, etc.
Effect on protein metabolism: reduces the amount of protein in plasma (due to globulins) with an increase in the albumin/globulin ratio, increases albumin synthesis in the liver and kidneys; enhances protein catabolism in muscle tissue.
Effect on lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (fat accumulation occurs mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.
Effect on carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract (GIT); increases the activity of glucose-6-phosphatase, which leads to an increase in the flow of glucose from the liver into the blood; increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases, which leads to the activation of gluconeogenesis.
Effect on water-electrolyte metabolism: retains sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, “washes” calcium from the bones, increases the excretion of calcium by the kidneys.
The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils; inducing the formation of lipocortin and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes and organelle membranes (especially lysosomal ones).
The antiallergic effect develops as a result of suppression of the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, a decrease in the number of circulating basophils, suppression of the development of lymphoid and connective tissue, a decrease in the number of T- and B-lymphocytes, mast cells , reducing the sensitivity of effector cells to allergy mediators, suppressing antibody formation, changing the body’s immune response.
In chronic obstructive pulmonary disease, the effect is based mainly on inhibition of inflammatory processes, inhibition of development or prevention of swelling of the mucous membranes, inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium, deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucous membrane. Increases the sensitivity of beta-adrenergic receptors of small and medium caliber bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of bronchial secretions due to inhibition or reduction of its production.
Antishock and antitoxic effects are associated with an increase in blood pressure (BP) (due to an increase in the concentration of circulating catecholamines and restoration of the sensitivity of adrenergic receptors to them, as well as vasoconstriction), a decrease in the permeability of the vascular wall, membrane protective properties, and activation of liver enzymes involved in the metabolism of endo- and xenobiotics .
The immunosuppressive effect is due to inhibition of the release of cytokines (interleukin-1 and interleukin-2, interferon gamma) from lymphocytes and macrophages. Suppresses the synthesis and release of adrenocorticotropic hormone (ACTH) by the pituitary gland and, secondarily, the synthesis of endogenous GCS. Inhibits the secretion of thyroid-stimulating hormone and follicle-stimulating hormone. Suppresses the release of beta-lipotropin, but does not reduce the content of circulating beta-endorphin.
Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
Increases the excitability of the central nervous system.
Reduces the number of lymphocytes and eosinophils, increases the number of red blood cells (by stimulating the production of erythropoietins).
The peculiarity of the action is significant inhibition of pituitary function and the almost complete absence of mineralocorticoid activity. Doses of 1-1.5 mg/day inhibit the adrenal cortex; biological half-life (T1/2) - 32-72 hours (duration of suppression of the hypothalamic-pituitary-adrenal system).
Pharmacokinetics
Absorption
The maximum concentration of dexamethasone in blood plasma is achieved within 5 minutes after intravenous administration and 1 hour after intramuscular administration.
Distribution
Communication with plasma proteins (mainly albumin) - 77%. Penetrates through the blood-brain and placental barriers. The half-life (T1/2) from plasma is 190 minutes.
Metabolism
Metabolized in the liver. A small amount of dexamethasone is metabolized in the kidneys and other organs.
Removal
Up to 65% of the dose is excreted by the kidneys within 24 hours; a small amount of dexamethasone passes into breast milk.
Indications for use Dexamethasone 4 mg/ml 1 ml 25 pcs. injection
Replacement therapy for adrenal insufficiency (in combination with sodium chloride and/or mineralocorticosteroids): acute adrenal insufficiency (Addison's disease, bilateral adrenalectomy); relative adrenal insufficiency that develops after discontinuation of GCS treatment; primary or secondary adrenal insufficiency.
Symptomatic and pathogenetic therapy of other diseases requiring the administration of fast-acting corticosteroids, as well as in cases where oral administration of the drug is impossible:
- endocrine diseases: congenital adrenal hyperplasia, subacute thyroiditis;
- shock (burn, traumatic, surgical, toxic) - if vasoconstrictors, plasma replacement drugs and other symptomatic therapy are ineffective;
- cerebral edema (only after confirmation of symptoms of increased intracranial pressure by magnetic resonance or computed tomography results, caused by a brain tumor, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury);
- status asthmaticus; severe bronchospasm (exacerbation of bronchial asthma);
- severe allergic reactions, anaphylactic shock;
- 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;
- blood diseases: acute hemolytic anemia, agranulocytosis, idiopathic thrombocytopenic purpura in adults;
- in ophthalmological practice (subconjunctival, retrobulbar or parabulbar administration): allergic conjunctivitis, keratitis, keratoconjunctivitis without damage to the epithelium, iritis, iridocyclitis, blepharitis, blepharoconjunctivitis, scleritis, episcleritis, inflammatory process after eye injuries and surgical interventions, sympathetic ophthalmia, immunosuppressive treatment after transplantation and cornea;
- local application (in the area of pathological formation): keloids, discoid lupus erythematosus, granuloma annulare;
- poisoning with cauterizing liquids (the need to reduce inflammation and prevent cicatricial contractions in case of poisoning with cauterizing liquids).
Contraindications
- For short-term use for “life-saving” indications, the only contraindication is hypersensitivity to the active substance or any other component of the drug;
- systemic mycoses;
- breastfeeding period;
- simultaneous use of live and attenuated vaccines with immunosuppressive doses of the drug.
The drug should be prescribed with caution for the following diseases/conditions/risk factors:
Systemic parasitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently suffered, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles; amebiasis, strongyloidiasis (established or suspected); active or latent tuberculosis. Use for severe infectious diseases is permissible only against the background of specific antimicrobial therapy.
Vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency conditions (including AIDS or HIV infection).
Gastrointestinal diseases: peptic ulcer of the stomach and duodenum, 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 (CVS), including recent myocardial infarction (in patients with acute and subacute myocardial infarction, the necrosis focus may spread, the formation of scar tissue may slow down and, as a result, rupture of the heart muscle), decompensated chronic heart failure (CHF) , arterial hypertension, hyperlipidemia.
Endocrine diseases - diabetes mellitus (including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, stage III-IV obesity.
Severe chronic renal and/or liver failure, nephrourolithiasis.
Hypoalbuminemia and conditions predisposing to its occurrence.
Liver failure.
Systemic osteoporosis, myasthenia gravis, poliomyelitis (except for the form of bulbar encephalitis), epilepsy, “steroid” myopathy.
Acute psychosis, severe affective disorders (including a history of, especially “steroid” psychosis).
Open- and closed-angle glaucoma, eye herpes (risk of corneal perforation).
Pregnancy.
Elderly patients - due to a high risk of developing osteoporosis and arterial hypertension.
In children during the growth period, Dexamethasone should be used only for absolute indications and under the careful supervision of the attending physician.
Application Dexamethasone 4 mg/ml 1 ml 25 pcs. solution for injection during pregnancy and lactation
Dexamethasone crosses the placenta and can reach high concentrations in the fetus. During pregnancy (especially in the first trimester) or in women planning a pregnancy, taking Dexamethasone is indicated if the expected therapeutic effect of the drug exceeds the risk of negative effects on the mother or fetus. GCS should be prescribed during pregnancy only for absolute indications. With long-term therapy during pregnancy, the possibility of impaired fetal growth cannot be ruled out. If used 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.
A small amount of dexamethasone passes into breast milk.
If it is necessary to carry out treatment with the drug during breastfeeding, breastfeeding should be discontinued, as this may lead to retardation of the child's growth and a decrease in the secretion of his endogenous corticosteroids.
special instructions
During treatment with Dexamethasone (especially long-term), observation by an ophthalmologist, monitoring of blood pressure and water-electrolyte balance, as well as peripheral blood patterns and blood glucose concentrations are necessary.
In order to reduce side effects, the intake of potassium into the body should be increased (diet, potassium supplements). Food should be rich in proteins, vitamins, and limit the content of fats, carbohydrates and table salt.
The effect of the drug is enhanced in patients with liver cirrhosis. It must be taken into account that in patients with hypothyroidism the clearance of dexamethasone is reduced, and in patients with thyrotoxicosis it is increased.
The drug may worsen existing emotional instability or psychotic disorders. If a history of psychosis is indicated, Dexamethasone in high doses is prescribed under the strict supervision of a physician.
The patient should be carefully monitored for a year after the end of long-term therapy with Dexamethasone due to the possible development of relative insufficiency of the adrenal cortex in stressful situations.
If Dexamethasone is suddenly discontinued, especially in the case of previous use of high doses, acute adrenal insufficiency may develop; “peritoneal irritation” syndrome in patients with perforation of the stomach or intestinal wall.
With the use of GCS, changes in sperm motility and number are possible.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, it is necessary to refrain from driving vehicles and other mechanisms that require increased concentration and speed of psychomotor reactions.
Overdose
Symptoms: increased blood pressure, edema (peripheral), peptic ulcer, hyperglycemia, impaired consciousness.
Treatment: symptomatic, there is no specific antidote.
Side effects Dexamethasone 4 mg/ml 1 ml 25 pcs. injection
The incidence and severity of side effects depend on the duration of use and the dose used.
Endocrine system disorders: decreased glucose tolerance, “steroidal” diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing syndrome (moon face, pituitary type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis, “ steroid stretch marks), delayed sexual development in children.
Gastrointestinal tract disorders: nausea, vomiting, pancreatitis, “steroid” gastric and duodenal ulcers, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups, abdominal pain, feeling of discomfort in the epigastric areas. In rare cases, increased activity of liver transaminases and alkaline phosphatase.
Cardiac disorders: arrhythmias, bradycardia (up to cardiac arrest), development (in predisposed patients) or aggravation of the severity of CHF, changes in the electrocardiogram characteristic of hypokalemia. In patients with acute and subacute myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.
Vascular disorders: increased blood pressure, hypercoagulation, thrombosis, with intravenous administration: flushing of blood to the face, vasculitis, increased capillary fragility.
Mental disorders: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, nervousness or anxiety, insomnia, emotional lability, suicidal tendencies.
Nervous system disorders: increased intracranial pressure, dizziness, vertigo, cerebellar pseudotumor, headache, convulsions.
Violations of the organ of vision: sudden loss of vision (with parenteral administration in the head, neck, nasal turbinates, scalp, deposition of drug crystals in the vessels of the eye is possible), posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos, chemosis, ptosis, mydriasis, corneal perforation, central serous chorioretinopathy.
Metabolic and nutritional disorders: increased calcium excretion, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating, hypercholesterolemia, epidural lipomatosis.
Caused by mineralocorticoid activity - fluid and sodium retention (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).
Disorders of the musculoskeletal and connective tissue: slowing of growth and ossification processes in children (premature closure of the epiphyseal growth plates), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and femur), rupture of muscle tendons, "steroid" myopathy, decreased muscle mass (atrophy).
Renal and urinary tract disorders: leukocyturia.
Disorders of the skin and subcutaneous tissues: delayed wound healing, petechiae, ecchymoses, thinning of the skin, hyper- or hypopigmentation, “steroid” acne, “steroid” stretch marks, a tendency to develop pyoderma and candidiasis.
Immune system disorders: generalized (skin rash, skin itching, anaphylactic shock), local allergic reactions.
General disorders and disorders at the injection site: development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination), flushing syndrome, convulsions.
Drug interactions
Dexamethasone is pharmaceutically incompatible with other drugs (may form insoluble compounds). It is recommended to administer it separately from other drugs (iv bolus, or through another dropper, as a second solution). When mixing a solution of dexamethasone with heparin, a precipitate forms. Dexamethasone increases the toxicity of cardiac glycosides (due to the resulting hypokalemia, the risk of developing arrhythmias increases).
Accelerates the elimination of acetylsacylic acid, reduces the content of its metabolites in the blood (when dexamethasone is discontinued, the concentration of salicylates in the blood increases and the risk of side effects increases).
When used simultaneously with live antiviral vaccines and against the background of other types of immunization, it increases the risk of viral activation and the development of infections.
Increases the metabolism of isoniazid, mexiletine (especially in “fast acetylators”), which leads to a decrease in their plasma concentrations.
Increases the risk of developing hepatotoxic effects of paracetamol (induction of liver enzymes and the formation of a toxic metabolite of paracetamol).
Increases (with long-term therapy) the content of folic acid.
Hypokalemia caused by dexamethasone may increase the severity and duration of muscle blockade due to muscle relaxants.
In high doses, it reduces the effect of somatropin.
Dexamethasone reduces the effect of hypoglycemic drugs; enhances the anticoagulant effect of coumarin derivatives.
Weakens the effect of vitamin D on calcium absorption in the intestinal lumen. Ergocalciferol and parathyroid hormone prevent the development of osteopathy caused by dexamethasone.
Reduces the concentration of praziquantel in the blood.
Cyclosporine (inhibits metabolism) and ketoconazole (reduces clearance) increase toxicity.
Thiazide diuretics, carbonic anhydrase inhibitors, other corticosteroids and amphotericin B increase the risk of hypokalemia, sodium-containing drugs - edema and increased blood pressure.
Nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol increase the risk of developing ulceration of the gastrointestinal mucosa and bleeding; in combination with NSAIDs for the treatment of arthritis, it is possible to reduce the dose of GCS due to the summation of the therapeutic effect.
Indomethacin, displacing dexamethasone from its association with albumin, increases the risk of developing its side effects.
Amphotericin B and carbonic anhydrase inhibitors increase the risk of osteoporosis.
The therapeutic effect of dexamethasone is reduced by the influence of phenytoin, barbiturates, ephedrine, theophylline, rifampicin and other inducers of microsomal liver enzymes (increased metabolic rate).
Mitotane and other inhibitors of adrenal function may necessitate an increase in the dose of dexamethasone.
Dexamethasone clearance increases with the use of thyroid hormone medications.
Immunosuppressants increase the risk of developing infections and lymphoma or other lymphoproliferative disorders caused by the Epstein-Barr virus.
Estrogens (including oral estrogen-containing contraceptives) reduce the clearance of dexamethasone, prolong T1/2 and their therapeutic and toxic effects. The appearance of hirsutism and acne is facilitated by the simultaneous use of other steroid hormonal drugs - androgens, estrogens, anabolic agents, oral contraceptives.
Tricyclic antidepressants may increase the severity of depression caused by the use of dexamethasone (not indicated for the treatment of these side effects).
The risk of developing cataracts increases when used in combination with other corticosteroids, antipsychotic drugs (neuroleptics), carbutamide and azathioprine.
Simultaneous administration with m-anticholinergics (including antihistamines, tricyclic antidepressants), nitrates contributes to the development of increased intraocular pressure.
When used simultaneously with fluoroquinolones, the risk of tendonopathy (mainly Achilles tendon) increases in elderly patients and in patients with tendon diseases.
Antimalarials (chloroquine, hydroxychloroquine, mefloquine) in combination with dexamethasone may increase the risk of developing myopathy and cardiomyopathy.
Angiotensin-converting enzyme inhibitors, when administered concomitantly with dexamethasone, can change the composition of peripheral blood.
Contraindications
The only contraindication for systemic use in a short course for health reasons is hypersensitivity to the components of the drug.
Contraindications to the use of Dexamethasone (IV, IM, per os):
- infectious and parasitic diseases of a bacterial or viral nature;
- systemic mycoses ;
- immunodeficiency states;
- the period before and after preventive vaccination (especially before and after antiviral vaccinations);
- myasthenia gravis , systemic osteoporosis ;
- gastrointestinal diseases ( ulcer , colitis , diverticulitis , newly created intestinal anostomosis, etc.);
- CVD diseases;
- diabetes;
- psychosis;
- acute liver and kidney failure .
Intra-articular administration is prohibited when:
- joint instability;
- pathological bleeding;
- previous arthroplasty;
- transarticular fractures;
- the presence of infected lesions of joints, intervertebral spaces,
- periarticular soft tissues;
- severe periarticular osteoporosis .
Contraindications to the use of eye drops:
- tuberculous, fungal, viral eye lesions;
- trachoma;
- glaucoma;
- epithelial damage to the cornea.
Instillations into the ear canal are contraindicated if the integrity of the eardrum is compromised.
Side effects of Dexamethasone
The incidence and severity of side effects of Dexamethasone depend on the dosage of the drug, duration of use of the drug, and the possibility of use taking into account the circadian rhythm.
Systemic side effects of Dexamethasone:
- from the sensory organs and the nervous system: delirium, euphoria, depressive/manic episode, disorientation, hallucinations, increased ICP with congestive optic disc syndrome (benign intracranial hypertension , the development of which is a consequence of a rapid reduction in the dosage of the drug and is accompanied by blurred vision and headaches), vertigo , sleep disturbances, headache, dizziness, loss of vision (when the solution is administered in the area of the nasal concha, head, neck, scalp), cataract with localization of clouding in the back of the lens, glaucoma , eye hypertension with the possibility of damage to the optic nerve, development of secondary viral/fungal infection of the eye, steroid exophthalmos ;
- from the cardiovascular system: arterial hypertension , myocardial dystrophy , ECG changes characteristic of hypokalemia, hypercoagulation , thrombosis , if predisposed - the development of CHF, with parenteral use - rushes of blood to the head;
- from the digestive system: nausea, hiccups, vomiting, pancreatitis , erosive and ulcerative lesions of the digestive canal, increased/decreased appetite, erosive esophagitis;
- metabolic disorders: peripheral edema due to water and Na+ retention, nitrogen deficiency, hypocalcemia , hypokalemia , weight gain;
- endocrine disorders: hyper- or hypocorticism syndrome, manifestation of latent diabetes mellitus , steroid diabetes, growth retardation in children, irregular menstrual bleeding, hirsutism ;
- from the locomotor system: joint or muscle pain, back pain, steroid myopathy, tendon rupture, osteoporosis , muscle weakness, decreased muscle mass; with intra-articular administration of the solution, the intensity of pain in the joint may increase;
- from the skin: stretch marks , ecchymosis and petechiae, steroid acne, thinning of the skin, increased sweating, poor wound healing;
- hypersensitivity reactions: urticaria , skin rashes, difficulty breathing, stridor, facial swelling, anaphylactic shock .
Also possible: decreased immune system function, activation of infectious diseases, withdrawal syndrome (general weakness, lethargy, nausea, anorexia, abdominal pain).
Local reactions when injecting the solution: numbness, burning, paresthesia, pain, infection at the injection site, scarring at the injection site, hypo- or hyperpigmentation. When administered intramuscularly, the process of atrophy of the subcutaneous tissue and skin may begin.
Reactions to the use of ophthalmic forms: long-term (more than 3 weeks in a row) use of eye drops may be accompanied by an increase in intraocular pressure, the formation of glaucoma with damage to the optic nerve fibers, posterior subcapsular cataracts , visual impairment (for example, loss of its fields), thinning/perforation cornea, spread of infection (bacterial or herpetic).
In case of hypersensitivity to benzalkonium chloride or dexamethasone blepharitis and conjunctivitis are possible .
Local reactions are manifested by burning and itching of the skin, irritation, and dermatitis.
Dexamethasone, 10 pcs., 2 ml, 4 mg/ml, solution for injection
Dexamethasone is a synthetic hormone of the adrenal cortex, a glucocorticosteroid (GCS), a methylated derivative of fluoroprednisolone. It has anti-inflammatory, antiallergic, desensitizing, antishock, antitoxic and immunosuppressive effects.
It interacts with specific cytoplasmic glucocorticosteroid receptors to form a complex that penetrates the cell nucleus and stimulates the synthesis of matrix ribonucleic acid, the latter inducing the formation of proteins, including lipocortin, that mediate cellular effects. Lipocortin inhibits phospholipase A2, suppresses the release of arachidonic acid and suppresses the synthesis of endoperoxides, prostaglandins, leukotrienes, which contribute to inflammation, allergies, etc.
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 (fat accumulation occurs mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.
Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract (GIT); increases the activity of glucose-6-phosphatase, which leads to an increase in the flow of glucose from the liver into the blood; increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases, which leads to the activation of gluconeogenesis.
Water-electrolyte metabolism: retains sodium (Na+) and water in the body, stimulates the excretion of potassium (K+) (mineralocorticoid activity), reduces the absorption of calcium (Ca2+) from the gastrointestinal tract, “washes out” Ca2+ from the bones, increases the excretion of Ca2+ by the kidneys.
The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils; inducing the formation of lipocortin and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes and organelle membranes (especially lysosomal ones).
The antiallergic effect develops as a result of suppression of the synthesis and secretion of allergic mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, a decrease in the number of circulating basophils, suppression of the development of lymphoid and connective tissue, a decrease in the number of T- and B-lymphocytes, mast cells , reducing the sensitivity of effector cells to allergy mediators, suppressing antibody formation, changing the body’s immune response.
In chronic obstructive pulmonary disease, the effect is based mainly on inhibition of inflammatory processes, inhibition of development or prevention of swelling of the mucous membranes, inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium, deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucous membrane. Increases the sensitivity of beta-adrenergic receptors of small and medium-caliber bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by inhibiting or reducing its production.
The antishock and antitoxic effect is associated with an increase in blood pressure (BP) due to an increase in the concentration of circulating catecholamines and restoration of the sensitivity of adrenergic receptors to them, as well as vasoconstriction), a decrease in the permeability of the vascular wall, membrane protective properties, and activation of liver enzymes involved in the metabolism of endo- and xenobiotics.
The immunosuppressive effect is due to inhibition of the release of cytokines (interleukin-1 and interleukin-2, interferon gamma) from lymphocytes and macrophages.
Dexamethasone has a 30 times more pronounced effect than endogenous cortisol. Therefore, it is a more potent inhibitor of the secretion of corticotropin-releasing hormone and ACTH. In pharmacological doses, it inhibits the hypothalamic-pituitary-adrenal system and promotes the development of secondary adrenal insufficiency. Suppresses the synthesis and release of adrenocorticotropic hormone (ACTH) by the pituitary gland and, secondarily, the synthesis of endogenous GCS. Inhibits the secretion of thyroid-stimulating hormone and follicle-stimulating hormone. Suppresses the release of beta-lipotropin, but does not reduce the content of circulating beta-endorphin.
Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
Increases the excitability of the central nervous system, reduces the number of lymphocytes and eosinophils, and increases the number of red blood cells (by stimulating the production of erythropoietin).
The peculiarity of the action is significant inhibition of pituitary function and the almost complete absence of mineralocorticoid activity.
Instructions for use of Dexamethasone (Method and dosage)
Dexamethasone injections, instructions for use
Methods of administration of Dexamethasone: intravenous, intramuscular, local.
The daily dose is equivalent to 1/3-01/2 of the oral dose and ranges from 0.5 to 24 mg. It should be given for 2 injections. Treatment is carried out in the minimum effective dose and for the shortest possible course. The drug is discontinued gradually. For long-term use, the highest dose is 0.5 mg/day.
Injections are prescribed for emergency conditions, as well as in cases where oral administration is not possible. In emergency conditions, higher doses of the drug (4-20 mg) are allowed, and the dose is repeated until the required therapeutic effect is achieved. The daily dose in rare cases exceeds 80 mg.
Once the required results are achieved, treatment is continued at a dose of 2-4 mg, gradually reducing it until the drug is completely discontinued.
To maintain a long-term effect, injections are indicated at intervals of 3-4 hours. It is also possible to administer Dexamethasone intravenously by long-term drip infusion.
After completion of the acute phase of the disease, the patient is transferred to taking the drug orally.
No more than 2 ml of the product can be injected into the muscle at the same place.
The treatment regimen depends on the indications:
- for shock - 2-6 mg/kg IV bolus, repeated injections - every 2-6 hours or as a long-term infusion using a dose of 3 mg/kg/day. The drug is prescribed as an addition to the main antishock therapy. The administration of these doses is permissible only for conditions that threaten the patient’s life, and, as a rule, this period lasts up to 72 hours.
- For cerebral edema (CBE), treatment begins with a dose of 10 mg (iv), then - until symptoms stop (within 12-24 hours) - 4 mg is administered every 6 hours. After 2-4 days, the dose is reduced and Dexamethasone administration is stopped within 5-7 days.
- For cancer, maintenance therapy may be required - 2 mg IV or IM 2 or 3 times a day.
- In case of acute AMG, the patient requires short-term intensive therapy. The loading dose of the drug for an adult is 50 mg, for a child weighing up to 35 kg - 20 mg (injected into a vein). After this, the dose is gradually reduced while increasing the intervals between drug administrations.
- For allergies (in particular, with exacerbation of chronic diseases of an allergic nature and with acute self-limiting reactions), parenteral administration is combined with oral administration of the drug. Allergy injections are given only on the first day, injecting the patient with 4 to 8 mg of Dexamethasone into a vein. On days 2-3, take 1 mg of the drug orally 2 times, on days 4-5 - 2 times 0.5 mg, on days 6-7 - 0.5 mg (once). On day 8, the effectiveness of treatment is assessed.
When status asthmaticus requires immediate intravenous administration of the drug, the combination Dexamethasone + Eufillin . The first medicine reduces the release of mediators ( heparin , histamine , serotonin ) from the cell, protects tissues from destructive processes, prevents the formation of arachidonic acid metabolites, and Eufillin reduces the resistance of blood vessels, relieves bronchospasm , inhibits platelet aggregation and dilates coronary vessels.
Instructions for Dexamethasone in ampoules for topical use
When applying the solution topically, 2 to 4 mg is injected into large joints, and 0.8 to 1 mg into small joints. Treatment of soft tissue infiltrates involves the use of 2-6 mg of the drug. 1-2 mg of the drug should be injected into the nerve ganglia, 2 to 3 mg into the joint capsules, and 0.4 to 1 mg into the synovial vagina. The dose is administered once. The course lasts from 3-5 to 14-20 days.
For children, the drug is administered in minimally effective doses.
Use of Dexamethasone in ampoules for inhalation
Inhaled use of Dexamethasone is indicated for acute inflammatory diseases of the respiratory tract (for example, bronchitis or laryngitis , as well as bronchial obstruction ).
Inhalations with Dexamethasone for children should be done 3 times a day, mixing 0.5 ml of the drug with 2-3 ml of saline solution. As a rule, treatment is continued for 3 to 7 days.
You can dilute the drug in saline in a ratio of 1:6, and then use 3-4 ml of the prepared solution for inhalation.
Dexamethasone tablets, instructions for use
The dose for oral administration is selected individually depending on the type of disease, the activity of its course and the nature of the patient’s response to the prescribed treatment.
The average daily dose ranges from 0.75 to 9 mg. For severe diseases, the dose can be increased, and it is divided into several doses. The highest dose is 15 mg/day.
The optimal dosage for children is selected depending on age, and usually ranges from 2.5 to 10 mg/m2/day. It must be divided into 3 or 4 doses.
The duration of the course is determined by the nature of the pathological process and the patient’s body’s response to treatment. In some cases, Dexamethasone is continued for several months.
Liddle's test
The test with Dexamethasone is carried out in the form of small and large tests.
A small test involves prescribing the patient 0.5 mg of Dexamethasone 4 times a day at regular intervals (6 hours). Urine to determine free cortisol should be collected from 8:00 to 8:00 on the second day before the drug is prescribed and at the same time intervals after taking the required dose.
2 mg of Dexamethasone taken over the course of 24 hours suppresses the production of corticosteroids in almost every healthy person. The cortisol content 6 hours after taking the last 0.5 mg of the drug does not exceed 135-138 nmol/l. A decrease in the daily excretion of free cortisol below 55 nmol, and 17‑OX below 3 mg/day. eliminates hyperfunction of the adrenal cortex.
In hypercortisolism syndrome, no changes in drug secretion are observed.
A large test involves prescribing 2 mg once every 6 hours for 48 hours. Hypercortisolism syndrome diagnosed by reducing free cortisol and 17-OCS levels by 50 (or more) percent.
In patients with ACTH-ectopic syndrome and adrenal tumors, drug excretion rates do not change. In some cases, with ACTH-ectopic syndrome, they do not change even when taking 32 mg of Dexamethasone per day.
Dexamethasone eye drops, instructions for use
Eye drops are intended for topical use. In case of severe inflammation, in the first day or two of treatment, 1-2 drops are instilled into the conjunctival sac. every 2 hours. Further, the intervals between instillations are extended to 4-6 hours.
To prevent the development of inflammation in the first 24 hours after injury or surgery, the patient is instilled 4 times a day. 1-2 drops, then treatment is continued at the same dose, but with a smaller frequency of applications (usually the procedure is repeated 3 times a day). The course lasts 14 days.
As an alternative to drops, Dexamethasone ointment can be used. It is squeezed out into a 1-1.5 cm strip and placed behind the lower eyelid. The frequency of procedures is 2-3 during the day. You can combine the use of ointment and drops (for example, drops during the day and ointment before bed).
To treat otitis media , the drug is injected into the ear canal of the diseased ear 2-3 times a day. 3-4 drops each.
Dexamethasone solution for injection 4 mg/ml 2 ml ampoule, 10 pcs.
Manufacturer
Ellara, Russia
Compound
Per 1 ml: Active substance:
dexamethasone sodium phosphate (in terms of dexamethasone phosphate) -4.0 mg.
Excipients: glycerol (distilled glycerin PK-94) - 22.5 mg, sodium hydrogen phosphate dodecahydrate (sodium phosphate disubstituted 12-water) -0.8 mg; disodium edetate dihydrate [(disodium salt ethylenediamine-N, N, N', N' - tetraacetic acid 2-aqueous (trilon B)] - 0.1 mg; water for injection - up to 1 ml.
pharmachologic effect
Pharmacotherapeutic group: glucocorticosteroid ATX code: Н02АВ02 Pharmacological properties
Pharmacodynamics
Dexamethasone is a synthetic hormone of the adrenal cortex, a glucocorticosteroid (GCS), a methylated derivative of fluoroprednisolone. It has anti-inflammatory, antiallergic, desensitizing, antishock, antitoxic and immunosuppressive effects.
Interacts with specific cytoplasmic GCS receptors to form a complex that penetrates the cell nucleus and stimulates the synthesis of matrix ribonucleic acid, the latter induces the formation of proteins, including lipocortin, that mediate cellular effects. Lipocortin inhibits phospholipase A2, suppresses the release of arachidonic acid and suppresses the synthesis of endoperoxides, prostaglandins, leukotrienes, which contribute to inflammation, allergies, etc.
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 (fat accumulation occurs mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.
Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract (GIT); increases the activity of glucose-6-phosphatase, which leads to an increase in the flow of glucose from the liver into the blood; increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases, which leads to the activation of gluconeogenesis.
Water-electrolyte metabolism: retains sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, “washes” calcium from the bones, increases the excretion of calcium by the kidneys.
The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils; inducing the formation of lipocortin and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes and organelle membranes (especially lysosomal ones).
The antiallergic effect develops as a result of suppression of the synthesis and secretion of allergic mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, a decrease in the number of circulating basophils, suppression of the development of lymphoid and connective tissue, a decrease in the number of T- and B-lymphocytes, mast cells , reducing the sensitivity of effector cells to allergy mediators, suppressing antibody formation, changing the body’s immune response.
In chronic obstructive pulmonary disease, the effect is based mainly on inhibition of inflammatory processes, inhibition of the development or prevention of swelling of the mucous membranes, inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium, deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucous membrane. Increases the sensitivity of beta-adrenergic receptors of small and medium caliber bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of bronchial secretions due to inhibition or reduction of its production.
Antishock and antitoxic effects are associated with an increase in blood pressure (due to an increase in the concentration of circulating catecholamines and restoration of the sensitivity of adrenergic receptors to them, as well as vasoconstriction), a decrease in the permeability of the vascular wall, membrane protective properties, and activation of liver enzymes involved in the metabolism of endo- and xenobiotics.
The immunosuppressive effect is due to inhibition of the release of cytokines (interleukin-1 and interleukin-2, interferon gamma) from lymphocytes and macrophages.
Dexamethasone has a 30 times more pronounced effect than endogenous cortisol. Therefore, it is a more potent inhibitor of the secretion of corticotropin-releasing hormone and adrenocorticotropic hormone (ACTH). In pharmacological doses, it inhibits the hypothalamic-pituitary-adrenal system and promotes the development of secondary adrenal insufficiency. Suppresses the synthesis and release of ACTH by the pituitary gland and, secondarily, the synthesis of endogenous corticosteroids. Inhibits the secretion of thyroid-stimulating hormone and follicle-stimulating hormone. Suppresses the release of beta-lipotropin, but does not reduce the content of circulating beta-endorphin.
Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
Increases the excitability of the central nervous system. Reduces the number of lymphocytes and eosinophils, increases - red blood cells (by stimulating the production of erythropoietins).
The peculiarity of the action is significant inhibition of pituitary function and the almost complete absence of mineralocorticoid activity.
Pharmacokinetics Absorption The maximum concentration of dexamethasone in the blood plasma is achieved within 5 minutes after intravenous administration and 1 hour after intramuscular administration.
Distribution: Bonding with plasma proteins (mainly albumin) - 77%. Penetrates through the blood-brain and placental barriers. The half-life (T 1/2) from plasma is 190 minutes.
Metabolism Metabolized in the liver. A small amount of dexamethasone is metabolized in the kidneys and other organs.
Excretion Up to 65% of the dose is excreted by the kidneys within 24 hours.
Time to develop clinical effect When administered intravenously, the effect develops quickly; with intramuscular use, the clinical effect develops after 8 hours. The effect is long-lasting: from 17 to 28 days after intramuscular use and from 3 days to 3 weeks after topical application. When administered locally into joints or soft tissues (into lesions), absorption occurs more slowly than with intramuscular use.
Indications
Replacement therapy for adrenal insufficiency (in combination with sodium chloride and/or mineralocorticosteroids): acute adrenal insufficiency (Addison's disease, bilateral adrenalectomy); relative insufficiency of the adrenal cortex, developing after discontinuation of treatment with corticosteroids; primary or secondary adrenal insufficiency.
Symptomatic and pathogenetic therapy of other diseases requiring the administration of fast-acting corticosteroids, as well as in cases where oral administration of the drug is impossible:
- endocrine diseases (congenital adrenal hyperplasia, subacute thyroiditis); — shock (burn, traumatic, surgical, toxic) — in case of ineffectiveness of vasoconstrictors, plasma replacement drugs and other symptomatic therapy; - cerebral edema (only after confirmation of symptoms of increased intracranial pressure by magnetic resonance or computed tomography results) caused by a brain tumor due to traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury; — asthmatic status; severe bronchospasm (exacerbation of bronchial asthma); - severe allergic reactions, anaphylactic shock; - 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 with malignant tumors, when oral treatment is not possible); - blood diseases (acute hemolytic anemia, agranulocytosis, idiopathic thrombocytopenic purpura in adults); - in ophthalmological practice (subconjunctival, retrobulbar or parabulbar administration): keratitis, keratoconjunctivitis without damage to the epithelium, iritis, iridocyclitis, blepharitis, blepharoconjunctivitis, scleritis, episcleritis, inflammatory process after eye injuries and surgical interventions, sympathetic ophthalmia, immunosuppressive treatment after corneal transplantation; — local application (in the area of pathological formation): keloids, discoid lupus erythematosus, granuloma annulare; - poisoning with cauterizing liquids (reducing inflammation and preventing cicatricial contractions).
Use during pregnancy and breastfeeding
Dexamethasone crosses the placenta and can reach high concentrations in the fetus. During pregnancy (especially in the first trimester) or in women planning a pregnancy, taking Dexamethasone is indicated if the expected therapeutic effect of the drug exceeds the risk of negative effects on the mother or fetus. GCS should be prescribed during pregnancy only for absolute indications. With long-term therapy during pregnancy, the possibility of impaired fetal growth cannot be excluded. If used 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.
A small amount of dexamethasone passes into breast milk.
If it is necessary to carry out treatment with the drug during breastfeeding, breastfeeding should be discontinued, as this may lead to retardation of the child's growth and a decrease in the secretion of his endogenous corticosteroids.
Contraindications
For short-term use for “life-saving” indications, the only contraindication is hypersensitivity to any of the components of the drug. Breastfeeding period, systemic mycoses. Concomitant use of live or attenuated vaccines with immunosuppressive doses of Dexamethasone.
Carefully
Systemic parasitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently suffered, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles; amebiasis, strongyloidiasis (established or suspected); active or latent tuberculosis. Use for severe infectious diseases is permissible only against the background of specific antimicrobial therapy.
Vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency conditions (including AIDS or HIV infection).
Gastrointestinal diseases: peptic ulcer of the stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis.
Liver failure.
Hypoalbuminemia and conditions predisposing to its occurrence.
Diseases of the cardiovascular system, including recent myocardial infarction, decompensated chronic heart failure, arterial hypertension, hyperlipidemia.
Endocrine diseases - diabetes mellitus (including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, stage III-IV obesity.
Severe chronic renal failure, nephrourolithiasis.
Systemic osteoporosis, myasthenia gravis, poliomyelitis (except for the form of bulbar encephalitis), epilepsy, “steroid” myopathy.
Acute psychosis, severe affective disorders (including a history of, especially “steroid” psychosis).
Open- and closed-angle glaucoma, eye herpes (risk of corneal perforation).
Pregnancy.
Elderly patients - due to a high risk of developing osteoporosis and arterial hypertension.
In children during the growth period, dexamethasone should be used only for absolute indications and under the careful supervision of the attending physician.
Side effects
The incidence and severity of side effects depend on the duration of use, the size of the dose used and the ability to comply with the circadian rhythm of the prescription.
Endocrine system disorders: decreased glucose tolerance, “steroidal” diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing syndrome (moon face, pituitary type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis, “ steroid stretch marks), delayed sexual development in children.
Blood and lymphatic system disorders: moderate leukocytosis, lymphopenia, eosinopenia, polycythemia.
Gastrointestinal tract disorders: nausea, vomiting, pancreatitis, “steroid” gastric and duodenal ulcers, erosive esophagitis, bleeding and perforation of the stomach or intestines, increased or decreased appetite, flatulence, hiccups, abdominal pain, discomfort in the stomach area. In rare cases, increased activity of liver transaminases and alkaline phosphatase.
Disorders of the heart and blood vessels: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or worsening of chronic heart failure; electrocardiogram changes characteristic of hypokalemia; increased blood pressure, hypercoagulation, thrombosis; with intravenous administration: “hot flashes” to the face, vasculitis, increased capillary fragility. In patients with acute and subacute myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.
Mental disorders: nervousness or anxiety, insomnia, emotional lability, delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, suicidal tendencies.
Nervous system disorders: increased intracranial pressure, dizziness, headache, vertigo, cerebellar pseudotumor, convulsions.
Violations of the organ of vision: sudden loss of vision (with parenteral administration in the head, neck, nasal turbinates, scalp, deposition of drug crystals in the vessels of the eye is possible), posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos, chemosis, ptosis, mydriasis, corneal perforation, central serous chorioretinopathy.
Metabolic and nutritional disorders: hypercholesterolemia, increased calcium excretion, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating, epidural lipomatosis.
Caused by mineralocorticoid activity - fluid and sodium retention (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).
Disorders of the musculoskeletal and connective tissue: slowing of growth and ossification processes in children (premature closure of the epiphyseal growth plates), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and femur), rupture of muscle tendons, "steroid" myopathy, decreased muscle mass (atrophy).
Renal and urinary tract disorders: leukocyturia.
Disorders of the skin and subcutaneous tissues: delayed wound healing, petechiae, ecchymoses, thinning of the skin, hyper- or hypopigmentation, “steroid” acne, “steroid” striae, a tendency to develop pyoderma and candidiasis, rosacea-like perioral dermatitis, suppression of reactions during skin samples, telangiectasia, hypertrichosis.
Immune system disorders: generalized (skin rash, skin itching, anaphylactic shock), local allergic reactions.
Infectious and parasitic diseases: development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination).
General disorders and disorders at the injection site: withdrawal syndrome, local with parenteral administration: 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 (injection into the deltoid muscle is especially dangerous).
Interaction
Dexamethasone is pharmaceutically incompatible with other drugs (may form insoluble compounds). It is recommended to administer it separately from other drugs (iv bolus, or through another dropper, as a second solution). When mixing a solution of dexamethasone with heparin, a precipitate forms.
Dexamethasone increases the toxicity of cardiac glycosides (due to the resulting hypokalemia, the risk of developing arrhythmias increases).
Accelerates the elimination of acetylsalicylic acid, reduces the content of its metabolites in the blood (when dexamethasone is discontinued, the concentration of salicylates in the blood increases and the risk of side effects increases).
When used simultaneously with live antiviral vaccines and against the background of other types of immunizations, it increases the risk of viral activation and the development of infections.
Increases the metabolism of isoniazid, mexiletine (especially in “fast acetylators”), which leads to a decrease in their concentrations in the blood plasma.
Increases the risk of developing hepatotoxic effects of paracetamol (induction of liver enzymes and the formation of a toxic metabolite of paracetamol).
Increases (with long-term therapy) the content of folic acid.
Hypokalemia caused by dexamethasone may increase the severity and duration of muscle blockade due to muscle relaxants.
In high doses, it reduces the effect of somatropin.
Dexamethasone reduces the effect of hypoglycemic drugs; enhances the anticoagulant effect of coumarin derivatives.
Weakens the effect of vitamin D on calcium absorption in the intestinal lumen. Ergocalciferol and parathyroid hormone prevent the development of osteopathy caused by dexamethasone.
Reduces the concentration of praziquantel in the blood.
Cyclosporine (inhibits metabolism) and ketoconazole (reduces clearance) increase toxicity.
Thiazide diuretics, carbonic anhydrase inhibitors, other corticosteroids and amphotericin B increase the risk of hypokalemia, Na-containing drugs - edema and increased blood pressure.
Nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol increase the risk of developing ulceration of the gastrointestinal mucosa and bleeding; in combination with NSAIDs for the treatment of arthritis, it is possible to reduce the dose of GCS due to the summation of the therapeutic effect.
Indomethacin, displacing dexamethasone from its association with albumin, increases the risk of developing its side effects.
Amphotericin B and carbonic anhydrase inhibitors increase the risk of osteoporosis. The therapeutic effect of dexamethasone is reduced under the influence of phenytoin, barbiturates, ephedrine, theophylline, rifampicin and other inducers of microsomal liver enzymes (increased metabolic rate). Mitotane and other inhibitors of adrenal function may necessitate an increase in the dose of dexamethasone.
Dexamethasone clearance increases with the use of thyroid hormone medications.
Immunosuppressants increase the risk of developing infections and lymphoma or other lymphoproliferative disorders caused by the Epstein-Barr virus.
Estrogens (including oral estrogen-containing contraceptives) reduce the clearance of dexamethasone, prolong the half-life and their therapeutic and toxic effects.
The appearance of hirsutism and acne is facilitated by the simultaneous use of other steroid hormonal drugs - androgens, estrogens, anabolic steroids, oral contraceptives.
Tricyclic antidepressants may increase the severity of depression caused by taking dexamethasone (not indicated for the treatment of these side effects).
The risk of developing cataracts increases when used in combination with other corticosteroids, antipsychotic drugs (neuroleptics), carbutamide and azathioprine. Simultaneous administration with m-anticholinergics (including antihistamines, tricyclic antidepressants), nitrates contributes to the development of increased intraocular pressure.
When used simultaneously with fluoroquinolones, the risk of tendonopathy (mainly Achilles tendon) increases in elderly patients and in patients with tendon diseases.
Antimalarials (chloroquine, hydroxychloroquine, mefloquine) in combination with dexamethasone may increase the risk of developing myopathy and cardiomyopathy.
Angiotensin-converting enzyme inhibitors, when administered concomitantly with dexamethasone, can change the composition of peripheral blood.
How to take, course of administration and dosage
The dosage regimen is individual and depends on the indications, the patient’s condition and his response to therapy. The drug is administered intravenously (IV) slowly in a stream or drip (in acute and emergency conditions); intramuscularly (i.m.); local (into the pathological formation) and subconjunctival, retrobulbar or parabulbar administration is also possible.
To prepare a solution for intravenous infusion, use an isotonic sodium chloride solution or a 5% dextrose solution.
The drug is administered intravenously and intramuscularly at a dose of 0.5-24 mg/day in 2 doses (equivalent to 1/3 - 1/2 oral dose) in the shortest possible course at the minimum effective dose, treatment is discontinued gradually. If high doses are used for more than a few days, the dose of the drug should be gradually reduced over the next few days or longer. Long-term treatment should be carried out at a dose not exceeding 0.5 mg/day. No more than 2 ml of solution is injected intramuscularly into the same place.
In emergency situations, higher doses are used: the initial dose is 4-20 mg, which is repeated until the desired effect is achieved, the total daily dose rarely exceeds 80 mg. After achieving a therapeutic effect, dexamethasone is administered at a dose of 2-4 mg as needed, followed by gradual withdrawal of the drug. To maintain a long-term effect, the drug is administered every 3-4 hours or as a long-term drip infusion. After relief of acute conditions, the patient is transferred to oral dexamethasone.
In case of shock, administer strictly intravenously as a bolus at a dose of 2-6 mg/kg. If necessary, repeated doses are administered every 2-6 hours or as a long-term intravenous infusion at a dose of 3 mg/kg/day. Treatment with dexamethasone should be carried out as part of complex therapy for shock. The use of pharmacological doses is permissible only in life-threatening conditions, and, as a rule, this time does not exceed 48 - 72 hours.
For cerebral edema, an initial dose of 10 mg is administered intravenously, then 4 mg every 6 hours until symptoms subside (usually within 12-24 hours). After 2-4 days, the dose is reduced and the use of the drug is gradually stopped over 5-7 days.
Patients with malignant neoplasms may require maintenance treatment - 2 mg IM or IV 2-3 times a day.
In case of acute cerebral edema, short-term intensive therapy is carried out: for adults, the loading dose is 50 mg IV, then on days 1-3, 8 mg is administered every 2 hours, on the 4th day - 4 mg every 2 hours, on days 5-8 day - 4 mg every 4 hours, then the daily dose is reduced by 4 mg/day until it is completely discontinued. For children weighing more than 35 kg, the loading dose is 25 mg IV, then 4 mg every 2 hours on days 1-3, 4 mg every 4 hours on days 4, 4 mg every 4 hours on days 5-8. mg every 6 hours, then the daily dose is reduced by 2 mg/day until it is completely discontinued. For children weighing less than 35 kg, the loading dose is 20 mg IV, then 4 mg every 3 hours on days 1-3, 4 mg every 6 hours on days 4, 2 mg every 6 hours on days 5-8. mg every 6 hours, then the daily dose is reduced by 1 mg/day until it is completely discontinued. In case of acute self-limiting allergic reactions or exacerbation of chronic allergic diseases, parenteral and oral administration of dexamethasone is combined: day 1 - IV 4-8 mg, days 2-3 - orally 1 mg 2 times a day, days 4-5 - orally 0.5 mg 2 times a day, 6-7 days - 0.5 mg orally once. On the 8th day, the effectiveness of therapy is assessed.
Doses of the drug for children (im): the dose of the drug during replacement therapy (for adrenal insufficiency) is 0.0233 mg/kg body weight or 0.67 mg/m2 body surface area, divided into 3 doses, each 3- th day or 0.00776-0.01165 mg/kg body weight or 0.233-0.335 mg/m2 body surface area daily. For other indications, the recommended dose is 0.02776 to 0.16665 mg/kg body weight or 0.833 to 5 mg/m2 body surface area every 12 to 24 hours.
Overdose
Symptoms: increased blood pressure, peripheral edema, peptic ulcer, hyperglycemia, impaired consciousness. Treatment: symptomatic, there is no specific antidote.
Description
Transparent colorless or yellowish liquid.
Special instructions
During treatment with dexamethasone (especially long-term), observation by an ophthalmologist, monitoring of blood pressure and water-electrolyte balance, as well as peripheral blood patterns and blood glucose levels are necessary.
In order to reduce side effects, the intake of K+ into the body should be increased (diet, potassium supplements). Food should be rich in proteins, vitamins, and limit the content of fats, carbohydrates and table salt.
The effect of the drug is enhanced in patients with liver cirrhosis. It must be taken into account that in patients with hypothyroidism the clearance of dexamethasone is reduced, and in patients with thyrotoxicosis it is increased.
The drug may worsen existing emotional instability or psychotic disorders. If a history of psychosis is indicated, dexamethasone in high doses is prescribed under the strict supervision of a physician.
It should be used with caution in acute and subacute myocardial infarction - the necrosis focus may spread, the formation of scar tissue may slow down, and the heart muscle may rupture.
The patient should be carefully monitored for a year after the end of long-term dexamethasone therapy due to the possible development of relative adrenal insufficiency in stressful situations.
Long-term use of high doses of the drug requires a gradual dose reduction in order to prevent the development of acute adrenal insufficiency.
When using dexamethasone, there is a risk of developing severe anaphylactic reactions and bradycardia.
During drug therapy, the risk of activation of strongyloidiasis increases.
The dose of dexamethasone must be temporarily increased in stressful situations during therapy (surgery, trauma). A temporary increase in the dose of the drug in stressful situations is necessary both before and after stress.
During treatment with dexamethasone, it is necessary to use specific antibacterial therapy in the treatment of latent tuberculosis, lymphadenitis after BCG vaccination, polio, acute and chronic bacterial and parasitic infections and specific therapy in patients with gastric and intestinal ulcers, osteoporosis.
During drug therapy, careful monitoring of the condition of patients with chronic heart failure, uncontrolled arterial hypertension, trauma and ulcerative lesions of the cornea, and glaucoma is necessary.
Myasthenia gravis may worsen.
If the drug is suddenly discontinued, especially in the case of previous use of high doses, acute adrenal insufficiency may develop; withdrawal syndrome (not caused by adrenal insufficiency): loss of appetite, nausea, vomiting; lethargy, headache, generalized musculoskeletal pain, asthenia; as well as exacerbation of the disease for which dexamethasone was prescribed.
In patients with diabetes mellitus, blood glucose concentrations should be monitored and, if necessary, doses of hypoglycemic drugs should be adjusted.
Dexamethasone may increase susceptibility to or mask symptoms of infectious diseases. Chickenpox, measles and other infections can be more severe and even fatal in unimmunized individuals. Immunosuppression most often develops with long-term use, but can also occur with short-term treatment with dexamethasone.
Taking the drug may mask the symptoms of “peritoneal irritation” in patients with perforation of the stomach or intestinal wall.
With the use of GCS, changes in sperm motility and number are possible.
Children who during the treatment period were in contact with patients with measles or chickenpox are prescribed specific immunoglobulins prophylactically. In children during long-term treatment with dexamethasone, careful monitoring of the dynamics of growth and development is necessary.
Impact on the ability to drive vehicles and machinery During treatment, driving, as well as engaging in potentially hazardous activities that require rapid psychomotor reactions and increased concentration of attention, are not recommended.
Storage conditions
In a place protected from light at a temperature not exceeding 25 °C. Keep out of the reach of children.
Best before date
2 years. Do not use the drug after the expiration date indicated on the package.
Active substance
Dexamethasone
Conditions for dispensing from pharmacies
On prescription
Dosage form
injection
Information in the State Register of Medicines
Go
Barcode and weight
Barcode: -, 4670008162619 Weight: 0.058 kg
special instructions
Application in bodybuilding
Taking Dexamethasone provokes a shift in metabolism towards anabolism, which, when using even a small dose of anabolic steroids, can accelerate the growth of muscle mass and make it more significant.
In addition, by suppressing the secretion of catabolic hormones , the drug helps increase endurance, accelerates the athlete's recovery after training, and suppresses pain and inflammation when ligaments and joints are damaged.
Since Dexamethasone belongs to the group of stress hormones, their use in sports is allowed only for short-term courses.
Dexamethasone in veterinary medicine
In veterinary medicine, the drug is used as an active anti-shock, anti-allergenic and anti-inflammatory agent.
Why is Dexamethasone prescribed to cats and dogs? The drug is used to treat shock conditions, injuries, arthritis, bursitis, allergic diseases, edema, poisoning, ketosis and acute mastitis.
The therapeutic dose for dogs and cats is 0.1-1 ml (depending on the size of the animal and indications).
Dexamethasone analogs
Level 4 ATC code matches:
Prednisolone
Polcortolon
Cortef
Dexazone
Metipred
Cortisone
Flosteron
Depo-Medrol
Medrol
Solu-Medrol
Diprospan
Kenalog
Analogues of solution and tablets:
- Dexazone
- Dexamethasone-Vial
- Dexamed
- Megadexane
- Dexamethasone-Ferrain
Similar preparations for eye drops:
- Dexamethasone-LENS
- Dexapos
- Ozurdex
- Maxidex
- Dexamethasonelong
The drug Maxidez, unlike other analogues, has 2 dosage forms: drops and eye ointment. Dexamethasone ointment can be replaced with Hydrocortisone .
Which is better: Prednisolone or Dexamethasone?
Prednisolone is a synthetic analogue of hydrocortisone , which is considered a standard agent with an average duration of action and is most often used in clinical practice.
Compared to Hydrocortisone, its glucocorticoid activity is 4 times higher, however, in terms of mineralocorticoid activity, Prednisolone is inferior to Hydrocortisone.
Dexamethasone is a long-acting medicine. Unlike its analogue, the drug is fluoridated. The glucocorticoid activity of the drug is 7 times higher than that of prednisolone . However, it does not have a mineralocorticoid effect.
To a greater extent than other drugs, it provokes inhibition of the hypothalamic-pituitary-adrenal axis, causes severe disturbances in calcium, lipid and carbohydrate metabolism, has a psychostimulating effect, and therefore is not recommended for long-term use.
CHARACTERISTICS OF INDIVIDUAL DRUGS
Depending on their structure, glucocorticoids differ in duration of action, severity of anti-inflammatory, mineralocorticoid, metabolic and immunosuppressive activity (Table 5). Moreover, there is no direct correlation between their immunosuppressive and anti-inflammatory effects. For example, dexamethasone has a powerful anti-inflammatory effect and relatively low immunosuppressive activity.
CORTISONE
The drug is a natural glucocorticoid, biologically inactive. Activated in the liver, turning into hydrocortisone. Has a short-term effect. Compared to other glucocorticoids, it has more pronounced mineralocorticoid activity, that is, it has a significant effect on water-electrolyte metabolism.
Features of application
Mainly used for replacement therapy
adrenal insufficiency in patients with normal liver function.
Release forms:
- tablets of 25 and 50 mg (cortisone acetate)
.
HYDROCORTISONE
A natural glucocorticoid, its glucocorticoid activity is 4 times weaker than prednisolone, but its mineralocorticoid activity is slightly superior. As with cortisone, there is a high risk of edema, sodium retention, and potassium loss.
Features of application
Hydrocortisone, like cortisone, is not recommended for pharmacodynamic therapy
, especially in patients with edema, hypertension, and heart failure.
It is used
mainly
for replacement therapy
for primary and secondary adrenal insufficiency. In acute adrenal insufficiency and other emergency conditions, the drug of choice is hydrocortisone hemisuccinate.
Release forms:
- hydrocortisone hemisuccinate, dry substance or solution in ampoules and bottles of 100 and 500 mg (hydrocortisone-meva, panukort, solu-cortef)
; - hydrocortisone acetate, suspension in ampoules and vials of 25 mg/ml.
PREDNISOONE
Synthetic glucocorticoid, most often used in clinical practice for pharmacodynamic therapy
and is considered as a standard drug. In glucocorticoid activity it is 4 times stronger than hydrocortisone, and in mineralocorticoid activity it is inferior to it. Refers to glucocorticoids with an average duration of action.
Release forms:
- tablets of 5, 10, 20 and 50 mg (ano-prednisone, decortin N, tednisol);
- prednisolone phosphate, 1 ml ampoules, 30 mg/ml;
- prednisolone hemisuccinate, powder in ampoules of 10, 25, 50 and 250 mg (decortin salt);
- prednisolone acetate, suspension in ampoules of 10, 20, 25 and 50 mg ( prednihexol).
PREDNISONE
In terms of activity and other parameters it is close to prednisolone. Initially, prednisone is a metabolically inactive drug (prodrug). Activated in the liver by hydroxylation and conversion to prednisolone. Therefore, it is not recommended to use it for severe liver diseases. The main advantage of prednisone is its lower cost.
Release forms:
- 5 mg tablets (prednisone).
METHYLPREDNISOLONE
Compared to prednisolone, it has slightly greater (20%) glucocorticoid activity, minimal mineralocorticoid effect, and is less likely to cause undesirable reactions (especially changes in the psyche, appetite, ulcerogenic effect). It has a higher cost than prednisolone.
Features of application
Just like prednisolone, it is used mainly for pharmacodynamic therapy. It is preferable in patients with mental disorders, obesity, peptic ulcer disease, as well as during pulse therapy.
Release forms:
- tablets of 4 and 16 mg (Medrol, Metypred, Urbazon, Prednol);
- methylprednisolone succinate, dry substance in ampoules and vials of 8, 20, 40, 125, 250, 500 mg, 1.0 and 2.0 g (metipred, prednol-L, solu-medrol);
- methylprednisolone acetate, suspension in 40 mg bottles (depo-medrol, metypred);
- methylprednisolone suleptanate, ampoules of 50 and 100 mg/ml (promedrol).
TRIAMCINOLONE
It is a fluorinated glucocorticoid. It has a stronger (20%) and longer-lasting glucocorticoid effect than prednisolone. Has no mineralocorticoid activity. More often causes undesirable reactions, especially from muscle tissue (“triamcinolone” myopathy) and skin (striae, hemorrhages, hirsutism).
Release forms:
- tablets of 2, 4 and 8 mg ( berlicort, delficort, kenacort, polcortolone
);
triamcinolone acetonide, suspension in ampoules of 40 mg/ml ( kenalog, tricort
); - triamcinolone hexacetonide, suspension in ampoules of 20 mg/ml ( Lederspan
).
DEXAMETHASONE
Just like triamcinolone, it is a fluorinated drug. One of the most powerful glucocorticoids: 7 times stronger than prednisolone in glucocorticoid activity. Does not have mineralocorticoid effect. It causes severe depression of the hypothalamic-pituitary-adrenal system, severe disturbances of carbohydrate, fat, calcium metabolism, and a psychostimulating effect, therefore it is not recommended to prescribe it for a long period.
Features of application
The drug has some special indications for use: bacterial meningitis; cerebral edema; in ophthalmology (keratitis, uveitis and others); prevention and treatment of nausea and vomiting during chemotherapy; treatment of severe withdrawal syndrome in alcoholism; prevention of respiratory distress syndrome in premature infants (dexamethasone stimulates the synthesis of surfactant in the alveoli of the lungs); leukemia (replacing prednisolone with dexamethasone in acute lymphoblastic leukemia significantly reduces the incidence of damage to the central nervous system).
Release forms:
- tablets of 0.5 and 1.5 mg (daxin, dexazone, cortidex);
- dexamethasone phosphate, ampoules of 1 and 2 ml, 4 mg/ml (daxin, dexabene, dexazone, sondex).
BETAMETHASONE
A fluorinated glucocorticoid, similar in strength and duration of action to dexamethasone. Glucocorticoid activity is 8-10 times higher than that of prednisolone. Does not have mineralocorticoid properties. It has a somewhat weaker effect on carbohydrate metabolism than dexamethasone. The best known drug is betamethasone phosphate/dipropionate, intended for intramuscular, intra-articular and periarticular administration. It consists of two esters, one of which - phosphate - is quickly absorbed from the injection site and gives a quick (within 30 minutes) effect, and the other - dipropionate - is absorbed slowly, but provides a prolonged effect - up to 4 weeks or more. It is a fine-crystalline suspension that cannot be administered intravenously. Water-soluble betamethasone phosphate is administered intravenously and subconjunctivally.
Dexamethasone during pregnancy and when planning pregnancy
Tablets are not used during treatment and breastfeeding.
Drops are not recommended during pregnancy. If used during lactation, breastfeeding should be stopped.
Injections during pregnancy are used only for health reasons (especially in the 1st trimester).
When planning pregnancy, Dexamethasone can be used in situations where the reason for the inability to get pregnant/bear a child is hyperandrogenism . During pregnancy, it is most often prescribed when there is a threat of miscarriage, when the immune system perceives the embryo as a foreign body (the drug helps suppress immune activity).
Reviews of Dexamethasone during pregnancy allow us to conclude that although the drug is in some cases the only chance to get pregnant and maintain a pregnancy, its use is almost always associated with certain inconveniences.
After all, Dexamethasone - what is it? A powerful hormonal drug. Therefore, almost all women who took it noted changes in body weight, hormonal disorders, and a tendency to depression.
Reviews about Dexamethasone
Reviews of Dexamethasone injections and reviews of Dexamethasone tablets allow us to draw the following conclusions: the drug is effective, has a wide range of indications (it is used as a remedy for allergies , for oncology , cerebral edema (including post-radiation), bacterial meningitis , for prevention and treatment vomiting and nausea during chemotherapy , to stimulate the synthesis of surfactant in the alveoli of the lungs in premature infants, when planning pregnancy, etc.), can only be used as prescribed by a doctor, in short courses and only after possible contraindications have been established.
Despite its effectiveness, the drug provokes pronounced adverse reactions, and this is its main disadvantage.
Reviews from doctors about eye drops and dosage forms for systemic use indicate that the danger of hormonal drugs is often exaggerated.
The main thing to consider when prescribing them is the presence/absence of direct contraindications. In addition, dose selection should be based on all available indicators: weight, age, test results for relevant hormones, etc.
The drug can be used in veterinary medicine. Why is Dexamethasone prescribed to animals? In principle, the medicine has the same indications as in humans. It is used for allergies, injuries, shock conditions.
Dexamethasone solution for injection 4 mg/ml 1 ml ampoule 10 pcs. in Moscow
Dexamethasone is a synthetic hormone of the adrenal cortex, a glucocorticosteroid (GCS), a methylated derivative of fluoroprednisolone. It has anti-inflammatory, antiallergic, desensitizing, antishock, antitoxic and immunosuppressive effects.
It interacts with specific cytoplasmic glucocorticosteroid receptors to form a complex that penetrates the cell nucleus and stimulates the synthesis of matrix ribonucleic acid, the latter inducing the formation of proteins, including lipocortin, that mediate cellular effects. Lipocortin inhibits phospholipase A2, suppresses the release of arachidonic acid and suppresses the synthesis of endoperoxides, prostaglandins, leukotrienes, which contribute to inflammation, allergies, etc.
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 (fat accumulation occurs mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.
Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract (GIT); increases the activity of glucose-6-phosphatase, which leads to an increase in the flow of glucose from the liver into the blood; increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases, which leads to the activation of gluconeogenesis.
Water-electrolyte metabolism: retains sodium (Na+) and water in the body, stimulates the excretion of potassium (K+) (mineralocorticoid activity), reduces the absorption of calcium (Ca2+) from the gastrointestinal tract, “washes out” Ca2+ from the bones, increases the excretion of Ca2+ by the kidneys.
The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils; inducing the formation of lipocortin and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes and organelle membranes (especially lysosomal ones).
The antiallergic effect develops as a result of suppression of the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, a decrease in the number of circulating basophils, suppression of the development of lymphoid and connective tissue, a decrease in the number of T- and B-lymphocytes, mast cells , reducing the sensitivity of effector cells to allergy mediators, suppressing antibody formation, changing the body’s immune response.
In chronic obstructive pulmonary disease, the effect is based mainly on inhibition of inflammatory processes, inhibition of development or prevention of swelling of the mucous membranes, inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium, deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucous membrane. Increases the sensitivity of beta-adrenergic receptors of small and medium-caliber bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by inhibiting or reducing its production.
Antishock and antitoxic effects are associated with an increase in blood pressure (BP) (due to an increase in the concentration of circulating catecholamines and restoration of the sensitivity of adrenergic receptors to them, as well as vasoconstriction), a decrease in the permeability of the vascular wall, membrane protective properties, and activation of liver enzymes involved in the metabolism of endo- and xenobiotics .
The immunosuppressive effect is due to inhibition of the release of cytokines (interleukin-1 and interleukin-2, interferon gamma) from lymphocytes and macrophages.
Therefore, it has a 30 times more pronounced effect than endogenous cortisol.
Dexamethasone has a 30 times more pronounced effect than endogenous cortisol. Therefore, it is a more potent inhibitor of the secretion of corticotropin-releasing hormone and ACTH. In pharmacological doses, it inhibits the hypothalamic-pituitary-adrenal system and promotes the development of secondary adrenal insufficiency. Suppresses the synthesis and release of adrenocorticotropic hormone (ACTH) by the pituitary gland and, secondarily, the synthesis of endogenous GCS. Inhibits the secretion of thyroid-stimulating hormone and follicle-stimulating hormone. Suppresses the release of beta-lipotropin, but does not reduce the content of circulating beta-endorphin.
Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
Increases the excitability of the central nervous system, reduces the number of lymphocytes and eosinophils, and increases the number of red blood cells (by stimulating the production of erythropoietin).
The peculiarity of the action is significant inhibition of pituitary function and the almost complete absence of mineralocorticoid activity.
Dexamethasone price, where to buy
In Russian pharmacies, the price for Dexamethasone eye drops starts from 80-150 rubles. The injections are sold for 120-170 rubles. for package No. 5, the price of tablets is from 40 rubles. Eye ointment with dexamethasone can be bought from 150 rubles.
In Ukraine, the price of Dexamethasone in 4 mg ampoules is from 15 UAH. Eye drops can be bought from 20 UAH. The price of Dexamethasone in tablets is from 30 UAH.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Dexamethasone tab.
0.5 mg 56pcs AO Update PFK 50 rub. order - Dexamethasone solution for injection. 4mg/ml amp 1ml 10 pcs. ELLARA LLC
120 rub. order
- Dexamethasone tablets 0.5 mg 10pcs JSC KRKA, d.d., Novo Mesto
40 rub. order
- Dexamethasone eye drops 0.1% 10mlS.C.Rompharm Company SrL
127 RUR order
- Dexamethasone eye drops 0.1% vial. 5ml RUP Belmedpreparaty
74 RUR order
Pharmacy Dialogue
- Dexamethasone 0.1% eye drops 10ml dropper bottleUpdate PFC JSC
119 RUR order
- Dexamethasone (0.5 mg tablet No. 10)KPKA
39 RUR order
- Dexamethasone tablets 0.5 mg No. 56Update PFC JSC
48 RUR order
- Dexamethasone (0.5 mg tablet No. 10) GNCLS/Zdorovye FC LLC
28 RUR order
- Dexamethasone (eye drops vial-drops 0.1% 10ml)Farmak
76 RUR order
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Pharmacy24
- Dexamethasone phosphate 0.4% 1 ml No. 10 solution PAT "Farmak", Ukraine
20 UAH. order - Dexamethasone 0.5 mg No. 10 tablets KPKA, d.d., Novo Mesto, Slovenia
35 UAH order
- Dexamethasone 4 mg/ml 1 ml N5 solution AT Lekhim-Kharkiv, Ukraine
10 UAH.order
- Dexamethasone Darnitsa 4 mg/ml 10 ampoules of 1 ml injection solution PrAT" Pharmaceutical company "Darnitsa", Ukraine
28 UAH order
- Dexamethasone-Biopharma 0.1% 10 ml eye drops TOV"FZ "Biopharma", Ukraine
19 UAH order
PaniPharmacy
- DEXAMETHASONE liquid Dexamethasone suspension. eye. 0.1% 5ml Poland, Warsaw Federal Law
58 UAH order
- Dexamethasone-Darnitsa solution d/in. 4 mg/ml amp. 1 ml No. 10
28 UAH order
- Dexamethasone ampoule Dexamethasone solution d/in. 0.4% amp. 1ml No. 5 Ukraine, Darnitsa ChAO
12 UAH order
- Dexamethasone liquid Dexamethasone h/c 0.1% 10ml Ukraine, Darnitsa ChAO
15 UAH order
- DEXAMETHASONE ampoule Dexamethasone solution d/in. 4mg amp. 1ml No. 25 Slovenia, KRKA dd Novo Mesto
337 UAH. order
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