Side effects from hormonal drugs dexamethasone. Dexamethasone for injection - instructions for use
Characteristics of the substance Dexamethasone
Hormonal agent (glucocorticoid for systemic and local use). Fluorinated homologue of hydrocortisone.
Dexamethasone is a white or almost white, odorless, crystalline powder. Solubility in water (25 °C): 10 mg/100 ml; soluble in acetone, ethanol, chloroform. Molecular weight 392.47.
Dexamethasone sodium phosphate is a white or slightly yellow crystalline powder. Easily soluble in water and very hygroscopic. Molecular weight 516.41.
Pharmacology
Pharmacological action- anti-inflammatory, antiallergic, immunosuppressive, antishock, glucocorticoid.Interacts with specific cytoplasmic receptors and forms a complex that penetrates the cell nucleus; causes expression or depression of mRNA, changing the formation of proteins on ribosomes, incl. lipocortin, mediating cellular effects. Lipocortin inhibits phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, PGs, leukotrienes, which contribute to inflammation, allergies, etc. It prevents the release of inflammatory mediators from eosinophils and mast cells. Inhibits the activity of hyaluronidase, collagenase and proteases, normalizes the functions of the intercellular matrix of cartilage and bone tissue. Reduces capillary permeability, stabilizes cell membranes, incl. lysosomal, inhibits the release of cytokines (interleukins 1 and 2, interferon gamma) from lymphocytes and macrophages. It affects all phases of inflammation, the antiproliferative effect is due to inhibition of the migration of monocytes into the inflammatory focus and the proliferation of fibroblasts. Causes involution of lymphoid tissue and lymphopenia, which causes immunosuppression. In addition to reducing the number of T-lymphocytes, their influence on B-lymphocytes is reduced and the production of immunoglobulins is inhibited. The effect on the complement system is to reduce the formation and increase the breakdown of its components. The antiallergic effect is a consequence of inhibition of the synthesis and secretion of allergy mediators and a decrease in the number of basophils. Restores the sensitivity of adrenergic receptors to catecholamines. Accelerates protein catabolism and reduces their content in plasma, reduces glucose utilization by peripheral tissues and increases gluconeogenesis in the liver. Stimulates the formation of enzyme proteins in the liver, surfactant, fibrinogen, erythropoietin, lipomodulin. Causes a redistribution of fat (increases lipolysis of adipose tissue of the extremities and fat deposition in the upper half of the body and on the face). Promotes the formation of higher fatty acids and triglycerides. Reduces absorption and increases excretion of calcium; retains sodium and water, ACTH secretion. Has an anti-shock effect.
After oral administration, it is quickly and completely absorbed from the gastrointestinal tract, Tmax - 1-2 hours. In the blood it binds (60-70%) to a specific carrier protein - transcortin. Easily passes through histohematic barriers, including the BBB and placental. Biotransforms in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites. T1/2 from plasma - 3-4.5 hours, T1/2 from tissues - 36-54 hours. Excreted by the kidneys and through the intestines, penetrates into breast milk.
After instillation into the conjunctival sac, it penetrates well into the epithelium of the cornea and conjunctiva, while therapeutic concentrations of the drug are created in the aqueous humor of the eye. When the mucous membrane is inflamed or damaged, the rate of penetration increases.
Use of the substance Dexamethasone
For systemic use (parenterally and orally)
Shock (burn, anaphylactic, post-traumatic, postoperative, toxic, cardiogenic, blood transfusion, etc.); cerebral edema (including due to tumors, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury); bronchial asthma, status asthmaticus; systemic connective tissue diseases (including systemic lupus erythematosus, rheumatoid arthritis, scleroderma, periarteritis nodosa, dermatomyositis); thyrotoxic crisis; hepatic coma; poisoning with cauterizing liquids (in order to reduce inflammation and prevent cicatricial contractions); acute and chronic inflammatory diseases of the joints, incl. gouty and psoriatic arthritis, osteoarthritis (including post-traumatic), polyarthritis, glenohumeral periarthritis, ankylosing spondylitis (ankylosing spondylitis), juvenile arthritis, Still's syndrome in adults, bursitis, nonspecific tenosynovitis, synovitis, epicondylitis; rheumatic fever, acute rheumatic carditis; acute and chronic allergic diseases: allergic reactions to drugs and foods, serum sickness, urticaria, allergic rhinitis, hay fever, angioedema, drug exanthema; skin diseases: pemphigus, psoriasis, dermatitis (contact dermatitis with damage to a large surface of the skin, atopic, exfoliative, bullous herpetiformis, seborrheic, etc.), eczema, toxicerma, toxic epidermal necrolysis (Lyell's syndrome), malignant exudative erythema (Stevens-Johnson syndrome ); allergic eye diseases: allergic corneal ulcers, allergic forms of conjunctivitis; inflammatory eye diseases: sympathetic ophthalmia, severe sluggish anterior and posterior uveitis, optic neuritis; primary or secondary adrenal insufficiency (including the condition after removal of the adrenal glands); congenital adrenal hyperplasia; kidney diseases of autoimmune origin (including acute glomerulonephritis), nephrotic syndrome; subacute thyroiditis; diseases of the hematopoietic organs: agranulocytosis, panmyelopathy, anemia (including autoimmune hemolytic, congenital hypoplastic, erythroblastopenia), idiopathic thrombocytopenic purpura, secondary thrombocytopenia in adults, lymphoma (Hodgkin, non-Hodgkin), leukemia, lymphocytic leukemia (acute, chronic); lung diseases: acute alveolitis, pulmonary fibrosis, stage II-III sarcoidosis; tuberculous meningitis, pulmonary tuberculosis, aspiration pneumonia (only in combination with specific therapy); berylliosis, Loeffler's syndrome (resistant to other therapy); lung cancer (in combination with cytostatics); multiple sclerosis; gastrointestinal diseases (to remove the patient from a critical condition): ulcerative colitis, Crohn's disease, local enteritis; hepatitis; prevention of transplant rejection; tumor hypercalcemia, nausea and vomiting during cytostatic therapy; multiple myeloma; carrying out a test for the differential diagnosis of hyperplasia (hyperfunction) and tumors of the adrenal cortex.
For topical use
Intra-articular, periarticular. Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, Reiter's disease, osteoarthritis (in the presence of severe signs of joint inflammation, synovitis).
Conjunctivally. Conjunctivitis (non-purulent and allergic), keratitis, keratoconjunctivitis (without damage to the epithelium), iritis, iridocyclitis, blepharitis, blepharoconjunctivitis, episcleritis, scleritis, uveitis of various origins, retinitis, optic neuritis, retrobulbar neuritis, superficial injuries of the cornea of various etiologies (after complete epithelialization cornea), inflammatory processes after eye injuries and eye surgeries, sympathetic ophthalmia.
Into the external auditory canal. Allergic and inflammatory diseases of the ear, incl. otitis.
Contraindications
Hypersensitivity (for short-term systemic use for health reasons is the only contraindication).
For intra-articular administration. Unstable joints, previous arthroplasty, pathological bleeding (endogenous or caused by the use of anticoagulants), transarticular bone fracture, infected lesions of joints, periarticular soft tissues and intervertebral spaces, severe periarticular osteoporosis.
Eye shapes. Viral, fungal and tuberculous eye infections, incl. keratitis caused Herpes simplex, viral conjunctivitis, acute purulent eye infection (in the absence of antibacterial therapy), violation of the integrity of the corneal epithelium, trachoma, glaucoma.
Ear shapes. Perforation of the eardrum.
Restrictions on use
For systemic use (parenterally and orally): Itsenko-Cushing's disease, stage III-IV obesity, convulsive conditions, hypoalbuminemia and conditions predisposing to its occurrence; open angle glaucoma.
For intra-articular administration: general serious condition of the patient, ineffectiveness or short duration of action of the two previous administrations (taking into account the individual properties of the glucocorticoids used).
Use during pregnancy and breastfeeding
The use of corticosteroids during pregnancy is possible if the expected effect of therapy outweighs the potential risk to the fetus (adequate and strictly controlled safety studies have not been conducted). Women of childbearing age should be warned of the potential risk to the fetus (corticosteroids cross the placenta). It is necessary to carefully monitor newborns whose mothers received corticosteroids during pregnancy (adrenal insufficiency may develop in the fetus and newborn).
Dexamethasone has been shown to be teratogenic in mice and rabbits after local ophthalmic applications of multiple therapeutic doses.
In mice, corticosteroids cause fetal resorption and a specific disorder - the development of cleft palate in the offspring. In rabbits, corticosteroids cause fetal resorption and multiple disorders, incl. developmental anomalies of the head, ear, limbs, palate, etc.
Breastfeeding women are advised to stop either breastfeeding or the use of drugs, especially in high doses (corticosteroids pass into breast milk and can suppress growth, the production of endogenous corticosteroids and cause undesirable effects in the newborn).
It should be borne in mind that when glucocorticoids are applied topically, systemic absorption occurs.
Side effects of the substance Dexamethasone
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 drug administration.
Systemic effects
From the nervous system and sensory organs: delirium (confusion, agitation, restlessness), disorientation, euphoria, hallucinations, manic/depressive episode, depression or paranoia, increased intracranial pressure with optic papilla congestion syndrome (pseudotumor cerebri - more common in children, usually after too rapid dose reduction, symptoms - headache, decreased visual acuity or double vision); sleep disturbance, dizziness, vertigo, headache; sudden loss of vision (with parenteral administration in the head, neck, turbinates, scalp), formation of posterior subcapsular cataracts, increased intraocular pressure with possible damage to the optic nerve, glaucoma, steroid exophthalmos, development of secondary fungal or viral eye infections.
From the cardiovascular system and blood (hematopoiesis, hemostasis): arterial hypertension, development of chronic heart failure (in predisposed patients), myocardial dystrophy, hypercoagulation, thrombosis, ECG changes characteristic of hypokalemia; with parenteral administration: flushes of blood to the face.
From the gastrointestinal tract: nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, pancreatitis, erosive esophagitis, hiccups, increased/decreased appetite.
From the side of metabolism: Na + and water retention (peripheral edema), hypokalemia, hypocalcemia, negative nitrogen balance due to protein catabolism, weight gain.
From the endocrine system: suppression of adrenal cortex function, decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, Itsenko-Cushing syndrome, hirsutism, irregular menstruation, growth retardation in children.
From the musculoskeletal system: muscle weakness, steroid myopathy, decreased muscle mass, osteoporosis (including spontaneous bone fractures, aseptic necrosis of the femoral head), tendon rupture; pain in muscles or joints, back; with intra-articular injection: increased pain in the joint.
From the skin: steroid acne, stretch marks, skin thinning, petechiae and ecchymosis, delayed wound healing, increased sweating.
Allergic reactions: skin rash, hives, facial swelling, stridor or difficulty breathing, anaphylactic shock.
Others: decreased immunity and activation of infectious diseases, withdrawal syndrome (anorexia, nausea, lethargy, abdominal pain, general weakness, etc.).
Local reactions after parenteral administration: burning, numbness, pain, paresthesia and infection at the injection site, scarring at the injection site; hyper- or hypopigmentation; atrophy of the skin and subcutaneous tissue (with intramuscular injection).
Eye shapes: with long-term use (more than 3 weeks), it is possible to increase intraocular pressure and/or develop glaucoma with damage to the optic nerve, decreased visual acuity and loss of visual fields, the formation of posterior subcapsular cataracts, thinning and perforation of the cornea; possible spread of herpes and bacterial infections; Patients with hypersensitivity to dexamethasone or benzalkonium chloride may develop conjunctivitis and blepharitis.
Dexamethasone is a synthetic glucocorticosteroid. It is available in several dosage forms: solution for intravenous and intramuscular administration, eye drops, tablets. Its glucocorticoid activity is 25 times greater than that of hydrocortisone, and 7 times greater than that of prednisolone. Inhibits the activity of white blood cells and resident mononuclear phagocytes. Prevents the migration of the former to the inflammatory focus. Stabilizes lysosome membranes, thereby reducing the level of proteases in the inflammatory focus. It neutralizes the effect of histamine on the walls of capillaries, thereby reducing their permeability. Inhibits the proliferative activity of fibroblasts and suppresses collagen synthesis. Reduces the intensity of formation of inflammatory mediators - prostaglandins and leukotrienes. Inhibits the release of cyclooxygenase-2. Promotes the migration of leukocytes from the blood to the lymph. When interacting directly with blood vessels, it exhibits a vasoconstrictor effect. Effect on protein metabolism: reduces the content of globulins in serum, stimulates the formation of albumin in the kidneys and liver, activates catabolic processes in skeletal muscles. Effect on fat metabolism: promotes the formation of fatty acids, redistributes adipose tissue from the extremities to the abdomen, face, shoulder girdle, increases the level of lipids in the blood. Effect on carbohydrate metabolism: promotes the absorption of carbohydrates from the gastrointestinal tract, increases blood glucose levels. In submaximal doses, it makes brain tissue more excitable and increases the risk of seizures. When used systemically, it exhibits anti-inflammatory, antiallergic effects, suppresses immunity and excessive cell proliferation. Local forms of the drug exhibit anti-inflammatory, anti-allergic effects, reduce the intensity of exudate flow into the site of inflammation (due to the vasoconstrictor effect).
Metabolized by microsomal liver enzymes. Half-life is 2-3 hours. Eliminated by the kidneys.
Bacterial, viral and fungal infections require constant medical monitoring of the patient taking Dexamethasone. Severe forms of infectious diseases allow the drug to be taken only in combination with specific therapy. Diseases and conditions in which the drug should also be taken with caution are: immunodeficiency diseases, BCG vaccination, diseases of the gastrointestinal tract (gastric and duodenal ulcers, inflammation of the esophageal mucosa, inflammation of the diverticulum, etc.), cardiovascular pathology, endocrine diseases. Before starting drug therapy with Dexamethasone, it is necessary to monitor blood counts, glucose and electrolytes in the blood. If you abruptly stop taking the drug (especially if it was taken in submaximal doses), rebound syndrome often develops, the manifestations of which are nausea, loss of appetite, musculoskeletal pain, and chronic fatigue. While taking the drug, it is necessary to monitor blood pressure, water-salt balance, and also be observed by an ophthalmologist.
When combined with certain medications, Dexamethasone can cause a number of unwanted side effects. Thus, taking it together with azathioprine or antipsychotic drugs can provoke cataracts, and with anticholinergics - glaucoma. In combination with oral contraceptives, testosterone preparations, female sex hormones, anabolic steroids, Dexamethasone can cause acne and increased male pattern hair growth. In combination with non-steroidal anti-inflammatory drugs, taking the drug increases the risk of erosive and ulcerative lesions of the gastrointestinal tract.
Pharmacology
GCS. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of inflammation. It disrupts the ability of macrophages to phagocytose, as well as to form interleukin-1. Helps stabilize lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of inflammation. Reduces capillary permeability due to the release of histamine. Suppresses fibroblast activity and collagen formation.
Inhibits the activity of phospholipase A 2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce the production of prostaglandins.
Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed into the lymphoid tissue; suppresses the formation of antibodies.
Dexamethasone suppresses the pituitary release of ACTH and β-lipotropin, but does not reduce the level of circulating β-endorphin. Inhibits the secretion of TSH and FSH.
When directly applied to blood vessels, it has a vasoconstrictor effect.
Dexamethasone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys, increases the activity of gluconeogenesis enzymes. In the liver, dexamethasone enhances the deposition of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from protein metabolism products. An increase in blood glucose levels activates the release of insulin.
Dexamethasone inhibits the uptake of glucose into fat cells, which leads to activation of lipolysis. However, due to increased insulin secretion, lipogenesis is stimulated, which leads to fat accumulation.
It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. Osteoporosis and Itsenko-Cushing syndrome are the main factors limiting long-term GCS therapy. As a result of the catabolic effect, growth suppression in children is possible.
In high doses, dexamethasone can increase the excitability of brain tissue and help lower the seizure threshold. Stimulates excess production of hydrochloric acid and pepsin in the stomach, which contributes to the development of peptic ulcers.
When used systemically, the therapeutic activity of dexamethasone is due to its anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.
When applied externally and locally, the therapeutic activity of dexamethasone is due to its anti-inflammatory, antiallergic and antiexudative (due to the vasoconstrictor effect) effect.
Its anti-inflammatory activity is 30 times higher than hydrocortisone, but does not have mineralocorticoid activity.
Pharmacokinetics
Plasma protein binding - 60-70%. Penetrates through histohematic barriers. A small amount is excreted in breast milk.
Metabolized in the liver.
T1/2 is 2-3 hours. Excreted by the kidneys.
When applied topically in ophthalmology, it is absorbed through the cornea with intact epithelium into the moisture of the anterior chamber of the eye. With inflammation of the eye tissue or damage to the mucous membrane and cornea, the rate of absorption of dexamethasone significantly increases.
Release form
1 ml - dark glass ampoules (5) - contour cell packaging (5) - cardboard packs.
250 ml - ampoules (50) - blister packaging (5) - cardboard boxes - transport boxes (in bulk)
Dosage
Individual. Orally for severe diseases at the beginning of treatment, up to 10-15 mg/day is prescribed; the maintenance dose can be 2-4.5 mg or more per day. The daily dose is divided into 2-3 doses. Take small doses 1 time/day in the morning.
For parenteral use, administered intravenously in a slow stream or drip (in acute and emergency conditions); i/m; Periarticular and intra-articular administration is also possible. During the day, you can administer from 4 to 20 mg of dexamethasone 3-4 times. The duration of parenteral use is usually 3-4 days, then they switch to maintenance therapy with an oral form. In the acute period for various diseases and at the beginning of treatment, dexamethasone is used in higher doses. When the effect is achieved, the dose is reduced at intervals of several days until the maintenance dose is reached or until treatment is stopped.
When used in ophthalmology for acute conditions, 1-2 drops are instilled into the conjunctival sac. every 1-2 hours, then, when inflammation decreases, every 4-6 hours. The duration of treatment is from 1-2 days to several weeks, depending on the clinical course of the disease.
Interaction
When used simultaneously with antipsychotics, bucarban, azathioprine, there is a risk of developing cataracts; with drugs that have an anticholinergic effect - the risk of developing glaucoma.
When used simultaneously with dexamethasone, the effectiveness of insulin and oral hypoglycemic drugs is reduced.
When used simultaneously with hormonal contraceptives, androgens, estrogens, and anabolic steroids, hirsutism and acne are possible.
When used simultaneously with diuretics, potassium excretion may be increased; with NSAIDs (including acetylsalicylic acid) - the incidence of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases.
When used simultaneously with oral anticoagulants, the anticoagulant effect may be weakened.
When used simultaneously with cardiac glycosides, the tolerability of cardiac glycosides may deteriorate due to potassium deficiency.
When used simultaneously with aminoglutethimide, the effects of dexamethasone may be reduced or inhibited; with carbamazepine - the effect of dexamethasone may be reduced; with ephedrine - increased excretion of dexamethasone from the body; with imatinib - a decrease in the concentration of imatinib in the blood plasma is possible due to the induction of its metabolism and increased excretion from the body.
When used simultaneously with itraconazole, the effects of dexamethasone are enhanced; with methotrexate - increased hepatotoxicity is possible; with praziquantel - a decrease in the concentration of praziquantel in the blood is possible.
When used simultaneously with rifampicin, phenytoin, and barbiturates, the effects of dexamethasone may be weakened due to increased excretion from the body.
Side effects
From the endocrine system: decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing syndrome (including moon face, pituitary type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis , striae), delayed sexual development in children.
Metabolism: increased excretion of calcium ions, hypocalcemia, increased body weight, negative nitrogen balance (increased protein breakdown), increased sweating, hypernatremia, hypokalemia.
From the central nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor of the cerebellum, headache, convulsions.
From the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of chronic heart failure, ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. 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; with intracranial administration - nosebleeds.
From the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups; rarely - increased activity of liver transaminases and alkaline phosphatase.
From the senses: 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.
From the musculoskeletal system: slower growth and ossification processes in children (premature closure of epiphyseal growth zones), 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).
Dermatological reactions: delayed wound healing, petechiae, ecchymosis, skin thinning, hyper- or hypopigmentation, steroid acne, stretch marks, tendency to develop pyoderma and candidiasis.
Allergic reactions: generalized (including skin rash, skin itching, anaphylactic shock) and when applied topically.
Effects associated with immunosuppressive effects: development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination).
Local reactions: with parenteral administration - tissue necrosis.
For external use: rarely - itching, hyperemia, burning, dryness, folliculitis, acne, hypopigmentation, perioral dermatitis, allergic dermatitis, skin maceration, secondary infection, skin atrophy, stretch marks, prickly heat. With long-term use or application to large areas of skin, systemic side effects characteristic of GCS may develop.
Indications
For oral administration: Addison-Biermer disease; acute and subacute thyroiditis, hypothyroidism, progressive ophthalmopathy associated with thyrotoxicosis; bronchial asthma; rheumatoid arthritis in the acute phase; UC; connective tissue diseases; autoimmune hemolytic anemia, thrombocytopenia, aplasia and hypoplasia of hematopoiesis, agranulocytosis, serum sickness; acute erythroderma, pemphigus (common), acute eczema (at the beginning of treatment); malignant tumors (as palliative therapy); congenital adrenogenital syndrome; cerebral edema (usually after preliminary parenteral use of GCS).
For parenteral administration: shock of various origins; cerebral edema (with a brain tumor, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury); status asthmaticus; severe allergic reactions (Quincke's edema, bronchospasm, dermatosis, acute anaphylactic reaction to drugs, serum transfusion, pyrogenic reactions); acute hemolytic anemia, thrombocytopenia, acute lymphoblastic leukemia, agranulocytosis; severe infectious diseases (in combination with antibiotics); acute adrenal insufficiency; acute croup; joint diseases (humeral periarthritis, epicondylitis, styloiditis, bursitis, tendovaginitis, compression neuropathy, osteochondrosis, arthritis of various etiologies, osteoarthritis).
For use in ophthalmological practice: non-purulent and allergic conjunctivitis, keratitis, keratoconjunctivitis without damage to the epithelium, iritis, iridocyclitis, blepharoconjunctivitis, blepharitis, episcleritis, scleritis, inflammatory process after eye injuries and surgical interventions, sympathetic ophthalmia.
Contraindications
For short-term use for health reasons - hypersensitivity to dexamethasone.
For intra-articular injection and injection directly into the lesion: previous arthroplasty, pathological bleeding (endogenous or caused by the use of anticoagulants), intra-articular bone fracture, infectious (septic) inflammatory process in the joint and periarticular infections (including a history), as well as general infectious disease, severe periarticular osteoporosis, absence of signs of inflammation in the joint ("dry" joint, for example, in osteoarthritis without synovitis), severe bone destruction and joint deformation (sharp narrowing of the joint space, ankylosis), joint instability as an outcome of arthritis, aseptic necrosis of the forming epiphyseal joint of bones.
For external use: bacterial, viral, fungal skin diseases, skin tuberculosis, skin manifestations of syphilis, skin tumors, post-vaccination period, violation of the integrity of the skin (ulcers, wounds), children's age (up to 2 years, with itching in the anus - up to 12 years), rosacea, acne vulgaris, perioral dermatitis.
For use in ophthalmology: bacterial, viral, fungal diseases of the eyes, tuberculosis of the eyes, disruption of the integrity of the ocular epithelium, acute form of purulent eye infection in the absence of specific therapy, diseases of the cornea combined with epithelial defects, trachoma, glaucoma.
Use with caution within 8 weeks before and 2 weeks after vaccination, with lymphadenitis after BCG vaccination, with immunodeficiency conditions (including AIDS or HIV infection).
Use with caution in diseases of the gastrointestinal tract: gastric and duodenal ulcers, esophagitis, gastritis, acute or latent peptic ulcers, recently created intestinal anastomosis, nonspecific ulcerative colitis with the threat of perforation or abscess formation, diverticulitis.
Should be used with caution for diseases of the cardiovascular system, incl. after a recent myocardial infarction (in patients with acute and subacute myocardial infarction, the necrosis focus may spread, slowing down the formation of scar tissue and, as a result, rupture of the heart muscle), with decompensated chronic heart failure, arterial hypertension, hyperlipidemia), with endocrine diseases - diabetes mellitus ( including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, with severe chronic renal and/or liver failure, nephrourolithiasis, with hypoalbuminemia and conditions predisposing to its occurrence, with systemic osteoporosis, myasthenia gravis, acute psychosis , obesity (III-IV degree), with poliomyelitis (with the exception of the form of bulbar encephalitis), open- and closed-angle glaucoma.
If intra-articular administration is necessary, it should be used with caution in patients with a general severe condition, ineffectiveness (or short duration) of the action of 2 previous injections (taking into account the individual properties of the GCS used).
Before and during GCS therapy, it is necessary to monitor a general blood count, glycemic levels and electrolyte levels in plasma.
For intercurrent infections, septic conditions and tuberculosis, simultaneous antibiotic therapy is necessary.
Relative adrenal insufficiency caused by dexamethasone may persist for several months after its discontinuation. Taking this into account, in stressful situations that arise during this period, hormonal therapy is resumed with the simultaneous administration of salts and/or mineralocorticoids.
When using dexamethasone in patients with corneal herpes, the possibility of corneal perforation should be kept in mind. During treatment, it is necessary to monitor intraocular pressure and the condition of the cornea.
With the sudden withdrawal of dexamethasone, especially in the case of previous use in high doses, a so-called withdrawal syndrome occurs (not caused by hypocortisolism), manifested by anorexia, nausea, lethargy, generalized musculoskeletal pain, and general weakness. After discontinuation of dexamethasone, relative adrenal insufficiency may persist for several months. If stressful situations arise during this period, GCS is prescribed (according to indications), if necessary in combination with mineralocorticoids.
During the treatment period, monitoring of blood pressure, water and electrolyte balance, peripheral blood picture and glycemic level is required, as well as observation by an ophthalmologist.
In children, during long-term treatment, careful monitoring of the dynamics of growth and development is necessary. Children who during the treatment period were in contact with patients with measles or chickenpox are prescribed specific immunoglobulins prophylactically.
In this article you can read the instructions for use of the drug Dexamethasone.
Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Dexamethasone in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Dexamethasone analogues in the presence of existing structural analogues. Use for the treatment of inflammatory and systemic diseases, including the eyes, in adults, children, as well as during pregnancy and lactation.
Dexamethasone is a synthetic glucocorticosteroid (GCS), a methylated derivative of fluoroprednisolone. It has anti-inflammatory, antiallergic, immunosuppressive effects, increases the sensitivity of beta-adrenergic receptors to endogenous catecholamines.
Interacts with specific cytoplasmic receptors (receptors for GCS are found in all tissues, especially in the liver) to form a complex that induces the formation of proteins (including enzymes that regulate vital processes in cells.)
Protein metabolism: reduces the amount of globulins in plasma, increases the synthesis of albumins in the liver and kidneys (with an increase in the albumin/globulin ratio), reduces synthesis and increases 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; increases the activity of glucose-6-phosphatase (increasing the flow of glucose from the liver into the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); promotes the development of hyperglycemia.
Water-electrolyte metabolism: retains Na+ and water in the body, stimulates the excretion of K+ (mineralocorticoid activity), reduces the absorption of Ca+ from the gastrointestinal tract, reduces bone mineralization.
The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils and mast cells; inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes (especially lysosomal) and organelle membranes. Acts on all stages of the inflammatory process: inhibits the synthesis of prostaglandins (Pg) at the level of arachidonic acid (lipocortin inhibits phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, which contribute to inflammation, allergies, etc.), the synthesis of “proinflammatory cytokines” ( interleukin 1, tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors.
The immunosuppressive effect is caused by the involution of lymphoid tissue, inhibition of the proliferation of lymphocytes (especially T-lymphocytes), suppression of the migration of B cells and the interaction of T and B lymphocytes, inhibition of the release of cytokines (interleukin-1, 2; interferon gamma) from lymphocytes and macrophages and decreased antibody formation.
The antiallergic effect develops as a result of a decrease in 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, T- and B-lymphocytes, mast cells; suppressing the development of lymphoid and connective tissue, reducing the sensitivity of effector cells to allergy mediators, inhibiting antibody formation, changing the body's immune response.
In obstructive diseases of the respiratory tract, the effect is due mainly to inhibition of inflammatory processes, prevention or reduction of the severity of swelling of the mucous membranes, reduction of eosinophilic infiltration of the submucosal layer of the bronchial epithelium and deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucosa. Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.
Suppresses the synthesis and secretion of ACTH and, secondarily, the synthesis of endogenous corticosteroids.
Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
The peculiarity of the action is significant inhibition of pituitary function and the almost complete absence of mineralocorticosteroid activity.
Doses of 1-1.5 mg per day inhibit the function of the adrenal cortex; biological half-life (duration of inhibition of the hypothalamus-pituitary-adrenal cortex system).
In terms of the strength of glucocorticoid activity, 0.5 mg of dexamethasone corresponds to approximately 3.5 mg of prednisone (or prednisolone), 15 mg of hydrocortisone or 17.5 mg of cortisone.
Easily passes through histohematic barriers (including blood-brain and placental barriers). Metabolized in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites. Excreted by the kidneys (a small part by the lactating glands).
Diseases requiring the administration of fast-acting corticosteroids, as well as cases when oral administration of the drug is impossible:
- endocrine diseases: acute adrenal insufficiency, primary or secondary adrenal insufficiency, congenital adrenal hyperplasia, subacute thyroiditis;
- shock (burn, traumatic, surgical, toxic) - if vasoconstrictors, plasma replacement drugs and other symptomatic therapy are ineffective;
- status asthmaticus; severe bronchospasm (exacerbation of bronchial asthma, chronic obstructive bronchitis);
- 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 corneas;
- local application (in the area of pathological formation): keloids, discoid lupus erythematosus, granuloma annulare.
Solution in ampoules for intravenous and intramuscular administration (injections for injections) 4 mg/ml.
Oftan eye drops 0.1%.
Ophthalmic suspension 0.1%.
Instructions for use 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 slowly in a stream or drip (for acute and emergency conditions); intramuscularly; local (into the pathological formation) administration is also possible. To prepare a solution for intravenous drip infusion (dropper), you should use an isotonic sodium chloride solution or a 5% dextrose solution.
In the acute period for various diseases and at the beginning of therapy, Dexamethasone is used in higher doses. During the day, you can administer from 4 to 20 mg of Dexamethasone 3-4 times.
Doses of the drug for children (intramuscular):
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..01165 mg/kg body weight or 0 ..335 mg/m2 body surface area daily. For other indications, the recommended dose is from 0.02776 to 0.16665 mg/kg body weight or 0.mg/m2 body surface area every hour.
When the effect is achieved, the dose is reduced to maintenance or until treatment is stopped. The duration of parenteral use is usually 3-4 days, then switch to maintenance therapy with dexamethasone tablets.
Long-term use of high doses of the drug requires a gradual dose reduction in order to prevent the development of acute adrenal insufficiency.
Conjunctivally, adults and children over 12 years of age in acute inflammatory conditions: 1-2 drops 4-5 times a day for 2 days, then 3-4 times a day for 4-6 days.
Chronic conditions: 1-2 drops 2 times a day for a maximum of 4 weeks (no more).
In post-operative and post-traumatic cases: starting from the 8th day after surgery for strabismus, retinal detachment, cataract extraction and from the moment of injury - 1-2 drops 2-4 times a day for 2-4 weeks; for antiglaucoma filtering surgery - on the day of surgery or the day after it.
Children from 6 to 12 years old with allergic inflammatory conditions: 1 drop 2-3 times a day for 7-10 days, if necessary, treatment is continued after monitoring the condition of the cornea on the 10th day.
Dexamethasone is usually well tolerated. It has low mineralocorticoid activity, i.e. its effect on water-electrolyte metabolism is small. As a rule, low and medium doses of Dexamethasone do not cause sodium and water retention in the body or increased potassium excretion. The following side effects are described:
- decreased glucose tolerance;
- steroid diabetes mellitus or manifestation of latent diabetes mellitus;
- suppression of adrenal function;
- Itsenko-Cushing syndrome (moon-shaped face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, stretch marks);
- delayed sexual development in children;
- nausea, vomiting;
- pancreatitis;
- steroid ulcer of the stomach and duodenum;
- erosive esophagitis;
- gastrointestinal bleeding and perforation of the wall of the gastrointestinal tract;
- increased or decreased appetite;
- indigestion;
- flatulence;
- arrhythmias;
- bradycardia (up to cardiac arrest);
- increased blood pressure;
- hypercoagulability;
- thrombosis;
- euphoria;
- hallucinations;
- manic-depressive psychosis;
- depression;
- paranoia;
- increased intracranial pressure;
- nervousness or anxiety;
- insomnia;
- dizziness;
- headache;
- convulsions;
- increased intraocular pressure with possible damage to the optic nerve;
- tendency to develop secondary bacterial, fungal or viral eye infections;
- trophic changes in the cornea;
- exophthalmos;
- 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);
- hypocalcemia;
- weight gain;
- negative nitrogen balance (increased protein breakdown);
- increased sweating;
- fluid and sodium retention (peripheral edema);
- slower growth and ossification processes in children (premature closure of epiphyseal growth zones);
- osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and femur);
- muscle tendon rupture;
- delayed wound healing;
- steroid acne;
- striae;
- tendency to develop pyoderma and candidiasis;
- skin rash;
- anaphylactic shock;
- local allergic reactions.
Local for parenteral administration: burning, numbness, pain, tingling at the injection site, 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).
For short-term use for health reasons, the only contraindication is hypersensitivity to dexamethasone or the components of the drug.
In children during the growth period, GCS should be used only for absolute indications and under the careful supervision of the attending physician.
The drug should be prescribed with caution for the following diseases and conditions:
Use during pregnancy and breastfeeding
During pregnancy (especially in the 1st trimester), the drug can be used only when the expected therapeutic effect outweighs the potential risk to the fetus. 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.
If it is necessary to carry out treatment with the drug during breastfeeding, breastfeeding should be stopped.
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, antacids can be prescribed, and 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 hypothyroidism and liver cirrhosis. 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 may spread, the formation of scar tissue may slow down, and the heart muscle may rupture.
In stressful situations during maintenance treatment (for example, surgery, trauma or infectious diseases), the dose of the drug should be adjusted due to an increased need for glucocorticosteroids. Patients 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.
With sudden withdrawal, especially in the case of previous use of high doses, the development of withdrawal syndrome (anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness) is possible, as well as an exacerbation of the disease for which Dexamethasone was prescribed.
During treatment with Dexamethasone, vaccination should not be carried out due to a decrease in its effectiveness (immune response).
When prescribing Dexamethasone for intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously treat with bactericidal antibiotics.
In children during long-term treatment with Dexamethasone, careful monitoring of the dynamics of growth and development is necessary. Children who during the treatment period were in contact with patients with measles or chickenpox are prescribed specific immunoglobulins prophylactically.
Due to the weak mineralocorticoid effect, Dexamethasone is used in combination with mineralocorticoids for replacement therapy for adrenal insufficiency.
In patients with diabetes mellitus, blood glucose levels should be monitored and therapy adjusted if necessary.
X-ray monitoring of the osteoarticular system (images of the spine, hand) is indicated.
In patients with latent infectious diseases of the kidneys and urinary tract, Dexamethasone can cause leukocyturia, which may have diagnostic value.
There may be pharmaceutical incompatibility of dexamethasone with other IV drugs - 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.
Simultaneous administration of dexamethasone with:
- inducers of hepatic microsomal enzymes (phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration;
- diuretics (especially thiazide and carbonic anhydrase inhibitors) and amphotericin B - can lead to increased excretion of K+ from the body and an increased risk of developing heart failure;
- with sodium-containing drugs - to the development of edema and increased blood pressure;
- cardiac glycosides - their tolerability worsens and the likelihood of developing ventricular extrasytolia increases (due to caused hypokalemia);
- indirect anticoagulants - weakens (less often enhances) their effect (dose adjustment required);
- anticoagulants and thrombolytics - the risk of bleeding from ulcers in the gastrointestinal tract increases;
- ethanol (alcohol) and nonsteroidal anti-inflammatory drugs - increases the risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding (in combination with NSAIDs in the treatment of arthritis, it is possible to reduce the dose of glucocorticosteroids due to the summation of the therapeutic effect);
- paracetamol - the risk of developing hepatotoxicity increases (induction of liver enzymes and the formation of a toxic metabolite of paracetamol);
- acetylsalicylic acid - accelerates its elimination and reduces its concentration in the blood (when dexamethasone is discontinued, the level of salicylates in the blood increases and the risk of side effects increases);
- insulin and oral hypoglycemic drugs, antihypertensive drugs - their effectiveness decreases;
- vitamin D - its effect on the absorption of Ca2+ in the intestine is reduced;
- growth hormone - reduces the effectiveness of the latter, and with praziquantel - its concentration;
- M-anticholinergics (including antihistamines and tricyclic antidepressants) and nitrates - helps increase intraocular pressure;
- isoniazid and mexiletine - increases their metabolism (especially in “slow” acetylators), which leads to a decrease in their plasma concentrations.
Carbonic anhydrase inhibitors and loop diuretics may increase the risk of osteoporosis.
Indomethacin, displacing dexamethasone from its connection with albumin, increases the risk of developing its side effects.
ACTH enhances the effect of dexamethasone.
Ergocalciferol and parathyroid hormone prevent the development of osteopathy caused by dexamethasone.
Cyclosporine and ketoconazole, by slowing down the metabolism of dexamethasone, can in some cases increase its toxicity.
The simultaneous administration of androgens and steroidal anabolic drugs with dexamethasone promotes the development of peripheral edema and hirsutism, and the appearance of acne.
Estrogens and oral contraceptives containing estrogen reduce the clearance of dexamethasone, which may be accompanied by an increase in the severity of its action.
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.
Antipsychotics (neuroleptics) and azathioprine increase the risk of developing cataracts when dexamethasone is prescribed.
When used simultaneously with antithyroid drugs, the clearance of dexamethasone decreases and with thyroid hormones increases.
Analogs of the drug Dexamethasone
Structural analogues of the active substance:
- Decadron;
- Dexaven;
- Dexazone;
- Dexamed;
- Dexamethasone Bufus;
- Dexamethasone Nycomed;
- Dexamethasone-Betalek;
- Dexamethasone Vial;
- Dexamethasone-LENS;
- Dexamethasone-Ferein;
- Dexamethasone sodium phosphate;
- Dexamethasone phosphate;
- Dexamethasonelong;
- Dexapos;
- Dexafar;
- Dexon;
- Maxidex;
- Oftan Dexamethasone;
- Fortecortin.
The benefits and harms of the popular drug Dexamethasone
Dexamethasone is often used to treat a huge number of diseases; its benefits and harms are known to all specialists, but an overdose can lead to unforeseen consequences.
Intoxication of the body occurs abruptly without additional problems. The human body is designed in such a way that a reaction to all possible stimuli can appear suddenly. For some, the real problem was poor nutrition, which resulted in severe intoxication, while others often encounter chemicals.
One of the most dangerous intoxications is drug poisoning. It seems that medications should relieve unpleasant symptoms, but in fact, excess dosage, individual intolerance or other reasons can cause acute poisoning and the development of a huge number of pathologies.
Application
This drug ensures good absorption in the body, making treatment as effective as possible. The maximum concentration of the drug is reached ninety minutes after taking the drug, and is excreted through the kidneys and intestines.
It is important to consider that this remedy is absorbed into all parts of the human body, so nursing mothers need to treat treatment with the utmost caution. The instructions for use must be followed without fail; this is the only way to eliminate all possible risks and ensure effective treatment.
For adults, the use of this drug is recommended only with the approval of a doctor. Under no circumstances should you begin treatment on your own. The benefits and harms of the drug can be strictly individual, and the medicine is used in the presence of the following diseases:
- Serious diseases associated with the field of gynecology, caused by disruption of the endocrine system.
- A state of shock that occurs for any of the possible reasons.
- Swelling of the brain resulting from injury, disease, or hemorrhage.
- Bronchial asthma of an acute or chronic nature.
- Severe allergic reactions.
- Anaphylactic shock resulting from an allergy.
- Diseases associated with adrenal insufficiency.
- Various diseases of the endocrine system.
- Infectious diseases, dermatoses of various types.
- Blood diseases, including leukemia.
In fact, the list of diseases for which this drug is used is much wider. Only the main and most popular ones are presented above, but experts often prescribe the remedy for the treatment of other diseases.
When using Dexamethasone, an overdose of which occurs at amounts above 20 mg per day, remember that exceeding the amount of the drug can result in serious dangerous consequences, and in some cases, death.
For children
Treatment of various diseases in a child with the help of this drug should occur under the strict supervision of parents and strictly as prescribed by a doctor. The fact is that the child’s body is susceptible to a lot of unpleasant diseases and is extremely susceptible to any unfamiliar substances, which is why symptoms of a Dexamethasone overdose occur quite often.
In this case, the baby’s growth criteria are monitored throughout the entire course of treatment, and if there is the slightest change in a negative direction, the medication must be stopped immediately.
Contraindications
Dexamethasone is a fairly strong drug, so you should never prescribe it yourself. It is worth paying close attention to the individual characteristics of the patient, his condition and the course of the disease. This drug should be excluded or replaced with an analogue by people with a history of the following diseases:
- allergic reactions to various irritants;
- fungal and viral infections;
- diseases of the cardiovascular system;
- stomach problems;
- diabetes mellitus
For many other diseases, this drug is prescribed only after a detailed examination and passing the necessary tests, and only a doctor can approve the therapy.
Overdose
Symptoms of overdose of this drug should be known to everyone who is prescribed treatment with this drug. This information is necessary at least in order to promptly detect excess of the permissible amount of medication and avoid unpleasant consequences for the body.
Signs of an overdose directly depend on the amount of the substance taken and the nature of the disease for which it is used, and can be as follows:
- Disorders of the central nervous system, including confusion, psychosis for no apparent reason, increased excitability, causeless anxiety and disorientation in space and time.
- Problems in the functioning of the cardiovascular system, including a sharp increase in blood pressure, tachycardia and even heart failure.
- Increased intracranial pressure and convulsions accompanying this symptom in the limbs or throughout the body.
- Allergic reactions manifested by skin rashes.
- Severe nausea, possible vomiting.
Exceeding the permissible amount of the drug once will not bring any serious consequences to the body. In this case, it is important to detect the problem in a timely manner and adjust the treatment. To do this, you need to not only stop taking the drug for a certain period of time, but also tell your doctor about your symptoms.
Video: Dexamethasone for joint pain.
First aid
If you or your loved ones experience symptoms of an overdose of this drug, first aid is a chance for a quick recovery and eliminating possible consequences. If the overdose is quite severe, be sure to call a team of specialists - they will provide all the necessary actions to help the victim.
Mandatory actions to help the victim are:
- Gastric lavage with plenty of warm water. You can add a weak solution of potassium permanganate to the liquid. Be sure to induce vomiting and remove the drug from the stomach.
- After the drug is removed, the victim must take sorbents. In this case, activated carbon comes to the rescue, which is in every first aid kit.
- The victim must be provided with complete rest, and only a doctor will prescribe additional therapy in case of overdose.
Each person must take care of their health independently, and only a responsible approach will not only get rid of an unpleasant disease, but also prevent consequences.
Active ingredient/beginning: dexamethasone
Vero-Dexamethasone; Daxin; Decadron; Decdan; Dexa-Allvoran; Dexabene; Dexaven; Dexazone; Dexacort; Dexamed; Dexamethasone; Dexamethasone Nycomed; Dexamethasone-Betalek; Dexamethasone-Vero; Dexamethasone-LENS; Dexamethasone-Ferein; Dexamethasone sodium phosphate; Dexamethasone phosphate; Dexamethasone phosphate disodium salt; Dexapos; Dexafar; Dexon; Dexon; Detazon; Detamethasone; Maxidex; Ozurdex; Oftan-Dexamethasone; Sondex; Fortecortin; Fortecortin Mono.
Dexamethasone is a synthetic fluorinated glucocorticoid drug - GCS. It has anti-inflammatory, antiexudative, antiproliferative, antiallergic, antishock, antitoxic, immunosuppressive effects. The range of indications is very wide and includes: endocrine diseases (Addison-Biermer disease, Sheehan syndrome, adrenogenital syndrome, adrenal insufficiency, thyroiditis), allergic diseases (bronchial asthma, allergic rhinitis, urticaria, atopic dermatitis, drug allergies), dermatological diseases (eczema, dermatitis, dermatoses, psoriasis), gastrointestinal diseases (ulcerative ileitis, colitis, active hepatitis), inflammatory and degenerative joint diseases (arthritis, periarthritis, osteoarthritis, ankylosing spondylitis), collagenosis and autoimmune diseases (lupus erythematosus, rheumatic carditis, myositis), blood diseases (autoimmune anemia, thrombocytopenia, agranulocytosis), malignant tumors (lymphoma, leukemia, lymphocytic leukemia), cerebral edema, shock of various origins, etc. Eye drops are used in ophthalmological practice for allergic conjunctivitis, keratitis, iritis, blepharitis, scleritis.
Solution for injection.
Eye drops (eye suspension).
Dexamethasone
Dexamethasone is a synthetic glucocorticoid drug - GCS, the molecule of which includes a fluorine atom.
When used systemically, the therapeutic activity of dexamethasone is due to anti-inflammatory and antiproliferative, antiallergic, antishock and antitoxic, immunosuppressive effects.
When applied externally and locally, the therapeutic activity of dexamethasone is due to its anti-inflammatory, antiallergic and antiexudative effects.
Its anti-inflammatory activity is 30 times higher than that of hydrocortisone, but does not have mineralocorticoid activity.
Effect of Dexamethasone on the immune system:
Effect of Dexamethasone on inflammation:
Effect of Dexamethasone on metabolism:
Dexamethasone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. The main effect of Dexamethasone on metabolism is associated with:
Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys, increases the activity of gluconeogenesis enzymes. In the liver, dexamethasone enhances the deposition of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from protein metabolism products. An increase in blood glucose levels activates the release of insulin. Dexamethasone inhibits the uptake of glucose into fat cells, which leads to activation of lipolysis. However, due to increased insulin secretion, lipogenesis is stimulated, which leads to fat accumulation.
It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. As a result of the catabolic effect, growth suppression in children is possible.
Dexamethasone inhibits the activity of vitamin D, which leads to decreased calcium absorption and increased excretion.
Suppresses the synthesis and secretion of ACTH and, secondarily, the synthesis of endogenous corticosteroids. A feature of the action of dexamethasone is significant inhibition of pituitary function.
Osteoporosis and Itsenko-Cushing syndrome are the main factors limiting long-term GCS therapy.
Effect of Dexamethasone on the endocrine system:
Dexamethasone suppresses the synthesis and secretion of ACTH and b-lipotropin by the pituitary gland, but does not reduce the level of circulating b-endorphin. Secondarily inhibits the synthesis of endogenous glucocorticoids.
Dexamethasone inhibits the secretion of TSH and FSH.
A peculiarity of the action of Dexamethasone is the absence of mineralocorticoid activity. Slightly retains sodium and water in the body.
Other effects of Dexamethasone:
When directly applied to blood vessels, it has a vasoconstrictor effect (anti-exudative effect).
In high doses, dexamethasone can increase the excitability of brain tissue and help lower the seizure threshold.
Stimulates excess production of hydrochloric acid and pepsin in the stomach, which contributes to the development of peptic ulcers.
Dexamethasone is a long-acting glucocorticoid. The bioavailability of Dexamethasone is more than 90%. Plasma half-life: about 3 - 4.5 hours. Half-life: 2-3 hours. Biological half-life: hours. Plasma protein binding: up to 80%. In the cerebrospinal fluid, the maximum concentrations of dexamethasone are detected 4 hours after intravenous administration (about% of the plasma concentration). The decrease in the concentration of dexamethasone in the cerebrospinal fluid occurs very slowly (about 2/3 of the maximum concentration can be detected even after 24 hours). Dexamethasone is metabolized in the liver much more slowly than cortisol, forming small amounts of 6-hydroxy- and 20-dihydroxymetasone. About 80% of the administered dose of Dexamethasone is excreted through the kidneys, mainly in the form of glucuronide, within 24 hours.
When applied topically in ophthalmology, Dexamethasone is absorbed through the cornea with intact epithelium into the aqueous humor of the anterior chamber of the eye. With inflammation of the eye tissue or damage to the mucous membrane and cornea, the rate of absorption of dexamethasone significantly increases.
For oral administration (tablets):
For parenteral administration (solution for injection):
Taking into account the indications and prescribed doses, they are recommended for the treatment of all those diseases that are amenable to systemic treatment with glucocorticoids (if necessary as an additional treatment to the main one), if local treatment or oral administration is impossible or ineffective:
For use in ophthalmic practice:
Directions for use and doses
Use strictly as prescribed by your doctor to avoid complications!
The dose of Dexamethasone is set individually, depending on the disease and condition of the patient.
Dexamethasone is administered intravenously in a slow stream or by drip and intramuscular injection. The dose of Dexamethasone is determined individually. During the day, you can administer from 4 to 20 mgraz. The maximum daily dose is 80 mg. In exceptional cases - higher. The duration of parenteral administration is usually 3-4 days, then they switch to maintenance therapy with the oral form of Dexamethasone. In the acute period for various diseases and at the beginning of treatment, Dexamethasone is used in higher doses. When the effect is achieved, the dose of Dexamethasone is reduced at intervals of several days until the maintenance dose is reached or until treatment is stopped.
For shock (adults) - IV, 20 mg once, then 3 mg/kg over 24 hours as a continuous infusion or IV once 2-6 mg/kg, or IV 40 mg every 2- 6 (4-6) hours.
For cerebral edema (adults) - 10 mg IV, then 4 mg every 6 hours IM until symptoms resolve; the dose is reduced after 2-4 days and gradually - over 5-7 days - treatment is stopped.
For adrenal insufficiency (children) - IM 0.0233 mg/kg (0.67 mg/m2) per day in 3 injections every third day, or daily 0.01165 mg/kg (0.233-0.335 mg/m2) m2) per day.
Orally (during or after meals) once, in the morning (small dose) or in 2-3 doses (large dose): otmg domg (for severe diseases at the beginning of treatment) per day, after achieving the effect, the dose of Dexamethasone is gradually reduced to maintenance - 0 .2 - 4.5 or more per day. Treatment is stopped gradually (at the end several injections of corticotropin are prescribed).
Children - 0.25-25 mg, or 0.0833-0.3333 mg/kg or 0.0025-0.0001 mg/m^2 per day in 3-4 doses, depending on age.
Intra-articular (into the lesion) or periarticular (into soft tissue):
Adults and adolescents - 0.2-6 mg (2-8 mg), repeated at intervals of 3 days to 3 weeks as needed
In acute conditions, 1-2 drops are instilled into the conjunctival sac every 1-2 hours, then, when inflammation decreases, every 4-6 hours. The duration of treatment is from 1-2 days to several weeks, depending on the clinical course of the disease.
The described side effects may increase.
Treatment: with the development of adverse events - symptomatic, Itsenko-Cushing syndrome - administration of aminoglutethimide.
For parenteral use and oral administration:
For use in ophthalmic practice (eye drops):
Use during pregnancy and lactation:
Dexamethasone can be used during pregnancy, especially in the first trimester, only for health reasons. With long-term therapy during pregnancy, the possibility of fetal growth disturbances 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. Breastfeeding during treatment with Dexamethasone is not allowed.
When administering high doses and/or long-term use of Dexamethasone, the possibility of the following side effects should be considered:
From the endocrine system: with short-term therapy - decreased glucose tolerance; with long-term therapy, the development of Itsenko-Cushing syndrome, hyperglycemia up to steroid diabetes, atrophy of the adrenal cortex, adrenal insufficiency, especially during stress (in case of injury, surgery, concomitant diseases); violation of the secretion of sex hormones (menstrual cycle disorders - dysmenorrhea, hirsutism, impotence); withdrawal syndrome (malaise, pain: headaches, stomach, joints and muscles).
Metabolism: hyperlipoproteinemia, sodium retention and development of edema, increased excretion of potassium and calcium; catabolic effect on protein metabolism (negative nitrogen balance), suppression of regenerative and repair processes; osteoporosis, myopathy (muscle weakness), growth retardation in children; in rare cases, aseptic necrosis of bones (head of the femur and humerus), pathological fractures, tendon ruptures;
From the cardiovascular system: with short-term therapy - bradycardia, arterial hypotension, collapse (especially with rapid administration of large doses), arrhythmias, cardiac arrest; with long-term therapy, myocardial dystrophy, congestive heart failure, and myocardial infarction are possible.
From the hematopoietic system: with long-term therapy, increased thrombus formation, thrombosis and thromboembolism are possible; the risk of developing vasculitis in rheumatism.
From the side of the central nervous system: with long-term therapy, mood disorders, increased appetite, psychosis, increased intracranial pressure, dizziness, headaches, and convulsions are possible.
From the digestive system: with short-term therapy, nausea, vomiting, and the development of a steroid gastric ulcer are possible; with long-term therapy, erosive and ulcerative lesions of the gastrointestinal tract are possible (exacerbation and development of gastric or duodenal ulcers, perforation in ulcerative colitis), gastrointestinal atony, pancreatitis (hemorrhagic pancreatitis), hepatomegaly.
Dermatological reactions: with long-term therapy, facial erythema, thinning and vulnerability of the skin, petechiae, ecchymosis, steroid acne, stretch marks, panniculitis, and delayed wound healing are possible.
Side effects associated with immunosuppressive effects: weakening of immune processes, increased risk of infection, rapid development, exacerbation of mycoses, development of viral or other infections (for example, tuberculosis); deterioration or exacerbation of old infectious processes (for example, tuberculosis).
Other: increased sweating; rarely - allergic reactions (rash, itching).
From the organ of vision: increased intraocular pressure, posterior subcapsular cataract, exophthalmos. With long-term use of dexamethasone in ophthalmic practice, an increase in intraocular pressure is possible; When the cornea becomes thinner, there is a risk of perforation.
Special instructions and precautions:
Dexamethasone is used with caution in the following diseases (while simultaneously treating the underlying disease):
During treatment (especially long-term treatment), observation by an ophthalmologist (periodic ophthalmological examination), monitoring of blood pressure and water-electrolyte balance, as well as peripheral blood patterns and glycemic levels (blood glucose levels) is necessary. Monitor the condition of the hypothalamic-pituitary-adrenal system.
In children during long-term treatment with Dexamethasone, careful monitoring of the dynamics of growth and development is necessary.
Before starting treatment with glucocorticoids, incl. With dexamethasone, it is necessary to conduct a thorough examination of the gastrointestinal tract to exclude gastric and duodenal ulcers.
In order to reduce side effects, you can prescribe anabolic steroids, antibiotics, antacids, and also increase the intake of potassium in the body (diet, potassium supplements). Food should be rich in potassium, proteins, vitamins and low in fat, carbohydrates and salt.
In children, to avoid overdose, the dose of Dexamethasone is calculated based on body surface area. During long-term treatment of children under 14 years of age, due to the risk of growth retardation, a break of 4 days must be taken every 3 days (intermittent therapy).
Children who during the treatment period were in contact with patients with measles or chickenpox are prescribed specific immunoglobulins prophylactically.
It is necessary to take into account the increased effect of Dexamethasone in hypothyroidism and liver cirrhosis.
Stop therapy only gradually. With the sudden withdrawal of dexamethasone, especially in the case of previous use in high doses, a so-called withdrawal syndrome occurs (not caused by hypocortisolism), manifested by anorexia, nausea, lethargy, generalized musculoskeletal pain, and general weakness.
After discontinuation of dexamethasone, especially in the case of long-term use, relative insufficiency of the adrenal cortex may persist for several months (up to a year). If stressful situations arise during this period, GCS is prescribed (according to indications), if necessary in combination with mineralocorticoids.
When using dexamethasone in patients with corneal herpes, the possibility of corneal perforation should be kept in mind. During treatment, it is necessary to monitor intraocular pressure and the condition of the cornea.
Interactions have been observed when using Dexamethasone in combination with the following drugs:
Store in a place protected from light at room temperature no higher than 25°C.
Keep out of the reach of children!
The expiration date is indicated on the packaging. Do not use after the expiration date!
Dispensing drugs from pharmacies - according to a doctor's prescription.
Dexamethasone is a systemic glucocorticosteroid. This is a synthetic hormonal drug that is similar to hormones produced by the adrenal cortex. It has strong anti-inflammatory, anti-shock and anti-allergic effects. It is used for many pathologies accompanied by serious disorders. When used correctly, Dexamethasone quickly relieves inflammation and allergic reactions, improving the patient's condition. But the problem is that for this you need to choose the exact dosage. If treatment is carried out without a doctor’s prescription or the patient violates medical recommendations, serious side effects may occur.
Features of application
Dexamethasone is very popular among other hormonal agents due to its low cost and high efficiency. Its action is based on the fact that the drug binds to glucocorticoid receptors of cells and penetrates them. It blocks the production of certain enzymes, interferes with metabolic processes, and inhibits the activity of the immune system. The result of this is a decrease in inflammation and pain, the disappearance of itching, swelling and redness of the skin, and easier breathing.
This drug is effective in many pathologies; its timely administration can save the patient’s life or significantly improve his condition. But it should be used only as prescribed by a doctor after examination. Sometimes careful monitoring of the patient during treatment is required. After all, some chronic pathologies may worsen due to the use of the drug or provoke the appearance of side effects.
Caution when treating with this drug and the use of the lowest possible doses is necessary for the following pathologies:
- osteoporosis;
- hypertension;
- heart failure;
- tuberculosis;
- diabetes mellitus;
- peptic ulcers;
- glaucoma;
- hypothyroidism;
- ulcerative colitis;
- epilepsy;
- psychosis.
Dexamethasone is also prescribed with caution to elderly patients and children. After myocardial infarction, they try not to prescribe the drug, as it slows down the formation of scar tissue and can accelerate the development of necrosis. And if long-term use is necessary, it is necessary to constantly monitor the level of potassium and glucose in the blood.
Contraindications
Sometimes Dexamethasone is prescribed in emergency cases, for example, in case of anaphylactic shock or Quincke's edema. In this case, the drug can save the patient’s life, so they usually do not pay attention to the presence of contraindications. This use of this medicine is short-term and therefore rarely causes negative reactions. But, if the situation is not critical, a full examination is necessary.
Attention: the doctor prescribes treatment only taking into account the presence of chronic diseases in the patient. This helps to avoid serious consequences.
There are the following contraindications to the use of Dexamethasone:
- myocardial infarction;
- internal bleeding;
- diabetes mellitus;
- pregnancy and breastfeeding;
- severe obesity;
- immunodeficiency;
- osteoporosis;
- mental illness;
- ulcers on the mucous membrane of the digestive tract;
- renal failure;
- infectious diseases.
It is not advisable to use Dexamethasone during pregnancy.
Vaccinations are contraindicated during treatment with Dexamethasone. In addition to the fact that they will be useless due to a decrease in the functions of the patient’s immune system, vaccination with a live vaccine can lead to the development of the disease. Therefore, the drug can be used no earlier than 2 weeks after vaccination, when antibodies have already formed. And after the course of treatment, at least 2 months must pass before starting Dexamethasone therapy.
Side effects
When choosing the correct dosage of the drug, it is well tolerated by all patients. Therefore, it is prescribed to everyone, regardless of age, even newborns. Dexamethasone causes side effects most often when used incorrectly. This happens when a patient uses a drug without a doctor’s prescription, does not take into account contraindications, or exceeds the recommended dosage. In this case, you should stop using the drug and consult a doctor.
Some people may have individual intolerance to the active ingredient of the drug. Moreover, after its administration or ingestion, an allergic reaction soon appears. It could be urticaria or even bronchospasm. Often the drug also affects the immune system. This usually manifests itself in increased susceptibility to infections. The patient is susceptible to bacterial, viral and fungal diseases. And infectious diseases such as measles or chicken pox occur in a very severe form.
If side effects occur, even if they are not severe, it is not advisable to use Dexamethasone. After all, it acts at the cellular level and accumulates in the body, affecting the functioning of various organs for several weeks. And the more the drug enters the cells, the more severe the negative reactions will be later. Therefore, even if you experience slight malaise, nausea or discomfort, you must inform your doctor. You may need to replace the drug with another one. But this also needs to be done correctly. Often the cause of side effects is sudden withdrawal of the drug.
Dexamethasone acts at the cellular level by binding to glucocorticoid receptors. And they are present in all organs and tissues of the body. Therefore, the side effects of Dexamethasone may vary. They can affect the functioning of the cardiovascular, endocrine and nervous systems; when taken orally, the digestive organs are most often affected; when administered by injection, local reactions may develop. This drug also has a strong effect on metabolic processes, often leading to the accumulation of fat deposits, increased sugar levels, and loss of calcium and potassium.
Attention: it is not advisable to use Dexamethasone after fractures and other injuries, although severe pain and shock are indications for its use. But this drug can slow down regeneration processes and impair the rate of wound healing.
When using Dexamethasone injections, negative local reactions often develop. This usually results in skin redness, swelling, burning or soreness at the injection site. Pigmentation disorders, subcutaneous tissue atrophy, and scar formation may also appear.
Endocrine system
The most dangerous consequence of using Dexamethasone is suppression of adrenal function. Moreover, this condition may not develop immediately, but a couple of months after treatment. The risk of this disorder is especially high with long-term use of the drug in high doses.
Dexamethasone also has a strong effect on carbohydrate metabolism. This is most evident in decreased glucose tolerance. Due to this condition, the development of steroid diabetes mellitus or an exacerbation of its latent form is possible, as hyperglycemia develops.
The drug affects fat metabolism. Dexmethasone binds to lipids and increases their absorption, which accelerates the accumulation of fatty deposits. Therefore, weight gain may be a consequence of treatment with this drug.
Obesity is often a consequence of Dexamethasone treatment.
One of the rare, but still possible side effects is Cushing's syndrome. It manifests itself with the following symptoms:
- increased blood pressure;
- moon-shaped face;
- muscle weakness;
- obesity;
- dysmenorrhea.
When using the drug in childhood, there is a high risk of delaying the child's growth and development. It especially strongly affects the growth of bone tissue, so the development of skeletal deformities is possible. The sexual development of children also slows down.
Cardiovascular system
Especially often, such side effects develop after using the drug in injections. If you do not follow the correct dosage and administration of the solution, they may appear immediately. This is an increase in blood pressure, a rush of blood to the face, and disruption of the heart muscle. This happens when large doses of the drug are administered quickly, and this can lead to cardiac arrest.
But even with proper use and compliance with the dosages recommended by the doctor, the development of disorders of the cardiovascular system is possible. Most often this is an increase in pressure and the development of arrhythmia. Bradycardia may develop, and the slowing of the heart rate can be so strong that it threatens to stop it. Thrombosis and increased blood clotting are also possible.
Patients predisposed to heart disease often develop heart failure. But this can happen even in healthy people. After all, Dexamethasone has a strong effect on electrolyte metabolism in the body, reducing the amount of potassium in the blood. And hypokalemia negatively affects the functioning of the heart.
Attention: it is especially dangerous to use this drug for treatment in patients who have had a myocardial infarction. Dexamethasone slows down the processes of tissue regeneration; on the contrary, its use may cause the area of necrosis to expand. This can damage the heart muscle.
Nervous system
After Dexamethasone injections and tablets, the patient’s nervous system and psyche also suffer greatly. Therefore, it is not recommended to use this steroid drug if you have any problems, as they may worsen. Typically, disruption of the nervous system appears almost immediately after the start of treatment. Most often it is mood instability and insomnia. But then, if the dosage is exceeded, the consequences can become more serious.
Most often, during treatment, patients experience headaches, dizziness, and insomnia. Convulsions are possible, which most often occur with an overdose, as well as increased intracranial pressure.
Sometimes mental disorders develop in patients after stopping treatment, especially if this happened abruptly. This may cause nervousness, hallucinations, disorientation, fear and anxiety. The serious consequences of Dexamethasone treatment also include paranoia, depression, manic-depressive neurosis, euphoria, mood swings and even thoughts of suicide.
Digestive system
The digestive organs most often suffer after using the drug in tablets. But injections can also damage the gastrointestinal tract, especially if there are any violations of its functions. Most often, nausea, vomiting, flatulence appear, appetite is disturbed, and digestion slows down.
But more serious consequences may develop:
- pancreatitis;
- peptic ulcer of the stomach and duodenum;
- esophagitis;
- erosive gastritis;
- perforation of the walls of the gastrointestinal tract;
- stomach bleeding;
- liver dysfunction.
Organs of vision
Dexamethasone is often used for various ophthalmological pathologies. For this purpose, a special form of the drug is usually used - eye drops. But it is also possible to use Dexamethasone in ampoules for intramuscular injection. This treatment is effective for various infectious, allergic and inflammatory eye diseases.
But the use of Dexamethasone can be harmful to the organ of vision. Incorrect dosage or long-term treatment sometimes leads to the development of cataracts, glaucoma, and retinopathy. This drug may cause increased intraocular pressure and the development of secondary infections.
Often Dexamethasone negatively affects the organ of vision
Musculoskeletal system
Despite the fact that the main indications for the use of Dexamethasone are various pathologies of the spine and joints, many of its side effects manifest themselves in this area. This drug affects metabolic processes and greatly reduces calcium absorption. This leads to decreased bone density. With long-term therapy with this drug, the risk of developing osteoporosis and resulting fractures increases. The tubular bones and vertebrae most often suffer from this.
Attention: when using Dexamethasone in large doses or with long-term treatment, aseptic bone necrosis may develop. This pathology most often affects the femur or humerus.
Frequent intra-articular injections of Dexamethasone can lead to the destruction of cartilage tissue. Therefore, it is better not to use this drug for the treatment of arthrosis. Tendons are also damaged and may even rupture. And the ligaments soften, stretch, and cease to perform their functions.
But the most common side effect of treatment with this drug is muscle weakening. The reason for this is a violation of metabolic processes in muscle tissue. This leads to a decrease in their tone and even atrophy. This condition is called steroid.
Withdrawal syndrome
If, after long-term treatment with the drug, you suddenly stop taking it, withdrawal syndrome develops. In the most serious cases, it manifests itself as a rapid drop in blood pressure, slow heart rate, and adrenal insufficiency. This condition can lead to death.
But this rarely happens. Most often, withdrawal syndrome manifests itself in the fact that the underlying disease that was treated with Dexamethasone “exacerbates.” For example, with rheumatoid arthritis, a relapse may occur: inflammation increases, joints become swollen and painful. Often, improper cessation of treatment is also manifested by disruption of the digestive system, loss of appetite, headaches, and weakness. Sometimes a febrile state develops, conjunctivitis, runny nose, arthralgia, and convulsions appear.
Therefore, the withdrawal of Dexamethasone should be gradual - over 1-2 weeks. The doctor will advise you on how to reduce the dosage so that it does not have negative consequences.
Overdose
Dexamethasone should only be used under the guidance of a doctor, as it is very important to choose the right dosage. It depends on the age of the patient, the severity of his condition and the type of pathology. This drug is usually used in the lowest possible doses. This avoids side effects.
But some patients use the drug on their own, without consulting a doctor. Others independently exceed the recommended dosage, believing that this will improve the effectiveness of treatment. But this approach leads to serious consequences.
An overdose of Dexamethasone is most often manifested by the appearance of edema and a strong increase in blood pressure. This happens because the drug causes fluid and sodium salts to be retained in the tissues. It is also possible to increase blood sugar levels, develop heart failure, and develop peptic ulcers.
Severely exceeding the dose of the drug threatens a sharp increase in blood pressure, the appearance of tachycardia, and nausea. The patient feels anxious and disoriented. He develops psychosis, confusion, and seizures. If you notice such symptoms, it is important to call an ambulance as soon as possible.
Drug interactions
Sometimes the side effects of Dexamethasone appear due to the fact that it is used as part of a complex treatment. But this drug is not compatible with all medications. This must be taken into account when prescribing treatment.
Most often, the occurrence of negative reactions is associated with the peculiarities of the drug’s action. Some diuretics remove potassium from the body. And when treated with Dexamethasone, its level decreases, so the risk of developing heart failure increases. It is also undesirable to use sodium-containing drugs together with it, as this will lead to edema and increased blood pressure.
When used together with cardiac glycosides, the risk of developing extrasystole increases. And anticoagulants and thrombolytics together with Dexamethasone can lead to internal bleeding. Non-steroidal anti-inflammatory drugs become more toxic and more damaging to the gastrointestinal mucosa.
You cannot use other hormonal drugs together with Dexamethasone, as this will increase the risk of side effects. It is also undesirable to combine it with Indomethacin, Cyclosporine, Ketoconazole, Paracetamol, Azathioprine and some other drugs.
Conclusions
Despite the effectiveness of Dexamethasone in many pathologies, it should be used only in the most extreme cases. After all, a large number of side effects can negate the positive effect of treatment or even worsen the patient’s condition. In addition, it is very important to use this remedy in the lowest possible doses, this will help reduce the risk of developing negative reactions.
Video on the topic
Name:
Dexamethasonum
Pharmacological
action:
Glucocorticosteroid hormone(a hormone of the adrenal cortex that affects carbohydrate and protein metabolism), which has strong anti-allergic and anti-inflammatory properties (35 times more active than cortisone).
Synthetic glucocorticoid (GCS), a methylated derivative of fluoroprednisolone. It has anti-inflammatory, antiallergic, immunosuppressive effects, increases the sensitivity of beta-adrenergic receptors to endogenous catecholamines.
Interacts with specific cytoplasmic receptors (receptors for GCS are found in all tissues, especially in the liver) to form a complex that induces the formation of proteins (including enzymes that regulate vital processes in cells.)
Protein metabolism: reduces the amount of globulins in plasma, increases albumin synthesis in the liver and kidneys (with an increase in the albumin/globulin ratio), reduces synthesis and 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; increases the activity of glucose-6-phosphatase (increasing the flow of glucose from the liver into the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); promotes the development of hyperglycemia.
Water-electrolyte metabolism: retains Na+ and water in the body, stimulates the excretion of K+ (mineralocorticoid activity), reduces the absorption of Ca+ from the gastrointestinal tract, reduces bone mineralization.
Anti-inflammatory effect associated with inhibition of the release of inflammatory mediators by eosinophils and mast cells; inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes (especially lysosomal) and organelle membranes. Acts on all stages of the inflammatory process: inhibits the synthesis of prostaglandins (Pg) at the level of arachidonic acid (lipocortin inhibits phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, which contribute to inflammation, allergies, etc.), the synthesis of “proinflammatory cytokines” ( interleukin 1, tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors.
Immunosuppressive effect caused by involution of lymphoid tissue, inhibition of the proliferation of lymphocytes (especially T-lymphocytes), suppression of the migration of B-cells and the interaction of T- and B-lymphocytes, inhibition of the release of cytokines (interleukin-1, 2; interferon gamma) from lymphocytes and macrophages and a decrease antibody formation.
Antiallergic effect develops as a result of a decrease in 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, T- and B-lymphocytes, mast cells; suppressing the development of lymphoid and connective tissue, reducing the sensitivity of effector cells to allergy mediators, inhibiting antibody formation, changing the body's immune response.
For obstructive respiratory diseases the effect is due mainly to inhibition of inflammatory processes, prevention or reduction of the severity of edema of the mucous membranes, reduction of eosinophilic infiltration of the submucosal layer of the bronchial epithelium and deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucosa. Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.
Indications for
application:
Circulatory collapse(sharp drop in blood pressure): shock during or after surgery, trauma, blood loss, myocardial infarction, burns.
Severe infections: toxemia (the presence of toxins in the blood - substances that can lead to illness or death of the body), vascular collapse (a sharp drop in blood pressure) with meningococcal infection (meningitis - purulent inflammation of the membranes of the brain), septicemia (a form of blood poisoning by microorganisms), diphtheria, abdominal typhus, pneumonia (pneumonia), influenza, peritonitis (inflammation of the peritoneum), eclampsia (toxicosis of the second half of pregnancy).
Emergency allergic conditions: status asthmaticus (a prolonged attack of bronchial asthma that cannot be treated with medications usually used by the patient), laryngeal edema, dermatosis (skin disease), acute anaphylactic reaction (immediate allergic reaction) to medications (including antibiotics), serum transfusion , pyrogenic reactions (increase in body temperature).
For oral administration: Addison-Biermer disease; acute and subacute thyroiditis, hypothyroidism, progressive ophthalmopathy associated with thyrotoxicosis; bronchial asthma; rheumatoid arthritis in the acute phase; UC; connective tissue diseases; autoimmune hemolytic anemia, thrombocytopenia, aplasia and hypoplasia of hematopoiesis, agranulocytosis, serum sickness; acute erythroderma, pemphigus (common), acute eczema (at the beginning of treatment); malignant tumors (as palliative therapy); congenital adrenogenital syndrome; cerebral edema (usually after preliminary parenteral use of GCS).
For parenteral administration: shock of various origins; cerebral edema (with a brain tumor, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury); status asthmaticus; severe allergic reactions (Quincke's edema, bronchospasm, dermatosis, acute anaphylactic reaction to drugs, serum transfusion, pyrogenic reactions); acute hemolytic anemia, thrombocytopenia, acute lymphoblastic leukemia, agranulocytosis; severe infectious diseases (in combination with antibiotics); acute adrenal insufficiency; acute croup; joint diseases (humeral periarthritis, epicondylitis, styloiditis, bursitis, tendovaginitis, compression neuropathy, osteochondrosis, arthritis of various etiologies, osteoarthritis).
For use in ophthalmic practice: non-purulent and allergic conjunctivitis, keratitis, keratoconjunctivitis without damage to the epithelium, iritis, iridocyclitis, blepharoconjunctivitis, blepharitis, episcleritis, scleritis, inflammatory process after eye injuries and surgical interventions, sympathetic ophthalmia.
Directions for use:
In the acute period of the disease and at the beginning of treatment, the drug is used in higher doses. When the effect is achieved, the dosage is reduced at intervals of several days until a maintenance dose is reached or until treatment is stopped. The dosage regimen is individual.
In severe cases and at the beginning of treatment, up to 10-15 mg of the drug per day is used, the maintenance dose can be 2-4.5 mg or more per day.
For status asthmaticus and acute allergic diseases, 2-3 mg of dexamethasone per day can be used for a short time.
In the treatment of adrenogenital syndrome(dysfunction of the adrenal cortex, accompanied by increased secretion of male sex hormones), the dose is selected depending on the excretion of 17-ketosteroids in the urine.
Usually the effect is achieved when prescribing 1-1.5 mg. The average daily dose of 2-3 mg is divided into 2-3 doses. When treated with small doses, the drug is prescribed once in the morning.
Side effects:
From the endocrine system: decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing syndrome (including moon face, pituitary type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis, stretch marks), delayed sexual development in children.
Metabolism: increased excretion of calcium ions, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating, hypernatremia, hypokalemia.
From the side of the central nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor of the cerebellum, headache, convulsions.
From the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of chronic heart failure, ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. 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; with intracranial administration - nosebleeds.
From the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups; rarely - increased activity of liver transaminases and alkaline phosphatase.
From the senses: 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.
From the musculoskeletal system: slower 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).
Dermatological reactions: delayed wound healing, petechiae, ecchymoses, skin thinning, hyper- or hypopigmentation, steroid acne, stretch marks, tendency to develop pyoderma and candidiasis.
Allergic reactions: generalized (including skin rash, skin itching, anaphylactic shock) and when applied topically.
Effects associated with immunosuppressive effects: development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination).
Local reactions: with parenteral administration - tissue necrosis.
For external use: rarely - itching, hyperemia, burning, dryness, folliculitis, acne, hypopigmentation, perioral dermatitis, allergic dermatitis, skin maceration, secondary infection, skin atrophy, stretch marks, prickly heat. With long-term use or application to large areas of skin, systemic side effects characteristic of GCS may develop.
Contraindications:
Interaction with
other medicinal
by other means:
When used simultaneously with antipsychotics, bucarban, azathioprine there is a risk of developing cataracts; with drugs that have an anticholinergic effect - the risk of developing glaucoma.
When used simultaneously with dexamethasone the effectiveness of insulin and oral hypoglycemic drugs decreases.
When used simultaneously with hormonal contraceptives, androgens, estrogens, anabolic steroids may cause hirsutism and acne.
When used simultaneously with diuretics Potassium excretion may be increased; with NSAIDs (including acetylsalicylic acid) - the incidence of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases.
When used simultaneously with oral anticoagulants the anticoagulant effect may be weakened.
When used simultaneously with cardiac glycosides There may be a deterioration in the tolerance of cardiac glycosides due to potassium deficiency.
When used simultaneously with aminoglutethimide it is possible to reduce or inhibit the effects of dexamethasone; with carbamazepine - the effect of dexamethasone may be reduced; with ephedrine - increased excretion of dexamethasone from the body; with imatinib - a decrease in the concentration of imatinib in the blood plasma is possible due to the induction of its metabolism and increased excretion from the body.
When used simultaneously with itraconazole the effects of dexamethasone are enhanced; with methotrexate - increased hepatotoxicity is possible; with praziquantel - a decrease in the concentration of praziquantel in the blood is possible.
When used simultaneously with rifampicin, phenytoin, barbiturates, the effects of dexamethasone may be weakened due to increased excretion from the body.
Storage conditions:
List B. In a place protected from light.
Compound: 1 tablet contains -
active substance: dexamethasone - 0.0005 g (0.5 mg);
excipients: sugar, potato starch, stearic acid.
Description: white tablets, flat-cylindrical, with a chamfer.
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