Dexamethasone - instructions for use, reviews, analogs and formulations (tablets 0.5 mg, injections in ampoules (solution for injections), drops ophthalmic ophthalmic) drugs for the treatment of inflammation in adults, children and pregnancy
In this article, you can read the instructions for using the drug Dexamethasone. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Dexamethasone in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Dexamethasone 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 - synthetic glucocorticosteroid (GCS), methylated derivative of fluoride prednisolone. Has anti-inflammatory, antiallergic, immunosuppressive action, increases the sensitivity of beta-adrenoreceptors to endogenous catecholamines.
Interacts with specific cytoplasmic receptors (receptors for GCS are present in all tissues, especially in the liver), with the formation of a complex inducing the formation of proteins (including enzymes that regulate vital processes in cells.)
Protein metabolism: reduces the number of globulins in the plasma, increases the synthesis of albumins in the liver and kidneys (with increasing albumin / globulin ratio), reduces synthesis and enhances protein catabolism in muscle tissue.
Lipid metabolism: increases synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat occurs mainly in the area of 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 (increased intakeglucose from the liver to the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); promotes the development of hyperglycemia.
Water-electrolyte metabolism: retards Na + and water in the body, stimulates the excretion of K + (mineralocorticoid activity), reduces the absorption of Ca + from the gastrointestinal tract, reduces the mineralization of bone tissue.
The anti-inflammatory effect is associated with the suppression of the release of eosinophils and mast cells by inflammatory mediators; inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in the permeability of capillaries; stabilization of cell membranes (especially lysosomal) and membranes of organelles. It acts on all stages of the inflammatory process: it inhibits the synthesis of prostaglandins (Pg) at the level of arachidonic acid (lipocortin depresses phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, promoting inflammation, allergies, etc.), the synthesis of "pro-inflammatory cytokines" ( interleukin 1, tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors.
Immunosuppressive effect is caused by induced lymphoid tissue involution, suppression of lymphocyte proliferation (especially T-lymphocytes), suppression of B-cell migration and interaction of T and B lymphocytes, inhibition of release of cytokines (interleukin-1, 2, gamma-interferon) from lymphocytes and macrophages and a decrease in the formation of antibodies.
The antiallergic effect develops as a result of a decrease in the synthesis and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils of histamine and other biologically active substances, a decrease in the number of circulating basophils, T- and B-lymphocytes, mast cells; suppression of the development of lymphoid and connective tissue, reducing the sensitivity of effector cells to mediators of allergy, inhibition of antibody formation, changes in the immune response of the body.
In obstructive airway diseases, the effect is mainly due to inhibition of inflammatory processes, prevention or reduction of mucosal edema, a decrease in the eosinophilic infiltration of the submucosal layer of the bronchial epithelium and the 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 bronchial tubes to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.
Suppresses the synthesis and secretion of ACTH and, again, the synthesis of endogenous GCS.
It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
The peculiarity of the action is a significant inhibition of the pituitary function and a virtually complete absence of mineralocorticosteroid activity.
Doses of 1-1.5 mg per day depress the function of the adrenal cortex; the biological half-life is 32-72 hours (the duration of oppression of the hypothalamic-pituitary-cortical adrenal gland system).
The strength of the glucocorticoid activity of 0.5 mg of dexamethasone corresponds to approximately 3.5 mg of prednisone (or prednisolone), 15 mg of Hydrocortisone or 17.5 mg of cortisone.
Pharmacokinetics
Easily passes through the histohematological barriers (including through blood-brain and placental). Metabolised in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites. It is excreted by the kidneys (a small part by the lactating glands).
Indications
Diseases requiring the introduction of high-speed GCS, as well as cases where oral administration of the drug is not possible:
- endocrine diseases: acute insufficiency of the adrenal cortex, primary or secondary insufficiency of the adrenal cortex, congenital hyperplasia of the adrenal cortex, subacute thyroiditis;
- shock (burn, traumatic, operating, toxic) - with ineffectiveness of vasoconstrictors, plasma-substituting drugs and other symptomatic therapy;
- cerebral edema (with a brain tumor, craniocerebral trauma, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury);
- asthmatic status; 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 with malignant tumors, with the impossibility of oral treatment;
- blood diseases: acute hemolytic anemia, agranulocytosis, idiopathic thrombocytopenic purpura in adults;
- severe infectious diseases (in combination with antibiotics);
- in ophthalmic practice (subconjunctival, retrobulbar or parabulbar injection): allergic conjunctivitis, keratitis, keratoconjunctivitis without epithelial damage, iritis, iridocyclitis, blepharitis, blepharoconjunctivitis, scleritis, episcleritis, inflammation after eye injuries and surgical interventions, sympathetic ophthalmia, immunosuppressive treatment after transplantation cornea;
- local application (in the area of pathological education): keloids, discoid lupus erythematosus, annular granuloma.
Forms of release
Tablets 0.5 mg.
Solution in ampoules for intravenous and intramuscular injection (injections for injections) 4 mg / ml.
Ophthalmic 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 reaction to therapy. The drug is administered intravenously slowly by jet or drip (in acute and urgent conditions); intramuscularly; possibly also local (in pathological education) introduction.To prepare a solution for intravenous drip infusion (dropper), an isotonic solution of sodium chloride or a 5% solution of Dextrose should be used.
In an acute period with various diseases and at the beginning of therapy, Dexamethasone is used in higher doses. During the day, you can inject 4 to 20 mg of Dexamethasone 3-4 times.
Doses of the drug for children (intramuscularly):
The dose of the drug for substitution therapy (with adrenal cortex insufficiency) is 0.0233 mg / kg body weight or 0.67 mg / m2 body surface area, divided into 3 doses, every 3rd day or 0.00776 - 0.01165 mg / kg body weight or 0.233 - 0.335 mg / m2 body surface area daily. For other indications, the recommended dose is from 0.02776 to 0.16665 mg / kg body weight or 0.833 to 5 mg / m2 body surface area every 12-24 hours.
When the effect is achieved, the dose is reduced to a maintenance dose or until the treatment is discontinued. The duration of parenteral use is usually 3-4 days, then switch to maintenance therapy with dexamethasone in tablets.
Long-term use of high doses of the drug requires a gradual dose reduction in order to prevent the development of acute adrenocortical insufficiency.
Drops
Conjunctival, adults and children over 12 years with 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 postoperative and post-traumatic cases: starting from the 8th day after surgery for strabismus, retinal detachment, cataract extraction and from the time of injury, 1-2 drops 2-4 times a day for 2-4 weeks; with antiglaucoma filtering operation - on the day of surgery or the day after it.
Children from 6 to 12 years with allergic inflammatory conditions: 1 drop 2-3 times a day for 7-10 days, if necessary, treatment is continued after 10 days of monitoring the condition of the cornea.
Side effect
Usually Dexamethasone is well tolerated. It has a low mineralocorticoid activity, i.e. its effect on water-electrolyte exchange is small. As a rule, low and medium doses of Dexamethasone do not cause delays in sodium and water in the body, increased excretion of potassium. The following side effects are described:
- decreased glucose tolerance;
- Steroid diabetes mellitus or manifestation of latent diabetes mellitus;
- oppression of adrenal function;
- Isenko-Cushing syndrome (moonlike face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae);
- delay in 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;
- hypercoagulation;
- thromboses;
- euphoria;
- hallucinations;
- affective insanity;
- depression;
- paranoia;
- increased intracranial pressure;
- nervousness or anxiety;
- insomnia;
- dizziness;
- headache;
- convulsions;
- increased intraocular pressure with possible damage to the optic nerve;
- propensity to develop secondary bacterial, fungal or viral infections of the eyes;
- trophic changes of the cornea;
- exophthalmos;
- sudden loss of vision (with parenteral administration in the area of the head, neck, nasal concha, scalp may deposition of drug crystals in the vessels of the eye);
- hypocalcemia;
- weight gain;
- negative nitrogen balance (increased protein breakdown);
- increased sweating;
- fluid retention and sodium (peripheral edema);
- slowing growth and ossification processes in children (premature closure of epiphyseal growth zones);
- osteoporosis (very rare - pathological bone fractures, aseptic necrosis of the head of the humerus and femur);
- rupture of muscle tendons;
- delayed healing of wounds;
- steroid acne;
- stria;
- propensity to develop pyoderma and candidiasis;
- skin rash;
- itching;
- anaphylactic shock;
- local allergic reactions.
Local with parenteral administration: burning, numbness, pain, tingling at the injection site, infection at the injection site, rarely - necrosis of surrounding tissues, scar formation at the injection site; atrophy of the skin and subcutaneous tissue with the / m introduction (especially dangerous is the introduction to the deltoid muscle).
Contraindications
For short-term use according to vital indications, the only contraindication is hypersensitivity to dexamethasone or the components of the drug.
In children during the growth period, SCS should be used only in absolute indications and under the strictest supervision of the attending physician.
With caution, the drug should be administered in the following conditions and conditions:
- gastrointestinal diseases - peptic ulcer of stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with perforation or abscessing threat, diverticulitis;
- parasitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently transferred, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles; amebiasis, strongyloidiasis; systemic mycosis; active and latent tuberculosis. The use in severe infectious diseases is permissible only against the background of specific therapy.
- pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination;
- immunodeficiency states (including AIDS or HIV infection);
- diseases of the cardiovascular system (incl.recently suffered myocardial infarction - in patients with acute and subacute myocardial infarction, a foci of necrosis may develop, a delay in the formation of scar tissue and, as a consequence, a rupture of the heart muscle), severe chronic heart failure, hypertension, hyperlipidemia);
- endocrine diseases - diabetes mellitus (including a violation of carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease, obesity (3-4 items)
- severe chronic renal and / or hepatic insufficiency, nephrourolythiasis;
- hypoalbuminemia and conditions predisposing to its occurrence;
- systemic osteoporosis, myasthenia gravis, acute psychosis, poliomyelitis (except for the form of bulbar encephalitis), open and closed angle glaucoma;
- pregnancy.
Application in pregnancy and lactation
In pregnancy (especially in 1 trimester), the drug can be used only when the expected therapeutic effect exceeds the potential risk to the fetus. With prolonged therapy during pregnancy, the possibility of impaired fetal growth is not ruled out. In case of application at the end of pregnancy there is a risk of atrophy of the adrenal cortex in the fetus,which may require replacement therapy in a newborn.
If it is necessary to carry out treatment with the drug during breastfeeding, then breastfeeding should be discontinued.
special instructions
During treatment with dexamethasone (especially long-term) it is necessary to observe the oculist, monitor blood pressure and the state of water-electrolyte balance, as well as patterns of peripheral blood and blood glucose levels.
To reduce side effects, antacids can be prescribed, and K + intake should be increased (diet, potassium preparations). Food should be rich in proteins, vitamins, with a restriction of fat, carbohydrates and table salt.
The effect of the drug is enhanced in patients with hypothyroidism and liver cirrhosis. The drug may enhance existing emotional instability or psychotic disorders. When referring to psychoses in an anamnesis, Dexamethasone is given in high doses under strict doctor's supervision.
With caution should be used in acute and subacute myocardial infarction - possibly spreading the focus of necrosis, slowing the formation of scar tissue and rupture of the heart muscle.
In stressful situations during maintenance treatment (for example, surgical operations, trauma or infectious diseases), a correction of the dose of the drug should be made in connection with an increase in the need for glucocorticosteroids. the patients should be carefully monitored for one year after the end of a long dexamethasone in connection with the possible development of relative adrenal insufficiency in stressful situations.
With the sudden cancellation, particularly in the case of the prior use of high doses may develop the syndrome of "lifting" (anorexia, nausea, lethargy, generalized musculoskeletal pain, fatigue), as well as worsening of the disease, about which he was appointed Dexamethasone.
During treatment, Dexamethasone should not be vaccinated due to a decrease in its effectiveness (immune response).
Assigning Dexamethasone with intercurrent infections, septic conditions, and tuberculosis, treatment with antibiotics is necessary to simultaneously bactericidal action.
Children during long-term treatment with Dexamethasone need careful monitoring of the dynamics of growth and development.Children who were in contact with sick measles or chickenpox during the treatment period prophylactically prescribe specific immunoglobulins.
Due to the weak mineralocorticoid effect for replacement therapy with adrenal insufficiency, Dexamethasone is used in combination with mineralocorticoids.
Patients with diabetes should monitor blood glucose and, if necessary, correct therapy.
An x-ray control of the osteoarticular system (images of the spine, hands) is shown.
In patients with latent infectious diseases of the kidneys and urinary tracts, Dexamethasone is able to cause leukocyturia, which can be of diagnostic significance.
Drug Interactions
The pharmaceutical incompatibility of dexamethasone with other intravenous drugs is possible. It is recommended that it be administered separately from other drugs (iv bolus, or via another drip as a second solution). When a solution of dexamethasone is mixed 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 inhibitors of carbonic anhydrase) 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 tolerance is worsened and the probability of ventricular extrasitolia increases (due to hypokalemia caused);
- indirect anticoagulants - weakens (less intensifies) their effect (dose adjustment required);
- anticoagulants and thrombolytics - the risk of bleeding from ulcers in the digestive tract increases;
- ethanol (alcohol) and non-steroidal anti-inflammatory drugs - increased risk of erosive ulcerative lesions in the gastrointestinal tract and development of bleeding (in combination with NSAIDs in the treatment of arthritis, a decrease in the dose of glucocorticosteroids due to the summation of the therapeutic effect);
- paracetamol - the risk of hepatotoxicity increases (induction of hepatic enzymes and the formation of a toxic metabolite of paracetamol);
- acetylsalicylic acid -accelerates its excretion and reduces the concentration in the blood (with the abolition of dexamethasone, the level of salicylates in the blood increases and the risk of side effects increases);
- insulin and oral hypoglycemic drugs, hypotensive drugs - their effectiveness decreases;
- vitamin D - its effect on absorption of Ca2 + in the intestine is reduced;
- somatotropic hormone - reduces the effectiveness of the latter, and with praziquantel - its concentration;
- M-holinoblokatorami (including antihistamines and tricyclic antidepressants) and nitrates - contributes to increased intraocular pressure;
- isoniazid and mexiletine - increases their metabolism (especially in "slow" acetylators), which leads to a decrease in their plasma concentrations.
Inhibitors of carbonic anhydrase and looped diuretics can increase the risk of osteoporosis.
Indomethacin, displacing dexamethasone from a bond with albumin, increases the risk of developing its side effects.
ACTH increases the effect of dexamethasone.
Ergocalciferol and parathyroid hormone interfere with the development of osteopathy caused by dexamethasone.
Cyclosporine and ketoconazole, slowing the metabolism of dexamethasone, may in some cases increase its toxicity.
Simultaneous appointment of androgens and steroid anabolic drugs with dexamethasone promotes the development of peripheral edema and hirsutism, the appearance of acne.
Estrogens and oral estrogen-containing contraceptives reduce the clearance of dexamethasone, which may be accompanied by an increase in the severity of its action.
With simultaneous use with live antiviral vaccines and against other types of immunization increases the risk of virus activation and the development of infections.
Antipsychotic drugs (antipsychotics) and azathioprine increase the risk of developing cataract in the appointment of dexamethasone.
With simultaneous use with antithyroid drugs is reduced, and with thyroid hormones - increases the clearance of dexamethasone.
Analogues of the drug Dexamethasone
Structural analogs for the active substance:
- Decadron;
- Dexaven;
- Dexazone;
- Dexamed;
- Dexamethasone buff;
- Dexamethasone Nycomed;
- Dexamethasone-Betalek;
- Dexamethasone-Vial;
- Dexamethasone-LENS;
- Dexamethasone-Ferein;
- Dexamethasone sodium phosphate;
- Dexamethasone phosphate;
- Dexamethasone-lang;
- Dexapos;
- Dexafar;
- Dexon;
- Maxidex;
- Oftan Dexamethasone;
- Fortecortin.
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