Buy Dexamethasone pills 0.5 mg, 10 pcs
  • Buy Dexamethasone pills 0.5 mg, 10 pcs

Dexamethasone

Krka dd Novo mesto AO
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2019-09-19
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Clinical Pharmacology

Dexamethasone is a synthetic glucocorticoid drug that contains a fluorine atom.
It has a pronounced anti-inflammatory, anti-allergic and desensitizing effect, has immunosuppressive activity. Slightly retains sodium and water in the body. These effects are associated with inhibition of the release of inflammatory mediators by eosinophils; inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes (especially lysosomal) and organelle membranes. The immunodepressive effect is due to the inhibition of the release of cytokinins (interleukin 1, 2, gamma-interferon) from lymphocytes and macrophages. The main effect on metabolism is associated with protein catabolism, increased gluconeogenesis in the liver, and decreased glucose utilization by peripheral tissues.

The drug inhibits the activity of vitamin D, which leads to a decrease in calcium absorption and an increase in its excretion. Dexamethasone inhibits the synthesis and secretion of ACTH and, secondarily, the synthesis of endogenous glucocorticoids. A feature of the drug is a significant inhibition of pituitary function and the complete absence of mineralocorticoid activity.

Pharmacokinetics

Dexamethasone is rapidly and almost completely absorbed after ingestion. The bioavailability of dexamethasone pills is approximately 80%. Cmax in the blood plasma and the maximum effect after ingestion is achieved in 1-2 hours; after taking a single dose, the effect lasts for about 2.75 days.

In blood plasma, approximately 77% of dexamethasone binds to proteins, mainly albumin. A small amount of dexamethasone binds to nonalbumin proteins. Dexamethasone is a fat-soluble substance that can penetrate into extracellular and intracellular spaces. In the CNS (hypothalamus, pituitary) its effects are due to binding to membrane receptors. In peripheral tissues, it binds to cytoplasmic receptors. Its disintegration occurs in the place of its action, i.e. in a cage. Metabolized mainly in the liver before the formation of inactive metabolites. Excreted by the kidneys.

Indications

On the part of the endocrine system: replacement therapy of primary and secondary (pituitary) adrenal insufficiency, congenital adrenal hyperplasia, subacute thyroiditis and severe post-radiation thyroiditis. Rheumatic diseases: rheumatoid arthritis (including juvenile chronic arthritis) and extra-articular lesions in rheumatoid arthritis (lungs, heart, eyes, skin vasculitis).

Systemic diseases of the connective tissue, vasculitis and amyloidosis (as part of combination therapy): systemic lupus erythematosus (treatment of polyserositis and lesions of internal organs), Sjogren syndrome (treatment of lesions of the lungs, kidneys and brain), systemic sclerosis (treatment of myositis, pericarditis and alveolitis), polymyositis, dermatomyositis, systemic vasculitis, amyloidosis (replacement therapy with adrenal glands) scleroderma.

Skin diseases: pemphigoid, bullous dermatitis, dermatitis herpetiformis, exfoliative dermatitis, exudative erythema (severe forms), erythema nodosum, seborrheic dermatitis (severe forms), psoriasis (severe forms), lichen, fungoidal mycoses, edema, acne, lymphoma, zygoma , serum sickness, allergic rhinitis, drug disease (hypersensitivity to drugs), urticaria after blood transfusion, systemic immune diseases (sarcoidosis, temporal arteritis).

Eye Disorders: proliferative changes in orbit (endocrine ophthalmopathy, pseudotumor), sympathetic ophthalmia, immunosuppressive therapy for cornea transplantation.

Diseases of the gastrointestinal tract: ulcerative colitis (severe exacerbations), Crohn's disease (severe exacerbations), chronic autoimmune hepatitis, rejection after liver transplantation.

Blood disorders: congenital or acquired acute net aplastic anemia, autoimmune hemolytic anemia, secondary thrombocytopenia in adults, erythroblastopenia, acute lymphoblastic leukemia (induction therapy), myelodysplastic syndrome, angioimmunoblastic malignant T-cell lymphoma (in combination with cytostatics) plastotsitoma (in combination with cytostatics) , anemia after myelofibrosis with myeloid metaplasia or lymphoplasmacytoid immunocytoma, systemic histiocytosis (systemic process).

Kidney disease: primary and secondary glomerulonephritis (Goodpasture’s syndrome), kidney damage in systemic connective tissue diseases (systemic lupus erythematosus, Sjogren's syndrome), systemic vasculitis (usually in combination with cyclophosphamide), glomerulonephritis in nodular polyarteritis, Churg-Strauss syndrome, a body pattern, a body pattern, a body pattern, a body pattern, a body pattern, a body pattern, a body pattern, a body pattern, a body mask, a glomerulonephritis, nodular arteritis, Churg-Strauss syndrome, a body pattern, a body pattern, a body mask, a nodular arterial syndrome Genoha, mixed cryoglobulinemia, kidney damage in Takayasu arteritis, interstitial nephritis, immunosuppressive therapy after kidney transplantation, induction of diuresis or reduction of protein anemia in idiopathic nephrotic syndrome (without uremia) and kidney damage in the presence of systemic lupus erythematosus.

Malignant Diseases: palliative therapy of leukemia and lymphoma in adults, acute leukemia in children, hypercalcemia in malignant tumors.

Other indications: tuberculous meningitis with subarachnoid block (in combination with adequate anti-tuberculosis therapy), trichinosis with neurological or myocardial manifestations.

Composition

1 tablet contains:

Active substance: dexamethasone 0.5 mg.

Dexamethasone is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Dexamethasone Krka dd Novo mesto AO Slovenia pills
Dexamethasone Llara Russia ampoules
Dexamethasone PFK Obnovlenie Russia pills
Dexamethasone Rompharm K.O.Romparm Company S.R.L Romania eye drops
Dexamethasone Vial Vial Russia ampoules
Dexamethasone Farmak Ukraine eye drops
Dexamethasone Belmed Belmedpreparaty Belarus eye drops
Dexamethasone Bryntsalov Russia ampoules
Maxidex Alcon USA eye drops
Oftan Dexamethasone Santen France eye drops

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Dexamethasone

Dosage and Administration

Doses are set individually for each patient, depending on the nature of the disease, the expected duration of treatment, the tolerability of the drug and the patient's response to therapy.

Recommended starting dose for adults ranges from 0.5 mg to 9 mg / day.

The usual maintenance dose is from 0.5 mg to 3 mg / day.

The minimum effective daily dose is 0.5-1 mg.

The maximum daily dose is 10-15 mg.

The daily dose can be divided into 2-4 doses.

After reaching the therapeutic effect, the dose is gradually reduced (usually by 0.5 mg every 3 days until the maintenance dose is reached).

With long-term use of high doses by mouth, the drug is recommended to be taken during meals, and in the intervals between meals, antacids should be taken. The duration of dexamethasone use depends on the nature of the pathological process and the effectiveness of treatment and ranges from several days to several months or more. The treatment is stopped gradually (at the end, several injections of corticotropin are prescribed).

  • with bronchial asthma, rheumatoid arthritis, ulcerative colitis - 1.5-3 mg / day;
  • with systemic lupus erythematosus - 2-4.5 mg /;
  • with hematologic diseases - 7.5-10 mg.

For the treatment of acute allergic diseases, it is advisable to combine parenteral and oral administration: 1 day - 4-8 mg parenterally; 2 day - inside, 4 mg 3 times a day; 3, 4 days - inside, 4 mg 2 times a day; 5, 6 day - 4 mg / day, inside; Day 7 - the abolition of the drug.

Dosing in children

Children (depending on age) are prescribed 2.5-10 mg / m2 of body surface area /, dividing the daily dose into 3-4 doses.

Diagnostic tests for hyperfunction of the adrenal cortex

Short 1-mg dexamethasone test: 1 mg of dexamethasone inside at 11.00; blood sampling to determine serum cortisol at 8.00 the next day.

Special 2-day test with 2 mg of dexamethasone: 2 mg of dexamethasone orally every 6 hours for 2 days; daily urine is collected to determine the concentration of 17-hydroxycorticosteroids.

Adverse reactions

On the part of the immune system: infrequently, hypersensitivity reactions, reduced immune response and increased susceptibility to infections.

On the part of the endocrine system: often - transient adrenal insufficiency, growth retardation in children and adolescents, adrenal insufficiency and atrophy (reduction of the stress response), Itsenko-Cushing syndrome, menstrual disorder, hirsuitism, the transition of latent diabetes mellitus to clinically manifest, increased insulin or oral hypoglycemic drugs in patients with diabetes mellitus, sodium and water retention, increased potassium loss; very rarely, hypokalemic alkalosis, negative nitrogen balance due to protein catabolism.

Metabolism and nutrition disorders: often - reduced tolerance to carbohydrates, increased appetite and weight gain, obesity; infrequently - hypertriglyceridemia.

From the nervous system: often - mental disorders; infrequently, swelling of the papillae of the optic nerve and increased intracranial pressure (brain pseudo-tumor) after discontinuation of therapy, dizziness, headache; very rarely - convulsions, euphoria, insomnia, irritability, hyperkinesia, depression; rarely - psychosis.

From the digestive system: infrequently - peptic ulcers, acute pancreatitis, nausea, hiccups, stomach or duodenal ulcers; very rarely - esophagitis, perforation of the ulcer and bleeding of the gastrointestinal tract (hematomesis, melena), pancreatitis, perforation of the gallbladder and intestines (especially in patients with chronic inflammatory diseases of the large intestine).

From the senses: infrequently - posterior subcapsular cataract, increased intraocular pressure, a tendency to develop secondary bacterial, fungal or viral infections of the eye, trophic changes of the cornea, exophthalmos.

Since the cardiovascular system: infrequently - arterial hypertension, hypertensive encephalopathy; very rarely, polyfocal ventricular extrasystoles, transient bradycardia, heart failure, myocardial rupture after a recent acute heart attack.

On the part of the skin: often - erythema, thinning and brittleness of the skin, delayed healing of wounds, striae, petechiae and ecchymosis, increased sweating, steroid acne, suppression of the skin reaction during allergological tests; very rarely - anginevrotic edema, allergic dermatitis, urticaria.

From the musculoskeletal system: often - muscle atrophy, osteoporosis, muscle weakness, steroid myopathy (muscle weakness due to catabolism of muscle tissue); infrequently - aseptic bone necrosis; very rarely - compression vertebral fractures, tendon ruptures (especially when some quinolones are used together), damage to articular cartilage, and bone necrosis (associated with frequent intra-articular injections).

From the hemopoietic system: rarely, thromboembolic complications, a decrease in the number of monocytes and / or lymphocytes, leukocytosis, eosinophilia (as with other glucocorticosteroids), thrombocytopenia, and not thrombocytopenic purpura.

Allergic reactions: rarely - skin rash, itching, angioedema, bronchospasm, anaphylactic shock.

From the genitourinary system: rarely - impotence.

Contraindications

For short-term use for "vital" indications, the only contraindication is hypersensitivity to the active substance or auxiliary components of the drug.

The drug is contraindicated in patients with galactosemia, lactase deficiency and glucose-galactose malabsorption syndrome, due to the fact that the preparation contains lactose.

Carefully.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 (established or suspected); systemic mycosis; active and latent tuberculosis, 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 gastrointestinal tract:peptic ulcer and 12 duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, a newly created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis.

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

Endocrine diseases:diabetes mellitus (including the violation of tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease.

Severe chronic renal and / or liver failure, nephroluritiasis; hypoalbuminemia and conditions predisposing to its occurrence; systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (III-IV cent.), polio (with the exception of the form of bulbar encephalitis), open-angle and angle-closure glaucoma, lactation period.

Drug interactions

The simultaneous use of dexamethasone and nonsteroidal anti-inflammatory drugs (NSAIDs) increases the risk of developing and forming ulcers of the gastrointestinal tract.

The effect of dexamethasone is reduced with the simultaneous use of CYPZA4 isoenzyme inducers (for example, phenytoin, phenobarbitone, carbamazepine, primidone, rifabutin, rifampicin) or drugs that increase the metabolic clearance of glucocorticoids (ephedrine and amino glutetimid); in such cases, it is necessary to increase the dose of dexamethasone.

The interaction between dexamethasone and the drugs listed above may distort the results of dexamethasone suppression samples.If samples with dexamethasone are to be conducted during therapy with one of the listed drugs, this interaction should be taken into account when interpreting the results of the samples.

Simultaneous use of dexamethasone and inhibitors of the CYPZA4 isoenzyme (for example, ketoconazole, macrolide antibiotics) can lead to an increase in the concentration of dexamethasone in the blood.

The simultaneous use of drugs that are metabolized by CYPZA4 (for example, indinavir, erythromycin) may increase their clearance, which may be accompanied by a decrease in their serum concentrations.

Dexamethasone reduces the effectiveness of hypoglycemic drugs, antihypertensive drugs, praziquantel and natriuretics (it is necessary to increase the dose of these drugs); increases the activity of heparin, albendazole and potassium-sparing diuretics (if necessary, reduce the dose of these drugs).

Dexamethasone can change the effect of coumarin anticoagulants, therefore during therapy more frequent monitoring of prothrombin time is recommended. Antacids reduce the absorption of dexamethasone in the stomach. Smoking does not affect the pharmacokinetics of dexamethasone.

With simultaneous use of oral contraceptives, T1 / 2 glucocorticosteroids may increase, with a corresponding increase in their biological effects and an increase in the incidence of adverse side effects.

Simultaneous use of ritodrine and dexamethasone during labor is contraindicated, as this may lead to the death of the mother due to pulmonary edema. The combined use of dexamethasone and thalidomide can cause toxic epidermal necrolysis.

Potential therapeutically beneficial interactions:simultaneous application of dexamethasone and metoclopramide, diphenhydramine, prochlorperazine or antagonists of 5-HT3 receptor antagonists (serotonin or 5-hydroxytryptamine receptors of 3 types), such as ondansetron or granisetron, is effective in the prevention of nausea and vomiting caused by chemotherapy (cisplatin, cyclophosphamide, methotrexate, fluorouracil) .

Pregnancy and Lactation

In pregnancy (especially in the first trimester), the drug can be applied only when the expected therapeutic effect exceeds the potential risk to the fetus. With long-term therapy during pregnancy, the possibility of fetal growth disorder is not excluded. In the case of use at the end of pregnancy there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

If it is necessary to carry out drug treatment during breastfeeding, breastfeeding should be stopped.

Special instructions

Patients requiring long-term therapy with dexamethasone, after discontinuation of therapy, may develop a "withdrawal" syndrome (also without clear signs of adrenal insufficiency): fever, nasal discharge, conjunctival hyperemia, headache, dizziness, drowsiness and irritability, pain in muscles and joints , vomiting, weight loss, weakness, convulsions. Therefore, dexamethasone should be abolished by gradually reducing the dose. Rapid withdrawal of the drug can be fatal.

In patients who have received long-term therapy with dexamethasone and have been stressed after it is canceled, it is necessary to resume the use of dexamethasone, due to the fact that induced adrenal insufficiency may persist for several months after discontinuation of the drug.

Dexamethasone therapy may mask signs of existing or new infections and signs of intestinal perforation in patients with ulcerative colitis. Dexamethasone can aggravate the course of systemic fungal infections, latent amebiasis or pulmonary tuberculosis.

Patients with acute pulmonary tuberculosis dexamethasone can be prescribed (along with anti-tuberculosis drugs) only in the case of a fulminant or severe disseminated process. Patients with inactive pulmonary tuberculosis receiving dexamethasone therapy, or patients with positive tuberculin tests should simultaneously receive anti-tuberculosis chemoprophylaxis.

Special attention and careful medical observation is necessary for patients with osteoporosis, hypertension, heart failure, tuberculosis, glaucoma, hepatic or renal insufficiency, diabetes, active peptic ulcers, fresh intestinal anastomoses, ulcerative colitis and epilepsy.Carefully the drug is prescribed in the first weeks after acute myocardial infarction, in patients with thromboembolism, myasthenia, glaucoma, hypothyroidism, psychosis or psychoneurosis, as well as in patients over 65 years of age.

During therapy with dexamethasone, decompensation of diabetes mellitus or transition from latent to clinically manifest diabetes mellitus is possible.

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

During therapy with dexamethasone, vaccination with live vaccines is contraindicated.

Immunization with killed viral or bacterial vaccines does not give the expected increase in the titer of specific antibodies and therefore does not have the necessary protective effect. Dexamethasone is usually not prescribed 8 weeks before vaccination and within 2 weeks after vaccination.

Patients taking high doses of dexamethasone for a long time should avoid contact with measles patients; in case of accidental contact, prophylactic immunoglobulin treatment is recommended.

Care must be taken when treating patients who have recently undergone surgery or a bone fracture, since dexamethasone may slow down the healing of wounds and fractures.

The effect of glucocorticosteroids is enhanced in patients with cirrhosis or hypothyroidism.

Dexamethasone is used in children and adolescents only according to strict indications. During treatment, strict control of the growth and development of the child or teenager is necessary.

Special information about some of the components of the drug

The composition of the drug Dexamethasone is lactose, and therefore, its use in patients with galactosemia, lactase deficiency and glucose-galactose malabsorption syndrome is contraindicated.

Impact on the ability to drive motor vehicles and other complex mechanisms

Dexamethasone does not affect the ability to control vehicles and work with technical devices that require concentration of attention and speed of psychomotor reactions.

Overdosage

A single use of a large number of tablets does not lead to clinically significant intoxication.

Symptoms: may increase the dose-dependent side effects. In this case, the dose should be reduced.

Treatment: supportive and symptomatic.

There is no specific antidote.

Hemodialysis is ineffective.

Studies and clinical trials of Dexamethasone (Click to expand)
  1. Avascular necrosis of bone after adult acute lymphocytic leukemia treatment with methotrexate, vincristine, L-asparaginase, and dexamethasone (MOAD)
  2. Failure of pulse high-dose dexamethasone in chronic idiopathic immune thrombocytopenia
  3. Phase II trial of high-dose dexamethasone for previously treated immunoglobulin light-chain amyloidosis
  4. Cyclophosphamide, etoposide, vincristine, adriamycin, and dexamethasone (CEVAD) regimen in refractory multiple myeloma: An international oncology study group (IOSG) phase II protocol
  5. Comparison of the antileukemic activity in vitro of dexamethasone and prednisolone in childhood acute lymphoblastic leukemia
  6. Effects of interleukin-1 and dexamethasone on interleukin-6 production and growth in human meningiomas
  7. The influence of prolonged dexamethasone treatment of pregnant rats on the perinatal development of the adrenal gland of their offspring
  8. Low dose methotrexate, bleomycin, doxorubicin, cyclophosphamide, vincristine, and dexamethasone with zalcitabine in patients with acquired immunodeficiency syndrome-related lymphoma: Effect on human immunodeficiency virus and serum interleukin-6 levels over time
  9. Dexamethasone, etoposide, ifosfamide, and cisplatin as second-line therapy in patients with aggressive non-hodgkin's lymphoma
  10. Hiccups with high dose dexamethasone administration : A case report
  11. A study evaluating the efficacy and tolerability of tropisetron in combination with dexamethasone in the prevention of delayed platinum-induced nausea and emesis
  12. Substituting dexamethasone for prednisone complicates remission induction in children with acute lymphoblastic leukemia
  13. Localization of glycogen phosphorylase activity in liver of fasted normal and adrenalectomized rats and in fasted adrenalectomized rats after injection of dexamethasone
  14. The Baxα:Bcl-2 ratio modulates the response to dexamethasone in leukaemic cells and is highly variable in childhood acute leukaemia
  15. Comparison of multiple assays for kinetic detection of apoptosis in thymocytes exposed to dexamethasone or diethylstilbesterol
  16. Stimulus-secretion coupling in porcine adrenal chromaffin cells: Effect of dexamethasone
  17. Effect of dexamethasone on elevated cytokine mRNA levels in chemical-induced hippocampal injury
  18. Effects of polyelectrolyte complex (PEC) on human periodontal ligament fibroblast (HPLF) function. II. Enhancement of HPLF differentiation and aggregation on PEC by L-ascorbic acid and dexamethasone
  19. Expression of bone matrix proteins during dexamethasone-induced mineralization of human bone marrow stromal cells
  20. Dexamethasone alters rapidly actin polymerization dynamics in human endometrial cells: Evidence for nongenomic actions involving cAMP turnover
  21. Dexamethasone regulation of marrow stromal-derived osteoblastic cells
  22. Dexamethasone stimulates leptin release from human adipocytes: Unexpected inhibition by insulin
  23. Dexamethasone induces rapid actin assembly in human endometrial cells without affecting its synthesis

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