Dexamethasone

  • Jul 04, 2018

Dexamethasone analogues:

Dexamethasone instruction:

Manufacturer:

Active ingredients Dexamethasone:

release form Dexamethasone:

  • tablets of 0.5 mgNo. 10
  • Solution for injection 1 ml( 4 mg) in ampoules No. 25

To whom is Dexamethasone shown?

Endocrine disorders:

  • substitution therapy for primary or secondary( pituitary)
  • adrenocortical insufficiency( with the exception of acute adrenal insufficiency, for which cortisone or hydrocortisone is more suitable because of their more pronounced mineralocorticoid action);
  • congenital adrenal hyperplasia;
  • subacute inflammation of the thyroid gland and severe radiation inflammation of the thyroid gland.

Rheumatic diseases:

  • Rheumatoid arthritis( including juvenile rheumatoid arthritis) and extraarticular disorders in rheumatoid arthritis( rheumatic lungs, rheumatic
    heart, eye, skin vasculitis);
  • As ancillary treatment - to support the patient during the period when the essential drugs are not yet effective, and also for the treatment of patients for whom non-steroidal anti-inflammatory drugs do not provide satisfactory analgesic and anti-inflammatory effects.

Systemic connective tissue diseases:

  • vasculitis syndrome and amyloidosis( as ancillary and symptomatic treatment during the underlying disease)
  • systemic red worm infection( treatment of polyserositis and disorders of internal organs function),
  • Sjogren's syndrome( treatment of lung, kidney and brain disorders),
  • systemic sclerosis( treatment of myositis, pericarditis and alveolitis),
  • polymyositis, dermatomyositis,
  • systemic vasculitis,
  • amyloidosis( adrenocortical replacement therapy).

Skin diseases:

  • pemphigus,
  • bullous dermatitis herpetiformis,
  • exfoliative dermatitis,
  • ( severe) erythema,
  • erythema nodosum,
  • ( heavy) seborrheic dermatitis,
  • ( heavy) psoriasis,
  • shingles,
  • dermatomycosis,
  • scleroderma.

Allergic diseases( which are not amenable to conventional treatment):

  • asthma,
  • contact dermatitis,
  • atopic dermatitis,
  • serum sickness,
  • allergic rhinitis,
  • allergy to medicines,
  • urticaria after blood transfusions,
  • urticaria( which does not respond to standard treatment),
  • Quincke edema.

Gastrointestinal diseases:

  • ulcerative colitis( severe exacerbation),
  • Crohn's disease( severe exacerbation),
  • chronic autoimmune hepatitis,
  • rejection reaction after liver transplantation.

Respiratory tract:

  • acute toxic bronchiolitis,
  • chronic bronchitis,
  • asthma( strong exacerbation),
  • allergic bronchopulmonary aspergiloz,
  • extrinsic allergic alveolitis,
  • sarcoidosis,
  • infiltration of eosinophils,
  • pulmonary tuberculosis, accompanied by severe general weakness( with appropriate antituberculous therapy),
  • tuberculous pleurisy( along with appropriate anti-tuberculosis therapy),
  • pleurisy with systemic connective tissue disease,
  • pulmonary diseaseulit,
  • berrilioz( granulomatous inflammation),
  • obliterative bronchitis after being poisoned with toxic gases and radiation
  • aspiration pneumonia.

Hematologic Disorders:

  • inherited or acquired chronic hypoplastic anemia,
  • autoimmune hemolytic anemia,
  • secondary thrombocytopenia in adults,
  • erythroblastopenia,
  • acute lymphoblastic leukemia( introductory therapy),
  • myelodysplasia syndrome,
  • angioimmunoblastic malignant T-cell lymphoma( in combination withcytostatics),
  • plasmacytoma( in combination with cytostatics),
  • severe anemia after myelofibrosis with myeloid metaplasia

Kidney diseases:

  • primary or secondary glomerulonephritis,
  • renal dysfunction in systemic connective tissue diseases( red lichen worm, Sjogren's syndrome),
  • systemic vasculitis( usually in combination with cyclophosphamide),
  • glomerulonephritis with nodular polyarteritis,
  • Chierg-Strauss syndrome,
  • Wegener's granulomatosis,
  • purpura Shenlaine-Genocha,
  • mixed cryoglobulinemia,
  • renal dysfunction in arteritis Takayasu,
  • interstitial nephritis,
  • immunosuppressive treatment for kidney transplant,
  • stimulation of diuresis or reduction of proteinuria in idiopathic nephrotic syndrome( without uremia) and impaired renal function in systemic wolfish lupus.

Malignant diseases:

  • palliative treatment of leukemia and lymphoma in adults,
  • acute leukemia in children,
  • hypercalcemia in patients with non-malignant diseases.

Brainstorm:

  • brain swelling due to primary or metastatic brain tumor, craniotomy or head trauma.

Other indications:

  • Tuberculous meningitis with subarachnoid blockade( together with due antituberculous therapy),
  • trichinosis with neurologic symptoms or myocardial trichinosis,
  • diagnostic test of adrenal hyperfunction.

How to use Dexamethasone?

Doses should be determined individually, according to the individual patient's disease, as prescribed by the treatment period, the tolerability of corticosteroids and the body's response.
The recommended initial dose for adults is 0.5-9 mg per day, which is taken for 2-4 admission. The maintenance dose is usually 0.5-3 mg per day.

Initial doses of dexamethasone are given before a clinical response occurs, and then the dose should be gradually reduced to the lowest clinically effective dose. If oral treatment with large doses continues for a period longer than several days, the dose should be gradually reduced for several consecutive days or even for a longer time.
During long-term treatment with large oral doses, it is recommended to take Dexamethasone with food, and between meals to use antacids.

For children, the recommended oral dose for substitution therapy is 0.02 mg / kg body weight or 0.67 mg / m2 body surface area in three divided doses, with all other indications the recommended dose is 0.08-0.3 mg /kg of body weight or 2.5-10 mg / m2 of body surface area, in three to four doses.

Diagnostic tests of adrenal hyperplasia

Fast test for 1mg of Dexamethasone: 1mg of Dexamethasone the patient takes at 11am, and blood for the determination of cortisone concentration in the serum is taken the next day at 8am.

Specific 2-day test with 2 mg of Dexamethasone: for two days the patient takes 2 mg of Dexamethasone orally every six hours. The concentration of 17-hydroxycorticosteroid is determined in urine collected per day.

A dose of 0.75 mg of dexamethasone is equivalent to a dose of 4 mg of methylprednisolone and triamcinolone or 5 mg of prednisone and prednisolone or 20 mg of hydrocortisone and 25 mg of cortisone.

The injection solution can be administered intravenously( by injection or infusion with a glucose solution or saline solution), intramuscularly or topically( via internal articular injection or injection into lesions on the skin or infiltrate into soft tissues).

The recommended average initial daily dose for intravenous or intramuscular administration varies from 0.5 to 9 mg per day or even more as needed. The initial dose of Dexamethasone should be given before a clinical response occurs, and then the dose should be gradually reduced to the lowest clinically effective dose. High doses are prescribed for a period longer than several days, then the dose should be gradually reduced over the next few days or even for a longer period.

For intraarticular administration, the recommended dosage is 0.4 mg to 4 mg. The dose depends on the size of the affected joint. Usually 2-4 mg is injected into the large joints and 0.8-1 mg into small ones. Intra-articular injection can be repeated after 3-4 months, it can be prescribed no more than 3 to 4 times in one joint throughout life;it can be done simultaneously in not more than 2 joints. More frequent use can damage articular cartilage.

The dose of Dexamethasone that is introduced into the synovial bag is usually 2-3 mg, the dose that is introduced into the tendon sheath is 0.4-1 mg, and the dose that is introduced into the tendon is 1 to 2 mg.

The dose of Dexamethasone, which is introduced into the lesion, is equal to the intra-articular dose. These drugs can be administered in parallel to no more than two lesions.

Doses of 2 to 6 mg of dexamethasone are recommended for administration in soft tissues( around the joint).

Dosage for children

In substitution therapy, 0.02 mg / kg body weight or 0.67 mg / m2 body surface is administered intramuscularly, divided into three doses per day, two days into the third or 0.008-0.01 mg /kg body weight or 0.2-0.3 mg / m2 body surface area daily.
For other indications, the recommended dose is from 0.02 to 0.1 mg / kg body weight or from 0.8 to 5 mg / m2 body surface area, every 12 to 24 hours.

A dose of 0.75 mg of dexamethasone is equivalent to a dose of 4 mg of methylprednisolone and triamcinolone, or 5 mg of prednisone and prednisolone or 20 mg of hydrocortisone and 25 mg of cortisone.

Patients who have been treated with Dexamethasone for a long time may have withdrawal symptoms( also without adrenal insufficiency) when treatment is discontinued( fever, runny nose, redness of the conjunctiva, headache, dizziness, drowsiness or irritability, muscle and joint pain, vomiting, weight loss, weakness, often also convulsions).Therefore, the dose of Dexamethasone should be reduced gradually. Sudden discontinuation may have fatal consequences.

If the patient is in a state of unusual stress( due to trauma, surgery, or severe illness) during therapy or with discontinuation of therapy with Dexamethasone, his dose should be increased or used hydrocortisone or cortisone.

Patients who took Dexamethasone for a long time and experience severe stress after discontinuing therapy should resume taking Dexamethasone, as the resulting adrenal insufficiency may continue for several months after discontinuation of treatment.

Treatment with dexamethasone or natural glucocorticoids may mask the symptoms of an existing or new infection, as well as symptoms of intestinal perforation.

Dexamethasone can exacerbate systemic fungal infection, latent amoebiasis and pulmonary tuberculosis.
Patients with pulmonary tuberculosis in active form should receive dexamethasone( along with anti-tuberculosis drugs) only with rapid or strongly disseminated pulmonary tuberculosis. Patients with inactive pulmonary tuberculosis who are treated with dexamethasone, or patients who respond to tuberculin, should receive chemical prophylaxis.

Caution and medical supervision are recommended for patients with osteoporosis, hypertension, heart failure, tuberculosis, glaucoma, hepatic or renal insufficiency, diabetes, active peptic ulcer, fresh intestinal anastamosis, ulcerative colitis and epilepsy. Particular care is required by patients during the first weeks after myocardial infarction, patients with thromboembolism, severe myasthenia gravis, hypothyroidism, psychosis or psychoneurosis, as well as patients of advanced age.
During treatment with Dexamethasone, there may be an exacerbation of diabetes or a transition from the latent phase to clinical manifestations of diabetes.

For long-term treatment with Dexamethasone, serum potassium levels should be monitored.

Vaccination with live vaccine is contraindicated during treatment with Dexamethasone. Vaccination of the killed virus or bacterial vaccine does not lead to the expected development of antibodies and does not have the expected protective effect. Dexamethasone usually does not give 8 weeks before vaccination and does not start giving earlier than 2 weeks after vaccination.

Patients who have been treated with long doses of Midexamethasone for a long time and have never had measles, should avoid contact with infected individuals;In case of accidental contact, prophylactic treatment with immunoglobulin is recommended.
It is advisable to take care of patients who recover after surgery or bone fracture, since dexamethasone can slow the healing of wounds and the formation of bone tissue.
The effect of glucocorticoids is enhanced in patients with cirrhosis of the liver or hypothyroidism.

Corticoids can disrupt the results of allergic skin tests.
Children and adolescents can be treated with Dexamethasone only if clearly needed. During treatment, Dexamethasone requires careful monitoring of the growth and development of children and adolescents.

Pregnancy and lactation

It is impossible to exclude the harmful effect of Dexamethasone on the fetus and newborn baby. These drugs suppress the intrauterine fetal development. Dexamethasone should be taken during pregnancy only in certain urgent cases, if the expected benefit from taking to the mother outweighs the possible risk to the fetus. Special precautions are recommended for pre-eclampsia. According to general recommendations, during pregnancy, the lowest effective dose should be used to control the underlying disease. Children born to mothers who took glucocorticoids during pregnancy should be carefully checked for adrenal insufficiency.

Glucocorticoids pass through the placenta and reach high concentrations in the fetus. Dexamethasone is not as intensively metabolized in the placenta, as, for example, prednisone, so it can manifest itself in the fetus in high concentrations. According to some reports, even pharmacological doses of glucocorticoids may increase the risk of placental insufficiency, oligohydramniosa, delayed fetal development or its intrauterine death, an increase in the number of leukocytes( neutrophils) in the fetus and insufficiency of the adrenal glands.

Women who received corticosteroids during pregnancy are recommended additional doses of corticosteroids during labor. For prolonged labor or when planning a cesarean section, intravenous administration of 100 mg hydrocortisone every 8 hours is recommended before the birth of the child.

Small amounts of glucocorticoids are found in breast milk. Therefore, breast-feeding is not recommended during therapy with Dexamethasone( especially when using doses greater than physiological ones).Possible effect is to slow the growth of the child and reduce the secretion of endogenous glucocorticoids.

Side effects of dexamethasone.

The incidence of side effects depends on the dose and duration of treatment. The most common side effects of short-term treatment are increased appetite and weight gain, mental disorders, glucose intolerance and temporary adrenal insufficiency. The more rare side effects are allergic reactions, hypertriglyceridemia, peptic ulcer and acute pancreatitis. Long-term treatment most often leads to central obesity, skin vulnerability, muscle atrophy, osteoporosis, delayed growth and prolonged impairment of adrenal function. Less often - to aseptic necrosis of bones, cataracts, glaucoma, hypertension and decreased immune defense and increased susceptibility to infectious diseases.

Patients who have been treated with Dexamethasone for a long time may have withdrawal symptoms( also without apparent signs of adrenal insufficiency) when treatment is discontinued( fever, runny nose, redness of the conjunctiva, headache, dizziness, drowsiness or irritability, muscle and joint pain, vomiting, weight loss, weakness, often also convulsions).

Side effects on organ systems

  • Hematologic: leukocytosis, eosinophilia( as with other glucocorticoids), a decrease in the number of monocytes and / or lymphocytes, cases of thromboembolism. Rarely, thrombocytopenia and non-thrombocytopenic purpura.
  • Cardiovascular: polytropic ventricular extrasystole, paroxysmal bradycardia, hypertension and hypertensive encephalopathy, cardiac rupture is possible in patients who have recently undergone myocardial infarction.
  • Central nervous system: changes in personality and behavior, which are most often manifested as euphoria. Other side effects have also been reported: insomnia, irritability, hyperkinesia, depression and rarely psychosis. After treatment, edema of the optic nerve disk and increased intracranial pressure( pseudotumour) may occur. Neurological side effects such as dizziness, convulsions and headache may also occur. Endocrine and metabolic: suppression and atrophy of the adrenal glands( decreased response to stress), Cushing's syndrome, hirsutism, menstrual irregularity, reduced carbohydrate tolerance, increased need for insulin or oral diabetes medicines in diabetic patients, the transition of latent diabetes to a clinically active form,negative nitrogen balance due to protein catabolism, sodium and water content in the body, increased loss of potassium, edema and hypokalemic alkalosis, impotence and slow growth of children and podrotkov.
  • Gastrointestinal: nausea, hiccough, esophagitis, peptic ulcer of the stomach and duodenum, ulcerative perforations and bleeding in the gastrointestinal tract( bloody vomiting, melena), pancreatitis and perforation of the gallbladder and intestine( especially in patients with chronic inflammation
  • Bones and muscles: weakness, steroid myopathy, osteoporosis and compression fractures of the spine, aseptic osteonecrosis( more often aseptic necrosis of the head or thighs and shoulders), tendon ruptures( especially in couplesallelic use of certain quinolones.)
  • Skin: delayed wound healing, thin and vulnerable skin, petechiae and bruises, erythema, increased sweating, acne, suppressed reaction to skin tests. Allergic dermatitis, urticaria and angioedema can also occur
  • Eyes: increased intraocularpressure, glaucoma, cataract,
  • Hypersensitivity reactions are rare, they affect as a rash, hives, angioedema, bronchospasm and anaphylactic reaction. Who is contraindicated with Dexamethasone?

    Hypersensitivity to Dexamethasone or to any other ingredient in the preparation.
    Dexamethasone is contraindicated in cases of acute viral, bacterial or systemic fungal infections( unless proper therapy is used), Cushing's syndrome, vaccination with live vaccine, and breastfeeding( except in urgent cases).

    Interaction of dexamethasone.

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

    The effectiveness of dexamethasone is reduced if rifampicin, carbamazepine, phenobarbital, phenytoin, primidon, ephedrine or aminoglutethimide are taken in parallel. Therefore, the dose of Dexamethasone in such combinations should increase.

    Dexamethasone reduces the therapeutic effect of drugs for diabetes, hypertension, coumarin anticoagulants, praziquantel and sodium nuretics( therefore, the dose of these drugs should be increased);it increases the activity of heparin, albenzazole and potassium-urethics( the dose of these drugs should be reduced if necessary).

    Dexamethasone can alter the action of coumarin anticoagulants, so when using this combination of drugs, prothrombin time should be checked more often.

    Parallel use of dexamethasone and high doses of glucocorticoids or b2 receptor agonists increases the risk of hypokalemia. In patients with hypokalemia cardiac glycosides are more conducive to rhythm disturbance and have greater toxicity.

    Antacids reduce the absorption of Dexamethasone in the stomach. It has not been established whether concurrent use of food or alcohol affects the pharmacokinetics of Dexamethasone, however, concurrent administration of drugs and foods high in sodium is not recommended.

    Glucocorticoids increase the renal clearance of salicylate, so it is sometimes difficult to obtain therapeutic concentrations of salicylates in the serum. Care should be taken in patients who gradually reduce the dose of corticosteroids, as this may lead to an increase in salicylate concentration in the serum and intoxication.

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

    The simultaneous use of ritordine and dexamethasone is contraindicated during labor, as this can lead to pulmonary edema. It was reported of the death of the woman giving birth because of the development of this condition.

    Interactions that have therapeutic benefits: the concomitant administration of Dexamethasone and metoclopramide, diphenhydramide, prochlorperazine or antagonists of 5-HT3 receptors( serotonin receptors or 5-hydroxyl-tryptamine such as ondansetron or granisetron) is effective in preventing nausea and vomiting caused by cisplatin chemotherapy, cyclophosphamide, methotrexate, fluorouracil.

    Overdose of Dexamethasone.

    There are rare reports of acute overdose or death due to acute overdose.
    Overdose, of course, only after a few weeks of excessive doses can cause most of the unwanted effects listed in the "Side Effects" section, primarily Cushing's syndrome.

    Single intake of excessive amounts of tablets usually does not lead to clinically significant intoxication. There is no specific antidote against this drug. Treatment of overdose should be supportive and symptomatic. Hemodialysis is not an effective method of accelerated excretion of Dexamethasone from the body.