Dexamethasone (Tablets, Solution, Drops) Instructions for Use

ATC Code

H02AB02 (Dexamethasone)

Active Substance

Dexamethasone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Corticosteroids for oral administration

Pharmacotherapeutic Group

Glucocorticosteroid

Pharmacological Action

Glucocorticosteroid. It suppresses the functions of leukocytes and tissue macrophages. It limits the migration of leukocytes to the area of inflammation. It impairs the ability of macrophages to phagocytose and to form interleukin-1. It promotes the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of inflammation. It reduces capillary permeability caused by the release of histamine. It suppresses fibroblast activity and collagen formation.

It inhibits the activity of phospholipase A₂, leading to the suppression of prostaglandin and leukotriene synthesis. It suppresses the release of COX (mainly COX-2), which also contributes to the reduction of prostaglandin production.

It 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; it suppresses antibody formation.

Dexamethasone suppresses the release of ACTH and β-lipotropin by the pituitary gland but does not reduce the level of circulating β-endorphin. It inhibits the secretion of TSH and FSH.

When applied directly to blood vessels, it has a vasoconstrictor effect.

Dexamethasone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins, and fats. It stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys, and increases the activity of gluconeogenesis enzymes. In the liver, Dexamethasone enhances glycogen storage by stimulating the activity of glycogen synthase and the synthesis of glucose from protein metabolism products. The increase in blood glucose levels stimulates insulin secretion.

Dexamethasone suppresses glucose uptake by fat cells, which leads to the activation of lipolysis. However, due to increased insulin secretion, lipogenesis is stimulated, leading to fat accumulation.

It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, and bone tissue. Osteoporosis and Cushing’s syndrome are the main factors limiting long-term glucocorticosteroid therapy. As a result of the catabolic effect, growth suppression in children is possible.

In high doses, Dexamethasone can increase the excitability of brain tissues and contribute to a lowering of the seizure threshold. It stimulates excessive production of hydrochloric acid and pepsin in the stomach, which contributes to the development of peptic ulcer.

When used systemically, the therapeutic activity of dexamethasone is due to its anti-inflammatory, anti-allergic, immunosuppressive, and anti-proliferative effects.

Pharmacokinetics

Plasma protein binding is 60-70%. It crosses histohematic barriers. It is excreted in small amounts in breast milk.

It is metabolized in the liver. T_1/2 is 2-3 hours. It is excreted by the kidneys.

Indications

Systemic connective tissue diseases (systemic lupus erythematosus, scleroderma, polyarteritis nodosa, dermatomyositis, rheumatoid arthritis); acute and chronic inflammatory joint diseases: gouty and psoriatic arthritis, osteoarthritis (including post-traumatic), polyarthritis, scapulohumeral periarthritis, ankylosing spondylitis (Bekhterev’s disease), juvenile arthritis, adult-onset Still’s disease, bursitis, nonspecific tenosynovitis, synovitis, and epicondylitis; rheumatic fever, acute rheumatic carditis; bronchial asthma, exacerbation; status asthmaticus; acute and chronic allergic diseases: allergic reactions to drugs and foods, serum sickness, urticaria, allergic rhinitis, angioedema, drug exanthema, hay fever; skin diseases: pemphigus, psoriasis, eczema, atopic dermatitis, diffuse neurodermatitis, contact dermatitis (with large skin surface involvement), toxicoderma, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell’s syndrome), bullous herpetiform dermatitis, malignant exudative erythema (Stevens-Johnson syndrome); cerebral edema (including due to brain tumor or associated with surgery, radiation therapy, or head trauma) after preliminary parenteral use of dexamethasone; 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 state after adrenalectomy; congenital adrenal hyperplasia; autoimmune kidney diseases (including acute glomerulonephritis); nephrotic syndrome; subacute thyroiditis; diseases of the hematopoietic organs: agranulocytosis, pannyelopathy, autoimmune hemolytic anemia, acute lymphoblastic and myeloid leukemias, lymphogranulomatosis, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocyte anemia), congenital (erythroid) hypoplastic anemia; lung diseases: acute alveolitis, pulmonary fibrosis, sarcoidosis stage II-III; tuberculous meningitis, pulmonary tuberculosis, aspiration pneumonia (in combination with specific chemotherapy); borreliosis, Loeffler’s syndrome (not amenable to other therapy); lung cancer (in combination with cytostatics); multiple sclerosis; gastrointestinal diseases: ulcerative colitis, Crohn’s disease, regional enteritis; hepatitis; prevention of transplant rejection reaction; multiple myeloma (in combination with lenalidomide); performing a test for the differential diagnosis of hyperplasia (hyperfunction) and tumors of the adrenal cortex.

ICD codes

Dosage Regimen

Solution

The dosing regimen is individualized and depends on the indications, the patient’s condition, and their response to therapy. The drug is administered intravenously slowly as a bolus or by drip (in acute and emergency conditions); intramuscularly; local administration (into the pathological formation) is also possible. To prepare a solution for intravenous drip infusion, isotonic sodium chloride solution or 5% dextrose solution should be used.

In the acute period of various diseases and at the beginning of therapy, Dexamethasone is used in higher doses. From 4 to 20 mg of Dexamethasone can be administered 3-4 times per day.

Doses of the drug for children (intramuscularly)

The dose of the drug for replacement therapy (in adrenal cortex insufficiency) is 0.0233 mg/kg of body weight or 0.67 mg/m² of body surface area, divided into 3 doses, every 3rd day, or 0.00776 – 0.01165 mg/kg of body weight or 0.233 – 0.335 mg/m² of body surface area daily. For other indications, the recommended dose ranges from 0.02776 to 0.16665 mg/kg of body weight or 0.833 – 5 mg/m² of body surface area every 12-24 hours.

Upon achieving the effect, the dose is reduced to a maintenance dose or until treatment is discontinued. The duration of parenteral application is usually 3-4 days, after which they switch to maintenance therapy with dexamethasone tablets.

Long-term use of high doses of the drug requires a gradual dose reduction to prevent the development of acute adrenal cortex insufficiency.

Drops

For adults with severe inflammatory process, instill 1-2 drops into the conjunctival sac every 2 hours during the first 24-48 hours of treatment; as inflammation decreases, instill every 4-6 hours.

For prevention of inflammatory processes after eye surgeries and injuries, instill the drug 4 times/day during the first 24 hours after surgery, then 3 times/day for the next 2 weeks.

Tablets

Orally. The dose is selected individually depending on the nature of the disease, its degree of activity, and the patient’s response to the treatment.

Usually, the daily dose is from 2 to 6 mg/day. In severe cases, higher doses may be used, divided into 3-4 doses. The maximum dose is 10-15 mg/day. After achieving the therapeutic effect, the dose is gradually reduced to a maintenance dose of 2-4 mg/day or more. The minimum effective dose is 0.5-1 mg/day.

Adverse Reactions

From the endocrine system: decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing’s syndrome (including moon face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia, striae), delayed sexual development in children.

From the metabolism: increased excretion of calcium ions, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating, hypernatremia, hypokalemia.

From the nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, cerebellar pseudotumor, 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 – spread of the necrosis focus, slowing of scar tissue formation, which can lead to rupture of the heart muscle; with intracranial administration – nosebleed.

From the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding and perforation, increased or decreased appetite, flatulence, hiccups; rarely – increased activity of hepatic transaminases and alkaline phosphatase.

From the organ of vision: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes of the cornea, exophthalmos.

From the musculoskeletal system: slowing of growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely – pathological bone fractures, aseptic necrosis of the humeral and femoral head), muscle tendon rupture, steroid myopathy, decreased muscle mass (atrophy).

Dermatological reactions: delayed wound healing, petechiae, ecchymoses, thinning of the skin, hyper- or hypopigmentation, steroid acne, striae, tendency to develop pyoderma and candidiasis.

Allergic reactions: skin rash, skin itching, anaphylactic shock.

Effects associated with immunosuppressive action: development or exacerbation of infections (the appearance of this side effect is facilitated by concurrently used immunosuppressants and vaccination).

Contraindications

Hypersensitivity to dexamethasone; systemic mycoses, other systemic infections in the absence of adequate antimicrobial therapy; simultaneous use with live antiviral vaccines; breastfeeding period.

For short-term use for vital indications, the only contraindication is hypersensitivity to dexamethasone or to any other of the excipients.

Use in Pregnancy and Lactation

During pregnancy, the drug can be used only when the expected benefit for the mother outweighs the potential risk to the fetus.

If it is necessary to carry out treatment with dexamethasone during breastfeeding, breastfeeding should be discontinued.

Use in Hepatic Impairment

Should be used with caution in severe chronic hepatic insufficiency.

Use in Renal Impairment

Should be used with caution in severe chronic renal insufficiency, nephrourolithiasis.

Pediatric Use

In children during the growth period, Dexamethasone should be used only for absolute indications and under the especially careful supervision of the attending physician.

Special Precautions

Dexamethasone should be used with caution in systemic parasitic and infectious diseases of viral, fungal or bacterial nature (including in the anamnesis, including recent contact with a patient) – herpes simplex, herpes zoster (viremic phase), chickenpox, measles, amoebiasis, strongyloidiasis (established or suspected), systemic mycosis, active or latent tuberculosis; during vaccination (8 weeks before and 2 weeks after vaccination), with lymphadenitis after BCG vaccination; immunodeficiency states (including AIDS or HIV infection); gastrointestinal diseases (gastric or duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with threat of perforation or abscess formation, diverticulitis); cardiovascular system diseases, including recently suffered myocardial infarction (in patients with acute and subacute myocardial infarction, spread of the necrosis focus, slowing of scar tissue formation and, as a result, rupture of the heart muscle is possible), decompensated chronic heart failure, arterial hypertension, hyperlipidemia; endocrine diseases: diabetes mellitus (including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing’s disease, obesity III-IV degree; severe chronic renal and/or hepatic insufficiency, nephrourolithiasis; hypoalbuminemia and conditions predisposing to its occurrence; systemic osteoporosis, myasthenia gravis, poliomyelitis (except for the form of bulbar encephalitis), epilepsy, steroid myopathy; acute psychosis, severe affective disorders (including in the anamnesis, especially steroid psychosis); open-angle and closed-angle glaucoma, herpetic eye disease (risk of corneal perforation); pregnancy.

During treatment with dexamethasone (especially long-term), observation by an ophthalmologist, monitoring of blood pressure and water-electrolyte balance, as well as peripheral blood picture and blood glucose concentration is necessary.

To reduce side effects, potassium intake should be increased (diet, potassium preparations). Food should be rich in proteins, vitamins, with limited content of fats, carbohydrates and table salt.

The effect of dexamethasone is enhanced in patients with hypothyroidism and liver cirrhosis.

Dexamethasone may exacerbate existing emotional instability or psychotic disorders. If there is a history of psychoses, Dexamethasone in high doses is prescribed under strict medical supervision.

In stressful situations during maintenance treatment (e.g., surgery, trauma or infectious disease), the dose of the drug should be adjusted due to the increased need for corticosteroids. Patients should be carefully observed for a year after the end of long-term therapy with dexamethasone due to the possible development of relative adrenal cortex insufficiency in stressful situations.

With sudden withdrawal, especially in the case of prior use of high doses, withdrawal syndrome (anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness), as well as exacerbation of the disease for which Dexamethasone was prescribed, may develop.

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 carry out treatment with bactericidal antibiotics.

In patients with diabetes mellitus, blood glucose content should be monitored and therapy adjusted if necessary.

X-ray control of the musculoskeletal system (X-ray images of the spine, hand) is indicated.

In patients with latent infectious disease of the kidneys and urinary tract, Dexamethasone can cause leukocyturia, which may have diagnostic significance.

Dexamethasone increases the content of metabolites: 11-hydroxycorticosteroids and 17-hydroxycorticosteroids.

Use in pediatrics

In children during the growth period, Dexamethasone should be used only for absolute indications and under the especially careful supervision of the attending physician. In children during long-term treatment with dexamethasone, careful monitoring of the dynamics of growth and development is necessary.

Children who were in contact with patients with measles or chickenpox during the treatment period are prophylactically prescribed specific immunoglobulins.

Influence on the ability to drive vehicles and mechanisms

During the treatment period, it is necessary to refrain from driving vehicles and mechanisms requiring increased concentration of attention and speed of psychomotor reactions.

Drug Interactions

Dexamethasone increases the toxicity of cardiac glycosides (due to the resulting hypokalemia, the risk of arrhythmias increases).

Accelerates the excretion of acetylsalicylic acid, reduces the content of its metabolites in the blood (upon withdrawal of dexamethasone, the concentration of salicylates in the blood plasma increases and the risk of side effects increases).

When used simultaneously with live antiviral vaccines and against the background of other types of immunizations, it increases the risk of virus activation and the development of infections.

Increases the metabolism of isoniazid, mexiletine (especially in “fast acetylators”), which leads to a decrease in their plasma concentrations.

Increases the risk of hepatotoxic action of paracetamol (induction of liver enzymes and formation of a toxic metabolite of paracetamol).

Increases (with long-term therapy) the content of folic acid.

Hypokalemia caused by dexamethasone may increase the severity and duration of muscle blockade against the background of muscle relaxants.

In high doses, it reduces the effect of somatropin.

Reduces the action of hypoglycemic drugs; enhances the anticoagulant effect of coumarin derivatives.

Weakens the effect of vitamin D on the absorption of calcium ions in the intestinal lumen. Ergocalciferol and parathyroid hormone prevent the development of osteopathy caused by dexamethasone.

Reduces the concentration of praziquantel in blood plasma.

Cyclosporine (inhibits metabolism) and ketoconazole (reduces clearance) increase toxicity.

Thiazide diuretics, carbonic anhydrase inhibitors, other corticosteroids and amphotericin B increase the risk of hypokalemia, sodium-containing drugs – edema and increased blood pressure.

NSAIDs and ethanol increase the risk of ulceration of the gastrointestinal mucosa and bleeding; in combination with NSAIDs for the treatment of arthritis, a reduction in the dose of corticosteroids is possible due to the summation of the therapeutic effect.

Indomethacin, displacing Dexamethasone from binding with albumins, increases the risk of its side effects.

Amphotericin B and carbonic anhydrase inhibitors increase the risk of osteoporosis.

The therapeutic effect of dexamethasone is reduced under the influence of phenytoin, barbiturates, ephedrine, theophylline, rifampicin and other inducers of liver microsomal enzymes (increased metabolic rate).

Mitotane and other inhibitors of adrenal cortex function may necessitate an increase in the dose of dexamethasone.

The clearance of dexamethasone increases against the background of the use of thyroid hormone preparations.

Immunosuppressants increase the risk of infections and lymphoma or other lymphoproliferative disorders caused by the Epstein-Barr virus.

Estrogens (including oral estrogen-containing contraceptives) reduce the clearance of dexamethasone, prolong the half-life and their therapeutic and toxic effects.

The appearance of hirsutism and acne is facilitated by the simultaneous use of other steroid hormonal drugs – androgens, estrogens, anabolic steroids, oral contraceptives.

Tricyclic antidepressants may exacerbate the severity of depression caused by dexamethasone intake, therefore they are not indicated for the therapy of these side effects.

The risk of cataract development increases when used against the background of other corticosteroids, antipsychotic drugs (neuroleptics), carbutamide and azathioprine.

Simultaneous administration with anticholinergics (including antihistamines, tricyclic antidepressants), nitrates contributes to the development of increased intraocular pressure.

Simultaneous administration of antacids reduces the absorption of dexamethasone.

When used simultaneously with antithyroid drugs, the clearance of dexamethasone decreases, and with thyroid hormones, it increases.

Storage Conditions

Store at 15°C (59°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.