What is Dexamethasone (corticosteroid)?

From the Guidelines

Dexamethasone is a potent synthetic corticosteroid medication used to treat various inflammatory conditions, allergic reactions, autoimmune disorders, and certain cancers, with its most recent and notable use being in the treatment of severe COVID-19, as evidenced by the RECOVERY trial published in 2020 1.

Key Characteristics of Dexamethasone

• It works by suppressing the immune system and reducing inflammation by inhibiting the release of inflammatory substances in the body.
• Dexamethasone is available in multiple forms including oral tablets (typical doses range from 0.5mg to 10mg), injectable solutions, eye drops, and topical preparations.
• The dosage and duration of treatment depend on the specific condition being treated, with short courses often prescribed for acute conditions and longer regimens for chronic disorders.

Common Uses and Side Effects

• Common uses include reducing brain swelling, treating severe COVID-19, managing chemotherapy side effects, and controlling symptoms in autoimmune diseases.
• Side effects can include increased blood sugar, mood changes, weight gain, increased infection risk, and bone thinning with long-term use.
• Patients should never stop taking dexamethasone abruptly as this can cause adrenal crisis; instead, the medication typically requires gradual tapering under medical supervision when discontinuing after prolonged use.

Recent Evidence and Guidelines

• The RECOVERY trial demonstrated a 3% absolute mortality benefit for patients hospitalized with COVID-19 treated with dexamethasone, with the greatest mortality reduction noted among patients receiving mechanical ventilation 1.
• However, a WHO-led meta-analysis of RCTs conducted during the pandemic concluded that glucocorticoids, including dexamethasone, were associated with a mortality reduction, but the benefit was not significant when using a random-effects model 1.
• Other studies and guidelines, such as those for multiple myeloma, also recommend the use of dexamethasone in combination with other therapies for the treatment of various conditions 1.

From the FDA Drug Label

Dexamethasone sodium phosphate is an adrenocortical steroid anti-inflammatory drug Chemically, dexamethasone sodium phosphate is 9-Fluoro-11ß,17,21-trihydroxy-16α-methylpregna-1,4-diene-3,20-dione 21-(dihydrogen phosphate) disodium salt Dexamethasone sodium phosphate, a synthetic adrenocortical steroid, is a white or slightly yellow, crystalline powder. The empirical formula is C 22H 28FNa 2O 8P and the structural formula is:

Dexamethasone is a synthetic adrenocortical steroid and an anti-inflammatory drug.

• It is also known as 9-Fluoro-11ß,17,21-trihydroxy-16α-methylpregna-1,4-diene-3,20-dione 21-(dihydrogen phosphate) disodium salt.
• The empirical formula of Dexamethasone sodium phosphate is C 22H 28FNa 2O 8P 2, 3.

From the Research

Definition and Uses of Dexamethasone

• Dexamethasone (DEX) is a potent synthetic glucocorticoid used for the treatment of a variety of inflammatory and immune-mediated disorders 4, 5, 6, 7.
• It is widely used in the treatment of brain cancer, as well as for inflammatory and autoimmune diseases 5.
• Dexamethasone has emerged as a promising therapy in the fight against severe COVID-19, due to its anti-inflammatory properties 4, 6.

Mechanism of Action

• The possible mechanism of action of DEX in the treatment of COVID-19 is related to its anti-inflammatory activity arising from inhibition of cytokine production 4.
• DEX may also influence immune cell trafficking and turnover, and has been shown to activate the pro-survival signalling pathway in the adult rat prefrontal cortex 4, 5.
• Dexamethasone modulates the activity of ion channels which regulate electrolyte and water transport across the airway epithelium, helping to reverse airway flooding in COVID-19 patients 6.

Properties and Delivery Systems

• Dexamethasone has poor water solubility, which can restrict its usage in the clinic and lead to severe side effects when administered systemically 7.
• Various nanoparticles have been developed to selectively deliver DEX, including liposomes, polymers, hydrogels, nanofibers, silica, calcium phosphate, and hydroxyapatite 7.
• The development of efficient DEX-loaded nanoformulations may help to ameliorate adverse disease effects and improve treatment outcomes 7.