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Dexamethasone

Dexamethasone is a potent synthetic glucocorticoid with anti-inflammatory, immunosuppressive, and metabolic properties. It is widely used in clinical practice for a variety of conditions, ranging from inflammatory disorders to certain types of cancer. This article provides a detailed overview of dexamethasone, including its mechanism of action, uses, dosage, side effects, precautions, drug interactions, and generic names, referencing authoritative sources such as the British National Formulary (BNF)Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology.

Dexamethasone exerts its effects by binding to intracellular glucocorticoid receptors, which then translocate to the nucleus and modulate gene transcription. This results in:

  1. Anti-inflammatory Effects: Dexamethasone inhibits the production of pro-inflammatory cytokines (e.g., IL-1, IL-6, TNF-α) and chemokines, reduces the migration of inflammatory cells to sites of inflammation, and stabilizes lysosomal membranes.
  2. Immunosuppressive Effects: It suppresses the activity of T-cells, B-cells, and macrophages, reducing the immune response.
  3. Metabolic Effects: Dexamethasone increases gluconeogenesis, reduces glucose uptake by cells, and promotes protein catabolism and lipolysis.
  4. Endocrine Effects: It suppresses the hypothalamic-pituitary-adrenal (HPA) axis, reducing the production of endogenous cortisol.

Dexamethasone is used in a wide range of clinical conditions, including:

  1. Inflammatory and Autoimmune Disorders:
    • Rheumatoid arthritis
    • Systemic lupus erythematosus
    • Asthma exacerbations
    • Allergic reactions
    • Inflammatory bowel disease (e.g., Crohn's disease, ulcerative colitis)
  2. Endocrine Disorders:
    • Adrenal insufficiency (as replacement therapy)
    • Congenital adrenal hyperplasia
  3. Oncology:
    • Management of chemotherapy-induced nausea and vomiting
    • Reduction of cerebral edema in brain tumors
    • Palliative treatment in certain cancers (e.g., multiple myeloma, lymphoma)
  4. Neurology:
    • Treatment of acute exacerbations of multiple sclerosis
    • Management of cerebral edema
  5. Other Uses:
    • Prevention of neonatal respiratory distress syndrome (antenatal use)
    • Treatment of croup in children
    • Management of septic shock (controversial, but sometimes used)

The dosage of dexamethasone varies depending on the condition being treated, the route of administration, and patient-specific factors. Below are general guidelines:

  1. Oral/Intravenous/Intramuscular:
    • Adults: 0.5–10 mg daily, depending on the condition. Higher doses may be used in acute conditions (e.g., cerebral edema: 10 mg initially, followed by 4 mg every 6 hours).
    • Children: 0.02–0.3 mg/kg/day in divided doses.
  2. Topical/Ophthalmic:
    • Applied as directed, typically 1–2 times daily.
  3. Special Populations:
    • Elderly: Lower doses may be required due to increased risk of side effects.

Renal/Hepatic Impairment: Dose adjustment may be necessary

Dexamethasone is generally well-tolerated when used short-term, but prolonged use can lead to significant side effects. These include:

  1. Common Side Effects:
    • Increased appetite and weight gain
    • Insomnia
    • Mood changes (e.g., anxiety, depression)
    • Gastrointestinal disturbances (e.g., nausea, peptic ulcers)
  2. Serious Side Effects:
    • Endocrine: Adrenal suppression, Cushing's syndrome, hyperglycemia.
    • Cardiovascular: Hypertension, fluid retention.
    • Musculoskeletal: Osteoporosis, muscle weakness.
    • Ophthalmic: Cataracts, glaucoma.
    • Infections: Increased susceptibility to infections due to immunosuppression.
  1. Contraindications:
    • Systemic fungal infections
    • Hypersensitivity to dexamethasone or other corticosteroids
  2. Warnings:
    • Use with caution in patients with diabetes, hypertension, peptic ulcer disease, osteoporosis, or psychiatric disorders.
    • Avoid abrupt discontinuation after prolonged use to prevent adrenal crisis.
  3. Monitoring:
    • Blood glucose levels
    • Blood pressure
    • Bone density (in long-term use)
    • Signs of infection

Dexamethasone interacts with several medications, including:

  1. Anticoagulants (e.g., warfarin): Increased risk of bleeding.
  2. Antidiabetic Agents: Reduced efficacy due to hyperglycemia.
  3. NSAIDs (e.g., ibuprofen): Increased risk of gastrointestinal bleeding.
  4. Vaccines: Reduced immune response to live vaccines.
  5. Enzyme Inducers (e.g., phenytoin, rifampin): Reduced dexamethasone levels.

Potassium-Depleting Drugs (e.g., diuretics): Increased risk of hypokalemia

Dexamethasone is available under various generic names and brand names worldwide. Some common generic names include:

  • Dexamethasone sodium phosphate
  • Dexamethasone acetate
  • Dexamethasone base

Brand names vary by region and formulation (e.g., Decadron, Dexasone, Hexadrol).

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