Betamethasone

Allopathic
Indications
  • Approved Indications:
    • Treatment of inflammatory and allergic disorders such as dermatitis, eczema, and psoriasis.
    • Management of severe allergic reactions and asthma exacerbations.
    • Autoimmune diseases like rheumatoid arthritis and systemic lupus erythematosus.
    • Replacement therapy for adrenocortical insufficiency and congenital adrenal hyperplasia.
    • Treatment of certain hematologic, neoplastic, and respiratory disorders.
  • Clinically Accepted Off-Label Uses:
    • Prevention of neonatal respiratory distress syndrome (antenatal corticosteroid therapy).
    • Management of cerebral edema due to tumors or trauma.
    • Treatment of inflammatory bowel disease flares (e.g., Crohn’s disease).
Dosage & Administration
  • Formulations: Oral tablets, injectable solutions, topical creams/ointments, inhalation aerosols, ophthalmic preparations.
  • Adults:
    • Oral or injectable doses vary widely depending on indication, typically 0.6 to 7.2 mg per day in divided doses.
    • For inflammatory conditions, 0.6 to 3 mg daily.
    • In severe asthma, higher doses may be used briefly.
    • Topical application as directed, typically 1–3 times daily.
  • Pediatrics:
    • Dose adjusted by body weight and severity; use lowest effective dose.
    • Caution to avoid growth suppression.
  • Elderly:
    • Start at lower doses due to increased susceptibility to side effects.
  • Special Populations:
    • No specific renal dosing adjustments; use cautiously in hepatic impairment.
    • Taper dose gradually after prolonged use to prevent adrenal insufficiency.
Mechanism of Action (MOA)

Betamethasone is a potent synthetic glucocorticoid that binds to cytoplasmic glucocorticoid receptors, forming a complex that translocates into the nucleus. This complex modulates gene expression, upregulating anti-inflammatory proteins and repressing pro-inflammatory genes. It suppresses multiple inflammatory pathways by inhibiting leukocyte migration, cytokine production, and immune cell activation. These effects reduce inflammation, allergic reactions, and immune responses, providing symptomatic relief in various conditions.

Pharmacokinetics
  • Absorption: Well absorbed orally; topical and inhaled absorption varies by formulation and site.
  • Distribution: Widely distributed, crosses the placenta and blood-brain barrier.
  • Metabolism: Primarily hepatic metabolism via CYP3A4 enzymes.
  • Elimination: Metabolites excreted mainly in urine; minimal unchanged drug.
  • Half-Life: Biological half-life approximately 36–54 hours; plasma half-life shorter (~2.5–5 hours).
  • Onset: Effects can begin within hours for systemic administration; topical effects vary.
Pregnancy Category & Lactation
  • Pregnancy: Category C (FDA) – Use only if benefits justify potential risk; crosses placenta and may affect fetal development.
  • Lactation: Excreted in breast milk; caution advised. Monitor infant for adverse effects if mother is treated.
Therapeutic Class
  • Glucocorticoid corticosteroid.
  • Potent anti-inflammatory and immunosuppressant agent.
Contraindications
  • Systemic fungal infections.
  • Hypersensitivity to betamethasone or formulation components.
  • Administration of live vaccines in immunocompromised patients.
  • Certain viral infections (e.g., herpes simplex of the eye) unless under antiviral therapy.
Warnings & Precautions
  • Risk of adrenal suppression, especially with prolonged use.
  • Monitor for hyperglycemia, hypertension, osteoporosis, cataracts, and infections.
  • Use with caution in patients with diabetes, hypertension, peptic ulcer disease, or psychiatric disorders.
  • Taper doses gradually to avoid withdrawal and adrenal crisis.
  • Avoid abrupt discontinuation after long-term therapy.
Side Effects
  • Common:
    • Increased appetite, weight gain, fluid retention
    • Mood changes, insomnia
    • Elevated blood glucose
    • Skin thinning, bruising with topical use
  • Serious/Rare:
    • Adrenal insufficiency
    • Osteoporosis and fractures
    • Immunosuppression leading to infections
    • Cushingoid appearance
    • Cataracts and glaucoma with prolonged use
Drug Interactions
  • CYP3A4 inducers (e.g., rifampin, phenytoin) may reduce betamethasone efficacy.
  • CYP3A4 inhibitors (e.g., ketoconazole) may increase toxicity risk.
  • Concurrent use with NSAIDs increases risk of gastrointestinal ulcers.
  • Live vaccines may be less effective or unsafe during therapy.
Recent Updates or Guidelines
  • Guidelines emphasize cautious use, minimizing dose and duration to reduce adverse effects.
  • Newer protocols favor topical or inhaled forms where appropriate to limit systemic exposure.
  • Updated recommendations on gradual tapering to prevent adrenal insufficiency.
Storage Conditions
  • Store at 20°C to 25°C (68°F to 77°F).
  • Protect from moisture and light.
  • Keep containers tightly closed and out of reach of children.
  • For injectable forms, protect from freezing and discard if precipitates form.