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Formoterol

Formoterol is a potent LABA for managing asthma and COPD, offering rapid and sustained bronchodilation. Its use requires careful monitoring for cardiovascular and metabolic side effects, particularly in high-risk patients. Adherence to guidelines from the BNFLippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology ensures safe and effective therapy.

Formoterol is a long-acting beta-2 adrenergic agonist (LABA) that selectively stimulates beta-2 receptors in bronchial smooth muscle. This activation leads to:

  1. Relaxation of bronchial smooth muscle: Via increased cyclic AMP (cAMP), reducing airway resistance.
  2. Inhibition of mast cell mediators: Reducing inflammation and bronchoconstriction.
  3. Enhanced mucociliary clearance: Improves airway function.

Formoterol has a rapid onset of action (1–3 minutes) and a long duration of effect (up to 12 hours), making it suitable for both maintenance and relief therapy in asthma and chronic obstructive pulmonary disease (COPD).

Formoterol is indicated for:

  1. Asthma:
    • Maintenance therapy in combination with inhaled corticosteroids (ICS).
    • Symptom relief in mild asthma (as part of a single maintenance and reliever therapy, SMART regimen).
  2. Chronic Obstructive Pulmonary Disease (COPD):
    • Maintenance therapy to improve lung function and reduce exacerbations.
  3. Exercise-Induced Bronchoconstriction:
    • Prophylaxis before exercise.

Adults and Adolescents (≥12 years):

  • Asthma/COPD: 6–12 mcg twice daily via inhalation.
  • SMART Regimen: 6 mcg as needed for symptom relief (max 72 mcg/day).
  • Exercise-Induced Bronchoconstriction: 6–12 mcg 15 minutes before exercise.

Children (6–11 years):

  • Asthma: 6 mcg twice daily (max 12 mcg/day).

Special Populations:

  • Renal/Hepatic Impairment: No dose adjustment required.
  • Elderly: Use with caution; monitor for cardiovascular effects.
  • Common: Tremor, headache, palpitations, muscle cramps.
  • Serious:
    • Cardiovascular: Tachycardia, arrhythmias, angina.
    • Hypokalemia: Due to intracellular potassium shift.
    • Paradoxical Bronchospasm: Rare; discontinue if occurs.
    • Allergic Reactions: Rash, angioedema.
  1. Asthma Mortality Risk:
    • LABAs should always be used with ICS in asthma to reduce the risk of severe exacerbations.
  2. Cardiovascular Disease:
    • Use with caution in patients with arrhythmias, ischemic heart disease, or hypertension.
  3. Diabetes:
    • May increase blood glucose levels; monitor in diabetics.
  4. Pregnancy/Lactation:
    • Category C: Use only if benefits outweigh risks.
    • Excreted in breast milk; avoid breastfeeding.

Formoterol interacts with:

  • Beta-Blockers:
    • Non-selective beta-blockers (e.g., propranolol) antagonize bronchodilatory effects.
  • Diuretics:
    • Increased risk of hypokalemia with loop or thiazide diuretics.
  • Xanthines (e.g., theophylline):
    • Increased risk of hypokalemia and arrhythmias.
  • Corticosteroids:
    • Enhanced hypokalemic effect.
  • QT-Prolonging Drugs:
    • Antiarrhythmics (e.g., amiodarone), macrolides (e.g., azithromycin) – additive risk of arrhythmias.
  • Generic: Formoterol fumarate.
  • Brand Names: Oxis (single agent), Symbicort (combination with budesonide), Foradil.

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