Za Pharmacy
Drugs, Supplies and Delivery
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 BNF, Lippincott 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:
- Relaxation of bronchial smooth muscle: Via increased cyclic AMP (cAMP), reducing airway resistance.
- Inhibition of mast cell mediators: Reducing inflammation and bronchoconstriction.
- 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:
- 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).
- Chronic Obstructive Pulmonary Disease (COPD):
- Maintenance therapy to improve lung function and reduce exacerbations.
- 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.
- Asthma Mortality Risk:
- LABAs should always be used with ICS in asthma to reduce the risk of severe exacerbations.
- Cardiovascular Disease:
- Use with caution in patients with arrhythmias, ischemic heart disease, or hypertension.
- Diabetes:
- May increase blood glucose levels; monitor in diabetics.
- 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.
