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Pharmacology of Olodaterol; Definition, Mechanism of action, Pharmacokinetics, Uses, Effect
🫁 Olodaterol Pharmacology Overview
Olodaterol is a long-acting β₂-adrenergic receptor agonist (LABA) used for once-daily maintenance treatment of chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. It’s marketed under brand names like Striverdi Respimat and often combined with tiotropium for enhanced bronchodilation.
⚡ Mechanism of Action
β₂-receptor agonism: Activates β₂ receptors in airway smooth muscle, stimulating adenylyl cyclase → ↑ cyclic AMP (cAMP) → bronchodilation.
Selectivity: Highly selective for β₂ over β₁ and β₃ receptors, minimizing cardiac and metabolic side effects.
Rapid onset: Begins working within 5–10 minutes of inhalation.
💊 Pharmacokinetics
Parameter Value
Bioavailability ~30% via inhalation
Peak plasma time 10–20 minutes
Protein binding ~60%
Metabolism Glucuronidation (UGT2B7, UGT1A1, etc.) and O-demethylation (CYP2C9, CYP2C8)
Half-life ~45 hours (inhalation)
Excretion ~53% feces, ~38% urine
🧬 Pharmacodynamics
Bronchodilation: Sustained for 24 hours, allowing once-daily dosing.
Improves FEV₁: Enhances lung function and reduces airflow obstruction.
Reverses bronchoconstriction: Potently counteracts active airway narrowing.
💊 Therapeutic Uses
Indication Role of Olodaterol
COPD (chronic bronchitis/emphysema) Maintenance bronchodilation
Asthma Not approved for monotherapy
Combination therapy Often paired with tiotropium
⚠️ Safety & Side Effects
Common: Nasopharyngitis, bronchitis, cough, dizziness, rash.
Serious risks:
Paradoxical bronchospasm
QT prolongation
Hypokalemia, tachycardia, hypertension
Contraindications:
Monotherapy in asthma
MAOI use within 14 days
Severe cardiovascular disease
🧪 Chemical Profile
Property Value
Molecular Formula C₂₁H₂₆N₂O₅
Molecular Weight 386.45 g/mol
Drug Class Long-acting β₂ agonist
Structure Type Phenylethanolamine derivative
IUPAC Name 6-Hydroxy-8-{(1R)-1-hydroxy-2-[1-(4-methoxy
#Olodaterol
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