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Albuterol

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From Pharmacopedia
Albuterol
Ventolin, ProAir, Proventil, AccuNeb

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Summary
Common uses
Asthma rescue0, Acute bronchospasm0, Exercise-induced bronchospasm0, COPD exacerbation0
Pharmacy
Starting dose
MDI 90 mcg/puff, 2 puffs q4-6h prn; nebulized 2.5 mg in 3 mL saline q4-6h
Preparations
MDI 90 mcg/puff; nebulizer solution 0.083% (2.5 mg/3 mL), 0.5%, 0.021%, 0.042%; syrup 2 mg/5 mL; 2 mg, 4 mg tablets; 4 mg, 8 mg ER
US FDA Max
12 inhalations/d (rescue); higher for severe exacerbation under monitoring
Pharmacology
Routes
Inhaled (MDI, nebulized), Oral
Onset
Inhaled: 5-15 minutes; PO: 30 minutes
Duration
4-6 hours
Half-life
4-6 hours (inhaled and PO)[1]
Bioavailability
~10% inhaled reaches systemic circulation; ~50% PO[1]
Pregnancy
Preferred SABA in pregnancy; benefits of asthma control outweigh limited risks.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Albuterol is a short-acting selective β2-adrenergic agonist; receptor binding raises intracellular cAMP via Gs-protein-coupled adenylyl cyclase activation, relaxing bronchial smooth muscle within minutes.0 At higher doses β2 selectivity is lost, producing β1 effects (tachycardia, tremor) and hypokalemia from intracellular potassium shift[1].

References

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  1. 1.0 1.1 1.2 FDA Prescribing Information, Ventolin HFA (albuterol sulfate), GlaxoSmithKline, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020983s039lbl.pdf