albuterol (Salbutamol, Ventolin, Proventil)

Introduction

Tradenames: Ventolin, Proventil.

salbutamol is generic name is most other countries.

FDA approves generic for Proventil April 2020

Indications

• relief/prevention of bronchospasm in patients with obstructive airway disease & exercise-induced bronchospasm

Contraindications

Caution:

• use with caution in patients with hyperthyroidism or diabetes mellitus

pregnancy category = c

safety in lactation = ?

Dosage

• nebulizer: 0.5 mL of 0.5% solution (2.5 mg) nebulized every 6 hours.
• inhaler (MDI): 2 puffs every 4-6 hours & just before exercise.
• oral:
  • adults: 2-4 mg PO TID/QID.
  • children 2-6 yo: 0.1 mg/kg up to 2 mg PO TID.

Tabs: 2 & 4 mg. 100 tabs.

Extended release: 4 mg. 100 tabs.

Syrup: 2 mg/5 mL, as sulfate, alcohol & sugar-free (480 mL)

Aerosol:* 90 ug/metered dose (17 g) dry powder: Albuterol RespiClick 97 ug & ProAir Digihaler 108 ug per actuation

Solution: for inhalation (nebulizer)

• • 0.5%, 20 mL; 0.083%, 3 mL (box of 25)
  • 2.5 mg/dose (0.083%) *Aerosols vs dry powders:
    • Ventolin & Proventil HFA (hydrofluorocarbon) allegedly have less effect than aerosols using chlorinated hydrocarbon propellants on the ozone layer of the earth
    • dry powders more environmentally friendly than HFA or aerosols

Pharmacokinetics

• onset of action:
  • 5-15 minutes after oral inhalation
  • within 30 minutes of oral administration of immediate- release tablets
• peak effect:
  • within 30 minutes after oral inhalation
  • within 2-3 hours after oral administration of immediate- release tablets
• duration of action
  • 3-4 hours (occasionally 6 hours or longer) after oral inhalation
  • 4-6 hours (occasionally 8 hours) after oral administration of immediate-release tablets
  • up to 12 hours after administration of extended-release tablets

elimination via liver

Adverse effects

• common (> 10%)
  • dose-related reflex tachycardia, tremor & palpitation
  • nausea/GI upset
• less common (1-10%)
  • nervousness, CNS stimulation, hyperactivity, insomnia, dizziness, facial flushing, lightheadedness, drowsiness, headache, dry mouth, heartburn, vomiting, unusual taste, difficult urination, tremor, weakness, muscle cramps, cough, sweating
• uncommon (< 1%)
  • chest pain, loss of appetite, paradoxical bronchospasm
• other
  • decreased serum K+ concentration (hypokalemia)
  • may increase risk of myocardial infarction

• drug adverse effects of adrenergic receptor agonists
• drug adverse effects of beta-adrenergic receptor agonists
• drug adverse effects of sympathomimetic(s)

Drug interactions

• beta blockers may antagonize effects
• MAO inhibitors potentiate cardiovascular effects
• tricyclic antidepressants (TCA) potentiate cardiovascular effects
• concurrent administration of other agents that may lower serum K+ may increase risk of hypokalemia

• drug interaction(s) of beta-2 adrenergic receptor agonists with beta adrenergic receptor antagonists
• drug interaction(s) of beta-2 adrenergic receptor agonists with loop diuretics
• drug interaction(s) of beta-2 adrenergic receptor agonists with thiazide diuretics

Mechanism of action

• selective beta 2-adrenergic agonist that produces
  • bronchodilation
  • central and peripheral vasodilation
  • uterine relaxation
  • skeletal muscle stimulation

More general terms

• inhaled beta-2 adrenergic receptor agonist
• antiasthmatic agent

More specific terms

• levalbuterol (Xopenex)

Component of

• albuterol/budesonide (Airspura)
• albuterol/ipratropium (Combivent, DuoNeb)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2083
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=123600
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=39859