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albuterol (Salbutamol, Ventolin, Proventil)

Tradenames: Ventolin, Proventil. salbutamol is generic name is most other countries. [7] FDA approves generic for Proventil April 2020 [8] 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 Dosage: 1) nebulizer: 0.5 mL of 0.5% solution (2.5 mg) nebulized every 6 hours. 2) inhaler (MDI): 2 puffs every 4-6 hours & just before exercise. 3) oral: a) adults: 2-4 mg PO TID/QID. b) 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) Solution: for inhalation (nebulizer) a) 0.5%, 20 mL; 0.083%, 3 mL (box of 25) b) 2.5 mg/dose (0.083%) *Aerosols: -> Ventolin & Proventil HFA (hydrofluorocarbon) allegedly have less effect than aerosols using chlorinated hydrocarbon propellants on the ozone layer of the earth Pharmacokinetics: 1) onset of action: a) 5-15 minutes after oral inhalation b) within 30 minutes of oral administration of immediate- release tablets 2) peak effect: a) within 30 minutes after oral inhalation b) within 2-3 hours after oral administration of immediate- release tablets 3) duration of action a) 3-4 hours (occasionally 6 hours or longer) after oral inhalation b) 4-6 hours (occasionally 8 hours) after oral administration of immediate-release tablets c) up to 12 hours after administration of extended-release tablets [3] Adverse effects: 1) common (> 10%) - dose-related reflex tachycardia, tremor & palpitation - nausea/GI upset 2) 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 3) uncommon (< 1%) - chest pain, loss of appetite, paradoxical bronchospasm 4) other - decreased serum K+ concentration (hypokalemia) - may increase risk of myocardial infarction [4] Drug interactions: 1) beta blockers may antagonize effects 2) MAO inhibitors potentiate cardiovascular effects 3) tricyclic antidepressants (TCA) potentiate cardiovascular effects 4) concurrent administration of other agents that may lower serum K+ may increase risk of hypokalemia Mechanism of action: 1) selective beta 2-adrenergic agonist that produces a) bronchodilation b) central and peripheral vasodilation c) uterine relaxation d) skeletal muscle stimulation

Interactions

drug interactions drug adverse effects (more general classes)

Specific

levalbuterol (Xopenex)

General

antiasthmatic agent inhaled beta-2 adrenergic receptor agonist

Properties

AGONIST-FOR: beta-2 adrenergic receptor MISC-INFO: elimination route LIVER pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Prescriber's Letter 9(6):33 2002
  5. Prescriber's Letter 13(5): 2006 Albuterol Inhaler Shortages Detail-Document#: 220514 (subscription needed) http://www.prescribersletter.com
  6. Prescriber's Letter 14(11): 2007 How do HFA Inhalers Compare to CFC Inhalers? Detail-Document#: 231108 (subscription needed) http://www.prescribersletter.com
  7. Prescriber's Letter 15(7): 2008 Detail-Document#: 240701 (subscription needed) http://www.prescribersletter.com
  8. FDA News Release. April 8, 2020 FDA Approves First Generic of a Commonly Used Albuterol Inhaler to Treat and Prevent Bronchospasm. https://www.fda.gov/news-events/press-announcements/fda-approves-first-generic-commonly-used-albuterol-inhaler-treat-and-prevent-bronchospasm

Component-of

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