Albuterol

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Contents 1 More Specific Terms 2 Introduction 3 Indications 4 Contraindications 5 Dosage 6 Pharmacokinetics 7 Adverse-effects 8 Drug-interactions 9 Mechanism-of-action 10 More General Terms 11 Internet Database 12 References

More Specific Terms

• levalbuterol (Xopenex)

Introduction

• Tradenames: Ventolin, Proventil. salbutamol is generic name is most other countries. [7]

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)
• Solution: for inhalation ( nebulizer)

• 0.5%, 20 mL; 0.083%, 3 mL (box of 25)
• 2.5 mg/dose (0.083%) *Aerosols:

• Ventolin & Proventil HFA (hydrofluorocarbon) alledgedly have less effect than aerosols using chlorinated hydrocarbon propellants on the ozone layer of the earth

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 tablets
• up to 12 hours after administration of extended-release tablets [3]
  

• 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
• may increase risk of myocardial infarction [4]
  
• drug adverse effects of adrenergic receptor agonists
• drug adverse effects of beta-adrenergic receptor agonists

Drug-interactions

• beta blockers may antagonize effects
• MAO inhibitors potentiate cardiovascular effects
• tricyclic antidepressants ( TCA) potentiate cardiovascular effects
  
• 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

• beta-2 adrenergic receptor agonist
• antiasthmatic agent

Internet Database

PubChem: 2083
PubChem: 123600
PubChem: 39859

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#: [1] (subscription needed) [2]
6. Prescriber's Letter 14(11): 2007 How do HFA Inhalers Compare to CFC Inhalers? Detail-Document#: [3] (subscription needed) [4]
7. Prescriber's Letter 15(7): 2008 Detail-Document#: [5] (subscription needed) [6]

albuterol (Salbutamol, Ventolin, Proventil)