Drug Interactions
Specific Drugs
| Drug |
Interaction |
Comments |
| β-Adrenergic blocking agents |
Antagonism of pulmonary effects resulting in severe bronchospasm in asthmatic patients |
If concomitant therapy required, consider cautious use of cardioselective β-adrenergic blocking agents |
| Digoxin |
Decreased serum digoxin concentrations |
Careful evaluation of serum digoxin concentrations recommended |
| Diuretics, nonpotassium-sparing |
Decreased serum potassium concentrations and/or ECG changes, especially when the recommended β-agonist dose is exceeded |
Cautious use recommended |
| MAO inhibitors |
Increased effect on vascular system |
Extreme caution recommended with concomitant therapy or in patients receiving albuterol within 2 weeks of discontinuance of these agents |
| Sympathomimetic agents (e.g., epinephrine) |
Increased cardiovascular adverse effects |
Avoid concomitant use of inhaled albuterol and other short-acting inhaled sympathomimetic amine bronchodilators or oral albuterol and other oral sympathomimetic agents
Concomitant oral albuterol and inhaled sympathomimetic agent may be used on individualized basis
If such concomitant use regularly required, consider alternative therapy |
Pharmacokinetics
Absorption
Single-dose oral bioavailability of extended-release albuterol sulfate tablets is about 80% that of conventional tablets. Efficacy of orally inhaled drug appears to result from local action rather than systemic absorption. Drug plasma concentrations do not predict therapeutic effect.
Onset
Conventional tablets or solution: Within 30 minutes.
Inhalation aerosol: Within 5–15 minutes.
Oral inhalation solution: Within 5 minutes.
Duration
Inhalation aerosol: 3–6 hours.
Oral inhalation solution: 2–4 hours, occasionally ≥6 hours.
Conventional tablets: Up to 8 hours.
Extended-release tablets: Up to 12 hours.
Oral solution: Up to 6 hours.
Food
Reduces the rate of absorption of albuterol sulfate extended-release tablets.
Distribution
Extent
Albuterol crosses the placenta. Not known whether albuterol distributes into milk.
Elimination
Metabolism
Extensively metabolized in the intestinal wall and liver to inactive metabolites.
Elimination Route
Substantially eliminated by kidneys. Approximately 72% of a dose (oral inhalation) excreted in urine as unchanged drug and metabolites within 24 hours. About 76% of a single dose (oral administration) excreted in urine over 3 days; about 4% is excreted in feces.
Half-life
Oral inhalation: 3.8–6 hours in healthy adults, 1.7–7.1 hours in patients with asthma.
Conventional tablets: 5–7.2 hours.
Extended-release tablets: 9.3 hours.
Oral solution: 5 hours in healthy individuals.
Stability
Storage
Oral
Extended-release tablets: 20–25°C; protect from light.
Conventional tablets: 20–25°C; protect from light.
Oral solution: 2–30°C or 20–25°C, depending on manufacturer; protect from light.
Oral Inhalation
Albuterol inhalation aerosol: 25°C (may be exposed to 15–30°C) for (Proventil®).
Albuterol sulfate inhalation aerosol: 15–25°C (ProAir® HFA, Proventil® HFA, Ventolin® HFA).
Failure to use inhalers within these respective temperature ranges could result in delivery of improper doses.
Albuterol sulfate in fixed combination with ipratropium bromide inhalation aerosol: 25°C (may be exposed to 15–30°C); protect from excessive humidity.
Albuterol sulfate oral inhalation solution: 2–25°C or 15–30°C depending on manufacturer. Discard albuterol sulfate oral inhalation concentrate solution if the solution changes color or becomes cloudy. Discard albuterol sulfate solution for nebulization (in single-use units) if it becomes discolored.
Albuterol sulfate in fixed combination with ipratropium bromide oral inhalation solution: 2–25°C.
Actions
- Stimulates β-adrenergic receptors with little or no effect on α-adrenergic receptors.
- Stimulates the production of cyclic adenosine-3null,5null-monophosphate (AMP), which mediates numerous cellular responses, including smooth muscle relaxation and inhibiting the release of mediators from mast cells in the airways.
- Relaxes smooth muscles from the trachea to the terminal bronchial tree.
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