Brands, Medical Use, Clinical Data
- Adrenergic beta-Agonists
- Tocolytic Agents
- Bronchodilator Agents
- Oral solution
- Tablet (extended-release)
- Injection (intramuscular, intravenous)
Brands / Synonyms
Accuneb; Aerolin; Albuterol; Albuterol HFA; Albuterol Sulfate; Albuterol Sulfate Hfa; Asmaven; Broncovaleas; Cetsim; Cobutolin; Combivent; Combivent Respimat; Duoneb; Ecovent; Ipratropium and Albuterol; Loftan; Proventil; Proventil Inhaler; Proventil-Hfa; Rotahaler; Salbulin; Salbutamol; Salbutamol Free Base; Salbutamol Sulfate; Salbutamol Sulphate; Salbutard; Salbutine; Salbuvent; Solbutamol; Sultanol; Venetlin; Ventalin Inhaler; Ventolin; Ventolin Hfa; Ventolin Inhaler; Ventolin Rotacaps; Volma; Volmax; Xopenex; Xopenex HFA
For relief and prevention of bronchospasm due to asthma, emphysema, and chronic bronchitis
Albuterol, a moderately selective beta(2)-receptor agonist similar in structure to terbutaline, is widely used as a bronchodilator to manage asthma and other chronic obstructive airway diseases. The R-isomer, levalbuterol, is responsible for bronchodilation while the S-isomer increases bronchial reactivity.
Mechanism of Action
Albuterol is a beta(2)-adrenergic agonist. It stimulates beta(2)-adrenergic receptors. Binding of albuterol to beta(2)-receptors in the lungs results in relaxation of bronchial smooth muscles. It is believed that Albuterol increases cAMP production by activating adenylate cyclase, and the actions of albuterol are mediated by cAMP. Increased intracellular cyclic AMP increases the activity of cAMP-dependent protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular calcium concentrations. A lowered intracellular calcium concentrations leads to a smooth muscle relaxation. Increased intracellular cyclic AMP concentrations also cause an inhibition of the release of mediators from mast cells in the airways.
Systemic absorption is rapid following aerosol administration
LD50=1100 mg/kg (orally in mice)
Biotrnasformation / Drug Metabolism
Hydrolyzed by esterases in tissue and blood to the active compound colterol. The drug is also conjugatively metabolized to albuterol 4'-O-sulfate.
VENTOLIN Inhalation Aerosol is contraindicated in patients with a history of hypersensitivity to
albuterol or any of its components.
Other short-acting sympathomimetic aerosol bronchodilators should not be used concomitantly with
albuterol. If additional adrenergic drugs are to be administered by any route, they should be used with caution to
avoid deleterious cardiovascular effects.
Monoamine Oxidase Inhibitors or Tricyclic Antidepressants: Albuterol should be
administered with extreme caution to patients being treated with monoamine oxidase inhibitors or tricyclic
antidepressants, or within 2 weeks of discontinuation of such agents, because the action of albuterol on the vascular
system may be potentiated.
Beta-Blockers: Beta-adrenergic receptor blocking agents not only block the pulmonary
effect of beta-agonists, such as VENTOLIN Inhalation Aerosol, but may produce severe bronchospasm in patients with
asthma. Therefore, patients with asthma should not normally be treated with beta-blockers. However, under certain
circumstances, e.g., as prophylaxis after myocardial infarction, there may be no acceptable alternatives to the use
of beta-adrenergic blocking agents in patients with asthma. In this setting, cardioselective beta-blockers could be
considered, although they should be administered with caution.
Diuretics: The ECG changes and/or hypokalemia that may result from the administration
of nonpotassium-sparing diuretics (such as loop or thiazide diuretics) can be acutely worsened by beta-agonists,
especially when the recommended dose of the beta-agonist is exceeded. Although the clinical significance of these
effects is not known, caution is advised in the coadministration of beta-agonists with nonpotassium-sparing
Digoxin: Mean decreases of 16% to 22% in serum digoxin levels were demonstrated after
single-dose intravenous and oral administration of albuterol, respectively, to normal volunteers who had received
digoxin for 10 days. The clinical significance of these findings for patients with obstructive airway disease who are
receiving albuterol and digoxin on a chronic basis is unclear. Nevertheless, it would be prudent to carefully
evaluate the serum digoxin levels in patients who are currently receiving digoxin and albuterol.