Active ingredient: Albuterol - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Adrenergic beta-Agonists
• Tocolytic Agents
• Bronchodilator Agents

Dosage Forms

• Oral solution
• Syrup
• Tablet
• 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; Proair HFA; 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

Indications

For relief and prevention of bronchospasm due to asthma, emphysema, and chronic bronchitis

Pharmacology

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.

Absorption

Systemic absorption is rapid following aerosol administration

Toxicity

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.

Contraindications

VENTOLIN Inhalation Aerosol is contraindicated in patients with a history of hypersensitivity to albuterol or any of its components.

Drug Interactions

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 diuretics.

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.