Flerobuterol

A beta-2 adrenergic receptor agonist

Flerobuterol
INN
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CAS Number	76792-18-2
PubChem	68770
DrugBank
ChemSpider	62013
KEGG

Flerobuterol is a beta-2 adrenergic receptor agonist that is used in the treatment of asthma and other conditions involving bronchoconstriction. It is a member of the class of drugs known as beta-adrenergic agonists, which work by stimulating the beta-2 adrenergic receptors in the lungs, leading to bronchodilation.

Chemical Structure

Chemical structure of Flerobuterol

Flerobuterol is chemically classified as a phenylethanolamine derivative. Its IUPAC name is (RS)-1-(4-amino-3,5-dichlorophenyl)-2-(tert-butylamino)ethanol. The presence of the tert-butyl group is characteristic of many beta-2 agonists, contributing to its selectivity and potency.

Mechanism of Action

Flerobuterol acts by binding to beta-2 adrenergic receptors located on the smooth muscle cells of the bronchi. This binding activates adenylate cyclase, which increases the levels of cyclic adenosine monophosphate (cAMP). Elevated cAMP levels lead to the activation of protein kinase A, which in turn phosphorylates target proteins that result in the relaxation of bronchial smooth muscle and subsequent bronchodilation.

Pharmacokinetics

The pharmacokinetic profile of flerobuterol includes its absorption, distribution, metabolism, and excretion. It is typically administered via inhalation, allowing for rapid onset of action. The drug is metabolized primarily in the liver, and its metabolites are excreted in the urine. The elimination half-life of flerobuterol is an important consideration in determining dosing frequency.

Clinical Use

Flerobuterol is primarily used in the management of asthma and chronic obstructive pulmonary disease (COPD). It is effective in relieving symptoms of bronchospasm and improving airflow in patients with obstructive airway diseases. The drug is often used in combination with other medications, such as corticosteroids, to enhance therapeutic outcomes.

Side Effects

Common side effects of flerobuterol include tremor, tachycardia, and nervousness. These effects are generally mild and result from the systemic absorption of the drug. In some cases, patients may experience hypokalemia or hyperglycemia, particularly with high doses or prolonged use.

Related Pages

• Beta-2 adrenergic receptor
• Asthma
• Chronic obstructive pulmonary disease
• Bronchodilator