Arformoterol

A long-acting beta-adrenoceptor agonist used in the treatment of chronic obstructive pulmonary disease

Chemical structure of Arformoterol

Arformoterol is a long-acting beta-adrenoceptor agonist (LABA) used in the management of chronic obstructive pulmonary disease (COPD). It is the (R,R)-enantiomer of formoterol, which is responsible for the drug's bronchodilatory effects. Arformoterol is marketed under the brand name Brovana and is administered via inhalation.

Pharmacology

Arformoterol works by stimulating beta-2 adrenergic receptors in the bronchial smooth muscle, leading to muscle relaxation and bronchodilation. This action helps to alleviate symptoms of COPD such as shortness of breath and wheezing.

Ball-and-stick model of Arformoterol

Mechanism of Action

The drug binds to beta-2 adrenergic receptors, which are G protein-coupled receptors located on the surface of bronchial smooth muscle cells. Upon activation, these receptors initiate a cascade of intracellular events that result in the relaxation of smooth muscle fibers, thereby dilating the airways and improving airflow.

Pharmacokinetics

Arformoterol is administered via inhalation, allowing for direct delivery to the lungs. It has a rapid onset of action, typically within 20 minutes, and its effects can last up to 12 hours, making it suitable for twice-daily dosing. The drug is metabolized primarily in the liver and excreted in the urine.

Clinical Use

Arformoterol is indicated for the long-term maintenance treatment of bronchoconstriction in patients with COPD, including chronic bronchitis and emphysema. It is not intended for the relief of acute bronchospasm or for the treatment of asthma.

Side Effects

Common side effects of arformoterol include tremor, nervousness, and headache. As with other beta-agonists, it may cause cardiovascular effects such as increased heart rate and blood pressure. Patients should be monitored for signs of worsening asthma or paradoxical bronchospasm.

Illustration of Skeletal Muscle

Illustration of skeletal muscle

Related Pages

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