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Long-Acting Beta-2 AgonistAka: Long-acting Beta Agonist, Salmeterol, Serevent, Formoterol

See Also
1. Short-acting Beta Agonist
2. Beta Agonist
Indications
1. Moderate Persistent Asthma
2. Severe Persistent Asthma
Precautions
1. Not a substitute for Inhaled Corticosteroids
  1. Steroids are key management of persistent Asthma
  2. Long-acting beta agonists are in addition to steroids
  3. Lazarus (2001) JAMA 285:2583
2. Do NOT exceed dosing schedule (e.g. Serevent bid)
  1. Use a short acting Beta agonist for rescue use
3. Tolerance over time to Protective effect
  1. Effect diminishes over one month of use
  2. Reference
    1. Simons (1997) Pediatrics 99:655
Preparations
1. Salmeterol (Serevent) Dry Powder Diskus (50 ug/inhale)
  1. One inhalation every 12 hours
2. Serevent Inhalation aerosol MDI (21 ug/puff)
  1. Adults: 2 puffs every 12 hours
  2. Child: 1-2 puffs every 12 hours
3. Formoterol (Foradil)
  1. One inhalation every 12 hours
References
1. (2001) Med Clin North Am 43(1104):39
2. Wilson (2001) Chest 119:2021

formoterol (C0060657)
Definition (NCI)	A long-acting beta-adrenergic receptor agonist with bronchodilator activity. Formoterol selectively binds to beta-2 adrenergic receptors in bronchial smooth muscle, thereby activating intracellular adenyl cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP levels cause relaxation of bronchial smooth muscle, relieve bronchospasms, improve mucociliary clearance and reduce mediator substance release from inflammatory cells, especially from mast cells.
Concepts	Organic Chemical (T109) , Pharmacologic Substance (T121)
English	Eformoterol, formoterol, FORMOTEROL PREPARATION
Spanish	eformoterol, formoterol
Credits	Derived from the NIH UMLS (Unified Medical Language System)

salmeterol (C0073992)
Definition (NCI)	A highly selective, long-acting beta2-adrenergic agonist with bronchodilatory activity. Salmeterol's benzene moiety resembles the structure of catecholamines, and occupies the active site of beta2-adrenergic receptor, while the long, lipophilic side chain of salmeterol, binds to the so called 'exosite' near the beta2-receptors. The binding at the exosite allows the active portion of the molecule to remain at the receptor site and continually engage and disengage with the receptor, therefore providing a long duration of action. This agent stimulates intracellular adenyl cyclase to catalyze the conversion of adenosine triphosphate to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP levels result in relaxation of bronchiolar smooth muscle, bronchodilation and increased bronchial airflow.
Concepts	Organic Chemical (T109) , Pharmacologic Substance (T121)
English	salmeterol, SALMETEROL PREPARATION, Salmeterol product
Spanish	salmeterol
Credits	Derived from the NIH UMLS (Unified Medical Language System)

Serevent (C0700491)
Concepts	Organic Chemical (T109) , Pharmacologic Substance (T121)
English	Serevent
Credits	Derived from the NIH UMLS (Unified Medical Language System)