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Long-Acting Beta-2 Agonist

Aka: Long-Acting Beta-2 Agonist, Long-acting Beta Agonist, Long-Acting Inhaled Bronchodilator, Salmeterol, Serevent, Formoterol

See Also
1. Short-acting Beta Agonist
2. Beta Agonist
Indications
1. Moderate Persistent Asthma
2. Severe Persistent Asthma
Precautions
1. Risk of increased mortality and of more severe and life threatening Asthma Exacerbations are FDA Black Box Warnings
2. 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 285:2583-93
3. Do NOT exceed dosing schedule (e.g. Serevent bid)
  1. Use a short acting Beta agonist for rescue use
4. Tolerance over time to Protective effect
  1. Effect diminishes over one month of use
  2. Reference
    1. Simons (1997) Pediatrics 99:655-9
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
4. Indacaterol (Arcapta)
  1. Once daily dosing
  2. FDA approved for COPD (not proven to prevent COPD exacerbations)
  3. Same cardiovascular risks as other long acting beta agonists
  4. Reference
    1. (2012) presc lett 19(1): 2
References
1. (2001) Med Clin North Am 43(1104):39-40
2. Wilson (2001) Chest 119:2021-6

Medication Costs
Serevent Diskus (on 2/9/2012 at DrugStore.com)
Serevent Diskus 60 50mcg/dose Powder Inhaler	#1 for $180.99	($180.99/unit)
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

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)
MSH	C012629
SnomedCT	386171009, 320260000, 414289007, 395969001
English	N-(2-hydroxy-5-(1-hydroxy-2-((2-(4-methoxyphenyl)-1-methylethyl)amino)ethyl)phenyl)formamide, (E)-2-butenedioate (2:1) (salt), eformoterol, formoterol [Chemical/Ingredient], Formoterol (product), Formoterol, Eformoterol (substance), Eformoterol, Formoterol (substance), Eformoterol (product), formoterol, FORMOTEROL
Spanish	eformoterol, eformoterol (producto), eformoterol (sustancia), formoterol (producto), formoterol, formoterol (sustancia)
Sources	Derived from the NIH UMLS (Unified Medical Language System)

salmeterol (C0073992)
Definition (NCI)	A highly selective, long-acting beta-2 adrenergic agonist with bronchodilatory activity. Salmeterol's benzene moiety resembles the structure of catecholamines, and occupies the active site of beta-2 adrenergic receptor, while the long, lipophilic side chain of salmeterol, binds to the so called 'exosite' near the beta-2 adrenergic 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)
MSH	C057823
SnomedCT	108605008, 372515005
English	salmeterol, SALMETEROL, salmeterol (medication), salmeterol [Chemical/Ingredient], Salmeterol, Salmeterol product, Salmeterol (product), Salmeterol (substance)
Spanish	salmeterol (producto), salmeterol (sustancia), salmeterol
Sources	Derived from the NIH UMLS (Unified Medical Language System)

Selective beta-2 adrenoceptor stimulants (C0354671)
Concepts	Pharmacologic Substance (T121)
SnomedCT	320073005, 373215002
English	Selective beta-2 stimulants, Selective beta-2 adrenoceptor stimulants, Selective beta-2 agonists, Selective beta-2 adrenoceptor stimulants (product), Selective beta-2 adrenoceptor stimulants (substance)
Spanish	estimulantes selectivos de receptores adrenérgicos beta 2 (sustancia), estimulantes selectivos de receptores adrenérgicos beta 2, estimulantes selectivos beta 2 adrenérgicos (producto), estimulantes selectivos beta 2 adrenérgicos (sustancia), estimulantes selectivos beta 2 adrenérgicos
Sources	Derived from the NIH UMLS (Unified Medical Language System)

Serevent (C0700491)
Concepts	Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH	C057823
English	Serevent, Glaxo Wellcome brand of salmeterol xinafoate, serevent
Sources	Derived from the NIH UMLS (Unified Medical Language System)