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salmeterol (Serevent, Serevent Diskus)

Tradename: Serevent. (salmeterol xinafoate) Indications: 1) prevention of bronchospasm in patients with COPD 2) patients with nocturnal asthma who require regular treatment with inhaled, short-acting beta-2 adrenergic agonists 3) prevention of exercise-induced asthma 4) for use in conjunction with inhaled corticosteroid [4,5,7,10]; NOT for use as monotherapy Contraindications: - not for use in treating asthma without an inhaled glucocorticoid [12] Dosage: 1) 2 puffs (42 ug) BID (12 hours apart) 2) 2 puffs 30-60 minutes prior to exercise dry powder inhaler: - 21 ug/actuation ], 60 inhalations (6.5 g), 120 inhalations (13 g) Storage: Serevent good for 6 weeks after opening Pharmacokinetics: 1) onset of action: 10-20 minutes 2) peak effect: 2-4 hours 3) prolonged duration of action: 10-12 hours 4) metabolized by CYP3A4 [14] Adverse effects: 1) common (> 10%) - headache, pharyngitis 2) less common (1-10%) - tachycardia, palpitations, elevation or depression in blood pressure, cardiac arrhythmias, nervousness, CNS stimulation, hyperactivity, insomnia, malaise, dizziness, GI upset, diarrhea, nausea, tremors*, myalgias, back pain, arthralgia, upper respiratory tract infection, cough, bronchitis 3) uncommon (< 1%) - immediate hypersensitivity reactions (rash, urticaria, bronchospasm) 4) other - similar to other beta-adrenergic receptor agonists - tachyphylaxis is uncommon with salmeterol - cardiovascular effects are not common when used at the recommended doses - increases risk of life-threatening asthma exacerbations in some patients [6,8,9] {severe asthma, NOT on inhaled glucocorticoid} * tremors may be more common in the elderly ;;;********|**********|**********|**********|**********|*********|**********|********* Drug interactions: 1) similar to other beta-adrenergic receptor agonists 2) MAO inhibitors 3) tricyclic antidepressants (TCA) 4) drugs that inhibit CYP3A4 can increase salmeterol levels, clarithromycin, itraconazole, ritonavir ... [14] Mechanism of action: 1) selective beta-2 adrenergic agonist - 50 X more beta-2 selective than albuterol 2) lipophilic agents, thus depot effect in tissues occurs 3) inhibits release of proinflammatory & spasmogenic mediators from respiratory cells - inhibits histamine release for up to 20 hours 4) effective in preventing: a) exercise-induced asthma b) methacholine-induced bronchospasm c) response to allergen challenge

Interactions

drug interactions drug adverse effects (more general classes)

General

antiasthmatic agent inhaled beta-2 adrenergic receptor agonist

Properties

AGONIST-FOR: beta-2 adrenergic receptor MISC-INFO: elimination route LIVER pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 741
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Murray et al, Allergy Asthma Proc 20:173, 1999
  5. Kelson et al, J Asthma 36:703, 1999
  6. Prescriber's Letter 10(2):8-9 2003
  7. Journal Watch 23(24):192, 2003 Bjermer L et al, BMJ 327:891, 2003 PMID: 14563743 http://bmj.bmjjournals.com/cgi/content/full/327/7420/891
  8. Prescriber's Letter 12(9): 2005 The Safety of Long-Acting Beta-2 Agonists in Patients with Asthma Detail-Document#: 210907 (subscription needed) http://www.prescribersletter.com - US Department of Health and Human Services. National Institutes of Health. National Heart, Lung and Blood Institute. Expert Panel Report: Guidelines for the Diagnosis and Management of Asthma-Update on selected topics 2002.
  9. FDA Medwatch http://www.fda.gov/medwatch/safety/2005/safety05.htm#LABA
  10. Nelson HS et al, The salmeterol multicenter asthma research trial: A comparison of usual pharmacotherapy for asthma or usual pharmacotherapy plus salmeterol Chest 2006, 129:15 PMID: 16424409
  11. Bateman E et al, Effects of adding salmeterol in inhaled corticosteroids on serious asthma-related events. Ann Intern Med 2008, June 3 PMID: 18523132 - Weiss KB Drug safety and salmeterol: The controversy continues. Ann Intern Med 2008, June 3 PMID: 18523132
  12. FDA advisory panel meeting Joint Meeting of the Pulmonary-Allergy Drugs Advisory Committee, Drug Safety & Risk Management Advisory Committee, and the Pediatric Advisory Committee December 10 & 11, 2008 http://www.fda.gov/ohrms/dockets/ac/08/briefing/2008-4398b1-00-index.htm
  13. Prescriber's Letter 16(9): 2009 COMMENTARY: Shortened Expiration Dating of Some Inhalation Products PATIENT HANDOUT: Tips for Correct Use of Inhalers Detail-Document#: 250903 (subscription needed) http://www.prescribersletter.com
  14. Prescriber's Letter 17(7): 2010 Clarithromycin Interaction with Salmeterol and Inhaled Corticosteroids Detail-Document#: 260703 (subscription needed) http://www.prescribersletter.com

Component-of

fluticasone/salmeterol (Advair/Seretide Diskus, Wixela, AirDuo Respiclick)