salmeterol (Serevent, Serevent Diskus)
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Introduction
Tradename: Serevent. (salmeterol xinafoate)
Indications
- prevention of bronchospasm in patients with COPD
- patients with noctural asthma who require regular treatment with inhaled, short-acting beta-2 adrenergic agonists
- prevention of exercise-induced asthma
- 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
dry powder inhaler:
- 21 ug/actuation ], 60 inhalations (6.5 g), 120 inhalations (13 g)
Storage
Serevent good for 6 weeks after opening
Pharmacokinetics
- onset of action: 10-20 minutes
- peak effect: 2-4 hours
- prolonged duration of action: 10-12 hours
- metabolized by CYP3A4[14]
elimination via liver
Adverse effects
- common (> 10%)
- 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
- uncommon (< 1%)
- immediate hypersensitivity reactions (rash, urticaria, bronchospasm)
- 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 adverse effects of adrenergic receptor agonists
- drug adverse effects of beta-adrenergic receptor agonists
- drug adverse effects of long-acting beta-adrenergic receptor agonists
- drug adverse effects of sympathomimetic(s)
Drug interactions
- similar to other beta-adrenergic receptor agonists
- MAO inhibitors
- tricyclic antidepressants (TCA)
- drugs that inhibit CYP3A4 can increase salmeterol levels, clarithromycin, itraconazole, ritonavir ...[14]
- drug interaction(s) of beta-2 adrenergic receptor agonists with beta adrenergic receptor antagonists
- drug interaction(s) of beta-2 adrenergic receptor agonists with loop diuretics
- drug interaction(s) of beta-2 adrenergic receptor agonists with thiazide diuretics
Mechanism of action
- selective beta-2 adrenergic agonist
- 50 X more beta-2 selective than albuterol
- lipophilic agents, thus depot effect in tissues occurs
- inhibits release of proinflammatory & spasmogenic mediators from respiratory cells
- inhibits histamine release for up to 20 hours
- effective in preventing:
- exercise-induced asthma
- methacholine-induced bronchospasm
- response to allergen challenge
More general terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 741
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 4.0 4.1 Murray et al, Allergy Asthma Proc 20:173, 1999
- ↑ 5.0 5.1 Kelson et al, J Asthma 36:703, 1999
- ↑ 6.0 6.1 Prescriber's Letter 10(2):8-9 2003
- ↑ 7.0 7.1 Journal Watch 23(24):192, 2003 Bjermer L et al, BMJ 327:891, 2003 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/14563743 <Internet> http://bmj.bmjjournals.com/cgi/content/full/327/7420/891
- ↑ 8.0 8.1 Prescriber's Letter 12(9): 2005 The Safety of Long-Acting Beta-2 Agonists in Patients with Asthma Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=210907&pb=PRL (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. - ↑ 9.0 9.1 FDA Medwatch http://www.fda.gov/medwatch/safety/2005/safety05.htm#LABA
- ↑ 10.0 10.1 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: https://www.ncbi.nlm.nih.gov/pubmed/16424409
- ↑ Bateman E et al, Effects of adding salmeterol in inhaled corticosteroids on serious asthma-related events. Ann Intern Med 2008, June 3 PMID: https://www.ncbi.nlm.nih.gov/pubmed/18523132
Weiss KB Drug safety and salmeterol: The controversy continues. Ann Intern Med 2008, June 3 PMID: https://www.ncbi.nlm.nih.gov/pubmed/18523132 - ↑ 12.0 12.1 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
- ↑ Prescriber's Letter 16(9): 2009 COMMENTARY: Shortened Expiration Dating of Some Inhalation Products PATIENT HANDOUT: Tips for Correct Use of Inhalers Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=250903&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 14.0 14.1 14.2 Prescriber's Letter 17(7): 2010 Clarithromycin Interaction with Salmeterol and Inhaled Corticosteroids Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260703&pb=PRL (subscription needed) http://www.prescribersletter.com