同: long-acting β-agonists

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/05/28 22:11:06」(JST)

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Long-acting beta-adrenoceptor agonists (LABAs, more specifically β₂-agonists) are usually prescribed for moderate to severe persistent asthma patients or patients with chronic obstructive pulmonary disease (COPD). They are designed to reduce the need for shorter-acting β₂-agonists such as salbutamol, as they have a duration of action of approximately 12 hours in comparison with the 4- to 6-hour duration of salbutamol, making them candidates for sparing high doses of corticosteroids^{[citation needed]} or treating nocturnal asthma and providing symptomatic improvement in patients with COPD. With the exception of formoterol, long-acting β₂-agonists are not recommended for the treatment of acute asthma exacerbations because of their slower onset of action compared to salbutamol. Their long duration of action is due to the addition of a long, lipophilic side-chain that binds to an exosite on adrenergic receptors. This allows the active portion of the molecule to continuously bind and unbind at β₂ receptors in the smooth muscle in the lungs.

Medical uses

When combined with inhaled steroids, beta-adrenoceptor agonists can improve symptoms.^[1]^[2] In children this benefit is uncertain and they may be potentially harmful.^[2]^[3] They should not be used without an accompanying steroid due to an increased risk of severe symptoms, including exacerbation in both children and adults.^[4]^[5]^[6]^[7] At least with formoterol, an increased risk appears to be present even when steroids are used^[8] and this risk has not been ruled out for salmeterol.^[9]

Agents

Some currently available long-acting beta-adrenoceptor agonists are:

Salmeterol
Formoterol
Bambuterol

Two ultra-long-acting beta-adrenoceptor agonists that have a duration of action of 24 hours, allowing for once-daily dosing^[10] are now approved.

Indacaterol (approved by the European Medicines Agency (EMA) under the trade name Onbrez on November 30, 2009,^[11] and by the United States Food and Drug Administration (FDA) under the trade name Arcapta Neohaler, on July 1, 2011^[12])
Olodaterol (approved in some European countries and by the United States Food and Drug Administration (FDA) on July 31, 2014 under Striverdi^[13])
Vilanterol (combination of the synthetic inhaled corticosteroid fluticasone furoate (FF) and the long-acting beta2-adrenergic agonist vilanterol trifenatate was approved by US Food and Drug Administration (FDA) in May 2013 as once-daily inhaled therapy for the treatment of chronic obstructive pulmonary disease (COPD). The product is called Breo Ellipta in the United States and Relvar Ellipta in Europe.^[14]
Carmoterol (Under Development)^[15]
LAS100977 (Under Development)^[15]
PF-610355 (Under Development)^[15]
Salmefamol (Salbutamol + PMA hybrid).

Concerns

While the use of inhaled LABAs are still recommended in asthma guidelines for the resulting improved symptom control,^[16] further concerns have been raised, by a large meta-analysis of the pooled results from 19 trials with 33,826 participants, that salmeterol may increase the small risks of asthma deaths, and this additional risk is not reduced with the additional use of inhaled steroids (e.g., as with the combination product Fluticasone/salmeterol).^[17] This seems to occur because although LABAs relieve asthma symptoms, they also promote bronchial inflammation and sensitivity without warning.^[18]

References

^ Higashi, AS; Zhu S; Stafford RS; Alexander GC (2011). "National trends in outpatient asthma treatment, 1997-2009.". Journal of General Internal Medicine 26 (12): 1465–70. doi:10.1007/s11606-011-1796-4. PMID 21769507.
^ ^a ^b Ducharme, FM; Ni Chroinin, M; Greenstone, I; Lasserson, TJ (May 12, 2010). "Addition of long-acting beta2-agonists to inhaled corticosteroids versus same dose inhaled corticosteroids for chronic asthma in adults and children.". Cochrane database of systematic reviews (Online) (5): CD005535. doi:10.1002/14651858.CD005535.pub2. PMID 20464739.
^ Ducharme, FM; Ni Chroinin, M; Greenstone, I; Lasserson, TJ (Apr 14, 2010). "Addition of long-acting beta2-agonists to inhaled steroids versus higher dose inhaled steroids in adults and children with persistent asthma.". Cochrane database of systematic reviews (Online) (4): CD005533. doi:10.1002/14651858.CD005533.pub2. PMID 20393943.
^ Fanta CH (March 2009). "Asthma". New England Journal of Medicine 360 (10): 1002–14. doi:10.1056/NEJMra0804579. PMID 19264689.
^ Cates CJ, Lasserson TJ, Jaeschke R (2009). Cates, Christopher J, ed. "Regular treatment with salmeterol and inhaled steroids for chronic asthma: serious adverse events". Cochrane Database Syst Rev (3): CD006922. doi:10.1002/14651858.CD006922.pub2. PMID 19588410.
^ Cates CJ, Cates MJ (2008). Cates, Christopher J, ed. "Regular treatment with salmeterol for chronic asthma: serious adverse events". Cochrane Database Syst Rev (3): CD006363. doi:10.1002/14651858.CD006363.pub2. PMID 18646149.
^ "FDA Drug Safety Communication: New safety requirements for long-acting inhaled asthma medications called Long-Acting Beta-Agonists (LABAs)". FDA. Feb 2010. Based on the available information, FDA concludes there is an increased risk for severe exacerbation of asthma symptoms, leading to hospitalizations in pediatric and adult patients as well as death in some patients using LABAs for the treatment of asthma. The agency is requiring the REMS and class-labeling changes to improve the safe use of these products.
^ Cates, CJ; Cates, MJ (Apr 18, 2012). "Regular treatment with formoterol for chronic asthma: serious adverse events.". Cochrane database of systematic reviews (Online) 4: CD006923. doi:10.1002/14651858.CD006923.pub3. PMID 22513944.
^ Cates, CJ; Cates, MJ (Jul 16, 2008). "Regular treatment with salmeterol for chronic asthma: serious adverse events.". Cochrane database of systematic reviews (Online) (3): CD006363. doi:10.1002/14651858.CD006363.pub2. PMID 18646149.
^ Cazzola M, Matera MG, Lötvall J (July 2005). "Ultra long-acting beta 2-agonists in development for asthma and chronic obstructive pulmonary disease". Expert Opin Investig Drugs 14 (7): 775–83. doi:10.1517/13543784.14.7.775. PMID 16022567.
^ European Public Assessment Report for Onbrez Breezhaler
^ "FDA approves Arcapta Neohaler to treat chronic obstructive pulmonary disease" (Press release). U.S. Food and Drug Administration. 2011-07-01. Retrieved 2011-07-02. [1]
^ "New once-daily Striverdi (olodaterol) Respimat gains approval in first EU countries". Boehringer-Ingelheim. 18 October 2013.
^ Osterweil, Neil (10 May 2013). "FDA Approves 'Son of Advair' for COPD Exacerbations". Medscape. Retrieved 17 April 2014.
^ ^a ^b ^c Cazzola, Mario; Luigino Calzetta; Maria Gabriella Matera3 (May 2011). "β2-adrenoceptor agonists: current and future direction". Br J Pharmacol. 163 (1): 4–17. doi:10.1111/j.1476-5381.2011.01216.x. PMC 3085864. PMID 21232045. Retrieved 17 April 2014.
^ British Thoracic Society & Scottish Intercollegiate Guidelines Network (SIGN). British Guideline on the Management of Asthma. Guideline No. 63. Edinburgh:SIGN; 2004. (HTML, Full PDF, Summary PDF)
^ Salpeter S, Buckley N, Ormiston T, Salpeter E (2006). "Meta-analysis: effect of long-acting beta-agonists on severe asthma exacerbations and asthma-related deaths". Ann Intern Med 144 (12): 904–12. doi:10.7326/0003-4819-144-12-200606200-00126. PMID 16754916.
^ Krishna Ramanujan (June 9, 2006). "Common asthma inhalers cause up to 80 percent of asthma-related deaths, Cornell and Stanford researchers assert". ChronicalOnline - Cornell University.

In 2011, the FDA issued a safety alert for Long-Acting Beta-Agonists (LABAs):

http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm201003.htm

UpToDate Contents

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1. 喘息のマネージメントの概要 an overview of asthma management
2. 喘息におけるβ刺激剤：長期使用に関する議論 beta agonists in asthma controversy regarding chronic use
3. 安定した慢性閉塞性肺疾患（COPD）のマネージメント management of stable chronic obstructive pulmonary disease
4. 思春期および成人における中等度持続型喘息の治療 treatment of moderate persistent asthma in adolescents and adults
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English Journal

Glycopyrronium once-daily significantly improves lung function and health status when combined with salmeterol/fluticasone in patients with COPD: the GLISTEN study-a randomised controlled trial.

Frith PA1, Thompson PJ2, Ratnavadivel R3, Chang CL4, Bremner P5, Day P6, Frenzel C7, Kurstjens N7; Glisten Study Group.
Thorax.Thorax.2015 Jun;70(6):519-27. doi: 10.1136/thoraxjnl-2014-206670. Epub 2015 Apr 3.
BACKGROUND: The optimal use of various therapeutic combinations for moderate/severe chronic obstructive pulmonary disease (COPD) is unclear. The GLISTEN trial compared the efficacy of two long-acting anti-muscarinic antagonists (LAMA), when combined with an inhaled corticosteroid (ICS) and a long-ac
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Prescribing of long-acting beta-2-agonists/inhaled corticosteroids after the SMART trial.

Rottenkolber M1, Fischer R2, Ibáñez L3,4, Fortuny J5, Reynolds R6, Amelio J7, Gerlach R8, Tauscher M9, Thürmann P10,11, Hasford J12, Schmiedl S13,14.
BMC pulmonary medicine.BMC Pulm Med.2015 May 6;15(1):55. doi: 10.1186/s12890-015-0051-x.
BACKGROUND: After the SMART trial evaluating the safety of salmeterol (long-acting beta-2-agonist (LABA)) in asthma patients, regulatory actions were taken to promote a guideline-adherent prescribing of LABA only to patients receiving inhaled corticosteroids (ICS). We aim to analyse LABA- and ICS-re
PMID 25943421

Patients' and Providers' Perspectives of a Polypill Strategy to Improve Cardiovascular Prevention in Australian Primary Health Care: A Qualitative Study Set Within a Pragmatic Randomized, Controlled Trial.

Liu H1, Massi L2, Laba TL2, Peiris D2, Usherwood T2, Patel A2, Cass A2, Eades AM2, Redfern J2, Hayman N2, Howard K2, Brien JA2, Jan S2.
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BACKGROUND: This study explores health provider and patient attitudes toward the use of a cardiovascular polypill as a health service strategy to improve cardiovascular prevention.METHODS AND RESULTS: In-depth, semistructured interviews (n=94) were conducted with health providers and patients from A
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Japanese Journal

気管支喘息治療薬 (特集これだけあれば大丈夫! Common diseaseのエッセンシャルドラッグ)

Gノート 3(1), 27-33, 2016-02
NAID 40020740301

従来治療でコントロール不十分な喘息患者におけるアドエアからフルティフォームへの切り替え効果 : 4試験のPooled解析

アレルギー・免疫 23(1), 110-118, 2016-01
NAID 40020687175

ブリーズヘラーの特性 (特集 LAMA/LABA配合剤ウルティブロによる新たなCOPD治療戦略)

吸入療法 8(1), 43-48, 2016
NAID 40020721456

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リンク元	「短時間作用型β2刺激薬」「長時間作用型β2刺激薬」
関連記事	「LA」「LABAs」

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英: short-acting β-agonists, SABA
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小発作から大発作の救急対応で反復吸入するkey drug
20-30分おきにネブライザーで吸入。脈拍が130/分以下を保つようにする。

「長時間作用型β2刺激薬」

　　[★]

英: short-acting β-agonists LABA
関: 短時間作用型β2刺激薬 SABA