beta-2 agonist

• β2刺激薬、β2アゴニスト

関

beta2 agonist

WordNet

1. to remain unmolested, undisturbed, or uninterrupted -- used only in infinitive form; "let her be"
2. work in a specific place, with a specific subject, or in a specific function; "He is a herpetologist"; "She is our resident philosopher" (同)follow
3. have life, be alive; "Our great leader is no more"; "My grandfather lived until the end of war" (同)live
4. be identical to; be someone or something; "The president of the company is John Smith"; "This is my house"
5. happen, occur, take place; "I lost my wallet; this was during the visit to my parents house"; "There were two hundred people at his funeral"; "There was a lot of noise in the kitchen"
6. have the quality of being; (copula, used with an adjective or a predicate noun); "John is rich"; "This is not a good answer"
7. occupy a certain position or area; be somewhere; "Where is my umbrella?" "The toolshed is in the back"; "What is behind this behavior?"
8. spend or use time; "I may be an hour"
9. stake on the outcome of an issue; "I bet $100 on that new horse"; "She played all her money on the dark horse" (同)wager, play
10. the act of gambling; "he did it on a bet" (同)wager
11. maintain with or as if with a bet; "I bet she will be there!" (同)wager
12. second in order of importance; "the candidate, considered a beta male, was perceived to be unable to lead his party to victory"
13. the 2nd letter of the Greek alphabet
14. preliminary or testing stage of a software or hardware product; "a beta version"; "beta software"
15. (biochemistry) a drug that can combine with a receptor on a cell to produce a physiological reaction
16. a muscle that contracts while another relaxes; "when bending the elbow the biceps are the agonist"
17. someone involved in a contest or battle (as in an agon)
18. beets (同)genus Beta

PrepTutorEJDIC

1. 《連結語として補語を伴なって…『である』,…だ,…です / 《位置・場所を表す語句を伴って》(…に)『ある』,いる(occupy a place or situation) / 〈物事が〉『存在する』,ある(exist);〈生物が〉生存する,生きている(live) / 行われる,起こる,発生する(take place, occur) / 存続する,そのままでいる(remain as before) / 《『be to』 do》 / …する予定である,…することになっている / …すべきだ / 《受動態の不定詞を伴って》…できる / 《命令》…するのだ / 《条件節に》…する意図がある / 《『if…were to』 do》…するとしたなら / 《『be』 do『ing』》《進行形》 / 《進行中の動作》…している,しつつある / 《近い未来》…しようとしている,するつもり / 《動作の反復》(いつも)…している / 《『be』+『他動詞の過去分詞』》《受動態》…される,されている / 《『be』+『自動詞の過去分詞』》《完了形》…した[状態にある]
2. 『かけ』・(…との)かけ《+『with』+『名』》 / かけた物(金) / かけの対象 / 〈金・物〉'を'『かける』 / (かけ事・ゲームなどで)〈人〉‘と'『かけをする』《+『名』〈人〉+『on』+『名』》 / (…に)『かける』《+『on』(『against』)+『名』(one's do『ing』)》
3. ベータ(ギリシア語アルファベットの第2文字;B,β;英語のB,b に遭当)

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/06/30 15:20:32」(JST)

wiki en

[Wiki en表示]

β₂-adrenergic agonists, also known as β₂-adrenergic receptor agonists, are a class of drugs that act on the beta₂-adrenergic receptor, thereby causing smooth muscle relaxation, resulting in dilation of bronchial passages, vasodilation in muscle and liver, relaxation of uterine muscle, and release of insulin.

They are primarily used to treat asthma and other pulmonary disorders.

Mechanism of action

Activation of beta-adrenergic receptors leads to relaxation of smooth muscle in the lung, and dilation and opening of the airways.

Beta-adrenergic receptors are coupled to a stimulatory G protein of adenylyl cyclase. This enzyme produces the second messenger cyclic adenosine monophosphate (cAMP). In the lung, cAMP decreases calcium concentrations within cells and activates protein kinase A. Both of these changes inactivate myosin light chain kinase and activate myosin light chain phosphatase. In addition, beta-2 agonists open large conductance calcium-activated potassium channels and thereby tend to hyperpolarize airway smooth muscle cells. The combination of decreased intracellular calcium, increased membrane potassium conductance, and decreased myosin light chain kinase activity leads to smooth muscle relaxation and bronchodilation.

Adverse effects

Findings indicate that Beta-2 stimulants, especially in parenteral administration such as inhalation or injection, can induce adverse effects:

• tachycardia secondary to peripheral vasodilation and cardiac stimulation; tachycardia can be accompanied by palpitations.
• tremor, sweats, agitation.
• more severe effects, pulmonary edema, myocardial ischemia, cardiac arrhythmia, are exceptional.

Asthma aggravation has been observed in patients using large dose of beta-2 stimulants, but it is not known if it results from spontaneous course of the disease or adverse effect of the drugs. The excipients, in particular sulphite, could contribute to the adverse effects. The possible loss of the bronchodilator activity of beta-2-mimetic could be attenuated by glucocorticoid intake.

Side effects

Side-effects such as insomnia, anxiety, increased heart rate, and tremor occur in some patients.

Delivery

All β₂ agonists are available in inhaler form, either metered-dose inhalers, which aerosolize the drug, or dry powder, which can be inhaled.

Salbutamol (known as albuterol in the U.S.) also comes in a solution form for nebulization, which is more commonly used in inhalers than in emergency rooms. Salbutamol and terbutaline are also both available in oral forms. Nebulizer form is as effective as administering the drug intravenously.

In addition, several of these medications are available in intravenous forms, including both salbutamol and terbutaline. It can be used in this form in severe cases of asthma, but it is more commonly used to suppress premature labor because it also relaxes uterine muscle, thereby inhibiting contractions.

Risks

On November 18, 2005, Food and Drug Administration (FDA) alerted healthcare professionals and patients that several long-acting bronchodilator medicines have been associated with possible increased risk of worsening wheezing in some people, and requested that manufacturers update warnings in their existing product labeling.

On June 29, 2006, Cornell University and Stanford University researchers reported that a meta-analysis they conducted found that "regularly inhaled beta-agonists (Orciprenaline/metaproterenol [Alupent], formoterol Foradil, fluticasone/salmeterol [Serevent, Advair], and salbutamol/albuterol [Proventil, Ventolin, Volmax, and others]) increased the risk of respiratory death more than twofold, compared with a placebo," while used to treat chronic obstructive pulmonary disease (COPD).

On December 11, 2008, a panel of experts convened by the Food and Drug Administration (FDA) voted to ban the drugs Serevent and Foradil from use in the treatment of asthma. It was shown that, when these two drugs are used without steroids, they increase the risks of more severe attacks. The experts said that two other much more popular asthma drugs containing long-acting beta-agonists, Advair and Symbicort, should continue to be used. The latter contains formoterol as contained in Foradil but also a steroid budesonide.

Types

They can be divided into short-acting (SABA) and long-acting beta-adrenoceptor agonist (LABA) groups:

Short-acting beta₂ agonists

generic name (Trade Name)

• salbutamol (albuterol (US name), Ventolin)
• levosalbutamol (levalbuterol (US name), Xopenex)
• terbutaline (Bricanyl)
• pirbuterol (Maxair)
• procaterol
• clenbuterol
• metaproterenol (Alupent)
• fenoterol
• bitolterol mesylate
• ritodrine
• isoprenaline

Long-acting beta₂ agonists

• salmeterol (Serevent Diskus)
• formoterol (Foradil, Symbicort)
• bambuterol
• clenbuterol

Ultra-long-acting beta₂ agonists

• indacaterol

References

External links

• beta-Adrenergic Receptor Agonists at the US National Library of Medicine Medical Subject Headings (MeSH)

UpToDate Contents

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• 1. 喘息におけるβ刺激剤：急性期投与および予防的使用 beta agonists in asthma acute administration and prophylactic use
• 2. 成人における喘息の急性増悪の治療 treatment of acute exacerbations of asthma in adults
• 3. 小児における高カリウム血症のマネージメント management of hyperkalemia in children
• 4. 成人における吸入剤の到達 delivery of inhaled medication in adults
• 5. 小児における喘息の急性増悪：救急外来によるマネージメント acute asthma exacerbations in children emergency department management

English Journal

• Formulation of a Novel Fixed Dose Combination of Salmeterol Xinafoate and Mometasone Furoate for Inhaled Drug Delivery.

• Liu S1, Watts AB2, Du J3, Bui A3, Hengsawas S3, Williams RO 3rd4.
• European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.Eur J Pharm Biopharm.2015 Jul 25. pii: S0939-6411(15)00317-3. doi: 10.1016/j.ejpb.2015.07.017. [Epub ahead of print]
• Co-administration of an inhaled corticosteroid and long acting beta agonist forchronic obstructive pulmonary disease has reduced mortality compared to either drug alone. This combination reduces exacerbations, hospitalization, emergency department visits and health care costs. A novel fixed-dose com
• PMID 26220015

• Inhaled Formoterol Diminishes Insulin-Induced Hypoglycemia in Type 1 Diabetes.

• Belfort-DeAguiar RD1, Naik S1, Hwang J1, Szepietowska B1, Sherwin RS2.
• Diabetes care.Diabetes Care.2015 Jul 7. pii: dc142472. [Epub ahead of print]
• OBJECTIVE: Hypoglycemia is one of the major factors limiting implementation of tight glycemic control in patients with type 1 diabetes and is associated with increased morbidity and mortality during intensive insulin treatment. β-2 Adrenergic receptor (AR) agonists have been reported to diminish no
• PMID 26153273

• Simple and sensitive monitoring of β2-agonist residues in meat by liquid chromatography-tandem mass spectrometry using a QuEChERS with preconcentration as the sample treatment.

• Xiong L1, Gao YQ2, Li WH2, Yang XL2, Shimo SP2.
• Meat science.Meat Sci.2015 Jul;105:96-107. doi: 10.1016/j.meatsci.2015.03.013. Epub 2015 Mar 20.
• A liquid chromatography with tandem mass spectrometric detection (LC-MS/MS) method was established for the simultaneous determination of the levels of 10 β2-agonists in meat. The samples were extracted using an aqueous acidic solution and cleaned up using a Quick, Easy, Cheap, Effective, Rugged and
• PMID 25828164

Japanese Journal

• On Prescription of Beta 2 Agonists for Pediatric Patients with Acute Bronchitis in Japan

• 神垣 有美,大森 崇,小田嶋 博,佐藤 俊哉
• 薬剤疫学 17(1), 1-12, 2012
• … Objective: In Japan, beta 2 agonist (BA) has an indication for acute bronchitis with airway obstruction. … Although BA prescription proportions in the asthma group decreased annually with the exception of 0-2 years old, those in the non-asthma group remain unchanged. …
• NAID 130003297452

• Protective Effects of Glycyrrhizin against .BETA.2-Adrenergic Receptor Agonist-Induced Receptor Internalization and Cell Apoptosis

• Shi Qian,Hou Yuanyuan,Yang Yang [他],Bai Gang
• Biological and Pharmaceutical Bulletin 34(5), 609-617, 2011
• … It has been reported that treatment with β2 adrenergic receptor (β2AR) agonist bronchodilators may result in airway β2ARs internalization and cardiac muscle cells apoptosis. … This could lead to the loss of pharmacological effect of β2AR agonists and increase adverse cardiovascular events in asthma patients receiving β2AR agonist therapy. …
• NAID 130000657769

• COPDの薬物療法--短時間作用性β2刺激薬の有効な使い方 (シンポジウム タバコによる肺病-COPDを診る--もうひとつのCommon Disease 第653回新潟医学会)

• 佐藤 英夫
• 新潟医学会雑誌 124(12), 665-667, 2010-12-00
• NAID 40018759194

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★リンクテーブル★

リンク元	「β2刺激薬」「β2アゴニスト」
関連記事	「beta」「be」

「β2刺激薬」

　　[★]

英

beta2 agonist、beta-2 agonist

関

β2作用薬、β2受容体刺激薬、β2アゴニスト

「β2アゴニスト」

　　[★]

英

beta2 agonist、beta-2 agonist

関

β2刺激薬、β2作用薬、β2受容体刺激薬

「beta」

　　[★]

β、ベータ 　 　 　 　

「be」

　　[★]