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Β受体阻滞剂：修订间差异

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我把Beta blockers做某種程度的選擇性翻譯，以避免內容冗長的缺點。然後用以取代前手文章內容過短的遺憾。敬請指教。
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{{Infobox drug class
{{Infobox drug class
| Name = β受体阻断药<br/>Beta blockers
| Name = Beta blockers
| Synonyms = beta-blockers、β-blockers、beta-adrenergic blocking agents、beta antagonists、beta-adrenergic antagonists、beta-adrenoreceptor antagonists、beta adrenergic receptor antagonists與BB
| Image = Propranolol-2D-skeletal.png
| Image = Propranolol.svg
| Alt = Propranolol
| Alt = Propranolol
| Use = [[高血压]]、[[心律不整]]等
| Use = [[高血壓]], [[心律不整]]等
| Caption = [[普萘洛尔]]的[[键线式]]结构，是第一种成功应用于临床的β受体阻断药
| Caption = [[普萘洛爾]]（全球首次合成具有臨床效果的β受體阻滯劑）的[[鍵線式|骨架式]]
| Biological_target = [[β受体]]
| Biological_target = β受體
| ATC_prefix = C07
| ATC_prefix = C07
| MeshID = D000319
| MeshID = D000319
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}}
}}


'''β受體阻滯劑'''（{{lang-en|Beta blockers}}），也拼寫為β-blockers），是一類主要用於控制[[心律不整]]，並於首次[[心臟病]]發作後用於保護心臟，免受再次發作侵害（[[預防醫學]]）的藥物。<ref name="pmid10381708">{{cite journal | vauthors = Freemantle N, Cleland J, Young P, Mason J, Harrison J | title = beta Blockade after myocardial infarction: systematic review and meta regression analysis | journal = BMJ | volume = 318 | issue = 7200 | pages = 1730–1737 | date = June 1999 | pmid = 10381708 | pmc = 31101 | doi = 10.1136/bmj.318.7200.1730 }}</ref>此藥物也廣泛用於治療[[高血壓]]，但已非大多數初次治療的首選藥物。<ref name="pmid24352797">{{cite journal | vauthors = James PA, Oparil S, Carter BL, Cushman WC, Dennison-Himmelfarb C, Handler J, Lackland DT, LeFevre ML, MacKenzie TD, Ogedegbe O, Smith SC, Svetkey LP, Taler SJ, Townsend RR, Wright JT, Narva AS, Ortiz E | display-authors = 6 | title = 2014 evidence-based guideline for the management of high blood pressure in adults: report from the panel members appointed to the Eighth Joint National Committee (JNC 8) | journal = JAMA | volume = 311 | issue = 5 | pages = 507–520 | date = February 2014 | pmid = 24352797 | doi = 10.1001/jama.2013.284427 | doi-access = free }}</ref>
'''β受体阻断药'''（{{lang-en|Beta blockers}}），又称'''Beta受体阻断药'''、'''β受体阻断剂'''、'''β受体阻滞剂'''、'''β受体拮抗剂'''或'''β阻断药、乙型阻斷劑'''，是一类用来治疗[[心律不整]]、防止[[心脏病]]发作后的二次心脏病发作（二级预防）和在某些情况下用来治疗[[高血压]]的[[药品|药物]]。<ref name="pmid10381708">{{cite journal | author = Freemantle N, Cleland J, Young P, Mason J, Harrison J | title = beta Blockade after myocardial infarction: systematic review and meta regression analysis | journal = BMJ | volume = 318 | issue = 7200 | pages = 1730–7 | date = June 1999 | pmid = 10381708 | pmc = 31101 | doi = 10.1136/bmj.318.7200.1730 }}</ref><ref name="pmid20692524">{{cite journal | author = Cruickshank JM | title = Beta blockers in hypertension | journal = Lancet | volume = 376 | issue = 9739 | pages = 415; author reply 415–6 | date = August 2010 | pmid = 20692524 | doi = 10.1016/S0140-6736(10)61217-2 }}</ref><ref name="UpToDateHypertension">{{cite journal | title=Choice of therapy in primary (essential) hypertension: Clinical trials | author=Kaplan, Norman M. | journal=UpToDate |date=October 2010 }}</ref>近期有相關證據顯示，此類阻滯劑可能具有協助癌症治療的潛能。<ref>{{Cite journal|title=β-Blocker use and reduced disease progression in patients with thick melanoma: 8 years of follow-up.|url=https://pubmed.ncbi.nlm.nih.gov/28346289/|last=De Giorgi|first=Vincenzoa|last2=Grazzini|first2=Martaa|date=June 2017|journal=Melanoma Research|doi=10.1097/CMR.000000000000031|volume=27|pages=268-270|last3=Benemei|first3=Silviab|last4=Marchionni|first4=Niccolòc|last5=Geppetti|first5=Pierangelob|last6=Gandini|first6=Sarad|access-date=2020-12-21|archive-date=2021-11-19|archive-url=https://web.archive.org/web/20211119011420/https://pubmed.ncbi.nlm.nih.gov/28346289/|dead-url=no}}</ref><ref>{{Cite journal|title=Improving survival rates in two models of spon- taneous postoperative metastasis in mice by combined administration of a β‐adrenergic antagonist and a cyclooxygenase‐2 inhibitor.|url=https://www.jimmunol.org/content/184/5/2449|last=Glasner|first=A|last2=Avraham|first2=R|date=March 2010|journal=Journal of Immunology|doi=10.4049/jimmunol.0903301|volume=184|pages=2449–2457|last3=Rosenne|first3=E|last4=Benish|first4=M|last5=Zmora|first5=O|last6=Shemer|first6=S|last7=Ben‐Eliyahu|first7=S|access-date=2020-12-21|archive-date=2021-11-19|archive-url=https://web.archive.org/web/20211119011518/https://www.jimmunol.org/content/184/5/2449|dead-url=no}}</ref><ref>{{Cite journal|title=β‐Blockers reduce breast cancer recurrence and breast cancer death: A meta‐analysis. Clinical Breast Cancer.|url=https://www.sciencedirect.com/science/article/pii/S1526820915001470?via%3Dihub|last=Childers|first= W. K.|last2=Hollenbeak|first2=C. S.|date=December 2015|journal=Clinical Breast Cancer|doi=10.1016/j.clbc.2015.07.001|volume=15|issue=6|pages=426-431|last3=Cheriyath|first3= P}}</ref>


此種藥物的給藥方式有[[口服給藥]]、[[靜脈注射]]及眼科製劑給藥。
β受体阻断药[[非竞争性]]阻断[[交感神经系统]]中内源性[[儿茶酚胺]][[肾上腺素]]和[[去甲肾上腺素]]的作用，尤其是肾上腺素能[[β受体]]。<ref name="urlCurrent Cardiovascular Drugs - Google Books">{{Cite book | url = http://books.google.com/?id=y3R1Vd3NHqcC&pg=PA152&dq=mode+of+action+of+beta+blockers#v=onepage&q=mode%20of%20action%20of%20beta%20blockers&f=false | title = Current Cardiovascular Drugs | author = Frishman W.H. | author2 = Cheng-Lai A | author3 = Nawarskas J | year = 2005 | publisher = Current Science Group | page = 152 | accessdate = 2010-09-07 | isbn = 978-1-57340-221-7 }}</ref><ref name="urlPharmacotherapeutics for advanced ... - Google Books">{{Cite book | url = http://books.google.com/?id=EaP1yJz4fkEC&pg=PA205&dq=beta+receptors+heart+kidneys#v=onepage&q=beta%20receptors%20heart%20kidneys&f=false | title = Pharmacotherapeutics for advanced practice: a practical approach | author = Arcangelo V.P. | author2 = Peterson A.M. | year = 2006 | publisher = Lippincott Williams & Wilkins | page = 205 | accessdate = 2010-09-07 | isbn = 978-0-7817-5784-3 }}</ref>有些药物阻断所有[[β-肾上腺素能受体]]，有些则为竞争性阻断。目前，市面上的藥物多以β受體中的β1及β2為目標，而針對β3的受體阻滯劑因藥理學特性仍無法良好掌握故持續處於研究階段。<ref>{{Cite journal|title=Everything You Always Wanted to Know about β3-AR * (* But Were Afraid to Ask)|url=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6523418/|last=Schena|first= G|last2=Caplan|first2=M. J.|date=Aprail 2019|journal=Cells|doi=10.3390/cells8040357|volume=8|issue=4|pages=357|last3=Benemei|first3=Silviab|last4=Marchionni|first4=Niccolòc|last5=Geppetti|first5=Pierangelob|last6=Gandini|first6=Sarad}}</ref>


β受體阻滯劑是種競爭性拮抗劑，可阻斷[[交感神經]]系統腎上腺素β受體中[[內源]]性[[兒茶酚胺]]的[[腎上腺素]]和[[正腎上腺素]]的受體位點，達到降低心率、血壓和其他"[[戰鬥或逃跑反應|戰鬥或逃跑]]"的相關反應。<ref name="Frishman_2005">{{Cite book | chapter = Beta-Adrenergic Blockers | chapter-url = https://books.google.com/books?id=y3R1Vd3NHqcC&q=mode+of+action+of+beta+blockers&pg=PA152 | title = Current Cardiovascular Drugs | veditors = Frishman WH, Cheng-Lai A, Nawarskas J | year = 2005 | publisher = Current Science Group | access-date = 2010-09-07 | isbn = 978-1-57340-221-7 }}</ref>{{rp|152}}<ref name="Barranger_2006">{{Cite book | vauthors = Barranger K, Vivian E, Peterson AM | chapter = Hypertension | chapter-url = https://books.google.com/books?id=EaP1yJz4fkEC&pg=PA205 | title = Pharmacotherapeutics for advanced practice: a practical approach | veditors = Arcangelo VP, Peterson AM | year = 2006 | publisher = Lippincott Williams & Wilkins | page = 205 | access-date = 2010-09-07 | isbn = 978-0-7817-5784-3 }}</ref>此類藥物中有些可阻斷所有類型β-腎上腺素受體的激活，另一些則對三種已知β-腎上腺受體（即β<sub>1</sub>、β<sub>2</sub> 和β<sub>3</sub>）之一具有選擇性。<ref name="Frishman_2005" />{{rp|153}}β<sub>1</sub>-腎上腺素受體主要位於[[心臟]]和[[腎]]臟。<ref name="Barranger_2006" />β<sub>2</sub>-的主要位於[[肺]]部、胃腸道、[[肝臟]]、[[子宮]]、[[血管平滑肌]]和[[骨骼肌]]。<ref name="Barranger_2006" />β<sub>3</sub>-的位於[[脂肪細胞]]。<ref name="pmid7609752">{{cite journal | vauthors = Clément K, Vaisse C, Manning BS, Basdevant A, Guy-Grand B, Ruiz J, Silver KD, Shuldiner AR, Froguel P, Strosberg AD | display-authors = 6 | title = Genetic variation in the beta 3-adrenergic receptor and an increased capacity to gain weight in patients with morbid obesity | journal = The New England Journal of Medicine | volume = 333 | issue = 6 | pages = 352–354 | date = August 1995 | pmid = 7609752 | doi = 10.1056/NEJM199508103330605 | doi-access = free }}</ref>
ESC/ESH指引指出對於合併心衰竭、心絞痛、心肌梗塞後或心房顫動的高血壓患者，以及育齡期或計畫懷孕的女性高血壓患者，可考慮在任何治療階段使用乙型阻斷劑。<ref>{{Cite journal|title=2018 ESC/ESH Guidelines for the management of arterial hypertensionThe Task Force for the management of arterial hypertension of the European Society of Cardiology (ESC) and the European Society of Hypertension (ESH)|url=https://academic.oup.com/eurheartj/article/39/33/3021/5079119|last=Williams|first=Bryan|last2=Mancia|first2=Giuseppe|date=2018-09-01|journal=European Heart Journal|issue=33|doi=10.1093/eurheartj/ehy339|volume=39|pages=3021–3104|language=en|issn=0195-668X|last3=Spiering|first3=Wilko|last4=Agabiti Rosei|first4=Enrico|last5=Azizi|first5=Michel|last6=Burnier|first6=Michel|last7=Clement|first7=Denis L.|last8=Coca|first8=Antonio|last9=de Simone|first9=Giovanni|access-date=2020-01-03|archive-date=2022-03-10|archive-url=https://web.archive.org/web/20220310103045/https://academic.oup.com/eurheartj/article/39/33/3021/5079119|dead-url=no}}</ref>


β受體所存在的組織是交感神經系統的一部分，會導致壓力反應，特別是當它們受到腎上腺素刺激後。 β受體阻滯劑可干擾腎上腺素和其他{{le|壓力激素|stress hormone}}受體的結合，將壓力激素作用降低。
最近有研究證明乙型阻斷劑carvedilol可以增強骨骼肌收縮力，但卻無法導致骨骼肌肥大; 該研究亦指出β2AR激動劑clenbuterol則可以增強骨骼肌收縮力和引起骨骼肌肥大的現象，而這些現象都是通過β-arrestin的信號傳遞所介導的。<ref>{{cite journal |last1=Kim |first1=Jihee |last2=Grotegut |first2=Chad A. |last3=Wisler |first3=James W. |last4=Mao |first4=Lan |last5=Rosenberg |first5=Paul B. |last6=Rockman |first6=Howard A. |last7=Lefkowitz |first7=Robert J. |title=The β-arrestin-biased β-adrenergic receptor blocker carvedilol enhances skeletal muscle contractility |journal=Proceedings of the National Academy of Sciences |date=2020-06-02 |volume=117 |issue=22 |pages=12435–12443 |doi=10.1073/pnas.1920310117}}</ref>


對於原發性高血壓的治療，於主要使用[[阿替洛爾]]（替代普萘洛爾作為治療高血壓的藥物）治療的[[統合分析]]顯示，雖然β受體阻滯劑在預防[[中風]]和整體心血管事件方面比[[安慰劑]]更有效，但不如[[利尿劑]]（抑制[[腎素-血管收縮素系統]]的藥物，例如[[血管紧张素转换酶抑制剂|ACE抑制劑]]或[[鈣通道阻滯劑]]）） 有效。<ref>{{cite journal | vauthors = Wiysonge CS, Bradley HA, Volmink J, Mayosi BM, Opie LH | title = Beta-blockers for hypertension | journal = The Cochrane Database of Systematic Reviews | volume = 1 | issue = 1 | pages = CD002003 | date = January 2017 | pmid = 28107561 | pmc = 5369873 | doi = 10.1002/14651858.CD002003.pub5 }}</ref><ref>{{Cite journal |last1=Reinhart |first1=Marcia |last2=Puil |first2=Lorri |last3=Salzwedel |first3=Douglas M. |last4=Wright |first4=James M. |date=2023-07-13 |title=First-line diuretics versus other classes of antihypertensive drugs for hypertension |journal=The Cochrane Database of Systematic Reviews |volume=2023 |issue=7 |pages=CD008161 |doi=10.1002/14651858.CD008161.pub3 |issn=1469-493X |pmc=10339786 |pmid=37439548|pmc-embargo-date=2023-07-13 }}</ref><ref>{{cite journal | vauthors = Zhu J, Chen N, Zhou M, Guo J, Zhu C, Zhou J, Ma M, He L | display-authors = 6 | title = Calcium channel blockers versus other classes of drugs for hypertension | journal = The Cochrane Database of Systematic Reviews | volume = 1 | issue = 1 | pages = CD003654 | date = January 2022 | pmid = 35000192 | pmc = 8742884 | doi = 10.1002/14651858.CD003654.pub6 }}</ref><ref>{{cite journal | vauthors = Wiysonge CS, Bradley HA, Volmink J, Mayosi BM, Opie LH | title = Beta-blockers for hypertension | journal = The Cochrane Database of Systematic Reviews | volume = 1 | issue = 1 | pages = CD002003 | date = January 2017 | pmid = 28107561 | pmc = 5369873 | doi = 10.1002/14651858.cd002003.pub5 }}</ref>
==例子==
[[Image:Dichloroisoprenaline.svg|thumb|{{le|二氯異丙腎上腺素|Dichloroisoprenaline}}，第一种β受体阻断药]]


==醫療用途==
* [[普萘洛尔]]（Propranolol）β1+β2
β受體阻滯劑用於治療與心臟和血管系統相關的各種疾病以及其他幾種醫學情況。 它已被廣泛用於治療常見的心臟相關疾病，包括[[心絞痛]]、[[急性冠狀動脈症候群]]、高血壓以及心律不整，也用於治療其他心臟疾病，例如{{le|肥厚性心肌病變|Hypertrophic cardiomyopathy|肥厚性阻塞心肌病變}}、[[二尖瓣狹窄]]或{{le|僧帽瓣脫垂|Mitral valve prolapse}}以及[[主動脈剝離]]。此外，β受體阻滯劑也可用於血管手術、焦慮、[[甲狀腺功能亢進症]]、[[青光眼]]、[[偏頭痛]]和{{le|食道靜脈曲張|Esophageal varices}}的治療。<ref name="Opie 2009 p.">{{cite book | vauthors = Opie LH | title=Drugs for the Heart | publisher=Saunders | publication-place=Philadelphia | date=2009 | isbn=978-1-4160-6158-8 | pages=6–18}}</ref>
* （Cardolol）β1+β2
* （Timolol）β1+β2


===心臟衰竭===
* [[毕索洛尔]]（Bisoprolol）β1
β受體阻滯劑因為會降低心肌收縮力，而有可能使病情惡化，曾在心臟衰竭案例中遭到禁用，但於20世紀90年代末所做的研究顯示它在降低發病率和死亡率方面具有功效。<ref name="pmid10714728">{{cite journal | vauthors = Hjalmarson A, Goldstein S, Fagerberg B, Wedel H, Waagstein F, Kjekshus J, Wikstrand J, El Allaf D, Vítovec J, Aldershvile J, Halinen M, Dietz R, Neuhaus KL, Jánosi A, Thorgeirsson G, Dunselman PH, Gullestad L, Kuch J, Herlitz J, Rickenbacher P, Ball S, Gottlieb S, Deedwania P | display-authors = 6 | title = Effects of controlled-release metoprolol on total mortality, hospitalizations, and well-being in patients with heart failure: the Metoprolol CR/XL Randomized Intervention Trial in congestive heart failure (MERIT-HF). MERIT-HF Study Group | journal = JAMA | volume = 283 | issue = 10 | pages = 1295–1302 | date = March 2000 | pmid = 10714728 | doi = 10.1001/jama.283.10.1295 | doi-access = free }}</ref><ref name="pmid11835035">{{cite journal | vauthors = Leizorovicz A, Lechat P, Cucherat M, Bugnard F | title = Bisoprolol for the treatment of chronic heart failure: a meta-analysis on individual data of two placebo-controlled studies—CIBIS and CIBIS II. Cardiac Insufficiency Bisoprolol Study | journal = American Heart Journal | volume = 143 | issue = 2 | pages = 301–307 | date = February 2002 | pmid = 11835035 | doi = 10.1067/mhj.2002.120768 }}</ref><ref name="pmid12390947">{{cite journal | vauthors = Packer M, Fowler MB, Roecker EB, Coats AJ, Katus HA, Krum H, Mohacsi P, Rouleau JL, Tendera M, Staiger C, Holcslaw TL, Amann-Zalan I, DeMets DL | display-authors = 6 | title = Effect of carvedilol on the morbidity of patients with severe chronic heart failure: results of the carvedilol prospective randomized cumulative survival (COPERNICUS) study | journal = Circulation | volume = 106 | issue = 17 | pages = 2194–2199 | date = October 2002 | pmid = 12390947 | doi = 10.1161/01.CIR.0000035653.72855.BF | doi-access = free }}</ref>[[比索洛爾]]、{{le|卡維地洛|Carvedilol}}和緩釋型[[美托洛爾]]被明確指定為心臟衰竭標準ACE抑制劑和利尿劑治療的輔助藥物，但其劑量通常遠低於用作其他疾病的治療。 β受體阻滯劑僅適用於代償性穩定心臟衰竭，在急性失代償性心臟衰竭的情況下，β受體阻滯劑會導致[[射血分數]]進一步降低，讓患者的症狀惡化。<ref>{{cite journal |last1=Philip J Podrid |first1=Philip J |last2= |first2= |date=2023-06-15 |title= Major side effects of beta blockers|url=https://www.uptodate.com/contents/major-side-effects-of-beta-blockers |journal= UpToDate|volume= |issue= |pages= |doi= |access-date=2024-03-22}}</ref>
* [[美托洛尔]]（Metoprolol）β1
* [[阿替洛尔]]（Atenolol）β1
*（Betaxolol）β1


β受體阻滯劑主要因其對心率的降低作用而聞名，但這並非用於治療心臟衰竭的唯一重要機制。<ref>{{Cite journal | vauthors = Fletcher P |title=Beta blockers in heart failure |journal=Australian Prescriber |year=2000 |volume=23 |issue=6 |pages=120–123 |url=https://www.nps.org.au/australian-prescriber/articles/beta-blockers-in-heart-failure |language=en |doi=10.18773/austprescr.2000.138|doi-access=free }}</ref>β受體阻滯劑除在心臟中的交感神經β<sub>1</sub>活性外，還會影響腎臟中的腎素-血管收縮素系統，它會導致腎素分泌減少，進而降低細胞外容量和增加血液的攜氧能力來減少心臟的需氧量。心臟衰竭的特徵在於心臟上兒茶酚胺活性增加，會導致多種有害影響，包括需氧量增加、發炎介質傳播和異常心臟組織重塑，所有這些都會降低心臟收縮效率並導致射血分數降低。<ref>{{cite web|title = Use of beta-blockers and ivabradine in heart failure with reduced ejection fraction|url = http://www.uptodate.com/contents/use-of-beta-blockers-and-ivabradine-in-heart-failure-with-reduced-ejection-fraction|website = www.uptodate.com|access-date = 2015-12-11|url-status = live|archive-url = https://web.archive.org/web/20151222081646/http://www.uptodate.com/contents/use-of-beta-blockers-and-ivabradine-in-heart-failure-with-reduced-ejection-fraction|archive-date = 2015-12-22|df = mdy-all}}</ref>
*（Carvedilol） mixed α+ β
* (Labetalol)針劑劑型，同時阻斷 α和 β


試驗結果顯示β受體阻滯劑在13個月的期間內可將絕對死亡風險降低4.5%。除降低死亡風險外，連就診和住院的次數也可減少。<ref name="pmid12173717">{{cite journal | vauthors = Pritchett AM, Redfield MM | title = Beta-blockers: new standard therapy for heart failure | journal = Mayo Clinic Proceedings | volume = 77 | issue = 8 | pages = 839–845; quiz 845–46 | date = August 2002 | pmid = 12173717 | doi = 10.4065/77.8.839 | doi-access = free }}</ref>一份於2020年發表的[[考科藍合作組織]]綜述提出支持使用β受體阻滯劑以治療兒童心臟衰竭的證據極少，但從已有數據中確實指出它們可能有益。<ref>{{cite journal | vauthors = Alabed S, Sabouni A, Al Dakhoul S, Bdaiwi Y | title = Beta-blockers for congestive heart failure in children | journal = The Cochrane Database of Systematic Reviews | volume = 2020 | issue = 7 | pages = CD007037 | date = July 2020 | pmid = 32700759 | pmc = 7389334 | doi = 10.1002/14651858.CD007037.pub4 | collaboration = Cochrane Heart Group }}</ref>
==引用==
{{reflist}}


治療心臟衰竭的β受體阻滯劑應從極低劑量（目標劑量的1/8）開始，然後逐漸增加。患者心臟必須適應較少兒茶酚胺刺激帶來的變化，並找到新的運作平衡點。<ref>{{Cite book|title=Goodman & Gilman's: The Pharmacological Basic of Therapeutics|publisher=McGraw-Hill|year=2018|isbn=9781259584732}}</ref>


====急性心肌梗塞====
{{主要药物分类}}
β受體阻滯劑適用於治療急性[[心肌梗塞]]。在發作期間，全身性壓力導致環兒茶酚胺循環增加，<ref name="Safi_2019">{{cite journal | vauthors = Safi S, Sethi NJ, Nielsen EE, Feinberg J, Jakobsen JC, Gluud C | title = Beta-blockers for suspected or diagnosed acute myocardial infarction | journal = The Cochrane Database of Systematic Reviews | volume = 12 | issue = 12 | pages = CD012484 | date = December 2019 | pmid = 31845756 | pmc = 6915833 | doi = 10.1002/14651858.CD012484.pub2 | collaboration = Cochrane Heart Group }}</ref><ref name="Farzam_2023">{{cite book | vauthors = Farzam K, Jan A | chapter = Beta Blockers |date=2023 |chapter-url= http://www.ncbi.nlm.nih.gov/books/NBK532906/ | title = StatPearls |access-date=2023-10-31 |place=Treasure Island (FL) |publisher=StatPearls Publishing |pmid=30422501 }}</ref>而導致心率和血壓增加，進而增加心肌需氧量。<ref name="Farzam_2023" /><ref name="Safi_2019" />β受體阻滯劑與兒茶酚胺競爭β<sub>1</sub>-腎上腺素受體結合部位而發揮作用，進一步降低心肌對氧氣的需求，而發揮治療作用。<ref name="Safi_2019" />


一份於2019年發佈的的考科藍合作組織綜述將β受體阻滯劑與安慰劑或無干預行動進行比較，發現β體阻滯劑可能降低短期再梗塞的風險，以及長期降低全因[[死亡率]]和心血管疾病死亡率的風險。<ref name="Safi_2019" />但報告說β受體阻滯劑可能對短期全因死亡率和心血管死亡率幾乎無影響。<ref name="Safi_2019" />
[[Category:抗高血压药]]

[[Category:抗心律不齐药]]
===高血壓===
[[Category:Β阻滞药|*]]
β受體阻滯劑被廣泛用於治療高血壓。<ref>{{cite book | vauthors = Iqbal AH, Jamal SF | chapter = Essential Hypertension |date=2023 | chapter-url = http://www.ncbi.nlm.nih.gov/books/NBK539859/ | title = StatPearls |access-date=2023-10-31 |place=Treasure Island (FL) |publisher=StatPearls Publishing |pmid=30969681 }}</ref>
[[Category:苏格兰发明]]

於2014年發佈的科考藍組織綜述提出在有輕度至中度高血壓的個體中，非選擇性β受體阻滯劑可導致-10/-7毫米汞柱（收縮壓/舒張壓）降低，且不會增加不良事件發生率。<ref name="Wong_2014">{{cite journal | vauthors = Wong GW, Wright JM | title = Blood pressure lowering efficacy of nonselective beta-blockers for primary hypertension | journal = The Cochrane Database of Systematic Reviews | volume = 2014 | issue = 2 | pages = CD007452 | date = February 2014 | pmid = 24585007 | pmc = 10603273 | doi = 10.1002/14651858.CD007452.pub2 | collaboration = Cochrane Hypertension Group }}</ref>但使用較高劑時會增加不良反應發生率，例如心率降低，但血壓卻沒相應降低。<ref name="Wong_2014"/>

於2017發佈的有關使用β受體阻滯劑治療高血壓的科考藍組織綜述提出心血管疾病略有減少，但死亡率幾乎沒變化，<ref name="Wiysonge_2017">{{cite journal | vauthors = Wiysonge CS, Bradley HA, Volmink J, Mayosi BM, Opie LH | title = Beta-blockers for hypertension | journal = The Cochrane Database of Systematic Reviews | volume = 1 | issue = 1 | pages = CD002003 | date = January 2017 | pmid = 28107561 | pmc = 5369873 | doi = 10.1002/14651858.CD002003.pub5 | collaboration = Cochrane Hypertension Group }}.</ref>顯示此藥物的效果不如其他抗高血壓藥物。<ref name="Wiysonge_2017"/>

===焦慮===
β受體阻滯劑並未被[[美國食品藥物管理局]]（FDA）核准用於[[抗焦慮藥|抗焦慮]]用途。<ref name="pmid16957148">{{cite journal | vauthors = Schneier FR | title = Clinical practice. Social anxiety disorder | journal = The New England Journal of Medicine | volume = 355 | issue = 10 | pages = 1029–1036 | date = September 2006 | pmid = 16957148 | doi = 10.1056/NEJMcp060145 }}</ref>然而在過去25年有許多對照試驗顯示β受體阻滯劑對治療[[焦慮症]]有效，然而對其作用機制尚不清楚。<ref>{{cite journal | vauthors = Tyrer P | title = Anxiolytics not acting at the benzodiazepine receptor: beta blockers | journal = Progress in Neuro-Psychopharmacology & Biological Psychiatry | volume = 16 | issue = 1 | pages = 17–26 | date = January 1992 | pmid = 1348368 | doi = 10.1016/0278-5846(92)90004-X | s2cid = 24742562 }}</ref>

===手術===
有低品質證據顯示在心臟手術期間使用β受體阻滯劑可能會降低心律不整和心房顫動的風險。<ref>{{cite journal | vauthors = Blessberger H, Lewis SR, Pritchard MW, Fawcett LJ, Domanovits H, Schlager O, Wildner B, Kammler J, Steinwender C | display-authors = 6 | title = Perioperative beta-blockers for preventing surgery-related mortality and morbidity in adults undergoing cardiac surgery | journal = The Cochrane Database of Systematic Reviews | volume = 9 | issue = 9 | pages = CD013435 | date = September 2019 | pmid = 31544227 | pmc = 6755267 | doi = 10.1002/14651858.CD013435 }}</ref>

==不良影響==
由於β受體遍佈全身，使用β受體阻滯劑可能會導致許多不良反應。心搏過緩和低血壓是兩種常見的，疲勞、[[頭暈]]、[[噁心]]和[[便秘]]也被廣泛報導。一些患者會發生[[性功能障礙]]和[[勃起功能障礙]]。<ref name="StatPearls"
>{{cite journal |last1=Farzam |first1=Khashayar |last2=Jan. |first2=Arif |date= 2023-08-22|title=Beta Blockers |url=https: //www.ncbi.nlm.nih.gov/books/NBK532906/ |journal=StatPearls|volume= |issue= |pages= |doi= |access-date=2024-03-22}}</ref>

較不常見的是患者會出現[[支氣管痙攣]]。[[氣喘]]患者的風險較高。[[雷諾氏症候群]]患者也有病情惡化的風險。 β受體阻滯劑可誘發[[高血糖]]並掩蓋[[低血糖]]患者常見的{{le|血液動力學|Hemodynamics}}症狀（例如[[心跳過速]]）。<ref name="StatPearls"/>

有些患者在使用β受體阻滯劑時會出現[[失眠]]、睡眠變化和作[[惡夢]]。對於會穿過[[血腦屏障]]的β受體阻滯劑，這種作用更為明顯。有些患者在服用後可能會感到疲勞或體重增加。處理這些不良事件的方法包括停止用藥。

服用β受體阻滯劑{{le|卡維地洛|Carvedilol}}可能會加重某些患者的[[水腫]]狀況。<ref name="StatPearls"/>

===禁忌症及注意事項===
{{div col|colwidth=30em}}
絕對禁止:
*[[心跳過緩]]<ref name="Wyeth Propranolol" />
*[[低血壓]]
*對β受體阻滯劑過敏
*[[心源性休克]]
*第二級或第三級[[房室傳導阻滯]]

相對禁忌症或是對特定阻滞劑禁忌症
*有[[長QT綜合症|長QT間期症候群]]者，不得使用{{le|索他洛爾|sotalol}}
*有{{le|尖端扭轉型室速|Torsades de Pointes}}病史者，不得使用索他洛爾

應予注意：
*突然停藥
*支氣管痙攣<ref name="Wyeth Propranolol">{{Cite web| author = Wyeth Pharmaceuticals Inc. |title=Propranolol hydrochloride |url= https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/016418s078lbl.pdf |access-date=2020-09-03 }}</ref>
*心臟衰竭
*氣喘：參見下文
*[[支氣管炎]]<ref name="Wyeth Propranolol" />
*[[腦血管疾病]]
*[[慢性阻塞性肺病]]（COPD）
*[[肺氣腫]]<ref name="Wyeth Propranolol" />
*[[腎衰竭]]
*肝病
*{{le|肌肉病變|Myopathy}}
*[[嗜鉻細胞瘤]]
*[[銀屑病|乾癬]]
*雷諾氏症候群
*中風
*{{le|變異型心絞痛|Vasospastic angina}}
*[[沃夫巴金森懷特症候群]]<ref name="Wyeth Propranolol" />
{{div col end}}

====氣喘====
{{le|美國國家心肺血液研究所|National Heart, Lung, and Blood Institute}} (NHLBI) 於2007年發佈的氣喘指引建議不提供氣喘患者使用非選擇性β受體阻滯劑，但允許使用心臟選擇性β受體阻滯劑。<ref name="NHLBI Asthma 07">{{cite journal | vauthors = ((National Heart, Lung, and Blood Institute)) | author-link = National Heart, Lung, and Blood Institute | title = Expert Panel Report 3 (EPR-3): Guidelines for the Diagnosis and Management of Asthma–Summary Report 2007 | journal = [[The Journal of Allergy and Clinical Immunology]] | volume = 120 | issue = 5 | pages = S94–S138 | year = 2007 | url = https://www.jacionline.org/article/S0091-6749(07)01823-4/fulltext | doi = 10.1016/j.jaci.2007.09.029 | access-date = 2017-12-09 | archive-url = https://web.archive.org/web/20210828002833/https://www.jacionline.org/article/S0091-6749%2807%2901823-4/fulltext | doi-access = free | archive-date = 2021-08-28 }}</ref>{{rp|182}}

對於有輕度至中度呼吸道症狀的患者，可使用盡可能低劑量心臟選擇性β受體阻滯劑（β<sub>1</sub>-受體阻滯劑）。<ref name="Morales Jackson Lipworth Donnan 2014 pp. 779–786">{{cite journal | vauthors = Morales DR, Jackson C, Lipworth BJ, Donnan PT, Guthrie B | title = Adverse respiratory effect of acute β-blocker exposure in asthma: a systematic review and meta-analysis of randomized controlled trials | journal = Chest | volume = 145 | issue = 4 | pages = 779–786 | date = April 2014 | pmid = 24202435 | doi = 10.1378/chest.13-1235 | publisher = Elsevier BV }}</ref><ref name="Salpeter Ormiston Salpeter p=715">{{cite journal | vauthors = Salpeter SR, Ormiston TM, Salpeter EE | title = Cardioselective beta-blockers in patients with reactive airway disease: a meta-analysis | journal = Annals of Internal Medicine | volume = 137 | issue = 9 | pages = 715–725 | date = November 2002 | pmid = 12416945 | doi = 10.7326/0003-4819-137-9-200211050-00035 | publisher = American College of Physicians | doi-access = free }}</ref>

====糖尿病====
腎上腺素是身體在感受即將發生低血糖時而分泌的一種激素， 可被視為低血糖的早期預警信號之一。<ref name="Sprague Arbeláez 2011 pp. 463–475">{{cite journal | vauthors = Sprague JE, Arbeláez AM | title = Glucose counterregulatory responses to hypoglycemia | journal = Pediatric Endocrinology Reviews | volume = 9 | issue = 1 | pages = 463–475 | date = September 2011 | pmid = 22783644 | pmc = 3755377 }}</ref>

β受體阻滯劑有抑制腎上腺素的作用，而干擾[[糖原分解|肝糖分解]]並掩蓋低血糖症狀（如心動過速、[[心悸]]、出[[汗液|汗]]和震顫）而在一定程度上會加劇低血糖。對於服用β受體阻滯劑的糖尿病患者來說，須認真監測血糖值。

====甲狀腺亢進====
突然停藥可能會導致[[甲狀腺風暴|甲狀腺危象]]。<ref name="Wyeth Propranolol" />

====心搏過緩或房室傳導阻滯====
對於接受過房室結消融術（AV node ablation）的老年患者，使用β受體阻滯劑可能增加心藏衰竭而住院的風險。<ref>{{cite journal |last1= Bertomeu-Gonzalez|first1=Vicente |last2= Moreno-Arribas |first2= Jose|date=2023-01-18 |title=Increased Risk of Heart Failure in Elderly Patients Treated with Beta-Blockers After AV Node Ablation|url= https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10006059/|journal = American Journal of Cardiovascular Drugs|volume= |issue= |pages= |doi=10.1007/s40256-022-00566-1 |access-date=2023}}</ref>

===毒性===
對於遭受β受體阻滯劑心臟毒性<ref name="pmid2857542">{{cite journal | vauthors = Weinstein RS, Cole S, Knaster HB, Dahlbert T | title = Beta blocker overdose with propranolol and with atenolol | journal = Annals of Emergency Medicine | volume = 14 | issue = 2 | pages = 161–163 | date = February 1985 | pmid = 2857542 | doi = 10.1016/S0196-0644(85)81081-7 }}</ref><ref name="urlToxicity, Beta-blocker: Treatment & Medication - eMedicine Emergency Medicine">{{cite web |url=http://emedicine.medscape.com/article/813342-treatment |title=Toxicity, Beta-blocker: Treatment & Medication – eMedicine Emergency Medicine |access-date=2009-03-06 |url-status=live |archive-url=https://web.archive.org/web/20090317113942/http://emedicine.medscape.com/article/813342-treatment |archive-date=2009 -03-17|df=mdy-all }}</ref>的患者可施用[[升糖素]]以治療。<ref>{{cite web |url=http://www.courses.ahc.umn.edu/pharmacy/6124/handouts/Beta%20blockers.pdf |title=Beta-Adrenergic Blocker Poisoning |author=John Gualtier |website=Courses.ahc.umn.edu |access-date=2017-03-28 |url-status=dead |archive-url=https://web.archive.org/web/20160303210046/http://www.courses.ahc.umn.edu/pharmacy/6124/handouts/Beta%20blockers.pdf |archive-date=2016-03-03 |df=mdy-all }}</ref><ref>USMLE WORLD 2009 Step1, Pharmacology, Q85</ref>

==β腎上腺素受體拮抗作用==
腎上腺素和正甲腎上腺素刺激β<sub>1</sub>-受體會對心臟產生{{le|時間轉率效應|Chronotropic}}和正性肌力作用，並增加心臟傳導速度和自動性。<ref>{{cite book | vauthors = Michel MC, Insel PA | chapter = Adrenergic Receptors in Clinical Medicine |title= The Adrenergic Receptors in the 21st Century | veditors = Perez DM |year= 2006 |publisher= Humana Press |isbn= 978-1-58829-423-4 |page= 135 | chapter-url= https://books.google.com/books?id=QNpIsKwp8PUC&q=%CE%B21+receptors+positive+chronotropic+inotropic+effect&pg=PA135 |access-date= 2010-09-08 }}{{Dead link|date=October 2023 |bot=InternetArchiveBot |fix-attempted=yes }}</ref>

β受體阻滯劑抑制這些正常的腎上腺素和正甲腎上腺素介導的交感神經活動，<ref name="Frishman_2005" />表示它們可減少興奮或體力消耗對心率和收縮力的影響，<ref>{{cite book | chapter = Beta-Blockers |title=Encyclopedia of Heart Diseases | vauthors = Khan MI |year=2006 |publisher=Elsevier |isbn=978-0-12-406061-6 |page=160 | chapter-url=https://books.google.com/books?id=xco9aJ_Y9XIC&q=beta+blockers+effects+on+heart+rate&pg=PA160 |access-date= 2010-09-10}}</ref>還有減少震顫，<ref>{{cite book |title=Improving Oral Health for the Elderly: An Interdisciplinary Approach | veditors = Lamster IB, Northridge ME |editor2-link=Mary Northridge | name-list-style = vanc |year=2008 |publisher= Springer|location=New York |isbn=978-0-387-74337-0 |page= 87|url=https://books.google.com/books?id=qs2v9Sm-dVoC&q=beta+blockers+reduce+tremor&pg=PA87 |access-date=2010-10-23}}</ref>和肝醣分解。 但β受體阻滯劑會對肺部支氣管產生收縮作用，可能會加重或引起氣喘症狀。<ref>{{cite book | chapter = Beta Antagonist (Blocker) Medications | vauthors = Rothfeld GS, Romaine DS |title= The Encyclopedia of Men's Health | chapter-url = https://books.google.com/books?id=AyPacn1o4nIC&q=beta+blockers+opening+of+bronchi&pg=PA48 |access-date= 2010-10-23 |year= 2005 |publisher= Amaranth |isbn= 978-0-8160-5177-9 |page=48}}</ref>

===血腦障障通透性===
不同β受體阻滯劑的[[親脂性]]（脂溶性）各不相同，而其穿過血腦屏障並在[[中樞神經系統]]中發揮作用的能力也各不相同。<ref name="pmid33572109">{{cite journal | vauthors = Cojocariu SA, Maștaleru A, Sascău RA, Stătescu C, Mitu F, Leon-Constantin MM | title = Neuropsychiatric Consequences of Lipophilic Beta-Blockers | journal = Medicina | volume = 57 | issue = 2 | date = February 2021 | page = 155 | pmid = 33572109 | pmc = 7914867 | doi = 10.3390/medicina57020155 | doi-access = free }}</ref>具有較高血腦屏障通透性的β受體阻滯劑可能具有治療神經精神的益處和副作用，以及不良的認知影響。<ref name="pmid33572109" />

==歷史==
[[蘇格蘭]][[藥理學家]][[詹姆士·懷特·布拉克]]於1964年<ref name="telegraph">{{cite news|url=https://www.telegraph.co.uk/news/obituaries/medicine-obituaries/7507080/Sir-James-Black-OM.html|title=Sir James Black, OM|date= 2010-03-23|newspaper=The Telegraph|access-date=25 March 2010|url-status=live|archive-url=https://web.archive.org/web/20100327031442/http://www.telegraph.co.uk/news/obituaries/medicine-obituaries/7507080/Sir-James-Black-OM.html|archive-date= 2010-03-27|df=mdy-all}}</ref>首次合成兩種具有臨床意義的β受體阻滯劑 - [[普萘洛爾]]和{{le|普奈洛爾|pronethalol}}（後者又稱耐利達），而徹底改變心絞痛的醫療管理，<ref name="pmid10378820">{{cite journal | vauthors = van der Vring JA, Daniëls MC, Holwerda NJ, Withagen PJ, Schelling A, Cleophas TJ, Hendriks MG | title = Combination of calcium channel blockers and beta blockers for patients with exercise-induced angina pectoris: a double-blind parallel-group comparison of different classes of calcium channel blockers. The Netherlands Working Group on Cardiovascular Research (WCN) | journal = Angiology | volume = 50 | issue = 6 | pages = 447–454 | date = June 1999 | pmid = 10378820 | doi = 10.1177/000331979905000602 | s2cid = 21885509 }}</ref>並被多人認為是對20世紀{{le|臨床醫學|clinical medicine}}和[[藥理學]]最重要的貢獻之一。<ref name="pmid9456487">{{cite journal | vauthors = Stapleton MP | title = Sir James Black and propranolol. The role of the basic sciences in the history of cardiovascular pharmacology | journal = Texas Heart Institute Journal | volume = 24 | issue = 4 | pages = 336–342 | year = 1997 | pmid = 9456487 | pmc = 325477 }}</ref>

==社會與文化==
β受體阻滯劑已包含於[[世界衛生組織基本藥物標準清單]]之內。

於2020年，有超過2,600萬[[美國人]]使用β-受體阻滯劑，開立的處方箋超過1.17億份。此藥物是美國使用最多的藥物之一。<ref>{{cite web| url =https://www.aacp.org/event/beta-blockers-one-size-blocks-them-all-updates-pharmacogenetic-education |title =Beta-Blockers–One Size Blocks Them All? Updates in Pharmacogenetic Education| publisher =AACP | date = | accessdate = 2024-03-24 }}</ref>

== 參見 ==
* {{le|α-受體阻滯劑|Alpha blockers}}

== 參考文獻 ==
{{Reflist|2}}

== 外部連結 ==
* [https://www.musiciansway.com/blog/2010/03/musicians-and-beta-blockers/ Musicians and beta-blockers] by Gerald Klickstein, 2010-03-11 (A blog post that considers "whether beta-blockers are safe, effective, and appropriate for performers to use.")
* [https://www.nytimes.com/2004/10/17/arts/music/17tind.html Better Playing Through Chemistry] by Blair Tindall, ''[[The New York Times]]'', 2004-10-17. (Discusses the use of beta blockers among professional musicians)
* [https://www.sfgate.com/health/article/Using-chemistry-to-create-better-music-Legal-2687828.php Musicians using beta blockers] by Blair Tindall. A condensed version of the above article.
* [https://www.theatlantic.com/doc/200808u/beta-blockers In Defense of the Beta Blocker] by Carl Elliott, ''[[The Atlantic]]'', 2008-08-20. (Discusses the use of propranolol by a North Korean pistol shooter in the 2008 Olympics)
* {{MeshName|beta-Adrenergic+Blockers}}

{{模板:Β受體阻滯劑}}
{{模板:主要藥物分類}}
{{模板:抗交感抗高血壓藥物}}
{{模板:抗青光眼製劑及縮瞳藥}}
{{模板:腎上腺素受體調節劑}}
{{Authority control}}

{{DEFAULTSORT:Beta Blocker}}

[[分類:Β阻滯藥| ]]
[[分類:蘇格蘭發明]]

2024年3月29日 (五) 12:38的版本

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Beta blockers
药物种类
Propranolol
普萘洛爾（全球首次合成具有臨床效果的β受體阻滯劑）的骨架式
用途高血壓, 心律不整等
生物靶标β受體
ATC代码C07
外部链接
MeSHD000319
AHFS/Drugs.com药物分类
消费者报告Best Buy Drugs
WebMDmedicinenet  rxlist

β受體阻滯劑（英語：Beta blockers），也拼寫為β-blockers），是一類主要用於控制心律不整，並於首次心臟病發作後用於保護心臟，免受再次發作侵害（預防醫學）的藥物。[1]此藥物也廣泛用於治療高血壓，但已非大多數初次治療的首選藥物。[2]

此種藥物的給藥方式有口服給藥、靜脈注射及眼科製劑給藥。

β受體阻滯劑是種競爭性拮抗劑，可阻斷交感神經系統腎上腺素β受體中內源性兒茶酚胺的腎上腺素和正腎上腺素的受體位點，達到降低心率、血壓和其他"戰鬥或逃跑"的相關反應。[3]:152[4]此類藥物中有些可阻斷所有類型β-腎上腺素受體的激活，另一些則對三種已知β-腎上腺受體（即β1、β2 和β3）之一具有選擇性。[3]:153β1-腎上腺素受體主要位於心臟和腎臟。[4]β2-的主要位於肺部、胃腸道、肝臟、子宮、血管平滑肌和骨骼肌。[4]β3-的位於脂肪細胞。[5]

β受體所存在的組織是交感神經系統的一部分，會導致壓力反應，特別是當它們受到腎上腺素刺激後。 β受體阻滯劑可干擾腎上腺素和其他壓力激素（英语：stress hormone）受體的結合，將壓力激素作用降低。

對於原發性高血壓的治療，於主要使用阿替洛爾（替代普萘洛爾作為治療高血壓的藥物）治療的統合分析顯示，雖然β受體阻滯劑在預防中風和整體心血管事件方面比安慰劑更有效，但不如利尿劑（抑制腎素-血管收縮素系統的藥物，例如ACE抑制劑或鈣通道阻滯劑）） 有效。[6][7][8][9]

醫療用途

β受體阻滯劑用於治療與心臟和血管系統相關的各種疾病以及其他幾種醫學情況。 它已被廣泛用於治療常見的心臟相關疾病，包括心絞痛、急性冠狀動脈症候群、高血壓以及心律不整，也用於治療其他心臟疾病，例如肥厚性阻塞心肌病變（英语：Hypertrophic cardiomyopathy）、二尖瓣狹窄或僧帽瓣脫垂（英语：Mitral valve prolapse）以及主動脈剝離。此外，β受體阻滯劑也可用於血管手術、焦慮、甲狀腺功能亢進症、青光眼、偏頭痛和食道靜脈曲張（英语：Esophageal varices）的治療。[10]

心臟衰竭

β受體阻滯劑因為會降低心肌收縮力，而有可能使病情惡化，曾在心臟衰竭案例中遭到禁用，但於20世紀90年代末所做的研究顯示它在降低發病率和死亡率方面具有功效。[11][12][13]比索洛爾、卡維地洛和緩釋型美托洛爾被明確指定為心臟衰竭標準ACE抑制劑和利尿劑治療的輔助藥物，但其劑量通常遠低於用作其他疾病的治療。 β受體阻滯劑僅適用於代償性穩定心臟衰竭，在急性失代償性心臟衰竭的情況下，β受體阻滯劑會導致射血分數進一步降低，讓患者的症狀惡化。[14]

β受體阻滯劑主要因其對心率的降低作用而聞名，但這並非用於治療心臟衰竭的唯一重要機制。[15]β受體阻滯劑除在心臟中的交感神經β1活性外，還會影響腎臟中的腎素-血管收縮素系統，它會導致腎素分泌減少，進而降低細胞外容量和增加血液的攜氧能力來減少心臟的需氧量。心臟衰竭的特徵在於心臟上兒茶酚胺活性增加，會導致多種有害影響，包括需氧量增加、發炎介質傳播和異常心臟組織重塑，所有這些都會降低心臟收縮效率並導致射血分數降低。[16]

試驗結果顯示β受體阻滯劑在13個月的期間內可將絕對死亡風險降低4.5%。除降低死亡風險外，連就診和住院的次數也可減少。[17]一份於2020年發表的考科藍合作組織綜述提出支持使用β受體阻滯劑以治療兒童心臟衰竭的證據極少，但從已有數據中確實指出它們可能有益。[18]

治療心臟衰竭的β受體阻滯劑應從極低劑量（目標劑量的1/8）開始，然後逐漸增加。患者心臟必須適應較少兒茶酚胺刺激帶來的變化，並找到新的運作平衡點。[19]

急性心肌梗塞

β受體阻滯劑適用於治療急性心肌梗塞。在發作期間，全身性壓力導致環兒茶酚胺循環增加，[20][21]而導致心率和血壓增加，進而增加心肌需氧量。[21][20]β受體阻滯劑與兒茶酚胺競爭β1-腎上腺素受體結合部位而發揮作用，進一步降低心肌對氧氣的需求，而發揮治療作用。[20]

一份於2019年發佈的的考科藍合作組織綜述將β受體阻滯劑與安慰劑或無干預行動進行比較，發現β體阻滯劑可能降低短期再梗塞的風險，以及長期降低全因死亡率和心血管疾病死亡率的風險。[20]但報告說β受體阻滯劑可能對短期全因死亡率和心血管死亡率幾乎無影響。[20]

高血壓

β受體阻滯劑被廣泛用於治療高血壓。[22]

於2014年發佈的科考藍組織綜述提出在有輕度至中度高血壓的個體中，非選擇性β受體阻滯劑可導致-10/-7毫米汞柱（收縮壓/舒張壓）降低，且不會增加不良事件發生率。[23]但使用較高劑時會增加不良反應發生率，例如心率降低，但血壓卻沒相應降低。[23]

於2017發佈的有關使用β受體阻滯劑治療高血壓的科考藍組織綜述提出心血管疾病略有減少，但死亡率幾乎沒變化，[24]顯示此藥物的效果不如其他抗高血壓藥物。[24]

焦慮

β受體阻滯劑並未被美國食品藥物管理局（FDA）核准用於抗焦慮用途。[25]然而在過去25年有許多對照試驗顯示β受體阻滯劑對治療焦慮症有效，然而對其作用機制尚不清楚。[26]

手術

有低品質證據顯示在心臟手術期間使用β受體阻滯劑可能會降低心律不整和心房顫動的風險。[27]

不良影響

由於β受體遍佈全身，使用β受體阻滯劑可能會導致許多不良反應。心搏過緩和低血壓是兩種常見的，疲勞、頭暈、噁心和便秘也被廣泛報導。一些患者會發生性功能障礙和勃起功能障礙。[28]

較不常見的是患者會出現支氣管痙攣。氣喘患者的風險較高。雷諾氏症候群患者也有病情惡化的風險。 β受體阻滯劑可誘發高血糖並掩蓋低血糖患者常見的血液動力學症狀（例如心跳過速）。[28]

有些患者在使用β受體阻滯劑時會出現失眠、睡眠變化和作惡夢。對於會穿過血腦屏障的β受體阻滯劑，這種作用更為明顯。有些患者在服用後可能會感到疲勞或體重增加。處理這些不良事件的方法包括停止用藥。

服用β受體阻滯劑卡維地洛可能會加重某些患者的水腫狀況。[28]

禁忌症及注意事項

絕對禁止:

相對禁忌症或是對特定阻滞劑禁忌症

應予注意：

氣喘

美國國家心肺血液研究所（英语：National Heart, Lung, and Blood Institute） (NHLBI) 於2007年發佈的氣喘指引建議不提供氣喘患者使用非選擇性β受體阻滯劑，但允許使用心臟選擇性β受體阻滯劑。[30]:182

對於有輕度至中度呼吸道症狀的患者，可使用盡可能低劑量心臟選擇性β受體阻滯劑（β1-受體阻滯劑）。[31][32]

糖尿病

腎上腺素是身體在感受即將發生低血糖時而分泌的一種激素， 可被視為低血糖的早期預警信號之一。[33]

β受體阻滯劑有抑制腎上腺素的作用，而干擾肝糖分解並掩蓋低血糖症狀（如心動過速、心悸、出汗和震顫）而在一定程度上會加劇低血糖。對於服用β受體阻滯劑的糖尿病患者來說，須認真監測血糖值。

甲狀腺亢進

突然停藥可能會導致甲狀腺危象。[29]

心搏過緩或房室傳導阻滯

對於接受過房室結消融術（AV node ablation）的老年患者，使用β受體阻滯劑可能增加心藏衰竭而住院的風險。[34]

毒性

對於遭受β受體阻滯劑心臟毒性[35][36]的患者可施用升糖素以治療。[37][38]

β腎上腺素受體拮抗作用

腎上腺素和正甲腎上腺素刺激β1-受體會對心臟產生時間轉率效應（英语：Chronotropic）和正性肌力作用，並增加心臟傳導速度和自動性。[39]

β受體阻滯劑抑制這些正常的腎上腺素和正甲腎上腺素介導的交感神經活動，[3]表示它們可減少興奮或體力消耗對心率和收縮力的影響，[40]還有減少震顫，[41]和肝醣分解。 但β受體阻滯劑會對肺部支氣管產生收縮作用，可能會加重或引起氣喘症狀。[42]

血腦障障通透性

不同β受體阻滯劑的親脂性（脂溶性）各不相同，而其穿過血腦屏障並在中樞神經系統中發揮作用的能力也各不相同。[43]具有較高血腦屏障通透性的β受體阻滯劑可能具有治療神經精神的益處和副作用，以及不良的認知影響。[43]

歷史

蘇格蘭藥理學家詹姆士·懷特·布拉克於1964年[44]首次合成兩種具有臨床意義的β受體阻滯劑 - 普萘洛爾和普奈洛爾（英语：pronethalol）（後者又稱耐利達），而徹底改變心絞痛的醫療管理，[45]並被多人認為是對20世紀臨床醫學和藥理學最重要的貢獻之一。[46]

社會與文化

β受體阻滯劑已包含於世界衛生組織基本藥物標準清單之內。

於2020年，有超過2,600萬美國人使用β-受體阻滯劑，開立的處方箋超過1.17億份。此藥物是美國使用最多的藥物之一。[47]

參見

參考文獻

  1. ^ Freemantle N, Cleland J, Young P, Mason J, Harrison J. beta Blockade after myocardial infarction: systematic review and meta regression analysis. BMJ. June 1999, 318 (7200): 1730–1737. PMC 31101 可免费查阅. PMID 10381708. doi:10.1136/bmj.318.7200.1730. 
  2. ^ James PA, Oparil S, Carter BL, Cushman WC, Dennison-Himmelfarb C, Handler J, et al. 2014 evidence-based guideline for the management of high blood pressure in adults: report from the panel members appointed to the Eighth Joint National Committee (JNC 8). JAMA. February 2014, 311 (5): 507–520. PMID 24352797. doi:10.1001/jama.2013.284427 可免费查阅. 
  3. ^ 3.0 3.1 3.2 Frishman WH, Cheng-Lai A, Nawarskas J (编). Beta-Adrenergic Blockers. Current Cardiovascular Drugs. Current Science Group. 2005 [2010-09-07]. ISBN 978-1-57340-221-7. 
  4. ^ 4.0 4.1 4.2 Barranger K, Vivian E, Peterson AM. Hypertension. Arcangelo VP, Peterson AM (编). Pharmacotherapeutics for advanced practice: a practical approach. Lippincott Williams & Wilkins. 2006: 205 [2010-09-07]. ISBN 978-0-7817-5784-3. 
  5. ^ Clément K, Vaisse C, Manning BS, Basdevant A, Guy-Grand B, Ruiz J, et al. Genetic variation in the beta 3-adrenergic receptor and an increased capacity to gain weight in patients with morbid obesity. The New England Journal of Medicine. August 1995, 333 (6): 352–354. PMID 7609752. doi:10.1056/NEJM199508103330605 可免费查阅. 
  6. ^ Wiysonge CS, Bradley HA, Volmink J, Mayosi BM, Opie LH. Beta-blockers for hypertension. The Cochrane Database of Systematic Reviews. January 2017, 1 (1): CD002003. PMC 5369873 可免费查阅. PMID 28107561. doi:10.1002/14651858.CD002003.pub5. 
  7. ^ Reinhart, Marcia; Puil, Lorri; Salzwedel, Douglas M.; Wright, James M. First-line diuretics versus other classes of antihypertensive drugs for hypertension. The Cochrane Database of Systematic Reviews. 2023-07-13, 2023 (7): CD008161. ISSN 1469-493X. PMC 10339786 可免费查阅. PMID 37439548. doi:10.1002/14651858.CD008161.pub3.  已忽略未知参数|pmc-embargo-date= (帮助)
  8. ^ Zhu J, Chen N, Zhou M, Guo J, Zhu C, Zhou J, et al. Calcium channel blockers versus other classes of drugs for hypertension. The Cochrane Database of Systematic Reviews. January 2022, 1 (1): CD003654. PMC 8742884 可免费查阅. PMID 35000192. doi:10.1002/14651858.CD003654.pub6. 
  9. ^ Wiysonge CS, Bradley HA, Volmink J, Mayosi BM, Opie LH. Beta-blockers for hypertension. The Cochrane Database of Systematic Reviews. January 2017, 1 (1): CD002003. PMC 5369873 可免费查阅. PMID 28107561. doi:10.1002/14651858.cd002003.pub5. 
  10. ^ Opie LH. Drugs for the Heart. Philadelphia: Saunders. 2009: 6–18. ISBN 978-1-4160-6158-8. 
  11. ^ Hjalmarson A, Goldstein S, Fagerberg B, Wedel H, Waagstein F, Kjekshus J, et al. Effects of controlled-release metoprolol on total mortality, hospitalizations, and well-being in patients with heart failure: the Metoprolol CR/XL Randomized Intervention Trial in congestive heart failure (MERIT-HF). MERIT-HF Study Group. JAMA. March 2000, 283 (10): 1295–1302. PMID 10714728. doi:10.1001/jama.283.10.1295 可免费查阅. 
  12. ^ Leizorovicz A, Lechat P, Cucherat M, Bugnard F. Bisoprolol for the treatment of chronic heart failure: a meta-analysis on individual data of two placebo-controlled studies—CIBIS and CIBIS II. Cardiac Insufficiency Bisoprolol Study. American Heart Journal. February 2002, 143 (2): 301–307. PMID 11835035. doi:10.1067/mhj.2002.120768. 
  13. ^ Packer M, Fowler MB, Roecker EB, Coats AJ, Katus HA, Krum H, et al. Effect of carvedilol on the morbidity of patients with severe chronic heart failure: results of the carvedilol prospective randomized cumulative survival (COPERNICUS) study. Circulation. October 2002, 106 (17): 2194–2199. PMID 12390947. doi:10.1161/01.CIR.0000035653.72855.BF 可免费查阅. 
  14. ^ Philip J Podrid, Philip J. Major side effects of beta blockers. UpToDate. 2023-06-15 [2024-03-22]. 
  15. ^ Fletcher P. Beta blockers in heart failure. Australian Prescriber. 2000, 23 (6): 120–123. doi:10.18773/austprescr.2000.138 可免费查阅 （英语）. 
  16. ^ Use of beta-blockers and ivabradine in heart failure with reduced ejection fraction. www.uptodate.com. [2015-12-11]. （原始内容存档于2015-12-22）.  已忽略未知参数|df= (帮助)
  17. ^ Pritchett AM, Redfield MM. Beta-blockers: new standard therapy for heart failure. Mayo Clinic Proceedings. August 2002, 77 (8): 839–845; quiz 845–46. PMID 12173717. doi:10.4065/77.8.839 可免费查阅. 
  18. ^ Alabed S, Sabouni A, Al Dakhoul S, Bdaiwi Y. Beta-blockers for congestive heart failure in children. The Cochrane Database of Systematic Reviews. July 2020, 2020 (7): CD007037. PMC 7389334 可免费查阅. PMID 32700759. doi:10.1002/14651858.CD007037.pub4.  已忽略未知参数|collaboration= (帮助)
  19. ^ Goodman & Gilman's: The Pharmacological Basic of Therapeutics. McGraw-Hill. 2018. ISBN 9781259584732. 
  20. ^ 20.0 20.1 20.2 20.3 20.4 Safi S, Sethi NJ, Nielsen EE, Feinberg J, Jakobsen JC, Gluud C. Beta-blockers for suspected or diagnosed acute myocardial infarction. The Cochrane Database of Systematic Reviews. December 2019, 12 (12): CD012484. PMC 6915833 可免费查阅. PMID 31845756. doi:10.1002/14651858.CD012484.pub2.  已忽略未知参数|collaboration= (帮助)
  21. ^ 21.0 21.1 Farzam K, Jan A. Beta Blockers. StatPearls. Treasure Island (FL): StatPearls Publishing. 2023 [2023-10-31]. PMID 30422501. 
  22. ^ Iqbal AH, Jamal SF. Essential Hypertension. StatPearls. Treasure Island (FL): StatPearls Publishing. 2023 [2023-10-31]. PMID 30969681. 
  23. ^ 23.0 23.1 Wong GW, Wright JM. Blood pressure lowering efficacy of nonselective beta-blockers for primary hypertension. The Cochrane Database of Systematic Reviews. February 2014, 2014 (2): CD007452. PMC 10603273 可免费查阅. PMID 24585007. doi:10.1002/14651858.CD007452.pub2.  已忽略未知参数|collaboration= (帮助)
  24. ^ 24.0 24.1 Wiysonge CS, Bradley HA, Volmink J, Mayosi BM, Opie LH. Beta-blockers for hypertension. The Cochrane Database of Systematic Reviews. January 2017, 1 (1): CD002003. PMC 5369873 可免费查阅. PMID 28107561. doi:10.1002/14651858.CD002003.pub5.  已忽略未知参数|collaboration= (帮助).
  25. ^ Schneier FR. Clinical practice. Social anxiety disorder. The New England Journal of Medicine. September 2006, 355 (10): 1029–1036. PMID 16957148. doi:10.1056/NEJMcp060145. 
  26. ^ Tyrer P. Anxiolytics not acting at the benzodiazepine receptor: beta blockers. Progress in Neuro-Psychopharmacology & Biological Psychiatry. January 1992, 16 (1): 17–26. PMID 1348368. S2CID 24742562. doi:10.1016/0278-5846(92)90004-X. 
  27. ^ Blessberger H, Lewis SR, Pritchard MW, Fawcett LJ, Domanovits H, Schlager O, et al. Perioperative beta-blockers for preventing surgery-related mortality and morbidity in adults undergoing cardiac surgery. The Cochrane Database of Systematic Reviews. September 2019, 9 (9): CD013435. PMC 6755267 可免费查阅. PMID 31544227. doi:10.1002/14651858.CD013435. 
  28. ^ 28.0 28.1 28.2 Farzam, Khashayar; Jan., Arif. [https: //www.ncbi.nlm.nih.gov/books/NBK532906/ Beta Blockers] 请检查|url=值 (帮助). StatPearls. 2023-08-22 [2024-03-22]. 
  29. ^ 29.0 29.1 29.2 29.3 29.4 29.5 Wyeth Pharmaceuticals Inc. Propranolol hydrochloride (PDF). [2020-09-03]. 
  30. ^ ((National Heart, Lung, and Blood Institute)). Expert Panel Report 3 (EPR-3): Guidelines for the Diagnosis and Management of Asthma–Summary Report 2007. The Journal of Allergy and Clinical Immunology. 2007, 120 (5): S94–S138 [2017-12-09]. doi:10.1016/j.jaci.2007.09.029 可免费查阅. （原始内容存档于2021-08-28）.  温哥华格式错误 (帮助)
  31. ^ Morales DR, Jackson C, Lipworth BJ, Donnan PT, Guthrie B. Adverse respiratory effect of acute β-blocker exposure in asthma: a systematic review and meta-analysis of randomized controlled trials. Chest (Elsevier BV). April 2014, 145 (4): 779–786. PMID 24202435. doi:10.1378/chest.13-1235. 
  32. ^ Salpeter SR, Ormiston TM, Salpeter EE. Cardioselective beta-blockers in patients with reactive airway disease: a meta-analysis. Annals of Internal Medicine (American College of Physicians). November 2002, 137 (9): 715–725. PMID 12416945. doi:10.7326/0003-4819-137-9-200211050-00035 可免费查阅. 
  33. ^ Sprague JE, Arbeláez AM. Glucose counterregulatory responses to hypoglycemia. Pediatric Endocrinology Reviews. September 2011, 9 (1): 463–475. PMC 3755377 可免费查阅. PMID 22783644. 
  34. ^ Bertomeu-Gonzalez, Vicente; Moreno-Arribas, Jose. Increased Risk of Heart Failure in Elderly Patients Treated with Beta-Blockers After AV Node Ablation. American Journal of Cardiovascular Drugs. 2023-01-18 [2023]. doi:10.1007/s40256-022-00566-1. 
  35. ^ Weinstein RS, Cole S, Knaster HB, Dahlbert T. Beta blocker overdose with propranolol and with atenolol. Annals of Emergency Medicine. February 1985, 14 (2): 161–163. PMID 2857542. doi:10.1016/S0196-0644(85)81081-7. 
  36. ^ Toxicity, Beta-blocker: Treatment & Medication – eMedicine Emergency Medicine. [2009-03-06]. （原始内容存档于2009 -03-17）.  已忽略未知参数|df= (帮助);
  37. ^ John Gualtier. Beta-Adrenergic Blocker Poisoning (PDF). Courses.ahc.umn.edu. [2017-03-28]. （原始内容 (PDF)存档于2016-03-03）.  已忽略未知参数|df= (帮助)
  38. ^ USMLE WORLD 2009 Step1, Pharmacology, Q85
  39. ^ Michel MC, Insel PA. Adrenergic Receptors in Clinical Medicine. Perez DM (编). The Adrenergic Receptors in the 21st Century. Humana Press. 2006: 135 [2010-09-08]. ISBN 978-1-58829-423-4. [永久失效連結]
  40. ^ Khan MI. Beta-Blockers. Encyclopedia of Heart Diseases. Elsevier. 2006: 160 [2010-09-10]. ISBN 978-0-12-406061-6. 
  41. ^ Lamster IB, Northridge ME (编). Improving Oral Health for the Elderly: An Interdisciplinary Approach. New York: Springer. 2008: 87 [2010-10-23]. ISBN 978-0-387-74337-0. 
  42. ^ Rothfeld GS, Romaine DS. Beta Antagonist (Blocker) Medications. The Encyclopedia of Men's Health. Amaranth. 2005: 48 [2010-10-23]. ISBN 978-0-8160-5177-9. 
  43. ^ 43.0 43.1 Cojocariu SA, Maștaleru A, Sascău RA, Stătescu C, Mitu F, Leon-Constantin MM. Neuropsychiatric Consequences of Lipophilic Beta-Blockers. Medicina. February 2021, 57 (2): 155. PMC 7914867 可免费查阅. PMID 33572109. doi:10.3390/medicina57020155 可免费查阅. 
  44. ^ Sir James Black, OM. The Telegraph. 2010-03-23 [25 March 2010]. （原始内容存档于2010-03-27）.  已忽略未知参数|df= (帮助)
  45. ^ van der Vring JA, Daniëls MC, Holwerda NJ, Withagen PJ, Schelling A, Cleophas TJ, Hendriks MG. Combination of calcium channel blockers and beta blockers for patients with exercise-induced angina pectoris: a double-blind parallel-group comparison of different classes of calcium channel blockers. The Netherlands Working Group on Cardiovascular Research (WCN). Angiology. June 1999, 50 (6): 447–454. PMID 10378820. S2CID 21885509. doi:10.1177/000331979905000602. 
  46. ^ Stapleton MP. Sir James Black and propranolol. The role of the basic sciences in the history of cardiovascular pharmacology. Texas Heart Institute Journal. 1997, 24 (4): 336–342. PMC 325477 可免费查阅. PMID 9456487. 
  47. ^ Beta-Blockers–One Size Blocks Them All? Updates in Pharmacogenetic Education. AACP. [2024-03-24]. 

外部連結

β, 非选择性
β1选择性
β2选择性
α1+β选择性
描述
疾病
治療
胃肠道/新陈代谢（A）
血液系统（B）
心血管系统（C）
皮肤科用药（D）
泌尿生殖系统及性类固醇（G）
体激素（H）
抗感染药（J、P、QI）
抗肿瘤药（L01-L02）
免疫用药（L03-L04）
肌肉、骨骼和关节系统（M）
脑、神经系统（N）
呼吸系统（R）
感觉系统（S）
其他（V）
交感神经 (及密切相关) 抗高血压药物 (C02)
交感阻滞
(拮抗α-肾上腺素能引起的血管收缩)
中枢
肾上腺素释放抑制剂
外周
间接
直接
非选择性α受体阻滞剂
其他拮抗剂
双重 (波生坦) • 选择性 (安贝生坦, 苯磺酸贝托司汀)
描述
疾病
治療
眼科: 抗青光眼制剂和缩瞳药（英语：Miosis） (S01E)
拟交感神经药
拟副交感神经药（英语：Parasympathomimetic drug）
碳酸酐酶抑制剂（英语：Carbonic anhydrase inhibitor）/
（磺胺类药）
乙型拟交感神经阻断剂
前列腺素类似物（英语：Prostaglandin analogue）（F2α）
其他药物
人眼索引
描述
疾病
治療
α1（英语：Alpha-1 adrenergic receptor）
α2（英语：Alpha-2 adrenergic receptor）
β
 
国际
各地
检索自“https://zh.wikipedia.org/w/index.php?title=Β受体阻滞剂&oldid=82073372”