β受体阻滞剂

(重定向自乙型交感神經阻斷劑

β受体阻断药(英語: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药物[1][2][3]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。[4][5][6]

β受体阻断药
Beta blockers
药物种类
Propranolol
普萘洛尔键线式结构,是第一种成功应用于临床的β受体阻断药
用途高血压心律不整
生物目标β受体
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去甲肾上腺素的作用,尤其是肾上腺素能β受体[7][8]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。[9]

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。[10]

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。[11]

例子编辑

 
二氯異丙腎上腺素英语Dichloroisoprenaline,第一种β受体阻断药

引用编辑

  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): 1730–7. PMC 31101. PMID 10381708. doi:10.1136/bmj.318.7200.1730. 
  2. ^ Cruickshank JM. Beta blockers in hypertension. Lancet. August 2010, 376 (9739): 415; author reply 415–6. PMID 20692524. doi:10.1016/S0140-6736(10)61217-2. 
  3. ^ Kaplan, Norman M. Choice of therapy in primary (essential) hypertension: Clinical trials. UpToDate. October 2010. 
  4. ^ De Giorgi, Vincenzoa; Grazzini, Martaa; Benemei, Silviab; Marchionni, Niccolòc; Geppetti, Pierangelob; Gandini, Sarad. β-Blocker use and reduced disease progression in patients with thick melanoma: 8 years of follow-up.. Melanoma Research. June 2017, 27: 268–270. doi:10.1097/CMR.000000000000031. 
  5. ^ Glasner, A; Avraham, R; Rosenne, E; Benish, M; Zmora, O; Shemer, S; Ben‐Eliyahu, S. 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.. Journal of Immunology. March 2010, 184: 2449–2457. doi:10.4049/jimmunol.0903301. 
  6. ^ Childers, W. K.; Hollenbeak, C. S.; Cheriyath, P. β‐Blockers reduce breast cancer recurrence and breast cancer death: A meta‐analysis. Clinical Breast Cancer.. Clinical Breast Cancer. December 2015, 15 (6): 426–431. doi:10.1016/j.clbc.2015.07.001. 
  7. ^ Frishman W.H.; Cheng-Lai A; Nawarskas J. Current Cardiovascular Drugs. Current Science Group. 2005: 152 [2010-09-07]. ISBN 978-1-57340-221-7. 
  8. ^ Arcangelo V.P.; Peterson A.M. Pharmacotherapeutics for advanced practice: a practical approach. Lippincott Williams & Wilkins. 2006: 205 [2010-09-07]. ISBN 978-0-7817-5784-3. 
  9. ^ Schena, G; Caplan, M. J.; Benemei, Silviab; Marchionni, Niccolòc; Geppetti, Pierangelob; Gandini, Sarad. Everything You Always Wanted to Know about β3-AR * (* But Were Afraid to Ask). Cells. Aprail 2019, 8 (4): 357. doi:10.3390/cells8040357. 
  10. ^ Williams, Bryan; Mancia, Giuseppe; Spiering, Wilko; Agabiti Rosei, Enrico; Azizi, Michel; Burnier, Michel; Clement, Denis L.; Coca, Antonio; de Simone, Giovanni. 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). European Heart Journal. 2018-09-01, 39 (33): 3021–3104. ISSN 0195-668X. doi:10.1093/eurheartj/ehy339 (英语). 
  11. ^ Kim, Jihee; Grotegut, Chad A.; Wisler, James W.; Mao, Lan; Rosenberg, Paul B.; Rockman, Howard A.; Lefkowitz, Robert J. The β-arrestin-biased β-adrenergic receptor blocker carvedilol enhances skeletal muscle contractility. Proceedings of the National Academy of Sciences. 2020-06-02, 117 (22): 12435–12443. doi:10.1073/pnas.1920310117.