β受体阻滞剂

β受体阻断药(英语: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、乙型阻断剂,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]近期有相关证据显示,此类阻滞剂可能具有协助癌症治疗的潜能。[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
生物靶标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,市面上的药物多以β受体中的β1及β2为目标,而针对β3的受体阻滞剂因药理学特性仍无法良好掌握故持续处于研究阶段。[9]

ESC/ESH指引指出对于合并心衰竭、心绞痛、心肌梗塞后或心房颤动的高血压患者,以及育龄期或计划怀孕的女性高血压患者,可考虑在任何治疗阶段使用乙型阻断剂。[10]

最近有研究证明乙型阻断剂carvedilol可以增强骨骼肌收缩力,但却无法导致骨骼肌肥大; 该研究亦指出β2AR激动剂clenbuterol则可以增强骨骼肌收缩力和引起骨骼肌肥大的现象,而这些现象都是通过β-arrestin的信号传递所介导的。[11]

例子 编辑

 
二氯异丙肾上腺素英语Dichloroisoprenaline,第一种β受体阻断药
  • 普萘洛尔(Propranolol)β1+β2
  • (Cardolol)β1+β2
  • (Timolol)β1+β2
  • (Carvedilol) mixed α+ β
  • (Labetalol)针剂剂型,同时阻断 α和 β

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 [2020-12-21]. doi:10.1097/CMR.000000000000031. (原始内容存档于2021-11-19). 
  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 [2020-12-21]. doi:10.4049/jimmunol.0903301. (原始内容存档于2021-11-19). 
  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 [2020-01-03]. ISSN 0195-668X. doi:10.1093/eurheartj/ehy339. (原始内容存档于2022-03-10) (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.