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毕索洛尔：修订间差异

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我把en:Bisoprolol翻譯為中文，用來補充與之連接，但篇幅較短的中文條目。敬請指教。
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{{Infobox drug
{{NoteTA
| Watchedfields = changed
|T=zh-cn:比索洛尔;zh-tw:畢索洛爾;zh-hk:比索洛爾;
| verifiedrevid = 459980153
|1=zh-cn:比索洛尔;zh-tw:畢索洛爾;;zh-hk:比索洛爾;
| image = Bisoprolol.svg
}}
| width = 240
{{medical}}
| alt =
{{Drugbox
| image2 = Bisoprolol ball-and-stick.png
| verifiedrevid = 459980153
| alt2 =
| IUPAC_name = (''RS'')-1-{4-[(2-isopropoxyethoxy)methyl]phenoxy}-<br/>3-(isopropylamino)propan-2-ol
| chirality = [[外消旋體]]
| image = Bisoprolol.svg
| width = 240px
| imagename = 1 : 1 mixture (racemate)
| drug_name = Bisoprolol


<!--Clinical data-->
<!-- Clinical data -->
| tradename = Concor
| tradename = Zebeta、Monocor及其他
| Drugs.com = {{drugs.com|monograph|zebeta}}
| Drugs.com = {{drugs.com|monograph|bisoprolol-fumarate}}
| MedlinePlus = a693024
| MedlinePlus = a693024
| pregnancy_AU = C
| licence_US = Bisoprolol
| pregnancy_category =
| pregnancy_AU = C
| routes_of_administration = [[口服給藥]]
| pregnancy_US = C
| ATC_prefix = C07
| pregnancy_category =
| ATC_suffix = AB07
| legal_status = Rx-only
| routes_of_administration = oral


<!--Pharmacokinetic data-->
<!-- Legal status -->
| legal_CA = Rx-only
| bioavailability = >90%
| legal_CA_comment = <ref>{{cite web | title=Monocor Product information | website=[[Health Canada]] | date= 2009-07-31 | url=https://health-products.canada.ca/dpd-bdpp/info?lang=eng&code=64754 | access-date=2024-04-19}}</ref>
| protein_bound = 30%<ref name="pmid2439794">{{cite journal | author = Bühring KU, Sailer H, Faro HP, Leopold G, Pabst J, Garbe A | title = Pharmacokinetics and metabolism of bisoprolol-14C in three animal species and in humans | journal = J. Cardiovasc. Pharmacol. | volume = 8 Suppl 11 | issue = | pages = S21–8 | year = 1986 | pmid = 2439794 | doi = | url = }}</ref>
| legal_US = Rx-only
| metabolism = 50% [[Liver|Hepatic]]
| legal_US_comment = <ref>{{cite web | title=Zebeta (Bisoprolol Fumarate) Tablets | website=DailyMed | url=https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=212148 | access-date=2024-04-19}}</ref><ref>{{cite web | title=Bisoprolol fumarate tablet, film coated | website=DailyMed | date=2024-03-06 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=7556f457-c4d3-49d6-b383-0ade6d489091 | access-date=2024-04-19 | archive-date=2024-04-19 | archive-url=https://web.archive.org/web/20240419035602/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=7556f457-c4d3-49d6-b383-0ade6d489091 | url-status=live }}</ref>
| elimination_half-life = 10–12&nbsp;hours<ref name="pmid2439789">{{cite journal | author = Leopold G | title = Balanced pharmacokinetics and metabolism of bisoprolol | journal = J. Cardiovasc. Pharmacol. | volume = 8 Suppl 11 | issue = | pages = S16–20 | year = 1986 | pmid = 2439789 | doi = | url = }}</ref>
| legal_status = Rx-only


<!--Identifiers-->
<!-- Pharmacokinetic data -->
| bioavailability = >90%
| CASNo_Ref = {{cascite|correct|CAS}}
| protein_bound = 30%<ref name="Bühring_1986">{{cite journal | vauthors = Bühring KU, Sailer H, Faro HP, Leopold G, Pabst J, Garbe A | title = Pharmacokinetics and metabolism of bisoprolol-14C in three animal species and in humans | journal = Journal of Cardiovascular Pharmacology | volume = 8 | issue = Suppl 11 | pages = S21–S28 | year = 1986 | pmid = 2439794 | doi = 10.1097/00005344-198511001-00004 | s2cid = 38147937 }}</ref>
| CAS_number_Ref = {{cascite|correct|??}}
| metabolism = 50% [[肝臟]], 及酵素[[CYP2D6]]和[[CYP3A4]]<ref>{{cite journal | vauthors = Horikiri Y, Suzuki T, Mizobe M | title = Pharmacokinetics and metabolism of bisoprolol enantiomers in humans | journal = Journal of Pharmaceutical Sciences | volume = 87 | issue = 3 | pages = 289–294 | date = March 1998 | pmid = 9523980 | doi = 10.1021/js970316d }}</ref>
| CAS_number = 66722-44-9
| elimination_half-life = 10–12小時<ref name="Leopold_1986">{{cite journal | vauthors = Leopold G | title = Balanced pharmacokinetics and metabolism of bisoprolol | journal = Journal of Cardiovascular Pharmacology | volume = 8 | issue = Suppl 11 | pages = S16–S20 | year = 1986 | pmid = 2439789 | doi = 10.1097/00005344-198511001-00003 | s2cid = 25731558 }}</ref>
| ATC_prefix = C07
| excretion = [[腎]]臟, 糞便 (<2%)
| ATC_suffix = AB07
| PubChem = 2405
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00612
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 2312
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = Y41JS2NL6U
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D02342
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 3127
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 645


<!--Chemical data-->
<!-- Identifiers -->
| CAS_number_Ref = {{cascite|correct|??}}
| C=18 | H=31 | N=1 | O=4
| CAS_number = 66722-44-9
| molecular_weight = 325.443 [[gram|g]]/[[Mole (unit)|mol]]
| PubChem = 2405
| smiles = O(c1ccc(cc1)COCCOC(C)C)CC(O)CNC(C)C
| IUPHAR_ligand = 7129
| InChI = 1/C18H31NO4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4/h5-8,14-15,17,19-20H,9-13H2,1-4H3
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| InChIKey = VHYCDWMUTMEGQY-UHFFFAOYAZ
| DrugBank = DB00612
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| StdInChI = 1S/C18H31NO4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4/h5-8,14-15,17,19-20H,9-13H2,1-4H3
| ChemSpiderID = 2312
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| UNII_Ref = {{fdacite|correct|FDA}}
| StdInChIKey = VHYCDWMUTMEGQY-UHFFFAOYSA-N
| UNII = Y41JS2NL6U
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D02342
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 3127
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 645

<!-- Chemical data -->
| IUPAC_name = (''RS'')-1-{4-[(2-Isopropoxyethoxy)methyl]phenoxy}-<br />3-(isopropylamino)propan-2-ol
| C = 18
| H = 31
| N = 1
| O = 4
| smiles = O(c1ccc(cc1)COCCOC(C)C)CC(O)CNC(C)C
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C18H31NO4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4/h5-8,14-15,17,19-20H,9-13H2,1-4H3
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = VHYCDWMUTMEGQY-UHFFFAOYSA-N
}}
}}


'''畢索洛爾'''（{{lang-en|Bisoprolol}}）以Zebeta、Concor（康肯）等商品名於市面上販售，是一種[[β受體阻滯劑]]，對{{le|β1腎上腺素受體|beta-1 adrenergic receptor}}具選擇性，<ref name=AHFS2016>{{cite web |title=Bisoprolol Fumarate |url=https://www.drugs.com/monograph/bisoprolol-fumarate.html |publisher=The American Society of Health-System Pharmacists |access-date=2016-12-08 |url-status=live |archive-url=https://web.archive.org/web/20161221004751/https://www.drugs.com/monograph/bisoprolol-fumarate.html |archive-date=2016-12-21}}</ref>用於治療[[心血管疾病]]<ref name=AHFS2016/>（包括[[心跳過速]]、[[高血壓]]、[[心絞痛]]和[[心臟衰竭]]<ref name=AHFS2016/>
'''比索洛尔'''（Bisoprolol，商品名：Concor）是一种[[Beta受体阻滞剂]]（beta-blocker)，它可以有选择性的通过阻断[[肾上腺素]]（adrenalin）与[[beta-1受体]]的连接来发挥作用，而不对[[beta-2受体]]产生影响。由于[[beta-1受体]]直接对[[心脏]]产生作用，故此药被分类为cardioselective beta-blockers（只对心脏产生作用的beta受体阻滞剂）<ref>根據文獻記載(Journal of cardiovascular pharmacology 1986;8(Suppl 11):2-15.)：Bisoprolol 為高度beta-1選擇性阻斷劑，對beta-2則幾乎無影響作用，而且對於心血管有作用的腎上腺受體為beta-1，所以藥劑學研究方向也應為beta-1受體阻斷的製劑相關方向</ref>。
<ref>{{cite web |title=Bisoprolol 2.5mg/5mg/10mg film coated tablet - Summary of Product Characteristics (SPC) - (eMC) |url=https://www.medicines.org.uk/emc/medicine/25983 |website=medicines.org.uk |access-date= 2016-12-14 |date=2014-02-18 |url-status=live |archive-url=https://web.archive.org/web/20161220180258/https://www.medicines.org.uk/emc/medicine/25983 |archive-date=2016-12-20}}</ref>）。此藥物係透過[[口服給藥|口服]]方式給藥。<ref name=AHFS2016/>


使用後常見的副作用有[[頭痛]]、疲倦、[[腹瀉]]和腿部腫脹。<ref name=AHFS2016/>較嚴重的副作用有[[氣喘]]惡化、遮蔽辨識[[低血糖]]的能力以及心臟衰竭惡化。 <ref name=Pro2016>{{cite web |title=Bisoprolol - FDA prescribing information, side effects and uses |url=https://www.drugs.com/pro/bisoprolol.html |website=drugs.com |access-date=2016-12-14 |url-status=live |archive-url=https://web.archive.org/web/20161221004233/https://www.drugs.com/pro/bisoprolol.html |archive-date=2016-12-21}}</ref>尚有個體於[[妊娠|懷孕]]期間使用可能會對胎兒有害的疑慮。<ref>{{cite web |title=Bisoprolol (Zebeta) Use During Pregnancy |url=https://www.drugs.com/pregnancy/bisoprolol.html |website=drugs.com |access-date=2016-12-14 |url-status=live |archive-url=https://web.archive.org/web/20161221004229/https://www.drugs.com/pregnancy/bisoprolol.html |archive-date=2016-12-21}}</ref>
此药通常用于暂时降低患者[[血压]]，但请注意，此药只能暂时降低患者血压，并无治愈[[高血压]]的作用。


畢索洛爾於1976年取得專利，並於1986年獲得[[瑞典]]批准用於醫療用途。<ref name=Fis2006>{{cite book | vauthors = Fischer J, Ganellin CR |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=461 |url=https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA461 |url-status=live |archive-url=https://web.archive.org/web/20170908140310/https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA461 |archive-date=2017-09-08}}</ref>於1992年獲得[[美國食品藥物管理局]]（FDA）批准用作醫療用途。<ref name=AHFS2016/>
==作用原理==
[[File:Concor Sales In China.jpg|thumb|250px|在中国大陆销售的富马酸比索洛尔片]]


此藥物已列入[[世界衛生組織基本藥物標準清單]]之中。<ref name="WHO23rd">{{cite book | vauthors = ((World Health Organization)) | title = The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023) | year = 2023 | hdl = 10665/371090 | author-link = World Health Organization | publisher = World Health Organization | location = Geneva | id = WHO/MHP/HPS/EML/2023.02 | hdl-access=free }}</ref>市面上有[[通用名藥物]]販售。<ref name=AHFS2016/><ref>{{Cite web |title=Drugs@FDA: FDA Approved Drug Products |url=http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.Overview&DrugName=BISOPROLOL%20FUMARATE |url-status=live |archive-url=https://web.archive.org/web/20150225122551/http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.Overview&DrugName=BISOPROLOL%20FUMARATE |archive-date=2015-02-25 |access-date=2013-11-13}}</ref>美國於2020年中最常使用的[[處方藥]]中，此藥物排名第267，開立的處方箋數量超過100萬張。<ref>{{cite web |title = The Top 300 of 2020 |url = https://clincalc.com/DrugStats/Top300Drugs.aspx |website = ClinCalc |access-date = 2022-10-07 |archive-date = 2021-02-12 |archive-url = https://web.archive.org/web/20210212142534/https://clincalc.com/DrugStats/Top300Drugs.aspx |url-status = live }}</ref><ref>{{cite web |title = Bisoprolol - Drug Usage Statistics |website = ClinCalc |url = https://clincalc.com/DrugStats/Drugs/Bisoprolol |access-date = 2022-10-07 |archive-date = 2022-09-28 |archive-url = https://web.archive.org/web/20220928031135/https://clincalc.com/DrugStats/Drugs/Bisoprolol |url-status = live }}</ref>
[[肾上腺素]](adrenalin)是一种[[肾上腺]](suprarenal gland)中部分泌的[[荷尔蒙]]（hormone），兴奋[[beta-1受体]]后：加快心跳，升高血糖，有助于甘油三酸酯分解（将甘油三酸酯分解为[[脂肪酸]](fat acid)和[[甘油]](glycerol)），收缩动脉血管直径，升高血压，扩张支气管直径等。


==醫療用途==
而比索洛尔的作用则是阻断[[肾上腺素]]对[[beta-1受体]]的作用，即它对人体的作用正好与肾上腺素相反，如：减慢心跳，舒张动脉血管直径，降低血压，收缩[[冠状动脉]]直径，减慢甘油三酸酯分解，降低血糖。如使用过量，可导致心跳过慢，血压过低，血糖过低，甘油三酸酯过多等等后果。
[[File:000859lg Zebeta 5 MG Oral Tablet.jpg|thumb|right|商品名為Zebeta的畢索洛爾[[片劑]]，每片劑量5毫克。]]


畢索洛爾可用於預防心臟病發作後，有疾病惡化風險的患者再度發生心血管事件、<ref name="Bangalore_2014">{{cite journal | vauthors = Bangalore S, Makani H, Radford M, Thakur K, Toklu B, Katz SD, DiNicolantonio JJ, Devereaux PJ, Alexander KP, Wetterslev J, Messerli FH | display-authors = 6 | title = Clinical outcomes with β-blockers for myocardial infarction: a meta-analysis of randomized trials | journal = The American Journal of Medicine | volume = 127 | issue = 10 | pages = 939–953 | date = October 2014 | pmid = 24927909 | doi = 10.1016/j.amjmed.2014.05.032 | doi-access = free }}</ref>用於治療鬱血性心臟衰竭導致的[[射血分數]]降低<ref>{{cite journal | author = CIBIS-II Investigators | title = The cardiac insufficiency bisoprolol study II (CIBIS-II): a randomised trial. | journal = The Lancet | date = January 1999 | volume = 353 | issue = 9146 | pages = 9–13 | doi = 10.1016/S0140-6736(98)11181-9 | s2cid = 10083527 }}></ref>以及作為治療高血壓的二線藥物。 <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 }}</ref>
==针对症状==


畢索洛爾可能有治療高血壓的功效，但不建議作為一線藥物。對於伴有合併症（例如鬱血性心臟衰竭）的患者，它可作為一線抗高血壓藥物的輔助藥物，對於已服用適當劑量的[[血管紧张素转换酶抑制剂|血管張力素轉化酶抑制劑]]，但仍存在輕度至中度症狀的患者，可添加此種β受體阻滯劑以促進療效。<ref>{{Cite web |title=Clinical information for Hypertension I Heart Foundation |url=https://heartfoundation-prod.azurewebsites.net/bundles/for-professionals/hypertension |access-date=2023-05-13 |website=heartfoundation-prod.azurewebsites.net |archive-date=2022-09-13 |archive-url=https://web.archive.org/web/20220913121141/https://heartfoundation-prod.azurewebsites.net/Bundles/For-Professionals/Hypertension |url-status=dead }}</ref>
* [[高血压]]
* 周期性稳定性[[心绞痛]]


該藥物在{{le|心臟缺血|Coronary ischemia}}時可減少心肌的活動，而減少對氧氣和營養的需求，並在血液供應較少的情況之下仍能輸送足夠量的氧氣和營養以滿足心臟的需求。<ref name=PMID7923660>{{cite journal | author = CIBIS Investigators and Committees | title = A randomized trial of beta-blockade in heart failure. The Cardiac Insufficiency Bisoprolol Study (CIBIS). | journal = Circulation | volume = 90 | issue = 4 | pages = 1765–1773 | date = October 1994 | pmid = 7923660 | doi = 10.1161/01.cir.90.4.1765 | doi-access = free }}</ref><ref name=PMID20354334>{{cite journal | vauthors = Konishi M, Haraguchi G, Kimura S, Inagaki H, Kawabata M, Hachiya H, Hirao K, Isobe M | display-authors = 6 | title = Comparative effects of carvedilol vs bisoprolol for severe congestive heart failure | journal = Circulation Journal | volume = 74 | issue = 6 | pages = 1127–1134 | date = June 2010 | pmid = 20354334 | doi = 10.1253/circj.cj-09-0989 | doi-access = free }}</ref><ref name=PMID20354032>{{cite journal | vauthors = Castagno D, Jhund PS, McMurray JJ, Lewsey JD, Erdmann E, Zannad F, Remme WJ, Lopez-Sendon JL, Lechat P, Follath F, Höglund C, Mareev V, Sadowski Z, Seabra-Gomes RJ, Dargie HJ | display-authors = 6 | title = Improved survival with bisoprolol in patients with heart failure and renal impairment: an analysis of the cardiac insufficiency bisoprolol study II (CIBIS-II) trial | journal = European Journal of Heart Failure | volume = 12 | issue = 6 | pages = 607–616 | date = June 2010 | pmid = 20354032 | doi = 10.1093/eurjhf/hfq038 | s2cid = 205048092 | doi-access = free | hdl = 2318/134969 | hdl-access = free }}</ref>
==以下情况禁止使用此药==

* [[儿童]]或[[未成年人]]。
* [[哺乳期]][[妇女]]
* 不可与[[胺碘酮]]（amiodarone）同时使用


==副作用==
==副作用==
過量使用可導致疲勞、[[低血壓]]、<ref name=PMID20354334/>[[低血糖]]、<ref name="Leopold_1986c"/><ref name="Leopold_1986b"/>[[支氣管痙攣]]和[[心跳過緩]]。發生支氣管痙攣和低血糖是因為體內有高濃度藥物時，可成為位於[[肺]]部和[[肝臟]]的{{le|β2腎上腺素受體|β2 adrenergic receptor}}的拮抗劑。支氣管痙攣是由於肺部β2受體受到阻滯而發生。低血糖是由於肝臟中透過β2受體對[[糖原分解|肝糖分解]]和[[糖質新生]]的刺激減少而發生。<ref name=PMID7923660/><ref name=PMID20354334/><ref name="Hauck_1994">{{cite journal | vauthors = Hauck RW, Schulz C, Emslander HP, Böhm M | title = Pharmacological actions of the selective and non-selective beta-adrenoceptor antagonists celiprolol, bisoprolol and propranolol on human bronchi | journal = British Journal of Pharmacology | volume = 113 | issue = 3 | pages = 1043–1049 | date = November 1994 | pmid = 7858847 | pmc = 1510470 | doi = 10.1111/j.1476-5381.1994.tb17098.x }}</ref>

目前尚無此藥物造成相關臨床明顯藥物性肝損傷的病例報告。<ref name="pmid31643790">{{cite book|pmid=31643790 |date=2012 |title=Bisoprolol }}</ref>

===注意事項===
罹患氣喘或支氣管痙攣的個體應避免使用非選擇性β受體阻滯劑，因為它們可能會引發惡化和症狀加劇。<ref name="Morales_2014">{{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 }}</ref><ref name="Morales_2017">{{cite journal | vauthors = Morales DR, Lipworth BJ, Donnan PT, Jackson C, Guthrie B | title = Respiratory effect of beta-blockers in people with asthma and cardiovascular disease: population-based nested case control study | journal = BMC Medicine | volume = 15 | issue = 1 | pages = 18 | date = January 2017 | pmid = 28126029 | pmc = 5270217 | doi = 10.1186/s12916-017-0781-0 | doi-access = free }}</ref><ref name="Bennett_2021">{{cite journal | vauthors = Bennett M, Chang CL, Tatley M, Savage R, Hancox RJ | title = The safety of cardioselective β1-blockers in asthma: literature review and search of global pharmacovigilance safety reports | journal = ERJ Open Research | volume = 7 | issue = 1 | pages = | date = January 2021 | pmid = 33681344 | pmc = 7917232 | doi = 10.1183/23120541.00801-2020 | url = }}</ref>選擇性β1腎上腺素受體阻斷劑（如畢索洛爾）尚未顯示會導致氣喘惡化，<ref name="Morales_2017" />對於患有心臟合併症的輕至中度氣喘，而已得到控制的患者可謹慎使用。

於2014年所做的一項[[統合分析]]發現，β1腎上腺受體選擇性阻滯劑（畢索洛爾）對肺功能影響很小（與非選擇性β受體阻滯劑比較），患者仍對[[沙丁胺醇]]（[[β2腎上腺素受體激動藥]]）救援治療產生反應，並贊同於選定有氣喘，但已受控制的患者使用畢索洛爾。 <ref name="Morales_2014" /><ref>{{cite journal | vauthors = Loth DW, Brusselle GG, Lahousse L, Hofman A, Leufkens HG, Stricker BH | title = β-Adrenoceptor blockers and pulmonary function in the general population: the Rotterdam Study | journal = British Journal of Clinical Pharmacology | volume = 77 | issue = 1 | pages = 190–200 | date = January 2014 | pmid = 23772842 | doi = 10.1111/bcp.12181 | pmc = 3895360 }}</ref>於2020年所做的一項[[臨床試驗]]支持前述觀點，使用畢索洛爾對個體在沙丁胺醇給藥後，不會對支氣管擴張發生顯著影響。 <ref>{{cite journal | vauthors = Bennett MR, Chang CL, Tuffery C, Hopping S, Hancox RJ | title = The impact of regular bisoprolol on the response to salbutamol in asthma: A double-blind randomized placebo-controlled crossover trial | journal = Respirology | volume = 26 | issue = 3 | pages = 225–232 | date = March 2021 | pmid = 33043552 | doi = 10.1111/resp.13955 | s2cid = 222301890 }}</ref>

==藥理學==
===作用機轉===
畢索洛爾具有心臟保護作用，因為它能選擇性、競爭性阻斷[[兒茶酚胺]]（[[腎上腺素]]）對β1受體（腎上腺素受體）的刺激，β1受體主要存於心肌細胞和[[心臟電傳導系統]]（心臟特有）中，但也存於[[腎]]臟的[[鄰腎小球細胞]]中。<ref name=PMID7923660/>通常腎上腺素和[[正腎上腺素]]對β1受體的刺激會活化[[訊息傳遞 (生物)|訊息傳遞]]級聯，最終分別導致{{le|心肌收縮力|Myocardial contractility }}增加以及心肌和心臟起搏功能增強。<ref name=PMID2564629>{{cite journal | vauthors = Bristow MR, Hershberger RE, Port JD, Minobe W, Rasmussen R | title = Beta 1- and beta 2-adrenergic receptor-mediated adenylate cyclase stimulation in nonfailing and failing human ventricular myocardium | journal = Molecular Pharmacology | volume = 35 | issue = 3 | pages = 295–303 | date = March 1989 | pmid = 2564629 }}</ref>畢索洛爾會競爭性地阻斷該級聯反應的活化，因此降低心肌和心臟起搏細胞的腎上腺素活性/刺激。降低的腎上腺素活性表現為心肌收缩力减弱和心率降低。<ref name="Leopold_1986c">{{cite journal | vauthors = Leopold G, Pabst J, Ungethüm W, Bühring KU | title = Basic pharmacokinetics of bisoprolol, a new highly beta 1-selective adrenoceptor antagonist | journal = Journal of Clinical Pharmacology | volume = 26 | issue = 8 | pages = 616–621 | year = 1986 | pmid = 2878941 | doi = 10.1002/j.1552-4604.1986.tb02959.x | s2cid = 42159046 }}</ref><ref name="Leopold_1986b">{{cite journal | vauthors = Leopold G, Ungethüm W, Pabst J, Simane Z, Bühring KU, Wiemann H | title = Pharmacodynamic profile of bisoprolol, a new beta 1-selective adrenoceptor antagonist | journal = British Journal of Clinical Pharmacology | volume = 22 | issue = 3 | pages = 293–300 | date = September 1986 | pmid = 2876722 | pmc = 1401121 | doi = 10.1111/j.1365-2125.1986.tb02890.x }}</ref><ref name="Haeusler_1986"/>

====β1受體選擇性====
畢索洛爾的β1腎上腺素受體選擇性在與其他非選擇性β腎上腺素受體阻滯劑相比時尤為重要。此藥物的作用僅限於含有β1腎上腺素受體的區域，主要是心臟和部分的腎臟。<ref name="Leopold_1986c" /><ref name="Haeusler_1986"/>雖然β1腎上腺素受體選擇性藥物（如畢索洛爾）可幫助患者避免某些與非選擇性β受體阻滯劑活性相關的副作用<ref name="Leopold_1986" />（作用於其他額外的腎上腺素受體，例如α1和β2），但並不表示它在治療β受體阻滯劑適用心臟疾病（例如心臟衰竭）方面更具優勢，但對於患有特定合併症的患者可能會有益處。<ref name="Taniguchi_2013">{{cite journal | vauthors = Taniguchi T, Ohtani T, Mizote I, Kanzaki M, Ichibori Y, Minamiguchi H, Asano Y, Sakata Y, Komuro I | display-authors = 6 | title = Switching from carvedilol to bisoprolol ameliorates adverse effects in heart failure patients with dizziness or hypotension | journal = Journal of Cardiology | volume = 61 | issue = 6 | pages = 417–422 | date = June 2013 | pmid = 23548374 | doi = 10.1016/j.jjcc.2013.01.009 | doi-access = free }}</ref><ref name="Düngen_2011">{{cite journal | vauthors = Düngen HD, Apostolovic S, Inkrot S, Tahirovic E, Töpper A, Mehrhof F, Prettin C, Putnikovic B, Neskovic AN, Krotin M, Sakac D, Lainscak M, Edelmann F, Wachter R, Rau T, Eschenhagen T, Doehner W, Anker SD, Waagstein F, Herrmann-Lingen C, Gelbrich G, Dietz R | display-authors = 6 | title = Titration to target dose of bisoprolol vs. carvedilol in elderly patients with heart failure: the CIBIS-ELD trial | journal = European Journal of Heart Failure | volume = 13 | issue = 6 | pages = 670–680 | date = June 2011 | pmid = 21429992 | pmc = 3101867 | doi = 10.1093/eurjhf/hfr020 }}</ref>

畢索洛爾比[[阿替洛爾]]、[[美托洛爾]]和{{le|倍他洛爾|betaxolol}}具有更高程度的β1腎上腺素受體選擇性。<ref name="pmid35093388">{{cite journal | vauthors = Muresan L, Cismaru G, Muresan C, Rosu R, Gusetu G, Puiu M, Mada RO, Martins RP | display-authors = 6 | title = Beta-blockers for the treatment of arrhythmias: Bisoprolol - a systematic review | journal = Annales Pharmaceutiques Françaises | volume = 80 | issue = 5 | pages = 617–634 | date = September 2022 | pmid = 35093388 | doi = 10.1016/j.pharma.2022.01.007 | s2cid = 246428722 | url = https://hal.archives-ouvertes.fr/hal-03719705/file/Muresan%20et%20al-2022-Beta%20blockers%20for%20the%20treatment%20of%20arrhythmias.pdf | access-date = 2023-10-26 | archive-date = 2024-04-19 | archive-url = https://web.archive.org/web/20240419035547/https://hal.archives-ouvertes.fr/hal-03719705/file/Muresan%20et%20al-2022-Beta%20blockers%20for%20the%20treatment%20of%20arrhythmias.pdf | url-status = live }}</ref>此藥物對β1受體的選擇性比對β2受體的高出11至15倍。<ref name="Haeusler_1986">{{cite journal | vauthors = Haeusler G, Schliep HJ, Schelling P, Becker KH, Klockow M, Minck KO, Enenkel HJ, Schulze E, Bergmann R, Schmitges CJ | display-authors = 6 | title = High beta 1-selectivity and favourable pharmacokinetics as the outstanding properties of bisoprolol | journal = Journal of Cardiovascular Pharmacology | volume = 8 | issue = Suppl 11 | pages = S2-15 | year = 1986 | pmid = 2439793 | doi = 10.1097/00005344-198511001-00002 | s2cid = 24617470 }}</ref><ref name="Harting_1986">{{cite journal | vauthors = Harting J, Becker KH, Bergmann R, Bourgois R, Enenkel HJ, Fuchs A, Jonas R, Lettenbaur H, Minck KO, Schelling P | display-authors = 6 | title = Pharmacodynamic profile of the selective beta 1-adrenoceptor antagonist bisoprolol | journal = Arzneimittel-Forschung | volume = 36 | issue = 2 | pages = 200–208 | date = February 1986 | pmid = 2870720 }}</ref><ref name="Kaumann_1985">{{cite journal | vauthors = Kaumann AJ, Lemoine H | title = Direct labelling of myocardial beta 1-adrenoceptors. Comparison of binding affinity of 3H-(-)-bisoprolol with its blocking potency | journal = Naunyn-Schmiedeberg's Archives of Pharmacology | volume = 331 | issue = 1 | pages = 27–39 | date = October 1985 | pmid = 2866449 | doi = 10.1007/bf00498849 | s2cid = 22328991 }}</ref><ref name="Klockow_1986">{{cite journal | vauthors = Klockow M, Greiner HE, Haase A, Schmitges CJ, Seyfried C | title = Studies on the receptor profile of bisoprolol | journal = Arzneimittel-Forschung | volume = 36 | issue = 2 | pages = 197–200 | date = February 1986 | pmid = 2870719 }}</ref><ref name="Manalan_1981">{{cite journal | vauthors = Manalan AS, Besch HR, Watanabe AM | title = Characterization of [3H](+/-)carazolol binding to beta-adrenergic receptors. Application to study of beta-adrenergic receptor subtypes in canine ventricular myocardium and lung | journal = Circulation Research | volume = 49 | issue = 2 | pages = 326–336 | date = August 1981 | pmid = 6113900 | doi = 10.1161/01.res.49.2.326 | doi-access = free }}</ref><ref name="Schliep_1986">{{cite journal | vauthors = Schliep HJ, Schulze E, Harting J, Haeusler G | title = Antagonistic effects of bisoprolol on several beta-adrenoceptor-mediated actions in anaesthetized cats | journal = European Journal of Pharmacology | volume = 123 | issue = 2 | pages = 253–261 | date = April 1986 | pmid = 3011461 | doi = 10.1016/0014-2999(86)90666-7 }}</ref><ref name="Schliep_1984">{{cite journal | vauthors = Schliep HJ, Harting J | title = Beta 1-selectivity of bisoprolol, a new beta-adrenoceptor antagonist, in anesthetized dogs and guinea pigs | journal = Journal of Cardiovascular Pharmacology | volume = 6 | issue = 6 | pages = 1156–1160 | year = 1984 | pmid = 6084774 | doi = 10.1097/00005344-198406060-00024 | doi-access = free }}</ref><ref name="Schnabel_2000">{{cite journal | vauthors = Schnabel P, Maack C, Mies F, Tyroller S, Scheer A, Böhm M | title = Binding properties of beta-blockers at recombinant beta1-, beta2-, and beta3-adrenoceptors | journal = Journal of Cardiovascular Pharmacology | volume = 36 | issue = 4 | pages = 466–471 | date = October 2000 | pmid = 11026647 | doi = 10.1097/00005344-200010000-00008 | doi-access = free }}</ref><ref name="Smith_1999">{{cite journal | vauthors = Smith C, Teitler M | title = Beta-blocker selectivity at cloned human beta 1- and beta 2-adrenergic receptors | journal = Cardiovascular Drugs and Therapy | volume = 13 | issue = 2 | pages = 123–126 | date = April 1999 | pmid = 10372227 | doi = 10.1023/A:1007784109255 | s2cid = 12639448 }}</ref><ref name="Wellstein_1986">{{cite journal | vauthors = Wellstein A, Palm D, Belz GG | title = Affinity and selectivity of beta-adrenoceptor antagonists in vitro | journal = Journal of Cardiovascular Pharmacology | volume = 8 | issue = Suppl 11 | pages = S36–S40 | year = 1986 | pmid = 2439796 | doi = 10.1097/00005344-198511001-00006 | s2cid = 30987576 }}</ref>另一種β受體阻滯劑{{le|奈必洛爾|nebivolol}}的β1受體選擇性則約為高出3.5倍。<ref name="Bundkirchen_2003">{{cite journal | vauthors = Bundkirchen A, Brixius K, Bölck B, Nguyen Q, Schwinger RH | title = Beta 1-adrenoceptor selectivity of nebivolol and bisoprolol. A comparison of [3H]CGP 12.177 and [125I]iodocyanopindolol binding studies | journal = European Journal of Pharmacology | volume = 460 | issue = 1 | pages = 19–26 | date = January 2003 | pmid = 12535855 | doi = 10.1016/S0014-2999(02)02875-3 }}</ref><ref name="Nuttall_2003">{{cite journal | vauthors = Nuttall SL, Routledge HC, Kendall MJ | title = A comparison of the beta1-selectivity of three beta1-selective beta-blockers | journal = Journal of Clinical Pharmacy and Therapeutics | volume = 28 | issue = 3 | pages = 179–186 | date = June 2003 | pmid = 12795776 | doi = 10.1046/j.1365-2710.2003.00477.x | s2cid = 58760796 }}</ref>

====腎素-血管張力素系統====
畢索洛爾可抑制[[腎素]]（也稱血管收縮素原酶）分泌約達65%，可抑制心搏過速約達30%。<ref name="Harting_1986"/>


===经常发生===
===藥物動力學===
進入人體的畢索洛爾，其[[生物利用度]]高達約90%，[[生物半衰期]]為10-12小時。<ref name="Leopold_1986c" /><ref name="Leopold_1986b" />循環中的畢索洛爾一半由肝臟代謝，其餘的以原有形式經腎臟排出，約少於2%可能經由糞便排出。<ref name="Leopold_1986c" /><ref name="Leopold_1986b" /><ref name="Haeusler_1986" />


畢索洛爾可溶於[[脂質]]和水。<ref name="Leopold_1986c" /><ref name="Haeusler_1986" />它被歸類為具有中等[[親脂性]]的β受體阻滯劑，因此具有中等穿越[[血腦屏障]]的潛力。<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 (Kaunas) | volume = 57 | issue = 2 | date = February 2021 | page = 155 | pmid = 33572109 | pmc = 7914867 | doi = 10.3390/medicina57020155 | url = | doi-access = free }}</ref>因而畢索洛爾與高親脂性β受體阻滯劑如[[普萘洛爾]]相比，可能會對[[中樞神經系統]]產生較小的的影響，且產生{{le|神經精神|Neuropsychiatry}}副作用的風險較低，相對而言，畢索洛爾比低親脂性β受體阻滯劑如阿替洛爾所產生的影響會較較大。<ref name="pmid33572109" />
* 血液循环系统：身体发冷，指尖或手指、脚趾发麻。如果患者跛脚，跛脚症状可能加重。
* 神经系统：感觉无力、疲惫、发晕。（通常会轻微的发生在疗程开始的前两个星期，然后会消失）
* 消化系统：恶心、呕吐、腹痛、[[腹泻]]、[[便秘]]iiiii


畢索洛爾與血漿蛋白結合率約為35%，分佈容積為3.5升/公斤，總清除率約15升/小時 。畢索洛爾經兩種方式從人體排除 - 50%在肝臟中轉化為無活性的代謝物，然後經腎臟排泄。其餘50%則經由腎臟以藥物原形排除。<ref>{{Cite web |title=Bisoprolol |url=https://go.drugbank.com/drugs/DB00612 |access-date=2022-08-17 |website=go.drugbank.com |archive-date=2022-08-17 |archive-url=https://web.archive.org/web/20220817143701/https://go.drugbank.com/drugs/DB00612 |url-status=live }}</ref>由於肝臟和腎臟的消除相同，因此肝或是腎功能不全的患者無需調整劑量。
===偶尔发生===


此藥物的[[藥物代謝動力學]]呈線性，且與年齡無關。<ref name="Leopold_1986" />
* [[肌肉]]虚弱、[[痉挛]]、无力。
* 血液循环系统：心跳过慢，[[低血压]]，加重心脏不足。（尤其是过量使用此药时发生）
* 神经系统：[[抑郁]]，[[失眠]]或睡眠不规律。
* 呼吸系统：患有[[哮喘]]的患者不建议使用此药。


在各項研究中，發現慢性心臟衰竭患者血漿中畢索洛爾的濃度高於健康受試者，生物半衰期也較長。目前尚缺乏此藥物於健康受試者和慢性心臟衰竭受試者之間的藥物代謝動力學直接比較證據。<ref>{{cite journal | vauthors = Kirch W, Rose I, Demers HG, Leopold G, Pabst J, Ohnhaus EE | title = Pharmacokinetics of bisoprolol during repeated oral administration to healthy volunteers and patients with kidney or liver disease | journal = Clinical Pharmacokinetics | volume = 13 | issue = 2 | pages = 110–117 | date = August 1987 | pmid = 2887325 | doi = 10.2165/00003088-198713020-00003 | s2cid = 25105692 }}</ref><ref>{{cite journal | vauthors = Cvan Trobec K, Grabnar I, Kerec Kos M, Vovk T, Trontelj J, Anker SD, Rosano G, Lainscak M | display-authors = 6 | title = Bisoprolol pharmacokinetics and body composition in patients with chronic heart failure: a longitudinal study | journal = European Journal of Clinical Pharmacology | volume = 72 | issue = 7 | pages = 813–822 | date = July 2016 | pmid = 26996442 | doi = 10.1007/s00228-016-2041-1 | s2cid = 14146663 }}</ref>
===罕见===


==社會與文化==
* [[神经]]系统：做恶梦，发生幻象。
===品牌名稱===
* 皮肤：[[皮肤]]接触神经过于敏感。
此藥物在印度以Bisotab品牌銷售。<ref>{{cite web |url=https://medicaldialogues.in/partner/jbcpl/bisotab-bisoprolol-fumarate-tablets |title=Bisotab-Physician Information Page |publisher=Medical Dialogues |date=2020-08-22 |access-date=2020-08-22 |archive-date=2020-08-09 |archive-url=https://web.archive.org/web/20200809225634/https://medicaldialogues.in/partner/jbcpl/bisotab-bisoprolol-fumarate-tablets |url-status=live }}</ref>於市面上的其他品牌尚有Cardicor, Congescor<ref>{{cite web| url =https://www.nhs.uk/medicines/bisoprolol/ |title =Bisoprolol| publisher =NHS | date = | accessdate = 2024-05-21 }}</ref>及Bisoprolol-ratiopharm<ref>{{cite web| url =https://www.ratiopharm.de/produkte/details/bisoprolol-ratiopharm-2-5-mg-tabletten-pzn-10330069.html|title =Bisoprolol-ratiopharm| publisher =ratiopharm | date = | accessdate = 2024-05-21 }}</ref>等。
* [[肝]]：[[ALAT]],[[ASAT]]两种[[酶]]的分泌增加
* [[新陈代谢]]：[[甘油三酸酯]](triglyceride)（脂肪）增加，[[血糖]]过低。
* 生殖系统：[[阳萎]]
* [[眼]]：[[眼泪]]分泌降低（如果患者配戴眼镜，请医生注意此项）
* [[耳]]：听觉下降。


==註解==
== 參考文獻 ==
{{reflist}}
{{Reflist|2}}


{{Β受体阻滞剂}}
{{模板:Β受體阻滯劑}}
{{Merck Serono|state=autocollapse}}
{{Portal bar|Medicine}}
{{Authority control}}


[[Category:Β阻滞药]]
[[分類:Β阻滯藥]]
[[Category:N-异丙基苯氧基丙醇胺]]
[[分類:N-異丙基苯氧基丙醇胺]]
[[分類:世界衛生組織基本藥物]]
[[分類:RTT]]
[[Category:Peripherally selective drugs]]
[[Category:Drugs developed by Merck]]

2024年5月29日 (三) 00:49的版本

毕索洛尔
臨床資料
商品名（英语：Drug nomenclature）Zebeta、Monocor及其他
AHFS/Drugs.comMonograph
MedlinePlusa693024
懷孕分級
  • 澳: C
给药途径口服給藥
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度>90%
血漿蛋白結合率30%[4]
药物代谢50% 肝臟, 及酵素CYP2D6和CYP3A4[6]
生物半衰期10–12小時[5]
排泄途徑腎臟, 糞便 (<2%)
识别信息
  • (RS)-14-[(2-Isopropoxyethoxy)methyl]phenoxy
    3-(isopropylamino)propan-2-ol
CAS号66722-44-9  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
ECHA InfoCard100.108.941 編輯維基數據鏈接
化学信息
化学式C18H31NO4
摩尔质量325.45 g·mol−1
3D模型（JSmol（英语：JSmol））
手性外消旋體
  • O(c1ccc(cc1)COCCOC(C)C)CC(O)CNC(C)C
  • InChI=1S/C18H31NO4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4/h5-8,14-15,17,19-20H,9-13H2,1-4H3 checkY
  • Key:VHYCDWMUTMEGQY-UHFFFAOYSA-N checkY

畢索洛爾（英語：Bisoprolol）以Zebeta、Concor（康肯）等商品名於市面上販售，是一種β受體阻滯劑，對β1腎上腺素受體（英语：beta-1 adrenergic receptor）具選擇性，[7]用於治療心血管疾病[7]（包括心跳過速、高血壓、心絞痛和心臟衰竭[7] [8]）。此藥物係透過口服方式給藥。[7]

使用後常見的副作用有頭痛、疲倦、腹瀉和腿部腫脹。[7]較嚴重的副作用有氣喘惡化、遮蔽辨識低血糖的能力以及心臟衰竭惡化。 [9]尚有個體於懷孕期間使用可能會對胎兒有害的疑慮。[10]

畢索洛爾於1976年取得專利，並於1986年獲得瑞典批准用於醫療用途。[11]於1992年獲得美國食品藥物管理局（FDA）批准用作醫療用途。[7]

此藥物已列入世界衛生組織基本藥物標準清單之中。[12]市面上有通用名藥物販售。[7][13]美國於2020年中最常使用的處方藥中，此藥物排名第267，開立的處方箋數量超過100萬張。[14][15]

醫療用途

商品名為Zebeta的畢索洛爾片劑，每片劑量5毫克。

畢索洛爾可用於預防心臟病發作後，有疾病惡化風險的患者再度發生心血管事件、[16]用於治療鬱血性心臟衰竭導致的射血分數降低[17]以及作為治療高血壓的二線藥物。 [18]

畢索洛爾可能有治療高血壓的功效，但不建議作為一線藥物。對於伴有合併症（例如鬱血性心臟衰竭）的患者，它可作為一線抗高血壓藥物的輔助藥物，對於已服用適當劑量的血管張力素轉化酶抑制劑，但仍存在輕度至中度症狀的患者，可添加此種β受體阻滯劑以促進療效。[19]

該藥物在心臟缺血（英语：Coronary ischemia）時可減少心肌的活動，而減少對氧氣和營養的需求，並在血液供應較少的情況之下仍能輸送足夠量的氧氣和營養以滿足心臟的需求。[20][21][22]

副作用

過量使用可導致疲勞、低血壓、[21]低血糖、[23][24]支氣管痙攣和心跳過緩。發生支氣管痙攣和低血糖是因為體內有高濃度藥物時，可成為位於肺部和肝臟的β2腎上腺素受體（英语：β2 adrenergic receptor）的拮抗劑。支氣管痙攣是由於肺部β2受體受到阻滯而發生。低血糖是由於肝臟中透過β2受體對肝糖分解和糖質新生的刺激減少而發生。[20][21][25]

目前尚無此藥物造成相關臨床明顯藥物性肝損傷的病例報告。[26]

注意事項

罹患氣喘或支氣管痙攣的個體應避免使用非選擇性β受體阻滯劑，因為它們可能會引發惡化和症狀加劇。[27][28][29]選擇性β1腎上腺素受體阻斷劑（如畢索洛爾）尚未顯示會導致氣喘惡化，[28]對於患有心臟合併症的輕至中度氣喘，而已得到控制的患者可謹慎使用。

於2014年所做的一項統合分析發現，β1腎上腺受體選擇性阻滯劑（畢索洛爾）對肺功能影響很小（與非選擇性β受體阻滯劑比較），患者仍對沙丁胺醇（β2腎上腺素受體激動藥）救援治療產生反應，並贊同於選定有氣喘，但已受控制的患者使用畢索洛爾。 [27][30]於2020年所做的一項臨床試驗支持前述觀點，使用畢索洛爾對個體在沙丁胺醇給藥後，不會對支氣管擴張發生顯著影響。 [31]

藥理學

作用機轉

畢索洛爾具有心臟保護作用，因為它能選擇性、競爭性阻斷兒茶酚胺（腎上腺素）對β1受體（腎上腺素受體）的刺激，β1受體主要存於心肌細胞和心臟電傳導系統（心臟特有）中，但也存於腎臟的鄰腎小球細胞中。[20]通常腎上腺素和正腎上腺素對β1受體的刺激會活化訊息傳遞級聯，最終分別導致心肌收縮力（英语：Myocardial contractility）增加以及心肌和心臟起搏功能增強。[32]畢索洛爾會競爭性地阻斷該級聯反應的活化，因此降低心肌和心臟起搏細胞的腎上腺素活性/刺激。降低的腎上腺素活性表現為心肌收缩力减弱和心率降低。[23][24][33]

β1受體選擇性

畢索洛爾的β1腎上腺素受體選擇性在與其他非選擇性β腎上腺素受體阻滯劑相比時尤為重要。此藥物的作用僅限於含有β1腎上腺素受體的區域，主要是心臟和部分的腎臟。[23][33]雖然β1腎上腺素受體選擇性藥物（如畢索洛爾）可幫助患者避免某些與非選擇性β受體阻滯劑活性相關的副作用[5]（作用於其他額外的腎上腺素受體，例如α1和β2），但並不表示它在治療β受體阻滯劑適用心臟疾病（例如心臟衰竭）方面更具優勢，但對於患有特定合併症的患者可能會有益處。[34][35]

畢索洛爾比阿替洛爾、美托洛爾和倍他洛爾（英语：betaxolol）具有更高程度的β1腎上腺素受體選擇性。[36]此藥物對β1受體的選擇性比對β2受體的高出11至15倍。[33][37][38][39][40][41][42][43][44][45]另一種β受體阻滯劑奈必洛爾（英语：nebivolol）的β1受體選擇性則約為高出3.5倍。[46][47]

腎素-血管張力素系統

畢索洛爾可抑制腎素（也稱血管收縮素原酶）分泌約達65%，可抑制心搏過速約達30%。[37]

藥物動力學

進入人體的畢索洛爾，其生物利用度高達約90%，生物半衰期為10-12小時。[23][24]循環中的畢索洛爾一半由肝臟代謝，其餘的以原有形式經腎臟排出，約少於2%可能經由糞便排出。[23][24][33]

畢索洛爾可溶於脂質和水。[23][33]它被歸類為具有中等親脂性的β受體阻滯劑，因此具有中等穿越血腦屏障的潛力。[48]因而畢索洛爾與高親脂性β受體阻滯劑如普萘洛爾相比，可能會對中樞神經系統產生較小的的影響，且產生神經精神（英语：Neuropsychiatry）副作用的風險較低，相對而言，畢索洛爾比低親脂性β受體阻滯劑如阿替洛爾所產生的影響會較較大。[48]

畢索洛爾與血漿蛋白結合率約為35%，分佈容積為3.5升/公斤，總清除率約15升/小時 。畢索洛爾經兩種方式從人體排除 - 50%在肝臟中轉化為無活性的代謝物，然後經腎臟排泄。其餘50%則經由腎臟以藥物原形排除。[49]由於肝臟和腎臟的消除相同，因此肝或是腎功能不全的患者無需調整劑量。

此藥物的藥物代謝動力學呈線性，且與年齡無關。[5]

在各項研究中，發現慢性心臟衰竭患者血漿中畢索洛爾的濃度高於健康受試者，生物半衰期也較長。目前尚缺乏此藥物於健康受試者和慢性心臟衰竭受試者之間的藥物代謝動力學直接比較證據。[50][51]

社會與文化

品牌名稱

此藥物在印度以Bisotab品牌銷售。[52]於市面上的其他品牌尚有Cardicor, Congescor[53]及Bisoprolol-ratiopharm[54]等。

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β, 非选择性
β1选择性
β2选择性
α1+β选择性
描述
疾病
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规范控制数据库：各地 編輯維基數據鏈接
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