卡维地洛
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临床资料 | |
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商品名 | Coreg及其他 |
其他名称 | BM-14190 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a697042 |
核准状况 | |
给药途径 | 口服给药 |
ATC码 | |
法律规范状态 | |
法律规范 |
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药物动力学数据 | |
生物利用度 | 25–35% |
血浆蛋白结合率 | 98% |
药物代谢 | 肝脏 (细胞色素CYP2D6及CYP2C9) |
生物半衰期 | 7–10小时 |
排泄途径 | 尿液 (16%), 粪便 (60%) |
识别信息 | |
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CAS号 | 72956-09-3 ![]() |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
PDB配体ID | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.117.236 |
化学信息 | |
化学式 | C24H26N2O4 |
摩尔质量 | 406.48 g·mol−1 |
3D模型(JSmol) | |
手性 | 外消旋体 |
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卡维地洛(英语:Carvedilol)以Coreg等商品名于市面贩售,是种用于治疗高血压、郁血性心脏衰竭 (CHF) 和左心室功能障碍的药物。[1]此药物于治疗高血压时通常是作为一种二线药物。[1]
使用后常见的副作用有头晕、疲倦、关节痛、低血压、恶心和呼吸困难。[1]严重的副作用有支气管痉挛。[1]个体于怀孕期间使用对于胎儿的安全,或个体进行母乳哺育时对于婴儿的安全尚未有充分的数据以供研究。[2]不建议罹患肝病的人使用。[3]卡维地洛是一种非选择性β受体阻滞剂,并具有选择性α-1受体阻滞剂的活性。[1]此药物发生作用的机制尚未被完全了解,但涉及的可能是血管舒张的结果。[1]
卡维地洛于1978年获得专利,并于1995年被美国食品药物管理局(FDA)核准作医疗用途。[1][4]它已被列入世界卫生组织基本药物标准清单中。[5]目前市面上有通用名药物贩售。[1]它于美国2021年最常使用处方药中排名第26,开立的处方笺数量超过2,100万张。[6][7]
医疗用途
[编辑]卡维地洛适用于郁血性心脏衰竭 (CHF)的治疗,通常作为血管张力素转化酶抑制剂 (ACE抑制剂) ,及利尿剂的辅助药物。临床证明它可降低CHF患者的死亡率和住院率。[8]卡维地洛治疗心脏衰竭的机制在于它能抑制交感神经系统中的受体(此系统会释放正肾上腺素至全身,包括心脏)。[9]正肾上腺素是一种可使心脏跳动更快、更努力运作的激素。[9]阻断正肾上腺素与心脏中受体的结合可导致血管舒张,降低心率和血压,并改善心肌收缩力,[10]最终把心脏的负荷降低。[9]
卡维地洛可降低心脏病发作后患者因心脏功能下降而致的死亡、住院和心脏病复发的风险。[11][12]卡维地洛也被证明可减少严重心脏衰竭患者的死亡和住院率。[13]
卡维地洛在一般医疗过程中已被用于治疗单纯性高血压,但研究显示它与其他降血压药物或是其他β受体阻滞剂相比,降血压的效果会相对较低。[14]
卡维地洛也具有预防肝硬化患者因食道静脉曲张发生流血的功效。[15]
配方形式
[编辑]卡维地洛的配方形式有:
禁忌症
[编辑]患有支气管气喘或支气管痉挛的患者不应使用卡维地洛,因为此药物会升高支气管收缩的风险。[18][19]患有二度或三度房室传导阻滞、窦房结功能障碍(心脏传导疾病 )、严重心跳过缓(除非个体安装有永久性心律调节器)或失代偿性心脏病(即心脏衰竭)的患者也不应使用此药物。有严重肝功能损害的患者应谨慎使用。[20][21][22]
副作用
[编辑]卡维地洛导致的副作用中最常见的(发生率 >10%)有:[16]
不建议患有恶化型支气管痉挛疾病(例如目前有气喘症状)的人使用卡维地洛,因为它会阻断有助于打开气道的受体。[16]
卡维地洛可能会将低血糖症状掩盖,[16]导致糖尿病低血糖症发生却不自觉的情况(低血糖无自觉症状)。这情况被称为β受体阻滞剂引起的低血糖无自觉症状。糖尿病低血糖症是指糖尿病患者的血糖水平低于正常范围(低血糖),它是急诊室和医院最常遇到的低血糖原因之一。根据美国国家电子伤害监测系统 - 全方位伤害程序 (National Electronic Injury Surveillance System-All Injury Program, NEISS-AIP) 的数据,美国在2004年至2005年之间抽样调查的案例中,估计有55,819起病例 (占总住院人数的8.0%) 与胰岛素使用有关联,其中严重低血糖症可能是最常见的一种结果。[23]
与其他药物交互作用
[编辑]如果将此药物与胺碘酮、地高辛、地尔硫䓬、伊伐布雷定或维拉帕米一起使用,会增加心跳过慢的风险。[24]此外,卡维地洛与非1,4-二氢吡啶类钙通道阻滞剂(包括地尔硫䓬和维拉帕米)组合使用,可增强其心脏抑制作用。[24]
药理学
[编辑]药效学
[编辑]卡维地洛既是一种非选择性β受体阻滞剂(β1与β2),也是一种选择性α-1受体阻滞剂(α1)。[1]
卡维地洛可阻断α-1受体,导致血管舒张。这种抑制作用造成周边血管阻力降低,而产生抗高血压作用。由于卡维地洛会阻断心脏中的β1受体,而停止产生反射性心跳过速反应。[25]
药物动力学
[编辑]口服卡维地洛后,由于广泛的首过代谢,药物的生物利用度约为25%至35%。饮食期间服用会将药物吸收减慢,但生物利用度无显著差异。给药期间同时进食可降低姿位性低血压的风险。[16]
大部分卡维地洛与血浆蛋白结合(主要是人类血清白蛋白),可达98%。卡维地洛是一种脂溶性药物,在动物实验中容易穿过血脑屏障。因此它不像是一些只会作用于外周组织(人体中枢神经系统以外的所有组织和器官)的药物。[26][27]
参考文献
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延伸阅读
[编辑]- Chakraborty S, Shukla D, Mishra B, Singh S. Clinical updates on carvedilol: a first choice beta-blocker in the treatment of cardiovascular diseases. Expert Opinion on Drug Metabolism & Toxicology. February 2010, 6 (2): 237–50. PMID 20073998. S2CID 25670550. doi:10.1517/17425250903540220.
- Dean L. Carvedilol Therapy and CYP2D6 Genotype. Pratt VM, McLeod HL, Rubinstein WS, et al (编). Medical Genetics Summaries. National Center for Biotechnology Information (NCBI). 2018 [2024-05-17]. PMID 30067327. Bookshelf ID: NBK518573. (原始内容存档于2020-10-26).
外部链接
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