Dubai Health Authority, P.O. Box: 4545, Dubai, United Arab Emirates.
Department of Pharmacology, J.K.K. Nattraja College of Pharmacy, Komarapalayam 638 183, India.
Curr Drug Metab. 2021;22(9):672-682. doi: 10.2174/1389200222666210614112529.
Adrenergic β-blockers are used to treat many conditions, including hypertension, cardiac arrhythmias, heart failure, angina pectoris, migraine, and tremors. The majority of the β-blockers including Propranolol, Metoprolol, Acebutolol, Alprenolol, Betaxolol, Carvedilol, Nebivolol and Oxprenolol are metabolised majorly by CYP2D6, and Bisoprolol is primarily metabolised by CYP3A4 enzymes. The drugs inhibiting or inducing them may alter the pharmacokinetics of those β-blockers. The plasma concentrations of Propranolol might be elevated by the concomitant use of drugs, such as SSRIs (Fluoxetine, Paroxetine), SNRIs (Duloxetine) and Cimetidine, while the plasma concentrations of Metoprolol increased by the concurrent use of SSRIs (Fluoxetine, Paroxetine), Amiodarone, Celecoxib, Cimetidine, Terbinafine, and Diphenhydramine. β-blockers can also interact pharmacodynamically with drugs, including fluoroquinolones, antidiabetic agents and NSAIDs. In addition, β-blockers may interact with herbs, such as curcumin, Ginkgo biloba, Schisandra chinensis, green tea, guggul, hawthorn, St. John's wort and Yohimbine. This article focuses on clinically relevant drug interactions of β-blockers with commonly prescribed medications. In addition to Pharmacokinetics and Pharmacodynamics of the drug interactions, recommendations for clinical practice are highlighted. The prescribers and the pharmacists are needed to be aware of the drugs interacting with β-blockers to prevent possible adverse drug interactions.
肾上腺素能β受体阻滞剂用于治疗多种疾病,包括高血压、心律失常、心力衰竭、心绞痛、偏头痛和震颤。大多数β受体阻滞剂,包括普萘洛尔、美托洛尔、醋丁洛尔、阿普洛尔、倍他洛尔、卡维地洛、比索洛尔和氧烯洛尔,主要通过 CYP2D6 代谢,而比索洛尔主要通过 CYP3A4 酶代谢。抑制或诱导这些酶的药物可能会改变这些β受体阻滞剂的药代动力学。同时使用药物(如 SSRIs[氟西汀、帕罗西汀]、SNRIs[度洛西汀]和西咪替丁)可使普萘洛尔的血浆浓度升高,而同时使用 SSRIs[氟西汀、帕罗西汀]、胺碘酮、塞来昔布、西咪替丁、特比萘芬和苯海拉明可使美托洛尔的血浆浓度升高。β受体阻滞剂还可以与药物发生药效学相互作用,包括氟喹诺酮类药物、抗糖尿病药物和 NSAIDs。此外,β受体阻滞剂可能与草药相互作用,如姜黄素、银杏叶、五味子、绿茶、古柯、山楂、贯叶连翘和育亨宾。本文重点介绍β受体阻滞剂与常用药物的临床相关药物相互作用。除了药物相互作用的药代动力学和药效动力学外,还强调了临床实践建议。需要医生和药剂师注意与β受体阻滞剂相互作用的药物,以防止可能发生的药物相互作用。