Department of Pharmacy, Quaid-i-Azam University, 45320, Islamabad, Pakistan.
Pharmacy Practice Department, Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan.
Curr Drug Metab. 2020;21(2):89-105. doi: 10.2174/1389200221666200414094644.
Nobel laureate Sir James Black's molecule, propranolol, still has broad potential in cardiovascular diseases, infantile haemangiomas and anxiety. A comprehensive and systematic review of the literature for the summarization of pharmacokinetic parameters would be effective to explore the new safe uses of propranolol in different scenarios, without exposing humans and using virtual-human modeling approaches.
This review encompasses physicochemical properties, pharmacokinetics and drug-drug interaction data of propranolol collected from various studies.
Clinical pharmacokinetic studies on propranolol were screened using Medline and Google Scholar databases. Eighty-three clinical trials, in which pharmacokinetic profiles and plasma time concentration were available after oral or IV administration, were included in the review.
The study depicts that propranolol is well absorbed after oral administration. It has dose-dependent bioavailability, and a 2-fold increase in dose results in a 2.5-fold increase in the area under the curve, a 1.3-fold increase in the time to reach maximum plasma concentration and finally, 2.2 and 1.8-fold increase in maximum plasma concentration in both immediate and long-acting formulations, respectively. Propranolol is a substrate of CYP2D6, CYP1A2 and CYP2C19, retaining potential pharmacokinetic interactions with co-administered drugs. Age, gender, race and ethnicity do not alter its pharmacokinetics. However, in renal and hepatic impairment, it needs a dose adjustment.
Physiochemical and pooled pharmacokinetic parameters of propranolol are beneficial to establish physiologically based pharmacokinetic modeling among the diseased population.
诺贝尔奖得主詹姆斯·布莱克爵士的分子普萘洛尔在心血管疾病、婴儿血管瘤和焦虑症方面仍有广泛的应用潜力。对文献进行全面、系统的回顾，总结药代动力学参数，有助于在不暴露于人体的情况下，利用虚拟人体建模方法，探索普萘洛尔在不同情况下的新的安全用途。
本综述涵盖了从各种研究中收集到的普萘洛尔的理化性质、药代动力学和药物相互作用数据。
使用 Medline 和 Google Scholar 数据库筛选关于普萘洛尔的临床药代动力学研究。纳入了 83 项临床试验，这些试验提供了口服或静脉给药后的药代动力学特征和血浆时间浓度。
研究表明，普萘洛尔口服吸收良好。它具有剂量依赖性的生物利用度，剂量增加两倍会导致曲线下面积增加 2.5 倍，达峰时间增加 1.3 倍，最大血浆浓度分别增加 2.2 倍和 1.8 倍，无论是即刻释放还是长效制剂。普萘洛尔是 CYP2D6、CYP1A2 和 CYP2C19 的底物，与合用药物存在潜在的药代动力学相互作用。年龄、性别、种族和民族不会改变其药代动力学。然而，在肾功能和肝功能受损的情况下，需要调整剂量。
普萘洛尔的理化和汇总药代动力学参数有助于在患病人群中建立基于生理学的药代动力学模型。
