Clinical Pharmacokinetics of Propranolol Hydrochloride: A Review.

Abstract:

BACKGROUND: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. OBJECTIVE:This review encompasses physicochemical properties, pharmacokinetics and drug-drug interaction data of propranolol collected from various studies. METHODS: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. RESULTS: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. CONCLUSION:Physiochemical and pooled pharmacokinetic parameters of propranolol are beneficial to establish physiologically based pharmacokinetic modeling among the diseased population.

journal_name

Curr Drug Metab

journal_title

Current drug metabolism

authors

Kalam MN,Rasool MF,Rehman AU,Ahmed N

doi

10.2174/1389200221666200414094644

subject

Has Abstract

pub_date

2020-01-01 00:00:00

pages

89-105

issue

2

eissn

1389-2002

issn

1875-5453

pii

CDM-EPUB-105789

journal_volume

21

pub_type

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