LAUSR

BACKGROUND Nobel laureate Sir James Black's molecule, propranolol, still has broad acceptance in cardiovascular diseases, infantile haemangiomas and anxiety. A comprehensive and systematic review of the literature for the summarization of pharmacokinetic parameters would be effective in order to explore the new safe uses of propranolol in different scenarios, without exposing humans and using virtual-human modeling approaches. OBJECTIVE This review encompasses physico-chemical properties, pharmacokinetics and drug-drug interaction data of propranolol collected from various studies. METHOD Clinical pharmacokinetic studies on propranolol were screened using Medline and Google scholar's 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 2.5-fold increase in the area under the curve, 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 in order to establish physiologically based pharmacokinetic modeling among the diseased population.