Pharmacokinetics of oral talinolol following a single dose and during steady state in patients with chronic renal failure and healthy volunteers

Determination of talinolol in human plasma by high performance liquid chromatography–electrospray ionization mass spectrometry: Application to pharmacokinetic study

“…All study procedures have been standardized as well as possible with regard to duration of fasting, physical activity, and body position during the period of absorption. Under these conditions, the pharmacokinetic results of the study (AUC, C max , t max , t 1/2 ) were similar to the dose-adjusted results with single oral 100 mg talinolol by other authors [11,18]. The mean plasma concentration versus time profiles after a single oral dose of 50 mg of talinolol is shown in Fig.…”

“…However, even if this compound has fewer undesirable side effects, it can lead to typical side effects, such as bradycardia, hypotension, bronchoconstriction, aggravation of cardiac failure, etc., overdose of beta-blockers may lead to life-threatening situations [6][7][8]. In conditions of renal impairment or comedication with inhibitors or inducers of p-glycoprotein [9][10][11][12][13][14][15], routine therapeutic drug monitoring (TDM) seemed to be useful, furthermore, TDM is a useful tool for determination of noncompliance. So, the development of a rapid and specific method allowing the screening and the determination of this compound in biologic fluids could be of great interest either in therapeutic drug monitoring use or in toxicologic screening in the case of suicide involving this compound [3].…”

Physiologically-based modelling in mice suggests an aggravated loss of clearance capacity after toxic liver damage

“…In humans, around 55% of talinolol is excreted unchanged in the urine 21 . In contrast, several metabolites were identified in the urine after talinolol administration in mice 22 .…”

A Systematic Evaluation of the Use of Physiologically Based Pharmacokinetic Modeling for Cross-Species Extrapolation

“…Only pravastatin and talinolol are taken up into liver cells by active transport and are excreted mostly unchanged in urine or in feces. 28,65 Note that only processes that substantially contribute to the metabolism or elimination of a drug were taken into account, whereas all others were neglected to limit the structural complexity of the models. In all PBPK models, tissuespecific gene expression was used to estimate the relative protein abundance in various tissues and organs.…”