Insights into the structure, function, and regulation of human cytochrome P450 1A2

SF Zhou, LP Yang, MQ Wei, W Duan… - Current drug …, 2009 - ingentaconnect.com
Rofecoxib at therapeutic doses of 25 mg perday increased more … did not affect the kinetics
of caffeine and tizanidine [206]. … : studies with tizanidine and caffeine in healthy subjects. Br. J…

Update on tizanidine for muscle spasticity and emerging indications

G Malanga, RD Reiter, E Garay - Expert Opinion on …, 2008 - Taylor & Francis
… The cytochrome P450 enzyme CYP1A2 primarily … In an open-label study of tizanidine (4
mg daily), 53.8% of patients with … , rofecoxib, rifampicin and recreational smoking Citation[66-69]. …

[HTML][HTML] Cytochrome P450 family 1 inhibitors and structure-activity relationships

J Liu, J Sridhar, M Foroozesh - Molecules, 2013 - mdpi.com
… design of selective P450 1A2 inhibitors as well as to study this enzyme’s active site cavity. …
) of caffeine in healthy volunteers [58]. Furafylline is a potent inhibitor of P450 1A2 phenacetin …

A practical overview of tizanidine use for spasticity secondary to multiple sclerosis, stroke, and spinal cord injury

L Kamen, HR Henney III, JD Runyan - Current medical research …, 2008 - Taylor & Francis
… (PK) trials, off-label use, and data on healthy volunteers further … that tizanidine is mainly
metabolized by cytochrome P450 … and rofecoxib have a major effect on tizanidine kinetics, …

Prediction of inter-individual variability on the pharmacokinetics of CYP1A2 substrates in non-smoking healthy volunteers

K Haraya, M Kato, K Chiba, Y Sugiyama - Drug Metabolism and …, 2016 - Elsevier
… In this study, caffeine, tizanidine, and phenacetin were selected as typical CYP1A2 substrates.
First, the CV of CL int,h of CYP1A2 substrates was estimated from the AUC/Dose (AUC/D) …

Interindividual differences in caffeine metabolism and factors driving caffeine consumption

A Nehlig - Pharmacological reviews, 2018 - ASPET
… of cytochrome P450, which metabolizes 95% of the caffeine … In healthy humans, caffeine
is apparently eliminated via first-… of the research available is concentrated on caffeine and, to …

Computational and in vitro studies on the inhibitory effects of herbal compounds on human cytochrome P450 1A2

LP Yang, ZW Zhou, XW Chen, CG Li, KB Sneed… - Xenobiotica, 2012 - Taylor & Francis
… ciprofloxacin (a CYP1A2 inhibitor) and tizanidine (a CYP1A2 … in this study included
acetaminophen, amitriptyline, caffeine, … model using 5 potent inhibitors of CYP1A2 and validated it …

Assessment of the CYP1A2 Inhibition-Mediated Drug Interaction Potential for Pinocembrin Using In Silico, In Vitro, and In Vivo Approaches

S Bhatt, S Dhiman, V Kumar, A Gour, D Manhas… - ACS …, 2022 - ACS Publications
… drugs, namely, caffeine and tacrine. In conclusion, pinocembrin has a … Rofecoxib
increased the plasma concentration of the CYP1A2 substrate tizanidine by 13.6-fold in humans

[PDF][PDF] Interactions of tizanidine with CYP1A2 enzyme inhibitors: Studies in vitro and in humans

M Granfors - 2005 - helda.helsinki.fi
… is also crucial for its elimination but the cytochrome P450 (CYP) enzymes … in healthy
volunteers, and (3) correlate tizanidine … effects of tizanidine were measured and a caffeine test, for …

Understanding interindividual variability in the drug interaction of a highly extracted CYP1A2 substrate tizanidine: application of a permeability-limited …

M Zhang, C Fisher, I Gardner, X Pan, P Kilford… - Drug Metabolism and …, 2022 - ASPET
… , it was observed that the subjects in this study were associated with … ) Rofecoxib is a potent
inhibitor of cytochrome P450 1A2: studies with tizanidine and caffeine in healthy subjects. Br …