Rofecoxib is a potent inhibitor of cytochrome P450 1A2: studies with tizanidine and caffeine in healthy subjects

JT Backman, MJ Karjalainen… - British journal of …, 2006 - Wiley Online Library
… may produce a modest inhibition of cytochrome P450 (CYP) 1A2’[4]. However, the findings
of the present study with caffeine and tizanidine indicate that rofecoxib is a potent inhibitor of …

Rofecoxib is a potent, metabolism-dependent inhibitor of CYP1A2: implications for in vitro prediction of drug interactions

MJ Karjalainen, PJ Neuvonen, JT Backman - Drug metabolism and …, 2006 - ASPET
… on tizanidine pharmacokinetics suggest that rofecoxib can … In the in vivo studies with healthy
volunteers, rofecoxib (25 mg … Rofecoxib has inhibited the metabolism of caffeine in healthy

[PDF][PDF] Inhibition of CYP1A2-mediated drug metabolism in vitro and in humans: With special emphasis on rofecoxib and other NSAIDs

M Karjalainen - 2008 - helda.helsinki.fi
Rofecoxib is a potent inhibitor of cytochrome P450 1A2: studies with tizanidine and caffeine
in healthy subjects… The purpose of this study was to investigate the effect of rofecoxib, several …

Celecoxib is a CYP1A2 inhibitor in vitro but not in vivo

MJ Karjalainen, PJ Neuvonen, JT Backman - European journal of clinical …, 2008 - Springer
… We recently discovered that rofecoxib is a potent mechanism-based inhibitor of … to humans,
does not inhibit the metabolism of tizanidine or the formation of paraxanthine from caffeine, …

Metabolism and mechanism of human cytochrome P450 enzyme 1A2

J Guo, X Zhu, S Badawy, A Ihsan, Z Liu… - Current Drug …, 2021 - ingentaconnect.com
… The interaction between tizanidine and CYP1A2 inhibitors has … Studies have also shown
that furafylline reduces caffeine … and explored the inhibitory effect of rofecoxib on CYP1A2. The …

Physiologically based pharmacokinetic modeling of altered tizanidine systemic exposure by CYP1A2 modulation: impact of drug-drug interactions and cigarette …

VK Jogiraju, T Heimbach, Y Toderika, DR Taft - Drug Metabolism and …, 2021 - Elsevier
Tizanidine is more sensitive than caffeine and theophylline as a probe substrate for … time
profile for tizanidine (upper panel) and rofecoxib (lower panel) in healthy volunteers. Included in …

Insights into the substrate specificity, inhibitors, regulation, and polymorphisms and the clinical impact of human cytochrome P450 1A2

SF Zhou, LP Yang, ZW Zhou, YH Liu, E Chan - The AAPS journal, 2009 - Springer
… (6-hydroxylation) and tizanidine (oxidation) are also used as … enzyme activity as measured
by the rate of caffeine 3-… patients (n = 75) and healthy volunteers (n = 159). Among asthmatic …

Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development

B Wang, SF Zhou - Current medicinal chemistry, 2009 - ingentaconnect.com
… data of 21 naturally occurring flavonoids against caffeine N … studies have demonstrated
that typical CYP1A2 inhibitors are … the major excretory route for tizanidine and its metabolites, …

Tolfenamic acid is a potent CYP1A2 inhibitor in vitro but does not interact in vivo: correction for protein binding is needed for data interpretation

MJ Karjalainen, PJ Neuvonen, JT Backman - European journal of clinical …, 2007 - Springer
… The nonsteroidal anti-inflammatory drug (NSAID) rofecoxib … of tizanidine after a single 4-mg
oral dose in 10 healthy subjects, … tizanidine concentration or the caffeine test in humans. …

Structure, function, regulation and polymorphism and the clinical significance of human cytochrome P450 1A2

SF Zhou, B Wang, LP Yang, JP Liu - Drug metabolism reviews, 2010 - Taylor & Francis
Rofecoxib also increased the urinary excretion of tizanidine … of tizanidine and its metabolite
M3 in healthy volunteers (n = … no significant effect on the caffeine-paraxanthine ratio. Since …