PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 23370523-0 2013 [Clinical survey of tizanidine-induced adverse effects--impact of concomitant drugs providing cytochrome P450 1A2 modification--]. tizanidine 20-30 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 94-113 23370523-5 2013 Tizanidine-induced adverse effects were examined in 100 patients treated with coadministration of tizanidine and 8 CYP1A2 inhibitors. tizanidine 0-10 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 115-121 23370523-8 2013 The present results suggest that coadministration of tizanidine and CYP1A2 inhibitors enhances tizanidine-induced adverse effects, especially in elderly patients treated with a higher dose of tizanidine. tizanidine 95-105 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 68-74 23370523-8 2013 The present results suggest that coadministration of tizanidine and CYP1A2 inhibitors enhances tizanidine-induced adverse effects, especially in elderly patients treated with a higher dose of tizanidine. tizanidine 95-105 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 68-74 19961320-1 2010 Human CYP1A2 is one of the major CYPs in human liver and metabolizes a number of clinical drugs (e.g., clozapine, tacrine, tizanidine, and theophylline; n > 110), a number of procarcinogens (e.g., benzo[a]pyrene and aromatic amines), and several important endogenous compounds (e.g., steroids). tizanidine 123-133 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 6-12 19789372-1 2010 The aim of this study was to determine whether mexiletine, a CYP1A2 inhibitor, altered the pharmacokinetics and pharmacodynamics of tizanidine. tizanidine 132-142 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 61-67 19590965-1 2009 Human CYP1A2 is one of the major CYPs in human liver and metabolizes a variety of clinically important drugs (e.g., clozapine, tacrine, tizanidine, and theophylline), a number of procarcinogens (e.g. benzo[a]pyrene and aflatoxin B(1)), and several important endogenous compounds (e.g. steroids and arachidonic acids). tizanidine 136-146 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 6-12 18816299-1 2008 The cytochrome P450 enzyme CYP1A2 is crucial for the metabolism of many drugs, for example, tizanidine. tizanidine 92-102 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 27-33 19754423-5 2009 Typical CYP1A2 substrates generally contain planar ring that can fit the narrow and planar active site of the enzyme, such as propranolol, clozapine, guanabenz, flutamide, imatinib, thalidomide, carbamazepine, lidocaine, theophylline, tacrine, tizanidine, zolpidem, riluzole, zileuton, and leflunomide. tizanidine 244-254 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 8-14 17618427-6 2007 On day 3, each ingested 4 mg of the CYP1A2 substrate tizanidine. tizanidine 53-63 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 36-42 17955229-0 2008 Effects of gender and moderate smoking on the pharmacokinetics and effects of the CYP1A2 substrate tizanidine. tizanidine 99-109 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 82-88 17955229-1 2008 OBJECTIVE: We studied the effects of gender and smoking on the pharmacokinetics and effects of the cytochrome P450 (CYP) 1A2 substrate tizanidine. tizanidine 135-145 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 99-124 16198659-0 2005 Oral contraceptives containing ethinyl estradiol and gestodene markedly increase plasma concentrations and effects of tizanidine by inhibiting cytochrome P450 1A2. tizanidine 118-128 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 143-162 16934051-1 2006 AIMS: Case reports suggest an interaction between rofecoxib and the CYP1A2 substrate tizanidine. tizanidine 85-95 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 68-74 16985100-1 2006 Rofecoxib was recently found to greatly increase plasma concentrations of the CYP1A2 substrate drug tizanidine in humans, but there are no published in vitro studies on the CYP1A2-inhibiting effects of rofecoxib. tizanidine 100-110 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 78-84 16198659-14 2005 CONCLUSIONS: OCs containing ethinyl estradiol and gestodene increase, to a clinically significant extent, the plasma concentrations and effects of tizanidine, probably mainly by inhibiting its CYP1A2-mediated presystemic metabolism. tizanidine 147-157 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 193-199 15592331-0 2004 Ciprofloxacin greatly increases concentrations and hypotensive effect of tizanidine by inhibiting its cytochrome P450 1A2-mediated presystemic metabolism. tizanidine 73-83 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 102-121 15592331-1 2004 BACKGROUND AND OBJECTIVE: Tizanidine, a centrally acting skeletal muscle relaxant, is metabolized mainly by cytochrome P450 (CYP) 1A2 and has a low oral bioavailability. tizanidine 26-36 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 108-133 15592331-12 2004 Tizanidine seems to be a useful probe drug for measuring presystemic metabolism by CYP1A2. tizanidine 0-10 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 83-89 14998432-0 2004 Tizanidine is mainly metabolized by cytochrome p450 1A2 in vitro. tizanidine 0-10 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 36-55 15060511-5 2004 A caffeine test was performed on day 3 to examine the role of cytochrome P450 (CYP) 1A2 in tizanidine pharmacokinetics. tizanidine 91-101 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 62-87 15060511-12 2004 Inhibition of tizanidine-metabolizing enzyme(s), mainly CYP1A2, by fluvoxamine seems to explain the observed interaction. tizanidine 14-24 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 56-62 14998432-8 2004 Recombinant CYP1A2 metabolized tizanidine to a substantial degree (35% in 45 min), but other recombinant CYPs had little metabolic capacity for the drug. tizanidine 31-41 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 12-18 14998432-9 2004 CONCLUSIONS: CYP1A2 is primarily responsible for the metabolism of tizanidine. tizanidine 67-77 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 13-19 33404754-1 2021 PURPOSE: Tizanidine, an alpha-adrenergic substance with antinociceptive and antihypertensive effects, is extensively metabolized via cytochrome P450 (CYP) 1A2. tizanidine 9-19 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 133-158 35504655-0 2022 Understanding Inter-individual Variability in the Drug Interaction of a Highly Extracted CYP1A2 Substrate Tizanidine: Application of a Permeability-limited Multi-compartment Liver Model in a Population Based PBPK Framework. tizanidine 106-116 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 89-95 35504655-1 2022 Tizanidine, a centrally acting skeletal muscle relaxant, is predominantly metabolised by CYP1A2 and undergoes extensive hepatic first-pass metabolism following oral administration. tizanidine 0-10 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 89-95 35504655-2 2022 As a highly extracted drug, the systemic exposure to tizanidine exhibits considerable inter-individual variability and is altered substantially when co-administered with CYP1A2 inhibitors or inducers. tizanidine 53-63 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 170-176 35504655-4 2022 Physiologically-based pharmacokinetic (PBPK) models were developed for tizanidine, incorporating the PerMCL model and the WSM, respectively, to simulate the interaction of tizanidine with a range of CYP1A2 inhibitors and inducers. tizanidine 71-81 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 199-205 35504655-4 2022 Physiologically-based pharmacokinetic (PBPK) models were developed for tizanidine, incorporating the PerMCL model and the WSM, respectively, to simulate the interaction of tizanidine with a range of CYP1A2 inhibitors and inducers. tizanidine 172-182 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 199-205 30223305-7 2019 In conclusion, CYP1A2 inhibition increases the risk of hypotensive episodes associated with the use of tizanidine in routine clinical practice. tizanidine 103-113 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 15-21 33561738-0 2021 Physiologically based pharmacokinetic modeling of altered tizanidine systemic exposure by CYP1A2 modulation: Impact of drug-drug interactions and cigarette consumption. tizanidine 58-68 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 90-96 33561738-2 2021 Tizanidine is primarily metabolized by CYP1A2 and is considered a sensitive index substrate for this enzyme. tizanidine 0-10 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 39-45 33561738-3 2021 The physiologically based pharmacokinetic (PBPK) modeling platform Simcyp was used to evaluate the impact of CYP1A2 modulation on tizanidine exposure through drug-drug interactions (DDIs) and host-dependent habits (cigarette smoking). tizanidine 131-141 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 110-116 33561738-6 2021 The model was then used to carry-out DDI simulations to predict alterations in tizanidine systemic exposure when co-administered with various CYP1A2 perpetrators including competitive inhibitors (fluvoxamine, ciprofloxacin), a mechanism-based inhibitor (rofecoxib), and an inducer (rifampin). tizanidine 79-89 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 142-148 33561738-8 2021 Under each scenario, the PBPK model was able to capture the observed fold changes in tizanidine Cmax and AUC of tizanidine when coadministered with CYP1A2 inhibitors or inducers. tizanidine 85-95 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 148-154 33561738-8 2021 Under each scenario, the PBPK model was able to capture the observed fold changes in tizanidine Cmax and AUC of tizanidine when coadministered with CYP1A2 inhibitors or inducers. tizanidine 112-122 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 148-154 33302490-0 2020 A Physiologically-Based Pharmacokinetic (PBPK) Model Network for the Prediction of CYP1A2 and CYP2C19 Drug-Drug-Gene Interactions with Fluvoxamine, Omeprazole, S-mephenytoin, Moclobemide, Tizanidine, Mexiletine, Ethinylestradiol, and Caffeine. tizanidine 188-198 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 83-89 32311241-0 2020 Effect of Vemurafenib on the Pharmacokinetics of a Single Dose of Tizanidine (a CYP1A2 Substrate) in Patients With BRAFV600 Mutation-Positive Malignancies. tizanidine 66-76 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 80-86 30223305-1 2019 Tizanidine, a widely used muscle relaxant that can lower blood pressure, is metabolized by the cytochrome P450 1A2 (CYP1A2). tizanidine 0-10 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 95-114 30223305-1 2019 Tizanidine, a widely used muscle relaxant that can lower blood pressure, is metabolized by the cytochrome P450 1A2 (CYP1A2). tizanidine 0-10 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 116-122 27318879-5 2016 Then, this estimated CV was validated by predicting the CVs of AUC/Dose of tizanidine and phenacetin, which are mainly metabolized by CYP1A2 and have negligible renal clearance. tizanidine 75-85 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 134-140