PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 32867117-6 2020 The potency of codeine and loperamide is strongly dependent on the individual enzymatic activity of CYP2D6 and CYP3A4, as well as P-glycoprotein function. Loperamide 27-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 111-117 31299239-6 2019 In vitro, axitinib inhibited loperamide metabolism with the IC50 of 18.34 muM for RLM, 1.705 muM for HLM and 1.604 muM for CYP3A4*1, and it was confirmed as a non-competitive inhibitor in all enzymes. Loperamide 29-39 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 123-129 31571937-0 2019 Functional characteristics of CYP3A4 allelic variants on the metabolism of loperamide in vitro. Loperamide 75-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-36 31571937-2 2019 Loperamide, identified as a CYP3A4 substrate, is prone to misuse and abuse and has high risks of life-threatening cardiotoxicity. Loperamide 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 28-34 31571937-3 2019 Methods: Thus, this study is designed to evaluate the enzymatic characteristics of 29 CYP3A4 alleles toward loperamide in vitro, including the 7 novel CYP3A4 variants (*28-*34). Loperamide 108-118 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-92 31571937-6 2019 Conclusion: As the first study to identify the properties of these CYP3A4 variants toward loperamide metabolism, our investigation may establish the genotype-phenotype relationship for loperamide, predict an individual"s capability in response to loperamide, and provide some guidance of clinical medication and treatment for loperamide. Loperamide 90-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-73 31571937-6 2019 Conclusion: As the first study to identify the properties of these CYP3A4 variants toward loperamide metabolism, our investigation may establish the genotype-phenotype relationship for loperamide, predict an individual"s capability in response to loperamide, and provide some guidance of clinical medication and treatment for loperamide. Loperamide 185-195 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-73 31571937-6 2019 Conclusion: As the first study to identify the properties of these CYP3A4 variants toward loperamide metabolism, our investigation may establish the genotype-phenotype relationship for loperamide, predict an individual"s capability in response to loperamide, and provide some guidance of clinical medication and treatment for loperamide. Loperamide 185-195 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-73 31571937-6 2019 Conclusion: As the first study to identify the properties of these CYP3A4 variants toward loperamide metabolism, our investigation may establish the genotype-phenotype relationship for loperamide, predict an individual"s capability in response to loperamide, and provide some guidance of clinical medication and treatment for loperamide. Loperamide 185-195 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-73 31116446-3 2019 Cytochrome P-450 (CYP)2C8, CYP3A, and P-glycoprotein inhibitors can increase the plasma and central nervous system concentrations and radically alter the risk profile of loperamide. Loperamide 170-180 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-32 28594339-13 2019 Three patients were concomitantly taking cimetidine, which is known to cause inhibition of CYP3A4 and CYP2C8 leading to increased levels of loperamide. Loperamide 140-150 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 91-97 29237391-3 2018 METHODS: It was found that, for CYP3A4/5 substrates such as midazolam, amprenavir and loperamide, in vitro metabolic clearance is generally lower in enterocytes compared to that of hepatocytes, which is consistent with the relative abundance of the enzyme between the intestine and liver. Loperamide 86-96 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 29237391-7 2018 As expected, ketoconazole inhibited CYP3A4/5-mediated metabolite formation in enterocytes for midazolam, amprenavir and loperamide, suggesting that cryopreserved enterocytes may be useful in determining intestinal CYP3A inhibition parameters. Loperamide 120-130 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-42 29237391-8 2018 Interestingly, elacridar, a P-gp inhibitor, suppressed metabolite formation in enterocytes for loperamide, a substrate of CYP3A4 and P-gp, suggesting that enterocytes in suspension do not have active P-gp efflux functions, and the suppression of metabolism in enterocytes is probably caused by inhibition of CYP3A4/5 by elacridar. Loperamide 95-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 122-128 18192961-8 2007 Loperamide is metabolized by the cytochrome P450 (CYP) system and is a substrate for the CYP3A4 isoenzyme. Loperamide 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 18192961-9 2007 Concurrent administration with CYP3A4 inhibitors may elevate loperamide concentrations. Loperamide 61-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37