Matches in SemOpenAlex for { <https://semopenalex.org/work/W2029388610> ?p ?o ?g. }
- W2029388610 endingPage "200" @default.
- W2029388610 startingPage "190" @default.
- W2029388610 abstract "Chlorzoxazone is metabolized by cytochrome P450 2E1 (CYP2E1) to a single oxidized metabolite, 6-hydroxychlorzoxazone. The aim of the study was to test the robustness of chlorzoxazone as an in vivo probe of CYP2E1 activity in humans, with emphasis on investigating short-term and long-term intra-individual variabilities and effects of different doses of the drug. In addition, the influences of body build, drug metabolizing enzyme genotype, blood sampling time, and moderate recent ethanol intake were investigated.The 6-hydroxychlorzoxazone:chlorzoxazone (metabolic) ratio in plasma was measured at 2 h in 28 male and nine female volunteers following a single oral dose of 500 mg chlorzoxazone. Similarly, the metabolic ratios at 4 h and 6 h were measured in 20 of the males. The metabolic ratio at 2 h was also determined 1.5 and 2.5 years later in 13 and seven males, respectively, and weekly for 3 weeks in seven males, after a dose of 500 mg, once at higher (750 mg) and lower (250 mg) doses, and once (500 mg) following moderate ethanol intake (0.5 g kg(-1) body weight) the preceding evening. Genotypes were determined for CYP2E1 as well as for N-acetyltransferase 2 and glutathione transferase M1.Excluding an outlier (ratio = 1.6) the metabolic ratio at 2 h ranged from 0.12 to 0.61 (n = 36). A positive correlation with body weight (r = 0.61, P < 0.001) suggested dose-dependent metabolism of chlorzoxazone. The metabolic ratio decreased with increasing chlorzoxazone dose (P = 0.01), again suggesting dose-dependent metabolism. Long-term (yearly intervals) and short-term (weekly intervals) intra- and interindividual variabilities in metabolic ratio were similar (30% and 63%vs 28% and 54%, respectively). Both inter- and intra-individual variabilities tended to decrease with increasing dose of chlorzoxazone. There was no significant influence of moderate ethanol intake the preceding evening, or of CYP2E1 genotype on the metabolic ratio.The relatively low intra-individual variability in the metabolism of chlorzoxazone suggests that a single-sample procedure may suffice to assess CYP2E1 activity in vivo. However, chlorzoxazone metabolism is dose-dependent at commonly used doses and it is therefore advisable to adjust the dose for body weight. Moderate intake of ethanol the preceding evening did not significantly affect the chlorzoxazone metabolic ratio." @default.
- W2029388610 created "2016-06-24" @default.
- W2029388610 creator A5001274275 @default.
- W2029388610 creator A5037623399 @default.
- W2029388610 creator A5055249382 @default.
- W2029388610 date "2004-06-04" @default.
- W2029388610 modified "2023-10-14" @default.
- W2029388610 title "Robustness of chlorzoxazone as an in vivo measure of cytochrome P450 2E1 activity" @default.
- W2029388610 cites W1505123413 @default.
- W2029388610 cites W1919753724 @default.
- W2029388610 cites W1923851271 @default.
- W2029388610 cites W1969499833 @default.
- W2029388610 cites W1971617741 @default.
- W2029388610 cites W1974472457 @default.
- W2029388610 cites W1975628073 @default.
- W2029388610 cites W1982375487 @default.
- W2029388610 cites W1983418892 @default.
- W2029388610 cites W1988292500 @default.
- W2029388610 cites W1989312960 @default.
- W2029388610 cites W1991239772 @default.
- W2029388610 cites W2004489118 @default.
- W2029388610 cites W2009954357 @default.
- W2029388610 cites W2029978452 @default.
- W2029388610 cites W2036232979 @default.
- W2029388610 cites W2039182670 @default.
- W2029388610 cites W2043108970 @default.
- W2029388610 cites W2045768784 @default.
- W2029388610 cites W2059293500 @default.
- W2029388610 cites W2064308700 @default.
- W2029388610 cites W2071313746 @default.
- W2029388610 cites W2073959427 @default.
- W2029388610 cites W2076589905 @default.
- W2029388610 cites W2080251006 @default.
- W2029388610 cites W2083676370 @default.
- W2029388610 cites W2084735442 @default.
- W2029388610 cites W2084937360 @default.
- W2029388610 cites W2086008118 @default.
- W2029388610 cites W2098528905 @default.
- W2029388610 cites W2108124990 @default.
- W2029388610 cites W2118094114 @default.
- W2029388610 cites W2124345456 @default.
- W2029388610 cites W2129256163 @default.
- W2029388610 cites W2130694306 @default.
- W2029388610 cites W2135748830 @default.
- W2029388610 cites W2140338711 @default.
- W2029388610 cites W2143498897 @default.
- W2029388610 cites W2148946238 @default.
- W2029388610 cites W2152709536 @default.
- W2029388610 cites W2254345563 @default.
- W2029388610 cites W2419391152 @default.
- W2029388610 cites W2428192919 @default.
- W2029388610 doi "https://doi.org/10.1111/j.1365-2125.2004.02132.x" @default.
- W2029388610 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/1884585" @default.
- W2029388610 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/15255802" @default.
- W2029388610 hasPublicationYear "2004" @default.
- W2029388610 type Work @default.
- W2029388610 sameAs 2029388610 @default.
- W2029388610 citedByCount "40" @default.
- W2029388610 countsByYear W20293886102012 @default.
- W2029388610 countsByYear W20293886102013 @default.
- W2029388610 countsByYear W20293886102015 @default.
- W2029388610 countsByYear W20293886102016 @default.
- W2029388610 countsByYear W20293886102017 @default.
- W2029388610 countsByYear W20293886102018 @default.
- W2029388610 countsByYear W20293886102019 @default.
- W2029388610 countsByYear W20293886102020 @default.
- W2029388610 countsByYear W20293886102021 @default.
- W2029388610 countsByYear W20293886102022 @default.
- W2029388610 countsByYear W20293886102023 @default.
- W2029388610 crossrefType "journal-article" @default.
- W2029388610 hasAuthorship W2029388610A5001274275 @default.
- W2029388610 hasAuthorship W2029388610A5037623399 @default.
- W2029388610 hasAuthorship W2029388610A5055249382 @default.
- W2029388610 hasBestOaLocation W20293886101 @default.
- W2029388610 hasConcept C126322002 @default.
- W2029388610 hasConcept C134018914 @default.
- W2029388610 hasConcept C140027455 @default.
- W2029388610 hasConcept C185592680 @default.
- W2029388610 hasConcept C2776658834 @default.
- W2029388610 hasConcept C2777477808 @default.
- W2029388610 hasConcept C526171541 @default.
- W2029388610 hasConcept C55493867 @default.
- W2029388610 hasConcept C62231903 @default.
- W2029388610 hasConcept C71924100 @default.
- W2029388610 hasConcept C98274493 @default.
- W2029388610 hasConceptScore W2029388610C126322002 @default.
- W2029388610 hasConceptScore W2029388610C134018914 @default.
- W2029388610 hasConceptScore W2029388610C140027455 @default.
- W2029388610 hasConceptScore W2029388610C185592680 @default.
- W2029388610 hasConceptScore W2029388610C2776658834 @default.
- W2029388610 hasConceptScore W2029388610C2777477808 @default.
- W2029388610 hasConceptScore W2029388610C526171541 @default.
- W2029388610 hasConceptScore W2029388610C55493867 @default.
- W2029388610 hasConceptScore W2029388610C62231903 @default.
- W2029388610 hasConceptScore W2029388610C71924100 @default.
- W2029388610 hasConceptScore W2029388610C98274493 @default.
- W2029388610 hasIssue "2" @default.
- W2029388610 hasLocation W20293886101 @default.