INT50403

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Context Info
Confidence 0.59
First Reported 1995
Last Reported 2010
Negated 0
Speculated 2
Reported most in Abstract
Documents 55
Total Number 57
Disease Relevance 8.97
Pain Relevance 17.79

This is a graph with borders and nodes. Maybe there is an Imagemap used so the nodes may be linking to some Pages.

small molecule metabolic process (CYP2C19) oxidoreductase activity (CYP2C19) endoplasmic reticulum (CYP2C19)
enzyme binding (CYP2C19)
Anatomy Link Frequency
liver 5
plasma 2
hepatocytes 1
urine 1
CYP2C19 (Homo sapiens)
Pain Link Frequency Relevance Heat
Dextromethorphan 8 100.00 Very High Very High Very High
fluoxetine 116 99.84 Very High Very High Very High
carbamazepine 28 99.52 Very High Very High Very High
sSRI 125 99.28 Very High Very High Very High
methadone 218 99.24 Very High Very High Very High
Versed 6 98.78 Very High Very High Very High
Angina 6 96.12 Very High Very High Very High
tricyclic antidepressant 50 95.84 Very High Very High Very High
withdrawal 85 94.80 High High
Opioid 186 94.36 High High
Disease Link Frequency Relevance Heat
Toxicity 260 99.70 Very High Very High Very High
Liver Disease 10 96.80 Very High Very High Very High
Cv General 3 Under Development 4 96.12 Very High Very High Very High
Opiate Addiction 33 94.80 High High
Arrhythmia Under Development 39 94.24 High High
Depression 162 92.36 High High
Hypersomnia 99 92.36 High High
Apnoea 30 92.12 High High
Sprains And Strains 19 91.68 High High
Cv Unclassified Under Development 6 91.64 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Since both drugs are metabolised primarily by CYP2C19 in human liver microsomes, they are both useful, competitive inhibitors of CYP2C19 activity available to researchers working in vitro.
Negative_regulation (inhibitors) of CYP2C19 in liver
1) Confidence 0.59 Published 1995 Journal Clin Pharmacokinet Section Abstract Doc Link 8846622 Disease Relevance 0 Pain Relevance 0.07
A number of drugs have been shown to inhibit CYP2C19 in vivo, including fluvoxamine and fluoxetine.
Negative_regulation (inhibit) of CYP2C19 associated with fluoxetine
2) Confidence 0.59 Published 1995 Journal Clin Pharmacokinet Section Abstract Doc Link 8846622 Disease Relevance 0 Pain Relevance 0.10
Important drug interactions may result from inhibition of hepatic CYP2C19 activity in extensive metabolisers or from the interaction of CYP2C19 substrates with other pathways in poor metabolisers.
Negative_regulation (inhibition) of CYP2C19
3) Confidence 0.59 Published 1995 Journal Clin Pharmacokinet Section Abstract Doc Link 8846622 Disease Relevance 0 Pain Relevance 0.10
CYP2C19 inhibition: the impact of substrate probe selection on in vitro inhibition profiles.
Negative_regulation (inhibition) of CYP2C19
4) Confidence 0.59 Published 2008 Journal Drug Metab. Dispos. Section Title Doc Link 18048485 Disease Relevance 0 Pain Relevance 0.12
Racemic fluoxetine also demonstrates time- and concentration-dependent inhibition of CYP2C19 catalytic activity in vitro.
Negative_regulation (inhibition) of CYP2C19 associated with fluoxetine
5) Confidence 0.59 Published 2009 Journal Drug Metab. Dispos. Section Abstract Doc Link 19144769 Disease Relevance 0.18 Pain Relevance 0.65
Differential time- and NADPH-dependent inhibition of CYP2C19 by enantiomers of fluoxetine.
Negative_regulation (inhibition) of CYP2C19 associated with fluoxetine
6) Confidence 0.59 Published 2009 Journal Drug Metab. Dispos. Section Title Doc Link 19144769 Disease Relevance 0.18 Pain Relevance 0.65
These data suggest that, in this patient, phenytoin toxicity was caused by inhibition of CYP2C19 by ticlopidine, and the data emphasize the importance of CYP2C19 in the metabolism of phenytoin.
Negative_regulation (inhibition) of CYP2C19 associated with toxicity
7) Confidence 0.58 Published 1997 Journal Clin. Pharmacol. Ther. Section Abstract Doc Link 9390115 Disease Relevance 0.25 Pain Relevance 0.07
Ticlopidine inhibition of phenytoin metabolism mediated by potent inhibition of CYP2C19.
Negative_regulation (inhibition) of CYP2C19
8) Confidence 0.58 Published 1997 Journal Clin. Pharmacol. Ther. Section Title Doc Link 9390115 Disease Relevance 0.25 Pain Relevance 0.10
For omeprazole, the highest concentration at which >70% inhibition of CYP2C19 was observed with no significant inhibitory effect on other isoforms was at least 20 times greater than K(i).
Negative_regulation (inhibition) of CYP2C19
9) Confidence 0.58 Published 1997 Journal Drug Metab. Dispos. Section Abstract Doc Link 9224780 Disease Relevance 0 Pain Relevance 0.08
Since its inhibition is very potent and has a broad "window of selectivity," omeprazole seems to be a useful, selective inhibitor of CYP2C19.
Negative_regulation (inhibitor) of CYP2C19
10) Confidence 0.58 Published 1997 Journal Drug Metab. Dispos. Section Abstract Doc Link 9224780 Disease Relevance 0 Pain Relevance 0.17
Dose-dependent inhibition of CYP1A2, CYP2C19 and CYP2D6 by citalopram, fluoxetine, fluvoxamine and paroxetine.
Negative_regulation (inhibition) of CYP2C19 associated with fluoxetine
11) Confidence 0.58 Published 1996 Journal Eur. J. Clin. Pharmacol. Section Title Doc Link 8880055 Disease Relevance 0 Pain Relevance 0.28
CONCLUSION: This investigation confirms that paroxetine and fluoxetine are potent inhibitors of CYP2D6, that fluvoxamine and fluoxetine are moderate inhibitors of CYP2C19 and that fluvoxamine is a potent inhibitor of CYP1A2 in humans in vivo.
Negative_regulation (inhibitors) of CYP2C19
12) Confidence 0.58 Published 1996 Journal Eur. J. Clin. Pharmacol. Section Body Doc Link 8880055 Disease Relevance 0 Pain Relevance 0
Fluvoxamine is a potent inhibitor of CYP1A2 and CYP2C19 and a moderate inhibitor of CYP2C9.
Negative_regulation (inhibitor) of CYP2C19
13) Confidence 0.57 Published 2004 Journal Therapie Section Abstract Doc Link 15199661 Disease Relevance 0 Pain Relevance 0.60
Inhibition assays demonstrated that tilidine and nortilidine can also inhibit CYP3A4, CYP2C19, CYP2D6, ABCB1, but not ABCG2, whereas inhibition of CYP2D6 and possibly also of CYP3A4 might be clinically relevant.
Negative_regulation (inhibit) of CYP2C19
14) Confidence 0.57 Published 2008 Journal Naunyn Schmiedebergs Arch. Pharmacol. Section Abstract Doc Link 18516595 Disease Relevance 0 Pain Relevance 0.11
Fluoxetine and fluvoxamine are moderate inhibitors of CYP2C19 ('S-mephenytoinhydroxylase'), and fluvoxamine might also be a moderate inhibitor of CYP2C9.
Negative_regulation (inhibitors) of CYP2C19 associated with fluoxetine
15) Confidence 0.57 Published 1996 Journal Int Clin Psychopharmacol Section Abstract Doc Link 8732441 Disease Relevance 0 Pain Relevance 0.49
Topiramate is not devoid of potential interaction properties: it decreases the plasma concentrations of ethinylestradiol, induces CYP3A4 and inhibits CYP2C19.
Negative_regulation (inhibits) of CYP2C19 in plasma
16) Confidence 0.56 Published 2000 Journal Fundam Clin Pharmacol Section Abstract Doc Link 11030437 Disease Relevance 0 Pain Relevance 0.26
Fluvoxamine interacts with these drugs by a mechanism involving inhibition of CYP1A2, CYP3A4, and CYP2C19.
Negative_regulation (inhibition) of CYP2C19
17) Confidence 0.55 Published 1995 Journal Int Clin Psychopharmacol Section Abstract Doc Link 7622807 Disease Relevance 0 Pain Relevance 0.65
Fluoxetine increases the plasma concentrations of alprazolam and diazepam by inhibiting CYP3A and CYP2C19, respectively.
Negative_regulation (inhibiting) of CYP2C19 in plasma associated with fluoxetine
18) Confidence 0.53 Published 1997 Journal Clin Pharmacokinet Section Abstract Doc Link 9435993 Disease Relevance 0 Pain Relevance 0.73
Fluoxetine dosing inhibited CYP2C19 activity in both age groups, increasing the (S)- to (R)-mephenytoin ratio 3- to 4-fold (p < .01).
Negative_regulation (inhibited) of CYP2C19 associated with fluoxetine
19) Confidence 0.52 Published 2001 Journal J Clin Psychopharmacol Section Abstract Doc Link 11270912 Disease Relevance 0 Pain Relevance 0.80
Renzapride did not inhibit the major CYP drug-metabolizing enzymes CYP2C9, CYP2D6, CYP1A2, CYP2A6, CYP2C19, CYP2E1 or CYP3A4 at concentrations consistent with use in a clinical setting.
Negative_regulation (inhibit) of CYP2C19
20) Confidence 0.51 Published 2008 Journal Drugs R D Section Body Doc Link 18095752 Disease Relevance 0 Pain Relevance 0

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