INT10797

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Context Info
Confidence 0.48
First Reported 1991
Last Reported 2011
Negated 6
Speculated 4
Reported most in Abstract
Documents 86
Total Number 90
Disease Relevance 15.09
Pain Relevance 31.16

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

mitochondrion (CYP2D6) small molecule metabolic process (CYP2D6) oxidoreductase activity (CYP2D6)
endoplasmic reticulum (CYP2D6)
Anatomy Link Frequency
liver 6
plasma 2
blood 1
hepatocytes 1
brain 1
CYP2D6 (Homo sapiens)
Pain Link Frequency Relevance Heat
Morphine 104 100.00 Very High Very High Very High
fluoxetine 68 100.00 Very High Very High Very High
sSRI 60 100.00 Very High Very High Very High
Potency 39 100.00 Very High Very High Very High
Endep 5 100.00 Very High Very High Very High
Codeine 188 99.96 Very High Very High Very High
methadone 112 99.80 Very High Very High Very High
Central nervous system 52 99.80 Very High Very High Very High
Opioid 74 99.72 Very High Very High Very High
tramadol 38 99.66 Very High Very High Very High
Disease Link Frequency Relevance Heat
Poisoning 8 99.88 Very High Very High Very High
Breast Cancer 219 99.40 Very High Very High Very High
Low Back Pain 13 99.40 Very High Very High Very High
Pain 346 98.92 Very High Very High Very High
Cancer 120 98.92 Very High Very High Very High
Hypoalagesia 4 98.76 Very High Very High Very High
Hepatic Insufficiency 1 98.28 Very High Very High Very High
Recurrence 101 98.00 Very High Very High Very High
Toxicity 44 97.60 Very High Very High Very High
Malignant Neoplastic Disease 7 97.44 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Life-threatening dextromethorphan intoxication associated with interaction with amitriptyline in a poor CYP2D6 metabolizer: a single case re-exposure study.
CYP2D6 Binding (interaction) of associated with dextromethorphan, endep and poisoning
1) Confidence 0.48 Published 2008 Journal J Pain Symptom Manage Section Title Doc Link 18359183 Disease Relevance 0.68 Pain Relevance 0.67
Less potent inhibitors, such as tricyclic antidepressants, will probably also reduce the pain relieving effect of codeine, since codeine has a low affinity for CYP2D6.
CYP2D6 Binding (affinity) of associated with pain, tricyclic antidepressant and codeine
2) Confidence 0.48 Published 1995 Journal Pharmacogenetics Section Abstract Doc Link 8845855 Disease Relevance 0.32 Pain Relevance 2.04
Assuming a prior probability of association of 1 in 10 for a hazard ratio of 1.5 the association between CYP2D6*6 and outcome has a 50% chance of being a false positive.
CYP2D6 Binding (association) of
3) Confidence 0.48 Published 2010 Journal Breast Cancer Res Section Body Doc Link PMC2949659 Disease Relevance 0.15 Pain Relevance 0
Prior to such a test being routinely implemented in clinical practice, it is important that large studies, with rigorous genotyping quality control are used to assess the magnitude, if any, of the association between CYP2D6 variants and valid clinical endpoints including BCSS and OS.
CYP2D6 Binding (association) of
4) Confidence 0.48 Published 2010 Journal Breast Cancer Res Section Body Doc Link PMC2949659 Disease Relevance 0.15 Pain Relevance 0
The similarity between the SERRS spectra of the same enzyme sample before the introduction of DX (Fig. 2, spectra a) and after its removal (Fig. 2, spectrum c) clearly demonstrates that the adsorbed CYP2D6 is able to reversibly bind a substrate, implying that the interaction with the coated electrode surface does not obstruct the substrate access routes to the enzyme active site.


CYP2D6 Binding (bind) of associated with dextromethorphan
5) Confidence 0.47 Published 2007 Journal J Biol Inorg Chem Section Body Doc Link PMC2099460 Disease Relevance 0 Pain Relevance 0.09
Subsequently, bound CYP2D6 was eluted with 0.2 M histidine.
CYP2D6 Binding (bound) of
6) Confidence 0.47 Published 2007 Journal J Biol Inorg Chem Section Body Doc Link PMC2099460 Disease Relevance 0.06 Pain Relevance 0
Moreover, the similar affinity of the two enzymes for DX (as was judged from optical titration experiments [6] as well as modeling studies [54]) does not indicate T309 to be involved in substrate binding in CYP2D6.
CYP2D6 Binding (binding) of
7) Confidence 0.47 Published 2007 Journal J Biol Inorg Chem Section Body Doc Link PMC1915625 Disease Relevance 0 Pain Relevance 0
No further spectral changes were detected upon increasing substrate concentration, indicating that all the CYP2D6 in the sample was bound to the substrate [37].
CYP2D6 Binding (bound) of
8) Confidence 0.47 Published 2007 Journal J Biol Inorg Chem Section Body Doc Link PMC1915625 Disease Relevance 0 Pain Relevance 0
CONCLUSIONS AND IMPLICATIONS: Drug-drug interactions via CYP2D6 and CYP3A affected oxycodone pharmacokinetics and its magnitude depended on CYP2D6 genotype.


CYP2D6 Binding (interactions) of
9) Confidence 0.44 Published 2010 Journal Br. J. Pharmacol. Section Body Doc Link 20590587 Disease Relevance 0 Pain Relevance 0
Significant within-family association of CYP2D6*4 alleles and AS was demonstrated.
CYP2D6 Binding (association) of associated with spinal inflammation
10) Confidence 0.43 Published 2000 Journal Hum. Mol. Genet. Section Abstract Doc Link 10861282 Disease Relevance 0.79 Pain Relevance 0.76
The model accounts for the process of metabolization through the cytochrome CYP2D6 and the interactions between molecules and target receptors.
cytochrome CYP2D6 Binding (interactions) of
11) Confidence 0.39 Published 2009 Journal J. Theor. Biol. Section Abstract Doc Link 19345694 Disease Relevance 0.10 Pain Relevance 0.29
Thus, more favourable tamoxifen treatment seems to be feasible through a priori genetic assessment of CYP2D6, and proper dose adjustment may be needed when the CYP2D6 genotype is determined in a patient.
CYP2D6 Binding (assessment) of
12) Confidence 0.37 Published 2009 Journal Clin Pharmacokinet Section Abstract Doc Link 19902987 Disease Relevance 0.58 Pain Relevance 0.45
Therapeutic drug monitoring has been strongly recommended for many antipsychotics, including haloperidol, chlorpromazine, fluphenazine, perphenazine, risperidone and thioridazine, which are all metabolized by CYP2D6.
CYP2D6 Binding (metabolized) of
13) Confidence 0.37 Published 2009 Journal Clin Pharmacokinet Section Abstract Doc Link 19902987 Disease Relevance 0.15 Pain Relevance 0.58
The CYP2D6 enzyme is part of the P450 enzyme system and is responsible for metabolizing tamoxifen to its most active form, endoxifen.
CYP2D6 Binding (metabolizing) of
14) Confidence 0.37 Published 2007 Journal Breast Cancer Res Section Body Doc Link PMC1868921 Disease Relevance 0.17 Pain Relevance 0
Dependence of codeine hypoalgesia on morphine formation via CYP2D6 makes this effect liable to interaction with drugs that are inhibitors of CYP2D6.
CYP2D6 Binding (interaction) of associated with addiction, hypoalgesia, morphine and codeine
15) Confidence 0.37 Published 1995 Journal Pharmacogenetics Section Abstract Doc Link 8845855 Disease Relevance 0.39 Pain Relevance 2.27
The contribution of cytochrome P450 2D6 (CYP2D6) to the formation of hydrocodone's active metabolite, hydromorphone, was examined in vitro and in vivo.
CYP2D6 Spec (examined) Binding (contribution) of
16) Confidence 0.37 Published 1993 Journal Clin. Pharmacol. Ther. Section Abstract Doc Link 7693389 Disease Relevance 0 Pain Relevance 0.06
Debrisoquine (20 mg) was orally administered to five poor metabolizers with no functional CYP2D6 gene, five heterozygous extensive metabolizers, five homozygous extensive metabolizers, five ultrarapid metabolizers with duplicated/triplicated CYP2D6*2 genes and one individual with 13 copies of CYP2D6*2.
CYP2D6 Binding (metabolizers) of
17) Confidence 0.37 Published 1999 Journal Pharmacogenetics Section Abstract Doc Link 10634132 Disease Relevance 0 Pain Relevance 0
Debrisoquine (20 mg) was orally administered to five poor metabolizers with no functional CYP2D6 gene, five heterozygous extensive metabolizers, five homozygous extensive metabolizers, five ultrarapid metabolizers with duplicated/triplicated CYP2D6*2 genes and one individual with 13 copies of CYP2D6*2.
CYP2D6 Neg (no) Binding (metabolizers) of
18) Confidence 0.37 Published 1999 Journal Pharmacogenetics Section Abstract Doc Link 10634132 Disease Relevance 0 Pain Relevance 0
The 0-96 h urinary recovery of debrisoquine differed 100-fold between the genotypes, being essentially complete in poor metabolizers and zero in the individual with 13 CYP2D6*2 genes. 4-hydroxydebrisoquine excretion increased according to the number of functional CYP2D6 genes.
CYP2D6 Binding (individual) of
19) Confidence 0.37 Published 1999 Journal Pharmacogenetics Section Abstract Doc Link 10634132 Disease Relevance 0 Pain Relevance 0
It was also shown that the widely used drug for treatment of breast cancer, trans-1-(4-beta-dimethylaminoethoxyphenyl)-,2-diphenyl-1-ene (tamoxifen), did not fit the molecular template and is unlikely to be metabolized by CYP2D6.
CYP2D6 Binding (metabolized) of associated with breast cancer
20) Confidence 0.37 Published 1991 Journal Carcinogenesis Section Abstract Doc Link 1747920 Disease Relevance 0.18 Pain Relevance 0.19

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