INT63057

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Context Info
Confidence 0.61
First Reported 1996
Last Reported 2010
Negated 4
Speculated 3
Reported most in Abstract
Documents 31
Total Number 33
Disease Relevance 5.75
Pain Relevance 6.92

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 (CYP3A4) oxidoreductase activity (CYP3A4) endoplasmic reticulum (CYP3A4)
enzyme binding (CYP3A4) lipid metabolic process (CYP3A4) cytoplasm (CYP3A4)
Anatomy Link Frequency
plasma 4
liver 4
intestinal cells 1
CYP3A4 (Homo sapiens)
Pain Link Frequency Relevance Heat
rapifen 20 100.00 Very High Very High Very High
Paracetamol 10 100.00 Very High Very High Very High
ketamine 13 99.80 Very High Very High Very High
Morphine 5 99.48 Very High Very High Very High
Opioid 5 98.64 Very High Very High Very High
lidocaine 29 98.56 Very High Very High Very High
methadone 25 97.80 Very High Very High Very High
Versed 17 97.80 Very High Very High Very High
carbamazepine 78 97.48 Very High Very High Very High
alcohol 7 97.40 Very High Very High Very High
Disease Link Frequency Relevance Heat
Nicotine Addiction 36 99.20 Very High Very High Very High
Fungal Infection 2 96.96 Very High Very High Very High
Lipodystrophy 2 96.16 Very High Very High Very High
Schistosomiasis 4 95.96 Very High Very High Very High
Targeted Disruption 69 94.16 High High
Chronic Disease 2 94.08 High High
Fibrosis 5 91.20 High High
Hypotension 2 88.88 High High
Acquired Immune Deficiency Syndrome Or Hiv Infection 154 88.24 High High
Vomiting 98 85.32 High High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Alterations in CYP3A4 levels or activity, as well as the concomitant administration of other therapeutic agents metabolized by this P450 enzyme, could lead to marked perturbations in fentanyl disposition and, hence, analgesic response.
Regulation (Alterations) of CYP3A4 associated with analgesic
1) Confidence 0.61 Published 1996 Journal Drug Metab. Dispos. Section Abstract Doc Link 8886601 Disease Relevance 0 Pain Relevance 0.24
In addition, different clinical trials conducted to study the effects of CYP3A4, CYP2D6, and MAO-A on the pharmacokinetics of almotriptan confirmed the involvement of these enzymes in the metabolic clearance of this drug and that no dose changes are required in the presence of inhibitors of these enzymes.
Regulation (effects) of CYP3A4
2) Confidence 0.58 Published 2003 Journal Drug Metab. Dispos. Section Abstract Doc Link 12642466 Disease Relevance 0.07 Pain Relevance 0.04
No drugs known to affect the activity of CYP3A4 were given to the patients (e.g. macrolide antibiotics, contraceptives, or antifungal agents of an azole structure).
Regulation (affect) of CYP3A4 associated with fungal infection
3) Confidence 0.56 Published 2006 Journal Biomark Insights Section Body Doc Link PMC2716776 Disease Relevance 1.19 Pain Relevance 0.13
CONCLUSION: Physicians should recognize the potential effects of CYP3A4 inhibitors particularly when administering or prescribing systemic corticosteroid medications.


Regulation (effects) of CYP3A4
4) Confidence 0.45 Published 2010 Journal Pain Med Section Body Doc Link 20456080 Disease Relevance 0 Pain Relevance 0
The capacity of the cells for metabolizing CYP3A4 substrates in vitro was evaluated.
Regulation (metabolizing) of CYP3A4
5) Confidence 0.45 Published 2008 Journal Xenobiotica Section Abstract Doc Link 18846481 Disease Relevance 0 Pain Relevance 0.07
Also determined was the effect of CYP3A4 inhibitors and non-inhibitors on nifedipine hydroxylation.
Regulation (effect) of CYP3A4
6) Confidence 0.45 Published 2008 Journal Xenobiotica Section Abstract Doc Link 18846481 Disease Relevance 0 Pain Relevance 0.08
We have examined the effects of the CYP3A4 inhibitors erythromycin and ketoconazole and the CYP1A2 inhibitor fluvoxamine on the N-deethylation, i.e. formation of monoethylglycinexylidide (MEGX), and 3-hydroxylation of lidocaine by human liver microsomes.
Spec (examined) Regulation (effects) of CYP3A4 in liver associated with lidocaine
7) Confidence 0.44 Published 1999 Journal Pharmacol. Toxicol. Section Abstract Doc Link 10608481 Disease Relevance 0 Pain Relevance 0.41
The present study demonstrates that CYP3A4 is the principal enzyme responsible for ketamine N-demethylation in human liver microsomes and that CYP2B6 and CYP2C9 have a minor contribution to ketamine N-demethylation at therapeutic concentrations of the drug.
Regulation (responsible) of CYP3A4 in liver associated with ketamine
8) Confidence 0.44 Published 2002 Journal Drug Metab. Dispos. Section Abstract Doc Link 12065445 Disease Relevance 0 Pain Relevance 0.42
In studies of CYP-mediated disposition in vitro, CYP3A4 appears to be the major isoform responsible for the metabolism of haloperidol in humans.
Regulation (responsible) of CYP3A4
9) Confidence 0.44 Published 1999 Journal Clin Pharmacokinet Section Abstract Doc Link 10628896 Disease Relevance 0.08 Pain Relevance 0
More than 90% of morphine N-demethylation could be accounted for via the action of both CYP3A4 and CYP2C8. 4.
Regulation (accounted) of CYP3A4 associated with morphine
10) Confidence 0.44 Published 2003 Journal Xenobiotica Section Abstract Doc Link 12936704 Disease Relevance 0 Pain Relevance 0.41
Two aspects have been particularly taken into account: the changes or absence of changes in plasma/serum concentrations of concomitant drugs and the direct or indirect evidence of induction, inhibition or lack of effect on the six major human hepatic CYP isozymes (CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4), as well as on other CYP isozymes or enzyme systems.
Regulation (effect) of CYP3A4 in plasma
11) Confidence 0.44 Published 2000 Journal Fundam Clin Pharmacol Section Abstract Doc Link 11030437 Disease Relevance 0 Pain Relevance 0.20
We have studied the effect of a potent CYP3A4 inhibitor, itraconazole, on the pharmacokinetics of inhaled lidocaine in ten healthy volunteers using a randomized, two-phase cross-over study design.
Regulation (effect) of CYP3A4 associated with lidocaine
12) Confidence 0.44 Published 2004 Journal Basic Clin. Pharmacol. Toxicol. Section Abstract Doc Link 15447735 Disease Relevance 0 Pain Relevance 0.65
The metabolic profile of aprepitant over a 2-week period of time can be described as an inhibitor, then an inducer, and then no effect on CYP3A4 after 2 weeks (Shadle et al 2004).
Neg (no) Regulation (effect) of CYP3A4
13) Confidence 0.39 Published 2007 Journal International Journal of Nanomedicine Section Body Doc Link PMC2673828 Disease Relevance 0.89 Pain Relevance 0.17
CYP3A4 is the major isoform responsible for erlotinib metabolism (Li et al 2007).
Regulation (responsible) of CYP3A4
14) Confidence 0.34 Published 2007 Journal Biologics : Targets & Therapy Section Body Doc Link PMC2721286 Disease Relevance 0.55 Pain Relevance 0
Inhibition studies using ketoconazole, furafylline, sulfaphenazole, omeprazole and quinidine suggested that CYP3A4 is the isoform responsible for this reaction whereas CYP1A2, CYP2C9, CYP2C19 and CYP2D6 do not seem to be involved.
Regulation (responsible) of CYP3A4
15) Confidence 0.33 Published 2000 Journal Brain Res. Section Abstract Doc Link 10677595 Disease Relevance 0 Pain Relevance 0.34
The actions of most drugs that affect CYP3A4 by inhibition or induction manifest as drug interactions with CBZ [5,6].
Regulation (affect) of CYP3A4 associated with carbamazepine
16) Confidence 0.31 Published 2008 Journal J Med Case Reports Section Body Doc Link PMC2495000 Disease Relevance 0.43 Pain Relevance 0.54
OBJECTIVE: The opioid alfentanil is a CYP3A4 substrate whose plasma clearance depends exclusively on hepatic CYP3A4 activity.
Regulation (depends) of CYP3A4 in plasma associated with rapifen and opioid
17) Confidence 0.27 Published 2001 Journal Clin. Pharmacol. Ther. Section Abstract Doc Link 11753266 Disease Relevance 0.15 Pain Relevance 0.38
Alfentanil-dependent miosis was significantly altered by CYP3A4 modulation, and log(diameter(0) - diameter(t)) versus time curves resembled alfentanil plasma disposition.
Regulation (modulation) of CYP3A4 in plasma
18) Confidence 0.27 Published 2001 Journal Clin. Pharmacol. Ther. Section Body Doc Link 11753266 Disease Relevance 0 Pain Relevance 0
Northern blots were used to examine the effects of acetaminophen (APAP) on CYP3A4-mRNA.
Spec (examine) Regulation (effects) of CYP3A4-mRNA associated with paracetamol
19) Confidence 0.27 Published 2002 Journal Arch. Biochem. Biophys. Section Abstract Doc Link 11811955 Disease Relevance 0 Pain Relevance 0.64
We conclude that CYP3A4 is responsible for fentanyl and sufentanil N-dealkylation in vitro.
Regulation (responsible) of CYP3A4
20) Confidence 0.27 Published 1996 Journal Anesth. Analg. Section Abstract Doc Link 8712396 Disease Relevance 0 Pain Relevance 0.03

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