INT22211

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Context Info
Confidence 0.70
First Reported 1990
Last Reported 2010
Negated 10
Speculated 3
Reported most in Abstract
Documents 110
Total Number 113
Disease Relevance 22.00
Pain Relevance 28.27

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
CAR 3
muscle 1
intestinal lumen 1
CYP3A4 (Homo sapiens)
Pain Link Frequency Relevance Heat
Potency 60 100.00 Very High Very High Very High
fluoxetine 44 100.00 Very High Very High Very High
agonist 178 99.98 Very High Very High Very High
cocaine 74 99.98 Very High Very High Very High
Paracetamol 85 99.84 Very High Very High Very High
Endep 18 99.78 Very High Very High Very High
dexamethasone 121 99.68 Very High Very High Very High
Versed 116 99.68 Very High Very High Very High
lidocaine 45 99.44 Very High Very High Very High
carbamazepine 100 99.20 Very High Very High Very High
Disease Link Frequency Relevance Heat
Toxicity 505 99.84 Very High Very High Very High
Gallstones 19 99.84 Very High Very High Very High
Osteogenic Sarcomas 124 99.76 Very High Very High Very High
Injury 204 99.32 Very High Very High Very High
Targeted Disruption 161 99.08 Very High Very High Very High
Hepatocellular Cancer 4 99.04 Very High Very High Very High
Substance Withdrawal Syndrome 138 98.72 Very High Very High Very High
Vomiting 617 98.28 Very High Very High Very High
Hypersensitivity 33 97.96 Very High Very High Very High
Nicotine Addiction 53 97.64 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
Each volunteer received 1 mg intravenous midazolam, followed 1 hour later by 15 microg/kg intravenous alfentanil, after CYP3A4 induction (rifampin [INN, rifampicin]), CYP3A4 inhibition (troleandomycin), and control.
Positive_regulation (induction) of CYP3A4
1) Confidence 0.70 Published 2001 Journal Clin. Pharmacol. Ther. Section Body Doc Link 11753266 Disease Relevance 0 Pain Relevance 0
RESULTS: Compared with control, CYP3A4 induction and inhibition significantly altered the clearances of alfentanil (2.8 +/- 1.4, 5.3 +/- 1.0, and 0.42 +/- 0.1 ml/kg/min, respectively; P <.05 versus control) and midazolam.
Positive_regulation (induction) of CYP3A4
2) Confidence 0.70 Published 2001 Journal Clin. Pharmacol. Ther. Section Body Doc Link 11753266 Disease Relevance 0 Pain Relevance 0
Induction of CYP3A4, measured as testosterone 6 beta-hydroxylation, was found to be dose-dependent, treatment duration-dependent, and reversible.
Positive_regulation (Induction) of CYP3A4
3) Confidence 0.70 Published 1997 Journal Cell Biol. Toxicol. Section Abstract Doc Link 9298257 Disease Relevance 0 Pain Relevance 0.16
A small number of drugs such as rifampin, phenytoin and ritonavir are identified as inducers of CYP3A4.
Positive_regulation (inducers) of CYP3A4
4) Confidence 0.70 Published 2008 Journal Curr. Drug Metab. Section Abstract Doc Link 18473749 Disease Relevance 0.23 Pain Relevance 0.16
At lower concentrations, APAP produced a dose-dependent increase in CYP3A4 activity and content.
Positive_regulation (increase) of CYP3A4 associated with paracetamol
5) Confidence 0.70 Published 2002 Journal Arch. Biochem. Biophys. Section Abstract Doc Link 11811955 Disease Relevance 0 Pain Relevance 0.75
No increases in CYP3A4-mRNA were seen.
Neg (No) Positive_regulation (increases) of CYP3A4-mRNA
6) Confidence 0.70 Published 2002 Journal Arch. Biochem. Biophys. Section Abstract Doc Link 11811955 Disease Relevance 0 Pain Relevance 0.76
The HepG2-GS-3A4 expressed a higher amount of CYP3A4 protein and mRNA than control.
Positive_regulation (amount) of CYP3A4
7) Confidence 0.69 Published 2008 Journal Xenobiotica Section Abstract Doc Link 18846481 Disease Relevance 0 Pain Relevance 0.08
Whereas this interaction can be explained by induction of phase I drug metabolism (CYP3A4), knowledge about induction of phase II metabolism (e.g., UDP-glucuronosyltransferases = UGTs) and its influence on drug effects in man, however, is very limited.
Positive_regulation (induction) of CYP3A4
8) Confidence 0.69 Published 1997 Journal Pain Section Abstract Doc Link 9272811 Disease Relevance 0.10 Pain Relevance 0.88
The amplitude of the increase in CYP3A4 protein and activity by 25 microM eletriptan was significantly lower, with a mean of 19 (P =.0015) and 26% (P =.0002), respectively, of that observed in response to 25 microM rifampicin.
Positive_regulation (increase) of CYP3A4
9) Confidence 0.69 Published 2000 Journal Drug Metab. Dispos. Section Abstract Doc Link 10611140 Disease Relevance 0.08 Pain Relevance 0.19
Eletriptan is therefore not an inducer of CYP3A4 at clinical doses.
Neg (not) Positive_regulation (inducer) of CYP3A4
10) Confidence 0.69 Published 2000 Journal Drug Metab. Dispos. Section Abstract Doc Link 10611140 Disease Relevance 0 Pain Relevance 0
Because the maximum blood concentration of eletriptan in humans after a therapeutic dose (maximum 80 mg) is 0.5 microM, the in vitro model would predict no clinically significant induction of CYP3A4 protein in vivo.
Neg (no) Positive_regulation (induction) of CYP3A4 in blood
11) Confidence 0.69 Published 2000 Journal Drug Metab. Dispos. Section Abstract Doc Link 10611140 Disease Relevance 0.05 Pain Relevance 0.08
Conversely, drugs that strongly induce CYP 3A4 (eg, Rifampin), can significantly lower levels of most NNRTIs and PIs, and thus concurrent administration is contraindicated.
Positive_regulation (induce) of CYP 3A4
12) Confidence 0.67 Published 2008 Journal Clinical Interventions in Aging Section Body Doc Link PMC2682378 Disease Relevance 0.58 Pain Relevance 0.10
In vitro metabolism studies show that there is a low potential for drug-drug interactions with VGB due to enzyme induction of CYP2B6 or CYP3A4.9 However, in some clinical studies, VGB was associated with modest decreases in plasma phenytoin levels.10,11 The cause of these findings is unclear, as VGB is not protein bound, and is not metabolized.12 A mild increase in carbamazepine (CBZ) levels in patients receiving adjunctive VGB has also been reported.13 These findings suggest that levels of concomitant antiepileptic drugs should be monitored, but dose adjustment is usually unnecessary.


Positive_regulation (induction) of CYP3A4 in plasma associated with antiepileptic drug and carbamazepine
13) Confidence 0.67 Published 2009 Journal Neuropsychiatric Disease and Treatment Section Body Doc Link PMC2762367 Disease Relevance 0.25 Pain Relevance 0.27
It induces enzymes such as CYP3A4 and inhibits enzymes such as CYP2C19 and those of the beta-oxidation pathway.
Positive_regulation (induces) of CYP3A4
14) Confidence 0.67 Published 2000 Journal Fundam Clin Pharmacol Section Abstract Doc Link 11030437 Disease Relevance 0 Pain Relevance 0.26
Lamotrigine appears to be a weak inducer of UGTs, whereas induction of CYP3A4 seems improbable as the compound does not change the concentrations of oral contraceptives or the urinary excretion of 6beta-hydroxycortisol.
Positive_regulation (induction) of CYP3A4 associated with lamotrigine
15) Confidence 0.67 Published 2000 Journal Fundam Clin Pharmacol Section Abstract Doc Link 11030437 Disease Relevance 0 Pain Relevance 0.25
Topiramate is not devoid of potential interaction properties: it decreases the plasma concentrations of ethinylestradiol, induces CYP3A4 and inhibits CYP2C19.
Positive_regulation (induces) of CYP3A4 in plasma
16) Confidence 0.67 Published 2000 Journal Fundam Clin Pharmacol Section Abstract Doc Link 11030437 Disease Relevance 0 Pain Relevance 0.26
Retinoids activate the RXR/SXR-mediated pathway and induce the endogenous CYP3A4 activity in Huh7 human hepatoma cells.
Positive_regulation (induce) of CYP3A4 associated with hepatocellular cancer
17) Confidence 0.67 Published 2006 Journal Toxicol. Sci. Section Title Doc Link 16632523 Disease Relevance 0.37 Pain Relevance 0.03
Additionally, retinoids can increase CYP3A4 enzyme activity in Huh7 cells.
Positive_regulation (increase) of CYP3A4
18) Confidence 0.67 Published 2006 Journal Toxicol. Sci. Section Abstract Doc Link 16632523 Disease Relevance 0.66 Pain Relevance 0.27
For efavirenz and nevirapine, these drug interactions are consistent with their induction of CYP3A4.
Positive_regulation (induction) of CYP3A4
19) Confidence 0.65 Published 2010 Journal Curr HIV/AIDS Rep Section Body Doc Link PMC2892618 Disease Relevance 0.22 Pain Relevance 1.43
If cocaine induces CYP3A4 in humans as well, it may decrease levels and effectiveness of the many ARVs that are CYP3A4 substrates, including most NNRTIs and PIs.
Positive_regulation (induces) of CYP3A4 associated with cocaine
20) Confidence 0.65 Published 2010 Journal Curr HIV/AIDS Rep Section Body Doc Link PMC2892618 Disease Relevance 0.41 Pain Relevance 0.87

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