INT60779

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Context Info
Confidence 0.59
First Reported 1995
Last Reported 2010
Negated 1
Speculated 4
Reported most in Abstract
Documents 63
Total Number 68
Disease Relevance 8.38
Pain Relevance 21.27

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

Anatomy Link Frequency
plasma 5
liver 3
brain 1
urine 1
CYP3A (Homo sapiens)
CYP3A - P4503A (1)
Pain Link Frequency Relevance Heat
dexamethasone 185 99.88 Very High Very High Very High
fluoxetine 45 99.88 Very High Very High Very High
antidepressant 8 99.80 Very High Very High Very High
methadone 90 99.52 Very High Very High Very High
Buprenorphine 49 99.52 Very High Very High Very High
Analgesic 31 99.50 Very High Very High Very High
sSRI 51 99.46 Very High Very High Very High
tricyclic antidepressant 15 99.44 Very High Very High Very High
rapifen 42 99.34 Very High Very High Very High
Potency 20 98.88 Very High Very High Very High
Disease Link Frequency Relevance Heat
Depression 9 99.62 Very High Very High Very High
Miosis 12 99.48 Very High Very High Very High
Fungal Infection 8 99.02 Very High Very High Very High
Liver Disease 9 98.68 Very High Very High Very High
Acquired Immune Deficiency Syndrome Or Hiv Infection 359 98.10 Very High Very High Very High
Renal Failure 3 97.32 Very High Very High Very High
Headache 24 97.16 Very High Very High Very High
Newborn Jaundice 2 96.68 Very High Very High Very High
INFLAMMATION 29 96.60 Very High Very High Very High
Diabetes Mellitus 13 96.28 Very High Very High Very High

Sentences Mentioned In

Key: Protein Mutation Event Anatomy Negation Speculation Pain term Disease term
The azole antifungal agents ketoconazole and itraconazole are potent inhibitors of human CYP3A isoforms.
Negative_regulation (inhibitors) of CYP3A associated with fungal infection
1) Confidence 0.59 Published 1995 Journal Clin Pharmacokinet Section Abstract Doc Link 8846621 Disease Relevance 0.10 Pain Relevance 0.29
Selective serotonin reuptake inhibitor (SSRI) antidepressants are also CYP3A inhibitors, but much less potent than ketoconazole or itraconazole.
Negative_regulation (inhibitors) of CYP3A associated with antidepressant and ssri
2) Confidence 0.59 Published 1995 Journal Clin Pharmacokinet Section Abstract Doc Link 8846621 Disease Relevance 0.09 Pain Relevance 0.30
These inhibition data were compared with ketoconazole, which was included as a positive control of CYP3A inhibition.
Negative_regulation (inhibition) of CYP3A
3) Confidence 0.59 Published 2002 Journal J Clin Psychopharmacol Section Abstract Doc Link 11910261 Disease Relevance 0.12 Pain Relevance 0.53
Since the IC50 for buprenorphine is roughly 2000 times higher than typical plasma concentrations, this drug is unlikely to cause clinically significant inhibition of CYP3A in patients.
Negative_regulation (inhibition) of CYP3A in plasma associated with buprenorphine
4) Confidence 0.59 Published 2000 Journal Life Sci. Section Abstract Doc Link 10755464 Disease Relevance 0.10 Pain Relevance 0.98
Buprenorphine was found to be a weak inhibitor of CYP3A with a 50% decrease in enzyme activity occurring at a concentration of 118 microM (IC50) in human liver microsomes.
Negative_regulation (inhibitor) of CYP3A in liver associated with buprenorphine
5) Confidence 0.59 Published 2000 Journal Life Sci. Section Abstract Doc Link 10755464 Disease Relevance 0.07 Pain Relevance 1.06
Intestinal and hepatic CYP3A was inhibited > 70%.
Negative_regulation (inhibited) of CYP3A
6) Confidence 0.59 Published 2008 Journal Clin. Pharmacol. Ther. Section Abstract Doc Link 19238655 Disease Relevance 0.25 Pain Relevance 1.01
Methadone disposition was unchanged, despite profound inhibition of CYP3A activity, suggesting little or no role for CYP3A in clinical methadone metabolism and clearance.
Negative_regulation (inhibition) of CYP3A
7) Confidence 0.58 Published 2009 Journal Anesthesiology Section Body Doc Link 19225389 Disease Relevance 0 Pain Relevance 0
They received OTF (10 microg/kg) after hepatic/intestinal CYP3A induction by rifampin, hepatic/intestinal CYP3A inhibition by troleandomycin, selective intestinal CYP3A inhibition by grapefruit juice, or nothing (control).
Negative_regulation (inhibition) of CYP3A
8) Confidence 0.58 Published 2004 Journal Anesthesiology Section Body Doc Link 15329598 Disease Relevance 0 Pain Relevance 0
Chronic ritonavir inhibits hepatic CYP3A (> 70%) and first-pass CYP3A (> 90%).
Negative_regulation (inhibits) of CYP3A
9) Confidence 0.57 Published 2008 Journal Clin. Pharmacol. Ther. Section Abstract Doc Link 19238656 Disease Relevance 0.08 Pain Relevance 0.47
In vitro, ritonavir is a potent inhibitor of CYP3A.
Negative_regulation (inhibitor) of CYP3A
10) Confidence 0.57 Published 1998 Journal Clin Pharmacokinet Section Abstract Doc Link 9812178 Disease Relevance 0.27 Pain Relevance 0.03
To inhibit the CYP3A located in the intestinal mucosa, components of grapefruit juice are very suitable.
Negative_regulation (inhibit) of CYP3A
11) Confidence 0.55 Published 2005 Journal Ther Drug Monit Section Abstract Doc Link 16175141 Disease Relevance 0 Pain Relevance 0
We investigated the influence of grapefruit juice, which contains inhibitors of intestinal CYP3A, on the steady-state pharmacokinetics of methadone.
Negative_regulation (inhibitors) of CYP3A associated with methadone
12) Confidence 0.55 Published 2004 Journal Clin. Pharmacol. Ther. Section Abstract Doc Link 15229464 Disease Relevance 0 Pain Relevance 0.27
The formation of 4-OH-ropivacaine, 2-OH-methyl-ropivacaine, and PPX was markedly inhibited in the presence of troleandomycin, an inhibitor of CYP3A.
Negative_regulation (inhibitor) of CYP3A
13) Confidence 0.54 Published 1996 Journal Drug Metab. Dispos. Section Abstract Doc Link 8886604 Disease Relevance 0 Pain Relevance 0.13
Fluoxetine increases the plasma concentrations of alprazolam and diazepam by inhibiting CYP3A and CYP2C19, respectively.
Negative_regulation (inhibiting) of CYP3A in plasma associated with fluoxetine
14) Confidence 0.52 Published 1997 Journal Clin Pharmacokinet Section Abstract Doc Link 9435993 Disease Relevance 0 Pain Relevance 0.73
The strongest inhibition of bupivacaine metabolism was obtained for troleandomycin (-95% at 50 microM), a specific CYP3A inhibitor.
Negative_regulation (inhibitor) of CYP3A
15) Confidence 0.52 Published 2000 Journal Drug Metab. Dispos. Section Abstract Doc Link 10725304 Disease Relevance 0 Pain Relevance 0.12
They received OTF (10 microg/kg) after hepatic/intestinal CYP3A induction by rifampin, hepatic/intestinal CYP3A inhibition by troleandomycin, selective intestinal CYP3A inhibition by grapefruit juice, or nothing (control).
Negative_regulation (inhibition) of CYP3A
16) Confidence 0.50 Published 2004 Journal Anesthesiology Section Body Doc Link 15329598 Disease Relevance 0 Pain Relevance 0
Clarithromycin, a potent inhibitor of CYP3A, greatly increases exposure to oral S-ketamine.
Negative_regulation (inhibitor) of CYP3A associated with ketamine and analgesic
17) Confidence 0.48 Published 2010 Journal Eur J Pain Section Title Doc Link 19897389 Disease Relevance 0.10 Pain Relevance 0.63
Tipranavir is metabolized by cytochrome P450 (CYP) 3A and, when combined with ritonavir in vitro, causes inhibition of CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A in addition to induction of glucuronidase and the drug transporter P-glycoprotein.
Negative_regulation (inhibition) of CYP3A
18) Confidence 0.46 Published 2007 Journal Pharmacotherapy Section Abstract Doc Link 17542771 Disease Relevance 0.24 Pain Relevance 0.18
Clinical and in vitro studies have demonstrated that the major enzymes involved in the metabolism of the NK-1 receptor antagonist casopitant are from the CYP3A family and that casopitant (and a major circulating metabolite) can result in weak to moderate inhibition of CYP3A.
Negative_regulation (inhibition) of CYP3A associated with antagonist
19) Confidence 0.44 Published 2009 Journal Support Care Cancer Section Body Doc Link PMC2726912 Disease Relevance 0.45 Pain Relevance 0.49
Induction of methadone metabolism occurred despite profound CYP3A inhibition, suggesting no role for CYP3A in clinical methadone metabolism and clearance.
Negative_regulation (inhibition) of CYP3A associated with methadone
20) Confidence 0.43 Published 2008 Journal Clin. Pharmacol. Ther. Section Abstract Doc Link 19238655 Disease Relevance 0.22 Pain Relevance 1.01

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