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Rescuing 21 sources and tagging 0 as dead.) #IABot (v2.0.9.5 |
Glaciersong (talk | contribs) putting it in a table bc other CYP pages do the same Tags: Reverted Visual edit: Switched |
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Following are the lists of selected [[enzyme substrate|substrates]], [[enzyme induction and inhibition|inducers]] and [[enzyme induction and inhibition|inhibitors]] of CYP3A4. Where classes of agents are listed, there may be exceptions within the class.
Inhibitors of CYP3A4 can be classified by their [[potency (pharmacology)|potency]], such as:▼
* '''Strong inhibitor''' being one that causes at least a 5-fold increase in the plasma [[area under the curve (pharmacokinetics)|AUC values]], or more than 80% decrease in [[clearance (medicine)|clearance]].<ref name=Flockhart/>▼
* '''Moderate inhibitor''' being one that causes at least a 2-fold increase in the plasma AUC values, or 50–80% decrease in clearance.<ref name=Flockhart/>▼
* '''Weak inhibitor''' being one that causes at least a 1.25-fold but less than 2-fold increase in the plasma AUC values, or 20–50% decrease in clearance.<ref name=Flockhart>{{cite web |vauthors=Flockhart DA |title=Drug Interactions: Cytochrome P<sub>450</sub> Drug Interaction Table |publisher=[[Indiana University School of Medicine]] |year=2007 |url=http://medicine.iupui.edu/flockhart/table.htm |access-date=25 December 2008 |archive-date=10 October 2007 |archive-url=https://web.archive.org/web/20071010053126/http://medicine.iupui.edu/flockhart/table.htm |url-status=live }} Retrieved on 25 December 2008.</ref>▼
Strong and moderate CYP3A4 inducers are drugs that decrease the AUC of sensitive substrates of a given pathway where CYP3A4 is involved by ≥80 percent and ≥50 to <80 percent, respectively.<ref name="FDA_drug_development"/><ref name="pmid34526892"/> Weak inducers decrease the AUC by ≥20 to <50 percent.<ref name="pmid34526892">{{cite journal |vauthors=Molenaar-Kuijsten L, Van Balen DE, Beijnen JH, Steeghs N, Huitema AD |title=A Review of CYP3A Drug-Drug Interaction Studies: Practical Guidelines for Patients Using Targeted Oral Anticancer Drugs |journal=Front Pharmacol |volume=12 |issue= |pages=670862 |date=2021 |pmid=34526892 |pmc=8435708 |doi=10.3389/fphar.2021.670862|doi-access=free }}</ref>▼
{| class="wikitable" width=100%
|+'''Selected inducers, inhibitors and substrates of CYP2D6'''
|-
! Substrates<br />↑ <small>= [[bioactivation]] by CYP2D6</small> !! Inhibitors !! Inducers
|- style="vertical-align: top;"
|<!--substrates-->
* some [[immunosuppressant]]s:
** [[ciclosporin]] (cyclosporin),<ref name=Flockhart/><ref name=FASS>[[FASS (drug formulary)]]: [http://www.fass.se/LIF/produktfakta/fakta_lakare_artikel.jsp?articleID=18352 Swedish environmental classification of pharmaceuticals] {{Webarchive|url=https://web.archive.org/web/20020611044953/http://www.fass.se/LIF/produktfakta/fakta_lakare_artikel.jsp?articleID=18352 |date=11 June 2002 }} Facts for prescribers (Fakta för förskrivare). Retrieved July 2011</ref>
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** [[losartan]], ([[sensitive substrates]])<ref name="LOSARTAN 2018">{{cite web | title=LOSARTAN- losartan potassium tablet, film coated | website=DailyMed | date=26 December 2018 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a98a821c-7b81-4f9b-9801-1a16d71871ce | access-date=6 February 2019 | archive-date=7 February 2019 | archive-url=https://web.archive.org/web/20190207015904/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a98a821c-7b81-4f9b-9801-1a16d71871ce | url-status=live }}</ref><ref name="pmid10877007">{{cite journal |vauthors=Taavitsainen P, Kiukaanniemi K, Pelkonen O |title=In vitro inhibition screening of human hepatic P450 enzymes by five angiotensin-II receptor antagonists |journal=Eur J Clin Pharmacol |volume=56 |issue=2 |pages=135–40 |date=May 2000 |pmid=10877007 |doi=10.1007/s002280050731 |s2cid=26865251 |url=}}</ref>
** [[irbesartan]].<ref name="pmid10877007"/>
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▲Inhibitors of CYP3A4 can be classified by their [[potency (pharmacology)|potency]], such as:
▲* '''Strong inhibitor''' being one that causes at least a 5-fold increase in the plasma [[area under the curve (pharmacokinetics)|AUC values]], or more than 80% decrease in [[clearance (medicine)|clearance]].<ref name=Flockhart/>
▲* '''Moderate inhibitor''' being one that causes at least a 2-fold increase in the plasma AUC values, or 50–80% decrease in clearance.<ref name=Flockhart/>
▲* '''Weak inhibitor''' being one that causes at least a 1.25-fold but less than 2-fold increase in the plasma AUC values, or 20–50% decrease in clearance.<ref name=Flockhart>{{cite web |vauthors=Flockhart DA |title=Drug Interactions: Cytochrome P<sub>450</sub> Drug Interaction Table |publisher=[[Indiana University School of Medicine]] |year=2007 |url=http://medicine.iupui.edu/flockhart/table.htm |access-date=25 December 2008 |archive-date=10 October 2007 |archive-url=https://web.archive.org/web/20071010053126/http://medicine.iupui.edu/flockhart/table.htm |url-status=live }} Retrieved on 25 December 2008.</ref>
▲====Strong inhibitors====
* [[boceprevir]],<ref name="FDA_drug_development">{{cite journal|title=Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers|journal=FDA|date=6 May 2023|url=https://www.fda.gov/drugs/drug-interactions-labeling/drug-development-and-drug-interactions-table-substrates-inhibitors-and-inducers|publisher=US Food and Drug Administration|access-date=21 June 2020|archive-date=4 November 2020|archive-url=https://web.archive.org/web/20201104173036/https://www.fda.gov/drugs/drug-interactions-labeling/drug-development-and-drug-interactions-table-substrates-inhibitors-and-inducers|url-status=live}}</ref>
* [[Pharmacologic protease inhibitor|protease inhibitors]]:
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* [[apigenin]] (compound present in plants such as [[celery]], [[parsley]], and [[chamomile]])<ref>{{cite journal | pmc=8158701 | date=2021 | last1=Kondža | first1=M. | last2=Bojić | first2=M. | last3=Tomić | first3=I. | last4=Rezić | first4=V. | last5=Ćavar | first5=I. | title=Characterization of the CYP3A4 Enzyme Inhibition Potential of Selected Flavonoids | journal=Molecules (Basel, Switzerland) | volume=26 | issue=10 | page=3018 | doi=10.3390/molecules26103018 | pmid=34069400 | doi-access=free }}</ref>
* [[amiodarone]] ([[class III antiarrhythmic]]),<ref name="FDA-labeling" />
* [[aprepitant]],<ref name="FDA_drug_development" /> ([[antiemetic]])
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* [[Valerian (herb)|valerian]].<ref>{{cite web|url=http://www.rxlist.com/valerian-page3/supplements.htm#Interactions|title=Valerian: Health Benefits, Side Effects, Uses, Dose & Precautions|access-date=10 April 2018|archive-date=16 January 2018|archive-url=https://web.archive.org/web/20180116055514/https://www.rxlist.com/valerian-page3/supplements.htm#Interactions|url-status=dead}}</ref>
'''Weak'''
* [[berberine]]<ref name="pmid34269665">{{cite journal |vauthors=Feng PF, Zhu LX, Jie J, Yang PX, Chen X |title=The Intracellular Mechanism of Berberine-Induced Inhibition of CYP3A4 Activity |journal=Curr Pharm Des |volume=27 |issue=40 |pages=4179–4185 |date=2021 |pmid=34269665 |doi=10.2174/1381612827666210715155809 |s2cid=235960940 |url=}}</ref><ref name="pmid37541764">{{cite journal |vauthors=Nguyen JT, Tian DD, Tanna RS, Arian CM, Calamia JC, Rettie AE, Thummel KE, Paine MF |title=An Integrative Approach to Elucidate Mechanisms Underlying the Pharmacokinetic Goldenseal-Midazolam Interaction: Application of In Vitro Assays and Physiologically Based Pharmacokinetic Models to Understand Clinical Observations |journal=J Pharmacol Exp Ther |volume=387 |issue=3 |pages=252–264 |date=December 2023 |pmid=37541764 |pmc=10658920 |doi=10.1124/jpet.123.001681 |url=}}</ref><ref name="pmid22855269">{{cite journal | vauthors = Hermann R, von Richter O | title = Clinical evidence of herbal drugs as perpetrators of pharmacokinetic drug interactions | journal = Planta Medica | volume = 78 | issue = 13 | pages = 1458–77 | date = September 2012 | pmid = 22855269 | doi = 10.1055/s-0032-1315117 | url = | doi-access = free }}</ref><ref name="pmid30086269">{{cite journal | vauthors = Feng P, Zhao L, Guo F, Zhang B, Fang L, Zhan G, Xu X, Fang Q, Liang Z, Li B | title = The enhancement of cardiotoxicity that results from inhibiton of CYP 3A4 activity and hERG channel by berberine in combination with statins | journal = Chemico-Biological Interactions | volume = 293 | issue = | pages = 115–123 | date = September 2018 | pmid = 30086269 | doi = 10.1016/j.cbi.2018.07.022 | bibcode = 2018CBI...293..115F | s2cid = 206489481 }}</ref> (an [[alkaloid]] found in plants such as [[berberis]] or [[goldenseal]]),
* [[buprenorphine]] ([[analgesic]]),<ref name="pmid12756210">{{cite journal | vauthors = Zhang W, Ramamoorthy Y, Tyndale RF, Sellers EM | s2cid = 16229370 | title = Interaction of buprenorphine and its metabolite norbuprenorphine with cytochromes p450 in vitro | journal = Drug Metabolism and Disposition | volume = 31 | issue = 6 | pages = 768–72 | date = June 2003 | pmid = 12756210 | doi = 10.1124/dmd.31.6.768 }}</ref>
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* [[azithromycin]] ([[macrolide antibiotic]]).<ref name="pmid31628882" />
'''Unspecified potency'''
* [[cannabidiol]],<ref name="pmid21356216">{{cite journal | vauthors = Yamaori S, Ebisawa J, Okushima Y, Yamamoto I, Watanabe K | title = Potent inhibition of human cytochrome P450 3A isoforms by cannabidiol: role of phenolic hydroxyl groups in the resorcinol moiety | journal = Life Sciences | volume = 88 | issue = 15–16 | pages = 730–6 | date = April 2011 | pmid = 21356216 | doi = 10.1016/j.lfs.2011.02.017 }}</ref>
* [[dithiocarbamate]]<ref name="Flockhart" /> (functional group),
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* [[serenoa]].<ref>{{cite journal | pmc=4033990 | date=2010 | last1=Ekstein | first1=D. | last2=Schachter | first2=S. C. | title=Natural Products in Epilepsy—the Present Situation and Perspectives for the Future | journal=Pharmaceuticals (Basel, Switzerland) | volume=3 | issue=5 | pages=1426–1445 | doi=10.3390/ph3051426 | pmid=27713311 | doi-access=free }}</ref>
▲Strong and moderate CYP3A4 inducers are drugs that decrease the AUC of sensitive substrates of a given pathway where CYP3A4 is involved by ≥80 percent and ≥50 to <80 percent, respectively.<ref name="FDA_drug_development"/><ref name="pmid34526892"/> Weak inducers decrease the AUC by ≥20 to <50 percent.<ref name="pmid34526892">{{cite journal |vauthors=Molenaar-Kuijsten L, Van Balen DE, Beijnen JH, Steeghs N, Huitema AD |title=A Review of CYP3A Drug-Drug Interaction Studies: Practical Guidelines for Patients Using Targeted Oral Anticancer Drugs |journal=Front Pharmacol |volume=12 |issue= |pages=670862 |date=2021 |pmid=34526892 |pmc=8435708 |doi=10.3389/fphar.2021.670862|doi-access=free }}</ref>
* [[carbamazepine]],<ref name="FDA_drug_development"/><ref name=lange6th>{{cite book | vauthors = Flower R, Rang HP, Dale MM, Ritter JM |title=Rang & Dale's pharmacology |publisher=Churchill Livingstone |location=Edinburgh |year=2007 |isbn=978-0-443-06911-6 }}{{page needed|date=November 2015}}</ref>
* [[antiandrogen]]s:
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* [[rifampin]].<ref name="FDA_drug_development"/>
'''Weak'''
* [[upadacitinib]].<ref name="Rinvoq-2020" /><ref name="Austria-Codex-DE" />
* [[anticonvulsant]]s, [[mood stabilizers]]:
** [[oxcarbazepine]],<ref name=Flockhart/>
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* [[perampanel]],<ref name=Flockhart/>
* [[telotristat]].<ref name=Flockhart/>
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==Interactive pathway map==
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