CYP450 inducers, inhibitors


  • cyclosporine, macrolides, azoles are all inhibitors

CYP450 Inducers

InducersInhibitorsSubstrates
St. John's WortGrapefruit JuiceWarfarin
CarbamazepineCimetidinePhenytoin
PhenytoinErythromycinTheophylline
PhenobarbitalCiprofloxacinStatin (except pravastatin)
RifampinAzolesTacrolimus, cyclosporine, cyclophosphamide
GriseofulvinRitonavirzaleplon
Chronic EtOHIsoniazidzolpidem
ModafinilBactrim/MetronidazolexBenzodiazepine
TrikaftaAmiodaroneTrikafta
SimprevirAmiodarone
DiltiazemNintedanib
Fluoroquinolones

  • Activated chrome bumper: barbiturates (e.g. phenobarbital) are potent inducers of the cytochrome P450 system

  • Speeding chrome bumper: rifampin activated cytochrome P450

  • Greased up chrome bumper: griseofulvin activates cytochrome P-450

CYP450 Inhibitors

InducersInhibitorsSubstrates
St. John's WortGrapefruit JuiceWarfarin
CarbamazepineCimetidinePhenytoin
PhenytoinErythromycinTheophylline
PhenobarbitalCiprofloxacinStatin (except pravastatin)
RifampinAzolesTacrolimus, cyclosporine, cyclophosphamide
GriseofulvinRitonavirzaleplon
Chronic EtOHIsoniazidzolpidem
ModafinilBactrim/MetronidazolexBenzodiazepine
TrikaftaAmiodaroneTrikafta
SimprevirAmiodarone
DiltiazemNintedanib
Fluoroquinolones

  • Broken chrome bumper: cytochrome P-450 inhibition

  • Broken chrome bumper: azole antifungals inhibit fungal cytochrome P-450 responsible for the conversion. Also SE because CYP 450

  • Right on!: ritonovir has greatest cytochrome P-450 inhibitory effect and boosts concentration of other protease inhibitors

  • Broken chrome bumper: INH inhibits cytochrome P450

  • Vandalized chrome bumper: inhibition of cytochrome P450

  • Broken chrome bumper: amiodarone inhibits the cytochrome P450 system

  • Broken chrome bumper: simeprevir inhibits cytochrome P450

Substrates

InducersInhibitorsSubstrates
St. John's WortGrapefruit JuiceWarfarin
CarbamazepineCimetidinePhenytoin
PhenytoinErythromycinTheophylline
PhenobarbitalCiprofloxacinStatin (except pravastatin)
RifampinAzolesTacrolimus, cyclosporine, cyclophosphamide
GriseofulvinRitonavirzaleplon
Chronic EtOHIsoniazidzolpidem
ModafinilBactrim/MetronidazolexBenzodiazepine
TrikaftaAmiodaroneTrikafta
SimprevirAmiodarone
DiltiazemNintedanib
Fluoroquinolones

  • chrome tank: all statins except for pravastatin are metabolized by cytochrome p450 (CYP-450) in the liver

  • Activating chrome bumper: cyclophosphamide is ACTIVATED by hepatic cytochrome P450 enzymes

  • Liver spot: zaleplon and zolpidem are rapidly metabolized by the liver, P450 system

  • CYP-450 chrome tank crushing warhead: warfarin is a substrate of cytochrome P-450 (drugs increase CYP activation increase warfarin metabolism)

  • Chrome bumper hitting energy drinks: methylxanthines (e.g. theophylline) are metabolized by the cytochrome P-450 system