CYP450 inducers, inhibitors
- related: Pharmacology
- tags: #literature #boards
- cyclosporine, macrolides, azoles are all inhibitors
CYP450 Inducers
| Inducers | Inhibitors | Substrates |
|---|---|---|
| St. John's Wort | Grapefruit Juice | Warfarin |
| Carbamazepine | Cimetidine | Phenytoin |
| Phenytoin | Erythromycin | Theophylline |
| Phenobarbital | Ciprofloxacin | Statin (except pravastatin) |
| Rifampin | Azoles | Cyclophosphamide |
| Griseofulvin | Ritonavir | zaleplon |
| Chronic EtOH | Isoniazid | zolpidem |
| Modafinil | Bactrim/Metronidazolex | Benzodiazepine |
| Trikafta | Amiodarone | Trikafta |
| Nintedanib | Simprevir | Tacrolimus, cyclosporine |
| Diltiazem | ||
| 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
| Inducers | Inhibitors | Substrates |
|---|---|---|
| St. John's Wort | Grapefruit Juice | Warfarin |
| Carbamazepine | Cimetidine | Phenytoin |
| Phenytoin | Erythromycin | Theophylline |
| Phenobarbital | Ciprofloxacin | Statin (except pravastatin) |
| Rifampin | Azoles | Cyclophosphamide |
| Griseofulvin | Ritonavir | zaleplon |
| Chronic EtOH | Isoniazid | zolpidem |
| Modafinil | Bactrim/Metronidazolex | Benzodiazepine |
| Trikafta | Amiodarone | Trikafta |
| Nintedanib | Simprevir | Tacrolimus, cyclosporine |
| Diltiazem | ||
| 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
Links to this note
| Inducers | Inhibitors | Substrates |
|---|---|---|
| St. John's Wort | Grapefruit Juice | Warfarin |
| Carbamazepine | Cimetidine | Phenytoin |
| Phenytoin | Erythromycin | Theophylline |
| Phenobarbital | Ciprofloxacin | Statin (except pravastatin) |
| Rifampin | Azoles | Cyclophosphamide |
| Griseofulvin | Ritonavir | zaleplon |
| Chronic EtOH | Isoniazid | zolpidem |
| Modafinil | Bactrim/Metronidazolex | Benzodiazepine |
| Trikafta | Amiodarone | Trikafta |
| Nintedanib | Simprevir | Tacrolimus, cyclosporine |
| Diltiazem | ||
| 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