CYP3A4 - CYP3A4 Ligands

CYP3A4 Ligands

Following is a table of selected substrates, inducers and 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, such as:

Strong inhibitor being one that causes at least a 5-fold increase in the plasma AUC values, or more than 80% decrease in clearance.
Moderate inhibitor being one that causes at least a 2-fold increase in the plasma AUC values, or 50-80% decrease in clearance.
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.

**Selected inducers, inhibitors and substrates of CYP3A4**
Substrates	Inhibitors	Inducers
some immunosuppressants ciclosporin (cyclosporin) tacrolimus sirolimus many chemotherapeutic docetaxel tamoxifen paclitaxel cyclophosphamide doxorubicin erlotinib etoposide ifosfamide teniposide vinblastine vincristine vindesine imatinib irinotecan sorafenib sunitinib temsirolimus anastrazole gefitinib azole antifungals ketoconazole itraconazole macrolides clarithromycin erythromycin telithromycin (not azithromycin) dapsone (in leprosy) tricyclic antidepressants amitriptyline clomipramine imipramine SSRIs citalopram norfluoxetine sertraline some other antidepressants mirtazapine (NaSSA) nefazodone reboxetine venlafaxine (SNRI) trazodone (SARI buspirone (anxiolytic) antipsychotics haloperidol aripiprazole risperidone ziprasidone pimozide quetiapine opiate (mainly analgesics) alfentanil buprenorphine codeine (analgesic, antitussive, antidiarrheal) fentanyl methadone (analgesic, anti-addictive) levacetylmethadol benzodiazepines alprazolam midazolam triazolam diazepam some hypnotics zopiclone zaleplon zolpidem donepezil (acetylcholinesterase inhibitor) statins atorvastatin lovastatin simvastatin cerivastatin (not pravastatin) (not rosuvastatin) calcium channel blockers diltiazem felodipine nifedipine verapamil amlodipine lercanidipine nitrendipine nisoldipine amiodarone (class III antiarrhythmic) dronedarone (class III antiarrhythmic) quinidine (class I antiarrhythmic) PDE5 inhibitors sildenafil tadalafil kinins (vasodilators, smooth muscle contractors) sex hormones agonists and antagonists finasteride (antiandrogen) estradiol (estrogen) progesterone ethinylestradiol (hormonal contraceptive) testosterone (androgen) toremifene (SERM) bicalutamide H1-receptor antagonists terfenadine astemizole chlorphenamine Protease inhibitors indinavir ritonavir saquinavir nelfinavir non-nucleoside reverse transcriptase inhibitors nevirapine some glucocorticoids budesonide hydrocortisone dexamethasone cisapride (5-HT4 receptor agonist) aprepitant (antiemetic) caffeine (stimulant) cocaine (stimulant) cilostazol (phosphodiesterase inhibitor) dextromethorphan (antitussive) domperidone (antidopaminergic) eplerenone (aldosterone antagonist) lidocaine (local anesthetic, antiarrhythmic) ondansetron (5-HT3 antagonist) propranolol (beta blocker) salmeterol (beta agonist) warfarin (anticoagulant) clopidogrel, becoming bioactivated (antiplatelet) esomeprazole (proton pump inhibitor) nateglinide (antidiabetic)	strong: protease inhibitors ritonavir indinavir nelfinavir saquinavir some macrolide antibiotics clarithromycin telithromycin chloramphenicol (antibiotic) some azole antifungals ketoconazole itraconazole nefazodone (antidepressant) moderate aprepitant (antiemetic) some calcium channel blockers verapamil diltiazem some macrolide antibiotics erythromycin some azole antifungals fluconazole bergamottin (constituent of grapefruit juice) Valerian weak: cimetidine (H2-receptor antagonist) buprenorphine (analgesic) cafestol (in unfiltered coffee) unspecified potency: amiodarone (antiarrhythmic) bicalutamide ciprofloxacin (antibiotic) dithiocarbamate (functional group) voriconazole (antifungal) imatinib (anticancer) mifepristone (abortifacient) norfloxacin (antibiotic) some non-nucleoside reverse transcriptase inhibitors delavirdine gestodene (hormonal contraceptive) mibefradil (in angina pectoris) SSRIs fluoxetine/norfluoxetine fluvoxamine star fruit milk thistle ginko biloba quercetin – Quercetin has been shown to act as an initial inhibitor and subsequent inducer. piperine	anticonvulsants, mood stabilizers carbamazepine phenytoin (anticonvulsant) oxcarbazepine barbiturates phenobarbital St. John's wort some bactericidals rifampicin rifabutin some non-nucleoside reverse transcriptase inhibitors efavirenz nevirapine some hypoglycemics pioglitazone troglitazone glucocorticoids (blood glucose increase, immunosuppressive) modafinil (stimulant) Read more about this topic: CYP3A4 Source(s): Wikipedia Ligands (Creative Commons) Copyright © 2024 • Contact Us • Privacy Policy