What are some CYP3A4 inhibitors?
Potent inhibitors of CYP3A4 include clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole, ritonavir, verapamil, goldenseal and grapefruit.
What are moderate CYP3A4 inhibitors?
Moderate inhibitors of CYP3A4 include: amiodarone, erythromycin, fluconazole, miconazole, diltiazem, verapamil, delavirdine, amprenavir, fosamprenavir, conivaptan.
What drugs are CYP3A inducers?
CYP3A inducers include the glucocorticoids, rifampin, carbamazepine, phenobarbital, and phenytoin. Among the many significant CYP3A inhibitors are grapefruit juice, erythromycin, ketoconazole, clarithromycin, and verapamil.
Is amiodarone a CYP3A4 inhibitor?
Amiodarone is a substrate of CYP3A4 and CYP2C8 and an inhibitor of CYP2C9, CYP2D6, CYP3A4, and p-glycoprotein.
Is azithromycin a CYP3A4 inhibitor?
Azithromycin has been shown to be a weak substrate for CYP3A4, to be minimally metabolized by the enzyme, and to neither induce nor inhibit CYP3A4 activity [16].
Is simvastatin a CYP3A4 inhibitor?
Simvastatin and atorvastatin, two widely prescribed cholesterol lowering medicines, are both metabolised by the isoenzyme cytochrome P450 3A4 (CYP3A4).
Is amoxicillin a CYP3A4 inhibitor?
Clarithromycin and amoxicillin, being respectively an inhibitor of CYP3A4 and CYP2C8, there is a possibility of developing drug interactions when used as triple therapy [12,13].
Is colchicine a CYP3A4 inhibitor?
7 DRUG INTERACTIONS Colchicine is a substrate of the CYP3A4 metabolizing enzyme and the P-glycoprotein (P-gp) efflux transporter. Fatal drug interactions have been reported when colchicine is administered with clarithromycin, a dual inhibitor of CYP3A4 and P- glycoprotein.
Is dexamethasone a CYP3A4 inducer?
Dexamethasone is a steroidal antiinflammatory agent which is used e.g. in the treatment of chronic inflammatory and autoimmune diseases. In cultures of human hepatocytes, dexamethasone is a potent inducer of CYP3A4 (Pichard et al. 1992).
What drugs are metabolised by CYP3A4?
Cytochrome P450 enzymes metabolize approximately 60% of prescribed drugs, with CYP3A4 responsible for about half of this metabolism; substrates include acetaminophen, codeine, ciclosporin (cyclosporin), diazepam, and erythromycin. The enzyme also metabolizes some steroids and carcinogens.
Is verapamil a CYP3A4 inhibitor?
However, verapamil and diltiazem are moderate mechanism-based inhibitors of CYP3A4 and may still cause significant inhibition of CYP3A4-mediated metabolism of simvastatin in vivo during chronic therapy.