What 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.

What are CYP3A4 inhibitors and inducers?

Potent inhibitors of CYP3A4 include clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole, ritonavir, verapamil, goldenseal and grapefruit. Inducers of CYP3A4 include phenobarbital, phenytoin, rifampicin, St. John’s Wort and glucocorticoids.

What is the role of P-glycoprotein on pharmacokinetic aspects?

P-glycoprotein, the most extensively studied ATP-binding cassette (ABC) transporter, functions as a biological barrier by extruding toxins and xenobiotics out of cells. In vitro and in vivo studies have demonstrated that P-glycoprotein plays a significant role in drug absorption and disposition.

What drugs are substrates of the P-gp efflux pump?

Examples of drugs that are substrates of P-gp efflux pump include: Apixaban, colchicine, cyclosporine, dabigatran, digoxin, edoxaban, rivaroxaban, and tacrolimus. The degree of effect on P-gp substrate serum concentration may be altered by dose and timing of orally administered P-gp inhibitor or inducer.

Does P-glycoprotein interact with drug transporters?

Expression of P-glycoprotein can have important effects on drug absorption, distribution and elimination. Although interactions with drug transporters can be clinically insignificant, an awareness of potential transporter-related drug-drug interactions is important.

What is the function of the efflux pump ATP-GP?

P-gp is an ATP-dependent drug efflux pump for xenobiotic compounds with broad substrate specificity. It is responsible for decreased drug accumulation in multidrug-resistant cells and often mediates the development of resistance to anticancer drugs.

What drugs are inhibitors of the P-glycoprotein?

Inhibitors and inducers of P-glycoprotein (P-gp) drug efflux pump (P-gp multidrug resistance transporter) Inhibitors of P-gp. Amiodarone. Neratinib. Azithromycin (systemic) Ombitasvir-paritaprevir-ritonavir (Technivie)*. Capmatinib. Osimertinib.