Table of Contents
What are P-glycoprotein inhibitors?
Some common pharmacological inhibitors of P-glycoprotein include: amiodarone, clarithromycin, ciclosporin, colchicine, diltiazem, erythromycin, felodipine, ketoconazole, lansoprazole, omeprazole and other proton-pump inhibitors, nifedipine, paroxetine, reserpine, saquinavir, sertraline, quinidine, tamoxifen, verapamil.
Does verapamil inhibit P-gp?
Conclusions: Verapamil may offer pharmacoresistant patients hope of improved seizure control due to its potential P-glycoprotein inhibitory effects.
Is aspirin a P-gp inhibitor?
Intestinal absorption, biliary excretion, and urinary excretion of P-gp substrates can therefore be altered by either the inhibition or induction of P-gp….Antiarrhythmic drugs.
| Drug | Substrate | Inhibitor |
|---|---|---|
| Antiplatelet agents | ||
| Aspirin∗ | ||
| Clopidogrel | × | |
| Dipyridamole | + |
Is P-glycoprotein the same as MDR1?
MDR1, more commonly referred to as P-gp or P-glycoprotein, is an efflux transporter that serves two major drug transport functions.
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 do P glycoproteins do?
P-glycoprotein is one of the drug transporters that determine the uptake and efflux of a range of drugs. This process affects their plasma and tissue concentrations and ultimately their final effects. P-glycoprotein functions as a transmembrane efflux pump, pumping its substrates from inside to outside the cell.
What are CYP3A4 inducers?
Inducers of CYP3A4 include phenobarbital, phenytoin, rifampicin, St. John’s Wort and glucocorticoids.