What drugs inhibit P-glycoprotein?

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.

What is the role of P-glycoprotein?

P-glycoprotein is one of the drug transporters that determine the uptake and efflux of a range of drugs. P-glycoprotein functions as a transmembrane efflux pump, pumping its substrates from inside to outside the cell. Drugs which induce or inhibit P-glycoprotein can interact with other drugs handled by the pump.

How does P-glycoprotein work in intestine?

P-glycoprotein, a membrane-associated transport protein, has recently been recognised as an important element of the intestinal epithelium. These data show that P-glycoprotein contributes to the elimination of many drugs by mediating their direct secretion from the blood into the intestinal lumen.

Does azithromycin inhibit P-glycoprotein?

Macrolides: Erythromycin, Azithromycin, and Clarithromycin The FDA approved macrolide antibiotics (erythromycin, azithromycin, and clarithromycin) were all reported as p-gp inhibitors. This has been supported by many studies in the literature (64–66).

What is expression of P-glycoprotein?

P-glycoprotein (Pgp) is the first detected and the best characterized of ABC drug efflux transporters. Apart from tumor cells, its constitutive expression has been reported in a variety of other tissues, such as the intestine, brain, liver, placenta, kidney, and others.

What is the clinical relevance of P-glycoprotein P-gp?

The drug efflux transporter P-glycoprotein (P-gp) is known to confer multidrug resistance in cancer chemotherapy. Because of its expression and localization, it has been suggested that P-gp plays an important role in cancer chemotherapy, intestinal absorption, and brain uptake.

What is P-glycoprotein role in multi drug resistant cancers?

P-glycoprotein (P-gp) is a well-identified membrane transporter with capability to efflux drug molecules out of the cancer cell leading to reduced efficiency of chemotherapy. Cancer cells upregulate P-gp expression as an adaptive response to evade chemotherapy mediated cell death.

Is carvedilol a P glycoprotein inhibitor?

Carvedilol inhibits P-gp activity to a similar degree as verapamil, increasing serum digoxin levels up to 32% (39). Significant P-gp inhibition was similarly observed for bisoprolol and propranolol, whereas atenolol (39), metoprolol (21), and sotalol (21) had no effect.

What is the impact of P-glycoprotein P-gp at the blood brain barrier?

Purpose: P-glycoprotein (Pgp) is an efflux transporter involved in transport of several compounds across the blood-brain barrier (BBB). Loss of Pgp function with increasing age may be involved in the development of age-related disorders, but this may differ between males and females.

What is the glycoprotein that is most commonly associated with multidrug resistance?

P-glycoprotein (P-gp) is a membrane protein associated with multidrug resistance (MDR) due to its key role in mediating the traffic of chemotherapeutic drugs outside cancer cells, leading to a cellular response that hinders efforts toward successful therapy.

How do you think this overexpression of P-glycoprotein may have happened?

However, overexpression of P-gp may be induced by selection and/or adaptation of cells during exposure to anticancer drugs; this particular example is known as acquired P-gp-mediated MDR. Drugs that are potential inducers of P-gp are often substrates of this transporter.