Miscellaneous

What drugs are P-gp inhibitors?

Contents

What drugs are P-gp 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.

Which transporters are efflux transporters?

These include members of the P-glycoprotein (P-gp) or ABCB family, the multidrug resistance protein (MRP) or ABCC family, and the breast cancer resistance protein (BCRP) transporter of the ABCG family. These proteins are commonly referred to as multidrug or efflux transporters.

What is a transport inhibitor?

A transport inhibitor was a device that blocked transporters attempting to dematerialize objects in a specific area.

Is amiodarone a P-gp inhibitor?

Amiodarone, a potent inhibitor of P-gp, increased mean serum digoxin levels from 0.97 to 1.98 μg/l when administered orally at doses of 600 to 1,600 mg/day (15). Oral amiodarone inhibits intestinal P-gp membrane efflux of digoxin and its secretion from renal tubules (15).

Is omeprazole a P-gp inhibitor?

… S-omeprazole, the active enantiomer, is a competitive and time-dependent inhibitor of CYP2C19 (68). Furthermore, omeprazole is a substrate of P-gp and other membrane transporters and also an inhibitor of P-gp (69) .

What do ABC transporters transport?

ABC transporters utilize the energy of ATP binding and hydrolysis to transport various substrates across cellular membranes. They are divided into three main functional categories. The substrates that can be transported include ions, amino acids, peptides, sugars, and other molecules that are mostly hydrophilic.

What is drug efflux transporters?

Efflux cell membrane transporters are not only responsible for moving the parent drug and metabolites of some medications out of the cell, but may also contribute to drug resistance by diminishing the desired therapeutic or biologic effect.

How does P glycoprotein decrease absorption?

Summary. Efflux transporters such as P-glycoprotein play an important role in drug transport in many organs. In the gut, P-glycoprotein pumps drugs back into the lumen, decreasing their absorption. Many, but not all, of the drugs which are transported by P-glycoprotein are also metabolised by cytochrome P450 3A4.

How are efflux pump inhibitors used in medicine?

The efflux pump inhibitors as new therapeutic agents. The continuous increase in the development of multidrug resistance by many pathogens has resulted in difficulties fighting many infectious diseases.

Which is part of the efflux pump transporter?

The efflux pump transporter in Pseudomonas aeruginosa belongs to the (RND) family. It is composed of three parts, the transporter, the linker, and the outer membrane pore that ensures that the extruded compound does not remain in the periplasm, hence, avoiding its return to the cytosol ( 15 ).

Which is a selective efflux transporter in Caco-2?

In Caco-2 cells, which express P-gp, BCRP, and MRP2, FTC (1 µM) selectively inhibited the efflux of BCRP substrates estrone-3-sulfate and genistein; however, at 10 µM, FTC partially inhibited the efflux of P-gp substrates paclitaxel and digoxin.

How is the efflux pump transporter in Pseudomonas aeruginosa?

The efflux pump transporter in Pseudomonas aeruginosa belongs to the (RND) family. It is composed of three parts, the transporter, the linker, and the outer membrane pore that ensures that the extruded compound does not remain in the periplasm, hence, avoiding its return to the cytosol (15).