What drugs are P-gp inhibitors?

What drugs are P-gp inhibitors?

Pgp inhibitors include amiodarone, clarithromycin, cyclosporine, diltiazem, erythromycin, ketoconazole, itraconazole, propafenone, quinidine, and verapamil.

What are inhibitors of P-gp or BCRP?

Inhibition of P-glycoprotein and/or BCRP is therefore a logical strategy to improve oral absorption, CNS penetration and delivery of anticancer agents to brain tumors or CNS metastases.

What anticancer drugs would be affected by P-glycoprotein?

A plethora of anticancer drugs that are central to many chemotherapeutic regimes are susceptible to P-gp-mediated efflux (Figure 1), such as the microtubule-targeting vinca alkaloids (e.g. vinblastine and vincristine) and taxanes (paclitaxel and docetaxel), the DNA-chelating anthracyclines (doxorubicin and daunorubicin …

Is azithromycin a P-gp inhibitor?

The FDA approved macrolide antibiotics (erythromycin, azithromycin, and clarithromycin) were all reported as p-gp inhibitors.

Is digoxin a P-gp inhibitor?

Conclusions—Quinidine and digoxin are both substrates for P-glycoprotein, and quinidine is a potent inhibitor of digoxin transport in vitro.

Is colchicine a P-gp inhibitor?

Colchicine is a known substrate for Pglycoprotein (PGP), a transmembrane protein that acts to eliminate drugs by expelling them into the bile, urine, and intestine and acting as a blood-brain barrier.

What are P glycoprotein inducers?

Common pharmacological inducers of P-glycoprotein include carbamazepine, dexamethasone, doxorubicin, nefazodone, phenobarbital, phenytoin, prazosin, rifampicin, St. John’s wort, tenofovir, tipranavir, trazodone, and vinblastine.

What is an example of an enzyme inhibitor?

Examples of enzyme-inhibiting agents are cimetidine, erythromycin, ciprofloxacin, and isoniazid.

Is omeprazole a P-gp inhibitor?

Omeprazole is primarily metabolized by CYP3A4 and CYP2C9 enzymes and is a substrate and inhibitor of P-gp efflux transporters [10] . …

Is bisoprolol a P-gp inhibitor?

Beta-Blockers Significant P-gp inhibition was similarly observed for bisoprolol and propranolol, whereas atenolol (39), metoprolol (21), and sotalol (21) had no effect.

What are CYP3A4 inducers?

CYP3A4 inducers are drugs that increase the activity of CYP3A4. Note that the CYP3A4 enzyme is particularly susceptible to enzyme inducers, and marked reductions in the plasma concentrations of CYP3A4 substrates may occur.

Is carbamazepine a P-gp inducer?

Conclusions: Carbamazepine induces Pgp in a manner comparable to rifampicin, by increasing binding to the DR4 element. This has implications for interactions involving drugs whose site of action is the lymphocyte.

Does tacrolimus inhibit P-gp?

The results showed that tacrolimus suppresses drug exclusion by inhibiting P-glycoprotein, thus allowing restoration of therapeutic levels of corticosteroids within the cells.

What are 3 examples of inhibitors?

Examples of slow-binding inhibitors include some important drugs, such methotrexate, allopurinol, and the activated form of acyclovir.

What are p450 inducers?

Cytochrome P-450 enzyme inducers (e.g., rifampin, phenytoin, phenobarbital) decrease the bioavailability and increase the clearance of verapamil and diltiazem. St. John’s wort also significantly decreases verapamil bioavailability through induction of first-pass metabolism in the gut.