What is P-glycoprotein transporter?
Pgp (P-glycoprotein) (ABCB1) is an ATP-powered efflux pump which can transport hundreds of structurally unrelated hydrophobic amphipathic compounds, including therapeutic drugs, peptides and lipid-like compounds. It forms a major component of the blood-brain barrier and restricts the uptake of drugs from the intestine.
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 atorvastatin a P-gp inhibitor?
Although atorvastatin has been described as an inhibitor of P-gp, higher concentrations are required for maximal P-gp inhibition. Patients receiving concomitant statin therapy with other P-gp-mediated agents should be monitored closely for adverse events.
Is diltiazem a P-gp inhibitor?
Pgp inhibitors include amiodarone, clarithromycin, cyclosporine, diltiazem, erythromycin, ketoconazole, itraconazole, propafenone, quinidine, and verapamil.
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 rifampin a P-gp inhibitor?
☑ Physiologically-based pharmacokinetic (PBPK) modeling is increasingly being applied to predict clinical drug–drug interactions (DDIs). Rifampin is a well-known inducer for not only cytochrome P450 (CYP) 3A but also P-glycoprotein (Pgp).
Is digoxin a P-gp substrate?
Digoxin is certainly a sensitive probe substrate of P-gp in in vitro studies, as evidenced by a high efflux ratio across Caco-2, MDR1-MDCK and MDR1-LLCPK1 cells, as well as effective inhibition of efflux in the presence of P-gp inhibitors.
What is milrinone contraindicated for?
Milrinone is contraindicated in patients with a milrinone hypersensitivity. Solutions containing dextrose may be contraindicated in those with a known corn hypersensitivity. Do not use milrinone in patients with severe obstructive aortic or pulmonic valvular heart disease in lieu of surgical relief of the obstruction.
