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Drug interactions with lipid‐lowering drugs: Mechanisms and clinical relevance
The effects of cyclosporine and gemfibrozil explain the increased plasma statin concentrations and, together with pharmacodynamic factors, the increased risk of myotoxicity when coadministered with statins.
Organic Anion Transporting Polypeptide 1B1: a Genetically Polymorphic Transporter of Major Importance for Hepatic Drug Uptake
Current knowledge about the expression, function, substrate characteristics, and pharmacogenetics of OATP1B1 as well as its role in drug interactions are reviewed, in parts comparing with those of other hepatocyte-expressed organic anion transporting polypeptides, OATp1B3 and O ATP2B1.
Gemfibrozil greatly increases plasma concentrations of cerivastatin
The effect of gemfibrozil on cerivastatin pharmacokinetics was studied to study the mechanism of this potentially fatal drug interaction.
Polymorphic Organic Anion Transporting Polypeptide 1B1 is a Major Determinant of Repaglinide Pharmacokinetics
The aim was to investigate possible associations between the pharmacokinetics of repaglinide and single nucleotide polymorphisms (SNPs) in the genes encoding for the drug transporters organic anion transporting polypeptide 1B1 and P‐glycoprotein and the drug‐metabolizing enzymes cytochrome P450 (CYP) 2C8 and CYP3A5.
SLCO1B1 polymorphism markedly affects the pharmacokinetics of simvastatin acid
Raised plasma concentrations of simvastatin acid in patients carrying the SLCO1B1 c.521C variant allele may enhance the risk of systemic adverse effects during simVastatin treatment and reduce its cholesterol-lowering efficacy, respectively.
High plasma pravastatin concentrations are associated with single nucleotide polymorphisms and haplotypes of organic anion transporting polypeptide-C (OATP-C, SLCO1B1).
This study aimed to characterize possible relationships between polymorphisms in the drug transporter genes organic anion transporting polypeptide-C (OATP-C, SLCO1B1), OATP-B (SLCO2B1), multidrug
Pharmacokinetic Interactions with Rifampicin
The antituberculosis drug rifampicin (rifampin) induces a number of drug-metabolising enzymes, having the greatest effects on the expression of cytochrome P450 (CYP) 3A4 in the liver and in the small intestine, which influences drug metabolism and transport.
Pharmacokinetics of metformin after intravenous and oral administration to man
The kinetics of14C-metformin have been studied in five healthy subjects after oral and intravenous administration, which resulted in a plasma concentration profile of “flip-flop” type for oral metformin.
Cyclosporine markedly raises the plasma concentrations of repaglinide
The effects of cyclosporine (INN, ciclosporin), an inhibitor of CYP3A4 and OATP1B1, on the pharmacokinetics and pharmacodynamics of repaglinide are studied.
Metabolism of repaglinide by CYP2C8 and CYP3A4 in vitro: effect of fibrates and rifampicin.
Both CYP2C8 and CYP3A4 are important in the metabolism of therapeutic concentrations of repaglinide in vitro, but their predicted contributions in vivo are highly dependent on the scaling factor used.