Effect of itraconazole on the pharmacokinetics of rosuvastatin

Rosuvastatin is a new 3‐hydroxy‐3‐methylglutaryl coenzyme A (HMG‐CoA) reductase inhibitor. Itraconazole, an inhibitor of cytochrome P450 (CYP) 3A4 and the transport protein P‐glycoprotein, is known to interact with other HMG‐CoA reductase inhibitors. The current trials aimed to examine in vivo the effect of itraconazole on the pharmacokinetics of rosuvastatin.

[1]  U. Christians,et al.  Comparison of cytochrome P-450-dependent metabolism and drug interactions of the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitors lovastatin and pravastatin in the liver. , 1999, Drug metabolism and disposition: the biological fate of chemicals.

[2]  P. Martin,et al.  Quantification of rosuvastatin in human plasma by automated solid-phase extraction using tandem mass spectrometric detection. , 2002, Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.

[3]  P. Neuvonen,et al.  Itraconazole drastically increases plasma concentrations of lovastatin and lovastatin acid , 1996, Clinical pharmacology and therapeutics.

[4]  A. Olsson,et al.  Effect of rosuvastatin on low-density lipoprotein cholesterol in patients with hypercholesterolemia. , 2001, The American journal of cardiology.

[5]  A. Mazzu,et al.  Itraconazole alters the pharmacokinetics of atorvastatin to a greater extent than either cerivastatin or pravastatin , 2000, Clinical pharmacology and therapeutics.

[6]  G. Granneman,et al.  Use of In Vitro and In Vivo Data to Estimate the Likelihood of Metabolic Pharmacokinetic Interactions , 1997, Clinical pharmacokinetics.

[7]  B H Arison,et al.  In vitro metabolism of simvastatin in humans [SBT]identification of metabolizing enzymes and effect of the drug on hepatic P450s. , 1997, Drug metabolism and disposition: the biological fate of chemicals.

[8]  Paul D. Martin,et al.  No Effect of Rosuvastatin on the Pharmacokinetics of Digoxin in Healthy Volunteers , 2002, Journal of clinical pharmacology.

[9]  P. Neuvonen,et al.  Different effects of itraconazole on the pharmacokinetics of fluvastatin and lovastatin. , 1998, British journal of clinical pharmacology.

[10]  P. Neuvonen,et al.  Simvastatin but not pravastatin is very susceptible to interaction with the CYP3A4 inhibitor itraconazole , 1998, Clinical pharmacology and therapeutics.

[11]  P. Neuvonen,et al.  Effect of itraconazole on the pharmacokinetics of atorvastatin , 1998, Clinical pharmacology and therapeutics.

[12]  K. Bleasby,et al.  Rosuvastatin is a high affinity substrate of hepatic organic anion transporter OATP-C , 2001 .

[13]  Shiew-Mei Huang,et al.  Optimizing Drug Development: Strategies to Assess Drug Metabolism/Transporter Interaction Potential—Toward a Consensus , 2001, Pharmaceutical Research.

[14]  No Effect of Age or Gender on the Pharmacokinetics of Rosuvastatin: A New HMG‐CoA Reductase Inhibitor , 2002, Journal of clinical pharmacology.

[15]  Paul D. Martin,et al.  Lack of effect of ketoconazole on the pharmacokinetics of rosuvastatin in healthy subjects. , 2003, British journal of clinical pharmacology.