Rosuvastatin pharmacokinetics

D. W. (2004) Rosuvastatin pharmacokinetics in heart transplant recipients administered an antirejection regimen including cyclosporine. Clinical Pharmacology and Therapeutics, 76, 167-177. 

Simonson, S.G., Raza, A., Martin, P.D., Mitchell, P.D., Jarcho, J.A., Brown, C.D.A., Windass, A.S. and Schneck, D.W. (2004) Rosuvastatin pharmacokinetics in heart transplant recipients administered an antirejection regimen including cyclosporine. Clinical Pharmacology and Therapeutics (St. Louis), 76, 167-177. 

Z. R., Fen, J., Huang, Y.F. and Zhou, H.H. (2006) Role of BCRP 421C>A polymorphism on rosuvastatin pharmacokinetics in healthy Chinese... 

Lee, E., Ryan, S., Birmingham, B., Zalikowski, J., March, R., Ambrose, H., Moore, R Lee, C., Chen, Y. and Schneck, D. (2005) Rosuvastatin pharmacokinetics and pharmacogenetics in white and Asian subjects residing in the same environment Clinical Pharmacology and Therapeutics, 78, 330—341. 

Atorva tatin and ro uva tatin may modestly increase the plasma levels of combined oral contraceptives. Rosuvastatin pharmacokinetics and lipid-lowering effects were unaffected by an oral contraceptive containing ethinylestradiol and norgestimate. The pharmacokinetics of a single dose of pravastatin were also unaffected by combined oral contraceptives. However, norethisterone abolished the beneficial effects of atorvastatin and/or estradiol on the lipid profile. 

Md.K. Pasha, S. Muzeeb, S.J.S. Basha, D. Shashikumar, R. Mullangi, N.R. Srinivas, Analysis of five HMG-CoA reductase inhibitors—atorvastatin, lovastatin, pravastatin, rosuvastatin and simvastatin pharmacological, pharmacokinetic and analytical overview and development of a new method for use in pharmaceutical formulations analysis and in vitro metabolism studies, Biomed. Chromatogr. 20 (2006) 282-293. 

The hydrophilic statins (pravastatin, rosuvastatin) are only partly metabolised by the liver [1, 17, 19]. Pravastatin is also metabolised in the stomach [26]. The pharmacokinetics of pravastatin have been shown to change in liver disease, despite its dual route (renal and hepatic) of elimination [27]. Nonetheless, it has been used in liver disease and has been suggested as the statin of choice [26]. Liver metabolism is of minor importance in the clearance of rosuvastatin and its pharmacokinetics are not altered by mild to moderate liver impairment. However, the area under the curve (AUC) is increased in severe liver impairment [1]. Clinical experience with rosuvastatin in liver disease is lacking, and it therefore cannot be recommended. 

Martin PD, Kemp J, Dane AL, Warwick MJ, Schneck DW. No effect of rosuvastatin on the pharmacokinetics of digoxin in healthy volunteers. J Clin Pharmacol 2002 42(12) 1352-7. 

The effect of fluconazole on the pharmacokinetics of rosuvastatin has been investigated in a randomized, double-blind, two-way, crossover, placebo-controlled study... 

The validated bioanalysis of rosuvastatin in human plasma by automated SPE in 96-well format with Oasis HLB material and positive-ion LC-ESI-MS-MS was reported using a [DJ-ILIS [54]. The stability of rosuvastatin and its potential conversion into the lactone due to sample pretreatment was thoroughly investigated. The method was applied in pharmacokinetic studies during clinical trials. A similar method was applied by the same group in the bioanalysis of the /V-desmethyl metabolite of rosuvastatin [55]. 

Keskitalo JE, Zolk O, Fromm MF, Kurkinen KJ, Neuvonen PJ, Niemi M (2009) ABCG2 polymorphism markedly affects the pharmacokinetics of atorvastatin and rosuvastatin. Clin Pharmacol Ther 86 197-203... 

Pasanen, M.K., Fredrikson, H., Neuvonen, P.J. and Niemi, M. (2007) Different effects of SLCOIBI polymorphism on the pharmacokinetics of atorvastatin and rosuvastatin. Clinical Pharmacology and Therapeutics, 82, 726-733. 

Vittal, S., Shitut, N.R., Kumar, T.R. et al. (2006) Simultaneous quantitation of rosuvastatin and gemfibrozil in human plasma by high-performance liquid chromatography and its application to a pharmacokinetic study. Biomed Chrom, 20 (11), 1252-1259. 

Simonson SG, Martin PD, Mitchell PD, Lasseter K, Gibson G, Schneck DW. Effect of rosuvastatin on warfarin pharmacodynamics and pharmacokinetics. J Clin Pharmacol 2005 45,927-34. 

Atorvastatin, fluvastatin and simvastatin cause small but probably clinically unimportant increases in the serum levels of digoxin. Pravastatin and rosuvastatin appear to have no effect on digoxin pharmacokinetics. 

Simonson SG, Martin PD, Warwick MJ, Mitchell PD, Schneck DW. The effect of rosuvastatin on oestrogen progestin pharmacokinetics in healthy women taking an oral contraceptive. Br J CUn Pharmacol (2004) 57, 279-86. 

Cooper KJ, Martin PD, Dane AL, Warwick MJ, Raa A, SdmeckDW. Lack of effect of ke-toconazole on the pharmacokinetics of rosuvastatin in healtl subjects. BrJ Clin Pharmacol (2003) 55,94-9. 

Ezetimibe does not appear to have adverse pharmacokinetic interactions with atorvastatin, fluvastatin, iovastatin, rosuvastatin or simvastatin. However, some evidence suggests that concurrent use may increase the risk of myopathy. 

In a placebo-controlled study 12 otherwise healthy subjects with hyperc-holesterolaemia were given ezetimibe 10 mg daily with rosuvastatin 10 mg daily for 14 days. The combination was well tolerated (no significant changes in liver enzymes or creatinine phosphokinase noted), the pharmacokinetics of both drugs were not significantly changed, and an enhanced lowering of LDL-cholesterol was noted, which was considered to be clinically favourable. ... 

The plasma levels of lovastatin, simvastatin, atorvastatin and pravastatin are increased by gemfibrozil, the levels of fluvastatin are increased by bezaflbrate, and the levels of pravastatin are increased by fenoflbrate. No pharmacokinetic interactions occur with the combinations of fluvastatin with gemfibrozil, lovastatin with bezaflbrate, and pravastatin, rosuvastatin or simvastatin with fenoflbrate. Both statins and fibrates are known to cause rhabdomyolysis, and their concurrent use increases the risk of this reaction. 

Martin PD, Dane AL, Schneck DW, Warwick MJ. An open-label, randomized, diree-way crossover ttial of the effect of coadministration of rosuvastatin and fenofibrate on die pharmacokinetic properties of rosuvastatin and fenofibric acid in healthy male volunteers. Clin Ther(2003) 25, 459-71. 

Schneck DW, Birmingham BK, ZaUkowski JA, Mitchell PD, Wmig Y, Martin PD, Lasseter KC, Brown CDA, Windass AS, Raza A. The effect of gemfibrozil on the pharmacokinetics of rosuvastatin. Clin Pharmacol Ther (2004) 75, 455-63. 

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