No Effect of Age or Gender on the Pharmacokinetics of Rosuvastatin: A New HMG-CoA Reductase Inhibitor

• Published in: Journal of clinical pharmacology 2002-10, Vol.42 (10), p.1116-1121
• Main Authors: Martin, Paul D., Dane, Aaron L., Nwose, Olise M., Schneck, Dennis W, Warwick, Mike J.
• Format: Article
• Language: English
• Subjects: Administration, Oral; Adolescent; Adult; Age Factors; Aged; Area Under Curve; Biological and medical sciences; Female; Fluorobenzenes - adverse effects; Fluorobenzenes - blood; Fluorobenzenes - pharmacokinetics; General and cellular metabolism. Vitamins; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors - adverse effects; Hydroxymethylglutaryl-CoA Reductase Inhibitors - blood; Hydroxymethylglutaryl-CoA Reductase Inhibitors - pharmacokinetics; Male; Medical sciences; Pharmacology. Drug treatments; Pyrimidines; Rosuvastatin Calcium; Sex Factors; Sulfonamides
• ISSN: 0091-2700; 1552-4604
• DOI: 10.1177/009127002237987

The effects of age and gender on the pharmacokinetics of rosuvastatin (Crestor™) were assessed in healthy young (18–35 years) and elderly (< 65 years) males and females in this open, nonrandomized, noncontrolled, parallel‐group trial. Sixteen males and 16 females (8 young and elderly volunteers per gender group) were enrolled. Mean (range) ages were 24 (18–33) and 68 (65–73) years for young and elderly volunteers, respectively. Volunteers were given a single oral 40 mg dose of rosuvastatin. Blood samples for measurement of rosuvastatin plasma concentration were collected up to 96 hours following dosing. Age and gender effects were assessed by constructing 90% confidence intervals (CIs) around the ratios of young/elderly and male/female geometric least square means (glsmeans) for AUC(0‐t) and Cmax (derived from ANOVA of log‐transformed parameters). Small differences in rosuvastatin pharmacokinetics were noted between age and gender groups. Glsmean AUC(0‐t) was 6% higher (90% CI = 0.86‐1.30) and glsmean Cmax 12% higher (90% CI= 0.83‐1.51) in the young compared with the elderly group. Glsmean AUC(0‐t) was 9% lower (90% CI= 0.74‐1.12) and glsmean Cmax 18% lower (90% CI = 0.61‐1.11) in the male compared with the female group. These small differences are not considered clinically relevant, and dose adjustments based on age or gender are not anticipated. Rosuvastatin was well tolerated in all volunteers.