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Influence of body weight and gender on the pharmacokinetics, pharmacodynamics, and antihypertensive efficacy of aliskiren.
J Clin Pharmacol. 2010 Dec; 50(12):1358-66.JC

Abstract

Gender and body weight influence the pharmacokinetics and pharmacodynamics of many drugs. This pooled analysis of 17 clinical studies evaluated the effect of gender, body mass index (BMI), body weight, and lean body weight (LBW) on the pharmacokinetics of the direct renin inhibitor aliskiren in healthy volunteers (n = 392). A separate pooled analysis of 5 clinical studies in patients with hypertension (n = 2327) assessed the influence of gender and BMI on the effects of aliskiren on plasma renin activity and blood pressure. Area under the aliskiren plasma concentration-time curve (AUC(τ)) was 22% lower and the peak aliskiren plasma concentration (C(max)) was 24% lower in men than women (P < .05). BMI was not significantly correlated with AUC(τ) (r = 0.005; P = .917); AUC(τ) was negatively correlated with body weight (r = -0.235; P < .0001) and LBW (r = -0.295; P < .0001). Results were similar for C(max). Adjusting individual aliskiren AUC(τ) and C(max) values for overall mean body weight or LBW abolished gender differences. Based on r(2) values, LBW variation accounted for 8.9% of aliskiren AUC(τ) variation. In patients with hypertension, gender and BMI did not significantly influence the effects of aliskiren on plasma renin activity or blood pressure. It was concluded that lower systemic exposure to aliskiren in men versus women relates to differences in body weight; neither gender nor body weight has clinically relevant effects on the pharmacokinetics or pharmacodynamics of aliskiren.

Authors+Show Affiliations

Novartis Pharmaceuticals Corporation, East Hanover, New Jersey, USA.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20150520

Citation

Jarugula, Venkateswar, et al. "Influence of Body Weight and Gender On the Pharmacokinetics, Pharmacodynamics, and Antihypertensive Efficacy of Aliskiren." Journal of Clinical Pharmacology, vol. 50, no. 12, 2010, pp. 1358-66.
Jarugula V, Yeh CM, Howard D, et al. Influence of body weight and gender on the pharmacokinetics, pharmacodynamics, and antihypertensive efficacy of aliskiren. J Clin Pharmacol. 2010;50(12):1358-66.
Jarugula, V., Yeh, C. M., Howard, D., Bush, C., Keefe, D. L., & Dole, W. P. (2010). Influence of body weight and gender on the pharmacokinetics, pharmacodynamics, and antihypertensive efficacy of aliskiren. Journal of Clinical Pharmacology, 50(12), 1358-66. https://doi.org/10.1177/0091270009359525
Jarugula V, et al. Influence of Body Weight and Gender On the Pharmacokinetics, Pharmacodynamics, and Antihypertensive Efficacy of Aliskiren. J Clin Pharmacol. 2010;50(12):1358-66. PubMed PMID: 20150520.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Influence of body weight and gender on the pharmacokinetics, pharmacodynamics, and antihypertensive efficacy of aliskiren. AU - Jarugula,Venkateswar, AU - Yeh,Ching-Ming, AU - Howard,Dan, AU - Bush,Christopher, AU - Keefe,Deborah L, AU - Dole,William P, Y1 - 2010/02/11/ PY - 2010/2/13/entrez PY - 2010/2/13/pubmed PY - 2011/3/5/medline SP - 1358 EP - 66 JF - Journal of clinical pharmacology JO - J Clin Pharmacol VL - 50 IS - 12 N2 - Gender and body weight influence the pharmacokinetics and pharmacodynamics of many drugs. This pooled analysis of 17 clinical studies evaluated the effect of gender, body mass index (BMI), body weight, and lean body weight (LBW) on the pharmacokinetics of the direct renin inhibitor aliskiren in healthy volunteers (n = 392). A separate pooled analysis of 5 clinical studies in patients with hypertension (n = 2327) assessed the influence of gender and BMI on the effects of aliskiren on plasma renin activity and blood pressure. Area under the aliskiren plasma concentration-time curve (AUC(τ)) was 22% lower and the peak aliskiren plasma concentration (C(max)) was 24% lower in men than women (P < .05). BMI was not significantly correlated with AUC(τ) (r = 0.005; P = .917); AUC(τ) was negatively correlated with body weight (r = -0.235; P < .0001) and LBW (r = -0.295; P < .0001). Results were similar for C(max). Adjusting individual aliskiren AUC(τ) and C(max) values for overall mean body weight or LBW abolished gender differences. Based on r(2) values, LBW variation accounted for 8.9% of aliskiren AUC(τ) variation. In patients with hypertension, gender and BMI did not significantly influence the effects of aliskiren on plasma renin activity or blood pressure. It was concluded that lower systemic exposure to aliskiren in men versus women relates to differences in body weight; neither gender nor body weight has clinically relevant effects on the pharmacokinetics or pharmacodynamics of aliskiren. SN - 1552-4604 UR - https://www.unboundmedicine.com/medline/citation/20150520/Influence_of_body_weight_and_gender_on_the_pharmacokinetics_pharmacodynamics_and_antihypertensive_efficacy_of_aliskiren_ L2 - https://doi.org/10.1177/0091270009359525 DB - PRIME DP - Unbound Medicine ER -