Aliskiren penetrates adipose and skeletal muscle tissue, and reduces Renin-Angiotensin System activity in obese hypertensive patients

Détails

ID Serval
serval:BIB_3DD0497B9CBF
Type
Actes de conférence (partie): contribution originale à la littérature scientifique, publiée à l'occasion de conférences scientifiques, dans un ouvrage de compte-rendu (proceedings), ou dans l'édition spéciale d'un journal reconnu (conference proceedings).
Sous-type
Abstract (résumé de présentation): article court qui reprend les éléments essentiels présentés à l'occasion d'une conférence scientifique dans un poster ou lors d'une intervention orale.
Collection
Publications
Institution
Titre
Aliskiren penetrates adipose and skeletal muscle tissue, and reduces Renin-Angiotensin System activity in obese hypertensive patients
Titre de la conférence
77th Annual Meeting on German-Society-for-Experimental-and-Clinical-Pharmacology-and-Toxicology
Auteur⸱e⸱s
Engeli S., Boschmann M., Nussberger J., Danser A. H. J., Yeh C. -M., Prescott M. F., Dahlke M., Jordan J.
Adresse
Frankfurt, Germany, March 30-April 01, 2011
ISBN
0028-1298
Statut éditorial
Publié
Date de publication
2011
Peer-reviewed
Oui
Volume
383
Série
Naunyn-Schmiedebergs Archives of Pharmacology
Pages
7-8
Langue
anglais
Notes
Publication type : Meeting Abstract
Résumé
Introduction: Tissue Renin-Angiotensin System activity is increased in obesity and may contribute to obesity-related hypertension and metabolic abnormalities. This open-label pilot study investigated the local effects of Aliskiren in adipose tissue and skeletal muscle.Methods: After a 1-2 week washout, 10 patients with hypertension and abdominal obesity received placebo for 2 weeks, then Aliskiren 300 mg once daily for 4 weeks, followed by a 4-week washout period and then another 4 weeks treatment period with Amlodipine 5 mg once daily. Drug concentrations and Renin-Angiotensin Systembiomarkers were measured in interstitial fluid employing the microdialysis zero-flow method, and in biopsies from abdominal subcutaneous adipose and skeletal muscle.Results: After 4 weeks treatment, microdialysate concentrations (mean±SD) of Aliskiren were 2.4±2.1 ng/ml in adipose tissue, and 7.1±4.2 ng/ml in skeletal muscle. These concentrations were similar to the mean plasma concentration of 8.4±4.4 ng/ml. Tissue concentrations (ng/g) of Aliskiren were 29.0±16.7 ng/g in adipose tissue, and 107.3±68.6 ng/g in skeletal muscle after 4 weeks treatment. Angiotensin II concentrations in microdialysates were below the lower limit of quantification in most patients, but pooled data from two patients suggested that Angiotensin II was reduced by Aliskiren and unchanged by Amlodipine. Aliskiren 300 mg significantly reduced mean plasma Renin activity by 68% and Angiotensin II by 61% (p<0.05 vs. baseline). Amlodipine 5 mg increased plasma Renin activity by 48% (p<0.05 vs. baseline), and non-significantly increased Angiotensin II by 60%. Both treatments increased plasma Renin concentration.Conclusion: Aliskiren 300 mg once daily penetrates adipose and skeletal muscle tissue at concentrations sufficient to reduce tissue Renin-Angiotensin System activity in obese patients with hypertension.
Web of science
Création de la notice
13/04/2011 10:24
Dernière modification de la notice
20/08/2019 13:34
Données d'usage