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      Comparative pharmacokinetics of a fixed-dose combination vs concomitant administration of telmisartan and S-amlodipine in healthy adult volunteers

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          This study compared the pharmacokinetic (PK) and safety profiles of a fixed-dose combination (FDC) formulation of telmisartan and S-amlodipine with those of concomitant administration of the two drugs.

          Materials and methods

          This was an open-label, randomized, crossover study in healthy male Koreans. All subjects were administered an FDC tablet containing 40 mg telmisartan and 5 mg S-amlodipine and were also coadministered the same dose of both drugs given separately. The crossover study design included a 14-day washout period between the two treatments. Blood samples were collected up to 168 h following drug administration. The plasma concentrations of telmisartan and S-amlodipine were determined by liquid chromatography tandem mass spectrometry. PK parameters and plasma concentration–time curves were compared. Safety was assessed by measuring vital signs, clinical laboratory tests, physical examinations, and patient interviews.


          The geometric mean ratios and 90% CIs for the maximum plasma concentration (C max) and area under the curve from time zero to the last sampling time (AUC t) were 0.8782 (0.8167–0.9444) and 0.9662 (0.9210–1.0136) for telmisartan and 1.0069 (0.9723–1.0427) and 1.0324 (0.9969–1.0690) for S-amlodipine, respectively. A total of 36 adverse events (AEs) were reported by 23 subjects, but no statistical differences were observed between the two treatments. The most frequently reported AE was a mild-to-moderate headache that was generally self-limiting.


          For both telmisartan and S-amlodipine, the C max and AUC t 90% CIs were between ln (0.8) and ln (1.25). These results suggest that the FDC formulation is pharmacokinetically bioequivalent and has a similar safety profile to the coadministration of these drugs.

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          Most cited references 27

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          2007 ESH-ESC Practice Guidelines for the Management of Arterial Hypertension: ESH-ESC Task Force on the Management of Arterial Hypertension

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            Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating activity.

            The metabolic syndrome is a common precursor of cardiovascular disease and type 2 diabetes that is characterized by the clustering of insulin resistance, dyslipidemia, and increased blood pressure. In humans, mutations in the peroxisome proliferator-activated receptor-gamma (PPARgamma) have been reported to cause the full-blown metabolic syndrome, and drugs that activate PPARgamma have proven to be effective agents for the prevention and treatment of insulin resistance and type 2 diabetes. Here we report that telmisartan, a structurally unique angiotensin II receptor antagonist used for the treatment of hypertension, can function as a partial agonist of PPARgamma; influence the expression of PPARgamma target genes involved in carbohydrate and lipid metabolism; and reduce glucose, insulin, and triglyceride levels in rats fed a high-fat, high-carbohydrate diet. None of the other commercially available angiotensin II receptor antagonists appeared to activate PPARgamma when tested at concentrations typically achieved in plasma with conventional oral dosing. In contrast to ordinary antihypertensive and antidiabetic agents, molecules that can simultaneously block the angiotensin II receptor and activate PPARgamma have the potential to treat both hemodynamic and biochemical features of the metabolic syndrome and could provide unique opportunities for the prevention and treatment of diabetes and cardiovascular disease in high-risk populations.
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              Hypertension among adults in the United States: National Health and Nutrition Examination Survey, 2011-2012.

              The overall prevalence of hypertension has not changed appreciably since 2009-2010. The age-adjusted prevalence of hypertension among U.S. adults was 29.1% in 2011-2012. Among adults with hypertension in 2011-2012, 82.8% were aware of their hypertension, 75.7% were currently taking medication to lower their blood pressure, and 51.9% had their blood pressure controlled to less than 140/90 mm Hg. Men and women had similar prevalence and awareness of hypertension, but more women than men were treating their hypertension and had it under control. Young adults aged 18-39 continued to have lower awareness, treatment, and control of their hypertension compared with older adults. Hypertension prevalence was still highest among non-Hispanic black adults. However, awareness, treatment, and control of hypertension were similar among non-Hispanic black, non-Hispanic white, and Hispanic adults. Non-Hispanic Asian adults had a lower prevalence of awareness than the other race and Hispanic origin groups, and lower treatment than non-Hispanic white and non-Hispanic black adults. However, hypertension control was similar among non-Hispanic Asian adults and the other race and Hispanic origin groups. Hypertension is a common and manageable chronic condition. Based on recent national data from 2011-2012, treatment of hypertension exceeded the Healthy People 2020 target goal of 69.5%. However, the control of hypertension has neither met the goal of the Healthy People 2020 (61.2% by 2020) nor the Million Hearts Initiative (65% by 2017). These results provide evidence for continued efforts to improve the management of hypertension in order to attain these goals. All material appearing in this report is in the public domain and may be reproduced or copied without permission; citation as to source, however, is appreciated.

                Author and article information

                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                Drug Design, Development and Therapy
                Dove Medical Press
                11 December 2017
                : 11
                : 3543-3550
                [1 ]Department of Pharmacology
                [2 ]PharmacoGenomics Research Center, Inje University College of Medicine, Busan
                [3 ]Department of Clinical Pharmacology, Inje University Busan Paik Hospital, Busan, Republic of Korea
                Author notes
                Correspondence: Eun-Young Kim, Department of Clinical Pharmacology, Inje University Busan Paik Hospital, 75 Bokji-ro, Busanjin-Gu, Busan 47392, Republic of Korea, Tel +82 51 890 8972, Fax +82 51 895 6438, Email eykim@ 123456inje.ac.kr

                These authors contributed equally to this work

                © 2017 Oh et al. This work is published and licensed by Dove Medical Press Limited

                The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed.

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