The Korean journal of internal medicine

  • 제32권6호
  • /
  • Pages.1025-1036
  • /
  • 2017
  • /
  • 1226-3303(pISSN)
  • /
  • 2005-6648(eISSN)
대한내과학회 (The Korean Association of Internal Medicine)
권호 표지
DOI QR코드

DOI QR Code

24-Hour blood pressure response to lower dose (30 mg) fimasartan in Korean patients with mild to moderate essential hypertension

  • Lee, Hae-Young (Department of Internal Medicine, Seoul National University Hospital) ;
  • Kim, Cheol-Ho (Seoul National University Bundang Hospital) ;
  • Song, Jae-Kwan (Asan Medical Center, University of Ulsan College of Medicine) ;
  • Chae, Shung Chull (Kyungpook National University Hospital) ;
  • Jeong, Myung Ho (The Heart Center of Chonnam National University Hospital) ;
  • Kim, Dong-Soo (Inje University Busan Paik Hospital) ;
  • Oh, Byung-Hee (Department of Internal Medicine, Seoul National University Hospital)
  • 투고 : 2016.03.20
  • 심사 : 2016.08.23
  • 발행 : 2017.11.01
⟨ 이전 논문 다음 논문 ⟩

초록

Background/Aims: Fimasartan is an angiotensin type 1 receptor blocker (ARB) which has comparable efficacy and tolerability with other ARBs. The aim of this study was to evaluate 24-hour blood pressure (BP) lowering efficacy and the tolerability of the low dose fimasartan compared with valsartan in patients with mild to moderate hypertension. Methods: This study was a phase II, prospective, multicenter, randomized, double-blind, parallel-grouped trial. A total of 75 hypertensive patients, whose mean ambulatory BP monitoring values were ${\geq}135/85mmHg$, were randomized to either fimasartan 30 mg or valsartan 80 mg daily. The primary efficacy endpoint was the change in the mean 24-hour systolic BP (SBP) values from the baseline and at the week 8. Secondary endpoints included the change in the mean 24-hour diastolic BP values, the daytime and the nighttime mean BP values at week 8, the trough-to-peak (T/P) ratio and the smoothness index. Results: At week 8, the mean 24-hour SBP values significantly decreased in both groups; $-10.5{\pm}11.9mmHg$ (p < 0.0001) in the fimasartan group and $-5.5{\pm}11.6mmHg$ (p = 0.0307) in the valsartan group. The difference between two groups was $4.3{\pm}2.9mmHg$ but there was no statistical significance (p = 0.1392). The global T/P ratio in the fimasartan 30 mg groups were 0.48 and 0.40 in the valsartan 80 mg group, respectively (p = 0.3411). The most frequent adverse events (AEs) were acute pharyngitis and there were no cases of severe AEs. Conclusions: In mild-to-moderate hypertensive patients, low dose (30 mg) fimasartan showed comparable 24-hour BP lowering efficacy compared with valsartan (80 mg). There was no difference in tolerability between two groups.

키워드

참고문헌

  1. Ezzati M, Vander Hoorn S, Lawes CM, et al. Rethinking the “diseases of affluence” paradigm: global patterns of nutritional risks in relation to economic development. PLoS Med 2005;2:e133. https://doi.org/10.1371/journal.pmed.0020133
  2. Neal B, MacMahon S, Chapman N; Blood Pressure Lowering Treatment Trialists' Collaboration. Effects of ACE inhibitors, calcium antagonists, and other blood-pressure-lowering drugs: results of prospectively designed overviews of randomised trials. Blood Pressure Lowering Treatment Trialists' Collaboration. Lancet 2000;356:1955-1964. https://doi.org/10.1016/S0140-6736(00)03307-9
  3. Lee HY, Chung WJ, Jeon HK, et al. Impact of the ${\beta}$-1 adrenergic receptor polymorphism on tolerability and efficacy of bisoprolol therapy in Korean heart failure patients: association between ${\beta}$ adrenergic receptor polymorphism and bisoprolol therapy in heart failure (ABBA) study. Korean J Intern Med 2016;31:277-287. https://doi.org/10.3904/kjim.2015.043
  4. James PA, Oparil S, Carter BL, et al. 2014 Evidence-based guideline for the management of high blood pressure in adults: report from the panel members appointed to the Eighth Joint National Committee (JNC 8). JAMA 2014;311:507-520. https://doi.org/10.1001/jama.2013.284427
  5. Weber MA, Schiffrin EL, White WB, et al. Clinical practice guidelines for the management of hypertension in the community: a statement by the American Society of Hypertension and the International Society of Hypertension. J Clin Hypertens (Greenwich) 2014;16:14-26. https://doi.org/10.1111/jch.12237
  6. Mancia G, Fagard R, Narkiewicz K, et al. 2013 ESH/ESC guidelines for the management of arterial hypertension: the Task Force for the management of arterial hypertension of the European Society of Hypertension (ESH) and of the European Society of Cardiology (ESC). J Hypertens 2013;31:1281-1357. https://doi.org/10.1097/01.hjh.0000431740.32696.cc
  7. Lee JH, Bae MH, Yang DH, et al. Angiotensin II type 1 receptor blockers as a first choice in patients with acute myocardial infarction. Korean J Intern Med 2016;31:267-276. https://doi.org/10.3904/kjim.2014.268
  8. Choi EK. Angiotensin receptor blocker for stroke prevention in atrial fibrillation: beyond blood pressure lowering? Korean Circ J 2016;46:307-308. https://doi.org/10.4070/kcj.2016.46.3.307
  9. Abraham HM, White CM, White WB. The comparative efficacy and safety of the angiotensin receptor blockers in the management of hypertension and other cardiovascular diseases. Drug Saf 2015;38:33-54. https://doi.org/10.1007/s40264-014-0239-7
  10. Lee HY, Oh BH. Fimasartan: a new angiotensin receptor blocker. Drugs 2016;76:1015-1022. https://doi.org/10.1007/s40265-016-0592-1
  11. Lee H, Kim KS, Chae SC, Jeong MH, Kim DS, Oh BH. Ambulatory blood pressure response to once-daily fimasartan: an 8-week, multicenter, randomized, double-blind, active-comparator, parallel-group study in Korean patients with mild to moderate essential hypertension. Clin Ther 2013;35:1337-1349. https://doi.org/10.1016/j.clinthera.2013.06.021
  12. Lee H, Yang HM, Lee HY, et al. Efficacy and tolerability of once-daily oral fimasartan 20 to 240 mg/d in Korean patients with hypertension: findings from two phase II, randomized, double-blind, placebo-controlled studies. Clin Ther 2012;34:1273-1289. https://doi.org/10.1016/j.clinthera.2012.04.021
  13. Lee SE, Kim YJ, Lee HY, et al. Efficacy and tolerability of fimasartan, a new angiotensin receptor blocker, compared with losartan (50/100 mg): a 12-week, phase III, multicenter, prospective, randomized, double-blind, parallel-group, dose escalation clinical trial with an optional 12-week extension phase in adult Korean patients with mild-to-moderate hypertension. Clin Ther 2012;34:552-568. https://doi.org/10.1016/j.clinthera.2012.01.024
  14. Rhee MY, Baek SH, Kim W, et al. Efficacy of fimasartan/hydrochlorothiazide combination in hypertensive patients inadequately controlled by fimasartan monotherapy. Drug Des Devel Ther 2015;9:2847-2854.
  15. Park JB, Sung KC, Kang SM, Cho EJ. Safety and efficacy of fimasartan in patients with arterial hypertension (Safe-KanArb study): an open-label observational study. Am J Cardiovasc Drugs 2013;13:47-56. https://doi.org/10.1007/s40256-013-0004-9
  16. Chang SA, Lim BK, Lee YJ, Hong MK, Choi JO, Jeon ES. A novel angiotensin type I receptor antagonist, fimasartan, prevents doxorubicin-induced cardiotoxicity in rats. J Korean Med Sci 2015;30:559-568.
  17. Kim JW, Yi S, Kim TE, et al. Increased systemic exposure of fimasartan, an angiotensin II receptor antagonist, by ketoconazole and rifampicin. J Clin Pharmacol 2013;53:75-81. https://doi.org/10.1177/0091270011433328
  18. Lee J, Han S, Jeon S, Hong T, Yim DS. Pharmacokineticpharmacodynamic model of fimasartan applied to predict the influence of a high fat diet on its blood pressurelowering effect in healthy subjects. Eur J Clin Pharmacol 2013;69:11-20.
  19. Chi YH, Lee H, Paik SH, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamics of fimasartan following single and repeated oral administration in the fasted and fed states in healthy subjects. Am J Cardiovasc Drugs 2011;11:335-346. https://doi.org/10.2165/11593840-000000000-00000
  20. Shin KH, Kim TE, Kim SE, et al. The effect of the newly developed angiotensin receptor II antagonist fimasartan on the pharmacokinetics of atorvastatin in relation to OATP1B1 in healthy male volunteers. J Cardiovasc Pharmacol 2011;58:492-499. https://doi.org/10.1097/FJC.0b013e31822b9092
  21. Kim CO, Lee HW, Oh ES, et al. Influence of hepatic dysfunction on the pharmacokinetics and safety of fimasartan. J Cardiovasc Pharmacol 2013;62:524-529. https://doi.org/10.1097/FJC.0000000000000010
  22. Lee HW, Lim MS, Seong SJ, et al. Effect of age on the pharmacokinetics of fimasartan (BR-A-657). Expert Opin Drug Metab Toxicol 2011;7:1337-1344. https://doi.org/10.1517/17425255.2011.618835
  23. Yi S, Kim TE, Yoon SH, et al. Pharmacokinetic interaction of fimasartan, a new angiotensin II receptor antagonist, with amlodipine in healthy volunteers. J Cardiovasc Pharmacol 2011;57:682-689. https://doi.org/10.1097/FJC.0b013e31821795d0
  24. Jeon H, Lim KS, Shin KH, et al. Assessment of the drugdrug interactions between fimasartan and hydrochlorothiazide in healthy volunteers. J Cardiovasc Pharmacol 2012;59:84-91. https://doi.org/10.1097/FJC.0b013e318237389e
  25. Yi S, Kim JW, Kim TE, et al. Effect of multiple doses of fimasartan, an angiotensin II receptor antagonist, on the steady-state pharmacokinetics of digoxin in healthy volunteers. Int J Clin Pharmacol Ther 2011;49:321-327. https://doi.org/10.5414/CP201533
  26. Youn JC, Ihm SH, Bae JH, et al. Efficacy and safety of 30-mg fimasartan for the treatment of patients with mild to moderate hypertension: an 8-week, multicenter, randomized, double-blind, phase III clinical study. Clin Ther 2014;36:1412-1421. https://doi.org/10.1016/j.clinthera.2014.07.004
  27. Diamant M, Vincent HH. Lisinopril versus enalapril: evaluation of trough:peak ratio by ambulatory blood pressure monitoring. J Hum Hypertens 1999;13:405-412. https://doi.org/10.1038/sj.jhh.1000821
  28. Staessen JA, Thijs L, Bijttebier G, et al. Determining the trough-to-peak ratio in parallel-group trials: Systolic Hypertension in Europe (SYST-EUR) Trial Investigators. Hypertension 1997;29:659-667. https://doi.org/10.1161/01.HYP.29.2.659
  29. Staessen JA, Bieniaszewski L, Buntinx F, et al. The troughto- peak ratio as an instrument to evaluate antihypertensive drugs: the APTH Investigators. Ambulatory Blood Pressure and Treatment of Hypertension Trial. Hypertension 1995;26:942-949. https://doi.org/10.1161/01.HYP.26.6.942
  30. Coca A, Sobrino J, Soler J, et al. Trough-to-peak ratio, smoothness index, and circadian blood pressure profile after treatment with once-daily fixed combination of losartan 100 and hydrochlorothiazide 25 in essential hypertension. J Cardiovasc Pharmacol 2002;39:824-833. https://doi.org/10.1097/00005344-200206000-00007
  31. Parati G, Omboni S, Rizzoni D, Agabiti-Rosei E, Mancia G. The smoothness index: a new, reproducible and clinically relevant measure of the homogeneity of the blood pressure reduction with treatment for hypertension. J Hypertens 1998;16:1685-1691. https://doi.org/10.1097/00004872-199816110-00016
  32. Heran BS, Wong MM, Heran IK, Wright JM. Blood pressure lowering efficacy of angiotensin receptor blockers for primary hypertension. Cochrane Database Syst Rev 2008;(4):CD003822.
  33. Forclaz A, Maillard M, Nussberger J, Brunner HR, Burnier M. Angiotensin II receptor blockade: is there truly a benefit of adding an ACE inhibitor? Hypertension 2003;41:31-36. https://doi.org/10.1161/01.HYP.0000047512.58862.A9
  34. Jo YI, Na HY, Moon JY, et al. Effect of low-dose valsartan on proteinuria in normotensive immunoglobulin A nephropathy with minimal proteinuria: a randomized trial. Korean J Intern Med 2016;31:335-343. https://doi.org/10.3904/kjim.2014.266
  35. Israili ZH. Clinical pharmacokinetics of angiotensin II (AT1) receptor blockers in hypertension. J Hum Hypertens 2000;14 Suppl 1:S73-S86. https://doi.org/10.1038/sj.jhh.1000991
  36. Taylor AA, Siragy H, Nesbitt S. Angiotensin receptor blockers: pharmacology, efficacy, and safety. J Clin Hypertens (Greenwich) 2011;13:677-686. https://doi.org/10.1111/j.1751-7176.2011.00518.x
  37. Morgan T, Griffiths C, Delbridge L. Interaction of ACE inhibitors and AT(1)-receptor blockers on maximum blood pressure response in spontaneous hypertensive rats. J Renin Angiotensin Aldosterone Syst 2002;3:16-18. https://doi.org/10.3317/jraas.2002.002
  38. Rose M, McMahon FG. Some problems with antihypertensive drug studies in the context of the new guidelines. Am J Hypertens 1990;3:151-155. https://doi.org/10.1093/ajh/3.2.151
  39. Food and Drug Administration, International Conference on Harmonization (ICH). Draft guidance: E12A principles for clinical evaluation of new antihypertensive drugs [Internet]. Silver Spring (MD): FDA, 2000 [cited 2017 Sep 1]. Available from: http://www.fda.gov/downloads/RegulatoryInformation/Guidances/ucm073147.pdf.

피인용 문헌

  1. PK/PD evaluation of fimasartan for the treatment of hypertension Current evidences and future perspectives vol.14, pp.5, 2018, https://doi.org/10.1080/17425255.2018.1468435
  2. Fimasartan: A new armament to fight hypertension vol.8, pp.7, 2017, https://doi.org/10.4103/jfmpc.jfmpc_300_19
  3. Long-Term Safety of a Novel Angiotensin Receptor Blocker, Fimasartan, According to the Absence or Presence of Underlying Liver Disease in Korean Hypertensive Patients: A Prospective, 12-Month, Observa vol.14, pp.None, 2020, https://doi.org/10.2147/dddt.s233174