Angiotensin II receptor blockers: focus on cardesartan


Cite item

Full Text

Open Access Open Access
Restricted Access Access granted
Restricted Access Subscription or Fee Access

Abstract

Candesartan cilexetil - selective angiotensin II type 1 receptor blocker, which is converted to an active metabolite, candesartan, after ingestion. The article presents the pharmacokinetic and pharmacological data and the results of clinical trials, reflecting the efficiency and safety of this drug. Candesartan is an effective, Long-acting and safe drug in the treatment of arterial hypertension and chronic heart failure. The good effect of candesartan was observed in the treatment of patients with acute stroke. In case of insufficient antihypertensive effect, candesartan may be combined with other drugs (thiazide diuretics, calcium channel blockers, β-bLockers). The frequency of side effects of candesartan is not higher than that of the comparison drugs.

Full Text

Restricted Access

About the authors

Viktor Vladimirovich Cheltsov

Russian peoples' friendship university

Email: vcheltsov@mail.ru
MD, professor of the Department of general and clinical pharmacology, Medical facult

Yulia Shamilevna Gushina

Russian peoples' friendship university

Email: gushchina@mail.ru
PhD, associate professor of the Department of general and clinical pharmacology, Medical faculty

Tatiana Semenovna Illarioniva

Russian Peoples' Friendship University

Email: illarionova@med.rudn.ru
PhD, Associate Professor, Department of General and Clinical Pharmacology, Medical Faculty

Elina Arkadevna Korovyakova

Russian Peoples' Friendship University

Email: elinakor@mail.ru
PhD, Associate Professor, Department of General and Clinical Pharmacology, Medical Faculty

Anna Eduardovna Moiseeva

Russian peoples' friendship university

assistant of the Department of general and clinical pharmacology, Medical faculty

Anton Pavlovich Pereversev

Russian peoples' friendship university

PhD, associate professor of the Department of general and clinical pharmacology, Medical faculty

Yevgeniya Yurievna Stefanenko

Russian peoples' friendship university

doctor of the Department of general and clinical pharmacology, Medical faculty

Sergey Kensarinovich Ziryanov

Russian peoples' friendship university

MD, professor, Head of the Department of general and clinical pharmacology, Medical faculty

References

  1. Mancia G., De Backer G., Domoniczak A., Cifkova R., Fagard R., Germano G., Grassi G., Heagerty A.M., Kjeldsen S.E., Laurent S., Narkiewicz K., et al. 2007 Guidelines for the management of arterial hypertension: the task force for the management of arterial hypertension of European Society of Hypertension (ESH) and of the European Society of Cardiology (ESC). Eur. Heart J. 2007;28:1462-536.
  2. Dzau V.J., Sasamura H., Hein L. Heterogeneity of angiotensin synthetic pathways and receptor subtypes: physiological and pharmacological implications. J. Hypertens. 1993;11 (suppl):13-8.
  3. Miura S., Karnik S.S., Saku K. Review: Angiotensin II type 1 receptor blockers: class effects versus molecular effects. J. Renin Angiotensin Aldosterone Syst. 2011;12:1-7.
  4. Fujino M., Miura S., Kiya Y., Tominaga Y., Matsuo Y., Karnik S.S., Saku K. A small difference in the molecular structure of angiotensin II receptor blockers induces AT1 receptor-dependent and independent beneficial effects. Hypertens. Res. 2010;33:1044-1052.
  5. Kiya Y., Miura S., Matsuo Y., Karnik S.S., Keiyiro S. Ability of candesartan and other AT1 receptor blockers to impair angiotensin II-induced AT1 receptor activation after wash-out. J. Renin Angiotensin Aldosterone Syst. 2012;13(1):76-83.
  6. Dohi Y., Ohashi M., Sugiyama M., Takase H., Sato K., Ueda R. Candesartan reduces oxidative stress and inflammation in patients with essential hypertension. Hypertens. Res. 2003;26:691-7.
  7. Koh K.K., Quon M.J., Han S.H., Chung W.J., Lee Y., Shin E.K. Anti-inflammatory and metabolic effects of candesartan in hypertensive patients. Int. J. Cardiol. 2006;108:96-100.
  8. van der Ziyl N.J., Moors C.C., Goossens G.H., Hermans M.M., Blaak E.E., Diamant M. Valsartan improves beta-cell function and insulin sensitivity in subjects with impaired glucose metabolism: a randomized controlled trial. Diabetes Care. 2011;34:845-51.
  9. Miura S., Karnik S.S., Saku K. Review: angiotensin II type 1 receptor blockers: class effects versus molecular effects. J. Renin Angiotensin Aldosteron Syst. 2011;12:1-7.
  10. Smith D.H. Comparison of angiotensin II type 1 receptor antagonist in the treatment of essential hypertension. Drugs. 2008;68:1207-25.
  11. Yasuda N. et al. цит. по Cernes R., Mashavi M., Zimlichman R. Differential clinical profile of candesartan compared to other angiotensin receptor blockers. Vasc. Health Risk Manag. 2011;7:749-59.
  12. Vanderheyden P.M.L., Frierens F.L.P., Vauquelin G. Angiotensin II type 1 receptor antagonists. Why do some of them produced insurmountable inhibition? Boichem. Pharmacol. 2000;60:1557.
  13. Csajka C., Buclin T., Brunner H.R., Biollaz J. Pharmacokinetic-pharmacodynamic profile of angiotensin II receptor antagonists. Clin.Pharmacokinet. 1997;32:1-290.
  14. Geiter C.H., Morike K.E. Clinical pharmacokinetics of candesartan. Clin. Pharmacokinet. 2002;41(1):7-17.
  15. Easthope S.E., Jarvis B. Candesartan cilexetil: an update of its use in essential hypertension. Drugs. 2002;62:1253-87.
  16. van Lier J.J., van Hieningen P.N., Sunzel M. Absorption, metabolism, and excretion of 14C-candesartan and 14C-candesartan cilexetil in health volunteers. J. Hum. Hypertens. 1997;11(suppl 2):27-8.
  17. Husain A., Azim M.S., Mitra M., Bhasin P.S. A review on candesartan: pharmacological and pharmaceutical profile. J. Appl. Pharm. Sci. 2011;1:(10)12-7.
  18. Chaturvedi N., Porta M., Klein R., Orchard T., Fuller J., Parving H.H., Bilous R., Sjolie A.K.; DIRECT Programme Study Group. Effect of candesartan on prevention (DIRECT-Prevent 1) and progression (DIRECT-Protect 1) of retinopathy in type 1 diabetes: randomized, placebo-controlled trials. Lancet. 2008;372:1394-1402.
  19. Benson S.C., Pershadsingh H.A., Ho C.I., Chittiboyina A., Desai P., Pravenec M., Qi N., Wang J., Avery M.A., Kurtz T.W. Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating activity. Hypertension. 2004;43:993-1002.
  20. Yan W.H., Pan C.Y., Dou J.T., Meng J.H., Wang B.A., Mu Y.M. Candesartan cilexetil prevent diet-induced insulin resistance via peroxisome proliferator-activated receptor-Y activation in an obese rat model. Exp. Ther. Med. 2016;12(1):272-8.
  21. Chobanian A.V., Bakris G.L., Black H.R., Cushman W.C., Green L.A., Izzo J.L. Jr, Jones D.W., Materson B.J., Oparil S., Wright J.T. Jr, Roccella E.J.; Joint National Committee on prevention, detection, evaluation and treatment of high blood pressure. national heart, lung and blood institute; national high blood pressure education program coordinating committee. Seven reports of the Join National Committee on prevention, detection, evaluation and treatment of high blood pressure. Hypertension. 2003;42:1206-1252.
  22. Lloyd-Jones D., Adams R., Carnethon M., De Simone G., Ferguson T.B., Flegal K., Ford E., Furie K., Go A., Greenlund K., Haase N., et al; American Heart Association statistics committee and stroke statistics subcommittee. Heart disease and stroke statistics - 2009 update: a report from the American Heart Association statistics subcommittee. Circulation. 2009;119(3):480-6.
  23. ESH Guidelines Committee. 2003 European Society of Hypertension - European Society of Cardiology guidelines for the management of arterial hypertension. J. Hypertens. 2003;21:1011-53.
  24. Hansson L. The relationship between dose and antihypertensive effect for different AT1-receptor blockers. Blood Press. 2001;10(suppl 3):33-9.
  25. Vasan R.S., Beiser A., Seshadri S., Larson M.G., Kannel W.B., D'Agostino R.B., Levy D. Residual life time risk for developing hypertension in middle-aged women and men: the Framingham Heart Study. JAMA. 2002;287:1003-10.
  26. New Zeland emedicines and medical devices safety authority date sheet- www.medsafe.govt.nz/profs/datesheet/a/ Atacandtab.htm.
  27. Thijs L., Hond E.D., Nawrot T., et al. Prevalence, pathophysiology and treatment of isolated systolic hypertension in the elderly. Expert Rev. Cardiovasc. Ther. 2004;2:761-9.
  28. Asmar R., Nisse-Durgeat S. A large scale study of angiotensin II inhibition therapy in elderly population: the CHANCE study. Vasc. Health Risk Manag. 2006;2(3):317-23.
  29. Bonner G., Landers B., Bramlage P. Candesartan cilexetil/hydrochlorothiazide combination treatment versus high-dose candesartan cilexetil monotherapy in patients with mild to moderate cardiovascular risk (CHILI Triple T). Vasc. Health Risk Manag. 2011;7:85-95.
  30. Shargorodsky M., Haas E., Boas M., Gavish D., Zimlichman R. High dose treatment with angiotensin II recepror blocker in patients with hypertension: differential effect of tissue protection versus blood pressure lowering. Atherosclerosis. 2008;197:303-10.
  31. Lacourciere Y., Asmar R. A comparison of the efficacy and durati on of action of candesartan cilexetil and losartan as assessed by clinic and ambulatory blood pressure after a missed dose, in truly hypertensive patients: a placebocontrolled, forced titration study. Candesartan/losartan study investigators. Am. J. Hypertens. 1999;12:1181-7.
  32. Papadopolous D., Makris T., Papademtriou V. Is it time to treat prehypertension? Hypertens. Res. 2008;31(9):1681-6.
  33. Cui J., Hopper J.L., Harrap S.B. Genes and family environment explain correlations between blood pressure and body mass index. Hypertension. 2002;40:7-12.
  34. Julius S., Nesbitt S.D., Egan B.M., Kaciroti N., Schork A., Grozinski M., Michelson E. for the TROPHY study group. Trial of preventing hypertension. Design and 2-year progress report. Hypertension. 2004;44:146-51.
  35. Skov K., Eiskjaer H., Hansen H.E., Madsen J.K., Kvist S., Mulvany M.J. Treatment of young subjects at high familial risk of future hypertension with an angiotensin-receptor blocker. Hypertension. 2007;50:89-95.
  36. Okpechi I.G. Rayner B.L. Update on the role of candesartan in the optimal management of hypertension and cardiovascular risk reduction. Integr. Blood Press. Control. 2000;3:45-55.
  37. Effects of enalapril on mortality in severe congestive heart failure. Results of the cooperative north Scandinavian enalapril study [CONSENSUS]. The CONSENSUS Trial Study Group. N. Engl. J. Med. 1987;316:1429-35.
  38. Effect of metoprolol CR/XL in chronic heart failure: metoprolol CR/XL randomized intervention trial in congestive heart failure (MERIT-HF). Lancet. 1999;353:2001-7.
  39. Packer M., Coats A.J., Fowler M.B., Katus H.A., Krum H., Mohacsi P., Rouleau J.L., Tendera M., Castaigne A., Roecker E.B., Schultz M.K., DeMets D.L.; Carvedilol prospective randomized cumulative survival study group. Effect of carvedilol on survival in severe chronic heart failure. N. Engl. J. Med. 2001;22:1651-8.
  40. Pitt B., Zannad F., Remme W.J., Cody R., Castaigne A., Perez A., Palensky J., Wittes J. The effect of spironolactone on morbidity and mortality in patients with severe heart failure. Randomized aldactone evaluation study investigators. N. Engl. J. Med. 1999;341:709-17.
  41. Cohn J.N., Levine T.B., Francis G.S., Goldsmith S. Neurohumoral control mechanisms in congestive heart failure. Am. Heart J. 1981;102:509-14.
  42. McMurray J.J. Heart failure in 10 year time: focus on pharmacological treatment. Heart. 2002;88 (suppl 2):40-6.
  43. McKelvie R.S., Yusuf S., Pericak D., Avezum A., Burns R.J., Probstfield J., Tsuyuki R.T., White M., Rouleau J., Latini R., Maggioni A., Young J., Pogue J. Comparison of candesartan, enalapril, and their combination in congestive heart failure: Randomized Evaluation of Strategies for Left Ventricular Dysfunction (RESOLVD) pilot study. RESOLVD pilot study investigators. Circulation. 1999;100:1056-64.
  44. McMurray J.J., Ostergren J., Swedberg K., Granger C.B., Held P., Michelson E.L., Olofsson B., Yusuf S., Pfeffer M.A.; CHARM Investigators and Committees. Effects of candesartan in patients with chronic heart failure and reduced left-ventricular systolic function taking angiotensin-converting-enzyme inhibitors: the CHARM-Added trial. Lancet. 2003;362:767-71.
  45. Granger C.B., McMurray J.J., Yusuf S., Held P., Michelson E.L., Olofsson B., Ostergren J., Pfeffer M.A., Swedberg K.; CHARM Investigators and Committees. Effects of candesartan in patients with chronic heart failure and reduced left-ventricular systolic function intolerant to angiotensin-converting enzyme inhibitors: the CHARM-Alternative trial. Lancet. 2003;362:772-6.
  46. Yusuf S., Pfeffer M.A., Swedberg K., Granger C.B., Held P., McMurray J.J., Michelson E.L., Olofsson B., Ostergren J.; CHARM Investigators and Committees. Effects of candesartan in patients with chronic heart failure and preserved left-ventricular ejection fraction: the CHARM-Preserved trial. Lancet. 2003;362:777-81.
  47. Truelsen T., Piechowski-Jozwiak B, Bonita R., Mathers C., Bogousslavsky J., Boysen G. Stroke incidence and prevalence in Europe: a review of available date. Eur. J. Neurol. 2006;13:581-98.
  48. Lawes C.M., Vander Hoorn S., Rodgers A. International Society of Hypertension. Global burden of blood-pressure-related disease. Lancet. 2008;371:1513-8.
  49. Graham D.I., McGeorge A., Fitch W., Jones J.V., MacKenzie E.T. Ischemic brain damage induced by rapid lowering of arterial pressure in hypertension. J. Hypertens. 1984;2:297-304.
  50. Wahlgren N.G., McMahon D.G., DeKeyser J. et al. Intravenous Nimodipine West European Stroke Trial (INVEST) of nimodipine in the treatment of acute ischemic stroke. Cerebrovasc. Dis. 1994;4:204-10.
  51. Fujii K., Weno B.L., Baumbach G.L., Heistad D.D. Effect of antihypertensive treatment on focal cerebral infarction. Hypertension. 1992;19:713-6.
  52. Lisk D.R., Grotta J.C., Lamki L.M., Tran H.D., Taylor J.W., Molony D.A., Barron B.J. Should hypertension be treated after acute stroke? A randomized controlled trial using single photon emission computed tomography. Arch. Neurol. 1993;50:855-62.
  53. Guppo Italiano per lo studio della Soppravvivenza nell'infarto Miocardico. GISSI-3: effects of lisinopril and transdermal nitrate singly and together on 6-week mortality and ventricular function after acute myocardial infarction. Lancet. 1994;343:1115-22.
  54. The Task Force on the management of acute myocardial infarction: prehospital and in-hospital management. Eur. Heart J. 1996;17:43-63.
  55. Pedelty L., Gorelick P.B. Management of hypertension and cerebrovascular disease in the elderly. Am. J. Med. 2008;121 (8 suppl):23-31.
  56. Schrader J., Luders S., Kulschewski A., Berger J., Zidek W., Treib J., Einhäupl K., Diener H.C., Dominiak P.; Acute Candesartan Cilexetil Therapy in Stroke Survivors Study Group. The ACCESS Study. Evaluation of acute candesartan cilexetil therapy in stroke survivors. Stroke. 2003;34:1699-1703.
  57. Lithell H., Hansson L., Skoog I., Elmfeldt D., Hofman A., Olofsson B., Trenkwalder P., Zanchetti A.; SCOPE Study Group. The Study on Cognition and Prognosis in the Elderly (SCOPE): principal results of randomized double-blind interventional trial. J. Hypertens. 2003;21:875-86.
  58. Sandset E.C., Bath P.M., Boysen G., Jatuzis D., Körv J., Lüders S., Murray G.D., Richter P.S., Roine R.O., Terént A., Thijs V., Berge E; SCAST Study Group. The angiotensin-receptor blocker candesartan for treatment of acute stroke (SCAST): a randomized placebo-controlled double-blind trial. Lancet. 2011;377:741-50.
  59. Cernes R., Mashavi M., Zimlichman R. Differential clinical profile of candesartan compared to other angiotensin recepror blockers. Vasc. Health Risk Manag. 2011;7:749-59.
  60. Trachtman H., Hainer J.W., Sugg J., Teng R., Sorof J.M., Radcliffe J. Candesartan in Children with Hypertension (CINCH) Investigators. Efficacy, safety, and pharmacokinetics of candesartan cilexetil in hypertensive children aged 6 to 17 years. J. Clin. Hypertens. (Greenwich). 2008;10:743-50.
  61. ARB Trialists Collaboration. Effects of telmisartan, irbesartan, valsartan, candesartan and losartan on cancers in 15 trials enrolling 138769 individuals. J. Hypertens. 2011;29:623-35.

Supplementary files

Supplementary Files
Action
1. JATS XML

Copyright (c) 2016 Bionika Media

This website uses cookies

You consent to our cookies if you continue to use our website.

About Cookies