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Current Drug Safety

Editor-in-Chief

ISSN (Print): 1574-8863
ISSN (Online): 2212-3911

Pharmacology, Efficacy and Safety of Felodipine with a Focus on Hypertension and Angina Pectoris

Author(s): Kinjal Navadiya and Sanjay Tiwari

Volume 10, Issue 3, 2015

Page: [194 - 201] Pages: 8

DOI: 10.2174/1574886310666150514114619

Price: $65

Abstract

Calcium channel blockers (CCBs) are a heterogeneous group of drugs often used in the therapy for hypertension and angina. Though CCBs are generally similar in terms of their efficacy yet, they differ in their ability of causing selective inhibition in the contractility of vascular smooth muscle in comparison to cardiac muscle. Felodipine is one of the most vascular selective of the available CCBs and it has no negative inotropic effects at clinically administered doses. Focus of this review is to comprehensively summarize the pharmacokinetics, efficacy, safety and tolerability of felodipine.

This review is based on evaluation of relevant literature on felodipine using meta-database PubMed and ScienceDirect and internet search engine (Google Scholar). Clinical studies summarized in this review testify, on technical lines, the clinical efficacy, safety and placebo- like tolerability profile of felodipine, administered alone as well as in combination.

Keywords: Angina pectoris, calcium channel blocker, felodipine, hypertension, tolerability.

[1]
Mitchell JA, Ventura HO, Mehra MR. Early recognition and treatment of hypertensive heart disease. Curr Opin Cardiol 2005; 20: 282-9.
[2]
Waeber B, Detry J-M, Dahlöf B, et al. Felodipine–metoprolol combination tablet: A valuable option to initiate antihypertensive therapy? Am J Hypertens 1999; 12: 915-20.
[3]
Kearney PM, Whelton M, Reynolds K, et al. Global burden of hypertension: Analysis of worldwide data. Lancet 2005; 365: 217-23.
[4]
Landmesser U, Drexler H. Endothelial function and hypertension. Curr Opin Card 2007; 22: 316-20.
[5]
Cordero A, Bertomeu-Martínez V, Mazón P, et al. Factors associated with uncontrolled hypertension in patients with and without cardiovascular disease. Rev ESP Cardiol 2011; 64: 587-93.
[6]
Fogari R, Zoppi A, Lusardi P, et al. Effects of benazepril alone and in combination with hydrochlorothiazide in comparison with felodipine extended release in elderly patients with mild-to-moderate essential hypertension. Curr Ther Res 1998; 59: 246-56.
[7]
Achilli F, Buono G, Di Fraia S, et al. Acute and chronic effects of felodipine extended release and amlodipine in patients with exertional angina: A double-masked, clinical comparison. Curr Ther Res 1996; 57: 523-36.
[8]
Wright JM, Musini VM. First-line drugs for hypertension. Cochrane Database Syst Rev 2009; 8CD001841
[9]
Pestana M. Hypertension in the elderly. Int Urol Nephrol 2001; 33: 563-9.
[10]
Emanuelsson H, Egstrup K, Nikus K, et al. Antianginal efficacy of the combination of felodipine-metoprolol 10/100 mg compared with each drug alone in patients with stable effort-induced angina pectoris: A multicenter parallel group study. Am Heart J 1999; 137: 854-62.
[11]
Chen J, Ren Y, Tang Y, et al. Acupuncture therapy for angina pectoris: A systematic review. J Trad Chin Med 2012; 32: 494-01.
[12]
Deckers JW. Classification of myocardial infarction and unstable angina: A re- assessment. Int J Cardiol 2013; 167: 2387-90.
[13]
Heart and Stroke Facts 1996. Statistical Supplement Dallas TX: American Heart Association.
[14]
Schoen M, Tanzi MG. Role of calcium channel blockers in treatment of hypertension. Today 2008; 14: 50-65.
[15]
Ljung B. Vascular selectivity of felodipine. Drugs 1985; 29: 46-58.
[16]
Freher M, Challapalli S, Pinto JV, et al. Current status of calcium channel blockers in patients with cardiovascular disease. Curr Prob Cardiol 1999; 24: 230-40.
[17]
Gradman AH. The evolving role of calcium channel blockers in the treatment of angina pectoris: Focus on felodipine. Can J Cardiol 1995; 11: 14B-21B.
[18]
Hedner T, Elmfeldt D, Schenck H, et al. Glucose tolerance in hypertensive patients during treatment with the calcium antagonist, felodipine. Br J Clin Pharmacol 1987; 24: 145-9.
[19]
Mann S. Dihydropyridines, felodipine, and pharmac. N Z Med J 2005; 118: U1569.
[20]
Little WC, Cheng C-P, Elvelin L, et al. Vascular selective calcium entry blockers in the treatment of cardiovascular disorders: Focus on felodipine. Cardiovasc Drugs Ther 1995; 9: 657-63.
[21]
Edgar B, Regardh C, Attman P, et al. Pharmacokinetics of felodipine in patients with impaired renal function. Br J Clin Pharmacol 1989; 27: 67-74.
[22]
Wade JR, Sambol NC. Felodipine population dose-response and concentration-response relationships in patients with essential hypertension. Clin Pharmacol Ther 1995; 57: 569-81.
[23]
Blychert E, Edgar B, Elmfeldt D, et al. Plasma concentration-effect relationships for felodipine: A meta-analysis. Br J Clin Pharmacol 1991; 31: 15-24.
[24]
Edgar B, Lundborg P, Regårdh C. Clinical pharmacokinetics of felodipine. Drugs 1987; 34: 16-27.
[25]
Blychert E, Edgar B, Elmfeldt D, et al. A population study of the pharmacokinetics of felodipine. Br J Clin Pharmacol 1991; 31: 15-24.
[26]
Li Y, Yin Y, Sun Z, et al. Sensitive and rapid quantification of felodipine by high- performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) and its pharmacokinetics in healthy chinese volunteers. Chem Res Chinese Univ 2006; 22: 479-83.
[27]
Hulthén UL, Katzman PL. Renal effects of acute and long-term treatment with felodipine in essential hypertension. J Hypertens 1988; 6: 2231-7.
[28]
Regårdh C, Edgar B, Olsson R, et al. Pharmacokinetics of felodipine in patients with liver disease. Eur J Clin Pharmacol 1989; 36: 473-9.
[29]
Lundahl J, Regårdh C, Edgar B, et al. Effects of grapefruit juice ingestion– pharmacokinetics and haemodynamics of intravenously and orally administered felodipine in healthy men. Eur J Clin Pharmacol 1997; 52: 139-45.
[30]
Bailey D, Arnold J, Bend J, et al. Grapefruit juice-felodipine interaction: Reproducibility and characterization with the extended release drug formulation. Br J Clin Pharmacol 1995; 40: 135-40.
[31]
Takanaga H, Ohnishi A, Matsuo H, et al. Pharmacokinetic analysis of felodipine– grapefruit juice interaction based on an irreversible enzyme inhibition model. Br J Clin Pharmacol 2000; 49: 49-58.
[32]
Wiklund I, Dimenäs E, Partridge S. Effects of felodipine extended release on quality of life—an analysis of four clinical trials. Curr Ther Res 1995; 56: 81-94.
[33]
Andersson O, Bengtsson C, Elmfeldt D, et al. Short‐term effects of felodipine, a new dihydropyridine, in hypertension. Br J Clin Pharmacol 1984; 17: 257-63.
[34]
Bossini A, Veroli C, Cavallotti G, et al. Felodipine ER formulation in the treatment of mild hypertension: Efficacy and tolerability vs placebo. Br J Clin Pharmacol 1990; 30: 567-71.
[35]
Bainbridge A, Macfadyen R, Stark S, et al. The antihypertensive efficacy and tolerability of a low dose combination of ramipril and felodipine ER in mild to moderate essential hypertension. Br J Clin Pharmacol 1993; 36: 323-30.
[36]
Lassen E, Frimodt-Møller J, Ahlstrøm F, et al. Antihypertensive efficacy and safety of felodipine compared with nitrendipine in mild to moderate hypertension. Curr Ther Res 1993; 53: 654-64.
[37]
Elliott WJ, Montoro R, Smith D, et al. Comparison of two strategies for intensifying antihypertensive treatment. Am J Hypertens 1999; 12: 691-6.
[38]
Lin M, Arnold Chan K, Wang C, et al. Effects of low-dose treatment with felodipine versus fosinopril in Chinese patients with non-ischemic heart failure and normal blood pressure: a double-blind, randomized, crossover study. Curr Ther Res 2004; 65: 204-21.
[39]
Gavras HP. Issues in hypertension: Drug tolerability and special populations. Am J Hypertens 2001; 14: 231S-6S.
[40]
van der Krogt JP, Brand R, Dawson EC. Amlodipine versus extended-release felodipine in general practice: A randomized, parallel-group study in patients with mild-to-moderate hypertension. Curr Ther Res 1996; 57: 145-58.
[41]
Hosie J, Langan J, Scott M, et al. Effectiveness and tolerability of felodipine once daily and nifedipine twice daily as monotherapies for mild hypertension. J Drug Dev 1992; 5: 129-36.
[42]
Gradman AH, Cutler NR, Davis PJ, et al. Long-term efficacy, tolerability, and safety of the combination of enalapril and felodipine err in the treatment of hypertension. Clin Ther 1998; 20: 527-38.
[43]
Nalbantgil S, Zoghi M, Özerkan F, et al. Comparison of candesartan and felodipine alone and combined in the treatment of hypertension: A single-center, double-blind, randomized, crossover trial. Curr Ther Res 2003; 64: 380-8.
[44]
Morgan T, Anderson A. A comparison of candesartan, felodipine, and their combination in the treatment of elderly patients with systolic hypertension. Am J Heart 2002; 15: 544-9.
[45]
Frishman WH, Hainer JW, Sugg J. A factorial study of combination hypertension treatment with metoprolol succinate extended release and felodipine extended release: Results of the metoprolol succinate-felodipine antihypertension combination trial (m-fact). Am J Hypertens 2006; 19: 388-95.
[46]
Fagan TC. Blood pressure reduction and tolerability of felodipine ER in older and younger hypertensive patients. The felodipine ER in the elderly versus young working group. J Am Geriatr Soc 1997; 45: 712-7.
[47]
Trachtman H, Frank R, Mahan JD, et al. Clinical trial of extended-release felodipine in pediatric essential hypertension. Pediatr Nephrol 2003; 18: 548-53.
[48]
Falkner B, Daniels SR. Summary of the fourth report on the diagnosis, evaluation, and treatment of high blood pressure in children and adolescents. Pediatrics 2004; 114: 555-76.
[49]
Plendil ER. Data Sheet 160412 C, AstraZeneca Limited [available from: http://www.medsafe.govt.nz/profs/datasheet/p/PlendilERtab. pdf
[50]
Evans CA, Jolivette LJ, Nagilla R, et al. Extrapolation of preclinical pharmacokinetics and molecular feature analysis of —discovery-like‖ molecules to predict human pharmacokinetics. Drug Metab Dispos 2006; 34: 1255-65.
[51]
Hardy B, Bartle W, Myers M, et al. Effect of indomethacin on the pharmacokinetics and pharmacodynamics of felodipine. Br J Clin Pharmacol 1988; 26: 557-62.
[52]
Dunselman P, Edgar B, Scaf A, et al. Pharmacokinetics of felodipine after intravenous and chronic oral administration in patients with congestive heart failure. Br J Clin Pharmacol 1989; 28: 45-52.
[53]
Carruthers S, Vint-Reed C. Antihypertensive effect and tolerability of felodipine extended release (ER) tablets in comparison with felodipine plain tablets (PT) and placebo in hypertensives on a diuretic. Clin Invest Med 1993; 16: 386-94.
[54]
Cheung BM, Lau C-P, Wu B-Z. Amlodipine, felodipine, and isradipine in the treatment of chinese patients with mild-to-moderate hypertension. Clin Ther 1998; 20: 1159-69.

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