506
Views
8
CrossRef citations to date
0
Altmetric
Reviews

Pharmacokinetics of selective β1-adrenergic blocking agents: prescribing implications

, MD DSc MSc Prim

Bibliography

  • Jankovic SM. Handbook of pharmacology and toxicology. 4th edition. Faculty of Medical Sciences, University of Kragujevac; Kragujevac: 2013
  • Mansoor AH, Kaul U. Beta-blockers in cardiovascular medicine. J Assoc Phys India 2009;57(Supp l):7-12
  • Brunton LL, Chabner BA, Knollmann BC. Goodman & Gilman’s the pharmacological basis of therapeutics. 12th edition. The McGraw-Hill Companies, Inc; New York: 2011
  • Kendall MJ. Clinical relevance of pharmacokinetic differences between betablockers. Am J Cardiol 1997;80(9B)):15J-9J
  • De Ferrari GM, Salvati P, Grossoni M, et al. Pharmacologic modulation of the autonomic nervous system in the prevention ofsudden cardiac death. A study with propranolol, methacholine and oxotremorine in conscious dogs with a healed myocardial infarction. J Am Coll Cardiol 1993;22(1):283-90
  • Hjalmarson A. Cardioprotection with beta-adrenoceptor blockers. Doeslipophilicity matter? Basic Res Cardiol 2000;95(Suppl 1)):I41-5
  • Cheng JW. Nebivolol: a third-generation beta-blocker for hypertension. Clin Ther 2009;31(3):447-62
  • Mason WD, Winer N, Kochak G, et al. Kinetics and absolute bioavailability of atenolol. Clin Pharmacol Ther 1979;25(4):408-15
  • Kirch W, Görg KG. Clinical pharmacokinetics of atenolol - a review. Eur J Drug Metab Pharmacokinet 1982;7(2):81-91
  • Mehvar R, Gross ME, Kreamer RN. Pharmacokinetics of atenolol enantiomers in humans and rats. J Pharm Sci 1990;79(10):881-5
  • Mehvar R, Brocks DR. Stereospecific pharmacokinetics and pharmacodynamics of beta-adrenergic blockers in humans. J Pharm Pharm Sci 2001;4(2):185-200
  • Regårdh CG, Johnsson G, Jordö L, et al. Plasma concentrations and beta-blocking effects in normal volunteers after intravenous doses of metoprolol and propranolol. J Cardiovasc Pharmacol 1980;2(6):715-23
  • Regårdh CG, Landahl S, Larsson M, et al. Pharmacokinetics of metoprolol and its metabolite alpha-OH-metoprolol in healthy, non-smoking, elderly individuals. Eur J Clin Pharmacol 1983;24(2):221-6
  • Leopold G, Pabst J, Ungethüm W, Bühring KU. Basic pharmacokinetics of bisoprolol, a new highly beta 1-selective adrenoceptor antagonist. J Clin Pharmacol 1986;26(8):616-21
  • Leopold G. Balanced pharmacokinetics and metabolism of bisoprolol. J Cardiovasc Pharmacol 1986;8(Suppl 11):S16-20
  • Cheymol G, Woestenborghs R, Snoeck E, et al. Pharmacokinetic study and cardiovascular monitoring of nebivolol in normal and obese subjects. Eur J Clin Pharmacol 1997;51(6):493-8
  • Veverka A, Salinas JL. Nebivolol in the treatment of chronic heart failure. Vasc Health Risk Manag 2007;3(5):647-54
  • Angaran DM, Schultz NJ, Tschida VH. Esmolol hydrochloride: an ultrashort-acting, beta-adrenergic blocking agent. Clin Pharm 1986;5(4):288-303
  • Piquette-Miller M, Foster RT, Kappagoda CT, Jamali F. Pharmacokinetics of acebutolol enantiomers in humans. J Pharm Sci 1991;80(4):313-16
  • Roux A, Henry JF, Fouache Y, et al. A pharmacokinetic study of acebutolol in aged subjects as compared to young subjects. Gerontology 1983;29(3):202-8
  • Cerqueira PM, Cesarino EJ, Mateus FH, et al. Enantioselectivity in the steady-state pharmacokinetics of metoprolol in hypertensive patients. Chirality 1999;11(7):591-7
  • Stagni G, Davis PJ, Ludden TM. Human pharmacokinetics of betaxolol enantiomers. J Pharm Sci 1991;80(4):321-4
  • Frishman WH, Tepper D, Lazar EJ, Behrman D. Betaxolol: a new long-acting beta 1-selective adrenergic blocker. J Clin Pharmacol 1990;30(8):686-92
  • Borchard U. Pharmacological properties ofbeta-adrenoceptor blocking drugs. J Clin Bas Cardiol 1998;1(1):5-9
  • Drayer DE. Lipophilicity, hydrophilicity, and the central nervous system side effects of beta blockers. Pharmacotherapy 1987;7(4):87-91
  • McAinsh J, Cruickshank JM. Beta-blockers and central nervous system side effects. Pharmacol Ther 1990;46(2):163-97
  • Neil-Dwyer G, Bartlett J, McAinsh J, Cruickshank JM. Beta-adrenoceptor blockers and the blood-brian barrier. Br J Clin Pharmacol 1981;11(6):549-53
  • López-Sendón J, Swedberg K, McMurray J, et al. Task ForceOnBeta-Blockers of the European Society of Cardiology. Expert consensus document onbeta-adrenergic receptor blockers. Eur Heart J 2004;25(15):1341-62
  • Cheymol G, Poirier JM, Carrupt PA, et al. Pharmacokinetics of beta-adrenoceptor blockers in obese and normal volunteers. Br J Clin Pharmacol 1997;43(6):563-70
  • Lakshmi N, VasantDnyandeo B. Physico-chemical characterization of some beta blockers and anti-diabetic drugs - potentiometric and spectrophotometric pKa determination in different co-solvents. Eur J Chem 2011;2(1):36-46
  • Carona G, Steyaerta G, Pagliaraa A, et al. Structure-Lipophilicity Relationships of Neutral and Protonated b-Blockers. Part I. Intra- and Intermolecular Effects in Isotropic Solvent Systems. Helvetica Chimica Acta 1999;82:1211-22
  • Samuels TL, Uncles DR, Willers JW, et al. Logging the potential for intravenous lipid emulsion in propranolol and other lipophilic drug overdoses. Anaesthesia 2011;66(3):221-2
  • Kadam RS, Kompella UB. Influence of lipophilicity on drug partitioning into sclera, choroid-retinal pigment epithelium, retina, trabecular meshwork, and optic nerve. J Pharmacol Exp Ther 2010;332(3):1107-20
  • Carda-Broch S, Berthod A. pH dependence of the hydrophobicity of beta-blocker amine compounds measured by counter-current chromatography. J Chromatogr A 2003;995(1-2):55-66
  • Tetko IV, Tanchuk VY, Villa AE. Prediction of n-octanol/water partition coefficients from PHYSPROP database using artificial neural networks and E-state indices. J Chem Inf Comput Sci 2001;41:1407-21
  • Goldner JA. Metoprolol-induced visual hallucinations: a case series. J Med Case Rep 2012;6(1):65
  • Ahmed AI, van Mierlo PJ, van Waarde JA, Jansen PA. Hallucinations and vividdreams by use of metoprolol. Tijdschr Psychiatr 2010;52(2):117-21
  • Mason WD, Winer N, Kochak G, et al. Kinetics and absolute bioavailability of atenolol. Clin Pharmacol Ther 1979;25(4):408-15
  • Kaye CM, Kumana CR, Leighton M, et al. Observations on the pharmacokinetics of acebutolol. Clin Pharmacol Ther 1976;19(4):416-20
  • Schmidt P, Takacs F, Pittner H, et al. Comparative pharmacokinetics of the beta-1 receptor blookaderceliprolol after a single oral administration in subjects with health kidneys and in patients with impaired renal function. Wien Klin Wochenschr 1985;97(18):729-32
  • Jordö L, Attman PO, Aurell M, et al. Pharmacokinetic and pharmacodynamic properties of metoprolol in patients with impaired renal function. Clin Pharmacokinet 1980;5(2):169-80
  • Payton CD, Fox JG, Pauleau NF, et al. The single dose pharmacokinetics of bisoprolol (10 mg) in renal insufficiency: the clinical significance of balanced clearance. Eur Heart J 1987;8(Suppl M):15-22
  • Höcht C, Bertera FM, Del Mauro JS, Taira CA. Models for evaluating thepharmacokinetics and pharmacodynamics for β-blockers. Expert Opin Drug Metab Toxicol 2014;10(4):525-41
  • Hartmann C, Frölich M, Krauss D, et al. Comparative enantioselective pharmacokinetic studies of celiprolol in healthy volunteers and patients with impaired renal function. Eur J Clin Pharmacol 1990;39(6):573-6
  • Palminteri R, Assael BM, Bianchetti G, et al. Betaxolol kinetics in hypertensive children with normal and abnormal renal function. Clin Pharmacol Ther 1984;35(2):141-7
  • Hoffmann KJ, Regårdh CG, Aurell M, et al. The effect of impaired renal function on the plasma concentration and urinary excretion of metoprolol metabolites. Clin Pharmacokinet 1980;5(2):181-91
  • Wiest D. Esmolol. A review of its therapeutic efficacy and pharmacokinetic characteristics. Clin Pharmacokinet 1995;28(3):190-202
  • Cohen-Solal A, Kotecha D, van Veldhuisen DJ, et al. SENIORS Investigators. Efficacy and safety of nebivolol in elderly heart failure patients with impaired renal function: insights from the SENIORS trial. Eur J Heart Fail 2009;11(9):872-80
  • McAinsh J, Holmes BF, Smith S, et al. Atenolol kinetics in renal failure. Clin Pharmacol Ther 1980;28(3):302-9
  • Smith RS, Warren DJ, Renwick AG, George CF. Acebutolol pharmacokinetics in renal failure. Br J Clin Pharmacol 1983;16(3):253-8
  • Pruss TP, Lamon KD, Hagen NS. Celiprolol - overview of 6 years of clinical trials experience. J Int Med Res 1988;16(Suppl 1):17A-22A
  • Stajić M, Granger RH, Beyer JC. Fatal metoprolol overdose. J Anal Toxicol 1984;8(5):228-30
  • Bühring KU, Sailer H, Faro HP, et al. Pharmacokinetics and metabolism of bisoprolol-14C in three animal species and in humans. J Cardiovasc Pharmacol 1986;8(Suppl 11):S21-8
  • Ryan JR. Clinical pharmacology of acebutolol. Am Heart J 1985;109(5 Pt 2):1131-6
  • Reeves PR, McAinsh J, McIntosh DA, Winrow MJ. Metabolism of atenolol in man. Xenobiotica 1978;8(5):313-20
  • Winkle RA, Meffin PJ, Ricks WB, Harrison DC. Acebutolol metabolite plasma concentration during chronic oral therapy. Br J Clin Pharmacol 1977;4(5):519-22
  • Ohashi K, Warrington SJ, Kaye CM, et al. Observations on the clinical pharmacology and plasma concentrations of diacetolol, the major human metabolite of acebutolol. Br J Clin Pharmacol 1981;12(4):561-5
  • Milne RJ, Buckley MM. Celiprolol. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in cardiovascular disease. Drugs 1991;41(6):941-69
  • Wellstein A, Palm D, Belz GG, et al. Concentration kinetics of propranolol, bisoprolol, and atenolol in humans assessed with chemical detection and a subtype-selective beta-adrenoceptor assay. J Cardiovasc Pharmacol 1986;8(Suppl 11):S41-5
  • Horikiri Y, Suzuki T, Mizobe M. Stereoselective metabolism of bisoprolol enantiomers in dogs and humans. Life Sci 1998;63(13):1097-108
  • Wong YW, Ludden TM. Determination of betaxolol and its metabolites in blood and urine by high-performance liquid chromatography with fluorimetric detection. J Chromatogr 1990;534:161-72
  • Minushkina LO, Zateishchikova AA, Zateishchikov DA, et al. Genetic aspects of individual sensitivity to betaxolol in patients with arterial hypertension. Kardiologiia 2008;48(3):20-6
  • Blake CM, Kharasch ED, Schwab M, Nagele P. A meta-analysis of CYP2D6 metabolizer phenotype and metoprolol pharmacokinetics. Clin Pharmacol Ther 2013;94(3):394-9
  • Xu T, Bao S, Geng P, et al. Determination of metoprolol and its two metabolites in human plasma and urine by high performance liquid chromatography with fluorescence detection and its application in pharmacokinetics. J Chromatogr B AnalytTechnol Biomed Life Sci 2013;937:60-6
  • Ebihara A, Fujimura A. Metabolites of antihypertensive drugs. An updated review of their clinical pharmacokinetic and therapeutic implications. Clin Pharmacokinet 1991;21(5):331-43
  • Prisant LM. Nebivolol: pharmacologic profile of an ultraselective, vasodilatory beta1-blocker. J Clin Pharmacol 2008;48(2):225-39
  • Jahn P, Eckrich B, Schneidrowski B, et al. Beta 1-adrenoceptor subtype selective antagonism of esmolol and its major metabolite in vitro and in man. Investigations using tricresylphosphate as red blood cell carboxylesterase inhibitor. Arzneimittelforschung 1995;45(5):536-41
  • Talbert RL. Pharmacokinetics and pharmacodynamics of beta blockers in heart failure. Heart Fail Rev 2004;9(2):131-7
  • Nikolic VN, Jevtovic-Stoimenov T, Velickovic-Radovanović R, et al. Population pharmacokinetics of bisoprolol in patients with chronic heart failure. Eur J Clin Pharmacol 2013;69(4):859-65
  • Taguchi M, Nozawa T, Igawa A, et al. Pharmacokinetic variability of routinely administered bisoprolol in middle-aged and elderly Japanese patients. Biol Pharm Bull 2005;28(5):876-81
  • Grevel J, Thomas P, Whiting B. Population pharmacokinetic analysis of bisoprolol. Clin Pharmacokinet 1989;17(1):53-63
  • Hayes PC, Jenkins D, Vavianos P, et al. Single oral dose pharmacokinetics of bisoprolol 10 mg in liver disease. Eur Heart J 1987;8(Suppl M):23-9
  • Rey E, Jammet P, d’Athis P, et al. Effect of cimetidine on the pharmacokinetics of the new beta-blocker betaxolol. Arzneimittelforschung 1987;37(8):953-6
  • Jin SK, Chung HJ, Chung MW, et al. Influence of CYP2D6*10 on the pharmacokinetics of metoprolol in healthy Korean volunteers. J Clin Pharm Ther 2008;33(5):567-73
  • Taguchi M, Nozawa T, Mizumaki K, et al. Nonlinear mixed effects model analysis of the pharmacokinetics of metoprolol in routinely treated Japanese patients. Biol Pharm Bull 2004;27(10):1642-8
  • Cheymol G, Woestenborghs R, Snoeck E, et al. Pharmacokinetic study and cardiovascular monitoring of nebivolol in normal and obese subjects. Eur J Clin Pharmacol 1997;51(6):493-8
  • Ieiri I, Doi Y, Maeda K, et al. Microdosing clinical study: pharmacokinetic,pharmacogenomic (SLCO2B1), and interaction (grapefruit juice) profiles ofceliprolol following the oral microdose and therapeutic dose. J Clin Pharmacol 2012;52(7):1078-89
  • Lilja JJ, Niemi M, Neuvonen PJ. Rifampicinreduces plasma concentrations of celiprolol. Eur J Clin Pharmacol 2004;59(11):819-24
  • Lilja JJ, Raaska K, Neuvonen PJ. Effects of orange juice on thepharmacokinetics of atenolol. Eur J Clin Pharmacol 2005;61(5-6):337-40
  • Shirasaka Y, Shichiri M, Mori T, et al. Major active components in grapefruit, orange, and apple juices responsible for OATP2B1-mediated drug interactions. J Pharm Sci 2013;102(9):3418-26
  • Kirch W, Spahn H, Ohnhaus EE, et al. Influence ofinflammatory disease on the clinical pharmacokinetics of atenolol and metoprolol.Biopharm Drug Dispos. 1983;4(1):73-81
  • Hallengren B, Nilsson OR, Karlberg BE, et al. Influence of hyperthyroidism on the kinetics of methimazole, propranolol, metoprolol and atenolol. Eur J Clin Pharmacol 1982;21(5):379-84
  • Roux A, Henry JF, Fouache Y, et al. A pharmacokinetic study of acebutolol in aged subjects as compared to young subjects. Gerontology 1983;29(3):202-8
  • Piquette-Miller M, Foster RT, Kappagoda CT, Jamali F. Effect of aging on the pharmacokinetics of acebutolol enantiomers. J Clin Pharmacol 1992;32(2):148-56

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.