Page 185 - Basic _ Clinical Pharmacology ( PDFDrive )
P. 185

CHAPTER 10  Adrenoceptor Antagonist Drugs     171



                                                                                                       Pharmacokinetics,
                      Subclass, Drug   Mechanism of Action  Effects             Clinical Applications  Toxicities, Interactions
                        •  Esmolol     β 1  > β 2           Very brief cardiac    Rapid control of BP and   Parenteral only • half-life
                                                            β blockade          arrhythmias, thyrotoxicosis,    ~10 min • Toxicity: Bradycardia
                                                                                and myocardial ischemia   • hypotension
                                                                                intraoperatively
                      TYROSINE HYDROXYLASE INHIBITOR
                        •  Metyrosine  Blocks tyrosine hydroxylase    Lowers BP • may elicit   Pheochromocytoma  Toxicity: Extrapyramidal
                                       • reduces synthesis of   extrapyramidal effects (due            symptoms • orthostatic
                                       dopamine, norepinephrine,    to low dopamine in CNS)            hypotension • crystalluria
                                       and epinephrine
                    1
                     Not available in the USA.



                    PREP AR A TIONS A V AIL ABLE                                 *


                          GENERIC NAME             AVAILABLE AS                GENERIC NAME             AVAILABLE AS
                                      ALPHA BLOCKERS                      Carvedilol             Coreg
                     Alfuzosin              Uroxatral                     Esmolol                Brevibloc
                     Doxazosin              Generic, Cardura              Labetalol              Generic, Normodyne, Trandate
                     Phenoxybenzamine       Dibenzyline                   Levobunolol            Betagan Liquifilm, others
                     Phentolamine           Generic                       Metipranolol           OptiPranolol
                     Prazosin               Generic, Minipress            Metoprolol             Generic, Lopressor, Toprol
                     Silodosin              Rapaflo                       Nadolol                Generic, Corgard
                     Tamsulosin             Flomax                        Nebivolol              Bystolic
                     Terazosin              Generic, Hytrin               Penbutolol             Levatol
                     Tolazoline             Priscoline                    Pindolol               Generic, Visken
                                       BETA BLOCKERS                      Propranolol            Generic, Inderal
                     Acebutolol             Generic, Sectral              Sotalol                Generic, Betapace
                     Atenolol               Generic, Tenormin             Timolol                 
                     Betaxolol                                              Oral                 Generic, Blocadren
                       Oral                 Kerlone                         Ophthalmic           Generic, Timoptic
                       Ophthalmic           Generic, Betoptic                      TYROSINE HYDROXYLASE INHIBITOR
                     Bisoprolol             Generic, Zebeta               Metyrosine             Demser
                     Carteolol               
                       Oral                 Cartrol
                       Ophthalmic           Generic, Ocupress
                    * In the USA.


                    REFERENCES                                           Blakely RD, DeFelice LJ: All aglow about presynaptic receptor regulation of
                                                                             neurotransmitter transporters. Mol Pharmacol 2007;71:1206.
                    Ambrosio G et al: β-Blockade with nebivolol for prevention of acute ischaemic   Blaufarb I, Pfeifer TM, Frishman WH: Beta-blockers: Drug interactions of clinical
                        events in elderly patients with heart failure. Heart 2011;97:209.  significance. Drug Saf 1995;13:359.
                    Arnold AC et al: Combination ergotamine and caffeine improves seated blood   Boyer TD: Primary prophylaxis for variceal bleeding: Are we there yet? Gastroen-
                        pressure and presyncopal symptoms in autonomic failure. Front Physiol   terology 2005;128:1120.
                        2014;5:270.
                    Ayers K et al: Differential effects of nebivolol and metoprolol on insulin sensitivity   Brantigan CO, Brantigan TA, Joseph N: Effect of beta blockade and beta stimula-
                                                                             tion on stage fright. Am J Med 1982;72:88.
                        and plasminogen activator inhibitor in the metabolic syndrome. Hyperten-
                        sion 2012;59:893.                                Bristow M: Antiadrenergic therapy of chronic heart failure: Surprises and new
                    Bell CM et al: Association between tamsulosin and serious ophthalmic adverse   opportunities. Circulation 2003;107:1100.
                        events in older men following cataract surgery. JAMA 2009;301:1991.  Cleland JG: Beta-blockers for heart failure: Why, which, when, and where. Med
                    Berruezo A, Brugada J: Beta blockers: Is the reduction of sudden death related to   Clin North Am 2003;87:339.
                        pure electrophysiologic effects? Cardiovasc Drug Ther 2008;22:163.  Eisenhofer G et al: Current progress and future challenges in the biochemical
                    Bird ST et al: Tamsulosin treatment for benign prostatic hyperplasia and risk   diagnosis and treatment of pheochromocytomas and paragangliomas. Horm
                                                                             Metab Res 2008;40:329.
                        of severe hypotension in men aged 40-85 years in the United States: Risk
                        window analyses using between and within patient methodology. BMJ   Ellison KE, Gandhi G: Optimising the use of beta-adrenoceptor antagonists in
                        2013;347:f6320.                                      coronary artery disease. Drugs 2005;65:787.
   180   181   182   183   184   185   186   187   188   189   190