Propranolol

  • Adam Schneeweiss
  • Gotthard Schettler
Part of the Developments in Cardiovascular Medicine book series (DICM, volume 72)

Abstract

Propranolol is the first beta-adrenoreceptor blocker introduced to clinical use that is still routinely used today. Moreover, at present, it is the most widely used beta-adrenoreceptor in the world. It is a nonselective beta-blocker, affecting both beta-1 and beta-2 adrenoreceptors. The potency of this effect serves as a standard against which newer beta-blockers are compared. Propranolol had local anesthetic activity (membrane-stabilizing or quinidine-like effect). It is devoid of intrinsic sympathomimetic activity.

Keywords

Placebo Fatigue Depression Migraine Radionuclide 

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References

  1. 1.
    Lake C, et al: Use of plasma norepinephrine for evaluation of sympathetic neuronal function in man. I. Science 18:1315, 1976.Google Scholar
  2. 2.
    Ledingham JGG, et al: The meaning of aldosteronism in hypertensive disease. Circ Res [Suppl 2] 21:177, 1967.Google Scholar
  3. 3.
    Thadani U, et al: Comparison of adrenergic beta-receptor antagonists in angina pectoris. Br Med J 1:138, 1973.PubMedCrossRefGoogle Scholar
  4. 4.
    Davidson C, et al: Comparison of antihypertensive activity of beta-blocking drugs during chronic treatment. Br Med J 2:7, 1976.PubMedCrossRefGoogle Scholar
  5. 5.
    Milne JR, et al: Effect of intravenous propranolol on QT interval: a new method of assessment. Br Heart J 43:1, 1980.PubMedCrossRefGoogle Scholar
  6. 6.
    Sonnenblick EH, et al: Effect of exercise on myocardial force-velocity relations in intact unanesthetized man: relative roles of changes in heart rate, sympathetic activity, and ventricular dimensions. J Clin Invest 44:2051, 1965.PubMedCrossRefGoogle Scholar
  7. 7.
    Friedman MJ, et al: Effects of propranolol on resting and postextrasystolic potentiated left ventricular function in patients with coronary artery disease. Am Heart J 106:81, 1983.CrossRefGoogle Scholar
  8. 8.
    Port S, et al: Effects of propranolol on left ventricular function in normal men. Circulation 61:358, 1980.PubMedGoogle Scholar
  9. 9.
    Sklar J, et al: The effects of a cardioloselective (metoprolol) and a nonselective (propranolol) beta-adrenergic blocker on the response to dynamic exercise in normal men. Circulation 65:894, 1982.PubMedCrossRefGoogle Scholar
  10. 10.
    Le Winter M, et al: Effects of oral propranolol in normal subjects. Clin Pharmacol Ther 17:709, 1975.Google Scholar
  11. 11.
    Sapru RP, et al: Effect of isoprenaline and propranolol on left ventricular function as determined by nuclear angiography. Br Heart J 44:75, 1980.PubMedCrossRefGoogle Scholar
  12. 12.
    Reduto LA, et al: Radionuclide assessment of ventricular performance during propranolol withdrawal prior to aortocoronary bypass surgery. Am Heart J 96:714, 1978.PubMedCrossRefGoogle Scholar
  13. 13.
    Marshall RC, et al: Effect of oral propranolol on rest, exercise and postexercise left ventricular performance in normal subjects and patients with coronary artery disease. Circulation 63:572, 1981.PubMedCrossRefGoogle Scholar
  14. 14.
    Dwyer EM Jr, et al: Effects of beta-adrenergic blockade on left ventricular hemodynamics and the electrocardiogram during exercise-induced angina pectoris. Circulation 38:250, 1968.PubMedGoogle Scholar
  15. 15.
    Bonow, et al: Effects of verapamil and propranolol on left ventricular systolic function and diastolic filling in patients with coronary artery disease. Circulation 65:1337, 1982.PubMedCrossRefGoogle Scholar
  16. 16.
    Lake CR, et al: Adjusted plasma norepinephrine levels are similar in normotensive and hypertensive subjects. N Engl J Med 296:208, 1977.PubMedCrossRefGoogle Scholar
  17. 17.
    Sever PS, et al: Plasma-noradrenaline in essential hypertension. Lancet 1:1078, 1977.PubMedGoogle Scholar
  18. 18.
    Schocken D, Roth G: Reduced beta-adrenergic receptor concentrations in aging man. Nature 267:856, 1977.PubMedCrossRefGoogle Scholar
  19. 19.
    Vestal RE, et al: Reduced beta-adrenoreceptor sensitivity in the elderly [abstr]. Clin Res 26:488A, 1978.Google Scholar
  20. 20.
    Conway J, et al: Sympathetic nervous activity during exercise in relation to age. Cardiovasc Res 5:577, 1971.PubMedCrossRefGoogle Scholar
  21. 21.
    ß-blocker Heart Attack Trial Research Group: A randomized trial of propranolol in patients with acute myocardial infarction. I. Mortality results. JAMA 247:1707, 1982.CrossRefGoogle Scholar
  22. 22.
    Baber NS, et al: Multicentre post-infarction trial of propranolol in 49 hospitals in the United Kingdom, Italy and Yugoslavia. Br Heart J 44:96, 1980.PubMedCrossRefGoogle Scholar
  23. 23.
    Andersen MP, et al: Effect of alprenolol on mortality among patients with definite or suspected acute myocrdial infarction: preliminary results. Lancet 2:865, 1979.PubMedCrossRefGoogle Scholar
  24. 24.
    Keelan P: Double-blind trial of propranolol (Inderal) in angina pectoris. Br Med 1:897, 1965.CrossRefGoogle Scholar
  25. 25.
    Wolfson S, et al: Propranolol and angina pectoris. Am J Cardiol 18:345, 1966.PubMedCrossRefGoogle Scholar
  26. 26.
    Amsterdam EA, et al: Evaluation of long term use of propranolol in angina pectoris. JAMA 201:103, 1969.CrossRefGoogle Scholar
  27. 27.
    Gillam PMS, Prichard BNC: Use of propranolol in angina pectoris. Br Med J 2:337, 1965.PubMedCrossRefGoogle Scholar
  28. 28.
    Srivastava SC, et al: Double-blind trial of propranolol (Inderal) in angina of effort. Br Med J 2:724, 1964.PubMedCrossRefGoogle Scholar
  29. 29.
    Zeft HJ, et al: The effect of propranolol in the long-term treatment of angina pectoris. Arch Intern Med 124:578, 1969.PubMedCrossRefGoogle Scholar
  30. 30.
    Guazzi M, et al: Clinical electrocardiographic and hemodynamic effects of long-term use of propranolol in Prinzmetal’s variant angina pectoris. Br Heart J 1971, 33:889.PubMedCrossRefGoogle Scholar
  31. 31.
    Guazzi M, et al: Treatment of spontaneous angina pectoris with beta-blocking agents: a clinical, electrocardiographic and hemodynamic appraisal. Br Heart J 37:1235, 1975.PubMedCrossRefGoogle Scholar
  32. 32.
    Fauchier JP, et al: Amiodarone injectable et par voie orale dans le traitment de l’angor de Prinzmetal severe et syncopal. Ann Cardiol Angeiol (Paris) 27:193, 1978.Google Scholar
  33. 33.
    Robertson RM, et al: Exacerbation of vasotonic angina pectoris by propranolol. Circulation 65:281, 1982.PubMedCrossRefGoogle Scholar
  34. 34.
    Tilmant PY, et al: Detrimental effect of propranolol in patients with coronary arterial spasm countered by combination with diltiazem. Am J Cardiol 52:230, 1983.PubMedCrossRefGoogle Scholar
  35. 35.
    Kern MJ, et al: Potentiation of coronary vasconstriction by beta-adrenergic blockade in patients with coronary artery disease. Circulation 67:1178, 1983.PubMedCrossRefGoogle Scholar
  36. 36.
    Jackson M, et al: Propranolol in the treatment of essential hypertension. JAMA 237:2303, 1977.CrossRefGoogle Scholar
  37. 37.
    Prichard BNC: Propranolol as an antihypertensive agent. Am Heart J 79:128, 1970.PubMedCrossRefGoogle Scholar
  38. 38.
    Frohlich ED, et al: The paradox of beta-adrenergic blockade in hypertension. Circulation 37:417, 1968.PubMedGoogle Scholar
  39. 39.
    Offerhaus L, Van Zweiten PA: Comparative studies on central factors contributing to the hypotensive action of propranolol, alprenolol and their enantiomers. Cardiovasc Res 8:488, 1974.PubMedCrossRefGoogle Scholar
  40. 40.
    Bühler FR, et al: Propranolol inhibition of renin secretion: a specific approach to diagnosis and treatment of renin-dependent hypertensive diseases. N Engl J Med 287:1209, 1972.PubMedCrossRefGoogle Scholar
  41. 41.
    Prichard BNC, Gillam PMS: Treatment of hypertension with propranolol. Br Med J 1:7, 1969.PubMedCrossRefGoogle Scholar
  42. 42.
    Prichard BNC, Gillam PMS: Propranolol in hypertension. Am J Cardiol 18:387, 1966.PubMedCrossRefGoogle Scholar
  43. 43.
    Bravo EL, et al: ß-adrenergic blockade in diuretic-treated patients with essential hypertension. N Engl J Med 292:66, 1975.PubMedCrossRefGoogle Scholar
  44. 44.
    Hollifield JW, et al: Proposed mechanisms of propranolol’s antihypertensive effect in essential hypertension. N Engl J Med 295:68, 1976.PubMedCrossRefGoogle Scholar
  45. 45.
    VandenBurg MJ, et al: Reduced peripheral vascular symptoms in elderly patients treated with α-methyldopa: a comparison with propranolol. Eur J Clin Pharmacol 26:325, 1984.PubMedCrossRefGoogle Scholar
  46. 46.
    Sloman G: Propranolol in management of muscular subaortic stenosis. Br Heart J 29:783, 1967.PubMedCrossRefGoogle Scholar
  47. 47.
    Swan DA, et al: Analysis of symptomatic course and prognosis and treatment of hypertrophic obstructive cardiomyopathy. Br Heart J 33:671, 1971.PubMedCrossRefGoogle Scholar
  48. 48.
    Frank MJ, et al: Long term medical management of hypertrophic obstructive cardiomyopathy. Am J Cardiol 42:993, 1978.PubMedCrossRefGoogle Scholar
  49. 49.
    Vasquez M, et al: Clinical electrophysiological effects of propranolol on normal sinus node function. Br Heart J 41:709, 1979.PubMedCrossRefGoogle Scholar
  50. 50.
    Rosen KM, et al: Effects of lidocaine and propranolol on the normal and anomalous pathways in patients with pre-excitation. Am J Cardiol 30:801, 1972.PubMedCrossRefGoogle Scholar
  51. 51.
    Seides SF, et al: The electrophysiology of propranolol in man. Am Heart J 88:733, 1974.PubMedCrossRefGoogle Scholar
  52. 52.
    Strauss HC, et al: Electrophysiologic effects of propranolol on sinus node function inpatients with sinus node dysfunction. Circulation 54:452, 1976.PubMedGoogle Scholar
  53. 53.
    Winkle RA, et al: Antiarrhythmic effect assessed from ventricular arrhythmia reduction in the ambulatory electrocardiogram and treadmill test: a comparison of propranolol, procainamide and quinidine. Am J Cardiol 42:473, 1978.PubMedCrossRefGoogle Scholar
  54. 54.
    Koppes GM, et al: Propranolol therapy for ventricular arrhythmias 2 months after acute myocardial infarction. Am J Cardiol 46:322, 1980.PubMedCrossRefGoogle Scholar
  55. 55.
    Singh SN, et al: Comparison of acebutolol and propranolol for treatment of chronic ventricular arrhythmia: a placebo-controlled, double-blind, randomized crossover study. Circulation 65:1356, 1982.PubMedCrossRefGoogle Scholar
  56. 56.
    Woosley RL, et al: Suppression of chronic ventricular arrhythmias with propranolol. Circulation 60:819, 1979.PubMedGoogle Scholar
  57. 57.
    Mueller HS, et al: Propranolol during the evolution and subsequent ten days of myocardial infarction in man. Clin Cardiol 2:393, 1979.PubMedCrossRefGoogle Scholar
  58. 58.
    Morganroth J, et al: Effect of propranolol on ventricular arrhythmias in the ß-blocker heart attack trial (BHAT). Circulation [Suppl 2] 66:1313, 1982.Google Scholar
  59. 59.
    Chung EK: Wolff-Parkinson-White syndrome: current views. Am J Med 62:252, 1977.PubMedCrossRefGoogle Scholar
  60. 60.
    Callagher JJ, et al: The Wolff-Parkinson-White syndrome and the preexcitation dysrhythmias. Med Clin North Am 60:101, 1976.Google Scholar
  61. 61.
    Frishman WH, et al: Comparative effects of abrupt withdrawal of propranolol and verapamil in angina pectoris. Am J Cardiol 50:1191, 1982.PubMedCrossRefGoogle Scholar
  62. 62.
    Frishman WH, et al: Reversal of abnormal platelet aggregability and change in exercise tolerance in patients with angina pectoris following oral propranolol. Circulation 50:887, 1974.PubMedGoogle Scholar
  63. 63.
    Boudoulas H, et al: Hypertensitivity to adrenergic stimulation after propranolol withdrawal in normal subjects. Ann Intern Med 87:433, 1977.PubMedGoogle Scholar
  64. 64.
    Glaubiger G, Lefkowitz RJ: Elevated beta-adrenergic receptor number after chromic propranolol treatment. Biochem Biophys Res Commun 78:720, 1977.PubMedCrossRefGoogle Scholar
  65. 65.
    Alderman EL, et al: Coronary artery syndromes after sudden propranolol withdrawal. Ann Intern Med 81:625, 1974.PubMedGoogle Scholar
  66. 66.
    Nattel S, et al: Mechanism of propranolol withdrawal phenomena. Circulation 59:1158, 1979.PubMedGoogle Scholar
  67. 67.
    Thadani U, Parker JO: Propranolol in the treatment of angina pectoris: comparison of duraton of action in acute and sustained oral therapy. Circulation 59:571, 1979.PubMedGoogle Scholar
  68. 68.
    Dart AM, et al: The effect of chronic propranolol treatment on overnight plasma levels of anterior pituitary and related hormones. Br J Clin Pharmacol 12:849, 1981.PubMedGoogle Scholar
  69. 69.
    Kawashima K, et al: Stereospecific radioimmunoassay for propranolol isomers. J Pharmacol Exp Ther 196:517, 1976.PubMedGoogle Scholar
  70. 70.
    Levy A, et al: Disposition of propranolol isomers in mice. Eur J Pharmacol 40:93, 1976.PubMedCrossRefGoogle Scholar
  71. 71.
    Jackman GP, et al: No stereoselective first-pass hepatic extraction of propranolol. Clin Pharmacol Ther 30:291, 1981.PubMedCrossRefGoogle Scholar
  72. 72.
    Mizgala HG, et al: Propranolol in the prophylactic treatment of angina pectoris. Can Med Assoc J 100:756, 1969.PubMedGoogle Scholar
  73. 73.
    Zacest R, Koch-Weser J: Relation of propranolol plasma level to beta-blockade during oral therapy. Pharmacology 7:178, 1972.PubMedCrossRefGoogle Scholar
  74. 74.
    Evans GH, et al: The disposition of propranolol. III. Decreased half-life and volume of distribution as a result of plasma binding in man, monkey, dog and rat. J Pharmacol Exp Ther 186:114, 1973.PubMedGoogle Scholar
  75. 75.
    Wood AJJ, et al: Direct measurement of propranolol bioavailability during accumulation to steady state. Br J Clin Pharmacol 6:345, 1978.PubMedGoogle Scholar
  76. 76.
    Shand DG, et al: Plasma propranolol levels in adults. Clin Pharmacol Ther 11:112, 1970.PubMedGoogle Scholar
  77. 77.
    Castleden CM, George CF: The effect of ageing on the hepatic clearance of propranolol. Br J Clin Pharmacol 7:49, 1979.PubMedGoogle Scholar
  78. 78.
    Vestal RE, et al: Effects of age and cigarette smoking on propranolol disposition. Clin Pharmacol Ther 26:8, 1979.PubMedGoogle Scholar
  79. 79.
    Bendayan R, et al: Influence of age on serum protein binding of propranolol. Eur J Clin Pharmacol 26:251, 1984.PubMedCrossRefGoogle Scholar
  80. 80.
    Paxton JW, Briant RH: α-acid glycoprotein concentrations and propranolol binding in elderly patients with acute illness. Br J Clin Pharmacol 18:806, 1984.PubMedGoogle Scholar
  81. 81.
    Waller DG, et al: Intravenous propranolol in patients with inflammation [letter]. Br J Clin Pharmacol 13:577, 1982.PubMedGoogle Scholar
  82. 82.
    Greenblatt DJ, Koch-Weser J: Adverse reactions to propranolol in hospitalized medical patients: a report from the Boston Collaborative Drug Surveillance Program. Am Heart J 86:478, 1973.PubMedCrossRefGoogle Scholar
  83. 83.
    Solomon S, et al: Impairment of memory function by antihypertensive medication. Arch Gen Psychiatry 40:1109, 1983.PubMedGoogle Scholar

Copyright information

© Martinus Nijhoff Publishing, Boston 1988

Authors and Affiliations

  • Adam Schneeweiss
    • 1
  • Gotthard Schettler
    • 2
  1. 1.Geriatric Cardiology Research FoundationTel-AvivIsrael
  2. 2.Department of MedicineUniversity of HeidelbergGermany

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