Skip to main content
Log in

State-of-the-Art: Comparative Pharmacology of the β-Adrenoceptor Blocking Drugs

  • Section 2A: Pharmacodynamics, Pharmacokinetics and Drug Interactions
  • Published:
Drugs Aims and scope Submit manuscript

Summary

There are certain pharmacological differences among the many β- adrenoceptor blocking drugs (β- blockers) available today. These properties may influence the clinical selection of a β- blocker and include cardioselectivity, partial agonist activity, membrane stabilising activity and lipophilicity. These properties are reviewed to assess their relevance and relative importance in clinical and experimental situations.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

References

  • Abramson, E.A.; Arky, R.A. and Wocker, K.A.: Effects of propranolol on the hormonal and metabolic responses to insulin-induced hypoglycaemia. Lancet 2: 1386–1391 (1966).

    Article  PubMed  CAS  Google Scholar 

  • Ariens, E.J. and Simonis, A.M.: Receptors and receptor mechanisms; in Saxena and Forsyth (Eds) Beta-adrenoceptor Blocking Agents pp.3–28 (North Holland American Elsevir, Amsterdam, New York 1976).

    Google Scholar 

  • Arnold, J.M.O. and McDevitt, D.G.: Interpretation of isoprenaline dose-response curves in the presence of selective and non-selective beta-adrenoceptor blocking drugs. British Journal of Clinical Pharmacology 13: 585P (1982).

    CAS  Google Scholar 

  • Baker, S.P.; Boyd, H.M. and Potter, L.T.: Distribution and function of beta-adrenoceptors in different chambers of the canine heart. British Journal of Pharmacology 68: 57–63 (1980).

    Article  PubMed  CAS  Google Scholar 

  • Benson, M.K.; Beril, W.T.; Cruickshank, J.M. and Sterling, G.S.: A comparison of four beta-adrenoceptor antagonists in patients with asthma. British Journal of Clinical Pharmacology 5: 415–419 (1978).

    Article  PubMed  CAS  Google Scholar 

  • Betts, T.A. and Alford, C.: β-Blocking drugs and sleep: a controlled trial. Drugs 25 (Suppl. 2): 268–272 (1983).

    Article  Google Scholar 

  • Brick, I.; Hutchinson, K.J.; McDevitt, D.G.; Broddie, I.C. and Shanks, R.G.: Comparison of the effects of I.C.I. 50172 and propranolol on the cardiovascular responses to adrenaline, isoprenaline and exercise. British Journal of Pharmacology 34: 127–140 (1968).

    Article  PubMed  CAS  Google Scholar 

  • Campbell, W.B.; Callahan, K.S.; Johnson, A.R. and Graham, R.M.: Antiplatelet action of beta-adrenergic antagonists: inhibition of thromboxane synthesis and platelet aggregation in patients receiving long-term propranolol treatment. Lancet 2: 1382–1384 (1981).

    Article  PubMed  CAS  Google Scholar 

  • Carlson, E.; Dahlof, C-G.; Hedberg, A.; Person, H. and Tangstrand, B.: Differentiation of cardiac chronotropic and inotropic effects of beta-adrenoceptor agonists. Naunyn-Schmiedebergs’s Archives of Pharmacology 300: 101–105 (1977).

    Article  Google Scholar 

  • Clark, B.J.: Pharmacology of beta-adrenoceptor blocking drugs; in Saxena and Forsyth (Eds) Beta-Adrenoceptor Blocking Agents, pp.45–78 (North Holland American Elsevir, Amsterdam, New York 1976).

    Google Scholar 

  • Coltart, D.J.; Gibson, D.G. and Shand, D.G.: Plasma propranolol levels associated with suppression of ventricular ectopic beats. British Medical Journal 1: 490–492 (1971).

    Article  PubMed  CAS  Google Scholar 

  • Conrad, K.A.: Comparison of the inotropic and chronotropic effects of metoprolol and propranolol. Journal of Clinical Pharmacology 21: 213–218 (1981).

    PubMed  CAS  Google Scholar 

  • Conway, F.J.; Fitzgerald, J.D.; McAinsh, T.; Rowlands, D.J.; and Shipson, W.T.: Human pharmacokinetic and pharmacodynamic studies on atenolol (I.C.I. 66082), a new cardioselective beta-adrenoceptor blocking drug. British Journal of Clinical Pharmacology 3: 267–272 (1976).

    Article  PubMed  CAS  Google Scholar 

  • Cruickshank, J.M.: The clinical importance of cardioselectivity and lipophilibility in beta blockers. American Heart Journal 100: 160–178 (1980).

    Article  PubMed  CAS  Google Scholar 

  • Deacon, S.P. and Barnett, D.: Comparison of atenolol and propranolol during insulin-induced hypoglycaemia. British Medical Journal 2: 272–274 (1976).

    Article  PubMed  CAS  Google Scholar 

  • Dreyer, A.C. and Offermeier, J.: Indications for the existence of two types of cardiac beta-adrenergic receptors. Pharmacological Research Communications 7: 151–161 (1975).

    Article  PubMed  CAS  Google Scholar 

  • Ellis, M.E.; Sabay, J.N.; Anatterjee, S.S.; Cruickshank, J.N. and Ellis, S.H.: Cardioselectivity in asthmatic patients. European Journal of Clinical Pharmacology 21: 173–176 (1981).

    Article  PubMed  CAS  Google Scholar 

  • Fitzgerald, D.; Gurnbrielle, T. and Harry, J.D.: Effects in man of I.C.I. 118551 (a selective beta2-adrenoceptor blocking drug) on some cardiovascular responses induced by isoprenaline. British Journal of Clinical Pharmacology 13: 586P (1982).

    CAS  Google Scholar 

  • Frishman, W.H.; Christodoulou, J.; Weksler, B.; Smithen, C. and Kilip, T.: Reversal of abnormal platelet aggregability and change in exercise tolerance in patients with angina pectoris following oral propranolol. Circulation 50: 887–891 (1974).

    Article  PubMed  CAS  Google Scholar 

  • Firsk-Holmberg, M.; Jorfeldt, L. and Juhlin-Dannfelt, J.: Metabolic effects in muscle during antihypertensive therapy with beta1- and beta2-adrenoceptor blockers. Clinical Pharmacology and Therapeutics 30: 611–618 (1981).

    Article  Google Scholar 

  • Gugler, R.; Kriat, R.; Raczinski, H.; Hoffgen, K. and Bodem, G.: Comparative pharmacodynamics and plasma levels of β-adrenoceptor blocking drugs. British Journal of Clinical Pharmacology 10: 337–343 (1980).

    PubMed  CAS  Google Scholar 

  • Heel, R.C.; Brogden, R.N.; Speight, T.M. and Avery, G.S.: Atenolol: a review of its pharmacological properties and therapeutic efficacy in hypertension. Drugs 17: 425–460 (1979).

    Article  PubMed  CAS  Google Scholar 

  • Hollifield, J.W.; Sherman, K..; Van der Zwagg, R. and Shand, D.G.: Proposed mechanisms of propranolol antihypertensive effect in essential hypertension. New England Journal of Medicine 295: 68–73 (1976).

    Article  PubMed  CAS  Google Scholar 

  • Houben, H.; Thien, T. and Van’t Laar, A.: Haemodynamic effects of cigarette smoking during selective and non-selective β-adrenoceptor blockade in patients with hypertension. British Journal of Clinical Pharmacology 12: 67–72 (1981).

    Article  PubMed  CAS  Google Scholar 

  • Johnsson, G.; Nyberg, G. and Solvell, L.: Influence of metoprolol and propranolol on haemodynamic effects induced by physical work and isoprenaline. Acta Pharmacologica and Toxicologica 36 (Suppl.V): 69–75 (1975).

    Article  CAS  Google Scholar 

  • Lands, A.M.; Arnold, A.; McAuliff, J.P.; Luduena, F.P. and Brown, T.G.: Differentiation of receptor systems activated by sympathomimetic amines. Nature 214: 597–589 (1967).

    Article  PubMed  CAS  Google Scholar 

  • Lager, I.; Blohme, G. and Smith, V.: Effect of cardioselective and non-selective blockade on the hypoglycaemic response in insulin-dependent diabetics. Lancet 1: 458–462 (1979).

    Article  PubMed  CAS  Google Scholar 

  • Lofdahl, C-G. and Svedmyr, N.: Cardioselectivity of atenolol and metoprolol: a study in asthmatic patients. European Journal of Respiratory Disease 62: 396–404 (1981a).

    CAS  Google Scholar 

  • Lofdahl, C-G. and Svedmyr, N.: Prenalterol — a selective β1 adrenoceptor agonist in asthmatics. European Journal of Respiratory Disease 113 (Suppl.): 111–112 (1981b).

    Google Scholar 

  • Lundborg, P.; Astrom, H.; Bengtsson, C.; Fellemis, E.; Von Schneck, H.; Svensson, L. and Smith, U.: Effect of beta-adrenoceptor blockade on exercise performance and metabolism. Clinical Science 61: 299–305 (1981).

    PubMed  CAS  Google Scholar 

  • McDevitt, D.G.: Clinical significance of cardioselectivity. State-of-the-Art. Drugs 25 (Suppl. 2): 219–226 (1983).

    Article  Google Scholar 

  • McDevitt, D.G.; Brown, H.C.; Carruthers, S.G. and Shanks, R.G.: Influence of intrinsic sympathomimetic activity and cardioselectivity on β-adrenoceptor blockade. Clinical Pharmacology and Therapeutics 21: 556–566 (1977).

    PubMed  CAS  Google Scholar 

  • Svendson, T.L.; Hartling, O.J.; Trap-Jensen, J.; McNair, A. and Bleddal, T.: Adrenergic beta receptor blockade: Haemodynamic importance of intrinsic sympathomimetic activity at rest. Clinical Pharmacology and Therapeutics 29: 711–718 (1981).

    Article  Google Scholar 

  • Taylor, E.A.; Jefferson, D.; Carrol, J.D. and Turner, P.: Cerebrospinal fluid concentration of propranolol, pindolol and atenolol in man: Evidence for central actions of beta-adrenoceptor antagonists. British Journal of Clinical Pharmacology 4: 549–560 (1981).

    Article  Google Scholar 

  • Trap-Jensen, J.; Carlsen, J.E.; Svendsen, T.L. and Christiensen, N.J.: Cardiovascular and adrenergic effects of cigarette smoking during immediate non-selective and selective beta-adrenoceptor blockade in humans. European Journal of Clinical Investigation 9: 181–183 (1979).

    Article  PubMed  CAS  Google Scholar 

  • Turner, P.: β-Blockade and the human central nervous system. Drugs 25 (Suppl. 2): 262–264 (1983).

    Article  Google Scholar 

  • William-Olson, T.; Felleminis, E.; Bjorntorp, P. and Smith, U.: Differences in metabolic response to beta-adrenergic stimulation after propranolol or metoprolol administration. Acta Medica Scandinavica 205: 201–206 (1979).

    Article  Google Scholar 

  • Woosley, R.L.; Kornhauser, D.; Smith, R.L.; Reele, S.; Higgins, S.B.; Nies, A.S.; Shand, D.G. and Oates J.A.: Suppression of chronic ventricular arrhythmias with propranolol. Circulation 60: 819–827 (1979).

    Article  PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Shand, D.G. State-of-the-Art: Comparative Pharmacology of the β-Adrenoceptor Blocking Drugs. Drugs 25 (Suppl 2), 92–99 (1983). https://doi.org/10.2165/00003495-198300252-00031

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003495-198300252-00031

Keywords

Navigation