Skip to main content

Labetalol: A Review of its Pharmacology and Therapeutic Use in Hypertension

  • Chapter
Antihypertensive Drugs Today

Part of the book series: Cardiovascular Drugs ((CADR,volume 4))

Abstract

Labetalol is a salicylamide derivative (fig. 1) synthesised by Dr L.H.C. Lunts and his colleagues which has been shown to be a specific competitive antagonist at both α- and β-adrenoceptors.

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

Access this chapter

eBook
USD 16.99
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 16.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  • Aggerbeck, M.; Guellaen, G. and Hanoure, J.: Biochemical evidence for the dual action of labetalol on a- and β-adrenoceptors. British Journal of Pharmacology 62: 543 (1978).

    PubMed  CAS  Google Scholar 

  • Anderson, C.C. and Gabriel, R.: Poor hypotensive response and tachyphylaxis following intravenous labetalol. Current Medical Research and Opinion 5: 424 (1978).

    Article  PubMed  CAS  Google Scholar 

  • Andersson, O.; Berglund, G. and Hansson, L.: Antihypertensive action, time of onset and effects on carbohydrate metabolism of labetalol. British Journal of Clinical Pharmacology 3 (Suppl.): 757 (1976).

    PubMed  CAS  Google Scholar 

  • Bailey, R.R.: Scalp tingling and difficulty in micturition in patients on labetalol. Lancet 2: 720 (1977).

    Article  PubMed  CAS  Google Scholar 

  • Barnett, A.J.; Kalowski, S. and Guest, C.: Labetalol compared with pindalol plus hydrallazine in the treatment of hypertension. Medical Journal of Australia 1: 105 (1978).

    PubMed  CAS  Google Scholar 

  • Blakeley, A.G.H. and Summers, R.J.: The effects of AH 5158 on the overflow of transmitter and the uptake of [3H]-(-)-noradrenaline in the cat spleen. British Journal of Pharmacology 56: 364P (1976).

    PubMed  CAS  Google Scholar 

  • Blakeley, A.G.H. and Summers, R.J.: The effects of labetalol (AH 5158) on adrenergic transmission in the cat spleen. British Journal of Pharmacology 59: 643 (1977).

    PubMed  CAS  Google Scholar 

  • Bolli, P.; Waal-Manning, H.J.; Wood, A.J. and Simpson, F.O.: Experience with labetalol in hypertension. British Journal of Clinical Pharmacology 3 (Suppl.): 765 (1976).

    PubMed  CAS  Google Scholar 

  • Bolli, P.; Waal-Manning, H.J.; Simpson, F.O. and Seeman, H.M.I.: Treatment of hypertension with labetalol, a new antihypertensive drug which combines α- and β-adrenoceptor blockade. New Zealand Medical Journal: in press (1978).

    Google Scholar 

  • Breckenridge, A.M.; Macnee, C.M.; Orme, M.L’E.; Richards, D.A. and Sterlin, M.J.: Rate of onset of hypotensive response with oral labetalol. British Journal of Clinical Pharmacology 4: 338P (1977a).

    Google Scholar 

  • Breckenridge, A.; Calvey, T.N.; Green, G.J.; Mclver, M.; Orme, M.L’E. and Serlin, M.J.: Labetalol in hypertension. Lancet 2: 36 (1977b).

    Article  PubMed  CAS  Google Scholar 

  • Briggs, R.S.J.; Birtwell, A.J. and Pohl, J.E.F.: Hypertensive response to labetalol in phaeochromocytoma. Lancet I: 1045 (1978).

    Google Scholar 

  • Brittain, R.T. and Levy, G.P.: A review of the animal pharmacology of labetalol, a combined α- and β- adrenoceptor blocking drug. British Journal of Clinical Pharmacology 3 (Suppl.): 681 (1976).

    PubMed  CAS  Google Scholar 

  • Brown, J.J.; Lever, A.F.; Cumming, A.M.M. and Robertson, J.I.S.: Labetalol in hypertension. Lancet 1: 1147 (1977).

    Article  Google Scholar 

  • Cambridge, D.; Davey, M.J. and Massingham, R.: Prazosin, a selective antagonist of post-synaptic a- adrenoceptors. British Journal of Pharmacology 59: 514P (1977).

    Google Scholar 

  • Collier, J.G.; Dawnay, N.A.H.; Nachev, C.H. and Robinson, B.F.: Clinical investigation of an antagonist at α- and β-adrenoceptors — AH 5158A. British Journal of Pharmacology 44: 286 (1972).

    PubMed  CAS  Google Scholar 

  • Craswell, P.; Williams, J. and de Voss, K.: Labetalol in chronic renal failure with hypertension. Australian and New Zealand Journal of Medicine 7: 441 (1977).

    Google Scholar 

  • Crofton, M. and Gabriel, R.: Pressor response after intravenous labetalol. British Medical Journal 2: 737 (1977).

    Article  PubMed  CAS  Google Scholar 

  • Dargie, H.J.; DoUery, C.T. and Daniel, J.: Labetalol in resistant hypertension. British Journal of Clinical Pharmacology 3 (Suppl.): 751 (1976).

    PubMed  CAS  Google Scholar 

  • Edwards, R.C. and Raftery, E.B.: Haemodynamic effects of long-term oral labetalol. British Journal of Clinical Pharmacology 3 (Suppl): 733 (1976).

    PubMed  CAS  Google Scholar 

  • Farmer, J.B.; Kennedy, I.; Levy, G.P. and Marshall, R.J.: Pharmacology of AH 5158; a drug which blocks both α- and β-adrenoceptors. British Journal of Pharmacology 45: 660 (1972).

    PubMed  CAS  Google Scholar 

  • Faulkner, J.K.; Stopher, D.A.; Waiden, R.; Singleton, W. and Taylor, W.: Pharmacokinetic and pharmacological studies with tolamolol in man. British Journal of Clinical Pharmacology 2: 423 (1975).

    PubMed  CAS  Google Scholar 

  • Frick, M.H. and Porsti, P.: Combined alpha- and beta-adrenoceptor blockade with labetalol in hypertension. British Medical Journal 1: 1046 (1976).

    Article  PubMed  CAS  Google Scholar 

  • Grange, R.W. and Jones, E.W.: Bullous lichen planus caused by labetalol. British Medical Journal 1:816 (1978).

    Article  Google Scholar 

  • Hansson, L. and Hanel, B.: Labetalol, a new α- and β-adrenoceptor blocking agent in hypertension. British Journal of Clinical Pharmacology 3 (Suppl.): 763 (1976a).

    PubMed  CAS  Google Scholar 

  • Hansson, L. and Hanel, B.: Antihypertensive effect of labetalol, a new alpha- and beta-adrenergic blocking agent. International Journal of Clinical Pharmacology 14: 195 (1976b).

    CAS  Google Scholar 

  • Harichaux, P. and Hary, L.: Some complementary data on AH 5158, an inhibitor of both α- and β- adrenoceptors. British Journal of Pharmacology 58: 412P (1976).

    Google Scholar 

  • Homeida, M.; Jackson, L. and Roberts, C.J.C.: Decreased first-pass metabolism of labetalol in chronic liver disease. Britsh Medical Journal 2: 1048 (1978).

    Article  CAS  Google Scholar 

  • Hopkins, R.; Martin, L.E. and Bland, R.: The metabolism of labetalol in animals and man. Biochemical Society Transactions 4: 726 (1976).

    PubMed  CAS  Google Scholar 

  • Hua, A.S.P.; Thomas, G.W. and Kincaid-Smith, P.: Scalp tingling in patients on labetalol. Lancet 2: 295 (1977).

    Article  PubMed  CAS  Google Scholar 

  • Jennings, K. and Parsons, V.: A study of labetalol in patients of European, West Indian and West African origin. British Journal of Clinical Pharmacology 3 (Suppl): 773 (1976).

    PubMed  CAS  Google Scholar 

  • Joekes, A.M. and Thompson, F.D.: Acute haemodynamic effects of labetalol and its subsequent use as an oral hypotensive agent. British Journal of Clinical Pharmacology 3 (Suppl): 789 (1976).

    PubMed  CAS  Google Scholar 

  • Johnson, B.F.; La Brooy, J. and Munro-Faure, A.D.: The anti-hypertensive efficacy of combined α- and β-adrenoceptor blockade with phentolamine-oxprenolol or with labetalol (AH 5158). Clinical Science and Molecular Medicine 51: 505s (1976a).

    Google Scholar 

  • Johnson, B.F.; La Brooy, J. and Munro-Faure, A.D.: Comparative anti-hypertensive effects of labetalol and the combination of Oxprenolol and phentolamine. British Journal of Clinical Pharmacology 3 (Suppl): 783 (1976b).

    PubMed  CAS  Google Scholar 

  • Kane, J.; Gregg, I. and Richards, D.A.: A double-blind trial of labetalol. British Journal of Clinical Pharmacology 3 (Suppl): 737 (1976).

    PubMed  CAS  Google Scholar 

  • Kennedy, I. and Levy, G.P.: Combined α- and β-adrenoceptor blocking drug AH 5158: Further studies on a-adrenoceptor blocking drug blockade in anaesthetised animals. British Journal of Pharmacology 53: 585 (1975).

    PubMed  CAS  Google Scholar 

  • Koch, G.: Haemodynamic effects of combined α- and β-adrenoceptor blockade after intravenous labetalol in hypertensive patients at rest and during exercise. British Journal of Clinical Pharmacology 3 (Suppl): 725 (1976a).

    PubMed  CAS  Google Scholar 

  • Koch, G.: Combined α- and β-adrenoceptor blockade with oral labetalol in hypertensive patients with reference to haemodynamic effects at rest and during exercise. British Journal of Clinical Pharmacology 3 (Suppl): 729 (1976b).

    PubMed  CAS  Google Scholar 

  • Koch, G.: Acute hemodynamic effects of an alpha- and beta-receptor blocking agent (AH 5158) on the systemic and pulmonary circulation at rest and during exercise in hypertensive patients. American Heart Journal 93: 585 (1977).

    Article  PubMed  CAS  Google Scholar 

  • Louis, W.J.; Brignell, M.J.; McNeil, J.J.; Christopher, N. and Vajda, F.J.E.: Labetalol in hypertension. Lancet 1: 452 (1978).

    Article  PubMed  CAS  Google Scholar 

  • Maconochie, J.G.; Richards, D.A. and Woodings, E.P.: Modification of pressor responses induced by ‘cold’. British Journal’of Clinical Pharmacology 4: 389P (1977a).

    CAS  Google Scholar 

  • Maconochie, J.G.; Woodings, E.P. and Richards, D.A.: Effects of labetalol and propranolol on histamine- induced bronchoconstriction in normal subjects. British Journal of Clinical Pharmacology 4: 157 (1977b).

    PubMed  CAS  Google Scholar 

  • MacCarthy, E.P.; Frost, G.W. and Stokes, G.S.: Labetalol in hypertensive emergencies: Medical Journal of Australia 1: 399 (1978).

    CAS  Google Scholar 

  • Martin, L.E.; Hopkins, R. and Bland, R.: Metabolism of labetalol by animals and man. British Journal of Clinical Pharmacology 3 (Suppl): 695 (1976).

    PubMed  CAS  Google Scholar 

  • Maxwell, G.M.: The effects of a new α- and β-adrenoceptor antagonist (AH 5158) upon the general and coronary haemodynamics of intact dogs. British Journal of Pharmacology 42: 370 (1973).

    Google Scholar 

  • Mehta, J. and Cohn, J.N.: Hemodynamic effects of labetalol, an alpha and beta adrenergic blocking agent, in hypertensive subjects. Circulation 55: 370 (1977).

    PubMed  CAS  Google Scholar 

  • Morgan, T.; Gillies, A.; Morgan. G. and Adam, W.: The effect of labetalol in the treatment of severe drug-resistant hypertension. Medical Journal of Australia 1: 393 (1978).

    PubMed  CAS  Google Scholar 

  • Pearson, R.M. and Havard, C.W.H.: Intravenous labetalol in hypertensive patients treated with ß- adrenoceptor blocking drugs. British Journal of Clinical Pharmacology 3 (Suppl): 795 (1976).

    PubMed  CAS  Google Scholar 

  • Pearson, R.M. and Havard, C.W.H.: Intravenous labetalol in hypertensive patients given by fast and slow injection. British Journal of Clinical Pharmacology 5: 401 (1978).

    PubMed  CAS  Google Scholar 

  • Poynter, D.; Martin, L.E.; Harrison, C. and Cook, J.: Affinity of labetalol for ocular melanin. British Journal of Clinical Pharmacology 3 (Suppl): 71 1 (1976).

    Google Scholar 

  • Prichard, B.N.C. and Boakes, A.J.: Labetalol in long-term treatment of hypertension. British Journal of Clinical Pharmacology 3 (Suppl): 743 (1976).

    PubMed  CAS  Google Scholar 

  • Prichard, B.N.C.; Thompson, P.O.; Boakes, A.J. and Joekes, A.M.: Some haemodynamic effects of compound AH 5158 compared with propranolol, propranolol plus hydrallazine, and diazoxide: the use of AH 5158 in the treatment of hypertension. Clinical Science and Molecular Medicine 48: 97s (1975).

    Google Scholar 

  • Pugsley, D.; Armstrong, B.; Nassim, M. and Beilin, L.J.: Combined α- and β-adrenoreceptor blockade in hypertension: a controlled trial of labetalol (AH 5158) compared with propranolol and placebo. Clinical Science and Molecular Medicine 51: 501s (1976a).

    Google Scholar 

  • Pugsley, D.J.; Armstrong, B.K.; Nassim, M.A. and Beilin, L.J.: Controlled comparison of labetalol and propranolol in the management of severe hypertension. British Journal of Clinical Pharmacology 3 (Suppl): 777 (1976b).

    PubMed  CAS  Google Scholar 

  • Regardh, C.-G.; Johnsson, G.; Jordo, L. and Solvell, L.: Comparative bioavailability and effect studies on metoprolol administered as ordinary and slow-release tablets in single and multiple doses. Acta Pharmacologica et Toxicologica 36 (Suppl. V): 45 (1975).

    CAS  Google Scholar 

  • Richards, D.A. and Prichard, B.N.C.: Concurrent antagonism of isoprenaline and noradrenaline after labetalol in man. Clinical Pharmacology and Therapeutics: 23: 253 (1978).

    PubMed  CAS  Google Scholar 

  • Richards, D.A.; Maconochie, J.G.; Bland, R.E.; Hopkins, R.; Woodings, E.P. and Martin, L.E.: Relationship between plasma concentrations and pharmacological effects of labetalol. European Journal of Clinical Pharmacology 11:85 (1977c).

    Article  PubMed  CAS  Google Scholar 

  • Richards, D.A.; Prichard, B.N.C.; Boakes, A.J.; Tuckman, J. and Knight E.J.: Pharmacological basis for antihypertensive effects of intravenous labetalol. British Heart Journal 39: 99 (1977b).

    Article  PubMed  CAS  Google Scholar 

  • Richards, D.A.; Tuckman, J. and Prichard, B.N.C.: Assessment of α- and β-adrenoceptor blocking actions of labetalol. British Journal of Clinical Pharmacology 3: 849 (1976a).

    PubMed  CAS  Google Scholar 

  • Richards, D.A.; Tuckman, J. and Prichard, B.N.C.: Combined α- and β-adrenoceptor blockade with labetalol at rest and during exercise. British Journal of Clinical Pharmacology 3: 967P (1976b).

    Google Scholar 

  • Richards, D.A.; Tuckman, J. and Prichard, B.N.C.: Assessment of the α- and β-adrenoceptor blocking properties of labetalol (AH 5158) after oral administration to normal volunteers. British Journal of Clinical Pharmacology 3: 343P (1976c).

    Google Scholar 

  • Richards, D.A.; Woodings, E.P. and Maconochie, J.G.: Comparison of the effects of labetalol and propranolol in healthy men at rest and during exercise. British Journal of Clinical Pharmacology 4: 15 (1977a).

    PubMed  CAS  Google Scholar 

  • Richards, D.A.; Woodings, E.P.; Stephens, M.D.B. and Maconochie, J.G.: The effects of oral AH 5158, a combined α- and β-adrenoceptor antagonist, in healthy volunteers. British Journal of Clinical Pharmacology 1: 505 (1974).

    CAS  Google Scholar 

  • Ronne-Rasmussen, J.O.; Andersen, G.S.; Bowal Jensen, N. and Andersson, E.: Acute effect of intravenous labetalol in the treatment of systemic arterial hypertension. British Journal of Clinical Pharmacology 3 (Suppl): 805 (1976).

    PubMed  CAS  Google Scholar 

  • Rosei, E.A.; Trust, P.M.; Brown, J.J.; Eraser, R.; Lever, A.F.; Morton, J.J. and Robertson, J.I.S.: Effects of intravenous labetalol on blood pressure, angiotensin II and aldosterone in hypertension: comparison with propranolol. Clinical Science and Molecular Medicine 51: 497s (1976a).

    Google Scholar 

  • Rosei, E.A.; Brown, J.J.; Eraser, R.; Lever, A.F.; Morton, J.J.; Robertson, J.I.S. and Trust, P.M: Labetalol (AH 5158), a competitive alpha- and beta-receptor blocking drug, in the management of hypertension. Australia and New Zealand Journal of Medicine 6 (Suppl. 3): 83 (1976b).

    Article  CAS  Google Scholar 

  • Rosei, E.A.; Brown, J.J.; Lever, A.E.; Robertson, A.S.; Robertson, J.I.S. and Trust, P.M: Treatment of phaeochromocytoma and of Clonidine withdrawal hypertension with labetalol. British Journal of Clinical Pharmacology 3 (Suppl): 809 (1976c).

    PubMed  CAS  Google Scholar 

  • Savage, R.L.; Lesna, M.; Mucklow, J.C. and Stevenson, C.J.: Cutaneous reactions to labetalol. British Medical Journal 1: 987 (1978).

    Article  Google Scholar 

  • Scott, D.B.; Buckley, F.P.; Drummond, G.B.; Litüewood, D.G. and Macrae, W.R.: Cardiovascular effects of labetalol during halothane anaesthesia. British Journal of Clinical Pharmacology 3 (Suppl): 817 (1976).

    PubMed  CAS  Google Scholar 

  • Scott, D.B.; Buckley, E.P.; Littlewood, D.G.; Macrae, W.R.; Arthur, G.R. and Drummond, G.B.: Circulatory effects of labetalol during halothane anaesthesia. Anaesthesia 33: 145 (1978).

    Article  PubMed  CAS  Google Scholar 

  • Scowen, E.: Scalp tingling on labetalol. Lancet 1: 98 (1978).

    Article  Google Scholar 

  • Skinner, C.; Gaddie, J. and Palmer, K.N.V.: Comparison of intravenous AH 5158 (ibidomide) and propranolol in asthma. British Medical Journal 2: 59 (1975).

    Article  PubMed  CAS  Google Scholar 

  • Thompson, E.D.; Joekes, A.M. and Hussein, M.M.: Labetalol used as a hypotensive agent in the presence of renal disease. Kidney International Journal 1 1: 287 (1977).

    Google Scholar 

  • Rosei, E.A.; Trust, P.M.; Brown, J.J.; Eraser, R.; Lever, A.F.; Morton, J.J. and Robertson, J.I.S.:: Effect on blood pressure, angiotensin II and aldosterone concentrations during treatment of severe hypertension with intravenous labetalol: comparison with propranolol. British Journal of Clinical Pharmacology 3 (Suppl): 799 (1976).

    PubMed  Google Scholar 

  • Weidman, P.; De Chatel, R.; Ziegler, W.H.; Flammer, J. and Reubi, E.: Alpha and beta adrenergic blockade with orally administered labetalol in hypertension. Studies on blood volume, plasma renin and aldosterone and catecholamine excretion. American Journal of Cardiology 41: 570 (1978).

    Article  Google Scholar 

  • Williams, J.G.; De Voss, K. and Craswell, P.W.; Labetalol in the treatment of hypertensive renal patients. Medical Journal of Australia 1: 225 (1978)

    PubMed  CAS  Google Scholar 

  • Wing, L.M.H.: Labetalol in hypertensive emergencies. Medical Journal of Australia I: 659 (1978).

    Google Scholar 

Download references

Authors

Editor information

R. N. Brogden

Rights and permissions

Reprints and permissions

Copyright information

© 1979 ADIS Press

About this chapter

Cite this chapter

Brogden, R.N., Heel, R.C., Speight, T.M., Avery, G.S. (1979). Labetalol: A Review of its Pharmacology and Therapeutic Use in Hypertension. In: Brogden, R.N. (eds) Antihypertensive Drugs Today. Cardiovascular Drugs, vol 4. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-7268-4_3

Download citation

  • DOI: https://doi.org/10.1007/978-94-011-7268-4_3

  • Publisher Name: Springer, Dordrecht

  • Print ISBN: 978-94-011-7270-7

  • Online ISBN: 978-94-011-7268-4

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics