Skip to main content
PMC home page
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1982;13(Suppl 1):41S–47S. doi: 10.1111/j.1365-2125.1982.tb01888.x

Comparison of labetalol with other anti-hypertensive drugs

B N C Prichard, D A Richards
PMCID: PMC1401845  PMID: 6124265

Abstract

1 The anti-hypertensive effects of labetalol have been compared and contrasted with other groups of anti-hypertensive drugs in this review of the published literature.

2 The data show that the pharmacological and haemodynamic profile of labetalol in man is distinctly different from that of other specific anti-hypertensive agents; namely the properties of competitive α- and β-adrenoceptor blockade leading to haemodynamic effects of reduced blood pressure and peripheral vascular resistance with little accompanying changes in resting heart rate or cardiac output.

3 The anti-hypertensive effects of labetalol are dose related. In fixed dose comparative studies equivalent anti-hypertensive effects to those of labetalol have been shown for individual drugs of the β-adrenoceptor-blocking and diuretic groups. In dose titration studies, equivalent anti-hypertensive effects at given doses of labetalol have been demonstrated for drugs of the following types: β-adrenoceptor blockers, β-blockers plus diuretics, methyldopa, adrenergic neurone blockers and the combination of β-blockers plus a peripheral vasodilator.

4 Comparing side-effect liabilities, it is clear that quantitatively labetalol produces no greater burden of side-effects than drugs of the β-adrenoceptor-blocking group. Qualitative differences, however, do exist; in particular, symptomatic postural hypotension is dose related and is more likely to occur when excessive doses (> 2 g daily) are used.

Full text

PDF
41S

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Andersson O., Berglund G., Hansson L. Anti-hypertensive action, time of onset and effects on carbohydrate metabolism of labetalol. Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):757–761. [PubMed] [Google Scholar]
  2. Bahlmann J., Brod J., Hubrich W., Cachovan M., Pretschner P. Effect of an alpha- and beta-adrenoceptor-blocking agent (labetalol) on haemodynamics in hypertension. Br J Clin Pharmacol. 1979;8(Suppl 2):113S–117S. [PMC free article] [PubMed] [Google Scholar]
  3. Barnett A. J., Kalowski S., Guest C. Labetalol compared with prindolol plus hydraliazine in the treatment of hypertension: a double-blind cross-over study. Med J Aust. 1978 Jan 28;1(2):105–109. [PubMed] [Google Scholar]
  4. Beilin L. J., Juel-Jensen B. E. Alpha and beta adrenergic blockade in hypertension. Lancet. 1972 May 6;1(7758):979–982. doi: 10.1016/s0140-6736(72)91154-3. [DOI] [PubMed] [Google Scholar]
  5. Boakes A. J., Prichard B. N. The effect of AH 5158, pindolol, propranolol, D-propranolol on acute exercise tolerance in angina pectoris. Br J Pharmacol. 1973 Mar;47(3):673P–674P. [PMC free article] [PubMed] [Google Scholar]
  6. Bolli P., Waal-Manning J., Wood A. J., Simpson F. O. Experience with labetalol in hypertension. Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):765–771. [PubMed] [Google Scholar]
  7. Cumming A. M., Brown J. J., Lever A. F., Mackay A., Robertson J. I. Treatment of severe hypertension by repeated bolus injections of labetalol. Br J Clin Pharmacol. 1979;8(Suppl 2):199S–204S. [PMC free article] [PubMed] [Google Scholar]
  8. Cumming A. M., Davies D. L. Intravenous labetalol in hypertensive emergency. Lancet. 1979 Apr 28;1(8122):929–930. doi: 10.1016/s0140-6736(79)91413-2. [DOI] [PubMed] [Google Scholar]
  9. Dargie H. J., Dollery C. T., Daniel J. Labetalol in resistant hypertension. Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):751–755. [PubMed] [Google Scholar]
  10. Dawson A., Johnson B. F., Smith I. K., Munro-Faure A. D. A comparison of the effects of labetalol, bendrofluazide and their combination in hypertension. Br J Clin Pharmacol. 1979 Aug;8(2):149–154. doi: 10.1111/j.1365-2125.1979.tb05813.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Dent R., Kellaway G. S. A pilot trial of labetalol (AH 5158A): a combined alpha and beta blocker in treatment of hypertension. N Z Med J. 1977 Sep 14;86(595):213–215. [PubMed] [Google Scholar]
  12. Drew G. M. Modulation of noradrenergic transmission by the presynaptic alpha-inhibitory feedback process in the rat heart [proceedings]. Br J Pharmacol. 1978 Mar;62(3):381P–382P. [PMC free article] [PubMed] [Google Scholar]
  13. Edwards R. C., Raftery E. B. Haemodynamic effects of long-term oral labetalol. Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):733–736. [PubMed] [Google Scholar]
  14. Ghose R. R., Sampson A. Rapid onset of action of oral labetalol in severe hypertension. Curr Med Res Opin. 1977;5(2):147–151. doi: 10.1185/03007997709110155. [DOI] [PubMed] [Google Scholar]
  15. Hansson L., Hänel B. Labetalol, a new alpha- and beta-adrenoreceptor blocking agent, in hypertension. Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):763–764. [PubMed] [Google Scholar]
  16. Horvath J. S., Caterson R. J., Collett P., Duggin G. G., Kelly D. H., Tiller D. J. Labetalol and bendrofluazide: comparison of their antihypertensive effects. Med J Aust. 1979 Jun 30;1(13):626–628. doi: 10.5694/j.1326-5377.1979.tb119425.x. [DOI] [PubMed] [Google Scholar]
  17. Hunyor S. N., Bauer G. E., Ross M., Larkin H. Labetalol and propranolol in mild hypertensives: comparison of blood pressure and plasma volume effects. Aust N Z J Med. 1980 Apr;10(2):162–166. doi: 10.1111/j.1445-5994.1980.tb03705.x. [DOI] [PubMed] [Google Scholar]
  18. Kane J., Gregg I., Richards D. A. Double-blind trial of labetalol. Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):737–741. [PubMed] [Google Scholar]
  19. Koch G. Cardiovascular dynamics after acute and long-term alpha- and beta-adrenoceptor blockade at rest, supine and standing, and during exercise. Br J Clin Pharmacol. 1979;8(Suppl 2):101S–105S. [PMC free article] [PubMed] [Google Scholar]
  20. Koch G. Combined alpha- and beta-adrenoreceptors blockade with oral labetalol in hypertensive patients with reference to haemodynamic effects at rest and during exercise. Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):729–732. [PubMed] [Google Scholar]
  21. Labetalol in hypertension. Lancet. 1977 May 28;1(8022):1147–1148. [PubMed] [Google Scholar]
  22. Lamming G. D., Broughton Pipkin F., Symonds E. M. Comparison of the alpha and beta blocking drug, labetalol, and methyl dopa in the treatment of moderate and severe pregnancy-induced hypertension. Clin Exp Hypertens. 1980;2(5):865–895. doi: 10.3109/10641968009037147. [DOI] [PubMed] [Google Scholar]
  23. Lehtonen A., Allonen H., Kleimola T. Antihypertensive effect and plasma levels of labetalol. A comparison with propranolol and dihydrallazine. Int J Clin Pharmacol Biopharm. 1979 Feb;17(2):71–75. [PubMed] [Google Scholar]
  24. Lund-Johansen P. Comparative haemodynamic effects of labetalol, timolol, prazosin and the combination of tolamolol and prazosin. Br J Clin Pharmacol. 1979;8(Suppl 2):107S–111S. [PMC free article] [PubMed] [Google Scholar]
  25. Marx P. G., Reid D. S. Labetalol infusion in acute myocardial infarction with systemic hypertension. Br J Clin Pharmacol. 1979;8(Suppl 2):233S–238S. [PMC free article] [PubMed] [Google Scholar]
  26. McGrath B. P., Matthews P. G., Walter N. M., Maydom B. W., Johnston C. I. Emergency treatment of severe hypertension with intravenous labetalol. Med J Aust. 1978 Oct 21;2(9):410–411. doi: 10.5694/j.1326-5377.1978.tb76817.x. [DOI] [PubMed] [Google Scholar]
  27. McNeil J. J., Louis W. J. A double-blind crossover comparison of pindolol, metoprolol, atenolol and labetalol in mild to moderate hypertension. Br J Clin Pharmacol. 1979;8(Suppl 2):163S–166S. [PMC free article] [PubMed] [Google Scholar]
  28. Mehta J., Cohn J. N. Hemodynamic effects of labetalol, an alpha and beta adrenergic blocking agent, in hypertensive subjects. Circulation. 1977 Feb;55(2):370–375. doi: 10.1161/01.cir.55.2.370. [DOI] [PubMed] [Google Scholar]
  29. Pearson R. M., Griffith D. N., Woollard M., James I. M., Havard C. W. Comparison of effects on cerebral blood flow of rapid reduction in systemic arterial pressure by diazoxide and labetalol in hypertensive patients: preliminary findings. Br J Clin Pharmacol. 1979;8(Suppl 2):195S–198S. [PMC free article] [PubMed] [Google Scholar]
  30. Pearson R. M., Havard C. W. Intravenous labetalol in hypertensive patients given by fast and slow injection. Br J Clin Pharmacol. 1978 May;5(5):401–405. doi: 10.1111/j.1365-2125.1978.tb01645.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  31. Prichard B. N., Boakes A. J., Hernández R. Long-term treatment of hypertension with labetalol. Br J Clin Pharmacol. 1979;8(Suppl 2):171S–177S. [PMC free article] [PubMed] [Google Scholar]
  32. Prichard B. N., Johnston A. W., Hill I. D., Rosenheim M. L. Bethanidine, Guanethidine, and Methyldopa in Treatment of Hypertension: a Within-patient Comparison. Br Med J. 1968 Jan 20;1(5585):135–144. doi: 10.1136/bmj.1.5585.135. [DOI] [PMC free article] [PubMed] [Google Scholar]
  33. Prichard B. N., Owens C. W. Mechanism of the antihypertensive action of beta-adrenergic blocking drugs. Cardiology. 1980;66 (Suppl 1):1–11. doi: 10.1159/000172983. [DOI] [PubMed] [Google Scholar]
  34. Prichard B. N., Thompson F. O., Boakes A. J., 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. Clin Sci Mol Med Suppl. 1975 Jun;2:97s–100s. doi: 10.1042/cs048097s. [DOI] [PubMed] [Google Scholar]
  35. Pugsley D. J., Armstrong B. K., Nassim M. A., Beilin L. J. Controlled comparison of labetalol and propranolol in the management of severe hypertension. Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):777–782. [PubMed] [Google Scholar]
  36. Pugsley D. J., Nassim M., Armstrong B. K., Beilin L. A controlled trial of labetalol (Trandate), propranolol and placebo in the management of mild to moderate hypertension. Br J Clin Pharmacol. 1979 Jan;7(1):63–68. doi: 10.1111/j.1365-2125.1979.tb00898.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  37. Pugsley D., Armstrong B., Nassim M., Beilin L. J. Combined alpha- and beta-adrenoreceptor blockade in hypertension: a controlled trial of labetalol (AH 5158) compared with propranolol and placebo. Clin Sci Mol Med Suppl. 1976 Dec;3:501s–503s. doi: 10.1042/cs051501s. [DOI] [PubMed] [Google Scholar]
  38. Richards D. A., Prichard B. N. Clinical pharmacology of labetalol. Br J Clin Pharmacol. 1979;8(Suppl 2):89S–93S. [PMC free article] [PubMed] [Google Scholar]
  39. Richards D. A., Prichard B. N., Hernández R. Circulatory effects of noradrenaline and adrenaline before and after labetalol. Br J Clin Pharmacol. 1979 Apr;7(4):371–378. [PMC free article] [PubMed] [Google Scholar]
  40. Romo M., Halttunen P., Saarinen P., Sarna S. Labetalol and pindolol in the treatment of hypertension: a comparative study. Ann Clin Res. 1979 Dec;11(6):249–252. [PubMed] [Google Scholar]
  41. Rosei E. A., Brown J. J., Lever A. F., Robertson A. S., Robertson J. I., Trust P. M. Treatment of phaeochromocytoma and of clonidine withdrawal hypertension with labetalol. Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):809–815. [PubMed] [Google Scholar]
  42. Sanders G. L., Davies D. M., Gales G. M., Rao J. G., Rawlins M. D., Routledge P. A. A comparative study of methyldopa and labetalol in the treatment of hypertension. Br J Clin Pharmacol. 1979;8(Suppl 2):149S–151S. [PMC free article] [PubMed] [Google Scholar]
  43. Serlin M. J., Orme M. C., Maciver M., Green G. J., Macnee C. M., Breckenridge A. M. Rate of onset of hypotensive effect of oral labetalol. Br J Clin Pharmacol. 1979 Feb;7(2):165–168. doi: 10.1111/j.1365-2125.1979.tb00916.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  44. Thibonnier M., Lardoux M. D., Corvol P. Comparative trial of labetalol and acebutolol, alone or associated with dihydralazine, in treatment of essential hypertension. Br J Clin Pharmacol. 1980 Jun;9(6):561–567. doi: 10.1111/j.1365-2125.1980.tb01081.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  45. Trust P. M., Rosei E. A., Brown J. J., Fraser R., Lever A. F., Morton J. J., Robertson J. I. Effect of blood pressure angiotensin II and aldosterone concentrations during treatment of severe hypertension with intravenous labetalol: comparison with propranolol. Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):799–803. [PubMed] [Google Scholar]
  46. West M. J., Wing L. M., Mulligan J., Walkley J., Grygiel J. J., Graham J. R., Chalmers J. P. Comparison of labetalol, hydrallazine, and propranolol in the therapy of moderate hypertension. Med J Aust. 1980 Mar 8;1(5):224–225. [PubMed] [Google Scholar]

Articles from British Journal of Clinical Pharmacology are provided here courtesy of British Pharmacological Society

RESOURCES