Skip to main content
NCBI home page
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1993 Jun;35(6):623–628. doi: 10.1111/j.1365-2125.1993.tb04192.x

Effects of dilevalol (R,R-labetalol) compared with nifedipine on heart rate, blood pressure and muscle blood flow at rest and on exercise in hypertensive patients.

T Walley 1, Y Tsao 1, A Scott 1, E Mackay 1, M Vandenburg 1, A Breckenridge 1
PMCID: PMC1381606  PMID: 8329290

Abstract

1. Dilevalol (R,R-labetalol) is a non-selective beta-adrenoceptor antagonist with beta 2-adrenoceptor agonist activity. Its effects after 1 month's administration on heart rate, blood pressure and muscle blood flow were studied in a double-blind crossover comparison with nifedipine in 16 hypertensive patients. 2. Dilevalol and nifedipine were similarly effective in lowering systolic and diastolic blood pressure at rest, but dilevalol limited the rise in systolic blood pressure induced by exercise more than nifedipine (rise of 27 vs 53 mm Hg respectively, P < 0.01). 3. Dilevalol decreased resting heart rate compared with nifedipine (73 vs 92 beats min-1 respectively, P < 0.01). Dilevalol limited the exercise induced rise in heart rate more than nifedipine (36 vs 48 beats min-1 respectively, P < 0.01). 4. Muscle blood flow (measured by strain gauge plethysmography) was not affected by either dilevalol or nifedipine at rest. After exercise, dilevalol caused an increase in excess blood flow compared with placebo (10.8 vs 5.1 ml min-1 dl-1 respectively, P < 0.01). The difference between dilevalol and nifedipine did not reach statistical significance (10.8 vs 6.5 ml min-1 dl-1 respectively, P > 0.05). 5. On blood pressure and heart rate, dilevalol demonstrated beta-adrenoceptor blocker activity at rest and on exercise. On muscle blood flow, dilevalol appeared to have no effect at rest, but may have acted as a beta-adrenoceptor blocker rather than as a beta 2-adrenoceptor agonist during exercise.

Full text

PDF
623

Selected References

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

  1. Baba T., Murabayashi S., Aoyagi K., Ishizaki T. Effects of dilevalol, an R, R-isomer of labetalol, on blood pressure and renal function in patients with mild-to-moderate essential hypertension. Eur J Clin Pharmacol. 1988;35(1):9–15. doi: 10.1007/BF00555500. [DOI] [PubMed] [Google Scholar]
  2. Baum T., Watkins R. W., Sybertz E. J., Vemulapalli S., Pula K. K., Eynon E., Nelson S., Vliet G. V., Glennon J., Moran R. M. Antihypertensive and hemodynamic actions of SCH 19927, the R,R-isomer and labetalol. J Pharmacol Exp Ther. 1981 Aug;218(2):444–452. [PubMed] [Google Scholar]
  3. Bugni W. J., Ayers C. W., Ashby R., Bittle P. A., Ramirez G. Effects of dilevalol on rest and supine exercise hemodynamics in mild to moderate systemic hypertension. Am J Cardiol. 1989 Feb 15;63(7):452–456. doi: 10.1016/0002-9149(89)90318-4. [DOI] [PubMed] [Google Scholar]
  4. Chrisp P., Goa K. L. Dilevalol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in hypertension. Drugs. 1990 Feb;39(2):234–263. doi: 10.2165/00003495-199039020-00007. [DOI] [PubMed] [Google Scholar]
  5. Clark J. A., Zimmerman H. J., Tanner L. A. Labetalol hepatotoxicity. Ann Intern Med. 1990 Aug 1;113(3):210–213. doi: 10.7326/0003-4819-113-3-210. [DOI] [PubMed] [Google Scholar]
  6. Fujimura A., Ohashi K., Tsuru M., Ebihara A., Kondo K. Clinical pharmacology of dilevalol (II). The pharmacokinetic, pharmacodynamic, and tolerance studies of dilevalol during repeated administration in healthy subjects. J Clin Pharmacol. 1989 Jul;29(7):643–649. doi: 10.1002/j.1552-4604.1989.tb03393.x. [DOI] [PubMed] [Google Scholar]
  7. Glover D. R., Tarbit W. J. Overview of clinical trials of dilevalol in essential hypertension. J Hum Hypertens. 1990 Jun;4 (Suppl 2):49–53. [PubMed] [Google Scholar]
  8. Lennard M. S. Clinical pharmacology through the looking glass: reflections on the racemate vs enantiomer debate. Br J Clin Pharmacol. 1991 Jun;31(6):623–625. doi: 10.1111/j.1365-2125.1991.tb05583.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Lund-Johansen P. Hemodynamic effects of beta-blocking compounds possessing vasodilating activity: a review of labetalol, prizidilol, and dilevalol. J Cardiovasc Pharmacol. 1988;11 (Suppl 2):S12–S17. doi: 10.1097/00005344-198800000-00004. [DOI] [PubMed] [Google Scholar]
  10. Roberts D. H., Tsao Y., Breckenridge A. M. The reproducibility of limb blood flow measurements in human volunteers at rest and after exercise by using mercury-in-Silastic strain gauge plethysmography under standardized conditions. Clin Sci (Lond) 1986 Jun;70(6):635–638. doi: 10.1042/cs0700635. [DOI] [PubMed] [Google Scholar]
  11. Roberts D. H., Tsao Y., Grimmer S. F., Winstanley P. A., Orme M. L., Breckenridge A. M. Haemodynamic effects of atenolol, labetalol, pindolol and captopril: a comparison in hypertensive patients with special reference to changes in limb blood flow, heart rate and left ventricular function. Br J Clin Pharmacol. 1987 Aug;24(2):163–172. doi: 10.1111/j.1365-2125.1987.tb03157.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Schoenberger J. A., Frishman W. H., Wallin J. D., Gorwit J., Davidov M. E., Michelson E. L., Bedsole G. D., Cubbon J., Poland M. P. Dilevalol compared with propranolol and placebo for systemic hypertension. Am J Cardiol. 1989 Jun 5;63(19):45I–49I. doi: 10.1016/0002-9149(89)90128-8. [DOI] [PubMed] [Google Scholar]
  13. Silagy C. A., McNeil J. J., Farish S., McGrath B. P. A comparison of dilevalol and placebo in the management of isolated systolic hypertension using ambulatory monitoring. Br J Clin Pharmacol. 1990 Nov;30(5):657–664. doi: 10.1111/j.1365-2125.1990.tb03833.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Sybertz E. J., Sabin C. S., Pula K. K., Vliet G. V., Glennon J., Gold E. H., Baum T. Alpha and beta adrenoceptor blocking properties of labetalol and its R,R-isomer, SCH 19927. J Pharmacol Exp Ther. 1981 Aug;218(2):435–443. [PubMed] [Google Scholar]
  15. Waller D. G. Beta-adrenoceptor partial agonists: a renaissance in cardiovascular therapy? Br J Clin Pharmacol. 1990 Aug;30(2):157–171. doi: 10.1111/j.1365-2125.1990.tb03760.x. [DOI] [PMC free article] [PubMed] [Google Scholar]

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

RESOURCES