Skip to main content
NCBI home page
Postgraduate Medical Journal logoLink to Postgraduate Medical Journal
. 1991 Mar;67(785):252–255. doi: 10.1136/pgmj.67.785.252

Biochemical effects of urapidil on red cell membrane ion transport systems in a population of elderly essential hypertensives.

R Antonicelli 1, E Balducci 1, G Lipponi 1, C Lucantoni 1, R Gaetti 1, E Paciaroni 1
PMCID: PMC2399009  PMID: 2062772

Abstract

The aim of our work was to verify the effect of urapidil on membrane ion transport systems. This was a randomized, double-blind, cross-over study which evaluated the clinical and biochemical effects of urapidil (30 mg twice daily in comparison with placebo) in a group of 10 elderly hypertensive patients (3 male, 7 female ranging from 68 to 90 years, mean age 79.2 +/- 7.6 years). For the evaluation in fresh erythrocytes of principal ion transport systems (cotransport Na+/K+, countertransport Na+/Li+, Na+/K+ ATPase pump. intracellular Na+ and K+) we used the nystatin technique. We found that urapidil activated the red cell membrane ions cotransport system (basal values: 83.7 +/- 50.3 mumol Na+ RBC 1-1.h-1, after 1 month of urapidil therapy: 181.5 +/- 89.3 mumol Na+ RBC 1-1.h-1) (P less than 0.01), without significant changes in the other biochemical parameters evaluated. Our data suggest that one of the mechanisms of the urapidil antihypertensive effect could involve an increase in the membrane sodium cotransport system.

Full text

PDF
252

Selected References

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

  1. Adragna N. C., Canessa M. L., Solomon H., Slater E., Tosteson D. C. Red cell lithium-sodium countertransport and sodium-potassium cotransport in patients with essential hypertension. Hypertension. 1982 Nov-Dec;4(6):795–804. doi: 10.1161/01.hyp.4.6.795. [DOI] [PubMed] [Google Scholar]
  2. Bielen E., Fagard R., Staessen J., Lijnen P., Van Hoof R., Amery A. Urapidil-induced hemodynamic changes in humans. Am J Cardiol. 1989 Aug 15;64(7):16D–21D. doi: 10.1016/0002-9149(89)90690-5. [DOI] [PubMed] [Google Scholar]
  3. Blaustein M. P. Sodium ions, calcium ions, blood pressure regulation, and hypertension: a reassessment and a hypothesis. Am J Physiol. 1977 May;232(5):C165–C173. doi: 10.1152/ajpcell.1977.232.5.C165. [DOI] [PubMed] [Google Scholar]
  4. Bottorff M. B., Hoon T. J., Rodman J. H., Gerlach P. A., Ramanathan K. B. Pharmacokinetics and pharmacodynamics of urapidil in severe hypertension. J Clin Pharmacol. 1988 May;28(5):420–426. doi: 10.1002/j.1552-4604.1988.tb05753.x. [DOI] [PubMed] [Google Scholar]
  5. Canessa M., Brugnara C., Cusi D., Tosteson D. C. Modes of operation and variable stoichiometry of the furosemide- sensitive Na and K fluxes in human red cells. J Gen Physiol. 1986 Jan;87(1):113–142. doi: 10.1085/jgp.87.1.113. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Cubeddu L. X. New alpha 1-adrenergic receptor antagonists for the treatment of hypertension: role of vascular alpha receptors in the control of peripheral resistance. Am Heart J. 1988 Jul;116(1 Pt 1):133–162. doi: 10.1016/0002-8703(88)90261-x. [DOI] [PubMed] [Google Scholar]
  7. Garay R. P., Dagher G., Pernollet M. G., Devynck M. A., Meyer P. Inherited defect in a Na+, K-co-transport system in erythrocytes from essential hypertensive patients. Nature. 1980 Mar 20;284(5753):281–283. doi: 10.1038/284281a0. [DOI] [PubMed] [Google Scholar]
  8. Garay R., Rosati C., Meyer P. Na+ transport in primary hypertension. Ann N Y Acad Sci. 1986;488:187–195. doi: 10.1111/j.1749-6632.1986.tb46557.x. [DOI] [PubMed] [Google Scholar]
  9. Kirsten R., Nelson K., Neff J., Haerlin R., Steinijans V., Radtke H. W. Pharmacodynamics and pharmacokinetics of three different doses of urapidil infused in hypertensive patients. Eur J Clin Pharmacol. 1986;30(5):549–552. doi: 10.1007/BF00542413. [DOI] [PubMed] [Google Scholar]
  10. Langtry H. D., Mammen G. J., Sorkin E. M. Urapidil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in the treatment of hypertension. Drugs. 1989 Dec;38(6):900–940. doi: 10.2165/00003495-198938060-00005. [DOI] [PubMed] [Google Scholar]
  11. Leonetti G. Effects of alpha-adrenoceptor blockers on renal function and blood pressure adjustment in human hypertension. Drugs. 1988;35 (Suppl 6):53–59. doi: 10.2165/00003495-198800356-00007. [DOI] [PubMed] [Google Scholar]
  12. Postnov Y. V., Orlov S. N. Ion transport across plasma membrane in primary hypertension. Physiol Rev. 1985 Oct;65(4):904–945. doi: 10.1152/physrev.1985.65.4.904. [DOI] [PubMed] [Google Scholar]
  13. Rosendorff C. Urapidil in the treatment of hypertension. Drugs. 1988;35 (Suppl 6):188–192. doi: 10.2165/00003495-198800356-00025. [DOI] [PubMed] [Google Scholar]
  14. Saitta M. N., Hannaert P. A., Rosati C., Diaz A. S., Senn N., Garay R. P. [Na+, K+, Cl-]-cotransport function and dysfunction in different forms of primary hypertension. Am J Hypertens. 1988 Jul;1(3 Pt 3):60S–63S. doi: 10.1093/ajh/1.3.60s. [DOI] [PubMed] [Google Scholar]
  15. Shepherd A. M. Human pharmacology of urapidil. Drugs. 1988;35 (Suppl 6):34–39. doi: 10.2165/00003495-198800356-00005. [DOI] [PubMed] [Google Scholar]
  16. Trimarco B., Rosiello G., Feldhaus P., Steinijans V. W., Vecchione F., Cuocolo A., Lembo G., Volpe M. Efficacy of once-daily urapidil treatment in mild or moderate essential hypertension assessed by ambulatory 24-hour blood pressure monitoring. Drugs. 1988;35 (Suppl 6):173–181. doi: 10.2165/00003495-198800356-00023. [DOI] [PubMed] [Google Scholar]
  17. Weder A. B. Red-cell lithium-sodium countertransport and renal lithium clearance in hypertension. N Engl J Med. 1986 Jan 23;314(4):198–201. doi: 10.1056/NEJM198601233140402. [DOI] [PubMed] [Google Scholar]
  18. de Leeuw P. W., van Es P. N., de Bruyn H. A., Birkenhäger W. H. Renal haemodynamic and neurohumoral responses to urapidil in hypertensive man. Drugs. 1988;35 (Suppl 6):74–77. doi: 10.2165/00003495-198800356-00010. [DOI] [PubMed] [Google Scholar]
  19. van Zwieten P. A. Antihypertensive drugs interacting with alpha- and beta-adrenoceptors. A review of basic pharmacology. Drugs. 1988;35 (Suppl 6):6–19. doi: 10.2165/00003495-198800356-00003. [DOI] [PubMed] [Google Scholar]

Articles from Postgraduate Medical Journal are provided here courtesy of BMJ Publishing Group

RESOURCES