Skip to main content
PMC home page
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1981 Oct;12(4):549–559. doi: 10.1111/j.1365-2125.1981.tb01264.x

Cerebrospinal fluid concentrations of propranolol, pindolol and atenolol in man: evidence for central actions of beta-adrenoceptor antagonists.

E A Taylor, D Jefferson, J D Carroll, P Turner
PMCID: PMC1401910  PMID: 6117308

Abstract

1 Single and multiple oral dose studies of the penetration into CSF of three beta-adrenoceptor antagonists were performed in groups of patients needing lumbar puncture as part of their neurological investigation. Propranolol, pindolol and atenolol were chosen because of their differing physico-chemical properties. 2 The CSF concentration of propranolol (lipid-soluble) and pindolol (moderately lipid-soluble) was proportional to the free plasma concentration and was similar to, although generally lower than, that theoretically predicted. 3 The CSF concentrations of the poorly lipid-soluble atenolol were similar in different patients and were independent of plasma concentration. This may be due to the slow rate of diffusion of atenolol into CSF preventing the predicted concentrations being achieved.

Full text

PDF
551

Selected References

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

  1. Atsmon A., Blum I., Steiner M., Latz A., Wijsenbeek H. Further studies with propranolol in psychotic patients. Relation to initial psychiatric state, urinary catecholamines and 3-methoxy-4-hydroxyphenylglycol excretion. Psychopharmacologia. 1972;27(3):249–254. doi: 10.1007/BF00422805. [DOI] [PubMed] [Google Scholar]
  2. Barber H. E., Hawksworth G. M., Kitteringham N. R., Petersen J., Petrie J. C., Swann J. M. Protein binding of atenolol and propranolol to human serum albumin and in human plasma [proceedings]. Br J Clin Pharmacol. 1978 Nov;6(5):446P–447P. [PubMed] [Google Scholar]
  3. Bodin N. O., Borg K. O., Johansson R., Obianwu H., Svensson R. Absorption, distribution and excretion of alprenolol in man, dog and rat. Acta Pharmacol Toxicol (Copenh) 1974 Oct;35(4):261–269. doi: 10.1111/j.1600-0773.1974.tb00745.x. [DOI] [PubMed] [Google Scholar]
  4. Conway J., Greenwood D. T., Middlemiss D. N. Central nervous actions of beta-adrenoreceptor antagonists. Clin Sci Mol Med. 1978 Feb;54(2):119–124. doi: 10.1042/cs0540119. [DOI] [PubMed] [Google Scholar]
  5. Evans G. H., Shand D. G. Disposition of propranolol. VI. Independent variation in steady-state circulating drug concentrations and half-life as a result of plasma drug binding in man. Clin Pharmacol Ther. 1973 Jul-Aug;14(4):494–500. doi: 10.1002/cpt1973144part1494. [DOI] [PubMed] [Google Scholar]
  6. Fleminger R. Visual hallucinations and illusions with propranolol. Br Med J. 1978 May 6;1(6121):1182–1182. doi: 10.1136/bmj.1.6121.1182. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Hayes A., Cooper R. G. Studies on the absorption, distribution and excretion of propranolol in rat, dog and monkey. J Pharmacol Exp Ther. 1971 Feb;176(2):302–311. [PubMed] [Google Scholar]
  8. Henningsen N. C., Mattiasson I. Long-term clinical experience with atenolol--a new selective beta-1-blocker with few side-effects from the central nervous system. Acta Med Scand. 1979;205(1-2):61–66. doi: 10.1111/j.0954-6820.1979.tb06004.x. [DOI] [PubMed] [Google Scholar]
  9. Hinshelwood R. D. Hallucinations and propranolol. Br Med J. 1969 May 17;2(5654):445–445. doi: 10.1136/bmj.2.5654.445. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. Matakas F., Stechele S., Keller F. Microcirculation within the cerebral extracellular space. Adv Neurol. 1978;20:125–131. [PubMed] [Google Scholar]
  11. Matsen F. A., 3rd, West C. R. Supracortical fluid: a monitor of albumin exchange in normal and injured brain. Am J Physiol. 1972 Mar;222(3):532–539. doi: 10.1152/ajplegacy.1972.222.3.532. [DOI] [PubMed] [Google Scholar]
  12. Mucklow J. C., Bending M. R., Kahn G. C., Dollery C. T. Drug concentration in saliva. Clin Pharmacol Ther. 1978 Nov;24(5):563–570. doi: 10.1002/cpt1978245563. [DOI] [PubMed] [Google Scholar]
  13. Pacha W. L. A method for the fluorimetric determination of 4-(2-hydroxy-3-isopropylaminopropoxy)-indole (LB46), a beta-blocking agent, in plasma and urine. Experientia. 1969 Aug 15;25(8):802–803. doi: 10.1007/BF01897885. [DOI] [PubMed] [Google Scholar]
  14. Penniston J. T., Beckett L., Bentley D. L., Hansch C. Passive permeation of organic compounds through biological tissue: a non-steady-state theory. Mol Pharmacol. 1969 Jul;5(4):333–341. [PubMed] [Google Scholar]
  15. Scales B., Cosgrove M. B. The metabolism and distribution of the selective adrenergic beta blocking agent, practolol. J Pharmacol Exp Ther. 1970 Nov;175(2):338–347. [PubMed] [Google Scholar]
  16. Shand D. G., Nuckolls E. M., Oates J. A. Plasma propranolol levels in adults with observations in four children. Clin Pharmacol Ther. 1970 Jan-Feb;11(1):112–120. doi: 10.1002/cpt1970111112. [DOI] [PubMed] [Google Scholar]
  17. Shaw J., England J. D. Nightmares, asthma and pindolol. Med J Aust. 1977 Sep 3;2(2 Suppl):12–14. doi: 10.5694/j.1326-5377.1977.tb113908.x. [DOI] [PubMed] [Google Scholar]
  18. Sheppard G. P. High-dose propranolol in schizophrenia. Br J Psychiatry. 1979 May;134:470–476. doi: 10.1192/bjp.134.5.470. [DOI] [PubMed] [Google Scholar]
  19. Simpson W. T. Nature and incidence of unwanted effects with atenolol. Postgrad Med J. 1977;53 (Suppl 3):162–167. [PubMed] [Google Scholar]
  20. Yorkston N. J., Zaki S. A., Pitcher D. R., Gruzelier J. H., Hollander D., Sergeant H. G. Propranolol as an adjunct to the treatment of schizophrenia. Lancet. 1977 Sep 17;2(8038):575–578. doi: 10.1016/s0140-6736(77)91427-1. [DOI] [PubMed] [Google Scholar]

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

RESOURCES