Cerebrospinal Fluid Concentrations of Propranolol, Pindolol and Atenolol in Man: Evidence for Central Actions of Beta-adrenoceptor Antagonists

Overview

Journal Br J Clin Pharmacol

Specialty Pharmacology

Date 1981 Oct 1

PMID 6117308

Citations 11

Authors

E A Taylor

D Jefferson

J D Carroll

P Turner

Affiliations

Soon will be listed here.

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.

Citing Articles

Effect of Propranolol on Motor Cortex Excitability in Essential Tremor: An Exploratory Study.

Miguel-Puga A, Villafuerte G, Trevino M, Ortega-Robles E, Arias-Carrion O Tremor Other Hyperkinet Mov (N Y). 2024; 14:1.

PMID: 38189055 PMC: 10768567. DOI: 10.5334/tohm.829.

Improving the prediction of the brain disposition for orally administered drugs using BDDCS.

Broccatelli F, Larregieu C, Cruciani G, Oprea T, Benet L Adv Drug Deliv Rev. 2012; 64(1):95-109.

PMID: 22261306 PMC: 3496430. DOI: 10.1016/j.addr.2011.12.008.

Psychiatric manifestations of Graves' hyperthyroidism: pathophysiology and treatment options.

Bunevicius R, Prange Jr A CNS Drugs. 2006; 20(11):897-909.

PMID: 17044727 DOI: 10.2165/00023210-200620110-00003.

Psychomotor performance and antihypertensive treatment.

Kalra L, Swift C, Jackson S Br J Clin Pharmacol. 1994; 37(2):165-72.

PMID: 8186062 PMC: 1364593. DOI: 10.1111/j.1365-2125.1994.tb04256.x.

Receptor occupancy in lumbar CSF as a measure of the antagonist activity of atenolol, metoprolol and propranolol in the CNS.

Kaila T, Marttila R Br J Clin Pharmacol. 1993; 35(5):507-15.

PMID: 8099803 PMC: 1381689. DOI: 10.1111/j.1365-2125.1993.tb04177.x.

References

Hinshelwood R . Hallucinations and propranolol. Br Med J. 1969; 2(5654):445. PMC: 1983350. DOI: 10.1136/bmj.2.5654.445. View

Sheppard G . High-dose propranolol in schizophrenia. Br J Psychiatry. 1979; 134:470-6. DOI: 10.1192/bjp.134.5.470. View

PACHA W . A method for the fluorimetric determination of 4-(2-hydroxy-3-isopropylaminopropoxy)-indole (LB46), a beta-blocking agent, in plasma and urine. Experientia. 1969; 25(8):802-3. DOI: 10.1007/BF01897885. View

SHAND D, Nuckolls E, OATES J . Plasma propranolol levels in adults with observations in four children. Clin Pharmacol Ther. 1970; 11(1):112-20. DOI: 10.1002/cpt1970111112. View

SCALES B, Cosgrove M . The metabolism and distribution of the selective adrenergic beta blocking agent, practolol. J Pharmacol Exp Ther. 1970; 175(2):338-47. View

Hayes A, Cooper R . Studies on the absorption, distribution and excretion of propranolol in rat, dog and monkey. J Pharmacol Exp Ther. 1971; 176(2):302-11. View

Matsen 3rd F, West C . Supracortical fluid: a monitor of albumin exchange in normal and injured brain. Am J Physiol. 1972; 222(3):532-9. DOI: 10.1152/ajplegacy.1972.222.3.532. View

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):249-54. DOI: 10.1007/BF00422805. View

Evans G, SHAND D . 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; 14(4):494-500. DOI: 10.1002/cpt1973144part1494. View

10.

BODIN N, Borg K, Johansson R, Obianwu H, Svensson R . Absorption, distribution and excretion of alprenolol in man, dog and rat. Acta Pharmacol Toxicol (Copenh). 1974; 35(4):261-9. DOI: 10.1111/j.1600-0773.1974.tb00745.x. View

11.

Yorkston N, Zaki S, Pitcher D, Gruzelier J, Hollander D, SERGEANT H . Propranolol as an adjunct to the treatment of schizophrenia. Lancet. 1977; 2(8038):575-8. DOI: 10.1016/s0140-6736(77)91427-1. View

12.

Shaw J, England J . Nightmares, asthma and pindolol. Med J Aust. 1977; 2(SP2):12-4. DOI: 10.5694/j.1326-5377.1977.tb113908.x. View

13.

SIMPSON W . Nature and incidence of unwanted effects with atenolol. Postgrad Med J. 1977; 53 Suppl 3:162-7. View

14.

Conway J, Greenwood D, Middlemiss D . Central nervous actions of beta-adrenoreceptor antagonists. Clin Sci Mol Med. 1978; 54(2):119-24. DOI: 10.1042/cs0540119. View

15.

Fleminger R . Visual hallucinations and illusions with propranolol. Br Med J. 1978; 1(6121):1182. PMC: 1604211. DOI: 10.1136/bmj.1.6121.1182. View

16.

MATAKAS F, Stechele S, Keller F . Microcirculation within the cerebral extracellular space. Adv Neurol. 1978; 20:125-31. View

17.

Mucklow J, Bending M, Kahn G, Dollery C . Drug concentration in saliva. Clin Pharmacol Ther. 1978; 24(5):563-70. DOI: 10.1002/cpt1978245563. View

18.

Barber H, Hawksworth G, Kitteringham N, Petersen J, Petrie J, Swann J . Protein binding of atenolol and propranolol to human serum albumin and in human plasma [proceedings]. Br J Clin Pharmacol. 1978; 6(5):446P-447P. View

19.

Henningsen N, 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):61-6. DOI: 10.1111/j.0954-6820.1979.tb06004.x. View

20.

Penniston J, Beckett L, Bentley D, HANSCH C . Passive permeation of organic compounds through biological tissue: a non-steady-state theory. Mol Pharmacol. 1969; 5(4):333-41. View