Literature DB >> 6252915

Pharmacokinetics, beta-adrenoceptor blockade and anti-hypertensive action of labetalol during chronic oral treatment.

G L Sanders, D M Davies, M D Rawlins.   

Abstract

1 beta-Adrenoceptor blockade, plasma labetalol concentrations and anti-hypertensive actions were investigated at 2 hourly intervals during the interdose period of chronic oral therapy in six hypertensive patients. 2 beta-adrenoceptor blockade varied during the inter-dose period and was maximal 2 and 4 h after the oral dose (P < 0.05). 3 Systolic pressure rose during the interdose period (P < 0.05). A significant correlation was found between the degree of beta-adrenoceptor blockade and the change in systolic pressure at 2 h after the oral dose. 4 Efficacy of labetalol as a beta-adrenoceptor antagonist and anti-hypertensive drug was assessed 2 h after an oral dose during chronic eight hourly dosage in sixteen hypertensive patients. Pharmacokinetics of labetalol were studied in the same patients. 5 Peak plasma labetalol concentration occurred 2 h after the oral dose and subsequently the plasma concentration declined monoexponentially. 6 The steady state concentration (CSS) of labetalol was correlated significantly with the daily oral dose in mg kg-1, the mid point labetalol concentration (Cmax+Cmin) divided by 2 and the isoprenaline dose ratio-1 at 2 h after the oral dose. 7 No correlation was found between the antihypertensive effect and the CSS ng ml-1 labetalol or between the isoprenaline dose ratio-1 and the CSS labetalol ng ml-1.

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Year:  1980        PMID: 6252915      PMCID: PMC1430048          DOI: 10.1111/j.1365-2125.1980.tb01728.x

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


  14 in total

1.  Pharmacokinetics and pharmacodynamics of alprenolol in the treatment of hypertension. I. Relationship between plasma concentration and adrenergic beta-receptor blockade.

Authors:  P Collste; K Haglund; M Frisk-Holmberg; M D Rawlins
Journal:  Eur J Clin Pharmacol       Date:  1976-06-15       Impact factor: 2.953

2.  The metabolism of labetalol in animals and man.

Authors:  R Hopkins; L E Martin; R Bland
Journal:  Biochem Soc Trans       Date:  1976       Impact factor: 5.407

3.  Steady-state plasma concentrations of alprenolol in man.

Authors:  M D Rawlins; P Collste; M Frisk-Holmberg; M Lind; J Ostman; F Sjöqvist
Journal:  Eur J Clin Pharmacol       Date:  1974-08-23       Impact factor: 2.953

4.  A random-zero sphygmomanometer.

Authors:  B M Wright; C F Dore
Journal:  Lancet       Date:  1970-02-14       Impact factor: 79.321

5.  Intravenously administered isoproterenol sulfate dose-response curves in man.

Authors:  C F George; M E Conolly; T Fenyvesi; R Briant; C T Dollery
Journal:  Arch Intern Med       Date:  1972-09

6.  Relation of propranolol plasma level to beta-blockade during oral therapy.

Authors:  R Zacest; J Koch-Weser
Journal:  Pharmacology       Date:  1972       Impact factor: 2.547

7.  Plasma propranolol levels in adults with observations in four children.

Authors:  D G Shand; E M Nuckolls; J A Oates
Journal:  Clin Pharmacol Ther       Date:  1970 Jan-Feb       Impact factor: 6.875

8.  Propranolol serum levels during twenty-four hours.

Authors:  E Vervloet; B F Pluym; J Cilissen; K Köhlen; F W Merkus
Journal:  Clin Pharmacol Ther       Date:  1977-12       Impact factor: 6.875

9.  Blood levels of drug at the equilibrium state after multiple dosing.

Authors:  J G Wagner; J I Northam; C D Alway; O S Carpenter
Journal:  Nature       Date:  1965-09-18       Impact factor: 49.962

10.  Relationship between plasma concentrations and pharmacological effects of labetalol.

Authors:  D A Richards; J G Maconochie; R E Bland; R Hopkins; E P Woodings; L E Martin
Journal:  Eur J Clin Pharmacol       Date:  1977-01-03       Impact factor: 2.953

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