Pharmacokinetics, pharmacology of atenolol and effect of renal disease.

Abstract

I The pharmacokinetics of intravenous and oral atenolol (50 mg) in six healthy volunteers was studied. Plasma, saliva and urine were collected up to 24 h after each dose.2 There was no significant difference in atenolol half-life when administered by the two routes. Bioavailability of the orally administered atenolol was 50%.3 Atenolol levels in saliva required about 2 h to reach equilibrium with plasma drug levels. 4 A comparison between the pharmacokinetics and pharmacology of atenolol was made in twelve healthy subjects.5 Dose-independent pharmacokinetics were observed. Reductions in resting heart rate and arterial blood pressure were proportional to either the logarithm of dose or area under the plasma concentration time curve or cumulative urinary atenolol excretion. 6 Plasma elimination half-life in five subjects with renal failure was prolonged.

Atenolol disposition in young and elderly subjects.

“…The half-life following the 10 mg intravenous dose was considerably shorter than that reported following a 50 mg i.v. dose (Mason et al, 1979;Wan et al, 1979) but very similar to that reported by another group using a 10 mg dose (FitzGerald et al, 1978). The elimination half-life following 50 mg intravenous and oral administration is the same (Mason et al, 1979).…”

Hydrophilic interaction liquid chromatographic tandem mass spectrometric determination of atenolol in human plasma

“…Many pharmacokinetic investigations have been carried out for atenolol during the past decades. In humans, the absorption of an oral dose (100-200 mg) of atenolol is rapid and consistent with approximately 50-60% absorbed from the gastrointestinal tract and peak plasma concentrations (1-2 µg/ mL) reached at 2-4 h (Leonetti et al, 1980;Kirch and Gorg, 1982;Wan et al, 1979;Wu et al, 2002Wu et al, , 2003 Sample preparation. Samples were thawed at room temperature and briefly vortex-mixed for 20 s at high speed using a standard multitube vortexer (VWR, West Chester, PA, USA).…”

Effect of Rifampicin on the Pharmacokinetics of Atenolol

“…Metabolism only plays a negligible role in its elimination, and over 90% of the absorbed atenolol dose can be found as unchanged drug in urine. The mean elimination half-life of atenolol is approximately 6 hr (Wan et al 1979).Also poorly metabolized compounds can be susceptible to pharmacokinetic drug-drug interactions. For instance, plasma concentrations of digoxin and celiprolol can be increased by concomitant itraconazole ingestion (Partanen et al 1996;Lilja et al 2003), and reduced by pretreatment with rifampicin (Greiner et al 1999;Lilja et al 2004).…”

“…Metabolism only plays a negligible role in its elimination, and over 90% of the absorbed atenolol dose can be found as unchanged drug in urine. The mean elimination half-life of atenolol is approximately 6 hr (Wan et al 1979).…”