Pharmacokinetics and oral bioavailability of scopolamine in normal subjects

The pharmacokinetics and bioavailability of scopolamine were evaluated in six healthy male subjects receiving 0.4 mg of the drug by either oral or intravenous administration. Plasma and urine samples were analyzed using a radioreceptor binding assay. After iv administration, scopolamine concentratio...

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Bibliographic Details
Published in:Pharmaceutical research 1989-06, Vol.6 (6), p.481-485
Main Authors: LAKSHMI PUTCHA, CINTRON, N. M, TSUI, J, VANDERPLOEG, J. M, KRAMER, W. G
Format: Article
Language:English
Subjects:
Administration, Oral
Adult
Biological and medical sciences
Biological Availability
Cholinergic system
Chromatography, Liquid
Half-Life
Humans
Injections, Intravenous
Male
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Scopolamine - administration & dosage
Scopolamine - pharmacokinetics
Space life sciences
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Summary:The pharmacokinetics and bioavailability of scopolamine were evaluated in six healthy male subjects receiving 0.4 mg of the drug by either oral or intravenous administration. Plasma and urine samples were analyzed using a radioreceptor binding assay. After iv administration, scopolamine concentrations in the plasma declined in a biexponential fashion, with a rapid distribution phase and a comparatively slow elimination phase. Mean and SE values for volume of distribution, systemic clearance, and renal clearance were 1.4 +/- 0.3 liters/kg, 65.3 +/- 5.2 liters/hr, and 4.2 +/- 1.4 liters/hr, respectively. Mean peak plasma concentrations were 2909.8 +/- 240.9 pg/ml following iv administration and 528.6 +/- 109.4 pg/ml following oral administration. Elimination half-life of the drug was 4.5 +/- 1.7 hr. Bioavailability of the oral dose was variable among subjects, ranging between 10.7 and 48.2%. The variability in absorption and poor bioavailability of oral scopolamine indicate that this route of administration may not be reliable and effective.
ISSN:0724-8741
1573-904X
DOI:10.1023/A:1015916423156