Document Detail


Single dose pharmacokinetics of (S)-atenolol administered orally as a single enantiomer formulation and as a racemic mixture (Tenormin).
MedLine Citation:
PMID:  8024947     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The purpose of this study was to describe the pharmacokinetics of and heart rate and blood pressure responses to (S)-atenolol (SATN) and (R)-atenolol (RATN) after oral administration of (S)-atenolol and (R,S)-atenolol (Tenormin) in man. Eight male subjects were given single oral doses of 50 mg of SATN as a single enantiomer formulation (SEF) and 100 mg of Tenormin (TMN) using a randomized, double-blind, 2-period, complete crossover study design. Subjects performed exercise tolerance tests (Bruce Protocol) before and 2, 4, 6, 8, 12, and 24 h after drug administration. Plasma samples were obtained 2 min before and 30 min, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 16, and 24 h after dosing. Urine was collected for the first 48 h after dosing. Plasma and urine samples were analyzed for SATN and RATN by an enantioselective HPLC method. SEF and Tenormin attenuate exercise-induced increases in heart rate and systolic blood pressure. Mean changes in exercise heart rates 4 h after dosing were -38 +/- 3 bpm and -37 +/- 3 bpm for SEF and TMN, respectively, P = 0.792. Mean changes in exercise systolic blood pressure were -42 +/- 12 mm Hg and -55 +/- 14 mm Hg for SEF and TMN, respectively, P = 0.484. Mean area under the plasma level time curve (AUC0-24) and mean Cmax for SATN for SEF were significantly lower than for SATN after TMN.(ABSTRACT TRUNCATED AT 250 WORDS)
Authors:
W A Clementi; T Q Garvey; G D Clifton; R A McCoy; S Brandt; S Schwartz
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Publication Detail:
Type:  Clinical Trial; Comparative Study; Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Chirality     Volume:  6     ISSN:  0899-0042     ISO Abbreviation:  Chirality     Publication Date:  1994  
Date Detail:
Created Date:  1994-08-05     Completed Date:  1994-08-05     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  8914261     Medline TA:  Chirality     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  169-74     Citation Subset:  IM    
Affiliation:
Clementi & Associates Ltd., Radnor, Pennsylvania.
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MeSH Terms
Descriptor/Qualifier:
Administration, Oral
Atenolol / administration & dosage,  pharmacokinetics*,  pharmacology*
Biological Availability
Double-Blind Method
Heart Rate / drug effects*
Humans
Male
Metabolic Clearance Rate
Physical Exertion
Random Allocation
Stereoisomerism
Structure-Activity Relationship
Systole / drug effects*
Chemical
Reg. No./Substance:
29122-68-7/Atenolol

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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