| Single dose pharmacokinetics of (S)-atenolol administered orally as a single enantiomer formulation and as a racemic mixture (Tenormin). | |
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MedLine Citation:
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PMID: 8024947 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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) |
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Authors:
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W A Clementi; T Q Garvey; G D Clifton; R A McCoy; S Brandt; S Schwartz |
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Publication Detail:
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Type: Clinical Trial; Comparative Study; Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Chirality Volume: 6 ISSN: 0899-0042 ISO Abbreviation: Chirality Publication Date: 1994 |
Date Detail:
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Created Date: 1994-08-05 Completed Date: 1994-08-05 Revised Date: 2008-11-21 |
Medline Journal Info:
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Nlm Unique ID: 8914261 Medline TA: Chirality Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 169-74 Citation Subset: IM |
Affiliation:
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Clementi & Associates Ltd., Radnor, Pennsylvania. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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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:
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29122-68-7/Atenolol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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