Lack of effect of ageing on the stereochemical disposition of propranolol. 1992

H H Zhou, and E Whelan, and A J Wood
Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-6602.

The elderly are more resistant to the effects of propranolol than the young. To determine whether the decreased sensitivity in the elderly could be due to stereoselective alteration in propranolol metabolism, we investigated the effect of age on the oral clearance of (-)- and (+)-propranolol. Six young (aged 24-32, mean 27.3 +/- 1.3 years) and six elderly (65-80, mean 71.3 +/- 2.7 years) white male volunteers were given a single 80 mg oral dose of racemic propranolol. The mean peak plasma concentrations of both (+)- and (-)-propranolol were significantly higher (P less than 0.05) in the elderly (105.7 +/- 19.7 and 165.0 +/- 29.7 nmol l-1) compared with the young subjects (68.6 +/- 10.1 and 115.7 +/- 18.1 nmol l-1). The oral clearances of both (+)- and (-)-propranolol were significantly higher (P less than 0.05) in the young (6933 +/- 598 and 4554 +/- 372 ml min-1) than in the elderly (4548 +/- 712 and 2941 +/- 473 ml min-1). Age had no effect on the relative concentration of the two isomers. Thus, the ratio of (+)-propranolol to (-)-propranolol was 0.67 +/- 0.05 in the young compared with 0.65 +/- 0.02 in the elderly.

UI MeSH Term Description Entries
D008102 Liver Circulation The circulation of BLOOD through the LIVER. Hepatic Circulation,Circulation, Liver,Circulation, Hepatic
D008297 Male Males
D008657 Metabolic Clearance Rate Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site. Total Body Clearance Rate,Clearance Rate, Metabolic,Clearance Rates, Metabolic,Metabolic Clearance Rates,Rate, Metabolic Clearance,Rates, Metabolic Clearance
D011433 Propranolol A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs. Dexpropranolol,AY-20694,Anaprilin,Anapriline,Avlocardyl,Betadren,Dociton,Inderal,Obsidan,Obzidan,Propanolol,Propranolol Hydrochloride,Rexigen,AY 20694,AY20694,Hydrochloride, Propranolol
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D000368 Aged A person 65 years of age or older. For a person older than 79 years, AGED, 80 AND OVER is available. Elderly
D000375 Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time. Senescence,Aging, Biological,Biological Aging
D013237 Stereoisomerism The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed) Molecular Stereochemistry,Stereoisomers,Stereochemistry, Molecular,Stereoisomer

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