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Antipyrine absorption and disposition in the elderly.
D J Greenblatt1, M K Divoll, J S Harmatz
1Department of Psychiatry, Tufts University School of Medicine, Boston, Mass.
Pharmacology
|January 1, 1988
Summary
Aging may affect antipyrine clearance in men, but absorption remains unimpaired. Elderly men showed prolonged elimination half-life and reduced clearance compared to young men, while women showed no significant differences.
Area of Science:
- Pharmacokinetics and Drug Metabolism
- Gerontology and Aging Research
Background:
- Age-related changes in drug metabolism and elimination can impact therapeutic efficacy and safety.
- Understanding how aging affects drug absorption and clearance is crucial for optimizing pharmacotherapy in older adults.
Purpose of the Study:
- To investigate the effects of age and gender on the pharmacokinetics of antipyrine.
- To assess age-related differences in antipyrine absorption following oral administration in fasting and fed states.
Main Methods:
- A single 1.0-gram dose of antipyrine was administered intravenously and orally (fasting and postprandial) to young (24-41 years) and elderly (62-77 years) volunteers.
- Plasma antipyrine concentrations were measured over 24 hours post-dose.
- Key pharmacokinetic parameters including elimination half-life, clearance, peak plasma concentration (Cmax), and time to peak concentration (Tmax) were determined.
Main Results:
- Elderly men exhibited a significantly prolonged elimination half-life (17 vs. 11 h) and reduced clearance (32 vs. 54 ml/min) compared to young men.
- No significant age-related differences in half-life or clearance were observed between elderly and young women.
- Oral administration of antipyrine, both fasting and postprandial, did not reveal significant age-related differences in Cmax, Tmax, or absolute bioavailability.
Conclusions:
- Aging may lead to reduced antipyrine clearance in men, suggesting potential age-related alterations in hepatic drug metabolism.
- There is no evidence of impaired gastrointestinal absorption rate or extent of antipyrine in the elderly.
- Gender-specific differences in age-related pharmacokinetic changes warrant further investigation.