Influence of age, frailty and liver function on the pharmacokinetics of brofaromine

The pharmacokinetics of brofaromine, a selective inhibitor of monoamine oxidase A, was evaluated in 12 frail elderly patients (66-92 y) and 12 healthy volunteers (20-35 y). Quantitative liver function tests were performed to show whether brofaromine elimination in the elderly could be predicted from...

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Bibliographic Details
Published in:European journal of clinical pharmacology 1996, Vol.49 (5), p.387-391
Main Authors: ZEEH, J, FUCHS, L, BERGMANN, W, ANTONIN, K.-H, DEGEL, F, BIECK, P, PLATT, D
Format: Article
Language:English
Subjects:
Administration, Oral
Adult
Aged
Aged, 80 and over
Aging - metabolism
Aging - pathology
Biological and medical sciences
Caffeine - blood
Chromatography, Gas
Cross-Over Studies
Cytochrome P-450 CYP1A2 - metabolism
Female
Frail Elderly
Half-Life
Humans
Liver Function Tests
Male
Medical sciences
Monoamine Oxidase Inhibitors - administration & dosage
Monoamine Oxidase Inhibitors - blood
Monoamine Oxidase Inhibitors - pharmacokinetics
Neuropharmacology
Pharmacology. Drug treatments
Piperidines - administration & dosage
Piperidines - blood
Piperidines - pharmacokinetics
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Regression Analysis
Sorbitol - blood
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Summary:The pharmacokinetics of brofaromine, a selective inhibitor of monoamine oxidase A, was evaluated in 12 frail elderly patients (66-92 y) and 12 healthy volunteers (20-35 y). Quantitative liver function tests were performed to show whether brofaromine elimination in the elderly could be predicted from noninvasive assessment of CYP1A2 activity (caffeine clearance) or liver plasma flow (sorbitol clearance). In the elderly the AUC of brofaromine was significantly increased (e.g. for the 75 mg dose 43.2 vs 19.9 mumol*h.l-1, clearance was reduced (5.0 vs. 11.8 l.h-1), the volume of distribution was smaller (130 vs. 230 l), and the half-life was slightly increased (19.0 vs. 14.2 h). No significant correlation was observed between hepatic plasma flow and brofaromine clearance (r = 0.41, P = 0.05), whereas CYP1A2 activity and brofaromine clearance were tightly correlated (r = 0.94, P < 0.0001). Caffeine clearance, a simple, noninvasive test of CYP1A2 activity, is predictive of brofaromine clearance.
ISSN:0031-6970
1432-1041
DOI:10.1007/BF00203783