Cerebrospinal fluid and plasma disposition of yohimbine and 11-hydroxy-yohimbine in young and older healthy subjects, and Alzheimer's disease patients.
OBJECTIVE
The plasma and cerebrospinal fluid (CSF) disposition of yohimbine (YO) and 11-hydroxy-yohimbine (11-OH-YO), after oral administration of a single dose of YO (0.65 mg.kg-1) were studied in young and older healthy subjects and in patients with Alzheimer's disease (AD).


RESULTS
Plasma disposition of YO displayed large variability; no significant differences among subject groups were observed. In contrast, 11-OH-YO Cmax and AUC were significantly lower in the older normal subjects than in the young normal or AD subjects. A strong positive correlation between CSF and plasma YO concentrations was observed. A weak positive correlation between CSF and plasma concentrations of 11-OH-YO was also observed. CSF to plasma concentration ratios for yohimbine and 11-OH-YO were low (approximately 2%).
Le Corre
P A
PA
Laboratoire de Pharmacie Galénique, Université de Rennes I, France. Pascal.Le-Corre@univ-rennesl.fr
Peskind
E R
ER
Chevanne
F
F
Raskind
M A
MA
Le Verge
R
R
D058669:Adrenergic alpha-2 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists / Q000097:blood* / Q000134:cerebrospinal fluid* / Q000494:pharmacology; D000328:Adult; D000368:Aged; D000375:Aging / Q000097:blood* / Q000134:cerebrospinal fluid*; D000544:Alzheimer Disease / Q000097:blood* / Q000134:cerebrospinal fluid*; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D009638:Norepinephrine / Q000502:physiology; D018341:Receptors, Adrenergic, alpha-2 / Q000502:physiology; D012016:Reference Values; D015016:Yohimbine / Q000031:analogs & derivatives* / Q000097:blood* / Q000134:cerebrospinal fluid* / Q000494:pharmacology
D058669:Adrenergic alpha-2 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists; D018341:Receptors, Adrenergic, alpha-2; C081038:11-hydroxyyohimbine; D015016:Yohimbine; D009638:Norepinephrine