Acute zolpidem administration produces pharmacodynamic
and receptor occupancy changes at similar doses

Fahey JM, Grassi JM, Reddi JM, Greenblatt DJ.
Department of Pharmacology and Experimental Therapeutics,
Tufts University School of Medicine and the Division of Clinical Pharmacology,
Tufts-New England Medical Center,
136 Harrison Avenue, Boston, MA 02111, USA.
Pharmacol Biochem Behav. 2006 Jan 23;


Zolpidem is chemically unrelated to classical benzodiazepines but has demonstrated relatively high affinity binding to the alpha(1) GABA(A) receptor. To assess pharmacodynamic and neurochemical effects of zolpidem, open-field behavior, pentylenetetrazole-induced seizure threshold and benzodiazepine receptor binding in vitro were evaluated in the same animal following a single dose of zolpidem. Zolpidem (2, 5 and 10 mg/kg), lorazepam (2 mg/kg) or vehicle was administered intraperitoneally in male CD-1 mice. Behavioral activity, assessed by three open-field parameters, was decreased following the two highest doses of zolpidem (5 and 10 mg/kg), and reached significance at the 10 mg/kg dose. Locomotor activity was also decreased significantly by lorazepam as expected. Pentylenetetrazole-induced seizure threshold was increased with the administration of 2 and 10 mg/kg zolpidem as well as with lorazepam. Apparent affinity (K(D)) of [(3)H]flunitrazepam, a non-selective ligand, for the benzodiazepine receptor in cortical membrane preparations was not significantly changed, while receptor number (B(max)) was decreased at all doses of zolpidem, reaching significance at the 10 mg/kg dose. These results confirm that the behavioral effects of zolpidem are similar to those of classical benzodiazepines. In addition, zolpidem had no significant effect on the affinity of the benzodiazepine receptor for [(3)H]flunitrazepam, but did decrease the density of receptor binding sites.
Dumb drugs
Sedative hypnotics
Sleeping-pill hype?
Zolpidem: structure
Zolpidem v zopiclone
Zolpidem v brotizolam
Eszopiclone (Lunesta)
Drugs to treat insomnia
Anxiolytics and antidepressants
Zolpidem (Ambien): prescribing information (PDF)

and further reading

Future Opioids
BLTC Research
Utopian Surgery?
The Abolitionist Project
The Hedonistic Imperative
The Reproductive Revolution
Critique of Huxley's Brave New World

The Good Drug Guide
The Good Drug Guide

The Responsible Parent's Guide
To Healthy Mood Boosters For All The Family