Zolpidem drug data and news

Zolpidem drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Zolpidem
Brand Names/Synonyms Ambien; CHEMBANK1625; Dea No. 2783; Ivadal; Lorex; Niotal; Stilnoct; Stilnox; Zolpidem; Zolpidem Tartrate; Zolpidemum [Latin]
Indication Indicated in the treatment of insomnia.
Sponsored links
Description Not Available
Pharmacology Zolpidem is a sedative or hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties. It interacts with a GABA-BZ receptor complex and shares some of the pharmacological properties of the benzodiazepines. In contrast to the benzodiazepines, which non-selectively bind to and activate all three alpha receptor subtypes, zolpidem in vitro binds the (alpha1) receptor preferentially. The (alpha1) receptor is found primarily on the Lamina IV of the sensorimotor cortical regions, substantia nigra (pars reticulata), cerebellum molecular layer, olfactory bulb, ventral thalamic complex, pons, inferior colliculus, and globus pallidus.
Mechanism Of Action Zolpidem modulates the alpha-subunit, known as the benzodiazepine receptor, within the GABAA receptor chloride channel macromolecular complex. Unlike the benzodiazepines, which non-selectively interact with all three alpha-receptor subtypes, Zolpidem preferentially binds to the alpha-1 receptor.
Zolpidem News
(When available)

Neurocrine Shares Dumped As FDA Sets Back Indiplon  17 May 2006
The insomnia space is led by immediate- and extended-release versions of Ambien (zolpidem), a blockbuster product from Paris-based Sanofi-Aventis Group. ... - BioWorld Online (subscription),

sanofi-aventis reiterates safety of zolpidem tartrate CIV as ...  Apr 19, 2006
2006 APR 19 - (NewsRx.com) -- sanofi-aventis (SNY) reports that Ambien (zolpidem tartrate) CIV, when taken as directed, provides a safe and effective treatment ... - Therapeutics Daily (subscription) (press release),

There's more to falling asleep than just counting sheep  May 15, 2006
RECENT news stories about the troubles of a well-known congressman mentioned the sleep disorder drug Ambien (zolpidem tartrate). ... - Inside Bay Area,

Snooze alarm: The pill that drove us to sleep  May 6, 2006
WASHINGTON - Zolpidem tartrate, the sedative-hypnotic better known to wide-awake, stressed-out sheet kickers as Ambien, is an efficacious little helper if you ... - Standard-Speaker,

Patrick Kennedy's Psychedelic Freak Out!  May 5, 2006
...opoids. But the reason for my post is to explain what happens to me when I mix phenergan with Ambien or Sonata (zolpidem or zaleplon). ... - Yahoo! News

ReGen Therapeutics Plc - Issue of Equity  May 12, 2006
Executive Chairman Percy Lomax commented, 'The capital raised will be used to fund the proposed Phase IIa trials of zolpidem and development of Colostrinin(TM ... - PharmaLive.com (press release),

Kennedy crashes car into DC traffic barrier  May 4, 2006
...vision, or dry mouth. Zolpidem, the generic name for Ambien, is used to treat sleep problems, according to the Web site. It may help ... - Providence Journal (subscription),

The Pill That Drove Us to Sleep  May 5, 2006
Zolpidem tartrate, the sedative-hypnotic better known to wide-awake, stressed-out sheet kickers as Ambien, is an efficacious little helper if you ever thought ... - Washington Post,

Zentiva NV 1st Quarter Results 2006  May 2, 2006
Out of our key promoted brands good sales growth was achieved by the hypnotic drug Hypnogen (zolpidem), the anti-hypertensive product Lozap (losartan) and the ... - PharmaLive.com (press release),

No More Counting Sheep  May 3, 2006
...are Somnatrol, Dormías and RevitaSleep. Ambien and Lunesta both use a sedative/hypnotic drug called Zolpidem. It helps you fall ... - University Daily Kansan,

Ambien User Paints During Sleep; Kennedy Use of Ambien Might Have ...  May 6, 2006
...events. New York, NY (PRWEB) May 6, 2006 -- Sanofi-Aventis, is the maker of the sleep drug Ambien (trade name for zolpidem). Many ... - PR Web (press release),

Sepracor Announces First Quarter 2006 Results  Apr 25, 2006
Among study participants, the most commonly used previoustherapies were AMBIEN(R) brand zolpidem tartrate, other prescriptioninsomnia medications, and trazodone ... - Finanzen.net,

Sepracor Announces First Quarter 2006 Results  Apr 25, 2006
Among study participants, the most commonly used previous therapies were AMBIEN(R) brand zolpidem tartrate, other prescription insomnia medications, and ... - Genetic Engineering News,

New weapons in travelers' round-the-clock jet-lag fight  Apr 21, 2006
..."Ambien (zolpidem tartrate) gets you seven or eight hours of sleep," she says. "Lunesta (eszopiclone) provides seven or eight hours. ... - Los Angeles Times,

Neurocrine Biosciences Reports First Quarter 2006 Results  Apr 24, 2006
...of affinity and selectivity for alpha 1 containing GABA-A receptors compared to the currently marketed non-benzodiazepine sleep agents zolpidem (Ambien(R ... - PR Newswire (press release),

Dosage Forms Not Available
Drug_Category Hypnotics and Sedatives; ATC:N05CF02
Absorption Zolpidem is rapidly absorbed from the GI tract.
Interactions -->Interactions for Zolpidem:

CNS-Active Drugs

Zolpidem tartrate was evaluated in healthy volunteers in single-dose interaction studies for several CNS drugs. A study involving haloperidol and zolpidem revealed no effect of haloperidol on the pharmacokinetics or pharmacodynamics of zolpidem. Imipramine in combination with zolpidem produced no pharmacokinetic interaction other a 20% decrease in peak levels of imipramine, but there was an additive effect of decreased alertness. Similarly, chlorpromazine in combination with zolpidem produced no pharmacokinetic interaction, but there was an additive effect of decreased alertness and psychomotor performance. The lack of a drug interaction following single-dose administration does not predict a lack following chronic administration.

An additive effect on psychomotor performance between alcohol and zolpidem was demonstrated.

A single-dose interaction study with zolpidem 10 mg and fluoxetine 20 mg at steady-state levels in male volunteers did not demonstrate any clinically significant pharmacokinetic or pharmacodynamic interactions. When multiple doses of zolpidem and fluoxetine at steady-state concentrations were evaluated in healthy females, the only significant change was a 17% increase in the zolpidem half-life. There was no evidence of an additive effect in psychomotor performance.

Following five consecutive nightly doses of zolpidem 10 mg in the presence of sertraline 50 mg (17 consecutive daily doses, at 7:00 am, in healthy female volunteers), zolpidem C max was significantly higher (43%) and T max was significantly decreased (53%). Pharmacokinetics of sertraline and N-desmethylsertraline were unaffected by zolpidem.

Since the systemic evaluation of zolpidem tartrate in combination with other CNS-active drugs have been limited, careful consideration should be given to the pharmacology of any CNS-active drug to be used with zolpidem. Any drug with CNS-depressant effects could potentially enhance the CNS- depressant effects of zolpidem.

Drugs that affect drug metabolism via cytochrome P450: A randomized, double-blind, crossover interaction study in ten healthy volunteers between itraconazole (200 mg once daily for 4 days) and a single dose of zolpidem (10 mg) given 5 hours after the last dose of itraconazole resulted in a 34% increase in AUC0->∞ of zolpidem. There were no significant pharmacodynamic effects of zolpidem on subjective drowsiness, postural sway, or psychomotor performance.

A randomized, placebo-controlled, crossover interaction study in eight healthy female volunteers between 5 consecutive daily doses of rifampin (600 mg) and a single dose of zolpidem (20 mg) given 17 hours after the last dose of rifampin showed significant reductions of the AUC (ñ73%), Cmax (ñ58%), and T1/2 (ñ36%) of zolpidem together with significant reductions in the pharmacodynamic effects of zolpidem.

Other Drugs

A study involving cimetidine/zolpidem and ranitidine/zolpidem combinations revealed no effect of either drug on the pharmacokinetics or pharmacodynamics of zolpidem. Zolpidem had no effect on digoxin kinetics and did not effect prothrombin time when given with warfarin in normal subjects. Zolpidem's sedative/hypnotic effect was reversed by flumazenil; however, no significant alterations in zolpidem pharmacokinetics were found.

Toxicity Oral (Male Rat) LD50 = 695 mg/kg
Organisms Affected Humans and other mammals
Chemical IUPAC Name N,N-dimethyl-2-[4-methyl-8-(4-methylphenyl)-6,9-diazabicyclo[4.3.0]nona-2,4,7,9-tetraen-7-yl]-ethanamide
Chemical Formula C19H21N3O
Molecular Weight 307.39 g/mol
Smiles String CC1=CC=C(C=C1)C2=C(N3C=C(C=CC3=N2)C)CC(=O)N(C)C
Melting Point 196 °C
Water Solubility 23 mg/ml
State Solid
LogP/Hphobicity 1.879
Isoelectric Point 6.2
Biotransformation Zolpidem tartrate is converted to inactive metabolites in the liver.
Half Life 2.6 hours
Protein Binding [%] 92%
RxList Link RXlist
Sponsored links
Drug Reference http://www.drugs.com/cons/Zolpidem.html
http://www.rxlist.com/cgi/generic/zolpid.htm
Drug Type Approved Drug
Accession No APRD00095
CAS Registry Number 82626-48-0
KEGG Compound ID C07219
PubChem ID SID:199579
PharmGKB ID PA451976
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available

Home | About | Cancers | Treatment | Medications
Copyright onconews.org 2005.
All Rights Reserved.
Google
 
Web onconews.org