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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.
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| 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 sanofi-aventis reiterates safety of zolpidem tartrate CIV as ... Apr 19, 2006 There's more to falling asleep than just counting sheep May 15, 2006 Snooze alarm: The pill that drove us to sleep May 6, 2006 Patrick Kennedy's Psychedelic Freak Out! May 5, 2006 ReGen Therapeutics Plc - Issue of Equity May 12, 2006 Kennedy crashes car into DC traffic barrier May 4, 2006 The Pill That Drove Us to Sleep May 5, 2006 Zentiva NV 1st Quarter Results 2006 May 2, 2006 No More Counting Sheep May 3, 2006 Ambien User Paints During Sleep; Kennedy Use of Ambien Might Have ... May 6, 2006 Sepracor Announces First Quarter 2006 Results Apr 25, 2006 Sepracor Announces First Quarter 2006 Results Apr 25, 2006 New weapons in travelers' round-the-clock jet-lag fight Apr 21, 2006 Neurocrine Biosciences Reports First Quarter 2006 Results Apr 24, 2006 | ||
| 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 |
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