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药品详细

Zolpidem(唑吡坦)

化学结构式图
中文名
唑吡坦
英文名
Zolpidem
分子式
C19H21N3O
化学名
N,N-dimethyl-2-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]acetamide
分子量
Average: 307.3895
Monoisotopic: 307.168462309
CAS号
82626-48-0
ATC分类
N05C 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Zolpidem is a prescription short-acting nonbenzodiazepine hypnotic that potentiates gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter, by binding to benzodiazepine receptors which are located on the gamma-aminobutyric acid receptors. Zolpidem is used for the short-term treatment of insomnia. It works quickly (usually within 15 minutes) and has a short half-life (2-3 hours). It is classified as an imidazopyridine. As an anticonvulsant and muscle relaxant, the beneficial effects start to emerge at 10 and 20 times the dose required for sedation, respectively. For that reason, it has never been approved for either muscle relaxation or seizure prevention. Recently, zolpidem has been cited in various medical reports mainly in the United Kingdom as waking persistent vegetative state (PVS) patients, and dramatically improving the conditions of people with brain injuries. [Wikipedia]

生产厂家
  • Apotex inc
  • Aurobindo pharma ltd
  • Biovail laboratories international srl
  • Caraco pharmaceutical laboratories ltd
  • Carlsbad technology inc
  • Dr reddys laboratories ltd
  • Genpharm inc
  • Hikma pharmaceuticals
  • Invagen pharmaceuticals inc
  • Lek pharmaceuticals dd
  • Meda pharmaceuticals
  • Mutual pharmacal co
  • Mylan pharmaceuticals inc
  • Novadel pharma inc
  • Pfizer Inc
  • Ranbaxy laboratories ltd
  • Roxane laboratories inc
  • Sanofi aventis us llc
  • Synthon pharmaceuticals ltd
  • Teva pharmaceuticals usa inc
  • Torrent pharmaceuticals ltd
  • Vintage pharmaceuticals llc
  • Watson laboratories inc
  • Wockhardt ltd
  • World gen llc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Lemmer B: The sleep-wake cycle and sleeping pills. Physiol Behav. 2007 Feb 28;90(2-3):285-93. Epub 2006 Oct 16. Pubmed
  2. Depoortere H, Zivkovic B, Lloyd KG, Sanger DJ, Perrault G, Langer SZ, Bartholini G: Zolpidem, a novel nonbenzodiazepine hypnotic. I. Neuropharmacological and behavioral effects. J Pharmacol Exp Ther. 1986 May;237(2):649-58. Pubmed
  3. Clauss RP, Guldenpfennig WM, Nel HW, Sathekge MM, Venkannagari RR: Extraordinary arousal from semi-comatose state on zolpidem. A case report. S Afr Med J. 2000 Jan;90(1):68-72. Pubmed
  4. Schlich D, L’Heritier C, Coquelin JP, Attali P, Kryrein HJ: Long-term treatment of insomnia with zolpidem: a multicentre general practitioner study of 107 patients. J Int Med Res. 1991 May-Jun;19(3):271-9. Pubmed
  5. Maarek L, Cramer P, Attali P, Coquelin JP, Morselli PL: The safety and efficacy of zolpidem in insomniac patients: a long-term open study in general practice. J Int Med Res. 1992 Apr;20(2):162-70. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Phenylpropenes
  • Imidazopyridines
Substructures
  • Amino Ketones
  • Phenylpropenes
  • Pyridines and Derivatives
  • Imidazopyridines
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Imidazoles
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Imines
  • Cyanamides
适应症
药理
Indication For the short-term treatment of insomnia.
Pharmacodynamics 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.
Absorption Zolpidem is rapidly absorbed from the GI tract.
Volume of distribution Not Available
Protein binding 92.5 ± 0.1% (independent of concentration between 40 and 790 ng/mL)
Metabolism
Zolpidem is converted to inactive metabolites in the liver.
Route of elimination Zolpidem tartrate tablets are converted to inactive metabolites that are eliminated primarily by renal excretion.
Half life 2.6 hours
Clearance Not Available
Toxicity Oral (male rat) LD50 = 695 mg/kg. Symptoms of overdose include impairment of consciousness ranging from somnolence to light coma.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 196 °C PhysProp
water solubility 23 mg/mL Not Available
logP 1.2 Not Available
pKa 6.2 MERCK INDEX (1996)
Predicted Properties
Property Value Source
water solubility 3.13e-02 g/l ALOGPS
logP 3.15 ALOGPS
logP 3.02 ChemAxon
logS -4 ALOGPS
pKa (strongest basic) 5.65 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 37.61 ChemAxon
rotatable bond count 3 ChemAxon
refractivity 93.58 ChemAxon
polarizability 35.06 ChemAxon
药物相互作用
Drug Interaction
Amprenavir Amprenavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if amprenavir is initiated, discontinued or dose changed.
Atazanavir Atazanavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if atazanavir is initiated, discontinued or dose changed.
Clarithromycin Clarithromycin, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if clarithromycin is initiated, discontinued or dose changed.
Conivaptan Conivaptan, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if conivaptan is initiated, discontinued or dose changed.
Darunavir Darunavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if darunavir is initiated, discontinued or dose changed.
Delavirdine Delavirdine, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if delavirdine is initiated, discontinued or dose changed.
Dihydrocodeine Enhanced CNS depressant effects contraindicates concurrent use for certain brand name formulations of zolpidem.
Fluconazole Fluconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if fluconazole is initiated, discontinued or dose changed.
Fosamprenavir Fosamprenavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if fosamprenavir is initiated, discontinued or dose changed.
Indinavir Indinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if indinavir is initiated, discontinued or dose changed.
Isoniazid Isoniazid, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if isoniazid is initiated, discontinued or dose changed.
Itraconazole Itraconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if itraconazole is initiated, discontinued or dose changed.
Ketoconazole Ketoconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if ketoconazole is initiated, discontinued or dose changed.
Lopinavir Lopinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if lopinavir is initiated, discontinued or dose changed.
Methotrimeprazine Additive CNS depressant effects. Reduce zolpidem dose by half upon initiation of methotrimeprazine. Zolpidem dose may be adjusted once methotrimeprazine dose has been established. Monitor for increased CNS depression.
Nefazodone Nefazodone, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if nefazodone is initiated, discontinued or dose changed.
Nelfinavir Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if nelfinavir is initiated, discontinued or dose changed.
Nicardipine Nicardipine, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if nicardipine is initiated, discontinued or dose changed.
Posaconazole Posaconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if posaconazole is initiated, discontinued or dose changed.
Quinidine Quinidine, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if quinidine is initiated, discontinued or dose changed.
Ritonavir Ritonavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if ritonavir is initiated, discontinued or dose changed.
Saquinavir Saquinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if saquinavir is initiated, discontinued or dose changed.
Telithromycin Telithromycin, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if telithromycin is initiated, discontinued or dose changed.
Triprolidine The CNS depressants, Triprolidine and Zolpidem, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if voriconazole is initiated, discontinued or dose changed.
食物相互作用
  • Avoid alcohol.
  • Should not be administered with or immediately after a meal.

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