Tìm theo
Zolpidem
Các tên gọi khác (3) :
  • N,N,6-Trimethyl-2-(4-methylphenyl)imidazo(1,2-a)pyridine-3-acetamide
  • Zolpidem
  • Zolpidemum
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 82626-48-0
ATC: N05CF02
ĐG : Actavis Group , http://www.actavis.com
CTHH: C19H21N3O
PTK: 307.3895
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]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H21N3O
Phân tử khối
307.3895
Monoisotopic mass
307.168462309
InChI
InChI=1S/C19H21N3O/c1-13-5-8-15(9-6-13)19-16(11-18(23)21(3)4)22-12-14(2)7-10-17(22)20-19/h5-10,12H,11H2,1-4H3
InChI Key
InChIKey=ZAFYATHCZYHLPB-UHFFFAOYSA-N
IUPAC Name
N,N-dimethyl-2-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]acetamide
Traditional IUPAC Name
zolpidem
SMILES
CN(C)C(=O)CC1=C(N=C2C=CC(C)=CN12)C1=CC=C(C)C=C1
Độ tan chảy
196 °C
Độ hòa tan
23 mg/mL
logP
1.2
logS
-4
pKa (Strongest Basic)
5.65
PSA
37.61 Å2
Refractivity
93.58 m3·mol-1
Polarizability
35.06 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
6.2
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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] 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.
Dược Động Học :
▧ Absorption :
Zolpidem is rapidly absorbed from the GI tract.
▧ 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
Độc Tính : Oral (male rat) LD50 = 695 mg/kg. Symptoms of overdose include impairment of consciousness ranging from somnolence to light coma.
Chỉ Định : For the short-term treatment of insomnia.
Tương Tác Thuốc :
  • 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.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Sanofi Pasteur
    Sản phẩm biệt dược : Adormix
  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Ambien
  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Ambien CR
  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Bikalm
  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Dormizol
  • Công ty :
    Sản phẩm biệt dược : Edluar
  • Công ty : Zentiva
    Sản phẩm biệt dược : Hypnogen
  • Công ty : Purdue
    Sản phẩm biệt dược : Intermezzo
  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Ivadal
  • Công ty : Winthrop
    Sản phẩm biệt dược : Ivedal
  • Công ty : Polfarmex
    Sản phẩm biệt dược : Nasen
  • Công ty : Sandoz
    Sản phẩm biệt dược : Nimadorm
  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Nottem
  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Stilnoct
  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Stilnox
  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Stilnox CR
  • Công ty :
    Sản phẩm biệt dược : Zolpimist
  • Công ty : Krka
    Sản phẩm biệt dược : Zolsana
  • Công ty : Biofarm
    Sản phẩm biệt dược : Zoltis
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00425
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5732
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507949
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07219
ChemSpider
http://www.chemspider.com/Chemical-Structure.5530.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=26266
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/54868-0845-0
PharmGKB
http://www.pharmgkb.org/drug/PA451976
Wikipedia
http://en.wikipedia.org/wiki/Zolpidem
RxList
http://www.rxlist.com/cgi/generic/zolpid.htm
Drugs.com
http://www.drugs.com/zolpidem.html
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