Tìm theo
Estazolam
Các tên gọi khác (2) :
  • 8-chloro-6-phenyl-4H-s-triazolo(4,3-a)(1,4)benzodiazepine
  • Estazolamum
Thuốc Gốc
Small Molecule
CAS: 29975-16-4
ATC: N05CD04
ĐG : Abbott Laboratories Ltd. , http://www.abbott.com
CTHH: C16H11ClN4
PTK: 294.738
A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H11ClN4
Phân tử khối
294.738
Monoisotopic mass
294.067224079
InChI
InChI=1S/C16H11ClN4/c17-12-6-7-14-13(8-12)16(11-4-2-1-3-5-11)18-9-15-20-19-10-21(14)15/h1-8,10H,9H2
InChI Key
InChIKey=CDCHDCWJMGXXRH-UHFFFAOYSA-N
IUPAC Name
12-chloro-9-phenyl-2,4,5,8-tetraazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,8,11,13-hexaene
Traditional IUPAC Name
estazolam
SMILES
ClC1=CC2=C(C=C1)N1C=NN=C1CN=C2C1=CC=CC=C1
Độ tan chảy
228-229
Độ hòa tan
Practically insoluble (1.5 mg/L)
logP
4.7
logS
-3.8
pKa (strongest acidic)
18.4
pKa (Strongest Basic)
4.97
PSA
43.07 Å2
Refractivity
94.44 m3·mol-1
Polarizability
29.83 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Estazolam, a triazolobenzodiazepine derivative, is an oral hypnotic agent with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam.
Cơ Chế Tác Dụng : A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam. [PubChem] Benzodiazepines bind nonspecifically to benzodiazepine receptors, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Dược Động Học :
▧ Absorption :
Tablets have been found to be equivalent in absorption to an orally administered solution of estazolam. In healthy subjects who received up to three times the recommended dose, peak estazolam plasma concentrations occurred within two hours after dosing (range 0.5 to 6.0 hours) and were proportional to the administered dose, suggesting linear pharmacokinetics over the dosage range tested.
▧ Protein binding :
93% protein bound, independant of concentration.
▧ Metabolism :
Extensively metabolized in the liver. In vitro studies with human liver microsomes indicate that the biotransformation of estazolam to the major circulating metabolite 4-hydroxy-estazolam is mediated by cytochrome P450 3A (CYP3A).
▧ Route of Elimination :
Estazolam is extensively metabolized. The elimination of the parent drug takes place via hepatic metabolism of estazolam to hydroxylated and other metabolites that are eliminated largely in the urine both free and conjugated. Less than 5% of a 2 mg dose of estazolam was excreted unchanged in the urine, with only 4% of the dose appearing in the feces. Radiolabel mass balance studies indicate that the main route of excretion is via the kidneys. After 5 days, 87% of the administered radioactivity was excreted in human urine. Less than 4% of the dose was excreted unchanged.
▧ Half Life :
The range of estimates for the mean elimination half-life of estazolam varies from 10 to 24 hours.
Độc Tính : Symptoms of overdose include confusion, depressed breathing, drowsiness and eventually coma, lack of coordination, and slurred speech.
Chỉ Định : For the short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings.
Tương Tác Thuốc :
  • Cimetidine Cimetidine may increase the effect of the benzodiazepine, estazolam.
  • Clozapine Increased risk of toxicity
  • Fluconazole Fluconazole may increase the effect of the benzodiazepine, estazolam.
  • Indinavir The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, estazolam.
  • Itraconazole Itraconazole may increase the effect of the benzodiazepine, estazolam.
  • Kava Kava may increase the effect of the benzodiazepine, estazolam.
  • Ketoconazole Ketoconazole may increase the effect of the benzodiazepine, estazolam.
  • Nelfinavir The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, estazolam.
  • Omeprazole Omeprazole may increase the effect of the benzodiazepine, estazolam.
  • Ritonavir The protease inhibitor, ritonavir, may increase the effect of the benzodiazepine, estazolam.
  • Saquinavir The protease inhibitor, saquinavir, may increase the effect of the benzodiazepine, estazolam.
  • Tipranavir Tipranavir may decrease the metabolism and clearance of Estazolam. Consider alternate therapy or monitor for Estazolam toxic effects if Tipranavir is initiated or dose increased.
  • Triprolidine The CNS depressants, Triprolidine and Estazolam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Voriconazole Voriconazole may increase the serum concentration of estazolam by decreasing its metabolism. Monitor for estazolam toxicity if voriconazole is initiated or dose increased.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Prosom 1 mg tablet
    Giá bán buôn : USD >1.53
    Đơn vị tính : tablet
  • Biệt dược thương mại : Prosom 2 mg tablet
    Giá bán buôn : USD >1.71
    Đơn vị tính : tablet
  • Biệt dược thương mại : Estazolam 1 mg tablet
    Giá bán buôn : USD >0.86
    Đơn vị tính : tablet
  • Biệt dược thương mại : Estazolam 2 mg tablet
    Giá bán buôn : USD >0.96
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty : Takeda
    Sản phẩm biệt dược : Esilgan
  • Công ty : Takeda
    Sản phẩm biệt dược : Eurodin
  • Công ty : Takeda
    Sản phẩm biệt dược : Nuctalon
  • Công ty :
    Sản phẩm biệt dược : ProSom
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01215
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3261
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507430
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00311
ChemSpider
http://www.chemspider.com/Chemical-Structure.3146.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50240450
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/49884-349-01
PharmGKB
http://www.pharmgkb.org/drug/PA449502
Wikipedia
http://en.wikipedia.org/wiki/Estazolam
RxList
http://www.rxlist.com/cgi/generic2/estaz.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/pro1359.shtml
Drugs.com
http://www.drugs.com/cdi/estazolam.html
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