Tìm theo
Oxazepam
Các tên gọi khác (5 ) :
  • (+-)-Oxazepam
  • (RS)-Oxazepam
  • Oxazepam
  • Serax
  • Tazepam
Thuốc chống lo âu, hoảng sợ
Thuốc Gốc
Small Molecule
CAS: 604-75-1
ATC: N05BA04
ĐG : Actavis Group , http://www.actavis.com
CTHH: C15H11ClN2O2
PTK: 286.713
Oxazepam is an intermediate-acting benzodiazepine used to treat alcohol withdrawal and anxiety disorders. Oxazepam is also the metabolite of other benzodiazpines.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H11ClN2O2
Phân tử khối
286.713
Monoisotopic mass
286.050905313
InChI
InChI=1S/C15H11ClN2O2/c16-10-6-7-12-11(8-10)13(9-4-2-1-3-5-9)18-15(20)14(19)17-12/h1-8,15,20H,(H,17,19)
InChI Key
InChIKey=ADIMAYPTOBDMTL-UHFFFAOYSA-N
IUPAC Name
7-chloro-3-hydroxy-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
Traditional IUPAC Name
oxazepam
SMILES
OC1N=C(C2=CC=CC=C2)C2=C(NC1=O)C=CC(Cl)=C2
Độ tan chảy
205-206 °C
Độ hòa tan
179 mg/L
logP
2.24
logS
-3.5
pKa (strongest acidic)
10.61
pKa (Strongest Basic)
-1.5
PSA
61.69 Å2
Refractivity
77.89 m3·mol-1
Polarizability
28.38 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Oxazepam is believed to stimulate GABA receptors in the ascending reticular activating system. Since GABA is inhibitory, receptor stimulation increases inhibition and blocks both cortical and limbic arousal following stimulation of the brain stem reticular formation.
Cơ Chế Tác Dụng : Oxazepam is an intermediate-acting benzodiazepine used to treat alcohol withdrawal and anxiety disorders. Oxazepam is also the metabolite of other benzodiazpines. Similar to other benzodiazepines, oxazepam exerts its anxiolytic effects by potentiating the effect of gamma-aminobutyric acid (GABA) on GABA-A receptors through a cooperative mechanism of action. GABA receptors are ionotropic chloride-linked channel receptors that produce inhibitory postsynaptic potentials. When activated by GABA, the GABA receptor/chloride ionophore complex undergoes a conformational change that allows the passage of chloride ions through the channel. Benzodiazepines are believed to exert their effect by increasing the effect of GABA at its receptor. Benzodiazepine binding increases chloride conductance in the presence of GABA by increasing the frequency at which the channel opens. In contrast, barbiturates increase chloride conductance in the presence of GABA by prolonging the time in which the channel remains open. There are 18 subtypes of the GABA receptor subunits. The α2 subunit of the α2β3γ2 receptor complex is thought to mediate anxiolytic effects while the α1 subunit of the α1β2γ2 receptor complex is thought to mediate sedative, anticonvulsant and anterograde amnesia effects.
Dược Động Học :
▧ Absorption :
Well absorbed from the gastrointestinal tract following oral administration however is absorbed at a slower rate compared to other benzodiazepines like diazepam or flurazepam. Time to peak concentration = 2-4 hours. Onset of action is slow, > 3 hours, following oral administration.
▧ Protein binding :
80-99%
▧ Metabolism :
No active metabolites. It is hepatically metabolized and undergoes glucuronidation. The glucuronidation of the S-isomer is catalyzed by UGT2B15. The glucuronidation of the R-isomer is catalyzed by UGT2B7 and UGT1A9.
▧ Route of Elimination :
This product has a single, major inactive metabolite in man, a glucuronide excreted in the urine.
▧ Half Life :
Mean elimination half-life - 8.2 hours (range of 5.7 to 10.9 hours)
Độc Tính : Symptoms of overdose include confusion, drowsiness, and lethargy.
Chỉ Định : For the treatment of anxiety disorders and alcohol withdrawal.
Tương Tác Thuốc :
  • Clozapine Increased risk of toxicity
  • Kava Kava may increase the effect of the benzodiazepine, oxazepam.
  • Triprolidine The CNS depressants, Triprolidine and Oxazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Capsule - Oral - 10 mg, 15 mg, 30 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Adumbran
  • Công ty :
    Sản phẩm biệt dược : Alepam
  • Công ty :
    Sản phẩm biệt dược : Alopam
  • Công ty :
    Sản phẩm biệt dược : Anxiolit
  • Công ty :
    Sản phẩm biệt dược : Durazepam
  • Công ty :
    Sản phẩm biệt dược : Limbial
  • Công ty :
    Sản phẩm biệt dược : Medopam
  • Công ty :
    Sản phẩm biệt dược : Murelax
  • Công ty :
    Sản phẩm biệt dược : Noripam
  • Công ty :
    Sản phẩm biệt dược : Opamox
  • Công ty :
    Sản phẩm biệt dược : Ox-Pam
  • Công ty :
    Sản phẩm biệt dược : Oxascand
  • Công ty :
    Sản phẩm biệt dược : Praxiten
  • Công ty :
    Sản phẩm biệt dược : Purata
  • Sản phẩm biệt dược : Serax
  • Công ty :
    Sản phẩm biệt dược : Serenal
  • Công ty :
    Sản phẩm biệt dược : Serenid
  • Công ty :
    Sản phẩm biệt dược : Serepax
  • Công ty :
    Sản phẩm biệt dược : Seresta
  • Công ty :
    Sản phẩm biệt dược : Serpax
  • Công ty :
    Sản phẩm biệt dược : Sobril
  • Công ty :
    Sản phẩm biệt dược : Tazepam
  • Công ty :
    Sản phẩm biệt dược : Vaben
  • Công ty :
    Sản phẩm biệt dược : Zaxpam
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00842
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4616
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506031
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07359
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00464
ChemSpider
http://www.chemspider.com/Chemical-Structure.4455.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0228-2067-10
PharmGKB
http://www.pharmgkb.org/drug/PA450731
Wikipedia
http://en.wikipedia.org/wiki/Oxazepam
RxList
http://www.rxlist.com/cgi/generic3/oxazepam.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/oxa1400.shtml
Drugs.com
http://www.drugs.com/cdi/oxazepam.html
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