Tìm theo
Cloxazolam
Các tên gọi khác (3) :
  • Cloxazolazepam
  • MT 14-411
  • Sepazon
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 24166-13-0
ATC: N05BA22
CTHH: C17H14Cl2N2O2
PTK: 349.211
Cloxazolam is a benzodiazepine with anxiolytic, sedative/hypnotic, muscle relaxant, and antiepileptic effects. [3] It is marketed in the Argentina, Australia, Portugal, Belgium, Switzerland, Luxembourg, Germany, Taiwan and Japan -- mainly for anti-anxiety. The usual dose of cloxazolam in adults is 3-12mg/day for anti-anxiety. [3] Although less commonly noted, it has also been reported as clinically effective in the treatment of depression, schizophrenia, and neurosis. [4] As well, it has also been studied in Japan in doses of 15-30mg/day as an adjunct in the treatment of intractable epilepsy, for which it has demonstrated effectiveness. [3]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H14Cl2N2O2
Phân tử khối
349.211
Monoisotopic mass
348.043233116
InChI
InChI=1S/C17H14Cl2N2O2/c18-11-5-6-15-13(9-11)17(12-3-1-2-4-14(12)19)21(7-8-23-17)10-16(22)20-15/h1-6,9H,7-8,10H2,(H,20,22)
InChI Key
InChIKey=ZIXNZOBDFKSQTC-UHFFFAOYSA-N
IUPAC Name
13-chloro-2-(2-chlorophenyl)-3-oxa-6,9-diazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),11,13-trien-8-one
Traditional IUPAC Name
cloxazolam
SMILES
ClC1=CC2=C(NC(=O)CN3CCOC23C2=CC=CC=C2Cl)C=C1
Độ tan chảy
202-204
Độ hòa tan
2.66e-02 g/l
logP
4.13
logS
-4.1
pKa (strongest acidic)
12.69
pKa (Strongest Basic)
2.6
PSA
41.57 Å2
Refractivity
91.05 m3·mol-1
Polarizability
33.62 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Studies have shown a superiority of 4mg/day of cloxazepam to 12mg/day of bromazepam in terms of anxiety, depressed mood, and sleep; an insignificant difference in terms of sedative effect; and less muscle relaxant effects. [3] Cloxazolam, administered as a single oral dose of 3mg, when compared to a single 5 mg dose of diazepam in one study, showed similar subjective measures; however, there cloxazolam caused more fatigue, and less mood improvement. Cloxazolam also induced a significant increase in heart rate in the control group of this study. [3]
Cơ Chế Tác Dụng : Cloxazolam is a benzodiazepine with anxiolytic, sedative/hypnotic, muscle relaxant, and antiepileptic effects. [3] It is marketed in the Argentina, Australia, Portugal, Belgium, Switzerland, Luxembourg, Germany, Taiwan and Japan -- mainly for anti-anxiety. The usual dose of cloxazolam in adults is 3-12mg/day for anti-anxiety. [3] Although less commonly noted, it has also been reported as clinically effective in the treatment of depression, schizophrenia, and neurosis. [4] As well, it has also been studied in Japan in doses of 15-30mg/day as an adjunct in the treatment of intractable epilepsy, for which it has demonstrated effectiveness. [3] Cloxazolam is a long acting benzodiazepine. It acts as a prodrug, with pharmacologically active metabolites, which bind to to the GABAa receptor, which other benzodiazepines bind to, to illicit a physiological response. [wiki]
Dược Động Học :

▧ Metabolism :
Cloxazolam is metabolised by the liver into the active metabolite chlordesmethyldiazepam (delorazepam). [5]
▧ Route of Elimination :
Renal elimination.
▧ Half Life :
65 hours
Độc Tính : Drowsiness and ataxia are dose related. Central nervous system toxicity may result in respiratory depression and loss of consciousness. As such, pre-existing central nervous system depression and severe hepatic impairment are two particular contraindications for use.
Chỉ Định : Used primarily as an anti-anxiety agent. Typically used short term, and may be given as a single dose of up to 100mcg/kg to reduce anxiety and tension experienced prior to surgery.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Nycomed
    Sản phẩm biệt dược : Akton
  • Công ty : Jaba Recordati
    Sản phẩm biệt dược : Cloxam
  • Sản phẩm biệt dược : Clozal
  • Công ty : Farmasa
    Sản phẩm biệt dược : Elum
  • Công ty : Novartis
    Sản phẩm biệt dược : Olcadil
  • Công ty : Daiichi Sankyo
    Sản phẩm biệt dược : Sepazon
  • Công ty : Roemmers
    Sản phẩm biệt dược : Tolestan
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01553
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2816
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505281
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01268
ChemSpider
http://www.chemspider.com/Chemical-Structure.2714.html
Wikipedia
http://en.wikipedia.org/wiki/Cloxazolam
Drugs.com
http://www.drugs.com/international/cloxazolam.html
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