Tìm theo
Halazepam
Các tên gọi khác (5 ) :
  • Halazepam
  • Halazépam
  • Halazepam
  • Halazepamum
  • Paxipam
Thuốc chống lo âu, hoảng sợ
Thuốc Gốc
Small Molecule
CAS: 23092-17-3
ATC: N05BA13
CTHH: C17H12ClF3N2O
PTK: 352.738
Halazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is a trifluoromethyl derivative of nordazepam. While its structure may be similar to chlordiazepoxide and diazepam, it has both less toxicity and less tendency to cause paradoxical hostility and aggression than either of them. Halazepam is no longer marketed in the United States, and was withdrawn by Schering-Plough due to poor sales. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H12ClF3N2O
Phân tử khối
352.738
Monoisotopic mass
352.059025338
InChI
InChI=1S/C17H12ClF3N2O/c18-12-6-7-14-13(8-12)16(11-4-2-1-3-5-11)22-9-15(24)23(14)10-17(19,20)21/h1-8H,9-10H2
InChI Key
InChIKey=WYCLKVQLVUQKNZ-UHFFFAOYSA-N
IUPAC Name
7-chloro-5-phenyl-1-(2,2,2-trifluoroethyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one
Traditional IUPAC Name
halazepam
SMILES
FC(F)(F)CN1C2=C(C=C(Cl)C=C2)C(=NCC1=O)C1=CC=CC=C1
Độ tan chảy
165 °C
Độ hòa tan
1.70e-03 g/l
logP
3.97
logS
-5.3
pKa (strongest acidic)
18.88
pKa (Strongest Basic)
2.33
PSA
32.67 Å2
Refractivity
85.26 m3·mol-1
Polarizability
31.82 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
Cơ Chế Tác Dụng : Halazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is a trifluoromethyl derivative of nordazepam. While its structure may be similar to chlordiazepoxide and diazepam, it has both less toxicity and less tendency to cause paradoxical hostility and aggression than either of them. Halazepam is no longer marketed in the United States, and was withdrawn by Schering-Plough due to poor sales. [Wikipedia] Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, 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 of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Dược Động Học :

▧ Metabolism :
Hepatic.
Chỉ Định : Used to relieve anxiety, nervousness, and tension associated with anxiety disorders.
Tương Tác Thuốc :
  • Cimetidine Cimetidine may increase the effect of the benzodiazepine, halazepam.
  • Clozapine Increased risk of toxicity
  • Fluconazole Fluconazole may increase the effect of the benzodiazepine, halazepam.
  • Indinavir The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, halazepam.
  • Itraconazole Itraconazole may increase the effect of the benzodiazepine, halazepam.
  • Ketoconazole Ketoconazole may increase the effect of the benzodiazepine, halazepam.
  • Nelfinavir The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, halazepam.
  • Omeprazole Omeprazole may increase the effect of the benzodiazepine, halazepam.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Menarini
    Sản phẩm biệt dược : Alapryl
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Pacinone
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Paxipam
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00801
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=31640
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508415
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00338
ChemSpider
http://www.chemspider.com/Chemical-Structure.29343.html
PharmGKB
http://www.pharmgkb.org/drug/PA164746526
Wikipedia
http://en.wikipedia.org/wiki/Halazepam
Drugs.com
http://www.drugs.com/mtm/halazepam.html
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