Tìm theo
Brotizolam
Các tên gọi khác (2) :
  • Brotizolam
  • Brotizolamum
Thuốc Gốc
Small Molecule
CAS: 57801-81-7
CTHH: C15H10BrClN4S
PTK: 393.689
Brotizolam is a sedative-hypnotic thienodiazepine drug which is a benzodiazepine analog. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties, and is considered to be similar in effect to short-acting benzodiazepines such as triazolam. It is used in the short term treatment of severe or debilitating insomnia. Brotizolam is an extremely potent drug and it is rapidly eliminated with an average half-life of 4.4 hours (range 3.6 - 7.9 hours). Brotizolam is not approved for sale in the UK, United States or Canada. It is approved for sale in the Netherlands, Germany, Spain, Belgium, Austria, Portugal, Israel, Italy and Japan.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H10BrClN4S
Phân tử khối
393.689
Monoisotopic mass
391.949807384
InChI
InChI=1S/C15H10BrClN4S/c1-8-19-20-13-7-18-14(9-4-2-3-5-11(9)17)10-6-12(16)22-15(10)21(8)13/h2-6H,7H2,1H3
InChI Key
InChIKey=UMSGKTJDUHERQW-UHFFFAOYSA-N
IUPAC Name
4-bromo-7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetraazatricyclo[8.3.0.0²,⁶]trideca-2(6),4,7,10,12-pentaene
Traditional IUPAC Name
brotizolam
SMILES
CC1=NN=C2CN=C(C3=C(SC(Br)=C3)N12)C1=CC=CC=C1Cl
Độ tan chảy
211-213
Độ hòa tan
5.80e-02 g/l
logP
2.68
logS
-3.8
pKa (strongest acidic)
18.49
pKa (Strongest Basic)
3.9
PSA
43.07 Å2
Refractivity
101.93 m3·mol-1
Polarizability
34.99 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 Động Học :
▧ Absorption :
The plasma concentration profile of brotizolam can be described as a one compartmental open model with first-order absorption.
▧ Volume of Distribution :
0.63 l/kg.
▧ Protein binding :
The mean value of the free fraction (%): 8.4 ± 0.7.
▧ Metabolism :
There are two primary metabolites: 1-methyl-hydroxy- and the 4-hydroxy-derivatives (Eberts et al., 1981; Boehringer Ingelheim, product information). The 4-hydroxymetabolites have a pharmacological activity which is far less than that of the parent drugs, but the 1-methyl-hydroxymetabolites probably have comparable activity (Gall et al., 1978; Jochemsen et al., 1982; Sethy & Harris, 1982; Jochemsen et al., unpublished results). These active compounds are, however, not present in plasma in measurable amounts following a single dose of brotizolam to young healthy subjects (Jochemsen et al., 1982; Jochemsen et al., unpublished results).
▧ Half Life :
4.4 hours.
▧ Clearance :
Total clearance: 109 ml/min.
Chỉ Định : Brotizolam is indicated for the short-term treatment (2-4 weeks) of severe or debilitating insomnia.
Liều Lượng & Cách Dùng : Tablet - Oral - 0.5 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB09017
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01744
Wikipedia
http://en.wikipedia.org/wiki/Brotizolam
Drugs.com
http://www.drugs.com/international/brotizolam.html
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