Tìm theo
Delorazepam
Các tên gọi khác (3) :
  • CDDZ
  • Chlordesmethyldiazepam
  • Dadumir
Thuốc chống co giật, chống động kinh
Thuốc Gốc
Small Molecule
CAS: 2894-67-9
CTHH: C15H10Cl2N2O
PTK: 305.159
Delorazepam is a benzodiazepine which, like other drugs in its class, possesses anxiolytic, skeletal muscle relaxant, hypnotic and anticonvulsant properties. It may have adverse effects such as drowsiness, and cognitive impairments such as short term memory impairment. [4] Delorazepam is an active metabolite of the benzodiazepine known as cloxazolam. It is a long acting benzodiazepine which makes it superior in this sense to lorazepam which is short acting. Lorazepam is also a major active metabolite of delorazepam. In addition to be long acting, delorazepam is relatively potent, with 1 mg of delorazepam being the equivalent of 10 mg diazepam. [Wikipedia] It has been approved for marketing in Italy.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H10Cl2N2O
Phân tử khối
305.159
Monoisotopic mass
304.017018366
InChI
InChI=1S/C15H10Cl2N2O/c16-9-5-6-13-11(7-9)15(18-8-14(20)19-13)10-3-1-2-4-12(10)17/h1-7H,8H2,(H,19,20)
InChI Key
InChIKey=CHIFCDOIPRCHCF-UHFFFAOYSA-N
IUPAC Name
7-chloro-5-(2-chlorophenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one
Traditional IUPAC Name
delorazepam
SMILES
ClC1=CC2=C(NC(=O)CN=C2C2=CC=CC=C2Cl)C=C1
Độ hòa tan
6.42e-03 g/l
logP
3.15
logS
-4.7
pKa (strongest acidic)
12.29
pKa (Strongest Basic)
2.05
PSA
41.46 Å2
Refractivity
81.5 m3·mol-1
Polarizability
29.44 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Động Học :
▧ Absorption :
77-87% oral bioavailability, with a relatively slow absorption rate. [5] Reaches peak plasma levels within 1-2 hours of administration. Food may slow absorption, however other pharmacokinetic variables remain unchanged. After multiple doses delorazepam accumulates, however accumulation is slower in younger patients.[1]
▧ Volume of Distribution :
140 L/kg apparent volume of distribution in 11 patients with normal renal function; 47 L/kg in 11 patients with renal failure and on regular hemodialysis. [5] In another study, apparent volume of distribution was 65 L/kg in 8 patients with liver disease and 118.4 L/kg in 12 healthy controls. [2]
▧ Protein binding :
>90% protein bound. [5]
▧ Metabolism :
Delorazepam is metabolized at a relatively slow pace by the liver. The major metabolite (15-34% of the parent drug) is lorazepam. Older patients metabolize delorazepam slower than younger patients. [1]
▧ Route of Elimination :
Renally eliminated.
▧ Half Life :
Very long elimination half life of 80-115 hours, varying with age. Elimination is slower as age increases. [1] Liver disease also impacts elimination half life, with impairment resulting in half lives up to 395 hours. [2]
▧ Clearance :
Still detectable 72 hours after dosing in healthy patients. Patients with liver disease experienced a reduction in clearance from 0.13 to 0.25 ng/mLh. [2]
Độc Tính : Older patients metabolize delorazepam slower than younger patients and thus suffer from more adverse effects. [1]
Chỉ Định : Mainly used as an anti-anxiety agent. Studies have found delorazepam to be more effective in the first 4 weeks of use than antidepressants; however, after 4 weeks, antidepressants showed superior anti-anxiety effects. [Wikipedia] Anti-anxiety effects also appear to be weaker in elderly patients. [1] Effectiveness has also been observed in the treatment of alcohol withdrawal. Delorazapam was reported to be a manageable drug in that it did not exhibit severe side effects and did not require further therapies to control symptoms of withdrawal. [3]
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Dadumir
  • Công ty : Almus
    Sản phẩm biệt dược : Delorazepam Almus
  • Công ty : Alter
    Sản phẩm biệt dược : Delorazepam Alter
  • Công ty : Aurobindo
    Sản phẩm biệt dược : Delorazepam Aurobindo
  • Công ty : DOC Generici
    Sản phẩm biệt dược : Delorazepam DOC
  • Công ty : EG
    Sản phẩm biệt dược : Delorazepam EG
  • Công ty : Germed Pharma
    Sản phẩm biệt dược : Delorazepam Germed
  • Công ty : Hexal
    Sản phẩm biệt dược : Delorazepam Hexal
  • Công ty : Mylan
    Sản phẩm biệt dược : Delorazepam Mylan
  • Công ty : Pensa Pharma
    Sản phẩm biệt dược : Delorazepam Pensa
  • Công ty : Ranbaxy Italia
    Sản phẩm biệt dược : Delorazepam Ranbaxy
  • Sản phẩm biệt dược : Delorazepam ratiopharm
  • Công ty : Sandoz
    Sản phẩm biệt dược : Delorazepam Sandoz
  • Công ty : Teva Italia,
    Sản phẩm biệt dược : Delorazepam Teva
  • Công ty : Sanofi Winthrop
    Sản phẩm biệt dược : Delorazepam Winthrop
  • Công ty : Abbott
    Sản phẩm biệt dược : EN
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01511
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=17925
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504957
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D07784
ChemSpider
http://www.chemspider.com/Chemical-Structure.16929.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50026858
Wikipedia
http://en.wikipedia.org/wiki/Delorazepam
Drugs.com
http://www.drugs.com/international/delorazepam.html
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