Tìm theo
Clorazepate
Các tên gọi khác (3) :
  • 7-chloro-2,3-dihydro-2,2-Dihydroxy-5-phenyl-1H-1,4-benzodiazepine-3-carboxylic acid
  • Clorazepate
  • Clorazepic acid
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 23887-31-2
ATC: N05BA05
ĐG : Abbott Laboratories Ltd. , http://www.abbott.com
CTHH: C16H11ClN2O3
PTK: 314.723
A water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H11ClN2O3
Phân tử khối
314.723
Monoisotopic mass
314.045819935
InChI
InChI=1S/C16H11ClN2O3/c17-10-6-7-12-11(8-10)13(9-4-2-1-3-5-9)19-14(16(21)22)15(20)18-12/h1-8,14H,(H,18,20)(H,21,22)
InChI Key
InChIKey=XDDJGVMJFWAHJX-UHFFFAOYSA-N
IUPAC Name
7-chloro-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepine-3-carboxylic acid
Traditional IUPAC Name
clorazepate
SMILES
OC(=O)C1N=C(C2=CC=CC=C2)C2=C(NC1=O)C=CC(Cl)=C2
Độ hòa tan
Very soluble
logP
3
logS
-4.1
pKa (strongest acidic)
3.32
pKa (Strongest Basic)
-0.64
PSA
78.76 Å2
Refractivity
82.68 m3·mol-1
Polarizability
30.63 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Clorazepate is a member of the group of drugs called benzodiazepines. Pharmacologically, clorazepate has the characteristics of the benzodiazepines. It has depressant effects on the central nervous system. The primary metabolite, nordiazepam, quickly appears in the blood stream. Studies in healthy men have shown that clorazenate has depressant effects on the central nervous system. Since orally administered clorazepate dipotassium is rapidly decarboxylated to form nordiazepam, there is essentially no circulating parent drug.
Cơ Chế Tác Dụng : A water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions. [PubChem] 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 the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration (bioavailability is 91%).
▧ Protein binding :
The protein binding of nordiazepam in plasma is high (97-98%).
▧ Metabolism :
The drug is metabolized in the liver and excreted primarily in the urine. The primary metabolite, nordiazepam, is further metabolized by hydroxylation. The major urinary metabolite is conjugated oxazepam (3-hydroxynordiazepam), and smaller amounts of conjugated p-hydroxynordiazepam and nordiazepam are also found in the urine.
▧ Route of Elimination :
The drug is metabolized in the liver and excreted primarily in the urine.
▧ Half Life :
The serum half-life is about 2 days. Nordiazepam, the primary metabolite, quickly appears in the blood and is eliminated from the plasma with an apparent half-life of about 40 to 50 hours.
Độc Tính : Oral LD50 in rats is 1320 mg/kg. In monkeys, oral LD50 exceed 1600 mg/kg. Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time.
Chỉ Định : For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety. Also used as adjunctive therapy in the management of partial seizures and for the symptomatic relief of acute alcohol withdrawal.
Tương Tác Thuốc :
  • Amprenavir Amprenavir may increase the effect and toxicity of the benzodiazepine, clorazepate.
  • Cimetidine Cimetidine may increase the effect of the benzodiazepine, clorazepate.
  • Clozapine Increased risk of toxicity
  • Ethotoin Ethotoin may increase the metabolism of clorazepate via CYP3A4.
  • Fluconazole Fluconazole may increase the effect of the benzodiazepine, clorazepate.
  • Fosamprenavir Fosamprenavir may increase the effect and toxicity of the benzodiazepine, clorazepate.
  • Fosphenytoin Fosphenytoin may increase the metabolism of clorazepate via CYP3A4.
  • Indinavir The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, clorazepate.
  • Itraconazole Itraconazole may increase the effect of the benzodiazepine, clorazepate.
  • Kava Kava may increase the effect of the benzodiazepine, clorazepate.
  • Ketoconazole Ketoconazole may increase the effect of the benzodiazepine, clorazepate.
  • Mephenytoin Mephenytoin may increase the metabolism of clorazepate via CYP3A4.
  • Nelfinavir The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, clorazepate.
  • Omeprazole Omeprazole may increase the effect of the benzodiazepine, clorazepate.
  • Phenytoin Phenytoin may increase the metabolism of clorazepate via CYP3A4.
  • Ritonavir The protease inhibitor, ritonavir, may increase the effect of the benzodiazepine, clorazepate.
  • Saquinavir The protease inhibitor, saquinavir, may increase the effect of the benzodiazepine, clorazepate.
  • Telithromycin Telithromycin may reduce clearance of Clorazepate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Clorazepate if Telithromycin is initiated, discontinued or dose changed.
  • Tipranavir Tipranavir may decrease the metabolism and clearance of Clorazepate. Consider alternate therapy or monitor for Clorazepate toxic effects if Tipranavir is initiated or dose increased.
  • Triprolidine The CNS depressants, Triprolidine and Clorazepate, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Voriconazole Voriconazole may increase the serum concentration of clorazepate by decreasing its metabolism. Monitor for clorazepate toxicity if voriconazole is initiated or dose increased.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
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    Sản phẩm biệt dược : Anksen
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    Sản phẩm biệt dược : Cloranxen
  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Clorazepatum
  • Công ty : Weidar
    Sản phẩm biệt dược : Clozene
  • Công ty : Asian
    Sản phẩm biệt dược : Dipot
  • Công ty : Pharmasant
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    Sản phẩm biệt dược : Gen-xene
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  • Công ty : March
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  • Công ty : Tecnifar
    Sản phẩm biệt dược : Medipax
  • Công ty : Abbott Japan
    Sản phẩm biệt dược : Mendon
  • Công ty : Polipharm
    Sản phẩm biệt dược : Polizep
  • Công ty : Finadiet
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  • Công ty : T P Drug
    Sản phẩm biệt dược : Trancap
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    Sản phẩm biệt dược : Tranxène
  • Công ty : Lundbeck
    Sản phẩm biệt dược : Tranxene
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  • Công ty : sanofi-aventis
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  • Công ty : sanofi-aventis
    Sản phẩm biệt dược : Tranxilium
  • Công ty : Masa Lab
    Sản phẩm biệt dược : Zetran-5
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00628
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2809
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506595
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00694
ChemSpider
http://www.chemspider.com/Chemical-Structure.2707.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-0030-01
PharmGKB
http://www.pharmgkb.org/drug/PA164749297
Wikipedia
http://en.wikipedia.org/wiki/Clorazepate
RxList
http://www.rxlist.com/cgi/generic2/clorazepate.htm
Drugs.com
http://www.drugs.com/cdi/clorazepate.html
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