Tìm theo
Bromazepam
Các tên gọi khác (2) :
  • Bromazepamum
  • Lectopam
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 1812-30-2
ATC: N05BA08
ĐG : United States Pharmacopeial Convention Inc. , http://www.usp.org
CTHH: C14H10BrN3O
PTK: 316.153
One of the benzodiazepines that is used in the treatment of anxiety disorders. [PubChem] It is a Schedule IV drug in the U.S. and Canada and under the Convention on Psychotropic Substances. It is a intermediate-acting benzodiazepines.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C14H10BrN3O
Phân tử khối
316.153
Monoisotopic mass
315.000724604
InChI
InChI=1S/C14H10BrN3O/c15-9-4-5-11-10(7-9)14(17-8-13(19)18-11)12-3-1-2-6-16-12/h1-7H,8H2,(H,18,19)
InChI Key
InChIKey=VMIYHDSEFNYJSL-UHFFFAOYSA-N
IUPAC Name
7-bromo-5-(pyridin-2-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one
Traditional IUPAC Name
bromazepam
SMILES
BrC1=CC2=C(NC(=O)CN=C2C2=CC=CC=N2)C=C1
Độ hòa tan
3.99e-02 g/l
logP
2.05
logS
-3.9
pKa (strongest acidic)
12.24
pKa (Strongest Basic)
2.68
PSA
54.35 Å2
Refractivity
76.99 m3·mol-1
Polarizability
28.11 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Bromazepam is a lipophilic, long-acting benzodiazepine and with sedative, hypnotic, anxiolytic and skeletal muscle relaxant properties. It does not possess any antidepressant qualities. Bromazepam shares with other benzodiazepines the risk of abuse, misuse, psychological and/or physical dependence. According to many psychiatric experts Bromazepam has a greater abuse potential than other benzodiazepines because of fast resorption and rapid onset of action.
Cơ Chế Tác Dụng : One of the benzodiazepines that is used in the treatment of anxiety disorders. [PubChem] It is a Schedule IV drug in the U.S. and Canada and under the Convention on Psychotropic Substances. It is a intermediate-acting benzodiazepines. Bromazepam binds to the GABA receptor GABAA, causing a conformational change and increasing inhibitory effects of GABA. Other neurotransmitters are not influenced.
Dược Động Học :
▧ Absorption :
Bioavailability is 84% following oral administration. The time to peak plasma level is 1 - 4 hours. Bromazepam is generally well absorbed after oral administration.
▧ Volume of Distribution :
1.56 L/kg
▧ Protein binding :
70%
▧ Metabolism :
Hepatically, via oxidative pathways (via an enzyme belonging to the Cytochrome P450 family of enzymes). One of the main metabolites is 3-hydroxybromazepam. It is pharmacologically active and the half life is similar to that of the parent compound.
▧ Route of Elimination :
Urine (69%), as metabolites
▧ Half Life :
10-20 hours
▧ Clearance :
0.82 mL/min/kg.
Chỉ Định : For the short-term treatment of insomnia, short-term treatment of anxiety or panic attacks, if a benzodiazepine is required, and the alleviation of the symptoms of alcohol- and opiate-withdrawal.
Tương Tác Thuốc :
  • Aminophylline Aminophylline may decrease the therapeutic effect of bromazepam. Monitor for changes in the therapeutic effects of bromazepam if aminophylline is initiated, discontinued or dose changed.
  • Atazanavir Atazanavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if atazanavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Cimetidine Co-administration with cimetidine will cause a reduction in bromazepam clearance and increases half-life.
  • Clarithromycin Clarithromycin, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if clarithromycin is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Clozapine Bromazepam may increase the adverse effects of clozapine. Consider alternate therapy or a reduction in the bromazepam dose. Monitor for respiratory depression and hypotension if concomitant therapy is initiated.
  • Conivaptan Conivaptan, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if conivaptan is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Darunavir Darunavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if darunavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Delavirdine Delavirdine, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if delavirdine is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Diltiazem Diltiazem may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or a reductin in the bromazepam dose. Monitor for changes in the therapeutic and adverse effects of bromazepam if diltiazem is initiated, discontinued or dose changed.
  • Dyphylline Dyphylline may decrease the therapeutic effect of bromazepam. Monitor for changes in the therapeutic effects of bromazepam if dyphylline is initiated, discontinued or dose changed.
  • Erythromycin Erythromcyin may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if erythromycin is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Fluconazole Fluconazole may increase the serum concentration of bromazepam by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if fluconazole is initiated, discontinued or dose changed.
  • Fosamprenavir Fosamprenavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if fosamprenavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Imatinib Imatinib, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if imatinib is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Indinavir Indinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if indinavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Isoniazid Isoniazid, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if isoniazid is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Itraconazole Itraconazole may increase the serum concentration of bromazepam by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if itraconazole is initiated, discontinued or dose changed.
  • Ketoconazole Ketoconazole may increase the serum concentration of bromazepam by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if ketoconazole is initiated, discontinued or dose changed.
  • Lopinavir Lopinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if lopinavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Methotrimeprazine Concomitant therapy may result in additive CNS depressant effects. The dosage of bromazepam should be decreased by 50% prior to initiating concomitant therapy. Monitor for increased CNS depression.
  • Nefazodone Nefazodone, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if nefazodone is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Nelfinavir Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if nelfinavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Nicardipine Nicardipine, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if nicardipine is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Posaconazole Posaconazole may increase the serum concentration of bromazepam by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if posaconazole is initiated, discontinued or dose changed.
  • Propranolol Co-administration with propranolol will cause a reduction in bromazepam clearance and increases half-life.
  • Quinidine Quinidine, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if quinidine is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Rifabutin Rifabutin may decrease the serum concentration of bromazepam by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if rifabutin is initiated, discontinued or dose changed.
  • Rifampicin Rifampin may decrease the serum concentration of bromazepam by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if rifampin is initiated, discontinued or dose changed.
  • Rifapentine Rifapentine may decrease the serum concentration of bromazepam by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if rifapentine is initiated, discontinued or dose changed.
  • Ritonavir Ritonavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if ritonavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Saquinavir Saquinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if saquinavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Telithromycin Telithromycin, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if telithromycin is initiated, discontinued or dose changed. Dosage adjustments may be required.
  • Theophylline Theophylline may decrease the therapeutic effect of bromazepam. Monitor for changes in the therapeutic effects of bromazepam if theophylline is initiated, discontinued or dose changed.
  • Tipranavir Tipranavir may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if tipranavir is initiated, discontinued or dose changed.
  • Triprolidine The CNS depressants, Triprolidine and Bromazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Verapamil Verapamil may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or a reductin in the bromazepam dose. Monitor for changes in the therapeutic and adverse effects of bromazepam if verapamil is initiated, discontinued or dose changed.
  • Voriconazole Voriconazole may increase the serum concentration of bromazepam by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral - 1.5 mg, 3 mg, 6 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Calmepam
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  • Công ty :
    Sản phẩm biệt dược : Durazanil
  • Công ty :
    Sản phẩm biệt dược : Lectopam
  • Công ty :
    Sản phẩm biệt dược : Lekotam
  • Công ty :
    Sản phẩm biệt dược : Lexaurin
  • Công ty :
    Sản phẩm biệt dược : Lexilium
  • Công ty :
    Sản phẩm biệt dược : Lexomil
  • Công ty :
    Sản phẩm biệt dược : Lexotan
  • Công ty :
    Sản phẩm biệt dược : Normoc
  • Công ty :
    Sản phẩm biệt dược : Ultramidol
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01558
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2441
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505694
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01245
ChemSpider
http://www.chemspider.com/Chemical-Structure.2347.html
PharmGKB
http://www.pharmgkb.org/drug/PA10035
Wikipedia
http://en.wikipedia.org/wiki/Bromazepam
Drugs.com
http://www.drugs.com/international/bromazepam.html
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