Tìm theo
Flurazepam
Các tên gọi khác (4 ) :
  • Flurazepam
  • Flurazépam
  • Flurazepamum
  • Insumin
Thuốc Gốc
Small Molecule
CAS: 17617-23-1
ATC: N05CD01
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C21H23ClFN3O
PTK: 387.878
A benzodiazepine derivative used mainly as a hypnotic. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H23ClFN3O
Phân tử khối
387.878
Monoisotopic mass
387.151368285
InChI
InChI=1S/C21H23ClFN3O/c1-3-25(4-2)11-12-26-19-10-9-15(22)13-17(19)21(24-14-20(26)27)16-7-5-6-8-18(16)23/h5-10,13H,3-4,11-12,14H2,1-2H3
InChI Key
InChIKey=SAADBVWGJQAEFS-UHFFFAOYSA-N
IUPAC Name
7-chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one
Traditional IUPAC Name
flurazepam
SMILES
CCN(CC)CCN1C2=C(C=C(Cl)C=C2)C(=NCC1=O)C1=CC=CC=C1F
Độ tan chảy
190-220
Độ hòa tan
500 mg/mL (HCl salt)
logP
3.8
logS
-4.6
pKa (Strongest Basic)
8.71
PSA
35.91 Å2
Refractivity
107.54 m3·mol-1
Polarizability
41.22 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Flurazepam, a benzodiazepine derivative, is a hypnotic agent which does not appear to decrease dream time as measured by rapid eye movements (REM). Furthermore, it decreases sleep latency and number of awakenings for a consequent increase in total sleep time.
Cơ Chế Tác Dụng : A benzodiazepine derivative used mainly as a hypnotic. [PubChem] Flurazepam binds to an allosteric site on GABA-A receptors. Binding potentiates the action of GABA on GABA-A receptors by opening the chloride channel within the receptor, causing chloride influx and hyperpolarization.
Dược Động Học :
▧ Absorption :
Flurazepam hydrochloride is rapidly (30 minutes) absorbed from the gastrointestinal tract
▧ Protein binding :
83%
▧ Metabolism :
Flurazepam is rapidly metabolized and is excreted primarily in the urine. Both hydroxyethyl flurazepam (the major metabolite) and N-desalkyl flurazepam are active. The N-desalkyl metabolite is slowly excreted in the urine as the conjugated form
▧ Route of Elimination :
Flurazepam is rapidly metabolized and is excreted primarily in the urine. Less than 1% of the dose is excreted in the urine as N1-desalkyl-flurazepam.
▧ Half Life :
The mean apparent half-life of flurazepam is 2.3 hours. The half life of elimination of N1-des-alkyl- flurazepam ranged from 47 to 100 hours
Độc Tính : Coma, confusion, low blood pressure, sleepiness
Chỉ Định : For short-term and intermittent use in patients with recurring insomnia and poor sleeping habits
Tương Tác Thuốc :
  • Amprenavir Amprenavir may increase the effect and toxicity of the benzodiazepine, flurazepam.
  • Cimetidine Cimetidine may increase the effect of the benzodiazepine, flurazepam.
  • Clozapine Increased risk of toxicity
  • Ethotoin Ethotoin may increase the metabolism of flurazepam via CYP3A4.
  • Fluconazole Fluconazole may increase the effect of the benzodiazepine, flurazepam.
  • Fosamprenavir Fosamprenavir may increase the effect and toxicity of the benzodiazepine, flurazepam.
  • Fosphenytoin Fosphenytoin may increase the metabolism of flurazepam via CYP3A4.
  • Indinavir The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, flurazepam.
  • Itraconazole Itraconazole may increase the effect of the benzodiazepine, flurazepam.
  • Kava Kava may increase the effect of the benzodiazepine, flurazepam.
  • Ketoconazole Ketoconazole may increase the effect of the benzodiazepine, flurazepam.
  • Mephenytoin Mephenytoin may increase the metabolism of flurazepam via CYP3A4.
  • Nelfinavir The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, flurazepam.
  • Omeprazole Omeprazole may increase the effect of the benzodiazepine, flurazepam.
  • Phenytoin Phenytoin may increase the metabolism of flurazepam via CYP3A4.
  • Ritonavir The protease inhibitor, ritonavir, may increase the effect of the benzodiazepine, flurazepam.
  • Saquinavir The protease inhibitor, saquinavir, may increase the effect of the benzodiazepine, flurazepam.
  • Telithromycin Telithromycin may reduce clearance of Flurazepam. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Flurazepam if Telithromycin is initiated, discontinued or dose changed.
  • Tipranavir Tipranavir may decrease the metabolism and clearance of Flurazepam. Consider alternate therapy or monitor for Flurazepam toxic effects if Tipranavir is initiated or dose increased.
  • Triprolidine The CNS depressants, Triprolidine and Flurazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of flurazepam by decreasing its metabolism. Monitor for flurazepam toxicity if voriconazole is initiated or dose increased.
Liều Lượng & Cách Dùng : Capsule - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Meda
    Sản phẩm biệt dược : Dalmadorm
  • Công ty : Meda
    Sản phẩm biệt dược : Dalmadorm medium
  • Công ty : Meda
    Sản phẩm biệt dược : Dalmane
  • Công ty : SIT
    Sản phẩm biệt dược : Felison
  • Công ty : Teofarma
    Sản phẩm biệt dược : Flunox
  • Công ty : I.C.N.
    Sản phẩm biệt dược : Sompan
  • Công ty : Valeas
    Sản phẩm biệt dược : Valdorm
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00690
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3393
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508451
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00329
ChemSpider
http://www.chemspider.com/Chemical-Structure.3276.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-4415-01
PharmGKB
http://www.pharmgkb.org/drug/PA449681
Wikipedia
http://en.wikipedia.org/wiki/Flurazepam
RxList
http://www.rxlist.com/cgi/generic2/fluraz.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/dal1113.shtml
Drugs.com
http://www.drugs.com/cdi/flurazepam.html
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