Tìm theo
Chlordiazepoxide
Các tên gọi khác (13 ) :
  • 7-chloro-2-Methylamino-5-phenyl-3H-1,4-benzodiazepin-4-oxide
  • CDP
  • Chloradiazepoxide
  • Chlordiazepoxide base
  • Chlordiazepoxidum
  • Clopoxide
  • Helogaphen
  • Libritabs
  • Methaminodiazepoxide
  • Multum
  • Risolid
  • Silibrin
  • Tropium
Thuốc chống lo âu, hoảng sợ
Thuốc Gốc
Small Molecule
CAS: 58-25-3
ATC: N05BA02
ĐG : A-S Medication Solutions LLC , http://orders.a-smeds.com
CTHH: C16H14ClN3O
PTK: 299.755
An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H14ClN3O
Phân tử khối
299.755
Monoisotopic mass
299.082539792
InChI
InChI=1S/C16H14ClN3O/c1-18-15-10-20(21)16(11-5-3-2-4-6-11)13-9-12(17)7-8-14(13)19-15/h2-9H,10H2,1H3,(H,18,19)
InChI Key
InChIKey=ANTSCNMPPGJYLG-UHFFFAOYSA-N
IUPAC Name
7-chloro-2-(methylamino)-5-phenyl-3H-1,4$l^{5}-benzodiazepin-4-one
Traditional IUPAC Name
multum
SMILES
CNC1=NC2=C(C=C(Cl)C=C2)C(C2=CC=CC=C2)=N(=O)C1
Độ tan chảy
236-236.5
Độ hòa tan
2000 mg/L
logP
2.44
logS
-4.2
pKa (strongest acidic)
18.52
pKa (Strongest Basic)
6.43
PSA
53.14 Å2
Refractivity
87.34 m3·mol-1
Polarizability
30.97 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
pKa
4.8
Dược Lực Học : Chlordiazepoxide has antianxiety, sedative, appetite-stimulating and weak analgesic actions. The drug seems to block EEG arousal from stimulation in the brain stem reticular formation. The drug has been studied extensively in many species of animals and these studies are suggestive of action on the limbic system of the brain, which recent evidence indicates is involved in emotional responses. Hostile monkeys were made tame by oral drug doses which did not cause sedation. Chlordiazepoxide revealed a "taming" action with the elimination of fear and aggression. The taming effect of chlordiazepoxide was further demonstrated in rats made vicious by lesions in the septal area of the brain. The drug dosage which effectively blocked the vicious reaction was well below the dose which caused sedation in these animals.
Cơ Chế Tác Dụng : An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal. [PubChem] Chlordiazepoxide binds to stereospecific benzodiazepine (BZD) binding sites on GABA (A) receptor complexes at several sites within the central nervous system, including the limbic system and reticular formation. This results in an increased binding of the inhibitory neurotransmitter GABA to the GABA(A) receptor.BZDs, therefore, enhance GABA-mediated chloride influx through GABA receptor channels, causing membrane hyperpolarization. The net neuro-inhibitory effects result in the observed sedative, hypnotic, anxiolytic, and muscle relaxant properties.
Dược Động Học :

▧ Metabolism :
Hepatic.
▧ Route of Elimination :
Chlordiazepoxide is excreted in the urine, with 1% to 2% unchanged and 3% to 6% as conjugate.
▧ Half Life :
24-48 hours
Độc Tính : LD50=537 mg/kg (Orally in rats). Signs of overdose include respiratory depression, muscle weakness, somnolence (general depressed activity).
Chỉ Định : For the management of anxiety disorders or for the short-term relief of symptoms of anxiety, withdrawal symptoms of acute alcoholism, and preoperative apprehension and anxiety.
Tương Tác Thuốc :
  • Cimetidine Cimetidine may increase the effect of the benzodiazepine, chlordiazepoxide.
  • Clozapine Increased risk of toxicity
  • Ethotoin Ethotoin may increase the metabolism of chlordiazepoxide via CYP3A4.
  • Fluconazole Fluconazole may increase the effect of the benzodiazepine, chlordiazepoxide.
  • Fosphenytoin Fosphenytoin may increase the metabolism of chlordiazepoxide via CYP3A4.
  • Indinavir The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, chlordiazepoxide.
  • Itraconazole Itraconazole may increase the effect of the benzodiazepine, chlordiazepoxide.
  • Kava Kava may increase the effect of the benzodiazepine, chlordiazepoxide.
  • Ketoconazole Ketoconazole may increase the effect of the benzodiazepine, chlordiazepoxide.
  • Mephenytoin Mephenytoin may increase the metabolism of chlordiazepoxide via CYP3A4.
  • Nelfinavir The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, chlordiazepoxide.
  • Omeprazole Omeprazole may increase the effect of the benzodiazepine, chlordiazepoxide.
  • Phenytoin Phenytoin may increase the metabolism of chlordiazepoxide via CYP3A4.
  • Ritonavir The protease inhibitor, ritonavir, may increase the effect of the benzodiazepine, chlordiazepoxide.
  • Saquinavir The protease inhibitor, saquinavir, may increase the effect of the benzodiazepine, chlordiazepoxide.
  • Telithromycin Telithromycin may reduce clearance of Chlordiazepoxide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Chlordiazepoxide if Telithromycin is initiated, discontinued or dose changed.
  • Tipranavir Tipranavir may decrease the metabolism and clearance of Chlordiazepoxide. Consider alternate therapy or monitor for Alprazolam toxic effects if Tipranavir is initiated or dose increased.
  • Triprolidine The CNS depressants, Triprolidine and Chlordiazepoxide, 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 chlordiazepoxide by decreasing its metabolism. Monitor for chlordiazepoxide toxicity if voriconazole is initiated or dose increased.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Angirex
  • Công ty : Polfa Tarchomin
    Sản phẩm biệt dược : Elenium
  • Công ty : Nycomed
    Sản phẩm biệt dược : Klopoxid
  • Công ty : Abbott
    Sản phẩm biệt dược : Librium
  • Công ty :
    Sản phẩm biệt dược : Napoton
  • Công ty : AWD
    Sản phẩm biệt dược : Radepur
  • Công ty : Actavis
    Sản phẩm biệt dược : Risolid
  • Công ty :
    Sản phẩm biệt dược : Silibrin
  • Công ty :
    Sản phẩm biệt dược : Sonimen
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00475
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00267
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0555-0158-02
PharmGKB
http://www.pharmgkb.org/drug/PA448932
Wikipedia
http://en.wikipedia.org/wiki/Chlordiazepoxide
RxList
http://www.rxlist.com/cgi/generic/chlordia.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/lib1225.shtml
Drugs.com
http://www.drugs.com/cdi/chlordiazepoxide.html
... loading
... loading