Tìm theo
Temazepam
Các tên gọi khác (1) :
  • Restoril
Thuốc an thần
Thuốc Gốc
Small Molecule
CAS: 846-50-4
ATC: N05CD07
ĐG : Actavis Group , http://www.actavis.com
CTHH: C16H13ClN2O2
PTK: 300.74
A benzodiazepine that acts as a gamma-aminobutyric acid modulator and anti-anxiety agent. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H13ClN2O2
Phân tử khối
300.74
Monoisotopic mass
300.066555377
InChI
InChI=1S/C16H13ClN2O2/c1-19-13-8-7-11(17)9-12(13)14(18-15(20)16(19)21)10-5-3-2-4-6-10/h2-9,15,20H,1H3
InChI Key
InChIKey=SEQDDYPDSLOBDC-UHFFFAOYSA-N
IUPAC Name
7-chloro-3-hydroxy-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
Traditional IUPAC Name
temazepam
SMILES
CN1C2=C(C=C(Cl)C=C2)C(=NC(O)C1=O)C1=CC=CC=C1
Độ tan chảy
119-121 °C
Độ hòa tan
164 mg/L
logP
2.19
logS
-3.8
pKa (strongest acidic)
10.68
pKa (Strongest Basic)
-1.4
PSA
52.9 Å2
Refractivity
81.01 m3·mol-1
Polarizability
30.32 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 : Temazepam is a benzodiazepine used as a hypnotic agent in the management of insomnia. Temazepam produces CNS depression at limbic, thalamic, and hypothalamic levels of the CNS. Temazepam increases the affinity of the neurotransmitter gamma-aminobutyric acid (GABA) for GABA receptors by binding to benzodiazepine receptors. Results are sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, and anxiolytic action.
Cơ Chế Tác Dụng : A benzodiazepine that acts as a gamma-aminobutyric acid modulator and anti-anxiety agent. [PubChem] Benzodiazepines bind nonspecifically to benzodiazepine receptors, which 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 :
Well absorbed, minimal first-pass metabolism.
▧ Protein binding :
96%
▧ Metabolism :
Hepatic. Temazepam is completely metabolized through conjugation prior to excretion. The major metabolite is the O-conjugate of temazepam (90%).
▧ Route of Elimination :
Temazepam was completely metabolized through conjugation prior to excretion; 80% to 90% of the dose appeared in the urine.
▧ Half Life :
10-20 hours
Chỉ Định : For the short-term treatment of insomnia (generally 7-10 days).
Tương Tác Thuốc :
  • Aminophylline Aminophylline may decrease the efficacy of Temazepam. Monitor for changes in the therapeutic effect of Temazepam if Aminophylline is initiated, discontinued or dose changed.
  • Clozapine The benzodiazepine, Temazepam, may increase the adverse effects of Clozapine. Monitor for respiratory depression and hypotension if concomitant therapy is initiated.
  • Dyphylline Dyphylline may decrease the efficacy of Temazepam. Monitor for changes in the therapeutic effect of Temazepam if Dyphylline is initiated, discontinued or dose changed.
  • Kava Kava may increase the effect of the benzodiazepine, temazepam.
  • Theophylline Theophylline may decrease the efficacy of Temazepam. Monitor for changes in the therapeutic effect of Temazepam if Theophylline is initiated, discontinued or dose changed.
  • Triprolidine The CNS depressants, Triprolidine and Temazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Euhypnos
  • Công ty :
    Sản phẩm biệt dược : Norkotral
  • Công ty :
    Sản phẩm biệt dược : Normison
  • Công ty :
    Sản phẩm biệt dược : Nortem
  • Công ty :
    Sản phẩm biệt dược : Remestan
  • Công ty :
    Sản phẩm biệt dược : Restoril
  • Công ty :
    Sản phẩm biệt dược : Temaze
  • Công ty :
    Sản phẩm biệt dược : Temtabs
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00231
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5391
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506604
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00370
ChemSpider
http://www.chemspider.com/Chemical-Structure.5198.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/53489-648-07
PharmGKB
http://www.pharmgkb.org/drug/PA451608
Wikipedia
http://en.wikipedia.org/wiki/Temazepam
RxList
http://www.rxlist.com/cgi/generic/temaz.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/res1373.shtml
Drugs.com
http://www.drugs.com/temazepam.html
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