Tìm theo
Triazolam
Các tên gọi khác (5 ) :
  • Halcion
  • Triazolam
  • Triazolam
  • Triazolam
  • Triazolamum
Thuốc chống lo âu, hoảng sợ
Thuốc Gốc
Small Molecule
CAS: 28911-01-5
ATC: N05CD05
ĐG : Alphapharm Party Ltd. , http://www.alphapharm.com.au
CTHH: C17H12Cl2N4
PTK: 343.21
Withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions. This drug continues to be available in the U.S. Internationally, triazolam is a Schedule IV drug under the Convention on Psychotropic Substances.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H12Cl2N4
Phân tử khối
343.21
Monoisotopic mass
342.043901818
InChI
InChI=1S/C17H12Cl2N4/c1-10-21-22-16-9-20-17(12-4-2-3-5-14(12)19)13-8-11(18)6-7-15(13)23(10)16/h2-8H,9H2,1H3
InChI Key
InChIKey=JOFWLTCLBGQGBO-UHFFFAOYSA-N
IUPAC Name
12-chloro-9-(2-chlorophenyl)-3-methyl-2,4,5,8-tetraazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,8,11,13-hexaene
Traditional IUPAC Name
triazolam
SMILES
CC1=NN=C2CN=C(C3=CC=CC=C3Cl)C3=C(C=CC(Cl)=C3)N12
Độ tan chảy
233-235 °C
Độ hòa tan
4.53 mg/L
logP
2.42
logS
-4.08
pKa (strongest acidic)
18.08
pKa (Strongest Basic)
4.32
PSA
43.07 Å2
Refractivity
103.68 m3·mol-1
Polarizability
34.19 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : A short-acting benzodiazepine used as a hypnotic agent in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. Triazolam has a shorter half-life than chlordiazepoxide, flurazepam, and prazepam and does not generate active metabolites.
Cơ Chế Tác Dụng : Withdrawn in the United Kingdom due to risk of psychiatric adverse drug reactions. This drug continues to be available in the U.S. Internationally, triazolam is a Schedule IV drug under the Convention on Psychotropic Substances. Benzodiazepines bind nonspecifically to bezodiazepine 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 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 :
Bioavailability is 44% (oral) and 53% (sublingual).
▧ Metabolism :
Hepatic. Small amounts of unmetabolized triazolam appear in the urine.
▧ Route of Elimination :
Triazolam and its metabolites, principally as conjugated glucuronides, which are presumably inactive, are excreted primarily in the urine. Only small amounts of unmetabolized triazolam appear in the urine. The two primary metabolites accounted for 79.9% of urinary excretion.
▧ Half Life :
1.5-5.5 hours
Độc Tính : Symptoms of overdose include drowsiness, slurred speech, motor inco-ordination, coma, and respiratory depression.
Chỉ Định : For the short-term treatment of insomnia.
Tương Tác Thuốc :
  • Amprenavir Amprenavir may increase the effect and toxicity of the benzodiazepine, triazolam.
  • Aprepitant Aprepitant may increase the effect and toxicity of the benzodiazepine, triazolam.
  • Atazanavir Atazanavir may increase the effect and toxicity of the benzodiazepine, triazolam.
  • Cimetidine Cimetidine may increase the serum concentration of triazolam by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of triazolam if cimetidine is initiated, discontinued or dose changed.
  • Clarithromycin The macrolide, clarithromycin, may increase the effect of the benzodiazepine, triazolam.
  • Clozapine Increased risk of toxicity
  • Delavirdine The antiviral agent, delavirdine, may increase the effect and toxicity of the benzodiazepine, triazolam.
  • Diltiazem The calcium channel blocker, diltiazem, may increase the effect and toxicity of the benzodiazepine, triazolam.
  • Efavirenz The antiviral agent, efavirenz, may increase the effect and toxicity of the benzodiazepine, triazolam.
  • Erythromycin The macrolide, erythromycin, may increase the effect of the benzodiazepine, triazolam.
  • Ethotoin Ethotoin may increase the metabolism of triazolam via CYP3A4.
  • Fluconazole Fluconazole may increase the effect of the benzodiazepine, triazolam.
  • Fosamprenavir Fosamprenavir may increase the effect and toxicity of the benzodiazepine, triazolam.
  • Fosphenytoin Fosphenytoin may increase the metabolism of triazolam via CYP3A4.
  • Indinavir The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, triazolam.
  • Itraconazole Itraconazole may increase the effect of the benzodiazepine, triazolam.
  • Josamycin The macrolide, josamycin, may increase the effect of the benzodiazepine, triazolam.
  • Kava Kava may increase the effect of the benzodiazepine, triazolam.
  • Ketoconazole Ketoconazole may increase the effect of the benzodiazepine, triazolam.
  • Mephenytoin Mephenytoin may increase the metabolism of triazolam via CYP3A4.
  • Modafinil Modafinil decreases the effect of triazolam
  • Nefazodone Nefazodone increases the effect of triazolam
  • Nelfinavir The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, triazolam.
  • Omeprazole Omeprazole may increase the effect of the benzodiazepine, triazolam.
  • Phenytoin Phenytoin may increase the metabolism of triazolam via CYP3A4.
  • Rifampicin Rifampin may decrease the effect of the benzodiazepine, triazolam.
  • Ritonavir The protease inhibitor, ritonavir, may increase the effect of the benzodiazepine, triazolam.
  • Saquinavir The protease inhibitor, saquinavir, may increase the effect of the benzodiazepine, triazolam.
  • St. John's Wort St. John's Wort may decrease the effect of the benzodiazepine, triazolam.
  • Telaprevir Telaprevir increases levels by affecting CYP3A4 metabolism. Concomitant therapy is contraindicated.
  • Telithromycin Telithromycin may increase the effect and toxicity of the benzodiazepine, triazolam.
  • Tipranavir Tipranavir, co-administered with Ritonavir, may increase the plasma concentration of Triazolam. Concomitant therapy is contraindicated.
  • Triprolidine The CNS depressants, Triprolidine and Triazolam, 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 Triazolam by decreasing its metabolism. Avoid concomitant therapy if possible or consider a dose reduction in the initial dose of Triazolam.
  • Voriconazole Voriconazole may increase the serum concentration of triazolam by decreasing its metabolism. Monitor for triazolam toxicity if voriconazole is initiated or dose increased.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00897
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5556
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509147
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00387
ChemSpider
http://www.chemspider.com/Chemical-Structure.5355.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0054-4858-51
PharmGKB
http://www.pharmgkb.org/drug/PA451753
Wikipedia
http://en.wikipedia.org/wiki/Triazolam
RxList
http://www.rxlist.com/cgi/generic/triazolam.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/hal1192.shtml
Drugs.com
http://www.drugs.com/cdi/triazolam.html
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