Tìm theo
Alprazolam
Các tên gọi khác (3) :
  • 8-Chloro-1-methyl-6-phenyl-4H-S-triazolo(4,3-a)(1,4)benzodiazepine
  • Alprazolam
  • Xanax
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 28981-97-7
ATC: N05BA12
ĐG : Actavis Group , http://www.actavis.com
CTHH: C17H13ClN4
PTK: 308.765
A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of panic disorders, with or without agoraphobia, and in generalized anxiety disorders. (From AMA Drug Evaluations Annual, 1994, p238)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H13ClN4
Phân tử khối
308.765
Monoisotopic mass
308.082874143
InChI
InChI=1S/C17H13ClN4/c1-11-20-21-16-10-19-17(12-5-3-2-4-6-12)14-9-13(18)7-8-15(14)22(11)16/h2-9H,10H2,1H3
InChI Key
InChIKey=VREFGVBLTWBCJP-UHFFFAOYSA-N
IUPAC Name
12-chloro-3-methyl-9-phenyl-2,4,5,8-tetraazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,8,11,13-hexaene
Traditional IUPAC Name
alprazolam
SMILES
CC1=NN=C2CN=C(C3=CC=CC=C3)C3=C(C=CC(Cl)=C3)N12
Độ tan chảy
228-229.5 °C
Độ hòa tan
40 mg/L at pH 7; 12 mg/mL at pH 1.2
logP
2.12
logS
-4
pKa (strongest acidic)
18.3
pKa (Strongest Basic)
5.08
PSA
43.07 Å2
Refractivity
98.88 m3·mol-1
Polarizability
32.22 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 : Alprazolam, a benzodiazepine, is used to treat panic disorder and anxiety disorder. Unlike chlordiazepoxide, clorazepate, and prazepam, alprazolam has a shorter half-life and metabolites with minimal activity. Like other triazolo benzodiazepines such as triazolam, alprazolam may have significant drug interactions involving the hepatic cytochrome P-450 3A4 isoenzyme. Clinically, all benzodiazepines cause a dose-related central nervous system depressant activity varying from mild impairment of task performance to hypnosis. Unlike other benzodiazepines, alprazolam may also have some antidepressant activity, although clinical evidence of this is lacking.
Cơ Chế Tác Dụng : A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of panic disorders, with or without agoraphobia, and in generalized anxiety disorders. (From AMA Drug Evaluations Annual, 1994, p238) Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, 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 :
Readily absorbed from the gastrointestinal tract. Bioavailability is 80-90%.
▧ Protein binding :
80% (mainly to albumin)
▧ Metabolism :
Hepatic. Hydroxylated in the liver to α-hydroxyalprazolam, which is also active. This and other metabolites are later excreted in urine as glucuronides.
▧ Route of Elimination :
Alprazolam and its metabolites are excreted primarily in the urine.
▧ Half Life :
6.3-26.9 hours
▧ Clearance :
* 2.13 +/- 0.54 mL/min/kg [CYP3A inducers] * 0.90 +/- 0.21 mL/min/kg [without CYP3A inducers]
Độc Tính : Oral, mouse: LD50=1020 mg/kg. Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time.
Chỉ Định : For the management of anxiety disorder or the short-term relief of symptoms of anxiety and for the treatment of panic disorder, with or without agoraphobia.
Tương Tác Thuốc :
  • Amprenavir Amprenavir may increase the effect and toxicity of the benzodiazepine, alprazolam.
  • Aprepitant Aprepitant may increase the effect and toxicity of the benzodiazepine, alprazolam.
  • Carbamazepine Carbamazepine may decrease the effect of the benzodiazepine, alprazolam.
  • Cimetidine Cimetidine may increase the effect of the benzodiazepine, alprazolam.
  • Clarithromycin The macrolide, clarithromycin, may increase the effect of the benzodiazepine, alprazolam.
  • Clozapine Increased risk of toxicity
  • Delavirdine The antiviral agent, delavirdine, may increase the effect and toxicity of the benzodiazepine, alprazolam.
  • Digoxin The benzodiazepine, alprazolam, may increase the effect of digoxin.
  • Efavirenz The antiviral agent, efavirenz, may increase the effect and toxicity of the benzodiazepine, alprazolam.
  • Erythromycin The macrolide, erythromycin, may increase the effect of the benzodiazepine, alprazolam.
  • Ethotoin Ethotoin may increase the metabolism of alprazolam via CYP3A4.
  • Fluconazole Fluconazole may increase the effect of the benzodiazepine, alprazolam.
  • Fosamprenavir Fosamprenavir may increase the effect and toxicity of the benzodiazepine, alprazolam.
  • Fosphenytoin Fosphenytoin may increase the metabolism of alprazolam via CYP3A4.
  • Indinavir The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, alprazolam.
  • Itraconazole Itraconazole may increase the effect of the benzodiazepine, alprazolam.
  • Josamycin The macrolide, josamycin, may increase the effect of the benzodiazepine, alprazolam.
  • Kava Kava may increase the effect of the benzodiazepine, alprazolam.
  • Ketoconazole Ketoconazole may increase the effect of the benzodiazepine, alprazolam.
  • Mephenytoin Mephenytoin may increase the metabolism of alprazolam via CYP3A4.
  • Nelfinavir The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, alprazolam.
  • Omeprazole Omeprazole may increase the effect of the benzodiazepine, alprazolam.
  • Phenytoin Phenytoin may increase the metabolism of alprazolam via CYP3A4.
  • Ritonavir The protease inhibitor, ritonavir, may increase the effect of the benzodiazepine, alprazolam.
  • Saquinavir The protease inhibitor, saquinavir, may increase the effect of the benzodiazepine, alprazolam.
  • St. John's Wort St. John's Wort may decrease the effect of the benzodiazepine, alprazolam.
  • Telaprevir Telaprevir inhibits systemic metabolism of alprazolam and dose adjustment may be necessary.
  • Telithromycin Telithromycin may increase the effect and toxicity of the benzodiazepine, alprazolam.
  • Tipranavir Tipranavir may decrease the metabolism and clearance of Alprazolam. Consider alternate therapy or monitor for Alprazolam toxic effects if Tipranavir is initiated or dose increased.
  • Triprolidine The CNS depressants, Triprolidine and Alprazolam, 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 alprazolam by decreasing its metabolism. Monitor for alprazolam toxicity if voriconazole is initiated or dose increased.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Alplax
  • Công ty :
    Sản phẩm biệt dược : Alprazolan
  • Công ty :
    Sản phẩm biệt dược : Alpronax
  • Công ty :
    Sản phẩm biệt dược : Alprox
  • Công ty :
    Sản phẩm biệt dược : Alviz
  • Công ty :
    Sản phẩm biệt dược : Cassadan
  • Công ty :
    Sản phẩm biệt dược : Esparon
  • Công ty :
    Sản phẩm biệt dược : Niravam
  • Công ty :
    Sản phẩm biệt dược : Ralozam
  • Công ty :
    Sản phẩm biệt dược : Restyl
  • Công ty :
    Sản phẩm biệt dược : Solanax
  • Công ty :
    Sản phẩm biệt dược : Tafil
  • Công ty :
    Sản phẩm biệt dược : Trankimazin
  • Công ty :
    Sản phẩm biệt dược : Tranquinal
  • Công ty : Upjohn
    Sản phẩm biệt dược : Xanax
  • Công ty : Upjohn
    Sản phẩm biệt dược : Xanax XR
  • Công ty :
    Sản phẩm biệt dược : Xanor
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00404
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2118
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507078
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06817
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00225
ChemSpider
http://www.chemspider.com/Chemical-Structure.2034.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/64980-140-06
PharmGKB
http://www.pharmgkb.org/drug/PA448333
Wikipedia
http://en.wikipedia.org/wiki/Alprazolam
RxList
http://www.rxlist.com/cgi/generic/alpraz.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/xan1491.shtml
Drugs.com
http://www.drugs.com/alprazolam.html
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