Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
386.026759579
InChI
InChI=1S/C17H11ClF4N2S/c18-10-5-6-14-12(7-10)16(11-3-1-2-4-13(11)19)23-8-15(25)24(14)9-17(20,21)22/h1-7H,8-9H2
InChI Key
InChIKey=IKMPWMZBZSAONZ-UHFFFAOYSA-N
IUPAC Name
7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-2,3-dihydro-1H-1,4-benzodiazepine-2-thione
Traditional IUPAC Name
quazepam
SMILES
FC1=CC=CC=C1C1=NCC(=S)N(CC(F)(F)F)C2=C1C=C(Cl)C=C2
pKa (strongest acidic)
18.93
pKa (Strongest Basic)
2.59
Refractivity
93.47 m3·mol-1
Dược Lực Học :
Quazepam is a benzodiazepine derivative. The main pharmacological action of quazepam is the enhancement of the neurotransmitter, GABA at the GABAA receptor.
Cơ Chế Tác Dụng :
Quazepam is a drug which is a benzodiazepine derivative. It induces impairment of motor function and has hypnotic properties. Quazepam is used to treat insomnia.
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 :
Bioavailability is 29-35% following oral administration.
▧ Metabolism :
Hepatic.
▧ Half Life :
39 hours
Chỉ Định :
Used to treat insomnia.
Tương Tác Thuốc :
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Cimetidine
Cimetidine may increase the effect of the benzodiazepine, quazepam.
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Clozapine
Increased risk of toxicity
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Fluconazole
Fluconazole may increase the effect of the benzodiazepine, quazepam.
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Indinavir
The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, quazepam.
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Itraconazole
Itraconazole may increase the effect of the benzodiazepine, quazepam.
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Ketoconazole
Ketoconazole may increase the effect of the benzodiazepine, quazepam.
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Nelfinavir
The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, quazepam.
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Omeprazole
Omeprazole may increase the effect of the benzodiazepine, quazepam.
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Tipranavir
Tipranavir may decrease the metabolism and clearance of Quazepam. Consider alternate therapy or monitor for Quazepam toxic effects if Tipranavir is initiated or dose increased.
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Triprolidine
The CNS depressants, Triprolidine and Quazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng :
Tablet - Oral