Tìm theo
Flupentixol
Các tên gọi khác (7 ) :
  • Flupenthixol
  • Flupenthixole
  • Flupentixol
  • Flupentixol
  • Flupentixol
  • Flupentixolo
  • Flupentixolum
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 2709-56-0
CTHH: C23H27F3N2OS
PTK: 436.533
Flupentixol is an antipsychotic neuroleptic drug. It is a thioxanthene, and therefore closely related to the phenothiazines. Its primary use is as a long acting injection given two or three weekly to people with schizophrenia who have a poor compliance with medication and suffer frequent relapses of illness. It is a D1 and D2 receptor antagonist. It is not approved in the United States.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C23H27F3N2OS
Phân tử khối
436.533
Monoisotopic mass
436.179618801
InChI
InChI=1S/C23H27F3N2OS/c24-23(25,26)17-7-8-22-20(16-17)18(19-4-1-2-6-21(19)30-22)5-3-9-27-10-12-28(13-11-27)14-15-29/h1-2,4-8,16,20,22,29H,3,9-15H2/b18-5-
InChI Key
InChIKey=DTTVNHWDONBIKE-DVZOWYKESA-N
IUPAC Name
2-(4-{3-[2-(trifluoromethyl)-9,9a-dihydro-4aH-thioxanthen-9-ylidene]propyl}piperazin-1-yl)ethan-1-ol
Traditional IUPAC Name
flupenthixol
SMILES
[H]C(CCN1CCN(CCO)CC1)=C1C2C=C(C=CC2SC2=C1C=CC=C2)C(F)(F)F
Độ hòa tan
0.000346 mg/ml
logP
4.51
logS
-5.2
pKa (strongest acidic)
15.59
pKa (Strongest Basic)
8.51
PSA
26.71 Å2
Refractivity
120.93 m3·mol-1
Polarizability
45.28 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Flupenthixol is an anxiolytic, antidepressive agent and a mood stabilizer. It inhibits the central monoamine receptors, particularly the dopamine D1 and D2 receptors. Therefore, it increases the amount of serotonin and noradrenaline that control mood and thinking, and improves mood.
Cơ Chế Tác Dụng : Flupentixol is an antipsychotic neuroleptic drug. It is a thioxanthene, and therefore closely related to the phenothiazines. Its primary use is as a long acting injection given two or three weekly to people with schizophrenia who have a poor compliance with medication and suffer frequent relapses of illness. It is a D1 and D2 receptor antagonist. It is not approved in the United States. Flupenthixol is a thioxanthene antipsychotic. The mechanism of action of Flupenthixol is not completely understood. Flupenthixol is a powerful antagonist of both D1 and D2 dopamine receptors, and an alpha-adrenergic receptor antagonist. It's antipsychotic activity is thought to be related to blocks postsynaptic dopamine receptors in the CNS.
Dược Động Học :
▧ Absorption :
Fairly slow and incomplete after oral administration
▧ Protein binding :
Highly bound to plasma proteins (>95%)
▧ Metabolism :
Mainly hepatic
▧ Half Life :
19 to 39 hours
Độc Tính : LD50=300 mk/kg (Oral in mice); LD50=791 mg/kg (Oral in rats); LD50=87 mk/kg (IV in mice); LD50=37 mg/kg (IV in rats)
Chỉ Định : For use in the treatment of schizophrenia and depression
Tương Tác Thuốc :
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Rivastigmine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Flupenthixol, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Tetrabenazine May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects. Similar pharmacologic properties thus combination therapy will worsen the severity of sedative, parkinsonian, and extrapyramidal adverse effects.
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Trimethobenzamide Trimethobenzamide and Flupenthixol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Triprolidine Triprolidine and Flupenthixol, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
  • Trospium Trospium and Flupenthixol, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Lundbeck A/S
    Sản phẩm biệt dược : Depixol
  • Công ty : Lundbeck A/S
    Sản phẩm biệt dược : Fluanxol
  • Công ty : Johnson
    Sản phẩm biệt dược : Jexit
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00875
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01044
PharmGKB
http://www.pharmgkb.org/drug/PA10268
Wikipedia
http://en.wikipedia.org/wiki/Flupenthixol
Drugs.com
http://www.drugs.com/international/flupentixol.html
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