Tìm theo
Trifluoperazine
Các tên gọi khác (8 ) :
  • 10-[3-(4-Methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)-10H-phenothiazine
  • 10-[3-(4-METHYL-piperazin-1-yl)-propyl]-2-trifluoromethyl-10H-phenothiazine
  • Trifluoperazina
  • Trifluoperazine
  • Trifluoperazinum
  • Trifluoromethyl-10-(3'-(1-methyl-4-piperazinyl)propyl)phenothiazine
  • Trifluoroperazine
  • Trifluperazine
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 117-89-5
ATC: N05AB06
ĐG : Apotheca Inc.
CTHH: C21H24F3N3S
PTK: 407.496
A phenothiazine with actions similar to chlorpromazine. It is used as an antipsychotic and an antiemetic. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H24F3N3S
Phân tử khối
407.496
Monoisotopic mass
407.164303088
InChI
InChI=1S/C21H24F3N3S/c1-25-11-13-26(14-12-25)9-4-10-27-17-5-2-3-6-19(17)28-20-8-7-16(15-18(20)27)21(22,23)24/h2-3,5-8,15H,4,9-14H2,1H3
InChI Key
InChIKey=ZEWQUBUPAILYHI-UHFFFAOYSA-N
IUPAC Name
10-[3-(4-methylpiperazin-1-yl)propyl]-2-(trifluoromethyl)-10H-phenothiazine
Traditional IUPAC Name
trifluoperazine
SMILES
CN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1
Độ hòa tan
12.2 mg/L (at 24 °C)
logP
5.03
logS
-4.52
pKa (Strongest Basic)
8.39
PSA
9.72 Å2
Refractivity
110.98 m3·mol-1
Polarizability
41.94 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Trifluoperazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Trifluoperazine has not been shown effective in the management of behaviorial complications in patients with mental retardation.
Cơ Chế Tác Dụng : A phenothiazine with actions similar to chlorpromazine. It is used as an antipsychotic and an antiemetic. [PubChem] Trifluoperazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.
Dược Động Học :

▧ Metabolism :
Hepatic.
▧ Half Life :
10-20 hours
Độc Tính : Symptoms of overdose include agitation, coma, convulsions, difficulty breathing, difficulty swallowing, dry mouth, extreme sleepiness, fever, intestinal blockage, irregular heart rate, low blood pressure, and restlessness.
Chỉ Định : For the treatment of anxiety disorders, depressive symptoms secondary to anxiety and agitation.
Tương Tác Thuốc :
  • Amphetamine Decreased anorexic effect, may increase psychotic symptoms
  • Benzphetamine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
  • Bromocriptine The phenothiazine decreases the effect of bromocriptine
  • Cisapride Increased risk of cardiotoxicity and arrhythmias
  • Dexfenfluramine Decreased anorexic effect, may increase psychotic symptoms
  • Dextroamphetamine Decreased anorexic effect, may increase psychotic symptoms
  • Diethylpropion Decreased anorexic effect, may increase psychotic symptoms
  • Donepezil Possible antagonism of action
  • Fenfluramine Decreased anorexic effect, may increase psychotic symptoms
  • Galantamine Possible antagonism of action
  • Gatifloxacin Increased risk of cardiotoxicity and arrhythmias
  • Grepafloxacin Increased risk of cardiotoxicity and arrhythmias
  • Guanethidine Trifluoperazine may decrease the effect of guanethidine.
  • Levofloxacin Increased risk of cardiotoxicity and arrhythmias
  • Mazindol Decreased anorexic effect, may increase psychotic symptoms
  • Methamphetamine Decreased anorexic effect, may increase psychotic symptoms
  • Metrizamide Increased risk of convulsions
  • Phendimetrazine Decreased anorexic effect, may increase psychotic symptoms
  • Phenmetrazine Decreased anorexic effect, may increase psychotic symptoms
  • Phentermine Decreased anorexic effect, may increase psychotic symptoms
  • Phenylpropanolamine Decreased anorexic effect, may increase psychotic symptoms
  • Rivastigmine Possible antagonism of action
  • Sparfloxacin Increased risk of cardiotoxicity and arrhythmias
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Trifluoperazine, 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.
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
  • Tetrabenazine May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
  • Thiabendazole The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Trifluoperazine by decreasing Trifluoperazine metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Trifluoperazine if Thiabendazole is initiated, discontinued or dose changed.
  • Trimethobenzamide Trimethobenzamide and Trifluoperazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine The antihistamine, Triprolidine, may increase the arrhythmogenic effect of the phenothiazine, Trifluoperazine. Monitor for symptoms of ventricular arrhythmias. Additive anticholinergic and CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
  • Trospium Trospium and Trifluoperazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Syrup - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Eskazine
  • Công ty :
    Sản phẩm biệt dược : Eskazinyl
  • Công ty :
    Sản phẩm biệt dược : Jatroneural
  • Công ty :
    Sản phẩm biệt dược : Modalina
  • Công ty :
    Sản phẩm biệt dược : Stelazine
  • Công ty :
    Sản phẩm biệt dược : Terfluzine
  • Công ty :
    Sản phẩm biệt dược : Trifluoperaz
  • Công ty :
    Sản phẩm biệt dược : Triftazin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00831
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5566
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507961
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07168
ChemSpider
http://www.chemspider.com/Chemical-Structure.5365.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50001886
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-2401-01
PharmGKB
http://www.pharmgkb.org/drug/PA451771
Wikipedia
http://en.wikipedia.org/wiki/Trifluoperazine
RxList
http://www.rxlist.com/cgi/generic3/trifluo.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/tri1412.shtml
Drugs.com
http://www.drugs.com/cdi/trifluoperazine.html
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