Tìm theo
Triflupromazine
Các tên gọi khác (8 ) :
  • 10-(3-(Dimethylamino)propyl)-2-(trifluoromethyl)phenothiazine
  • 2-(Trifluoromethyl)promazine
  • 2-Trifluoromethyl-10-(gamma-dimethylaminopropyl)phenothiazine
  • Fluopromazine
  • Triflupromazin
  • Triflupromazina
  • Triflupromazine
  • Triflupromazinum
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 146-54-3
CTHH: C18H19F3N2S
PTK: 352.417
A phenothiazine used as an antipsychotic agent and as an antiemetic. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H19F3N2S
Phân tử khối
352.417
Monoisotopic mass
352.122103923
InChI
InChI=1S/C18H19F3N2S/c1-22(2)10-5-11-23-14-6-3-4-7-16(14)24-17-9-8-13(12-15(17)23)18(19,20)21/h3-4,6-9,12H,5,10-11H2,1-2H3
InChI Key
InChIKey=XSCGXQMFQXDFCW-UHFFFAOYSA-N
IUPAC Name
dimethyl({3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl})amine
Traditional IUPAC Name
triflupromazine
SMILES
CN(C)CCCN1C2=CC=CC=C2SC2=C1C=C(C=C2)C(F)(F)F
Độ hòa tan
1.80e-03 g/l
logP
5.54
logS
-5.3
pKa (Strongest Basic)
9.2
PSA
6.48 Å2
Refractivity
94.93 m3·mol-1
Polarizability
35.29 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Triflupromazine is a member of a class of drugs called phenthiazines, which are dopamine D1/D2 receptor antagonists. Phenothiazines are used to treat serious mental and emotional disorders, including schizophrenia and other psychotic disorders. It reduces anxiety, emotional withdrawal, hallucinations, disorganized thoughts, blunted mood, and suspiciousness. Triflupromazine is used particularly to control violent behavior during acute episodes of psychotic disorders. It can also be used to control severe nausea and vomiting, severe hiccups, and moderate to severe pain in some hospitalized patients. Triflupromazine acts on the central nervous system.
Cơ Chế Tác Dụng : A phenothiazine used as an antipsychotic agent and as an antiemetic. [PubChem] Triflupromazine binds to the dopamine D1 and dopamine D2 receptors and inhibits their activity. The mechanism of the anti-emetic effect is due predominantly to blockage of the dopamine D2 neurotransmitter receptors in the chemoreceptor trigger zone (CTZ) and vomiting centre. Triflupromazine blocks the neurotransmitter dopamine and the vagus nerve in the gastrointestinal tract. Triflupromazine also binds the muscarinic acetylcholine receptors (M1 and M2) and the tryptamine D receptors (5HT2B).
Dược Động Học :
▧ Absorption :
Absorption may be erratic and peak plasma concentrations show large interindividual differences.
▧ Protein binding :
Very high (90% or more).
▧ Metabolism :
Hepatic.
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 : Used mainly in the management of psychoses. Also used to control nausea and vomiting.
Tương Tác Thuốc :
  • Bromocriptine The phenothiazine decreases the effect of bromocriptine
  • Cisapride Increased risk of cardiotoxicity and arrhythmias
  • Dexfenfluramine 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 Triflupromazine may decrease the effect of guanethidine.
  • Levofloxacin Increased risk of cardiotoxicity and arrhythmias
  • Mazindol Decreased anorexic effect, may increase psychotic symptoms
  • Phentermine Decreased anorexic effect, may increase psychotic symptoms
  • Phenylpropanolamine Decreased anorexic effect, may increase psychotic symptoms
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00508
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5568
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507344
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00390
ChemSpider
http://www.chemspider.com/Chemical-Structure.5367.html
PharmGKB
http://www.pharmgkb.org/drug/PA451773
Wikipedia
http://en.wikipedia.org/wiki/Triflupromazine
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