Tìm theo
Perphenazine
Các tên gọi khác (15 ) :
  • 2-(4-[3-(2-chloro-10H-Phenothiazin-10-yl)propyl]-1-piperazinyl)ethanol
  • 2-chloro-10-(3-(4-(2-Hydroxyethyl)piperazin-1-yl)propyl)phenothiazine
  • 4-[3-(2-chloro-10H-Phenothiazin-10-yl)propyl]-1-piperazineethanol
  • 4-[3-(2-Chlorophenothiazin-10-yl)propyl]-1-piperazineethanol
  • Chlorpiprazine
  • Etaperazin
  • Etaperazine
  • Ethaperazine
  • gamma-(4-(beta-Hydroxyethyl)piperazin-1-yl)propyl-2-chlorophenothiazine
  • Perfenazina
  • Perfenazine
  • Perphenazin
  • Perphénazine
  • Perphenazinum
  • Trilafon
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 58-39-9
ATC: N05AB03
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C21H26ClN3OS
PTK: 403.969
An antipsychotic phenothiazine derivative with actions and uses similar to those of chlorpromazine. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H26ClN3OS
Phân tử khối
403.969
Monoisotopic mass
403.148510866
InChI
InChI=1S/C21H26ClN3OS/c22-17-6-7-21-19(16-17)25(18-4-1-2-5-20(18)27-21)9-3-8-23-10-12-24(13-11-23)14-15-26/h1-2,4-7,16,26H,3,8-15H2
InChI Key
InChIKey=RGCVKNLCSQQDEP-UHFFFAOYSA-N
IUPAC Name
2-{4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazin-1-yl}ethan-1-ol
Traditional IUPAC Name
perphenazine
SMILES
OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(Cl)C=C3)CC1
Độ tan chảy
97 °C
Độ sôi
278-281 °C at 1.00E+00 mm Hg
Độ hòa tan
28.3 mg/L (at 24 °C)
logP
4.20
logS
-4.16
pKa (strongest acidic)
15.59
pKa (Strongest Basic)
8.21
PSA
29.95 Å2
Refractivity
116.1 m3·mol-1
Polarizability
44.77 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
4
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
pKa
7.94
Dược Lực Học : Perphenazine is a piperazinyl phenothiazine, acts on the central nervous system, and has a greater behavioral potency than other phenothiazine derivatives whose side chains do not contain a piperazine moiety. It is a member of a class of drugs called phenothiazines, which are dopamine D1/D2 receptor antagonists. Perphenazine is 10 to 15 times as potent as chlorpromazine; that means perphenazine is a highly potent antipsychotic. In equivalent doses it has approximately the same frequency and severity of early and late extrapypramidal side-effects compared to Haloperidol.
Cơ Chế Tác Dụng : An antipsychotic phenothiazine derivative with actions and uses similar to those of chlorpromazine. [PubChem] 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 and vomiting centre. Perphenazine also binds the alpha andrenergic receptor. This receptor's action is mediated by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Dược Động Học :
▧ Absorption :
Absolute bioavailability is 40% following oral administration.
▧ Metabolism :
Hepatic.
▧ Route of Elimination :
Perphenazine is extensively metabolized in the liver to a number of metabolites by sulfoxidation, hydroxylation, dealkylation, and glucuronidation.
▧ Half Life :
8-12 hours, but ranges up to 20 hours.
Độc Tính : Symptoms of overdose include stupor or coma, and children may have convulsive seizures. Signs of arousal may not occur for 48 hours. Oral LD50=318 mg/kg (rat); IPR LD50=64 mg/kg (mouse)
Chỉ Định : For use in the management of the manifestations of psychotic disorders and for the control of severe nausea and vomiting in adults.
Tương Tác Thuốc :
  • Amphetamine Decreased anorexic effect, may increase psychotic symptoms
  • Atomoxetine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • 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 Perphenazine 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, Perphenazine, 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.
  • Terbinafine Terbinafine may reduce the metabolism and clearance of Perphenazine. Consider alternate therapy or monitor for therapeutic/adverse effects of Perphenazine if Terbinafine is initiated, discontinued or dose changed.
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
  • Tetrabenazine May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
  • Trimethobenzamide Trimethobenzamide and Perphenazine, 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, Perphenazine. 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 Perphenazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Liquid - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Merck
    Sản phẩm biệt dược : Decentan
  • Công ty :
    Sản phẩm biệt dược : Emesinal
  • Công ty : Mercury
    Sản phẩm biệt dược : Fentazin
  • Công ty : Taro
    Sản phẩm biệt dược : Perphenan
  • Sản phẩm biệt dược : PZC
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Trilafon
  • Công ty :
    Sản phẩm biệt dược : Trilifan
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00850
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4748
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507058
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07427
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00503
ChemSpider
http://www.chemspider.com/Chemical-Structure.4586.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0781-1046-01
PharmGKB
http://www.pharmgkb.org/drug/PA450882
Wikipedia
http://en.wikipedia.org/wiki/Perphenazine
RxList
http://www.rxlist.com/cgi/generic3/perphenazine.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/tri1616.shtml
Drugs.com
http://www.drugs.com/cdi/perphenazine.html
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