Tìm theo
Prochlorperazine
Các tên gọi khác (17 ) :
  • 2-Chloro-10-(3-(1-methyl-4-piperazinyl)propyl)-phenothiazine
  • 2-Chloro-10-(3-(4-methyl-1-piperazinyl)propyl)phenothiazine
  • 3-Chloro-10-(3-(1-methyl-4-piperazinyl)propyl)phenothiazine
  • 3-Chloro-10-(3-(4-methyl-1-piperazinyl)propyl)phenothiazine
  • Capazine
  • Chlormeprazine
  • Chloro-3 (N-methylpiperazinyl-3 propyl)-10 phenothiazine
  • Chloropernazine
  • Emetiral
  • N-(gamma-(4'-Methylpiperazinyl-1')propyl)-3-chlorophenothiazine
  • Prochlorperazin
  • Prochlorpérazine
  • Prochlorperazinum
  • Prochlorpermazine
  • Prochlorpromazine
  • Procloperazine
  • Proclorperazina
Thuốc đường tiêu hóa
Thuốc Gốc
Small Molecule
CAS: 58-38-8
ATC: N05AB04
ĐG : Apotheca Inc.
CTHH: C20H24ClN3S
PTK: 373.943
A phenothiazine antipsychotic used principally in the treatment of nausea; vomiting; and vertigo. It is more likely than chlorpromazine to cause extrapyramidal disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C20H24ClN3S
Phân tử khối
373.943
Monoisotopic mass
373.13794618
InChI
InChI=1S/C20H24ClN3S/c1-22-11-13-23(14-12-22)9-4-10-24-17-5-2-3-6-19(17)25-20-8-7-16(21)15-18(20)24/h2-3,5-8,15H,4,9-14H2,1H3
InChI Key
InChIKey=WIKYUJGCLQQFNW-UHFFFAOYSA-N
IUPAC Name
2-chloro-10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine
Traditional IUPAC Name
prochlorperazine
SMILES
CN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(Cl)C=C3)CC1
Độ tan chảy
228 °C
Độ hòa tan
15 mg/L (at 24 °C)
logP
4.88
logS
-4.4
pKa (Strongest Basic)
8.39
PSA
9.72 Å2
Refractivity
109.81 m3·mol-1
Polarizability
41.77 Å3
Rotatable Bond Count
4
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
pKa
8.1
Dược Lực Học : Prochlorperazine is a piperazine phenothiazine related to high-potency neuroleptics such as perphenazine. It shares many of the actions and adverse effects of the antipsychotics.
Cơ Chế Tác Dụng : A phenothiazine antipsychotic used principally in the treatment of nausea; vomiting; and vertigo. It is more likely than chlorpromazine to cause extrapyramidal disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612) The mechanism of action of prochlorperazine has not been fully determined, but may be primarily related to its antidopaminergic effects. Prochlorperazine blocks the D2 somatodendritic autoreceptor, resulting in the blockade of postsynaptic dopamine receptors in the mesolimbic system and an increased dopamine turnover. Prochlorperazine also has anti-emetic effects, which can be attributed to dopamine blockade in the chemoreceptor trigger zone. Prochlorperazine also blocks anticholinergic and alpha-adrenergic receptors, the blockade of alpha(1)-adrenergic receptors resulting in sedation, muscle relaxation, and hypotension.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration
▧ Protein binding :
91-99%
▧ Metabolism :
Hepatic. Undergoes metabolism in the gastric mucosa and on first pass through the liver, CYP2D6 and/or CYP3A4.
▧ Half Life :
6 to 8 hours
Độc Tính : Symptoms of central nervous system depression to the point of somnolence or coma. Agitation and restlessness may also occur. Other possible manifestations include convulsions, EKG changes and cardiac arrhythmias, fever and autonomic reactions such as hypotension, dry mouth and ileus; LD50=400mg/kg (orally in mice)
Chỉ Định : For the symptomatic management of psychotic disorders, short term management of nonpsychotic anxiety in patients with generalized anxiety disorder, and for the control of severe nausea and vomiting of various causes.
Tương Tác Thuốc :
  • Amphetamine Decreased anorexic effect, may increase pyschotic 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 pyschotic 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 Prochlorperazine 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 pyschotic symptoms
  • Metrizamide Increased risk of convulsions
  • Phendimetrazine Decreased anorexic effect, may increase pyschotic symptoms
  • Phenmetrazine Decreased anorexic effect, may increase pyschotic 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, Prochlorperazine, 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.
  • Trimethobenzamide Trimethobenzamide and Prochlorperazine, 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, Prochlorperazine. 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 Prochlorperazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Liquid - Intravenous
Solution - Intravenous
Suppository - Rectal
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Sản phẩm biệt dược : Buccastem
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Compazine
  • Công ty : Paddock
    Sản phẩm biệt dược : Compro
  • Công ty : Zentiva
    Sản phẩm biệt dược : Emetiral
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Stemetil
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Stemzine
  • Công ty : Chin Teng
    Sản phẩm biệt dược : Volimin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00433
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4917
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509018
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07403
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00493
ChemSpider
http://www.chemspider.com/Chemical-Structure.4748.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0574-7226-12
PharmGKB
http://www.pharmgkb.org/drug/PA451114
Wikipedia
http://en.wikipedia.org/wiki/Prochlorperazine
RxList
http://www.rxlist.com/cgi/generic/prochlr.htm
Drugs.com
http://www.drugs.com/cdi/prochlorperazine.html
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