Tìm theo
Thioridazine
Các tên gọi khác (16 ) :
  • 10-[2-(1-Methyl-2-piperidyl)ethyl]-2-methylsulfanyl-phenothiazine
  • 2-Methylmercapto-10-(2-(N-methyl-2-piperidyl)ethyl)phenothiazine
  • 3-Methylmercapto-N-(2'-(N-methyl-2-piperidyl)ethyl)phenothiazine
  • Mallorol
  • Malloryl
  • Meleril
  • Mellaril
  • Mellaril-S
  • Mellerets
  • Mellerette
  • Melleril
  • Orsanil
  • Sonapax
  • Thioridazin
  • Thioridazinum
  • Tioridazina
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 50-52-2
ATC: N05AC02
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C21H26N2S2
PTK: 370.575
A phenothiazine antipsychotic used in the management of psychoses, including schizophrenia, and in the control of severely disturbed or agitated behavior. It has little antiemetic activity. Thioridazine has a higher incidence of antimuscarinic effects, but a lower incidence of extrapyramidal symptoms, than chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p618)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H26N2S2
Phân tử khối
370.575
Monoisotopic mass
370.153740222
InChI
InChI=1S/C21H26N2S2/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(24-2)15-19(21)23/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3
InChI Key
InChIKey=KLBQZWRITKRQQV-UHFFFAOYSA-N
IUPAC Name
10-[2-(1-methylpiperidin-2-yl)ethyl]-2-(methylsulfanyl)-10H-phenothiazine
Traditional IUPAC Name
thioridazine
SMILES
CSC1=CC2=C(SC3=CC=CC=C3N2CCC2CCCCN2C)C=C1
Độ tan chảy
73 °C
Độ sôi
230 °C at 2.00E-02 mm Hg
Độ hòa tan
0.0336 mg/L
logP
5.90
logS
-5.6
pKa (Strongest Basic)
8.93
PSA
6.48 Å2
Refractivity
113.52 m3·mol-1
Polarizability
43.26 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Ghose Filter
true
pKa
9.5
Dược Lực Học : Thioridazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Thioridazine has not been shown effective in the management of behaviorial complications in patients with mental retardation.
Cơ Chế Tác Dụng : A phenothiazine antipsychotic used in the management of psychoses, including schizophrenia, and in the control of severely disturbed or agitated behavior. It has little antiemetic activity. Thioridazine has a higher incidence of antimuscarinic effects, but a lower incidence of extrapyramidal symptoms, than chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p618) Thioridazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; blocks alpha-adrenergic effect, 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 :
▧ Absorption :
60%
▧ Protein binding :
95%
▧ Metabolism :
Hepatic
▧ Half Life :
21-25 hours
Độc Tính : LD50=956-1034 mg/kg (Orally in rats); Agitation, blurred vision, coma, confusion, constipation, difficulty breathing, dilated or constricted pupils, diminished flow of urine, dry mouth, dry skin, excessively high or low body temperature, extremely low blood pressure, fluid in the lungs, heart abnormalities, inability to urinate, intestinal blockage, nasal congestion, restlessness, sedation, seizures, shock
Chỉ Định : For the treatment of schizophrenia and generalized anxiety disorder.
Tương Tác Thuốc :
  • Abiraterone Abiraterone increases levels by affecting CYP2D6 metabolism. Interaction is significant so monitor closely.
  • Amiodarone Increased risk of cardiotoxicity and arrhythmias
  • Amitriptyline Increased risk of cardiotoxicity and arrhythmias
  • Amphetamine Decreased anorexic effect, may increase psychotic symptoms
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy is contraindicated.
  • Asenapine Thioridazine is a CYP2D6 substrate in which concomitant therapy with asenapine will increase serum levels of thioridazine. Consider alternative therapy.
  • Astemizole Increased risk of cardiotoxicity and arrhythmias
  • 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.
  • Benzylpenicillin Increased risk of cardiotoxicity and arrhythmias
  • Bretylium Increased risk of cardiotoxicity and arrhythmias
  • Bromocriptine The phenothiazine decreases the effect of bromocriptine
  • Bupropion Bupropion may increase the effect and toxicity of thioridazine.
  • Chloroquine Increased risk of cardiotoxicity and arrhythmias
  • Chlorpromazine Increased risk of cardiotoxicity and arrhythmias
  • Cisapride Increased risk of cardiotoxicity and arrhythmias
  • Crizotinib Concurrent use with drugs that prolong QTc interval is contraindicated.
  • Dexfenfluramine Decreased anorexic effect, may increase psychotic symptoms
  • Dextroamphetamine Decreased anorexic effect, may increase psychotic symptoms
  • Diethylpropion Decreased anorexic effect, may increase psychotic symptoms
  • Diltiazem Increased risk of cardiotoxicity and arrhythmias
  • Diphenhydramine Increased risk of cardiotoxicity and arrhythmias
  • Disopyramide Increased risk of cardiotoxicity and arrhythmias
  • Dofetilide Increased risk of cardiotoxicity and arrhythmias
  • Donepezil Possible antagonism of action
  • Doxepin Increased risk of cardiotoxicity and arrhythmias
  • Duloxetine Increased risk of cardiotoxicity and arrhythmias
  • Erythromycin Increased risk of cardiotoxicity and arrhythmias
  • Fenfluramine Decreased anorexic effect, may increase psychotic symptoms
  • Flecainide Increased risk of cardiotoxicity and arrhythmias
  • Fluoxetine Increased risk of cardiotoxicity and arrhythmias
  • Fluvoxamine Increased risk of cardiotoxicity and arrhythmias
  • Galantamine Possible antagonism of action
  • Gatifloxacin Increased risk of cardiotoxicity and arrhythmias
  • Grepafloxacin Increased risk of cardiotoxicity and arrhythmias
  • Guanethidine Thioridazine may decrease the effect of guanethidine.
  • Halofantrine Increased risk of cardiotoxicity and arrhythmias
  • Haloperidol Increased risk of cardiotoxicity and arrhythmias
  • Imipramine Increased risk of cardiotoxicity and arrhythmias
  • Josamycin Increased risk of cardiotoxicity and arrhythmias
  • Levofloxacin Increased risk of cardiotoxicity and arrhythmias
  • Lorcaserin Avoid combination.The combination is likely to reduce the metabolism of Thioridazine.
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Maprotiline 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
  • Mirabegron Mirabegron is a moderate CYP2D6 inhibitor and may cause an increase in exposure of CYP2D6 substrates. Monitor concomitant therapy closely.
  • Paroxetine Increased risk of cardiotoxicity and arrhythmias
  • Pentamidine Increased risk of cardiotoxicity and arrhythmias
  • 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
  • Pimozide Increased risk of cardiotoxicity and arrhythmias
  • Pindolol Increased risk of cardiotoxicity and arrhythmias
  • Procainamide Increased risk of cardiotoxicity and arrhythmias
  • Propafenone Increased risk of cardiotoxicity and arrhythmias.
  • Propranolol Increased risk of cardiotoxicity and arrhythmias
  • Quinidine Increased risk of cardiotoxicity and arrhythmias
  • Quinidine barbiturate Increased risk of cardiotoxicity and arrhythmias
  • Quinine Increased risk of cardiotoxicity and arrhythmias
  • Ranolazine Possible additive effect on QT prolongation
  • Rivastigmine Possible antagonism of action
  • Sertindole Increased risk of cardiotoxicity and arrhythmias
  • Sotalol Increased risk of cardiotoxicity and arrhythmias
  • Sparfloxacin Increased risk of cardiotoxicity and arrhythmias
  • Spiramycin Increased risk of cardiotoxicity and arrhythmias
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Thioridazine, 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 May cause additive QTc-prolonging effects. Concomitant therapy is contraindicated.
  • Tamoxifen Thioridazine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.
  • Tamsulosin Thioridazine, a CYP2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Thioridazine is initiated, discontinued, or dose changed.
  • Telithromycin Telithromycin may increase the QTc-prolonging effect of Thioridazine. Concomitant therapy should be avoided.
  • Terbinafine Terbinafine may increase serum concentrations of Thioridazine. Concomitant therapy is contraindicated.
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
  • Tetrabenazine May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
  • Thiothixene May cause additive QTc-prolonging effects. Concomitant therapy is contraindicated.
  • Ticlopidine Ticlopidine may decrease the metabolism of thioridazine. Concomitant therapy is contraindicated.
  • Toremifene May cause additive QTc-prolonging effects. Concomitant therapy is contraindicated.
  • Tramadol Thioridazine may decrease the effect of Tramadol by decreasing active metabolite production.
  • Tranylcypromine Tranylcypromine, a CYP2D6 inhibitor, may decrease the metabolism and clearance of Thioridazine. Concomitant therapy is contraindicated.
  • Trimethobenzamide Trimethobenzamide and Thioridazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trimipramine May cause additive QTc-prolonging effects. Concomitant therapy is contraindicated.
  • Triprolidine The antihistamine, Triprolidine, may increase the arrhythmogenic effect of the phenothiazine, Thioridazine. 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 Thioridazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Vilazodone Thioridazine prescribing information contraindicates the concomitant use of agents that inhibit CYP2D6 isoenzymes. Avoid combination.
  • Voriconazole Additive QTc prolongation may occur. Concomitant use is contraindicated.
  • 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 should be avoided.
  • Zuclopenthixol Additive QTc-prolonging effects increases risk of cardiac arrhythmias. Concomitant therapy is contraindicated.
Liều Lượng & Cách Dùng : Solution - Oral
Suspension - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aldazine
  • Công ty :
    Sản phẩm biệt dược : Mallorol
  • Công ty :
    Sản phẩm biệt dược : Meleril
  • Công ty :
    Sản phẩm biệt dược : Mellaril
  • Công ty :
    Sản phẩm biệt dược : Mellerette
  • Công ty :
    Sản phẩm biệt dược : Melleretten
  • Công ty :
    Sản phẩm biệt dược : Melleril
  • Công ty :
    Sản phẩm biệt dược : Novoridazine
  • Công ty :
    Sản phẩm biệt dược : Ridazin
  • Công ty :
    Sản phẩm biệt dược : Ridazine
  • Công ty :
    Sản phẩm biệt dược : Sonapax
  • Công ty :
    Sản phẩm biệt dược : Thioril
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00679
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5452
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509070
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00373
ChemSpider
http://www.chemspider.com/Chemical-Structure.5253.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-0612-01
PharmGKB
http://www.pharmgkb.org/drug/PA451666
Wikipedia
http://en.wikipedia.org/wiki/Thioridazine
RxList
http://www.rxlist.com/cgi/generic3/thioridazine.htm
Drugs.com
http://www.drugs.com/cdi/thioridazine.html
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