Tìm theo
Mesoridazine
Các tên gọi khác (9 ) :
  • 10-(2-(1-Methyl-2-piperidyl)ethyl)-2-methylsulfinyl phenothiazine
  • 10-(2(1-Methyl-2-piperidyl)ethyl)-2-(methylsulfinyl)phenothiazine
  • 2-Methanesulfinyl-10-[2-(1-methyl-piperidin-2-yl)-ethyl]-10H-phenothiazine
  • Mesoridazina
  • Mesoridazine
  • Mesoridazinum
  • Thioridazine Thiomethyl Sulfoxide
  • thioridazine-2-sulfoxide
  • TPS-23
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 5588-33-0
ATC: N05AC03
ĐG : Novartis AG , http://www.novartis.com
CTHH: C21H26N2OS2
PTK: 386.574
A phenothiazine antipsychotic with effects similar to chlorpromazine. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H26N2OS2
Phân tử khối
386.574
Monoisotopic mass
386.148654844
InChI
InChI=1S/C21H26N2OS2/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(26(2)24)15-19(21)23/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3
InChI Key
InChIKey=SLVMESMUVMCQIY-UHFFFAOYSA-N
IUPAC Name
2-methanesulfinyl-10-[2-(1-methylpiperidin-2-yl)ethyl]-10H-phenothiazine
Traditional IUPAC Name
mesoridazine
SMILES
CN1CCCCC1CCN1C2=CC=CC=C2SC2=C1C=C(C=C2)S(C)=O
Độ hòa tan
7.67e-02 g/l
logP
3.9
logS
-3.7
pKa (strongest acidic)
19.36
pKa (Strongest Basic)
8.19
PSA
23.55 Å2
Refractivity
115.13 m3·mol-1
Polarizability
43.83 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
Dược Lực Học : Mesoridazine, the besylate salt of a metabolite of thioridazine, is a phenothiazine tranquilizer. Pharmacological studies in laboratory animals have established that mesoridazine has a spectrum of pharmacodynamic actions typical of a major tranquilizer. In common with other tranquilizers it inhibits spontaneous motor activity in mice, prolongs thiopental and hexobarbital sleeping time in mice and produces spindles and block of arousal reaction in the EEG of rabbits. It is effective in blocking spinal reflexes in the cut and antagonizes d-amphetamine excitation and toxicity in grouped mice. It shows a moderate adrenergic blocking activity in vitro and in vivo and antagonizes 5-hydroxytryptamine in vivo. Intravenously administered, it lowers the blood pressure of anesthetized dogs. It has a weak antiacetylcholine effect in vitro.
Cơ Chế Tác Dụng : A phenothiazine antipsychotic with effects similar to chlorpromazine. [PubChem] Based upon animal studies, mesoridazine, as with other phenothiazines, acts indirectly on reticular formation, whereby neuronal activity into reticular formation is reduced without affecting its intrinsic ability to activate the cerebral cortex. In addition, the phenothiazines exhibit at least part of their activities through depression of hypothalamic centers. Neurochemically, the phenothiazines are thought to exert their effects by a central adrenergic blocking action.
Dược Động Học :
▧ Absorption :
Well absorbed from the gastrointestinal tract.
▧ Protein binding :
4%
▧ Half Life :
24 to 48 hours
Độc Tính : Oral LD50 is 560 ± 62.5 mg/kg and 644 ± 48 mg/kg in mouse and rat, respectively. Symptoms of overdose may include emesis, muscle tremors, decreased food intake and death associated with aspiration of oral-gastric contents into the respiratory system.
Chỉ Định : Used in the treatment of schizophrenia, organic brain disorders, alcoholism and psychoneuroses.
Tương Tác Thuốc :
  • 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 should be avoided.
  • Astemizole Increased risk of cardiotoxicity and arrhythmias
  • 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
  • Chloroquine Increased risk of cardiotoxicity and arrhythmias
  • Chlorpromazine Increased risk of cardiotoxicity and arrhythmias
  • 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
  • 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
  • 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 Mesoridazine 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
  • 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 cardiotoxicity and arrhythmias
  • 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
  • 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, Mesoridazine, 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 Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
  • Tetrabenazine May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Trimethobenzamide Trimethobenzamide and Mesoridazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Triprolidine The antihistamine, Triprolidine, may increase the arrhythmogenic effect of the phenothiazine, Mesoridazine. 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 Mesoridazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • 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 prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng : Injection, solution - Intramuscular
Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Lidanar
  • Công ty :
    Sản phẩm biệt dược : Lidanil
  • Công ty :
    Sản phẩm biệt dược : Serentil
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00933
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4078
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506724
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07143
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02671
ChemSpider
http://www.chemspider.com/Chemical-Structure.3936.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50131440
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0597-0020-01
PharmGKB
http://www.pharmgkb.org/drug/PA450386
Wikipedia
http://en.wikipedia.org/wiki/Mesoridazine
RxList
http://www.rxlist.com/cgi/generic3/mesoridazine.htm
Drugs.com
http://www.drugs.com/mtm/mesoridazine.html
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