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

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

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

Công ty : Novartis AG

Website : http://www.novartis.com
Công ty : Physicians Total Care Inc.

Website : http://www.physicianstotalcare.com

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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