药品详细
Thioridazine(硫利达嗪)
化学结构式图
中文名
硫利达嗪
英文名
Thioridazine
分子式
C21H26N2S2
化学名
10-[2-(1-methylpiperidin-2-yl)ethyl]-2-(methylsulfanyl)-10H-phenothiazine
分子量
Average: 370.575
Monoisotopic: 370.153740222
Monoisotopic: 370.153740222
CAS号
50-52-2
ATC分类
N05A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
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)
生产厂家
- Actavis mid atlantic llc
- Alpharma us pharmaceuticals division
- Hi tech pharmacal co inc
- Ivax pharmaceuticals inc
- Mutual pharmaceutical co inc
- Mylan pharmaceuticals inc
- Novartis pharmaceuticals corp
- Par pharmaceutical inc
- Pharmaceutical assoc inc div beach products
- Roxane laboratories inc
- Sandoz inc
- Superpharm corp
- Teva pharmaceuticals usa
- Teva pharmaceuticals usa inc
- Watson laboratories inc
- West ward pharmaceutical corp
- Wockhardt eu operations (swiss) ag
封装厂家
- Advanced Pharmaceutical Services Inc.
- Direct Dispensing Inc.
- Dispensing Solutions
- Heartland Repack Services LLC
- Interpharm Pharmaceutical Products Inc.
- Major Pharmaceuticals
- Murfreesboro Pharmaceutical Nursing Supply
- Mutual Pharmaceutical Co.
- Mylan
- Novartis AG
- Pharmaceutical Packaging Center
- Pharmedix
- Physicians Total Care Inc.
- Professional Co.
- Qualitest
- Remedy Repack
- Roxane Labs
- Sandhills Packaging Inc.
- Sandoz
- Southwood Pharmaceuticals
- UDL Laboratories
- United Research Laboratories Inc.
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
药理
| Indication | For the treatment of schizophrenia and generalized anxiety disorder. |
| Pharmacodynamics | 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. |
| Mechanism of action | 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. |
| Absorption | 60% |
| Volume of distribution | Not Available |
| Protein binding | 95% |
| Metabolism |
Hepatic
|
| Route of elimination | Not Available |
| Half life | 21-25 hours |
| Clearance | Not Available |
| Toxicity | 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 |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | solid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| 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. |
| 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 |
| Penicillin G | 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. |
食物相互作用
Not Available
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