PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
thioridazine

2D structure

Overview

Generic Names: Thioridazin; Thioridazine Chloride; Thioridazine Hcl; Thioridazine Hydrochloride; Thoridazine Hydrochloride
Trade Names: Aldazine; Mallorol; Malloryl; Meleril; Mellaril; Mellaril Hydrochloride; Mellaril-S; Mellarit; Mellerets; Mellerette; Melleretten; Melleril; Metlaril; Novoridazine; Orsanil; Ridazin; Ridazine; Sonapax; Sonapax Hydrochloride; Stalleril; Thioridazine Hcl Intensol; Thioridazine, Prolongatum; Tioridazin
PharmGKB Accession Id: PA451666

Description

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) (source: Drug Bank)

Indication

For the treatment of schizophrenia and generalized anxiety disorder. (source: Drug Bank)

ATC Therapeutic Category

  • N05AC:Phenothiazines with piperidine structure

Pharmacology, Interactions, and Contraindications

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. (source: Drug Bank)

Pharmacology

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. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic (source: Drug Bank)

Protein Binding

95% (source: Drug Bank)

Absorption

60% (source: Drug Bank)

Toxicity

LD<sub>50</sub>=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 (source: Drug Bank)

Isomeric SMILES Code:

CN1CCCCC1CCN2c3ccccc3Sc4c2cc(cc4)SC (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C19
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  • PK
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  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2D6
  • CO
  •   
  • PK
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP2E1
  •   
  •   
  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
KCNH2
  •   
  • PD
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  • FA
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Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
HTR2A Uncurated Annotation (source: Drug Bank)
ADRA1A Uncurated Annotation (source: Drug Bank)
DRD1 Uncurated Annotation (source: Drug Bank)
DRD2 Uncurated Annotation (source: Drug Bank)

PharmGKB Curated Pathways

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
paroxetine
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Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
tamoxifen
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  •   
Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
amiodarone Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
amitriptyline Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
amphetamine Uncurated Annotation Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank)
astemizole Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
atomoxetine Uncurated Annotation The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine (source: Drug Bank)
benzphetamine Uncurated Annotation Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank)
bretylium Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
bromocriptine Uncurated Annotation The phenothiazine decreases the effect of bromocriptine (source: Drug Bank)
bupropion Uncurated Annotation Bupropion increases the effect and toxicity of thioridazine (source: Drug Bank)
chloroquine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
chlorpromazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
cisapride Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
dexfenfluramine Uncurated Annotation Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank)
dextroamphetamine Uncurated Annotation Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank)
diethylpropion Uncurated Annotation Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank)
diltiazem Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
diphenhydramine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
disopyramide Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
dofetilide Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
donepezil Uncurated Annotation Possible antagonism of action (source: Drug Bank)
doxepin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
duloxetine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
erythromycin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
fenfluramine Uncurated Annotation Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank)
flecainide Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
fluoxetine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
fluvoxamine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
galantamine Uncurated Annotation Possible antagonism of action (source: Drug Bank)
gatifloxacin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
grepafloxacin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
guanethidine Uncurated Annotation The agent decreases the effect of guanethidine (source: Drug Bank)
halofantrine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
haloperidol Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
imipramine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
josamycin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
levofloxacin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
maprotiline Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
mazindol Uncurated Annotation Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank)
methamphetamine Uncurated Annotation Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank)
metrizamide Uncurated Annotation Increased risk of convulsions (source: Drug Bank)
paroxetine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
penicillin g Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
pentamidine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
phendimetrazine Uncurated Annotation Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank)
phenmetrazine Uncurated Annotation Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank)
phentermine Uncurated Annotation Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank)
phenylpropanolamine Uncurated Annotation Decreased anorexic effect, may increase psychotic symptoms (source: Drug Bank)
pimozide Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
pindolol Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
procainamide Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
propafenone Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
propranolol Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
quinidine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
quinidine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
quinine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
ranolazine Uncurated Annotation Possible additive effect on QT prolongation (source: Drug Bank)
rivastigmine Uncurated Annotation Possible antagonism of action (source: Drug Bank)
sertindole Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
sotalol Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
sparfloxacin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
terfenadine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
ziprasidone Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Acquired Long QT Syndrome (aLQTS)
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Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Parkinson Disease
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  • PD
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  •   
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Curated Phenotype Datasets

These datasets are sorted alphabetically by title.

  1. Drug-Induced Long QT Intervals
    • Genotype data available
    • Phenotype data available
    • No literature annotations
    • Not annotated
    • PD
    Submitted by Dan Roden, MD involving ADRB1, ADRB2, KCNE1, KCNE2, KCNH2, KCNQ1, SCN5A, almokalant, amiodarone, amitriptyline, bretylium, bupivacaine, cisapride, disopyramide, dofetilide, encainide, fluconazole, haloperidol, hydroquinidine, isoflurane, itraconazole, ketoconazole, lithium, loratadine, metoclopramide, nortriptyline, procainamide, quinidine, sematilide, sotalol, sulfamethoxazole, thioridazine, trimethoprim, , Long QT Syndrome, Proarrhythmia and Torsades de Pointes

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

Downloads

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LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00679
KEGG Drug ID:
D00373
PubChem Compound ID:
5452
PubChem Substance ID:
148555
IUPHAR Ligand ID:
100

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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