Drug/Small Molecule:
disopyramide

2D structure

Overview

Generic Names: Disopiramida [INN-Spanish]; Disopyramide Free Base; Disopyramide Phosphate; Disopyramidum [INN-Latin]
Trade Names: Dicorantil; Isorythm; Lispine; Norpace; Norpace CR; Ritmodan; Rythmodan; Rythmodan P; Rythmodan-La; Searle 703; Xi-Disopyramide
PharmGKB Accession Id: PA449373

Description

A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties. PubChem (source: Drug Bank)

Indication

For the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, ventricular pre-excitation and cardiac dysrhythmias. (source: Drug Bank)

ATC Therapeutic Category

  • C01BA:Antiarrhythmics, class Ia

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Disopyramide is a Type 1 antiarrhythmic drug (ie, similar to procainamide and quinidine). It inhibits the fast sodium channels. In animal studies Disopyramide decreases the rate of diastolic depolarization (phase 4) in cells with augmented automaticity, decreases the upstroke velocity (phase 0) and increases the action potential duration of normal cardiac cells, decreases the disparity in refractoriness between infarcted and adjacent normally perfused myocardium, and has no effect on alpha- or beta-adrenergic receptors. (source: Drug Bank)

Pharmacology

Disopyramide is an antiarrhythmic drug indicated for the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia that are life-threatening. In man, Disopyramide at therapeutic plasma levels shortens the sinus node recovery time, lengthens the effective refractory period of the atrium, and has a minimal effect on the effective refractory period of the AV node. Little effect has been shown on AV-nodal and His-Purkinje conduction times or QRS duration. However, prolongation of conduction in accessory pathways occurs. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Take without regard to meals. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic (source: Drug Bank)

Protein Binding

50%-65% (source: Drug Bank)

Absorption

Nearly complete (source: Drug Bank)

Toxicity

LD<sub>50</sub>=580 mg/kg in rats (source: Drug Bank)

Isomeric SMILES Code:

CC(C)N(CC[C@](C1=CC=CC=C1)(C2=CC=CC=N2)C(=O)N)C(C)C (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
HRH1
  •   
  • PD
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
KCNH2
  •   
  • PD
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
ORM1
  •   
  •   
  • PK
  •   
  •   
Publications

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

Drug Targets

Gene Description
ORM1 Uncurated Annotation (source: Drug Bank)
SCN5A Uncurated Annotation (source: Drug Bank)

PharmGKB Curated Pathways

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

Drug Interactions

Drug Description
acebutolol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
atenolol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
azithromycin Uncurated Annotation The macrolide increases the effect of disopyramide (source: Drug Bank)
betaxolol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
bisoprolol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
carvedilol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
cisapride Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
clarithromycin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
donepezil Uncurated Annotation Possible antagonism of action (source: Drug Bank)
erythromycin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
esmolol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (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)
levofloxacin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
mephenytoin Uncurated Annotation The hydantoin decreases the effect of disopyramide (source: Drug Bank)
mesoridazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
metoprolol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
moxifloxacin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
nadolol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
oxprenolol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
phenobarbital Uncurated Annotation Phenobarbital decreases levels of disopyramide (source: Drug Bank)
phenytoin Uncurated Annotation The hydantoin decreases the effect of disopyramide (source: Drug Bank)
pindolol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
propranolol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
rifampin Uncurated Annotation Rifampin decreases the effect of disopyramide (source: Drug Bank)
rivastigmine Uncurated Annotation Possible antagonism of action (source: Drug Bank)
sotalol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
sparfloxacin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
telithromycin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
terfenadine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
thioridazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
timolol Uncurated Annotation The beta-blocker increases toxicity of disopyramide (source: Drug Bank)
ziprasidone Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)

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.

Additional Datasets

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

  1. Genetic Associations in Drug-induced QT Prolongation and Torsades
  2. Physicochemical determinants of human renal clearance
  3. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

Downloads

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LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00280
KEGG Compound ID:
C06965
KEGG Drug ID:
D00303
PubChem Compound ID:
3114
PubChem Substance ID:
162448

Common Searches

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Non-Curated Publications

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

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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