PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
cisapride

2D structure

Overview

Generic Names: cisapride
Trade Names: Acenalin; Alimix; Cipril; Enteropride; Kinestase; Prepulsid; Pridesia; Propulsid; Propulsid Quicksolv; Propulsin; Risamal; Syspride
PharmGKB Accession Id: PA449011

Description

In many countries (including Canada) cisapride has been either withdrawn or has had its indications limited due to reports about long QT syndrome due to cisapride, which predisposes to arrhythmias. The FDA issued a warning letter regarding this risk to health care professionals and patients. (source: Drug Bank)

Indication

For the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease. (source: Drug Bank)

ATC Therapeutic Category

  • A03FA:Propulsives

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Cisapride acts through the stimulation of the serotonin 5-HT<sub>4</sub> receptors which increases acetylcholine release in the enteric nervous system (specifically the myenteric plexus). This results in increased tone and amplitude of gastric (especially antral) contractions, relaxation of the pyloric sphincter and the duodenal bulb, and increased peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. (source: Drug Bank)

Pharmacology

Cisapride is a parasympathomimetic which acts as a serotonin 5-HT<sub>4</sub> agonist. Stimulation of the serotonin receptors increases acetylcholine release in the enteric nervous system. Cisapride stimulates motility of the upper gastrointestinal tract without stimulating gastric, biliary, or pancreatic secretions. Cisapride increases the tone and amplitude of gastric (especially antral) contractions, relaxes the pyloric sphincter and the duodenal bulb, and increases peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. It increases the resting tone of the lower esophageal sphincter. It has little, if any, effect on the motility of the colon or gallbladder. Cisapride does not induce muscarinic or nicotinic receptor stimulation, nor does it inhibit acetylcholinesterase activity. (source: Drug Bank)

Food Interactions

Grapefruit and grapefruit juice should be avoided throughout treatment, grapefruit can significantly increase serum levels of this product.
Increases absorption, take 30 minutes before a meal. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. Extensively metabolized via cytochrome P450 3A4 enzyme. (source: Drug Bank)

Protein Binding

97.5% (source: Drug Bank)

Absorption

Cisapride is rapidly absorbed after oral administration, with an absolute bioavailability of 35-40%. (source: Drug Bank)

Isomeric SMILES Code:

COc1cc(c(cc1C(=O)N[C@H]2CCN(C[C@@H]2OC)CCCOc3ccc(cc3)F)Cl)N (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
No phenotype data Genotype Data Available Literature annotations available Has annotations
CYP2A6
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  •   
  •   
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
  •   
  •   
  • PK
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP3A7
  •   
  •   
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
KCNH2
  • CO
  • PD
  •   
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
KCNQ1
  • CO
  • PD
  •   
  • FA
  • GN
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)
HTR3A Uncurated Annotation (source: Drug Bank)
HTR4 Uncurated Annotation (source: Drug Bank)
KCNH2 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
acenocoumarol Uncurated Annotation Increases the anticoagulant effect (source: Drug Bank)
acetophenazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
amiodarone Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
amitriptyline Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
amoxapine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
amprenavir Uncurated Annotation Amprenavir increases the effect and toxicity of cisapride (source: Drug Bank)
anisindione Uncurated Annotation Increases the anticoagulant effect (source: Drug Bank)
aprepitant Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
astemizole Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
atazanavir Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
bepridil Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
bretylium Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
chlorpromazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
clarithromycin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
clomipramine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
delavirdine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
desipramine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
dicumarol Uncurated Annotation Increases the anticoagulant effect (source: Drug Bank)
diltiazem Uncurated Annotation Diltiazem increases the levels of cisapride (source: Drug Bank)
disopyramide Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
doxepin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
efavirenz Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
encainide Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
erythromycin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
ethopropazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
fexofenadine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
flecainide Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
fluconazole Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
fluphenazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
fosamprenavir Uncurated Annotation Amprenavir increases the effect and toxicity of cisapride (source: Drug Bank)
ibutilide Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
imipramine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
indinavir Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
itraconazole Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
josamycin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
ketoconazole Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
maprotiline Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
mesoridazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
methdilazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
methotrimeprazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
mibefradil Uncurated Annotation Mibefradil increases levels of cisapride (source: Drug Bank)
nefazodone Uncurated Annotation Nefazodone increases serum levels of cisapride (source: Drug Bank)
nelfinavir Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
nifedipine Uncurated Annotation Increases the effect and toxicity of nifedipine (source: Drug Bank)
nortriptyline Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
perphenazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
posaconazole Uncurated Annotation Contraindicated co-administration (source: Drug Bank)
procainamide Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
prochlorperazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
promazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
promethazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
propafenone Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
propiomazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
protriptyline 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)
quinupristin Uncurated Annotation This combination presents an increased risk of toxicity (source: Drug Bank)
ritonavir Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
saquinavir Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
sotalol 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)
thiethylperazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
thioridazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
trifluoperazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
triflupromazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
trimeprazine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
trimipramine Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
troleandomycin Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
voriconazole Uncurated Annotation Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
warfarin Uncurated Annotation Increases the anticoagulant effect (source: Drug Bank)
zafirlukast 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)
  • CO
  • PD
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
congenital long QT syndrome
  •   
  • PD
  •   
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Long QT Syndrome
  • CO
  • PD
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Romano-Ward Syndrome
  • CO
  •   
  •   
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Torsades de Pointes
  • CO
  • PD
  •   
  •   
  •   
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. Genetic Associations in Drug-induced QT Prolongation and Torsades
  2. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

Downloads

You must sign in before you can download data.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00604
KEGG Compound ID:
C06910
KEGG Drug ID:
D00274
PubChem Compound ID:
2769
PubChem Substance ID:
192212
IUPHAR Ligand ID:
240

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

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.
Add New Alternate Name
Add New ATC Term
Add Cross Reference
Add a metabolite
Add a text annotation
Add a drug target
hint: enter a gene
    Add a drug interaction
    hint: enter a drug
    PharmGKB® is a registered trademark of HHS and is financially supported by NIH/NIGMS. It is managed at Stanford University (GM61374).
    ©2001-2010 PharmGKB.