- Overview
- Properties
- Related Genes
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- Related Drugs
- Related Diseases
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Overview
| Generic Names: | Flecainida [INN-Spanish]; Flecainide acetate; Flecainidum [INN-Latin] |
|---|---|
| Trade Names: | Flecaine; Tambocor |
| PharmGKB Accession Id: | PA449646 |
Description
A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial arrhythmias and tachycardias. Paradoxically, however, in myocardial infarct patients with either symptomatic or asymptomatic arrhythmia, flecainide exacerbates the arrhythmia and is not recommended for use in these patients. PubChem (source: Drug Bank)
Indication
For the prevention of paroxysmal supraventricular tachycardias (PSVT), including atrioventricular nodal reentrant tachycardia, atrioventricular reentrant tachycardia and other supraventricular tachycardias of unspecified mechanism associated with disablin. (source: Drug Bank)
ATC Therapeutic Category
- C01BC:Antiarrhythmics, class Ic
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Flecainide acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers. (source: Drug Bank)
Pharmacology
Flecainide has local anesthetic activity and belongs to the membrane stabilizing (Class 1) group of antiarrhythmic agents; it has electrophysiologic effects characteristic of the IC class of antiarrhythmics. (source: Drug Bank)
Food Interactions
Take without regard to meals. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic. Flecainide does not undergo any consequential presystemic biotransformation. The two major urinary metabolites are meta-O-dealkylated flecainide (active, but about one-fifth as potent) and the meta-O-dealkylated lactam of flecainide (non-active metabolite). (source: Drug Bank)
Protein Binding
40% (source: Drug Bank)
Absorption
Nearly complete following oral administration. (source: Drug Bank)
Toxicity
Oral LD50 is 50-498 mg/kg in rat. Symptoms of overdose include nausea and vomiting, convulsions, hypotension, bradycardia, syncope, extreme widening of the QRS complex, widening of the QT interval, widening of the PR interval, ventricular tachycardia, AV nodal block, asystole, bundle branch block, cardiac failure, and cardiac arrest. (source: Drug Bank)
Isomeric SMILES Code:
c1cc(c(cc1OCC(F)(F)F)C(=O)NCC2CCCCN2)OCC(F)(F)F (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
|
CYP2D6 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| SCN5A |
|
(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 | |
|---|---|---|
| amiodarone |
|
Amiodarone increases the effect and toxicity of flecainide (source: Drug Bank) |
| cimetidine |
|
Cimetidine increases serum levels of flecainide (source: Drug Bank) |
| cisapride |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| duloxetine |
|
Possible increase in the levels of this agent when used with duloxetine (source: Drug Bank) |
| mesoridazine |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| quinupristin |
|
This combination presents an increased risk of toxicity (source: Drug Bank) |
| ritonavir |
|
Ritonavir increases the toxicity of the anti-arrhythmic (source: Drug Bank) |
| terfenadine |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| thioridazine |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Atrial Fibrillation |
|
Publications |
|
|
Tachycardia, Ventricular |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
- Genetic Associations in Drug-induced QT Prolongation and Torsades
- Measured and Predicted Changes in QT Intervals During Atrial Fibrillation
- OCTN1 Phenotype
- Physicochemical determinants of human renal clearance
- The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
