- Overview
- Properties
- Genetics
- Related Genes
- Pathways
- Related Drugs
- Related Diseases
- Datasets
- Downloads/LinkOuts
Overview
| Generic Names: | Dofetilida [INN-Spanish]; Dofetilidum [INN-Latin] |
|---|---|
| Trade Names: | Dofetilida; Tikosyn |
| PharmGKB Accession Id: | PA449389 |
Description
Dofetilide is a class III antiarrhythmic agent that is approved by the Food and Drug Administration (FDA) for the maintenance of sinus rhythm in individuals prone to the formation of atrial fibrillation and flutter, and for the chemical cardioversion to sinus rhythm from atrial fibrillation and flutter. Wikipedia (source: Drug Bank)
Indication
For the maintenance of normal sinus rhythm (delay in time to recurrence of atrial fibrillation/atrial flutter AF/AFl) in patients with atrial fibrillation/atrial flutter of greater than one week duration who have been converted to normal sinus rhythm (source: Drug Bank)
ATC Therapeutic Category
- C01BD:Antiarrhythmics, class III
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
The mechanism of action of Dofetilide is a blockade of the cardiac ion channel carrying the rapid component of the delayed rectifier potassium current, IKr. This inhibition of potassium channels results in a prolongation of action potential duration and the effective refractory period of accessory pathways (both anterograde and retrograde conduction in the accessory pathway). (source: Drug Bank)
Pharmacology
Dofetilide is an antiarrhythmic drug with Class III (cardiac action potential duration prolonging) properties and is indicated for the maintenance of normal sinus rhythm. Dofetilide increases the monophasic action potential duration in a predictable, concentration-dependent manner, primarily due to delayed repolarization. At concentrations covering several orders of magnitude, Dofetilide blocks only IKr with no relevant block of the other repolarizing potassium currents (e.g., IKs, IK1). At clinically relevant concentrations, Dofetilide has no effect on sodium channels (associated with Class I effect), adrenergic alpha-receptors, or adrenergic beta-receptors. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Protein Binding
60% -70% (source: Drug Bank)
Absorption
>90% (source: Drug Bank)
Isomeric SMILES Code:
CN(CCc1ccc(cc1)NS(=O)(=O)C)CCOc2ccc(cc2)NS(=O)(=O)C (source: Drug Bank)
Curated Annotations (
)
-
rs36210421
at chr7:150275361
in
KCNH2
Results of in vitro assays from this study suggest that the R1047L polymorphism leads to a functional impairment of the channel, which may contribute to the higher incidence of Torsades de Pointes in 1047L carriers when challenged with a channel blocker.- Variant Name:
- KCNH2: R1047L
- Related Drugs:
- dofetilide
- Related Diseases:
- Torsades de Pointes
- Evidence:
-
PMID:15522280
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
KCNH2 |
|
Publications, Variants |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| KCNK2 |
|
(source: Drug Bank) |
| KCNJ12 |
|
(source: Drug Bank) |
| KCNH2 |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
A list of non-curated publications that mention this drug along with other drugs is available.
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
Long QT Syndrome |
|
Publications |
|
|
Torsades de Pointes |
|
Publications, Variants |
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.
- A modulator of HERG Potassium Channel block
- FA
Submitted by Dan Roden, MD involving ALG10, KCNH2, dofetilide, qt-prolonging drugs, and Torsades de Pointes - Drug-Induced Long QT Intervals
- 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.
Downloads
You must sign in before you can download data.
LinkOuts
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.