Ibutilide--recent molecular insights and accumulating evidence for use in atrial flutter and fibrillation.
Article Details
- CitationCopy to clipboard
Doggrell SA, Hancox JC
Ibutilide--recent molecular insights and accumulating evidence for use in atrial flutter and fibrillation.
Expert Opin Investig Drugs. 2005 May;14(5):655-69.
- PubMed ID
- 15926871 [ View in PubMed]
- Abstract
Ibutilide is a 'pure' class III antiarrhythmic drug, used intravenously against atrial flutter and fibrillation. At a cellular level it exerts two main actions: induction of a persistent Na+ current sensitive to dihydropyridine Ca2+ channel blockers and potent inhibition of the cardiac rapid delayed rectifier K+ current, by binding within the channel pore cavity upon channel gating. Ibutilide has been shown to terminate atrial flutter and fibrillation in animal studies, with some risk of ventricular pro-arrhythmia. Experimental models of hypertrophy/heart failure show altered sensitivity to ibutilide, with increased dispersion of repolarisation and incidence of pro-arrhythmia. Patient trials show that ibutilide is effective at terminating atrial arrhythmias when given alone, and that it can increase effectiveness and reduce energy requirements of electrical cardioversion. The risk to patients of polymorphic ventricular tachycardia necessitates careful patient selection and monitoring during and after treatment. An ibutilide analogue, trecetilide, requires further investigation but may offer a less readily metabolised and pro-arrhythmic alternative to ibutilide.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Ibutilide ATP-sensitive inward rectifier potassium channel 11 Protein Humans UnknownInhibitorDetails Ibutilide Potassium channel subfamily K member 1 Protein Humans UnknownInhibitorDetails Ibutilide Potassium channel subfamily K member 6 Protein Humans UnknownInhibitorDetails Ibutilide Potassium voltage-gated channel subfamily H member 2 Protein Humans YesInhibitorDetails Ibutilide Potassium voltage-gated channel subfamily H member 6 Protein Humans UnknownInhibitorDetails Ibutilide Potassium voltage-gated channel subfamily H member 7 Protein Humans UnknownInhibitorDetails Ibutilide Voltage-dependent calcium channel gamma-1 subunit Protein Humans UnknownActivatorDetails Ibutilide Voltage-dependent calcium channel subunit alpha-2/delta-1 Protein Humans UnknownActivatorDetails Ibutilide Voltage-dependent L-type calcium channel subunit alpha-1C Protein Humans YesActivatorDetails Ibutilide Voltage-dependent L-type calcium channel subunit beta-1 Protein Humans YesActivatorDetails