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QuickView for Ibutilide (compound)

Name: ibutilide
PubChem Compound ID: 10255436
Molecular formula: C24H40N2O7S
Molecular weight: 500.65 g/mol
Name: ibutilide
Name (isomeric): DB00308
Drug Type: small molecule
Ibutilide Fumarate; Ibutilida [INN-Spanish]; Ibutilidum [INN-Latin]
Brand: Corvert
Category: Anti-Arrhythmia Agents
CAS number: 122647-32-9
Indication: Indicated for the rapid conversion of atrial fibrillation or atrial flutter of recent onset to sinus rhythm.
Ibutilide prolongs the action potential duration and increases both atrial and ventricular refractoriness in vivo, i.e., class III electrophysiologic effects. Voltage clamp studies indicate that ibutilide, at nanomolar concentrations, delays repolarization by activation of a slow, inward current (predominantly sodium), rather than by blocking outwa...
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Mechanism of Action:
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 bi...
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Absorption: Rapid after intravenous injection
Protein binding: 40%
Biotransformation: Primarily hepatic. Eight metabolites of ibutilide were detected in metabolic profiling of urine. These metabolites are thought to be formed primarily by o-oxidation followed by sequential b-oxidation of the heptyl side chain of ibutilide. Of the eight metabolites, only the o-hydroxy metabolite possesses class III electrophysiologic properties similar to that of ibutilide in an in vitro isolated rabbit myocardium model.
Route of elimination: In healthy male volunteers, about 82% of a 0.01 mg/kg dose of [14C] ibutilide fumarate was excreted in the urine (about 7% of the dose as unchanged ibutilide) and the remainder (about 19%) was recovered in the feces.
Half Life: 6 hours (ranges from 2-12 hours)
Clearance: 29 mL/min/kg
Toxicity: Acute overdose in animals results in CNS toxicity; notably, CNS depression, rapid gasping breathing, and convulsions. The intravenous median lethal dose in the rat was more than 50 mg/kg which is, on a mg/m2 basis, at least 250 times the maximum recommended human dose.
Affected organisms: Humans and other mammals
Drug interaction:
TacrolimusAdditive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
LumefantrineAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
ThiothixeneMay cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
VorinostatAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
ToremifeneAdditive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
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