Corvert
Corvert - General Information
Corvert is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm. [Wikipedia]
Pharmacology of Corvert
Corvert 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 outward potassium currents, which is the mechanism by which most other class III antiarrhythmics act.
Corvert for patients
Use in Patients With Hepatic or Renal Dysfunction
The safety, effectiveness, and pharmacokinetics of CORVERT have not been established in patients with hepatic or renal dysfunction. However, it is unlikely that dosing adjustments would be necessary in patients with compromised renal or hepatic function based on the following considerations:
- CORVERT is indicated for rapid intravenous therapy (duration <30 minutes) and is dosed to a known, well-defined pharmacologic action (termination of arrhythmia) or to a maximum of two 10-minute infusions;
- less than 10% of the dose of CORVERT is excreted unchanged in the urine; and
- drug distribution appears to be one of the primary mechanisms responsible for termination of the pharmacologic effect. Nonetheless, patients with abnormal liver function should be monitored by telemetry for more than the 4-hour period generally recommended.
In 285 patients with atrial fibrillation or atrial flutter who were treated with CORVERT, the clearance of ibutilide was independent of renal function, as assessed by creatinine clearance (range 21 to 140 mL/min).
Corvert Interactions
No specific pharmacokinetic or other formal drug interaction studies were conducted.
Digoxin: Supraventricular arrhythmias may mask the cardiotoxicity associated with excessive digoxin levels. Therefore, it is advisable to be particularly cautious in patients whose plasma digoxin levels are above or suspected to be above the usual therapeutic range. Coadministration of digoxin did not have effects on either the safety or efficacy of ibutilide in the clinical trials.
Calcium channel blocking agents: Coadministration of calcium channel blockers did not have any effect on either the safety or efficacy of ibutilide in the clinical trials.
Beta-adrenergic blocking agents: Coadministration of beta-adrenergic blocking agents did not have any effect on either the safety or efficacy of ibutilide in the clinical trials.
Corvert Contraindications
CORVERT Injection is contraindicated in patients who have previously demonstrated hypersensitivity to ibutilide fumarate or any of the other product components.
Additional information about Corvert
Corvert Indication: Indicated for the rapid conversion of atrial fibrillation or atrial flutter of recent onset to sinus rhythm.
Mechanism Of Action: Corvert 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 potassium channel pores. In other words, Corvert binds to and alters the activity of hERG potassium channels, delayed inward rectifier potassium (IKr) channels and L-type (dihydropyridine sensitive) calcium channels
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Ibutilide
Synonyms: Ibutilide Fumarate; Ibutilida [INN-Spanish]; Ibutilide; Ibutilidum [INN-Latin]
Drug Category: Anti-Arrhythmia Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Ibutilide: Corvert;
Absorption: Rapid after intravenous injection
Toxicity (Overdose): 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.
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.
Half Life: 6 hours (ranges from 2-12 hours)
Dosage Forms of Corvert: Solution Intravenous
Chemical IUPAC Name: N-[4-[4-(ethyl-heptylamino)-1-hydroxybutyl]phenyl]methanesulfonamide
Chemical Formula: C20H36N2O3S
Ibutilide on Wikipedia: https://en.wikipedia.org/wiki/Ibutilide
Organisms Affected: Humans and other mammals