Ibutilide fumarate Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Covert was launched in the US and UK for treatment of atrial fibrillation and
flutter and can be synthesized in three steps from N-phenyl rnethanesulfonamide.
While ibutilide has an asymmetric center, it has been determined that the racemate is
equipotent with either enantiomer. The antiarrhythmic action is derived from the
compounds ability to prolong the action potential duration and lengthen the refractory
period of myocardial tissue. Class Ⅲ antiarrhythrnic agents accomplish this by
blocking outward potassium channels, however, ibutilide elicits the same effect by
activation of slow inward sodium channels. Recent evidence indicates that it also is
a potent blocker of the rapidly acting delayed rectifier potassium current (l
kr)and may
block the ATP-inhibited potassium channel.
Chemische Eigenschaften
White to Off-White Solid
Verwenden
A methanesulfonanilide antiarrhythmic agent; prologns myocardial action potential duration, predominantly by activation of slow inward sodium current. Antiarrhythmic (class III).
Clinical Use
Ibutilide (Corvert) is a structural analog of sotalol and
produces cardiac electrophysiological effects similar to
those of the antiarrhythmic agents in class III.
Ibutilide is approved for the chemical cardioversion of
recent-onset atrial fibrillation and atrial flutter. Ibutilide
appears to be more effective in terminating atrial flutter
than atrial fibrillation. It can also lower the defibrillation threshold for atrial fibrillation resistant to chemical
cardioversion.
Nebenwirkungen
The major adverse effect associated with the use of ibutilide
is the risk of torsades de pointes due to QT prolongation.
Other reported adverse cardiovascular
events (all 2%) include hypotension and hypertension,
bradycardia and tachycardia, and varying degrees
of A-V block. The incidence of noncardiac adverse
events with the exception of nausea does not differ
from that of placebo.
Arzneimittelwechselwirkung
Ibutilide has significant drug interactions.
Vorsichtsmaßnahmen
Contraindications to the use of ibutilide include baseline
prolongation of the QT interval, use of other QTprolonging
drugs, history of torsades de pointes, hypersensitivity
to ibutilide, uncorrected hypokalemia or
hypomagnesemia, and pregnancy or breast-feeding.
Ibutilide fumarate Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
