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| {{drugbox
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| | IUPAC_name = ''N''-[4-[4-(ethyl-heptyl-amino)- 1-hydroxy-butyl]phenyl] methanesulfonamide
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| | image = Ibutilide.svg
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| | width = 250px
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| | CAS_number = 122647-32-9
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| | ATC_prefix = C01
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| | ATC_suffix = BD05
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| | ATC_supplemental =
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| | PubChem = 60753
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| | DrugBank = APRD01025
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| | C = 20 | H = 36 | N = 2 | O = 3 | S = 1
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| | molecular_weight = 384.578 g/mol
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| | bioavailability =
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| | protein_bound = 40%
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| | metabolism = Hepatic oxidation
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| | elimination_half-life = 6 hours (2-12 hours)
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| | excretion = [[Kidney|Renal]] (82%), fecal
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| | pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
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| | pregnancy_US = <!-- A / B / C / D / X -->
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| | pregnancy_category = C
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| | legal_AU = <!-- Unscheduled / S2 / S4 / S8 -->
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| | legal_UK = <!-- GSL / P / POM / CD -->
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| | legal_US = <!-- OTC / Rx-only -->
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| | legal_status =
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| | routes_of_administration = Intravenous
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| }}
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| {{SI}}
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| {{CMG}}
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| '''Ibutilide''' 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. It exerts its antiarrhythmic effect by induction of slow inward sodium current, which prolongs action potential and [[refractory period]] of myocardial cells. Because of its Class III antiarrhythmic activity, there should not be concomitant administration of Class Ia and Class III agents.
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| == Mechanism of action ==
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| Unlike most other Class III antiarrhythmic drugs, ibutilide does not produce its prolongation of action potential via blockade of cardiac delayed rectifier of potassium current, nor does it have a sodium-blocking, antiadrenergic, and calcium blocking activity that other Class III agents possess. Thus it is often referred as a “pure” Class III antiarrhythmic drug.
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| It does have action on the slow sodium channel and promotes the influx of sodium through these slow channels.
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| Although potassium current seems to play a role, their interactions are complex and not well understood.<ref name=Howard>Howard, P.A., Ibutilide: An antiarrhythmic agent for the treatment of atrial fibrillation or flutter. Annals of Pharmacotherapy, 1999. 33(1): p. 38-47.</ref> Ibutilide’s unique mechanism works by an activation of a specific inward sodium current, thus producing its therapeutic response in which a prolonged [[action potential]] increases myocytes’ cardiac refractoriness in case of atrial fibrillation and flutter.
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| == Pharmacokinetics ==
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| ===Absorption===
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| Ibutilide is intravenously administered. However, it has a high first-pass metabolism, which results a poor [[bioavailability]]. Individual pharmacokinetic properties are highly viable during the clinical trial.<ref name=Howard/><ref name=PI>Pharmacia-Upjohn, Corvert (ibutilide fumarate) injection package insert. July 2002: Kalamazoo, MI.</ref>
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| ===Distribution===
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| Ibutilide has a relatively large volume of distribution among individual subjects, which is about 11L/kg. Approximately 40% of the drug is bound with plasma albumin of healthy volunteers in a trial. This is also approximately close to patients with atrial fibrillation and flutter.<ref name=PI/>
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| ===Metabolism===
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| Ibutilide has a high systemic plasma clearance that closes to the hepatic blood flow (29mL/min/kg). Its metabolic pathway is via liver’s cytochrome P450 system by isoenzymes other than CYP2A4 and [[CYP2D6]] by which the heptyl side chain of ibutilide is oxidized.<ref name=Howard/><ref name=PI/> With eight metabolites are detected in the urine, however, only one is an active metabolite that shares the similar electrophysiologic property of the Class III antiarrhythmic agents.<ref name=Howard/><ref name=PI/><ref>Kelly C. Rogers, P., and Douglas A. Wolfe MD, Ibutilide: A class III rapidly acting antidysrhythmic for atrial fibrillation or atrial flutter. Journal of Emergency Medicine January 2001. Volume 20( Issue 1): p. 67-71.</ref> The plasma concentration of this metabolite is only less than 10% of ibutilide.<ref name=PI/>
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| ===Excretion===
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| After administration of ibutilide, it is quickly excreted by renal pathway with a half-life of approximately 6 hours. Approximately 82% of a 0.01mg/kg dose is excreted in the urine during the trial. Among those, around 7% is excreted as unchanged drug. The reminder of the drug is excreted in feces (about 19%).<ref name=Howard/>
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| == Patient Information ==
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| This medication will be given intravenously for your heart disease. You will have continuously ECG monitoring during the infusion and 4 hours after your infusion. Some of the minor side effects are headache and irregular heartbeat. If you experience chest pain and respiratory difficulties, you should report to your doctors immediately.<ref>Lexi-Comp, Lexi-Drugs Online : Ibutilide.</ref>
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| == References ==
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| <references/>
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| {{Antiarrhythmic agents}}
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| [[Category:Antiarrhythmic agents]]
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| [[Category:Drugs]]
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