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Details on Person Antiarrhythmic drugs are a class of cardiovascular drugs tha...
| Class:Id | Summation:9612739 |
|---|---|
| _displayName | Antiarrhythmic drugs are a class of cardiovascular drugs tha... |
| _timestamp | 2018-07-02 10:53:45 |
| created | [InstanceEdit:9612712] Jassal, Bijay, 2018-06-29 |
| literatureReference | [LiteratureReference:9612724] Classification of antidysrhythmic drugs [LiteratureReference:9612749] Quinidine in short QT syndrome: an old drug for a new disease [LiteratureReference:9612730] Conversion of atrial fibrillation to sinus rhythm by acute intravenous procainamide infusion [LiteratureReference:9612736] Effects of intravenous disopyramide and quinidine on normal myocardium and on the characteristics of arrhythmias: intraindividual comparison in patients with sustained ventricular tachycardia [LiteratureReference:9612735] Cardiac sodium channels (hH1) are intrinsically more sensitive to block by lidocaine than are skeletal muscle (mu 1) channels [LiteratureReference:9612710] Antiarrhythmic Mexiletine: A Review on Synthetic Routes to Racemic and Homochiral Mexiletine and its Enantioseparation [LiteratureReference:9612717] Pharmacological targeting of long QT mutant sodium channels [LiteratureReference:9612721] The use of oral mexiletine for the treatment of pain after peripheral nerve injury [LiteratureReference:9612714] Mexiletine for treatment of myotonia: a trial triumph for rare disease networks [LiteratureReference:9612744] Tocainide: a new drug for ventricular arrhythmias [LiteratureReference:9612719] Chemistry, pharmacology, antiarrhythmic efficacy and adverse effects of tocainide hydrochloride, an orally active structural analog of lidocaine [LiteratureReference:9612904] Propafenone: a new antiarrhythmic agent [LiteratureReference:9612902] Flecainide: a new prototype antiarrhythmic agent |
| modified | [InstanceEdit:9612905] Jassal, Bijay, 2018-07-02 [InstanceEdit:9612917] Jassal, Bijay, 2018-07-02 |
| text | Antiarrhythmic drugs are a class of cardiovascular drugs that affect the cardiac action potential to suppress abnormal rhythms of the heart (cardiac arrhythmias) such as atrial fibrillation, atrial flutter, ventricular tachycardia and ventricular fibrillation. In the Vaughan Williams classification of cardiovascular drugs ((Williams 1975), class I agents interfere with the sodium (Na+) channel (Tikhonov & Zhorov 2017). Blockade of the cardiac Na+ channel reduces the initial depolarization of the action potential, thereby slowing impulse propagation. As well their use in cardiovascular medicine, Na+ channel blockers are also used as local anesthetics and anticonvulsants. There are three subgroups of class I agents (Milne et al. 1984), Ia, Ib and Ic (Milne et al. 1984). Class Ia agents block the fast sodium channel, which depresses the phase 0 depolarization (i.e. reduces Vmax), which prolongs the action potential duration by slowing conduction. Agents in this class also cause decreased conductivity and increased refractoriness (recovery time). The overall effect of class Ia agents is to lengthen the action potential (shift it to the right of normal). Example drugs of this class are quinidine, procainamide and disopryamide. Quinidine is a stereoisimer of quinine, originally derived from the bark of the cinchona tree. It is used as an antiarrhythmic drug to prevent ventricular arrhythmias, to maintain sinus rhythm after cardioversion of atrial fibrillation and to treat short QT syndrome (Kaufman 2007). Procainamide is an aminobenzamide, structurally similar to procaine. It is used to treat various cardiac arrhythmias (Fenster et al. 1983). Disopyramide is used in the treatment of ventricular tachycardia, decreasing/blocking the inward Na+ current (Rizos et al. 1987). Class Ib agents block Na+ channels which decrease the action potential frequency by lengthening the depolarization phase. The overall effect is to shorten the action potential (shift it to the left of normal). Example drugs of this class are lidocaine, phenytoin, mexiletine and tocainide. Lidocaine is used to treat ventricular tachycardia and to perform nerve blocks, but also serves as a local anaesthetic (Nuss et al. 1995). Phenytoin is an anti-seizure medication that may also be used for certain heart arrhythmias when other antiarrhythmic medications have failed. Mexiletine is a racemic mixture of two enantiomers (Catalano & Carocci 2016) and is an analogue of lidocaine. It is used to treat cardiac arrhythmias or seriously irregular heartbeats (Wang et al. 1997). It is also used for the treatment of neuropathic pain (Chabal et al. 1992) and myotonia (Hoffman & Kaminski 2012). Tocainide is also a lidocaine analogue and is found as a mixture of two enantiomers. The R isomer is 4x as potent as the S. It is used in the treatment of ventricular arrhythmias (Volosin & Greenspon 1986, Alpert et al. 1983). Class Ic agents depress the phase 0 depolarization (decreasing Vmax) thereby decrease conductivity, but have a minimal effect on the action potential duration. Of the three class I agents, class Ic agents are the most potent sodium channel blockers. Example drugs of this class are propafenone and flecainide. Propafenone is a racemate of S(+)- and R(-)-enantiomers and is used to treat atrial and ventricular arrhythmias (Chow et al. 1988). Propafenone differs from prototypical Ic drugs in that it has additional beta-adrenergic blocker activity which can cause bradycardia and bronchospasm. Flecainide is used in the treatment of many types of supraventricular tachycardias, including AV nodal re-entrant tachycardia (AVNRT) and Wolff-Parkinson-White syndrome (WPW) (Nappi & Anderson 1985). |
| (summation) | [Reaction:9612559] Class I antiarrhythmics bind SCNAs:SNCBs [Homo sapiens] |
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