ANTI-ARRHYTHMICS DRUGS - CARDIOVASCULAR DRUGS (2/7)
Class l Na+ Channel Blocker
Block voltage gated Na+ channel like local anesthetics..slow the rate of rise of Phase 0.
High affinity for Active & Inactive channels..little effect on resting..decrease excitability & conduction velocity..
Cause Pro-Arrhthymic effects……
QT interval prolongation.
Use- Dependance
Class l bind to open or inactivated sodium channel than are fully repolarized…show great degree of blockade during depolarizing stage
Block the cell discharging at high frequency without interfering normal mal one
S.E=anticholinergic side effects like dry mouth, urinary retention,constipation etc
channel..little effect on Rate of Depolarization
Lidocaine= Class lB drug...Local Anesthetic..Shorten Phase 3 repolarization..
T.E=used in Ventrical Arrhythmia in Myocardial Infarction(M.I)…
S.E=Slurred speech, Paresthesia, Convulsion, Cradiac Arrhythmia
Mexiletine & Tocainide=Class lB drugs ...similar actions to Lidocaine…
Mexiletine used for Chronic Treatment of Ventricular Arrhythmia with previous M.I
Tocainide used for Ventricular Tachyarrhythmia…has Pulmonary toxicity
Class lC=Depress the Rate of rise of Action Potential..marked slowing of conduction…little effect on Duration of Action Potential…bind Slowly to Na+ channel
Flecainide= Class lC drug….suppress Phase 0 stroke in Perkinji & Myocardial fibres…
Automaticity reduced by increasing Threshold Potential
T.E=used for Refractive Ventricular Arrhythmia…Prevention of Paroxysmal Atrial
Fibrillation/Flutter…-Ve Inotropic aggravate CHF….Suppress Premature Contractions
S.E= t1/2 16-20hr...dizziness, headache, blurred vision
Propafenone= Broad Spectrum Anti-Arrhythmic agent
Class ll Anti-arrhythmic
β-Adrenergic Antagonists..diminish Phase 4 depolarization..Prolong AV conduction..
Decreasing Heart rate & contractility
Propranolol=prevent Arrhythmia after M.I
Metoprolol=used in Cardiac Arrhythmia
Esmolol=in Acute arrhythmia in surgery or emergency situation
Class lll Antiarrhythmic
Block K+ channel...diminish K+ in repolarization stage..Prolong Duration of Action Potential...Prolong Refractory period..
Amiodarone=AntiAnginal drug...contain Iodine(I2)...structure like Thyroxine...
show Class I, Class ll, Class lll, ClassIV activity
T.E= used in Refractive Supraventricular & Ventricular TachyarrhythmiaS.E=t1/2 of 6week…cause Blue color skin...Photosensitivity, Hypo or
Hyperthyroidism.. Neuropathy, Muscle weakness
Dronedarone=Benzofuran Amiodarone derivative...dont have I2...used in Atrial Fibrillation
Sotalol=β-Blocker + Antiarrhythmic……….TWO isomer : L-Isomer & d-Isomer….
used in Acute M.I…..Block rapid outward K+ current, known as”Delay Rectifier”
S.E= Prolong QT interval
Dofetilide= First line Antiarrhythmic in Patients with persistent Atrial Fibrillation & Heart Disease….risk of Pro-Arrhythmia…
Class IV Antiarrhythmic
Block Ca++channel...decrease Phase 4 depolarization…slow conduction
Verapamil & Diltiazim=greater action on heart…-Ve Inotropic…use-dependent..
T.E=used in Ventricular arrhythmia, Supraventricular Tachycardia, Atrial Flutter
Other Antiarrhythmic
Digoxin=shorten Refractory period in Atrial & Ventricular …prolong effective Refractory period...slow conduction
Adenosine= naturally occurring Nucleoside…extreme short duration of action 15sec…..
DOC in Acute SupraVentricular Tachycardia…cause Flushing, Chest pain, Hypotension
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