Na+ Channel Blockers, Phase 0
Class effects: Proarrhthy mic effects
Monitor for QTc prolongation
Class 1C
Class 1A Class 1B
Do not use in pts with structural heart disease
Propafenone (Rythmol)
Procainamide Lidocaine (Xylocaine) - Ventricular arrhythmia
Disopyramide (Norpace) - V-tach Mexiletine Flecainide
Quinidine - Ventricular arrhythmia (IR)
- AVRT (off-label) - Ventricular arrhythmia - Ventricular arrhythmia
- A-fib/flutter (Vfib, pulseless VT) - a-fib/flutter, SVT,
- Ventricular arrhythmia - a-fib w/preexcitation - A-fib/flutter or SVT
- paroxymal a-fib/flutter - local anesthesia maintenance of sinus
(off-label)
- ventricular arrhthymia rhythm (ER and IR)
- Malaria (children)
IV Formulation Capsule
Capsule: IR and ER Tablet Capsule:
IR/ER
Tablet: IR and ER
Contiuous infusion, IV, IM
MOA: MOA:
- MOA: decreases - Supresses MOA: MOA:
- slows conduction of
myocardial automaticity of - Dec rate of rise of - local anesthetic
cardiac tissue by
excitability and conduction tissue, by phase 0, inc effective properties
altering ion transport
conduction velocity; MOA: inc stimulation refractory period/AP
MOA: across membranes - blocks inward Na
reduces disparity b/n - Phase 0 depression threshold of duration ratio
- Dec myocardial - slight prolongation of current and slows
normal and infarcted of AP ventricle, - Dosing:
excitability, refractory periods
myocardium - Dec myocardial his-purkinje system, - Take w/food or rate of increase of
conduction velocity, - decreases rate of
- Dosing: excitability, spontaneous antacid (alkaline AP
and may depress rise of AP w/o
- CrCl <40 not rec conduction velocity, depolarization of enviornment) - Prolongs conduction
contractility by inc affecting duration
- Renal dose adj. and contractility by ventricles during - Max 1.2 g/day
stimulation threshold - inc stimulation and refractory in
- Weight based dec Na influx in diastole by direct - Can use loading dose
of ventricle, threshold of myocardium w/
- Q6hrs depolarization and K action on tissue. - BBW:
his-purkinje system, ventricle, slightly more
efflux in - blocks - AKI (esp w/CHF or his-purkinje system
direct cardiac effects
repolarization initiation/conduction ischemia) - local anesthetic and pronounced effect on
- Dosing:
- Reduces Ca+ of nerve impulses by negative inotropic IV conduction;
- Renal adj CrCl <50
transport across dec membrane effects prolongs refractory
- NAPA: 15-25mcg/mL
membrane permeability to Na,
- Procainamide: 4-10 period, reduces
inhibition of
mcg/mL spontaneous
depolarization
w/resultant blockade automaticity, and
of conduction C/I: exhibits
C/I: C/I:
- Cardiogenic beta-blockade
- Cardiogenic - Hypersensitivity
shock activity
shock C/I: - 2nd/3rd deg AV
- 2nd/3rd deg AV - some neg inotropic
- 2nd/3rd deg - Heart block >1st block w/o block or RBBB
block w/o activity
degree C/I: C/I: pacemaker associated w/left
pacemaker - Idioventricular - Sensitivity to any - Hypersensitivity hemiblock
- Congenital long conduction delays component of - cardiogenic shock
- Adam-stokes
Qt syndrome w/o pacemaker formulation syndrome - concurrent use of
- Use w/quinolones - complete heart ritonavir C/I:
- WPW
(prolong QT), block - Dosing: - Hypersensitivity
- Severe degrees
cisapride, or - AV block (2nd) or - Renal adj CrCl <35 - SA, AV, IV
of SA/AV/IV
ritonavir any hemiblock w/o - Avoid in disorders of
block SE:
- Thrombocytopenia pacemaker hepatic/renal impulse generation
- corn-derived - Blood dyscrasias
SE: and TTP - SLE impairment or conduction w/o
Monitoring: dextrose - DRESS
- xerostomia - Sensitivity to - Torsades de pointes pacemaker
- ECG/BP - Arrhythmia exac
- constipation anticholinergic BBW - Brugada syndrome
- Urinary retention - Dizziness
- urinary hesitancy effects - SLE (drug induced) - Bradycardia
- CNS - Ataxia
- Anticholinergic - blood dyscrasias SE: - cardiogenic shock
anticholinergic - nervousness
and inotropic - Proarrhythmic - heart failure
effects - GI distress Monitoring:
effects effects - marked
- S/s heart failure - N/V - ECG/HR/BP
- 1:1 AV conduction hypotension
- drug levels - Tremor - Serum conc (esp
Monitoring: - Fatal - bronchospastic
SE: hepatic/renal disorder/severe
- LFTs complications
Warnings: SE: - Bradycardia impairment, COPD]
- ECG w/structural heart
- Hemolysis-G6PD - QT prolongation - Hypotension pediatric and - marked electrolyte
SE: Monitoring: - Neuro s/s of disease
- Hepatotoxicity - thrombocytopenia - vomiting amiodarone use) balance
- Agranulocytosis - ECG/BP toxicity - Dizziness
IR: q6h - diarrhea/stomach - tinnitus - Visual
- hypotension - Renal/Liver - Serum conc (>24
ER: q8-12hr cramps - blurred vision distubances
- bradycardia - CBC w diff hr infusion)
Take w/food: GI upset - GI distress - CNS toxicity
- rash - blood conc Monitoring:
Monitoring: - dizziness SE:
- lupus-like (kidney/liver - ECG/BP/Pulse
- ECG, CBC, Liver/Renal - drug-induced lupus - N/V
syndrome impairment or IV Drug interactions:
- cinchonism - Metallic taste
- diarrhea infusion) - inc digoxin conc
- Dizziness
- inc warfarin
- Visual
conc
disturbances