DA II exam 3 (kuhl - chart)

class 1 blocks what channel?

sodium → phase 0

class 1 MOA

block fast sodium channels → slower phase 0 → slower conduction (increased QRS)

increased threshold → decreased automaticity

block builds at fast heart rates and in depolarized (ischemic) tissue

acidosis increases block

which drug class blocks fast sodium channels → slower phase 0 → slower conduction (increased QRS)?

class 1

which class increased threshold → decreased automaticity?

class 1

which class causes block to build at fast heart rates and in depolarized (ischemic) tissue?

class 1

which class increases block with acidosis?

class 1

class 1 BBW

reserve for life-threatening ventricular arrhthymias

which class has a BBW of being reserved for life-threatening ventricular arrhthymias?

class 1

T/F: slowing atrial flutter can allow 1:1 AV conduction (faster ventricular rate)

true

what should be given when 1:1 AV conduction?

give AV nodal blocker first with 1A and 1C agents

when is an AV-nodal blocker (1A and 1C) given?

1:1 AV conduction

what are the class 1A drugs?

procainamide

disopyramide

quinidine

procainamide class

1A sodium

procainamide class

1A sodium

quinidine class

1A sodium

what is the net effect of class 1A?

moderate sodium/potassium block → increase APD/ERP/QT (TdP risk)

which class has a moderate Na/K block that leads to an increase in ADP/ERP/QT?

class 1A

what does class 1A do in damaged tissue?

increase threshold and decrease phase-4 slope

which class increases threshold and decreases phase-4 slope in damaged tissue?

class 1A

what kind of activity is additive across all 1A agents?

anticholinergic (vagolytic)

quinidine has what kind of block?

sodium/potassium channel block

no beta block

alpha-block & vagolytic (anticholinergic) → IV hypotension

which class 1A drug has mainly sodium/potassium channel block and no beta blocking activity?

quinidine

which class 1A drug has alpha blocking + vagolytic that increases risk of hypotension with IV?

quinidine

what class 1A drug used to be used for severe falciparum malaria?

quinidine

what was quinidine used for?

severe falciparum malaria

how is quinidine eliminated?

hepatically

quinidine BBW

increased mortality with antiarrhythmic therapy

which drug has a BBW of increased mortality with antiarrhythmic therapy?

quinidine

quinidine ADRs

NVD

cinchonism

immune thrombocytopenia

increased QTc/TdP

which drug has ADRs of cinchonism, immune thrombocytopenia, and increased QTc/TdP?

quinidine

quinidine DDI

potent CYP2D6 inhibitor

Pgp inhibitor - increased digoxin conc. → should reduce digoxin dose

which class 1A drug has interaction with CYP2D6 enzyme and Pgp?

quinidine

what does procainamide block?

potassium

which class 1A drug blocks only potassium?

procainamide

what is the active metabolite of procainamide?

NAPA (N-acetylprocainamide)

NAPA is the active metabolite of what drug?

procainamide

how is procainamide eliminated?

renally

which class 1A drug is eliminated renally?

procainamide

which class 1A drug causes hypotension from ganglionic blockade (rapid IV, LV dysfunction)?

procainamide

what can procainamide cause due to ganglionic blockade (rapid IV, LV dysfunction)?

hypotension

procainamide BBW

(+) ANA → lupus-like syndrome (sooner in slow acetylators)

blood dyscrasias/bone marrow suppression - agranulocytosis (first 12 weeks)

reserve for life-threatening ventricular arrhythmias (increased mortality)

which drug has a BBW of (+) ANA → lupus-like syndrome (sooner in slow acetylators), blood dyscrasias/bone marrow suppression - agranulocytosis (first 12 weeks), and reserve for life-threatening ventricular arrhythmias (increased mortality)?

procainamide

disopyramide niche

obstructive hypertrophic cardiomyopathy

which drug has niche of obstructive hypertrophic cardiomyopathy?

disopyramide

disopyramide pharmacology activity

prominent anticholinergic activity

negative inotrope

which drug has prominent anticholinergic activity + negative inotropy?

disopyramide

how is disopyramide eliminated?

hepatic + renally

which class 1A drug is eliminated both renally and hepatically?

disopyramide

what dose should disopyramide be reduced at?

CrCl <40; avoid CR

which class 1A drug only has BBW of reserved life-threatening ventricular arrhythmias (increased mortality)?

disopyramide

disopyramide ADRs

anticholinergic - urinary retention (esp prostatic hypertrophy), constipation, dry eyes/mouth

HF exacerbation

which class 1A drug has prominent anticholinergic side effects + HF exacerbation?

disopyramide

which class 1A drug should be avoided due to anticholinergic/HF risk according to beer’s criteria?

disopyramide

which class 1A drug should specifically be given an AV-nodal blocker first in AF/flutter?

disopyramide

disopyramide should be avoided in what population?

older adults due to anticholinergic/HF risk

what drug is given when one has AF/flutter while taking disopyramide?

AV-nodal blocker

what is the net effect of class 1B drugs?

slight decrease (or no change) in APD/ERP

rapid association/dissociation

weak sodium block (T<1s) → acts mainly in ischemic, depolarized, or rapidly firing ventricle tissue

little effect in atria

which drug class has net effect of slight decrease in ADP/ERP, rapid association/dissociation, weak sodium block that acts mainly in ischemic, depolarized, or rapidly firing ventricle tissue, and very little effect in atria?

class 1B

what are the class 1B drugs?

lidocaine

mexiletine

lidocaine class

1B sodium channel

mexiletine class

1B sodium channel

how is lidocaine given?

IV load + infusion due to rapid hepatic elimination

which class 1B drug is given via IV load + infusion?

lidocaine due to rapid hepatic elimination

when does lidocaine clearance decrease?

HF (decreased volume distribution may also occur)

hepatic disease

beta-blockers or cimetidine

infusions given longer than 24 hours

which drug has decreased clearance with HF or hepatic disease or beta blockers/cimetidine or longer infusions?

lidocaine

risk of lidocaine metabolites

accumulation in renal failure → toxicity

lidocaine CI

wolff-parkinson-white

which drug is contraindicated in wolff-parkinson-white?

lidocaine

lidocaine ADRs

CNS toxicity (perioral numbness, lightheadedness, dizziness, blurred vision, nystagmus, paresthesias, slurred speech)

tremor → seizures at high levels

which drug has lots of CNS side effects + tremors that can lead to seizures (high bolus)?

lidocaine

lidocaine DDI

amiodarone

beta blockers (propranolol)

cimetidine

all decrease clearance → increase levels/toxicity

which drug has DDI with amiodarone, beta blockers (propranolol), and cimetidine?

lidocaine

lidocaine acts a what?

local anesthetic

why can mexiletine be given PO?

resists first-pass metabolism

which drug can be given PO because it resists first-pass metabolism?

mexiletine

how is mexiletine eliminated?

hepatically

mexiletine BBW

reserve for life-threatening ventricular arrhythmias

which 1B drug has BBW of being reserved for life-threatening ventricular arrhythmias?

mexiletine

mexiletine ADRs

NV

CNS - tremor, dizziness, incoordination, numbness/paresthesias, blurred vision

which 1B drug has both GI and CNS side effects?

mexiletine

mexiletine DDI

increased theophylline levels

which drug increases theophylline levels?

mexiletine

how should mexiletine be taken?

with food

which 1B drug has a counseling point of being taken with food?

mexiletine

class 1C drugs

flecainide

propafenone

encainide (discontinued)

flecainide class

1C sodium channel

propafenone class

1C sodium channel

1C class net effect

strong sodium block (T >10s) → increased PR/QRS

which drug class has a net effect of strong sodium block leading to increased PR/QRS?

1C sodium channel

when is class 1C not given?

structural heart disease or prior MI → proarrhythmia (CAST)

which drug class should only be given in structurally normal hearts and not in structural heart disease or prior MI?

class 1C sodium

how is flecainide metabolized?

CYP2D6

which class 1C drug is metabolized by CYP2D6?

flecainide

which drug should not be given when CrCl<35?

flecainide → reduce dose

when should flecainide dose be reduced?

CrCl < 35

flecainide BBW

CAST - increased mortality/no-fatal arrest post MI

not recommended for chronic AF

ventricular proarrhythmia in AF/flutter

which 1C drug has BBW of increased mortality/non-fatal arrest post-MI, not recommended for chronic afib, and ventricular proarrhythmia in afib/flutter?

flecainide

flecainide ADRs

visual disturbances (blurred vision)

HF exacerbation

which 1C drug has ADRs of visual disturbances and HF exacerberation?

flecainide

flecainide DDI

CYP2D6 inhibitors (quinidine/fluoxetine)