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Cardiovascular Drug Introduction
Cardiovascular medications can be broken down into the following categories
Antiarrhythmics
Antihypertensives
Inotropes
Vasodilators
Diuretics
Antihyperlipidemics
Antiplateletes
Thrombolytics
Class I Na+ Channel Blockers
General principles
slow or block Na+ conduction preferentially in depolarized cells
selective for abnormal cardiac tissue that is frequently depolarized
use and state dependence
phase 4 depolarization in SA node (automaticity current) is dependent on Na+ channel
opening
blockage results in ↓ slope of phase 4 depolarization and ↓ SA node rate
hyperkalemia causes ↑ toxicity for all class I drugs
Class IA
Examples
quinidine, procainamide, disopyramide
remember: quin + the amides
Effects
acts on atrial and ventricular arrhythmias
especially reentrant and ectopic
supraventricular and ventricular tachycardia
↓ rate of phase 0 depolarizating resulting in
↑ QT interval
↑ AP duration
↑ effective refractory period (ERP)
Toxicity
quinidine
cinchonism
headache, tinnitus, vertigo
thrombocytopenia
↑ QT interval
can result in torsades de pointes
can enchance digoxin toxicity
procainamide
reversible SLElike syndrome
remember: procAiNAmide (antinuclear antibody in SLE)
Class IB
Examples
lidocaine, mexiletine, tocainide
phenytoin can also fall into class IB
Effects
acts on ischemic or depolarized Purkinje and
ventricular tissue
does not act on healthy or atrial tissue
effective in treating structurally abnormal tissue
(especially postMI)
useful in acute ventricular arrhythmias and in digitalisinduced arrhythmias
↓ rate of phase 3 repolarization resulting in
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↓ AP duration
Toxicity
local anesthetic
CNS stimulation/depression
Class IC
Examples
flecainide, encainide, propafenone
Effects
acts on HisPurkinje system in cardiac tissue
WITHOUT structural abnormalities
useful in Vtachs progressing to VF and
refractory SVT
drugs of last resort
no effect on AP duration
Toxicity
proarrhythmic
contraindicted with structural abnormalities
e.g., postMI
significantly prolongs refractory period in AV node
Use Dependence
Higer rates of depolarization = increased Na+ channel blockade due to channels spending less
time in the resting state
type 1C antiarrythmics
bind Na+ channels the strongest
have the highest likelihood of use dependence
type 1B antiarrythmics
bind the least avidly to Na+ channels
minimal cumulative effect over multiple cardiac cycles
more selective for ischemic myocardium
lowest likelihood of use dependence
Na+ channel binding strength:
1C > 1A > 1B
Class II βblockers
Examples
propranolol, esmolol, metoprolol, atenolol, timolol
esmolol very short acting
Mechanism
↓ slope of phase 4 resulting in ↓ automaticity
due to ↓ cAMP, ↓ Ca2+ currents
results in ↑ PR interval, ↓ conduction in AV node
Clinical use
ventricular tachycardia, SVT
slowing ventricular rate during atrial fibrillation and atrial flutter
postMI arrhythmia prophylaxis (cardioprotective)
Toxicity
cardiovascular effects
bradycardia, AV block, CHF
CNS effects
sedation, sleep alterations, depression
may mask the signs of hypoglycemia
impotence
exacerbation of asthma
only for nonselective (nonbeta1 specific)
metoprolol can cause dyslipidemia
treat overdose with glucagon
↑ cAMP via a mechanism independent of beta receptors
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Class III K+ Channel Blockers
Examples
sotalol, ibutilide, bretylium, dofetilide, amiodarone
Mechanism
↑ phase 3
due to ↓ K+ current
results in ↑ AP duration, ↑ ERP, ↑ QT interval
effective for antrial and ventricular arrhythmias
antiarrhythmics of last resort
amiodarone has class I, II, III, and IV effects
due to alterations lipid membrane
Toxicity
torsades de pointes due to ↑ QT interval
amiodarone is the only example of a drug that lengthens QT but does not have risk of
torsades de pointes
sinus bradycardia
sotalol
excessive β blockade
bretylium
new arrhythmias
↓ BP
amiodarone
pulmonary fibrosis
hepatotoxicity
hypothyroidism/hyperthyroidism
amiodarone is 40% iodine by weight (amIODarone)
must watch LFTs, TFTs, PFTs
corneal deposits
photosensitivity
skin color changes (blue/gray)
neurologic effects
constipation
cardiovascular effects
bradycardia, heart block, CHF
Class IV Ca2+ Channel Blockers
Examples
verapamil, diltiazem
note: other Ca2+ channel blockers (nifedipine, amlodipine) have little action on the
heart
Mechanism
↓ Ltype Ca2+ channels current primarily in AV nodal cells
Ltype Ca2+ channels responsible for the plateau phase
results in ↓ conduction velocity, ↑ ERP, ↑ PR interval
used in prevention of nodal arrhythmias, AV nodal reentry
Toxicity
antimuscarinic effects
constipation, diziness, flushing
edema
CV effects
negative ionotropy, AV block, sinus node depression
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