THE SECTION Cardiovascular Disorders

Arrhythmias and Conduction

MERCK MANUALS FOR HEALTHCARE
SUBJECT
TOPIC
Disorders
Introduction
ONLINE MEDICAL LIBRARY P R O F E S S I O N A L S

ANTIARRHYTHMIC DRUGS (VAUGHAN-WILLIAMS

CLASSIFICATION)
Target
Drug Dosage Levels Adverse Effects Comments

CLASS IA Uses: APB and VPB suppression, SVT and VT suppression, AF or atrial flut-
ter, and VF suppression
Disopyramide IV: Initially, 1.5 2–7.5 Anticholinergic Drug should be used
mg/kg over µg/mL effects (urinary cautiously in
> 5 min, retention, glaucoma, patients with
followed by an dry mouth, blurred impaired LV func-
infusion of 0.4 vision, intestinal tion.
mg/kg/h upset), hypo- Dosage should be
Oral immediate- glycemia, torsades decreased in
release: 100 or de pointes, ventricu- patients with renal
150 mg q 6 h lar tachycardia; neg- insufficiency.
ative inotropic
Oral controlled- effects (which may Adverse effects may
release: 200 or worsen heart failure contribute to non-
300 mg q 12 h or hypotension), adherence.
torsade de pointes, If QRS interval
ventricular tachy- widens (> 50% if
cardia initially < 120
msec or > 25% if
initially > 120
msec) or if QTc
interval is pro-
longed > 550
msec, infusion rate
or dosage should
be decreased or
drug stopped.
IV form is not avail-
able in the US.
Procainamide IV: 10–15 mg/kg 4–8 g/mL Hypotension (with IV Sustained-release
bolus at 25–50 infusion), serologic preparations obvi-
mg/min, fol- abnormalities (espe- ate the need for
lowed by a con- cially ANA) in frequent dosing.
stant IV infu- almost 100% taking
sion of 1–4 drug for > 12 mo,
mg/min drug-induced lupus If QRS interval
(arthralgia, fever, widens (> 50% if
Oral: 250–625
mg (rarely, up pleural effusions) in initially < 120
15–20%, agranulo- msec or > 25% if
to 1 g) q 3 or initially >120
4h cytosis in < 1%, tor-
sades de pointes, msec) or if QTc
ventricular tachy- interval is pro-
cardia longed > 550
msec, infusion rate
or dosage should
be decreased or
drug stopped.
 THE SECTION Cardiovascular Disorders
Arrhythmias and Conduction
MERCK MANUALS FOR HEALTHCARE
SUBJECT
TOPIC
Disorders
Introduction
ONLINE MEDICAL LIBRARY P R O F E S S I O N A L S

ANTIARRHYTHMIC DRUGS (VAUGHAN-WILLIAMS

CLASSIFICATION)—Continued
Target
Drug Dosage Levels Adverse Effects Comments

Quinidine Oral: 200–400 2–6 Diarrhea, colic, flatu- If QRS interval

mg q 4–6 h µg/mL lence, fever, throm- widens (> 50% if
bocytopenia, liver initially < 120
function abnormali- msec or > 25% if
ties, torsades de initially >120
pointes, ventricular msec) or if QTc
tachycardia; overall interval is pro-
adverse effect rate of longed > 550
30% msec, infusion rate
or dosage should
be decreased or
drug stopped.

CLASS IB Uses: Suppression of ventricular arrhythmias (VPB, VT, VF)

Lidocaine IV: 100 mg over 2–5 µg/L Tremor, seizures; if To reduce toxicity
2 min, followed administration is too risk, dosage or
by continuous rapid, drowsiness, infusion rate
infusion of 4 delirium, paresthe- should be reduced
mg/min (2 sias; possibly to 2 mg/min after
mg/min in increased risk of 24 h.
patients > 65); bradyarrhythmias Extensive first-pass
5 min after first after acute MI hepatic metabo-
dose, a 2nd 50- lism occurs.
mg bolus is
given

Mexiletine Oral immediate- 0.5–2 Nausea, vomiting, Oral slow-release

release: µg/mL tremor, seizures and IV forms are
100–250 mg po not available in
q8h the US.
Oral slow-
release: 360 mg
po q 12 h
IV: 2 mg/kg at 25
mg/min, fol-
lowed by 250-
mg infusion
over 1 h, 250-
mg infusion
over next 2 h,
and mainte-
nance infusion
of 0.5 mg/min
 THE SECTION Cardiovascular Disorders
Arrhythmias and Conduction
MERCK MANUALS FOR HEALTHCARE
SUBJECT
TOPIC
Disorders
Introduction
ONLINE MEDICAL LIBRARY P R O F E S S I O N A L S

ANTIARRHYTHMIC DRUGS (VAUGHAN-WILLIAMS

CLASSIFICATION)—Continued
Target
Drug Dosage Levels Adverse Effects Comments

CLASS IC Uses: APB and VPB suppression, SVT and VT suppression, AF or atrial flut-
ter, and ventricular fibrillation suppression
Flecainide Oral: 100 mg q 8 0.2–1 Occasionally, blurred IV form is not avail-
or 12 h µg/mL vision and paresthe- able in US.
IV: 1–2 mg/kg sias If QRS complex
over 10 min widens (> 50% if
initially < 120
msec and > 25% if
initially > 120
msec), dose must
be decreased or
drug stopped.

Propafenone Oral: Initially, 0.1–1.0 β-blocking activity, Pharmacokinetics is

150 mg tid, µg/mL possible worsening nonlinear; increases
titrated up to of reactive airway in dose should not
150–300 mg tid disorders; occasion- exceed 50% of
ally, GI upset previous dose.
IV: 2-mg/kg Bioavailability and
bolus, followed protein binding
by 2 mg/min vary; drug has sat-
infusion urable first-pass
metabolism.
IV form is not avail-
able in the US.

CLASS II Uses: Supraventricular tachyarrhythmias (APB, ST, SVT, AF, atrial flutter)
β-Blockers and ventricular arrhythmias (often in a supportive role)

Atenolol Oral: 50–100 mg Drug GI disturbances, These drugs are

once/day levels not insomnia, night- contraindicated in
measured; mares, lethargy, patients with bron-
dose erectile dysfunction, chospastic airway
adjusted possible AV block disorders.
to reduce in patients with AV
heart rate node dysfunction
by
> 25%

Carvedilol Oral: Initially,

6.25 mg bid,
followed by
titration to 25
mg bid
 THE SECTION Cardiovascular Disorders
Arrhythmias and Conduction
MERCK MANUALS FOR HEALTHCARE
SUBJECT
TOPIC
Disorders
Introduction
ONLINE MEDICAL LIBRARY P R O F E S S I O N A L S

ANTIARRHYTHMIC DRUGS (VAUGHAN-WILLIAMS

CLASSIFICATION)—Continued
Target
Drug Dosage Levels Adverse Effects Comments

Acebutolol Oral: 200 mg bid

Betaxolol Oral: 20 mg
once/day

Bisoprolol Oral: 5–10 mg

once/day

Esmolol IV: 50–200

µg/kg/min

Metoprolol Oral: 50–100 mg

bid
IV: 5 mg q 5 min
up to 15 mg

Nadolol Oral: 60–80 mg

once/day
Propranolol Oral: 10–30 mg
tid or qid
IV: 1–3 mg (may
repeat once
after 5 min if
needed)
Timolol Oral:10–20 mg
bid
CLASS III Uses: Any tachyarrhythmia except torsades de pointes VT
Membrane-
stabilizing
drugs
Amiodarone Oral: 600–1200 1–2.5 Pulmonary fibrosis (in Drug has noncom-
mg/day for µg/mL up to 5% of patients petitive β-block-
7–10 days, then treated for > 5 yr), ing, Ca channel
400 mg/day for which may be fatal; blocking, and Na
3 wk, followed QTc prolongation; channel blocking
by a mainte- torsades de pointes effects, with a long
nance dose (rare); bradycardia; delay in onset of
(ideally, £ 200 gray or blue discol- action.
mg/day) oration of sun- By prolonging
IV: 150–450 mg exposed skin; sun refractoriness,
over 1–6 h sensitivity; hepatic drug may produce
(depending on abnormalities; homogeneous con-
urgency), fol- peripheral neuropa- ditions of repolar-
lowed by a thy; corneal ization throughout
maintenance microdeposits (in the heart.
dose of 0.5–2.0 almost all treated
patients), usually IV form can be used
mg/min for conversion.
without serious
visual effects and
reversed by stopping
the drug; changes in
thyroid function;
slow clearance pos-
sibly prolonging
adverse effects
 THE SECTION Cardiovascular Disorders
Arrhythmias and Conduction
MERCK MANUALS FOR HEALTHCARE
SUBJECT
TOPIC
Disorders
Introduction
ONLINE MEDICAL LIBRARY P R O F E S S I O N A L S

ANTIARRHYTHMIC DRUGS (VAUGHAN-WILLIAMS

CLASSIFICATION)—Continued
Target
Drug Dosage Levels Adverse Effects Comments

Azimilide Oral: 100–200 200–1000 Torsades de pointes —

mg once/day ng/mL VT

Bretylium* IV: Initially, 5 0.8–2.4 Hypotension Drug has class II

mg/kg, fol- µg/mL properties.
lowed by 1–2 Effects may be
mg/min as a delayed 10–20
constant infu- min.
sion
Drug is used to treat
IM: Initially, potentially lethal
5–10 mg/kg, refractory ventric-
which may be ular tachyarrhyth-
repeated to a mias (intractable
total dose of VT, recurrent VF),
30 mg/kg for which it is usu-
IM maintenance ally effective with-
dose of 5 mg/kg in 30 min of injec-
q 6–8 h tion.

Dofetilide IV: 2.5–4 µg/mL N/A Torsades de pointes Drug is contraindi-

Oral: 500 mg bid VT cated if QTc > 440
if CrCl > 60 msec or if CrCl <
mL/min; 250 20 mL/min.
mg bid if CrCl
is 40–60
mL/min; 125
mg bid if CrCl
is 20–40
mL/min
 THE SECTION Cardiovascular Disorders
Arrhythmias and Conduction
MERCK MANUALS FOR HEALTHCARE
SUBJECT
TOPIC
Disorders
Introduction
ONLINE MEDICAL LIBRARY P R O F E S S I O N A L S

ANTIARRHYTHMIC DRUGS (VAUGHAN-WILLIAMS

CLASSIFICATION)—Continued
Target
Drug Dosage Levels Adverse Effects Comments

Ibutilide IV: For patients N/A Torsades de pointes Drug is used to ter-
60 kg, 1 mg VT (in 2%) minate AF (suc-
infusion or, for cess rate, about
patients < 60 40%) and atrial
kg, 0.01 mg/kg flutter (success
over 10 min, rate, about 65%).
with dose
repeated after
10 min if the
first infusion is
unsuccessful

Sotalol Oral: 80–160 mg 0.5–4 Similar to class II; Racemic [D-L] form
q 12 h µg/mL possible depressed has class II (beta-
IV: 10 mg over left ventricular func- blocking) proper-
1–2 min tion and torsades de ties, [D] form does
pointes VT not. Both forms
have class III
activity. Only
racemic sotalol is
available for clini-
cal use.
Drug should not be
used in patients
with renal insuffi-
ciency.

CLASS IV Uses: Termination of SVT and slowing of rapid AF or atrial flutter

Ca channel
blockers
Diltiazem Oral slow-release 0.1–0.4 Possible precipitation IV form is most
(diltiazem CD): µg/mL of VF in patients commonly used to
120 mg to 360 with VT, negative slow ventricular
mg once/day inotropy response rate to
IV: 5–15 mg/h AF or atrial flutter.
for up to 24 h
Verapamil Oral: 40–120 mg N/A Possible precipitation IV form is used to
tid or, for sus- of VF in patients terminate narrow-
tained-release with VT, negative complex tachycar-
form, 180 mg inotropy dias involving the
once/day to 240 AV node (success
mg bid rate, almost 100%
IV: 5–15 mg over with 5–10 mg IV
10 min over 10 min).
Oral prophylaxis:
40–120 mg tid
 THE SECTION Cardiovascular Disorders
Arrhythmias and Conduction
MERCK MANUALS FOR HEALTHCARE
SUBJECT
TOPIC
Disorders
Introduction
ONLINE MEDICAL LIBRARY P R O F E S S I O N A L S

ANTIARRHYTHMIC DRUGS (VAUGHAN-WILLIAMS

CLASSIFICATION)—Continued
Target
Drug Dosage Levels Adverse Effects Comments

OTHER ANTIARRHYTHMICS
Adenosine 6 mg rapid IV N/A Transient dyspnea, Drug slows or
bolus, repeated chest discomfort, blocks AV nodal
twice at 12 mg and flushing (in conduction.
if needed; flush 30–60%), transient Duration of action is
bolus with addi- bronchospasm extremely short.
tional 20 mL
saline Contraindications
include asthma
and high-grade
heart block.
Dipyridamole poten-
tiates effects.

Digoxin IV loading dose: 0.8–1.6 Anorexia, nausea, Contraindications

0.5 mg µg/mL vomiting, and often include antegrade
Oral maintenance serious arrhythmias conduction over
dose: (VPBs, VT, APBs, an accessory AV
0.125–0.25 atrial tachycardia, connection path-
mg/day 2nd-degree or 3rd- way (manifest
degree AV block, Wolff-Parkinson-
combinations of White syndrome)
these arrhythmias) because if AF
occurs, ventricular
responses may be
excessive (digoxin
shortens refractory
periods of the
accessory connec-
tion).

*Availability uncertain.
AF = atrial fibrillation; ANA = antinuclear antibody; APB = atrial premature beat; AV = atri-
oventricular; CrCl = creatinine clearance; LV = left ventricular; QTc = QT interval corrected for
heart rate; SVT = supraventricular tachycardia; VF = ventricular fibrillation; VPB = ventricular
premature beat; VT = ventricular tachycardia.