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Pronunciation |
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(bre
TIL ee
um) |
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U.S. Brand
Names |
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Bretylol® |
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Generic
Available |
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No |
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Canadian Brand
Names |
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Bretylate® |
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Synonyms |
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Bretylium Tosylate |
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Pharmacological Index |
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Antiarrhythmic Agent, Class III |
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Use |
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Treatment of ventricular tachycardia and fibrillation; treatment of other
serious ventricular arrhythmias resistant to lidocaine |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Hypersensitivity to bretylium or any component; severe aortic stenosis;
severe pulmonary hypertension |
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Warnings/Precautions |
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Use only in areas where there is equipment and staff familiar with management
of life-threatening arrhythmias. Use continuous cardiac and blood pressure
monitoring. Keep patients supine (postural hypotension common). Initially, may
see transient hypertension and increased frequency of arrhythmias. Adjust dose
in patients with impaired renal function. Give to a pregnant woman only if
clearly needed. Rapid I.V. administration may cause nausea and
vomiting. |
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Adverse
Reactions |
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>10%: Cardiovascular: Hypotension (both postural and supine)
1% to 10%: Gastrointestinal: Nausea, vomiting
<1% (Limited to important or life-threatening symptoms): Transient initial
hypertension, increase in premature ventricular contractions (PVCs),
bradycardia, chest pain, flushing, syncope, postural hypotension, renal
impairment, respiratory depression, nasal congestion, shortness of breath
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Overdosage/Toxicology |
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Symptoms of overdose include significant hypertension followed by severe
hypotension due to inhibition of catecholamine release
After GI decontamination, supportive treatment is required. Note: Quinidine
and other type Ia should not be used to treat cardiotoxicity caused by
bretylium; continuously monitor vital signs and EKG for a minimum of 6 hours
after exposure and admit the patient for 24 hours of intensive monitoring if
there is evidence of toxicity. Dialysis and hemoperfusion unlikely to assist.
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Drug
Interactions |
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Increased toxicity when used with pressor catecholamines, and digitalis.
Agents which may prolong QT interval (including cisapride, tricyclic
antidepressants, antipsychotics, erythromycin, Class Ia and Class III
antiarrhythmics): Toxicity may be increased.
Quinolones: Risk of cardiotoxicity is increased with concurrent use of
sparfloxacin, moxifloxacin, or gatifloxacin may increase toxicity due to the
potential to prolong QT interval.
Sympathomimetic amines with initial use of bretylium may cause hypertension.
Digoxin toxicity may be aggravated by bretylium. |
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Stability |
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Standard diluent: 2 g/250 mL D5W; the premix infusion should be
stored at room temperature and protected from freezing |
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Mechanism of
Action |
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Class II antiarrhythmic; after an initial release of norepinephrine at the
peripheral adrenergic nerve terminals, inhibits further release by
postganglionic nerve endings in response to sympathetic nerve
stimulation |
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Pharmacodynamics/Kinetics |
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Onset of antiarrhythmic effect: I.M.: May require 2 hours; I.V.: Within 6-20
minutes
Peak effect: 6-9 hours
Duration: 6-24 hours
Protein binding: 1% to 6%
Metabolism: Not metabolized
Half-life: 7-11 hours; average: 4-17 hours
End-stage renal disease: 16-32 hours
Elimination: 70% to 80% excreted over the first 24 hours; excreted unchanged
in the urine |
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Usual Dosage |
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Note: Patients should undergo defibrillation/cardioversion before and
after bretylium doses as necessary.
I.M.: 2-5 mg/kg as a single dose
I.V.: Acute ventricular fibrillation: Initial: 5 mg/kg, then attempt
electrical defibrillation; repeat with 10 mg/kg if ventricular fibrillation
persists at 15- to 30-minute intervals to maximum total of 30 mg/kg.
Maintenance dose: I.M., I.V.: 5 mg/kg every 6 hours
Adults:
Immediate life-threatening ventricular arrhythmias (ventricular fibrillation,
unstable ventricular tachycardia): Initial dose: I.V.: 5 mg/kg (undiluted) over
1 minute; if arrhythmia persists, administer 10 mg/kg (undiluted) over 1 minute
and repeat as necessary (usually at 15- to 30-minute intervals) up to a total
dose of 30-35 mg/kg.
Other life-threatening ventricular arrhythmias:
Initial dose: I.M., I.V.: 5-10 mg/kg, may repeat every 1-2 hours if
arrhythmia persists; administer I.V. dose (diluted) over 8-10 minutes.
Maintenance dose: I.M.: 5-10 mg/kg every 6-8 hours; I.V. (diluted): 5-10
mg/kg every 6 hours; I.V. infusion (diluted): 1-2 mg/minute (little experience
with doses >40 mg/kg/day)
Example dilution: 2 g/250 mL D5W (infusion pump should be used for
I.V. infusion administration)
Rate of I.V. infusion: 1-4 mg/minute
1 mg/minute = 7 mL/hour
2 mg/minute = 15 mL/hour
3 mg/minute = 22 mL/hour
4 mg/minute = 30 mL/hour
Dosing adjustment in renal impairment:
Clcr 10-50 mL/minute: Administer 25% to 50% of dose.
Clcr <10 mL/minute: Administer 25% of dose.
Dialysis: Not dialyzable (0% to 5%) via hemo- or peritoneal dialysis;
supplemental doses are not needed. |
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Monitoring
Parameters |
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EKG, heart rate, blood pressure; requires a cardiac
monitor |
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Mental Health: Effects
on Mental Status |
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May cause confusion |
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Mental Health:
Effects on Psychiatric
Treatment |
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Hypotension is common; use caution with concurrent
psychotropics |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Emergency use: Patient education is determined by patient condition. You may
experience nausea or vomiting (call for assistance if this occurs, do not try to
get out of bed or change position on your own). Report chest pain, acute
dizziness, or difficulty breathing immediately. Breast-feeding
precautions: Consult prescriber if breast-feeding. |
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Nursing
Implications |
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Monitor EKG and blood pressure throughout therapy; onset of action may be
delayed 15-30 minutes; rapid infusion may result in nausea and
vomiting |
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Dosage Forms |
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Injection, as tosylate: 50 mg/mL (10 mL, 20 mL)
Injection, as tosylate, premixed in D5W: 1 mg/mL (500 mL); 2 mg/mL
(250 mL); 4 mg/mL (250 mL, 500 mL) |
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References |
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Bodnar T, Nowak R, Tomlanovich MC, et al,
"Massive Intravenous Bolus Bretylium Tosylate," Ann Emerg Med, 1980,
9(12):630-3.
Emergency Cardiac Care Committee and Subcommittees, American Heart
Association,
"Guidelines for Cardiopulmonary Resuscitation and Emergency Cardiac Care, III: Adult Advanced Cardiac Life Support"
and "VI: Pediatric Advanced Life Support," JAMA, 1992, 268(16):2199-241
and 2262-75.
Gibson JS and Munter DW, "Intravenous Bretylium Overdose," Am J Emerg
Med, 1995, 13(2):177-9.
Perlman PE, Adams WG Jr, and Ridgeway NA,
"Extreme Pyrexia During Bretylium Administration," Postgrad Med, 1989,
85(1):111-2.
Thompson AE and Sussmane JB,
"Bretylium Intoxication Resembling Clinical Brain Death," Crit Care Med,
1989, 17(2):14-9. |
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