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Bretylium
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Monitoring Parameters
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(bre TIL ee um)

U.S. Brand Names
Bretylol®

Generic Available

No


Canadian Brand Names
Bretylate®

Synonyms
Bretylium Tosylate

Pharmacological Index

Antiarrhythmic Agent, Class III


Use

Treatment of ventricular tachycardia and fibrillation; treatment of other serious ventricular arrhythmias resistant to lidocaine


Pregnancy Risk Factor

C


Contraindications

Hypersensitivity to bretylium or any component; severe aortic stenosis; severe pulmonary hypertension


Warnings/Precautions

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.


Adverse Reactions

>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


Overdosage/Toxicology

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.


Drug Interactions

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.


Stability

Standard diluent: 2 g/250 mL D5W; the premix infusion should be stored at room temperature and protected from freezing


Mechanism of Action

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


Pharmacodynamics/Kinetics

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


Usual Dosage

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.


Monitoring Parameters

EKG, heart rate, blood pressure; requires a cardiac monitor


Mental Health: Effects on Mental Status

May cause confusion


Mental Health: Effects on Psychiatric Treatment

Hypotension is common; use caution with concurrent psychotropics


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

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.


Nursing Implications

Monitor EKG and blood pressure throughout therapy; onset of action may be delayed 15-30 minutes; rapid infusion may result in nausea and vomiting


Dosage Forms

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)


References

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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