bretylium (Rx)

Brand and Other Names:
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

solution for injection

  • 500mg/10mL (50mg/mL single-dose vial)

Ventricular Arrhythmia

Indicated for prophylaxis and treatment of ventricular fibrillation (VF); also indicated for treatment of life-threatening ventricular arrhythmias (eg, ventricular tachycardia [VT] unresponsive to first-line antiarrhythmic agents [eg, lidocaine])

Immediately life-threatening ventricular arrhythmias (eg, VF, unstable VT)

  • Other usual cardiopulmonary resuscitative procedures, including electrical cardioversion, should be used prior to and following the injection in accordance with good medical practice
  • Undiluted solution: 5 mg/kg IV by rapid injection; if arrhythmia persists, may increase dose to 10 mg/kg and repeat prn
  • Diluted solution for continuous suppression: 1-2 mg/min IV; alternatively, 5-10 mg/kg IV over at least 8 min q6hr

Other ventricular arrhythmias

  • IV
    • Use diluted solution
    • 5-10 mg/kg IV over at least 8 min; may repeat dose at 1- to 2-hr intervals if arrhythmia persists
    • Maintenance: 5-10 mg/kg IV over at least 8 min q6hr; alternatively, 1-2 mg/min IV continuous infusion
  • IM
    • Use undiluted solution
    • 5-10 mg/kg IM; may repeat dose at 1- to 2-hr intervals if arrhythmia persists
    • Maintenance: 5-10 mg/kg IM q6-8hr
    • Switch of oral antiarrhythmic agent as soon as possible for continued maintenance therapy

Dosage Modifications

Renal impairment

  • Primarily excreted via kidneys; increase dosage interval in patients with impaired renal function
  • Removed by hemodialysis

Dosing Considerations

Limit use to intensive care units, coronary care units, or other facilities where equipment and personnel for constant monitoring of cardiac arrhythmias and blood pressure are available

Following administration, onset of antiarrhythmic action may occur between 20 minutes and 2 hr; although, it appears to act within minutes in VF; delay in effect appears to be longer after IM than after IV injection

Dosage Modifications

Renal impairment

  • Primarily excreted via kidneys; increase dosage interval in patients with impaired renal function
  • Removed by hemodialysis

Dosing Considerations

Drug is substantially excreted by the kidneys, carefully select dose for geriatric patients; consider monitoring renal function

Limit use to intensive care units, coronary care units, or other facilities where equipment and personnel for constant monitoring of cardiac arrhythmias and blood pressure are available

Following administration, onset of antiarrhythmic action may occur between 20 minutes to 2 hr; although, it appears to act within minutes in ventricular fibrillation; delay in effect appears to be longer after IM than after IV injection

Safety and efficacy not established

Ventricular Arrhythmia

Indicated for prophylaxis and treatment of ventricular fibrillation (VF); also indicated for treatment of life-threatening ventricular arrhythmias (eg, ventricular tachycardia [VT] unresponsive to first-line antiarrhythmic agents [eg, lidocaine])

In general, dose selection for geriatric patients should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or drug therapy

Risk of orthostatic hypotension exists, particularly if administered IV at rate exceeding recommendations

Immediately life-threatening ventricular arrhythmias (eg, VF, unstable VT)

  • Other usual cardiopulmonary resuscitative procedures, including electrical cardioversion, should be used prior to and following the injection in accordance with good medical practice
  • Undiluted solution: 5 mg/kg IV by rapid injection; if arrhythmia persists, may increase dose to 10 mg/kg and repeat prn
  • Diluted solution for continuous suppression: 1-2 mg/min IV; alternatively, 5-10 mg/kg IV over at least 8 min q6hr

Other ventricular arrhythmias (IV)

  • Use diluted solution
  • 5-10 mg/kg IV over at least 8 min; may repeat dose at 1- to 2-hr intervals if arrhythmia persists
  • Maintenance: 5-10 mg/kg IV over at least 8 min q6hr; alternatively, 1-2 mg/min IV continuous infusion

Other ventricular arrhythmias (IM)

  • Use undiluted solution
  • 5-10 mg/kg IM; may repeat dose at 1- to 2-hr intervals if arrhythmia persists
  • Maintenance: 5-10 mg/kg IM q6-8hr
  • Switch of oral antiarrhythmic agent as soon as possible for continued maintenance therapy

Dosing Considerations

Drug is substantially excreted by the kidneys; carefully select dose for geriatric patients; consider monitoring renal function

Limit use to intensive care units, coronary care units, or other facilities where equipment and personnel for constant monitoring of cardiac arrhythmias and blood pressure are available

Following administration, onset of antiarrhythmic action may occur between 20 minutes and 2 hr; although, it appears to act within minutes in VF; delay in effect appears to be longer after IM than after IV injection

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Interactions

Interaction Checker

and bretylium

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              • digoxin

                bretylium increases toxicity of digoxin by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Avoid or Use Alternate Drug. Avoid simultaneous initiation of therapy with digitalis glycosides and bretylium. Initial release of norepinephrine caused by bretylium may aggravate digitalis toxicity. When a life-threatening cardiac arrhythmia occurs in a digitalized patient, bretylium should be used only if the etiology of the arrhythmia does not appear to be digitalis toxicity and other antiarrhythmic drugs are not effective. Bretylium is contraindicated for digitalis-induced arrhythmias.

              Monitor Closely (91)

              • alprostadil IV

                alprostadil IV, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • amiloride

                amiloride, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • amlodipine

                amlodipine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • amyl nitrite

                amyl nitrite, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • atenolol

                atenolol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • azilsartan

                azilsartan, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • benazepril

                benazepril, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • bendroflumethiazide

                bendroflumethiazide, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • betaxolol

                betaxolol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • bisoprolol

                bisoprolol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • bumetanide

                bumetanide, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • candesartan

                candesartan, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • captopril

                captopril, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • carvedilol

                carvedilol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • celiprolol

                celiprolol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • chlorothiazide

                chlorothiazide, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • chlorthalidone

                chlorthalidone, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • clevidipine

                clevidipine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • clonidine

                clonidine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • diltiazem

                diltiazem, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • dopamine

                bretylium increases effects of dopamine by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. If catecholamines are administered to treat systolic BP <75 mmHg, a dilute solution should be employed and blood pressure monitored closely. Bretylium causes an initial norepinephrine release and may enhance catecholamine pressor effects.

              • enalapril

                enalapril, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • ephedrine

                bretylium increases effects of ephedrine by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. If catecholamines are administered to treat systolic BP <75 mmHg, a dilute solution should be employed and blood pressure monitored closely. Bretylium causes an initial norepinephrine release and may enhance catecholamine pressor effects.

              • epinephrine

                bretylium increases effects of epinephrine by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. If catecholamines are administered to treat systolic BP <75 mmHg, a dilute solution should be employed and blood pressure monitored closely. Bretylium causes an initial norepinephrine release and may enhance catecholamine pressor effects.

              • eprosartan

                eprosartan, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • esmolol

                esmolol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • ethacrynic acid

                ethacrynic acid, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • felodipine

                felodipine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • fenoldopam

                fenoldopam, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • fosinopril

                fosinopril, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • furosemide

                furosemide, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • hydralazine

                hydralazine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • hydrochlorothiazide

                hydrochlorothiazide, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • irbesartan

                irbesartan, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • isocarboxazid

                isocarboxazid increases effects of bretylium by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. Bretylium produces release of catecholamines from nerve endings. This increased catecholamine release is potentiated by MAOIs.

              • isosorbide dinitrate

                isosorbide dinitrate, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • isosorbide mononitrate

                isosorbide mononitrate, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • isradipine

                isradipine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • labetalol

                labetalol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • lisinopril

                lisinopril, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • losartan

                losartan, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • methyclothiazide

                methyclothiazide, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • methyldopa

                methyldopa, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • metoprolol

                metoprolol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • minoxidil

                minoxidil, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • moexipril

                moexipril, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nadolol

                nadolol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nebivolol

                nebivolol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nesiritide

                nesiritide, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nicardipine

                nicardipine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nifedipine

                nifedipine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nimodipine

                nimodipine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nisoldipine

                nisoldipine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nitroglycerin IV

                nitroglycerin IV, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nitroglycerin PO

                nitroglycerin PO, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nitroglycerin sublingual

                nitroglycerin sublingual, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nitroglycerin topical

                nitroglycerin topical, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nitroglycerin transdermal

                nitroglycerin transdermal, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nitroglycerin translingual

                nitroglycerin translingual, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • nitroprusside sodium

                nitroprusside sodium, bretylium. Either decreases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • norepinephrine

                bretylium increases effects of norepinephrine by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. If catecholamines are administered to treat systolic BP <75 mmHg, a dilute solution should be employed and blood pressure monitored closely. Bretylium causes an initial norepinephrine release and may enhance catecholamine pressor effects.

              • nylidrin

                nylidrin, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • olmesartan

                olmesartan, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • papaverine

                papaverine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • penbutolol

                penbutolol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • perindopril

                perindopril, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • phenelzine

                phenelzine increases effects of bretylium by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. Bretylium produces release of catecholamines from nerve endings. This increased catecholamine release is potentiated by MAOIs.

              • phenoxybenzamine

                phenoxybenzamine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • phentolamine

                phentolamine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • ponesimod

                ponesimod, bretylium. Either increases effects of the other by QTc interval. Use Caution/Monitor. Consult cardiologist if considering treatment. Class III (eg, amiodarone, dofetilide, sotalol) anti-arrhythmic drugs have been associated with cases of torsades de pointes in patients with bradycardia.

              • prazosin

                prazosin, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • procarbazine

                procarbazine increases effects of bretylium by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. Bretylium produces release of catecholamines from nerve endings. This increased catecholamine release is potentiated by MAOIs.

              • propranolol

                propranolol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • quinapril

                quinapril, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • ramipril

                ramipril, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • rasagiline

                rasagiline increases effects of bretylium by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. Bretylium produces release of catecholamines from nerve endings. This increased catecholamine release is potentiated by MAOIs.

              • sacubitril/valsartan

                sacubitril/valsartan, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • safinamide

                safinamide increases effects of bretylium by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. Bretylium produces release of catecholamines from nerve endings. This increased catecholamine release is potentiated by MAOIs.

              • selegiline

                selegiline increases effects of bretylium by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. Bretylium produces release of catecholamines from nerve endings. This increased catecholamine release is potentiated by MAOIs.

              • selegiline transdermal

                selegiline transdermal increases effects of bretylium by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. Bretylium produces release of catecholamines from nerve endings. This increased catecholamine release is potentiated by MAOIs.

              • sotalol

                sotalol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • spironolactone

                spironolactone, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • telmisartan

                telmisartan, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • terazosin

                terazosin, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • timolol

                timolol, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • torsemide

                torsemide, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • trandolapril

                trandolapril, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • tranylcypromine

                tranylcypromine increases effects of bretylium by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Modify Therapy/Monitor Closely. Bretylium produces release of catecholamines from nerve endings. This increased catecholamine release is potentiated by MAOIs.

              • triamterene

                triamterene, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • valsartan

                valsartan, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              • verapamil

                verapamil, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.

              Minor (0)

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                Adverse Effects

                >10%

                Hypotension, some degree even while supine (50%)

                <1%

                ~0.7%

                • Vertigo
                • Dizziness
                • Lightheadedness
                • Syncope

                ~0.2%

                • Increased frequency of premature ventricular contractions
                • Transitory hypertension
                • Initial increase in arrhythmias
                • Precipitation of anginal attacks
                • Sensation of substernal pressure

                ~0.1%

                • Renal dysfunction
                • Diarrhea, abdominal pain
                • Hiccups
                • Erythematous macular rash
                • Flushing
                • Hyperthermia
                • Confusion, paranoid psychosis, emotional lability, anxiety
                • Lethargy
                • Generalized tenderness
                • Shortness of breath, diaphoresis, nasal stuffiness
                • Mild conjunctivitis
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                Warnings

                Contraindications

                Digitalis-induced arrhythmias

                Cautions

                Hypotension

                • Administration regularly results in postural hypotension, subjectively recognized by dizziness, lightheadedness, vertigo, or faintness
                • Some degree of hypotension is present in ~50% of patients while they are supine
                • Hypotension may occur at doses lower than those needed to suppress arrhythmias
                • Keep patients in supine position until tolerance to hypotensive effect develops; tolerance occurs unpredictably, but may be present after several days
                • Patients aged >65 years may be at increased risk of developing orthostatic hypotension, especially if recommended IV infusion exceeded
                • Hypotension with supine systolic pressure >75 mm Hg need not be treated unless there are associated symptoms
                • If supine systolic pressure falls below 75 mm Hg, dopamine or norepinephrine infusion may be used to raise blood pressure
                • When catecholamines are administered, use a dilute solution and closely monitor blood pressure (pressor effects catecholamines enhanced by bretylium)
                • Volume expansion with blood or plasma and correction of dehydration should be carried out where appropriate

                Transient hypertension

                • Bretylium causes an initial norepinephrine release from adrenergic postganglionic nerve terminals
                • Transient hypertension or increased frequency of premature ventricular contractions and other arrhythmias may occur in some patients, especially after too vigorous a dosing

                Fixed cardiac output

                • Avoid use in patients with fixed cardiac output (eg, severe aortic stenosis or pulmonary hypertension) since severe hypotension may result from a fall in peripheral resistance without a compensatory increased cardiac output
                • If survival is threatened by the arrhythmia, bretylium may be used, but vasoconstrictive catecholamines should be given promptly if severe hypotension occurs

                Hyperthermia

                • Hyperthermia, characterized by temperature excess of 106°F, reported; temperature rise can begin within 1 hr or later after administration and peak within 1-3 days
                • If suspected or diagnosed, discontinue bretylium and institute treatment immediately

                Drug interaction overview

                • Digoxin
                  • Initial release of norepinephrine caused by bretylium may aggravate digitalis toxicity
                  • When a life-threatening cardiac arrhythmia occurs in a digitalized patient, bretylium should be used only if the etiology of the arrhythmia does not appear to be digitalis toxicity and other antiarrhythmic drugs are not effective
                  • Avoid simultaneous initiation of therapy with digitalis glycosides and bretylium
                • Monoamine oxidase inhibitors (MAOIs)
                  • Bretylium produces release of catecholamines from nerve endings
                  • This increased catecholamine release is potentiated by MAOIs
                • Catecholamines
                  • If catecholamines (ie, dopamine, norepinephrine) are administered to treat systolic blood pressure <75 mm Hg, a dilute solution should be used and blood pressure monitored closely because the pressor effects of the catecholamines are enhanced by bretylium
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                Pregnancy & Lactation

                Pregnancy

                Unknown whether bretylium can cause fetal harm when administered to pregnant women or can affect reproduction capacity

                Administer during pregnancy only if clearly needed

                Animal reproduction studies have not been conducted

                Lactation

                Data are not available

                Pregnancy Categories

                A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                NA: Information not available.

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                Pharmacology

                Mechanism of Action

                Accumulates in sympathetic ganglia and their postganglionic adrenergic neurons when administered slowly or incrementally, where it inhibits norepinephrine release by depressing adrenergic nerve terminal excitability

                Also suppresses ventricular fibrillation (VF) and ventricular arrhythmias; mechanisms of antifibrillatory and antiarrhythmic actions are not established, although electrophysiologic actions have been described in animal studies

                Electrophysiologic effects observed in animal studies

                • Increased VF threshold
                • Increased action potential duration and effective refractory period without changes in heart rate
                • Little effect on the rate of rise or amplitude of the cardiac action potential (Phase 0) or in resting membrane potential (Phase 4) in normal myocardium; however, when cell injury slows the rate of rise, decreases amplitude, and lowers resting membrane potential, bretylium transiently restores these parameters toward normal
                • In canine hearts with infarcted areas, bretylium decreases disparity in action potential duration between normal and infarcted regions
                • Increased impulse formation and spontaneous firing rate of pacemaker tissue, as well as increased ventricular conduction velocity

                Absorption

                Onset of action: 20 minutes to 2 hr

                Elimination

                Half-life: 6-10 hr (normal renal function)

                Excretion: Urine (80% within 24 hr; additional 10% within 96 hr)

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                Administration

                IV Compatibility

                D5W

                0.9% NaCl

                IV Preparation

                Solution should appear clear; slight discoloration does not alter potency

                Rapid IV bolus: Do NOT dilute solution

                Continuous or intermittent IV infusion: Dilute 500 mg to a minimum of 50 mL with D52 or 0.9% NaCl

                IM Preparation

                Solution should appear clear; slight discoloration does not alter potency

                Do NOT dilute solution

                IV Administration

                Patients should remain in supine position until tolerance to the hypotensive effect of bretylium develops; tolerance occurs unpredictably but may be present after several days

                Immediately life-threatening ventricular arrhythmias

                • Rapid IV bolus (undiluted drug): When used for immediately life-threatening ventricular arrhythmias (eg, VF, hemodynamically unstable VT), give rapid IV bolus and if continuous suppression needed, follow with continuous or intermittent IV infusion (dilute drug as described above)
                • Continuous IV solution infusion: 1-2 mg/min
                • Intermittent IV infusion: 5-10 mg/kg infused over at least 8 min q6hr
                • Rapid infusion
                  • More rapid infusion may cause nausea and vomiting, and possibly provoke hypertensive crisis
                  • May increase orthostatic hypotension risk, especially in patients aged ≥65 yr

                IM Administration

                Patients should be kept in supine position until tolerance to the hypotensive effect of bretylium develops; tolerance occurs unpredictably but may be present after several days

                Do not dilute for IM injection

                Do not inject directly into or near a major nerve

                Rotate injection site if repeated

                Do not exceed 5 mL/injection site

                As soon as possible, and when indicated, change to oral antiarrhythmic agent for maintenance therapy

                Storage

                Store at 20-25°C (68-77°F)

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                Images

                BRAND FORM. UNIT PRICE PILL IMAGE
                bretylium tosylate injection
                -
                50 mg/mL vial

                Copyright © 2010 First DataBank, Inc.

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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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                Formulary

                FormularyPatient Discounts

                Adding plans allows you to compare formulary status to other drugs in the same class.

                To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

                Adding plans allows you to:

                • View the formulary and any restrictions for each plan.
                • Manage and view all your plans together – even plans in different states.
                • Compare formulary status to other drugs in the same class.
                • Access your plan list on any device – mobile or desktop.

                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
                Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.