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Isoproterenol: Drug information

Isoproterenol: Drug information
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For additional information see "Isoproterenol: Patient drug information" and "Isoproterenol: Pediatric drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: US
  • Isuprel [DSC]
Pharmacologic Category
  • Beta1/Beta2 Agonist
Dosing: Adult

Note: May cause dose-dependent hypotension due to beta-2 agonist effects.

Atrioventricular block, symptomatic and/or hemodynamically unstable

Atrioventricular block, symptomatic and/or hemodynamically unstable:

Note: Should only be used as a temporizing measure until a permanent pacemaker can be placed, if clinically indicated. In most cases, pharmacologic agents will not be effective and temporary transcutaneous or transvenous pacing is necessary as a bridge to permanent pacemaker placement (Ref).

Continuous infusion: IV: Usual dosage range: 1 to 20 mcg/minute; initiate at the low end of the dosage range and titrate to clinical response (Ref).

Bradycardia, symptomatic and/or hemodynamically unstable

Bradycardia, symptomatic and/or hemodynamically unstable (unresponsive to atropine) (off-label use): Continuous infusion: IV: Usual dosage range: 1 to 20 mcg/minute; initiate at the low end of the dosage range and titrate to clinical response (Ref).

Cardiogenic shock due to bradycardia

Cardiogenic shock due to bradycardia (off-label use): Continuous infusion: IV: 2 to 20 mcg/minute (Ref).

Provocation during tilt table testing, diagnostic agent for syncope

Provocation during tilt table testing, diagnostic agent for syncope (off-label use): Note: Timing of initiation and dose adjustment during test may be institution specific; refer to institutional protocols.

Continuous infusion: IV: Initial: 1 mcg/minute; increase as necessary based on clinical response up to 3 mcg/minute (Ref).

Torsade de pointes, to reduce recurrence

Torsade de pointes, to reduce recurrence (off-label use):

Note: For use only in patients who have a bradycardia-mediated cause of torsades de pointes. Avoid use in congenital long QT syndrome. Patient should be under the care of a clinician experienced with using isoproterenol for this condition (Ref).

Continuous infusion: IV: Usual dosage range: 2 to 10 mcg/minute; titrate to clinical response (Ref).

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Liver Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric

(For additional information see "Isoproterenol: Pediatric drug information")

Note: Patients may exhibit dose-dependent vasodilation due to unopposed beta2-agonism elicited by isoproterenol.

Bradycardia, severe; atrioventricular nodal block

Bradycardia, severe; atrioventricular nodal block: Limited data available: Infants, Children, and Adolescents: Continuous IV infusion: 0.05 to 0.5 mcg/kg/minute; titrate to effect; doses as high as 2 mcg/kg/minute may be needed in some patients (Ref); usual adult range: 2 to 10 mcg/minute (Ref)

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Liver Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer’s labeling.

Adverse Reactions

The following adverse drug reactions are derived from product labeling unless otherwise specified.

Postmarketing:

Cardiovascular: Adams-Stokes syndrome, angina pectoris, atrioventricular block (Barold 2015), bradycardia (Duong 2020), chest pain (Duong 2020), coronary artery vasospasm (Duong 2020), flushing, hypertension, hypotension (Suwa 2004), increased ST segment on ECG (Okuya 2021), palpitations, tachyarrhythmia, tachycardia, ventricular arrhythmia (including non-sustained ventricular fibrillation) (Okuya 2021), ventricular premature contractions (Okuya 2021)

Dermatologic: Diaphoresis, pallor

Gastrointestinal: Nausea

Nervous system: Dizziness, headache, nervousness, tremor

Ophthalmic: Blurred vision (Duong 2020)

Respiratory: Dyspnea, pulmonary edema

Contraindications

Angina, preexisting ventricular arrhythmias, tachycardia or tachyarrhythmias; cardiac glycoside intoxication induced heart block or tachycardia.

Warnings/Precautions

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with cardiovascular disease (eg, coronary artery disease); may increase myocardial oxygen demand resulting in ischemia.

• Diabetes: Use with caution in patients with diabetes mellitus; may transiently increase blood glucose levels.

• Distributive shock: Avoid use in patients with distributive shock; may reduce systemic vascular resistance (SVR) further resulting in hemodynamic compromise.

Special populations:

• Older patients: Use with caution in older patients.

Dosage form specific issues:

• Sulfites: Contains sulfites; may cause allergic reaction in susceptible individuals.

Other warnings/precautions:

• Appropriate use: Use with extreme caution; not currently a treatment of choice. Excessive or prolonged use may result in decreased effectiveness.

Warnings: Additional Pediatric Considerations

Isoproterenol is not recommended for treatment of bronchospasm. In children with refractory asthma, continuous isoproterenol infusion was associated with myocardial necrosis, congestive heart failure, further clinical deterioration, and death in some cases. The risk of cardiac toxicity was observed to be increased by concomitant corticosteroids or methylxanthines, acidosis, or hypoxemia; monitor patients closely (vital signs, ECG, cardiac enzymes) with therapy.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Injection, as hydrochloride:

Isuprel: 0.2 mg/mL (1 mL [DSC], 5 mL [DSC]) [contains disodium edta]

Generic: 0.2 mg/mL (1 mL, 5 mL)

Solution, Injection, as hydrochloride [preservative free]:

Generic: 0.2 mg/mL (1 mL, 5 mL)

Generic Equivalent Available: US

Yes

Pricing: US

Solution (Isoproterenol HCl Injection)

0.2 mg/mL (per mL): $16.80 - $130.80

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Injection, as hydrochloride:

Generic: 0.2 mg/mL (1 mL, 5 mL)

Administration: Adult

IV: IV infusion administration requires the use of an infusion pump.

Administration: Pediatric

Parenteral: Administer by continuous IV infusion; requires the use of an infusion pump

Usual Infusion Concentrations: Adult

IV infusion: 1 mg in 500 mL (2 mcg/mL), 2 mg in 500 mL (4 mcg/mL), 1 mg in 100 mL (10 mcg/mL), or 4 mg in 250 mL (16 mcg/mL) of D5W or NS.

Usual Infusion Concentrations: Pediatric

IV infusion: 20 mcg/mL

Use: Labeled Indications

Mild or transient episodes of heart block that do not require electric shock or pacemaker therapy; serious episodes of heart block and Adams-Stokes attacks (except when caused by ventricular tachycardia or fibrillation); adjunct to fluid and electrolyte replacement therapy and other drugs and procedures in the treatment of low cardiac output states (eg, decompensated heart failure, cardiogenic shock).

Use: Off-Label: Adult

Bradycardia, symptomatic and/or hemodynamically unstable (unresponsive to atropine); Cardiogenic shock due to bradycardia; Provocation during tilt table testing, diagnostic agent for syncope; Torsades de pointes, to reduce recurrence

Medication Safety Issues
Sound-alike/look-alike issues:

Isuprel may be confused with Disophrol, Isordil

High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes (antiarrhythmic agent, IV) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Acute Care Settings).

Metabolism/Transport Effects

Substrate of COMT;

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Atomoxetine: May increase hypertensive effects of Sympathomimetics. Atomoxetine may increase tachycardic effects of Sympathomimetics. Risk C: Monitor

Beta-Blockers: May decrease therapeutic effects of Isoproterenol. Risk C: Monitor

Bornaprine: Sympathomimetics may increase anticholinergic effects of Bornaprine. Risk C: Monitor

Cannabinoid-Containing Products: May increase tachycardic effects of Sympathomimetics. Risk C: Monitor

Chlorpheniramine: May increase therapeutic effects of Isoproterenol. Risk C: Monitor

Cocaine (Topical): May increase hypertensive effects of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Risk D: Consider Therapy Modification

COMT Inhibitors: May increase serum concentration of COMT Substrates. Risk C: Monitor

Dihydralazine: Sympathomimetics may decrease therapeutic effects of Dihydralazine. Risk C: Monitor

DiphenhydrAMINE (Systemic): May increase therapeutic effects of Isoproterenol. Risk C: Monitor

Doxofylline: Sympathomimetics may increase adverse/toxic effects of Doxofylline. Risk C: Monitor

EPINEPHrine (Systemic): Isoproterenol may increase therapeutic effects of EPINEPHrine (Systemic). Risk X: Avoid

Esketamine (Injection): May increase adverse/toxic effects of Sympathomimetics. Specifically, the risk for elevated heart rate, hypertension, and arrhythmias may be increased. Risk C: Monitor

Guanethidine: May increase hypertensive effects of Sympathomimetics. Guanethidine may increase arrhythmogenic effects of Sympathomimetics. Risk C: Monitor

Hexoprenaline: May increase adverse/toxic effects of Isoproterenol. Risk X: Avoid

Inhalational Anesthetics: May increase arrhythmogenic effects of Isoproterenol. Risk X: Avoid

Kratom: May increase adverse/toxic effects of Sympathomimetics. Risk X: Avoid

Levothyroxine: May increase therapeutic effects of Isoproterenol. Risk C: Monitor

Linezolid: May increase hypertensive effects of Sympathomimetics. Management: Consider initial dose reductions of sympathomimetic agents, and closely monitor for enhanced blood pressure elevations, in patients receiving linezolid. Risk D: Consider Therapy Modification

Monoamine Oxidase Inhibitors: May increase therapeutic effects of Isoproterenol. Risk C: Monitor

Solriamfetol: Sympathomimetics may increase hypertensive effects of Solriamfetol. Sympathomimetics may increase tachycardic effects of Solriamfetol. Risk C: Monitor

Sympathomimetics: May increase adverse/toxic effects of Sympathomimetics. Risk C: Monitor

Tedizolid: May increase adverse/toxic effects of Sympathomimetics. Specifically, the risk for increased blood pressure and heart rate may be increased. Risk C: Monitor

Theophylline Derivatives: Isoproterenol may decrease serum concentration of Theophylline Derivatives. Risk C: Monitor

Pregnancy Considerations

Animal reproduction studies have not been conducted by the manufacturer. Use of isoproterenol may interfere with uterine contractions at term (Mahon 1967).

Breastfeeding Considerations

It is not known if isoproterenol is present in breast milk. The manufacturer recommends that caution be exercised when administering isoproterenol to breastfeeding women.

Monitoring Parameters

Hemodynamic monitoring (eg, intracardiac pressures and cardiac output); continuous cardiac monitoring, heart rate, respiratory rate, BP, serum glucose, serum potassium, serum magnesium.

Mechanism of Action

Stimulates beta1- and beta2-receptors resulting in relaxation of bronchial, GI, and uterine smooth muscle, increased heart rate and contractility, vasodilation of peripheral vasculature

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: IV: Immediate

Duration: IV: 10-15 minutes

Metabolism: Via conjugation in many tissues including hepatic and pulmonary

Half-life elimination: 2.5-5 minutes

Excretion: Urine (primarily as sulfate conjugates)

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AR) Argentina: Isoproterenol phoroneus;
  • (AT) Austria: Isoprenalin macure | Isuprel;
  • (AU) Australia: Cipla isoprenaline | Isoprenaline macure;
  • (BE) Belgium: Isoprenaline hcl macure | Isuprel;
  • (DK) Denmark: Isoprenalin sad;
  • (FI) Finland: Isoprenaline macure;
  • (FR) France: Isoprenaline hydrochloride tillomed | Isuprel;
  • (GB) United Kingdom: Ims isoprenaline | Suscardia;
  • (GR) Greece: Isoprenalina;
  • (IE) Ireland: Isoprenaline;
  • (IT) Italy: Isoprenalina cloridrato galenica senese | Isoprenalina cloridrato salf;
  • (KW) Kuwait: Isuprel;
  • (LT) Lithuania: Aleudrina;
  • (LU) Luxembourg: Isuprel;
  • (NL) Netherlands: Isoprenaline hcl macure | Isoprenalinesulfaat;
  • (NO) Norway: Isoprenaline macure;
  • (PR) Puerto Rico: Isoproterenol HCL;
  • (PT) Portugal: Isoprenalina macure;
  • (QA) Qatar: Enaxil | Isuprel;
  • (RO) Romania: Isoprenalin macure;
  • (SE) Sweden: Isoprenaline macure;
  • (SI) Slovenia: Izoprenalin macure;
  • (TW) Taiwan: Isoproterenol | Proternol L
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