Look Up > Drugs > Isoproterenol
Isoproterenol
Pronunciation
U.S. Brand Names
Generic Available
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
(eye soe proe TER e nole)

U.S. Brand Names
Arm-a-Med® Isoproterenol; Dey-Dose® Isoproterenol; Isuprel®; Medihaler-Iso®

Generic Available

Yes


Synonyms
Isoprenaline Hydrochloride; Isoproterenol Hydrochloride; Isoproterenol Sulfate

Pharmacological Index

Beta1/Beta2 Agonist


Use

Treatment of reversible airway obstruction as in asthma or COPD; used parenterally in ventricular arrhythmias due to A-V nodal block; hemodynamically compromised bradyarrhythmias or atropine-resistant bradyarrhythmias; temporary use in third degree A-V block until pacemaker insertion; low cardiac output; vasoconstrictive shock states


Pregnancy Risk Factor

C


Contraindications

Angina, pre-existing cardiac arrhythmias (ventricular); tachycardia or A-V block caused by cardiac glycoside intoxication; allergy to sulfites or isoproterenol or other sympathomimetic amines


Warnings/Precautions

Elderly patients, diabetics, renal or cardiovascular disease, hyperthyroidism; excessive or prolonged use may result in decreased effectiveness


Adverse Reactions

>10%:

Central nervous system: Insomnia, restlessness

Gastrointestinal: Dry throat, xerostomia, discoloration of saliva (pinkish-red)

1% to 10%:

Cardiovascular: Flushing of the face or skin, ventricular arrhythmias, tachycardias, profound hypotension, hypertension

Central nervous system: Nervousness, anxiety, dizziness, headache, lightheadedness

Gastrointestinal: Vomiting, nausea

Neuromuscular & skeletal: Trembling, tremor, weakness

Miscellaneous: Diaphoresis

<1%: Arrhythmias, chest pain, paradoxical bronchospasm


Overdosage/Toxicology

Symptoms of overdose include tremors, nausea, vomiting, hypotension; beta-adrenergic stimulation can cause increased heart rate, decreased blood pressure, and CNS excitation

Heart rate can be treated with beta-blockers, decreased blood pressure can be treated with pure alpha-adrenergic agents, diazepam 0.07 mg/kg can be used for excitation, seizures


Drug Interactions

Increased toxicity: Sympathomimetic agents may cause headaches and elevate blood pressure; general anesthetics may cause arrhythmias


Stability

Isoproterenol solution should be stored at room temperature; it should not be used if a color or precipitate is present

Exposure to air, light, or increased temperature may cause a pink to brownish pink color to develop

Stability of parenteral admixture at room temperature (25°C) or at refrigeration (4°C): 24 hours

Standard diluent: 2 mg/500 mL D5W; 4 mg/500 mL D5W

Minimum volume: 1 mg/100 mL D5W

Incompatible with alkaline solutions, aminophylline and furosemide


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


Pharmacodynamics/Kinetics

Onset of bronchodilation: Oral inhalation: Immediately

Time to peak serum concentration: Oral: Within 1-2 hours

Duration: Oral inhalation: 1 hour; S.C.: Up to 2 hours

Metabolism: By conjugation in many tissues including the liver and lungs

Half-life: 2.5-5 minutes

Elimination: In urine principally as sulfate conjugates


Usual Dosage

Children:

Bronchodilation: Inhalation: Metered dose inhaler: 1-2 metered doses up to 5 times/day

Bronchodilation (using 1:200 inhalation solution) 0.01 mL/kg/dose every 4 hours as needed (maximum: 0.05 mL/dose) diluted with NS to 2 mL

Sublingual: 5-10 mg every 3-4 hours, not to exceed 30 mg/day

Cardiac arrhythmias: I.V.: Start 0.1 mcg/kg/minute (usual effective dose 0.2-2 mcg/kg/minute)

Adults:

Bronchodilation: Inhalation: Metered dose inhaler: 1-2 metered doses 4-6 times/day

Bronchodilation: 1-2 inhalations of a 0.25% solution, no more than 2 inhalations at any one time (1-5 minutes between inhalations); no more than 6 inhalations in any hour during a 24-hour period; maintenance therapy: 1-2 inhalations 4-6 times/day. Alternatively: 0.5% solution via hand bulb nebulizer is 5-15 deep inhalations repeated once in 5-10 minutes if necessary; treatments may be repeated up to 5 times/day.

Sublingual: 10-20 mg every 3-4 hours; not to exceed 60 mg/day

Cardiac arrhythmias: I.V.: 5 mcg/minute initially, titrate to patient response (2-20 mcg/minute)

Shock: I.V.: 0.5-5 mcg/minute; adjust according to response


Monitoring Parameters

EKG, heart rate, respiratory rate, arterial blood gas, arterial blood pressure, CVP


Mental Health: Effects on Mental Status

Insomnia and restlessness are common


Mental Health: Effects on Psychiatric Treatment

None reported


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

Isoproterenol is selective for beta-adrenergic receptors and not alpha receptors; therefore, there is no precaution in the use of vasoconstrictor such as epinephrine


Dental Health: Effects on Dental Treatment

>10% of patients experience dry mouth


Patient Information

Sublingual: Do not chew or swallow tables, let them dissolve under the tongue.

Inhalant: Shake canister before use. Administer pressurized inhalation during the second half of inspiration. If more than one dose is necessary, wait at least 1 full minute between inhalations; second inhalation is best delivered after 5-10 minutes. Do not use more often than recommended. Store solution away from light or excess heat or cold.

You may experience nervousness, dizziness, or fatigue. Use caution when driving or engaging in tasks requiring alertness until response to drug is known. Frequent small meals may reduce the incidence of nausea or vomiting. Report chest pain, rapid heartbeat or palpitations, unresolved/persistent GI upset, dizziness, fatigue, trembling, increased anxiety, sleeplessness, or difficulty breathing.

Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Consult prescriber if breast-feeding.


Nursing Implications

Elderly may find it useful to utilize a spacer device when using a metered dose inhaler


Dosage Forms

Inhalation:

Aerosol: 0.2% (1:500) (15 mL, 22.5 mL); 0.25% (1:400) (15 mL)

Solution for nebulization: 0.031% (4 mL); 0.062% (4 mL); 0.25% (0.5 mL, 30 mL); 0.5% (0.5 mL, 10 mL, 60 mL); 1% (10 mL)

Injection: 0.2 mg/mL (1:5000) (1 mL, 5 mL, 10 mL)

Tablet, sublingual: 10 mg, 15 mg


References

Almquist A, Goldenberg IF, Milstein S, et al, "Provocation of Bradycardia and Hypotension by Isoproterenol and Upright Posture in Patients With Unexplained Syncope," N Engl J Med, 1989, 320(6):346-51.

Hemstreet MP, Miles MV, and Rutland RO, "Effect of Intravenous Isoproterenol on Theophylline Kinetics," J Allergy Clin Immunol, 1982, 69(4):360-4.

Illi A, Sundberg S, Ojala-Karlsson P, et al, "The Effect of Entacapone on the Disposition and Hemodynamic Effects of Intravenous Isoproterenol and Epinephrine," Clin Pharmacol Ther, 1995, 58(2):221-7.

Lang CC, Stein CM, Brown RM, et al, "Attenuation of Isoproterenol-Mediated Vasodilatation in Blacks," N Engl J Med, 1995, 333(3):155-60.

Rachelefsky GS and Siegel SC, "Asthma in Infants and Children - Treatment of Childhood Asthma: Part 1l," J Allergy Clin Immunol, 1985, 76(3):409-25.


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