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Pronunciation |
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(eye
soe proe TER e
nole) |
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U.S. Brand
Names |
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Arm-a-Med® Isoproterenol;
Dey-Dose® Isoproterenol; Isuprel®;
Medihaler-Iso® |
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Generic
Available |
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Yes |
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Synonyms |
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Isoprenaline Hydrochloride; Isoproterenol Hydrochloride; Isoproterenol
Sulfate |
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Pharmacological Index |
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Beta1/Beta2 Agonist |
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Use |
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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 |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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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 |
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Warnings/Precautions |
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Elderly patients, diabetics, renal or cardiovascular disease,
hyperthyroidism; excessive or prolonged use may result in decreased
effectiveness |
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Adverse
Reactions |
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>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
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Overdosage/Toxicology |
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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 |
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Drug
Interactions |
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Increased toxicity: Sympathomimetic agents may cause headaches and elevate
blood pressure; general anesthetics may cause arrhythmias |
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Stability |
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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
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Mechanism of
Action |
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Stimulates beta1- and beta2-receptors resulting in
relaxation of bronchial, GI, and uterine smooth muscle, increased heart rate and
contractility, vasodilation of peripheral vasculature |
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Pharmacodynamics/Kinetics |
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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 |
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Usual Dosage |
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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
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Monitoring
Parameters |
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EKG, heart rate, respiratory rate, arterial blood gas, arterial blood
pressure, CVP |
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Mental Health: Effects
on Mental Status |
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Insomnia and restlessness are common |
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Mental Health:
Effects on Psychiatric
Treatment |
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None reported |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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Isoproterenol is selective for beta-adrenergic receptors and not alpha
receptors; therefore, there is no precaution in the use of vasoconstrictor such
as epinephrine |
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Dental Health:
Effects on Dental Treatment |
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>10% of patients experience dry mouth |
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Patient
Information |
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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. |
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Nursing
Implications |
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Elderly may find it useful to utilize a spacer device when using a metered
dose inhaler |
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Dosage Forms |
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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 |
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References |
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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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