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Isuprel
Overview
What is Isuprel?
Isoproterenol hydrochloride is 3,4-Dihydroxy-α-[(isopropylamino)methyl] benzyl alcohol hydrochloride, a synthetic sympathomimetic amine that is structurally related to epinephrine but acts almost exclusively on beta receptors. The molecular formula is CHNO • HCl. It has a molecular weight of 247.72 and the following structural formula:
Isoproterenol hydrochloride is a racemic compound.
Each milliliter of the sterile solution contains:
Isoproterenol hydrochloride injection, USP 0.2 mg
Edetate Disodium (EDTA) 0.2 mg
Sodium Chloride 7.0 mg
Sodium Citrate, Dihydrate 2.07 mg
Citric Acid, Anhydrous 2.5 mg
Water for Injection 1.0 mL
The pH is adjusted between 3.5 and 4.5 with hydrochloric acid or sodium hydroxide.
The sterile solution is nonpyrogenic and can be administered by the intravenous, intramuscular, subcutaneous or intracardiac routes.
What does Isuprel look like?
What are the available doses of Isuprel?
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What should I talk to my health care provider before I take Isuprel?
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How should I use Isuprel?
Isoproterenol hydrochloride injection is indicated:
Start ISUPREL injection at the lowest recommended dose and increase the rate of administration gradually if necessary while carefully monitoring the patient. The usual route of administration is by intravenous infusion or bolus intravenous injection. In dire emergencies, the drug may be administered by intracardiac injection. If time is not of the utmost importance, initial therapy by intramuscular or subcutaneous injection is preferred.
There are no well-controlled studies in children to establish appropriate dosing; however, the American Heart Association recommends an initial infusion rate of 0.1 mcg/kg/min, with the usual range being 0.1 mcg/kg/min to 1 mcg/kg/min.
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. Such solution should not be used.
What interacts with Isuprel?
Use of isoproterenol hydrochloride injection is contraindicated in patients with tachyarrhythmias; tachycardia or heart block caused by digitalis intoxication; ventricular arrhythmias which require inotropic therapy; and angina pectoris.
What are the warnings of Isuprel?
Hemorrhagic occlusive retinal vasculitis, including permanent loss of vision, occurred in patients receiving intracameral or intravitreal administration of vancomycin during or after cataract surgery. The safety and efficacy of vancomycin administered by the intracameral or the intravitreal route have not been established by adequate and well-controlled trials. Vancomycin is not indicated for the prophylaxis of endophthalmitis.
Isoproterenol hydrochloride injection, by increasing myocardial oxygen requirements while decreasing effective coronary perfusion, may have a deleterious effect on the injured or failing heart. Most experts discourage its use as the initial agent in treating cardiogenic shock following myocardial infarction. However, when a low arterial pressure has been elevated by other means, isoproterenol hydrochloride injection may produce beneficial hemodynamic and metabolic effects.
In a few patients, presumably with organic disease of the AV node and its branches, isoproterenol hydrochloride injection has paradoxically been reported to worsen heart block or to precipitate Adams-Stokes attacks during normal sinus rhythm or transient heart block.
What are the precautions of Isuprel?
General
Adequate filling of the intravascular compartment by suitable volume expanders is of primary importance in most cases of shock and should precede the administration of vasoactive drugs. In patients with normal cardiac function, determination of central venous pressure is a reliable guide during volume replacement. If evidence of hypoperfusion persists after adequate volume replacement, isoproterenol hydrochloride injection may be given.
In addition to the routine monitoring of systemic blood pressure, heart rate, urine flow, and the electrocardiograph, monitor the response to therapy by frequent determination of the central venous pressure and blood gases. Closely observe patients in shock during isoproterenol hydrochloride injection administration. If the heart rate exceeds 110 beats per minute, it may be advisable to decrease the infusion rate or temporarily discontinue the infusion. Determinations of cardiac output and circulation time may also be helpful. Take appropriate measures to ensure adequate ventilation. Pay attention to acid-base balance and to the correction of electrolyte disturbances.
Drug Interactions
Avoid ISUPREL when potent inhalational anesthetics such as halothane are employed because of potential to sensitize the myocardium to effects of sympathomimetic amines.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Pregnancy
Nursing Mothers
Pediatric Use
Intravenous infusions of isoproterenol in refractory asthmatic children at rates of 0.05‑2.7 mcg/kg/min have caused clinical deterioration, myocardial necrosis, congestive heart failure and death. The risks of cardiac toxicity appear to be increased by some factors [acidosis, hypoxemia, coadministration of corticosteroids, coadministration of methylxanthines (theophylline, theobromine) or aminophylline] that are especially likely to be present in these patients. If I.V. isoproterenol is used in children with refractory asthma, patient monitoring must include continuous assessment of vital signs, frequent electrocardiography, and daily measurements of cardiac enzymes, including CPK-MB.
Geriatric Use
What are the side effects of Isuprel?
The following reactions to isoproterenol hydrochloride injection have been reported:
CNS:
Cardiovascular:
In a few patients, presumably with organic disease of the AV node and its branches, isoproterenol hydrochloride injection has been reported to precipitate Adams-Stokes seizures during normal sinus rhythm or transient heart block.
Respiratory:
Other:
What should I look out for while using Isuprel?
Use of isoproterenol hydrochloride injection is contraindicated in patients with tachyarrhythmias; tachycardia or heart block caused by digitalis intoxication; ventricular arrhythmias which require inotropic therapy; and angina pectoris.
Isoproterenol hydrochloride injection, by increasing myocardial oxygen requirements while decreasing effective coronary perfusion, may have a deleterious effect on the injured or failing heart. Most experts discourage its use as the initial agent in treating cardiogenic shock following myocardial infarction. However, when a low arterial pressure has been elevated by other means, isoproterenol hydrochloride injection may produce beneficial hemodynamic and metabolic effects.
In a few patients, presumably with organic disease of the AV node and its branches, isoproterenol hydrochloride injection has paradoxically been reported to worsen heart block or to precipitate Adams-Stokes attacks during normal sinus rhythm or transient heart block.
What might happen if I take too much Isuprel?
The acute toxicity of isoproterenol hydrochloride in animals is much less than that of epinephrine. Excessive doses in animals or man can cause a striking drop in blood pressure, and repeated large doses in animals may result in cardiac enlargement and focal myocarditis.
In case of accidental overdosage as evidenced mainly by tachycardia or other arrhythmias, palpitations, angina, hypotension, or hypertension, reduce rate of administration or discontinue isoproterenol hydrochloride injection until patient’s condition stabilizes. Blood pressure, pulse, respiration, and ECG should be monitored.
It is not known whether isoproterenol hydrochloride is dialyzable.
The oral LD of isoproterenol hydrochloride in mice is 3,850 mg/kg ± 1,190 mg/kg of pure drug in solution.
How should I store and handle Isuprel?
ArrayProtect from light. Keep in opaque container until used.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Do not use if the injection is pinkish or darker than slightly yellow or contains a precipitate.Hospira, Inc., Lake Forest, IL 60045 USALAB-1243-1.0Revised: 01/2018Protect from light. Keep in opaque container until used.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Do not use if the injection is pinkish or darker than slightly yellow or contains a precipitate.Hospira, Inc., Lake Forest, IL 60045 USALAB-1243-1.0Revised: 01/2018Protect from light. Keep in opaque container until used.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Do not use if the injection is pinkish or darker than slightly yellow or contains a precipitate.Hospira, Inc., Lake Forest, IL 60045 USALAB-1243-1.0Revised: 01/2018Protect from light. Keep in opaque container until used.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Do not use if the injection is pinkish or darker than slightly yellow or contains a precipitate.Hospira, Inc., Lake Forest, IL 60045 USALAB-1243-1.0Revised: 01/2018Protect from light. Keep in opaque container until used.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Do not use if the injection is pinkish or darker than slightly yellow or contains a precipitate.Hospira, Inc., Lake Forest, IL 60045 USALAB-1243-1.0Revised: 01/2018Protect from light. Keep in opaque container until used.Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]Do not use if the injection is pinkish or darker than slightly yellow or contains a precipitate.Hospira, Inc., Lake Forest, IL 60045 USALAB-1243-1.0Revised: 01/2018
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Isoproterenol is a potent nonselective beta-adrenergic agonist with very low affinity for alpha‑adrenergic receptors. Intravenous infusion of isoproterenol in man lowers peripheral vascular resistance, primarily in skeletal muscle but also in renal and mesenteric vascular beds. Diastolic pressure falls. Renal blood flow is decreased in normotensive subjects but is increased markedly in shock. Systolic blood pressure may remain unchanged or rise, although mean arterial pressure typically falls. Cardiac output is increased because of the positive inotropic and chronotropic effects of the drug in the face of diminished peripheral vascular resistance. The cardiac effects of isoproterenol may lead to palpitations, sinus tachycardia, and more serious arrhythmias; large doses of isoproterenol may cause myocardial necrosis in animals.
Isoproterenol relaxes almost all varieties of smooth muscle when the tone is high, but this action is most pronounced on bronchial and gastrointestinal smooth muscle. It prevents or relieves bronchoconstriction, but tolerance to this effect develops with overuse of the drug.
In man, isoproterenol causes less hyperglycemia than does epinephrine. Isoproterenol and epinephrine are equally effective in stimulating the release of free fatty acids and energy production.
Absorption, Fate, and Excretion
Non-Clinical Toxicology
Use of isoproterenol hydrochloride injection is contraindicated in patients with tachyarrhythmias; tachycardia or heart block caused by digitalis intoxication; ventricular arrhythmias which require inotropic therapy; and angina pectoris.Isoproterenol hydrochloride injection, by increasing myocardial oxygen requirements while decreasing effective coronary perfusion, may have a deleterious effect on the injured or failing heart. Most experts discourage its use as the initial agent in treating cardiogenic shock following myocardial infarction. However, when a low arterial pressure has been elevated by other means, isoproterenol hydrochloride injection may produce beneficial hemodynamic and metabolic effects.
In a few patients, presumably with organic disease of the AV node and its branches, isoproterenol hydrochloride injection has paradoxically been reported to worsen heart block or to precipitate Adams-Stokes attacks during normal sinus rhythm or transient heart block.
Theophylline interacts with a wide variety of drugs. The interaction may be pharmacodynamic, i.e., alterations in the therapeutic response to theophylline or another drug or occurrence of adverse effects without a change in serum theophylline concentration. More frequently, however, the interaction is pharmacokinetic, i.e., the rate of theophylline clearance is altered by another drug resulting in increased or decreased serum theophylline concentrations. Theophylline only rarely alters the pharmacokinetics of other drugs.
The drugs listed in have the potential to produce clinically significant pharmacodynamic or pharmacokinetic interactions with theophylline. The information in the "Effect" column of assumes that the interacting drug is being added to a steady-state theophylline regimen. If theophylline is being initiated in a patient who is already taking a drug that inhibits theophylline clearance (e.g., cimetidine, erythromycin), the dose of theophylline required to achieve a therapeutic serum theophylline concentration will be smaller. Conversely, if theophylline is being initiated in a patient who is already taking a drug that enhances theophylline clearance (e.g., rifampin), the dose of theophylline required to achieve a therapeutic serum theophylline concentration will be larger. Discontinuation of a concomitant drug that increases theophylline clearance will result in accumulation of theophylline to potentially toxic levels, unless the theophylline dose is appropriately reduced. Discontinuation of a concomitant drug that inhibits theophylline clearance will result in decreased serum theophylline concentrations, unless the theophylline dose is appropriately increased.
The drugs listed in have either been documented not to interact with theophylline or do not produce a clinically significant interaction (i.e., <15% change in theophylline clearance).
The listing of drugs in are current as of September 1, 1995. New interactions are continuously being reported for theophylline, especially with new chemical entities. Before addition of a newly available drug in a patient receiving theophylline, the package insert of the new drug and/or the medical literature should be consulted to determine if an interaction between the new drug and theophylline has been reported.
Most serum theophylline assays in clinical use are immunoassays which are specific for theophylline. Other xanthines such as caffeine, dyphylline, and pentoxifylline are not detected by these assays. Some drugs (e.g., cefazolin, cephalothin), however, may interfere with certain HPLC techniques. Caffeine and xanthine metabolites in neonates or patients with renal dysfunction may cause the reading from some dry reagent office methods to be higher than the actual serum theophylline concentration.
General
Adequate filling of the intravascular compartment by suitable volume expanders is of primary importance in most cases of shock and should precede the administration of vasoactive drugs. In patients with normal cardiac function, determination of central venous pressure is a reliable guide during volume replacement. If evidence of hypoperfusion persists after adequate volume replacement, isoproterenol hydrochloride injection may be given.
In addition to the routine monitoring of systemic blood pressure, heart rate, urine flow, and the electrocardiograph, monitor the response to therapy by frequent determination of the central venous pressure and blood gases. Closely observe patients in shock during isoproterenol hydrochloride injection administration. If the heart rate exceeds 110 beats per minute, it may be advisable to decrease the infusion rate or temporarily discontinue the infusion. Determinations of cardiac output and circulation time may also be helpful. Take appropriate measures to ensure adequate ventilation. Pay attention to acid-base balance and to the correction of electrolyte disturbances.
Drug Interactions
Avoid ISUPREL when potent inhalational anesthetics such as halothane are employed because of potential to sensitize the myocardium to effects of sympathomimetic amines.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Pregnancy
Nursing Mothers
Pediatric Use
Intravenous infusions of isoproterenol in refractory asthmatic children at rates of 0.05‑2.7 mcg/kg/min have caused clinical deterioration, myocardial necrosis, congestive heart failure and death. The risks of cardiac toxicity appear to be increased by some factors [acidosis, hypoxemia, coadministration of corticosteroids, coadministration of methylxanthines (theophylline, theobromine) or aminophylline] that are especially likely to be present in these patients. If I.V. isoproterenol is used in children with refractory asthma, patient monitoring must include continuous assessment of vital signs, frequent electrocardiography, and daily measurements of cardiac enzymes, including CPK-MB.
Geriatric Use
The following reactions to isoproterenol hydrochloride injection have been reported:
CNS:
Cardiovascular:
In a few patients, presumably with organic disease of the AV node and its branches, isoproterenol hydrochloride injection has been reported to precipitate Adams-Stokes seizures during normal sinus rhythm or transient heart block.
Respiratory:
Other:
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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