Isoproterenol Hcl (isoproterenol HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Isoproterenol hydrochloride is a synthetic sympathomimetic agent that acts directly on both beta1- and beta2-adrenergic receptors (nonselective beta-agonist).
Isoproterenol is a potent nonselective beta-adrenergic agonist with very low affinity for alpha-adrenergic receptors. Isoproterenol is a synthetic sympathomimetic drug that is structurally related to epinephrine.
IV infusion of isoproterenol in humans produces a reduction in peripheral vascular resistance, predominantly within skeletal muscle and, to a lesser extent, in the renal and mesenteric vascular beds. Consequently, diastolic blood pressure decreases. Renal blood flow usually is decreased in normotensive patients, but is substantially increased in patients with shock.
Systolic arterial pressure may remain unchanged or increase; however, mean arterial pressure typically declines. Cardiac output increases due to the positive inotropic and chronotropic effects of the drug in the setting of reduced peripheral vascular resistance.
Isoproterenol induces relaxation of smooth muscle in most tissues when baseline tone is elevated, with the most pronounced effects observed in bronchial and GI smooth muscle. The drug prevents or alleviates bronchoconstriction, although repeated or excessive use leads to the development of tolerance. In humans, isoproterenol produces less hyperglycemia than epinephrine.
Both drugs are equally effective in stimulating free fatty acid release and enhancing energy production.
Isoproterenol is readily absorbed when administered parenterally or as an aerosol. The drug is metabolized primarily in the liver and other tissues by the enzyme catechol-O-methyltransferase (COMT). Isoproterenol is a relatively poor substrate for monoamine oxidase and is taken up by sympathetic neurons to a lesser extent than epinephrine and norepinephrine.
Consequently, its duration of action may exceed that of epinephrine, although it remains brief. Isoproterenol has a short half-life.
Generic name: isoproterenol HCl
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
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Indications
The following indications are listed for Isoproterenol Hcl:
- Atrioventricular Block
- Cardiac Arrest
- Hypovolemic Shock
- Low Cardiac Output
- Syncope Due To Heart Block
Also known as: Av Block, Heart Arrest, Hypovolemic Shock Syndrome, Subnormal Or Depressed Cardiac Output, Ventricular Arrest.
Dosing
Dosage of isoproterenol hydrochloride is expressed in terms of the salt.
Isoproterenol should be initiated at the lowest recommended dose and increased gradually based on patient response. Adjust dosage according to clinical and hemodynamic parameters including heart rate, central venous pressure, systemic blood pressure, and urine output.
Isoproterenol hydrochloride injection is available in single-dose vials containing 0.2 mg/mL of the drug. Isoproterenol hydrochloride usually is administered by direct (''bolus'') IV injection or IV infusion. The drug may also be administered by IM, subcutaneous, or intracardiac injection.
For IM, subcutaneous, or intracardiac injection, commercially available isoproterenol hydrochloride injection is administered undiluted. For IV administration, the drug should be diluted prior to administration.
Isoproterenol should be stored at 20-25degreesC. Protect from light, and keep in an opaque container until use.
Isoproterenol should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit. The injection should be discarded if the solution is pinkish or darker than slightly yellow or contains a precipitate. Unused portions should be discarded.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Angina pectoris.
*Ventricular arrhythmias.
*Tachycardia.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Common adverse effects with isoproterenol include tachycardia and palpitations.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
The safety and efficacy of isoproterenol hydrochloride in pediatric patients have not been established. However, the drug has been used in pediatric patients+ for certain conditions.
IV infusions of isoproterenol hydrochloride (0.05-2.7 mcg/kg per minute) in pediatric patients with refractory asthma have caused clinical deterioration, myocardial necrosis, congestive heart failure (CHF), and death. The risk of developing such cardiac toxicity may be increased by acidosis, hypoxia, and/or concomitant use of other agents such as xanthine derivatives or corticosteroids, drugs that are likely to be used in these children. If IV isoproterenol is used in pediatric patients with refractory asthma, vital signs should be monitored continuously, ECG monitored frequently, and cardiac-specific serum isoenzyme MB concentrations of serum CK (CPK) should be determined daily.
Based on published literature, prolonged experience with isoproterenol use in pregnant women spanning several decades has not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
Hypotension associated with shock during pregnancy constitutes a medical emergency and may be fatal if not promptly treated. Delayed management of hypotension in pregnant patients with shock may increase the risk of maternal and fetal morbidity and mortality. Accordingly, life-sustaining therapy for the pregnant patient should not be withheld due to potential concerns regarding fetal effects of isoproterenol.
The use of isoproterenol during labor and delivery is associated with risks to both the mother and the fetus. Isoproterenol generally inhibits spontaneous and oxytocin-induced uterine contractions and may prolong the second stage of labor. Use of isoproterenol should be avoided during the second stage of labor and in obstetric settings when maternal blood pressure exceeds 130/80 mmHg. Although isoproterenol may improve maternal hypotension associated with shock, it may also cause uterine vasoconstriction, reduced uterine blood flow, uterine atony with hemorrhage, and fetal anoxia.
There are no available data regarding the presence of isoproterenol in human milk, its effects on the breast-fed infant, or its impact on milk production. However, given the short elimination half-life of isoproterenol, infant exposure through breast milk is anticipated to be minimal.
The manufacturer makes no specific dosage recommendations for geriatric patients. In general, dosage should be titrated carefully in geriatric patients, usually initiating therapy at the low end of the dosage range. The greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly also should be considered.
Clinical studies of isoproterenol hydrochloride did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger patients. Some data suggest that geriatric healthy individuals or hypertensive patients are less responsive to beta-adrenergic stimulation than younger adults. In general, dosage should be titrated carefully in geriatric patients, usually initiating therapy at the low end of the dosage range. The greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly also should be considered.
ICD codes
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Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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