Brand Name :
Isuprel [DSC]
Synonyms :
isoprenaline
Class :
Beta1/Beta2 Agonist
Dosage Forms & Strengths
Intravenous Injection
Isuprel: 0.2 mg/mL (of 1 mL [DSC], 5 mL [DSC]) [containing disodium edta]
1 to 20 mcg/minute usual dose of Continuous intravenous infusion; titrate to the clinical response
2 to 10 mcg/minute usual dose of Continuous intravenous infusion; titrate to the clinical response
Cardiogenic shock (off-label):
2 to 20 mcg/minute Continuous intravenous infusion
Provocation during tilt table testing, diagnostic agent for syncope (off-label):
Initial dose: 1 mcg/minute Continuous intravenous infusion; may increase based on the clinical response till 3 mcg/minute
Dosage Forms & Strengths
Intravenous Injection
Isuprel: 0.2 mg/mL (of 1 mL [DSC], 5 mL [DSC]) [containing disodium edta]
Infants, Children & Adolescents: 0.05 to 0.5 mcg/kg/minute continuous intravenous infusion; titrate to the effect; doses as high as 2 mcg/kg/minute can be required in some patients; 2 to 10 mcg/minute is the usual adult range
Dose Adjustments
Dosing modifications
Kidney Impairment
Dose adjustment is not necessary
Hepatic Impairment
Dose adjustment is not necessary
Refer to the adult dosing regimen
Beta-Blockers decrease the effect of bronchiodilation of Beta2-Agonists
Beta-Blockers decrease the effect of bronchiodilation of Beta2-Agonists
Beta-Blockers decrease the effect of bronchiodilation of Beta2-Agonists
Beta-Blockers decrease the effect of bronchiodilation of Beta2-Agonists
Beta-Blockers decrease the effect of bronchiodilation of Beta2-Agonists
may decrease the therapeutic effect when combined with methacholine
May increase the adverse effect when combined
may increase the adverse effect of other beta2-agonists
may increase the adverse effect of other beta2-agonists
may increase the adverse effect of other beta2-agonists
may increase the adverse effect of other beta2-agonists
may increase the adverse effect of other beta2-agonists
may have an increasingly adverse effect when combined with other beta2-agonists
may have an increasingly adverse effect when combined with other beta2-agonists
may have an increasingly adverse effect when combined with other beta2-agonists
may increase the adverse effect of other beta2-agonists
may increase the adverse effect of other beta2-agonists
may increase the adverse effect of other beta2-agonists
may increase the adverse effect of other beta2-agonists
may increase the adverse effect of other beta2-agonists
may decrease the bronchodilatory effect of beta2-agonists
may decrease the bronchodilatory effect of beta2-agonists
may increase the toxic effect of beta2 agonists
may decrease the bronchodilatory effect
may increase the toxic effect of beta2 agonists
may increase the toxic effect of beta2 agonists
may decrease the bronchodilatory effect of beta blockers
may decrease the bronchodilatory effect when combined with beta2-agonists
may decrease the bronchodilatory effect when combined with beta2-agonists
may decrease the bronchodilatory effect when combined with beta2-agonists
may decrease the bronchodilatory effect when combined with beta2-agonists
may decrease the bronchodilatory effect when combined with beta2-agonists
may have an increasingly adverse effect when combined with other beta2-agonists
may have an increasingly adverse effect when combined with other beta2-agonists
may have an increasingly adverse effect when combined with other beta2-agonists
may decrease the therapeutic effect of each other when combined
may decrease the bronchodilatory effect when combined with beta2-agonists
may decrease the bronchodilatory effect when combined with beta2-agonists
may decrease the bronchodilatory effect when combined with beta2-agonists
may decrease the bronchodilatory effect of beta-blockers
may decrease the bronchodilatory effect of beta-blockers
may increase the adverse effect of monoamine oxidase inhibitors
may increase the adverse effect of monoamine oxidase inhibitors
may increase the adverse effect of monoamine oxidase inhibitors
may increase the adverse effect of monoamine oxidase inhibitors
may increase the adverse effect of monoamine oxidase inhibitors
may reduce the bronchodilatory effect
may reduce the bronchodilatory effect
may reduce the bronchodilatory effect
may reduce the bronchodilatory effect
may reduce the bronchodilatory effect
may reduce the bronchodilatory effect
may reduce the bronchodilatory effect
may have an increased hypokalemic effect when combined with loop diuretics
may have an increased hypokalemic effect when combined with loop diuretics
may have an increased hypokalemic effect when combined with loop diuretics
Beta2-Agonists: they mayincrease the hypokalemic effect when combined with thiazides
Beta2-Agonists: they mayincrease the hypokalemic effect when combined with thiazides
Beta2-Agonists: they mayincrease the hypokalemic effect when combined with thiazides
Beta2-Agonists: they mayincrease the hypokalemic effect when combined with thiazides
may increase the tachycardic effect of atomoxetine
may increase the hypokalemic effect of beta2-agonists
may increase the hypokalemic effect of beta2-agonists
may increase the hypokalemic effect of beta2-agonists
may decrease the bronchodilatory effect of beta blockers
lisinopril/hydrochlorothiazide
may increase the hypokalemic effect of blood pressure-lowering agents
eprosartan/hydrochlorothiazide
may increase the toxic effect of thiazide and thiazide like diuretics
may increase the hypokalaemia effect of thiazide and thiazide like diuretics
may have an increasingly adverse effect when combined with atosiban
may have an increasingly adverse effect when combined with beta2-agonists
may have an increasingly adverse effect when combined with beta2-agonists
may have an increasingly adverse effect when combined with beta2-agonists
may have an increasingly adverse effect when combined with beta2-agonists
may have an increasingly adverse effect when combined with beta2-agonists
may have an increasingly adverse effect when combined with beta2-agonists
theophylline derivatives: they may increase the toxic effect of Beta2-Agonists
tricyclic antidepressants: they may increase the toxic effect of Beta2-Agonists
tricyclic antidepressants: they may increase the toxic effect of Beta2-Agonists
tricyclic antidepressants: they may increase the toxic effect of Beta2-Agonists
may have an increasingly adverse effect when combined with beta2-agonists
Actions and spectrum:
Cardiac stimulation: isoprenaline increases heart rate and contractility, leading to an increase in cardiac output.
Bronchodilation: isoprenaline relaxes the smooth muscles of the bronchioles, improving airflow and relieving symptoms of bronchospasm.
Vasodilation: isoprenaline relaxes the smooth muscles of blood vessels, leading to vasodilation and a decrease in peripheral vascular resistance.
Positive inotropic and chronotropic effects: isoprenaline enhances the force of myocardial contraction and increases heart rate.
Management of bradycardia: isoprenaline is used to treat severe bradycardia or heart block.
The spectrum of isoprenaline’s effects primarily targets the cardiovascular and respiratory systems, making it useful in the management of certain cardiac and respiratory conditions.
Post marketing reports:
Dermatologic: pallor, Diaphoresis
Nervous system: headache, tremor, Dizziness, nervousness
Respiratory: pulmonary edema, Dyspnea
Cardiovascular: angina pectoris, bradycardia, coronary artery vasospasm, hypertension, increased ST segment, tachyarrhythmia, ventricular arrhythmia, Adams-Stokes syndrome, atrioventricular block, chest pain, flushing, hypotension, tachycardia, ventricular premature contraction
Gastrointestinal: Nausea
Ophthalmic: Blurred vision
Black Box Warning:
isoprenaline does not have a specific black box warning.
Contraindication/Caution:
Contraindication:
Hypersensitivity: Individuals who have a known hypersensitivity or allergy to isoprenaline or any of its components should not use this medication.
Severe heart disease: isoprenaline is contraindicated in patients with severe heart disease, such as severe coronary artery disease, severe heart failure, or a recent myocardial infarction (heart attack).
Untreated thyrotoxicosis: isoprenaline should not be used in patients with untreated thyrotoxicosis, a condition characterized by excessive thyroid hormone production.
Pheochromocytoma: isoprenaline is contraindicated in patients with pheochromocytoma that can causes high blood pressure and cardiovascular effects.
Arrhythmias: isoprenaline should be used with caution in patients with certain arrhythmias, such as ventricular tachycardia or atrial fibrillation, as it can potentially worsen these conditions.
Caution:
Diabetes: isoprenaline can mask the symptoms of low blood sugar in patients with diabetes, so careful monitoring of blood glucose levels is necessary.
Heart disease: isoprenaline can have a stimulating effect on the heart, so caution is required in patients with underlying heart disease, including angina, arrhythmias, or previous heart attacks.
Asthma and other respiratory conditions: isoprenaline can cause bronchodilation, so caution is advised in patients with asthma or other respiratory conditions, as it may exacerbate symptoms.
Prostatic hypertrophy: isoprenaline can cause urinary retention, so caution is needed in patients with prostatic hypertrophy (enlarged prostate).
Pregnancy and lactation: isoprenaline should be used with caution during pregnancy and lactation, as its safety in these populations has not been fully established.
Comorbidities:
Hypertension: isoprenaline can increase blood pressure, so careful monitoring is required in patients with hypertension.
Coronary artery disease: isoprenaline can increase heart rate and cardiac workload, which may be concerning in patients with underlying coronary artery disease. Caution is advised, and careful monitoring of cardiac function is necessary.
Arrhythmias: isoprenaline can have pro-arrhythmic effects and may exacerbate existing arrhythmias. Patients with pre-existing arrhythmias should be closely monitored if isoprenaline is used.
Hyperthyroidism: isoprenaline can have stimulatory effects on the thyroid gland, so caution is advised in patients with hyperthyroidism.
Pregnancy consideration: pregnancy category: not assigned
Lactation: excreted into human milk: unknown
Pregnancy category:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category.
Pharmacology:
isoprenaline, also known as isoproterenol, is a synthetic sympathomimetic amine that acts primarily as a non-selective β-adrenergic receptor agonist. It stimulates β1-adrenergic receptors in the heart, leading to increased heart rate and contractility. It also activates β2-adrenergic receptors in the smooth muscles of the bronchioles, resulting in bronchodilation. isoprenaline’s pharmacological effects include positive inotropic and chronotropic actions on the heart, bronchodilation, vasodilation, and uterine relaxation. It is used in the management of various conditions such as bradycardia, heart block, asthma, and certain types of shock.
Pharmacodynamics:
Cardiac stimulation: isoprenaline stimulates beta-1 adrenergic receptors in the heart, leading to an increased heart rate (positive chronotropic effect) and increased force of contraction (positive inotropic effect). This results in enhanced cardiac output.
Bronchodilation: isoprenaline activates beta-2 adrenergic receptors in the smooth muscle of the bronchioles, causing relaxation and dilation of the airways. This leads to bronchodilation and improved airflow in the lungs.
Vasodilation: isoprenaline stimulates beta-2 adrenergic receptors in blood vessels, causing relaxation of smooth muscle and subsequent vasodilation. This results in decreased peripheral vascular resistance and increased blood flow to various organs.
Metabolic effects: isoprenaline activates beta-adrenergic receptors in adipose tissue, promoting the breakdown of stored fats (lipolysis). It also stimulates glycogenolysis in the liver, leading to increased blood glucose levels.
Pharmacokinetics:
Absorption
isoprenaline can be administered via various routes, including oral, intravenous, intramuscular, and inhalation. The oral route is less commonly used due to extensive first-pass metabolism. When administered intravenously or by inhalation, isoprenaline is rapidly absorbed into the bloodstream.
Distribution
isoprenaline is distributed throughout the body and readily crosses the blood-brain barrier. It has a relatively short duration of action due to rapid distribution into tissues and subsequent metabolism.
Metabolism
isoprenaline is primarily metabolized in the liver by enzymes such as catechol-O-methyltransferase (COMT). It undergoes extensive first-pass metabolism, resulting in a low bioavailability when taken orally. The major metabolites of isoprenaline include inactive conjugates and small amounts of isopropylnorepinephrine.
Elimination and excretion
The metabolites of isoprenaline, along with a small portion of unchanged drug, are excreted primarily in the urine. The elimination half-life of isoprenaline is relatively short, ranging from a few minutes to a couple of hours, depending on the route of administration.
Administration:
Intravenous (IV) injection: isoprenaline can be administered directly into a vein by a healthcare professional. This route is often used in emergency situations or when immediate effects are desired.
Inhalation: isoprenaline can be administered using an inhaler or nebulizer device, allowing it to be inhaled into the lungs. This route is commonly used for the management of acute bronchospasm or asthma.
Intramuscular (IM) injection: isoprenaline can be injected into a muscle, usually in the upper arm or thigh. This route may be used in specific clinical situations or when intravenous access is not readily available.
Patient information leaflet
Generic Name: isoprenaline
Pronounced: Eye-soh-PREN-uh-leen
Why do we use isoprenaline?
Cardiac stimulation: isoprenaline is used to stimulate the heart in cases of bradycardia (slow heart rate) or heart block. It can increase heart rate and improve cardiac output.
Bronchodilation: isoprenaline is used as a bronchodilator to relax and open up the airways in conditions such as asthma, COPD, and bronchospasm.
Diagnosis of coronary artery disease: isoprenaline can be used during stress tests to assess coronary artery blood flow and detect potential blockages or ischemia (lack of blood supply) in the heart.
Treatment of certain arrhythmias: isoprenaline may be used to manage specific types of arrhythmias, such as supraventricular tachycardia (SVT) or atrioventricular (AV) nodal reentry tachycardia.
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