Isoprenaline
Clinical data | |
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Trade names | Many[1] |
Other names | Isoproterenol (USAN US) |
MedlinePlus | a601236 |
Pregnancy category |
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Routes of administration | Inhalation (80–120 μg), intravenous injection (IV) |
ATC code | |
Legal status | |
Legal status |
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Pharmacokinetic data | |
Elimination half-life | ~2 minutes |
Identifiers | |
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Isoprenaline, or isoproterenol, is a
Medical uses
It is used to treat
Historically, it was used to treat asthma via metered aerosol or nebulizing devices; it was also available in sublingual, oral, intravenous, and intramuscular formulations.[4] The U.S. National Asthma Education and Prevention Program Expert Panel recommends against its use as a nebulizer for acute bronchoconstriction.[5]
Isoprenaline can also ameliorate the impairment of intestinal stem cells mediated by β2-adrenoreceptors after chemotherapy.[6]
Contraindications
It should not be used in people with tachyarrhythmias (except in special circumstances),[7] tachycardia or heart block caused by digitalis poisoning, ventricular arrhythmias which require inotropic therapy, or with angina.[2]
Adverse effects
Adverse effects of isoprenaline include nervousness, headache, dizziness, nausea, visual blurring, tachycardia, palpitations, angina, Adams-Stokes attacks, pulmonary edema, hypertension, hypotension, ventricular arrhythmias, tachyarrhythmias, difficulty breathing, sweating, mild tremors, weakness, flushing, and pallor.[2] Isoproterenol has been reported to cause insulin resistance leading to diabetic ketoacidosis.[8]
Pharmacology
The adverse effects of isoprenaline are also related to the drug's cardiovascular effects. Isoprenaline can produce
Pharmacodynamics
Isoprenaline is a
Isoprenaline's effects on the
The
Pharmacokinetics
The plasma half-life for isoproterenol is approximately two to five minutes. It is degraded enzymatically via catechol O-methyltransferase (COMT) primarily in the liver and excreted in the urine as sulfated conjugates.[14][15]
Chemistry
It is structurally related to
History
It was first approved in the US in 1947.[4] Between 1963 and 1968 in England, Wales, Scotland, Ireland, Australia, and New Zealand there was an increase in deaths among people using isoprenaline to treat asthma. This was attributed to overdose: the inhalers produced in that area were dispensing five times the dosage dispensed by inhalers produced in the US and Canada, where the deaths were not observed.[16][17]
Society and culture
Brands
Isoprenaline is marketed under many brand names worldwide, including Aleudrina, Asthpul, Iludrin, Isomenyl, Isuprel, Neo-Epinine, Neodrenal, Proternol, and Saventrine.[1] It is also marketed as a combination drug with cromoglicic acid as Frenal Compositum, in combination with pronase as Isopal P, and in combination with atropine as Stmerin D.[1]
References
- ^ a b c "Isoprenaline international brands". Drugs.com. Archived from the original on June 26, 2019. Retrieved June 21, 2017.
- ^ a b c d e "Label: Isoproterenol hydrochloride injection, solution". NIH DailyMed. September 10, 2013. Retrieved June 21, 2017.
- .
- ^ ISBN 978-1-59259-654-6.
- ^ National Asthma Education and Prevention Program Expert Panel (August 28, 2007). "Expert Panel Report 3: Guidelines for the Diagnosis and Management of Asthma" (PDF). NIH National Heart, Lung, and Blood Institute.
- PMID 31648381.
- PMID 17612676.
- PMID 30647979.
- PMID 13062084.
- PMID 25606852.
- PMID 22073124.
Table 1. EC50 values of different agonists at hTAAR1, hADRB1 and hADRB2
- ISBN 978-83-200-5368-5.
- ^ Mehta A (January 27, 2011). "Notes - Medicinal Chemistry of the Peripheral Nervous System - Adrenergics and Cholinergic". Pharmaxchange. Archived from the original on 4 November 2010. Retrieved June 21, 2017.
- S2CID 81053428.
- .
- PMID 9919437.
- S2CID 31732029.