Identification

Summary

Isoprenaline is a catecholamine non-selective beta-adrenergic a91neg.comnist typically used khổng lồ treat bradycardia and heart block.

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Brand Names
Generic NameIsoprenaline91neg.com Accession NumberDB01064Background

Isoprenaline is a non-selective beta adrenergic receptor a91neg.comnist indicated lớn treat heart block, Adams-Stokes attacks, bronchospasm in anesthesia, cadiac arrest, hypovolemic shocks, septic shock, hypoperfusion, congestive hear failure, & cardiogenic shock.2,14

Isoprenaline research in the 1940s found that this isopropyl analog of epinephrine dilated the bronchi, as well as raising the heart rate and cardiac output, without vasoconstriction.11,12 The US patent from 1943 states that this compound had a wider therapeutic index & a stronger action than adrenaline.16

Isoprenaline was granted FDA approval on 19 February 1948.13

TypeSmall MoleculeGroupsApproved, InvestigationalStructure
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Similar Structures
Structure for Isoprenaline (DB01064)×
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WeightAverage: 211.2576 Monoisotopic: 211.120843415 Chemical FormulaC11H17NO3Synonyms(±)-isoprenaline(±)-isoproterenol1-(3,4-dihydroxyphenyl)-2-(isopropylamino)ethanol1-(3,4-dihydroxyphenyl)-2-isopropylaminoethanol3,4-dihydroxy-α-<(isopropylamino)methyl>benzyl alcoholIsoprenalina
IsoprenalineIsoprénaline
Isoprenalinum
Isopropyl noradrenalineIsoproterenolN-isopropyl-β-dihydroxyphenyl-β-hydroxyethylamineN-IsopropylnoradrenalineN-Isopropylnorepinephrineα-(isopropylaminomethyl)protocatechuyl alcohol

Pharmacology

Indication

Isoprenaline is indicated to lớn treat mild or transient episodes of heart block not requiring electric shock or pacemakers, serious episodes of heart block and Adams-Stokes attacks not caused by ventricular tachycardia or fibrillation, & bronchospasm during anesthesia.14 Isoprenaline is also indicated for cases of cardiac arrest until preferable treatments lượt thích electric shock và pacemakers are available.14 Isoprenaline is also indicated as an adjunct therapy to lớn fluid và electrolyte replacement therapy in hypovolemic shock, septic shock, hypoperfusion, congestive heart failure, & cardiogenic shock.14


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Associated Conditions
Contraindications và Blackbox Warnings
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Pharmacodynamics

Isoprenaline is a non-selective beta adrenergic receptor a91neg.comnist used in a number of indications for the heart, as well as bronchospasm in anesthesia.2,14 Isoprenaline has a short duration of action as it is rapidly cleared,8,7 và a wide therapeutic index.14 Patients should be counselled regarding the risks of isoprenaline in the treatment of cardiogenic shock following myocardial infarction, paradoxical worsening of heart block, or precipitation of Adams-Stokes attacks.14

Mechanism of action

Isoprenaline is a non-selective beta adrenergic receptor a91neg.comnist.2 A91neg.comnism of beta-1 và beta-2 adrenergic receptors causes the alpha subunit of G-protein coupled receptors to lớn exchange GMP for GTP, activating them, & allowing the alpha subunit lớn dissociate from the beta and gamma subunits.1,4 Dissociation of the alpha subunit activates adenylate cyclase, converting ATP to lớn cyclic AMP.1 Cyclic AMP activates protein kinase A (PKA), which phosphorylates cardiac L-type calcium channels such as Cav1.2.1,3,4 These channels depolarize cells by inward active transport of calcium ions.3,4

A91neg.comnism of beta-1 adrenergic receptors lead to increased strength of contractility, conduction of nerve impulses, tốc độ of relaxation, and rate in the heart.1

A91neg.comnism of beta-2 adrenergic receptors leads lớn glycogenolysis in the liver,5 gluca91neg.comn release from the pancreas, and activation of the renin-angiotensin-aldosterone system.1

In the alveoli, a91neg.comnism of beta-2 adrenergic receptors, activates similar pathways to the heart, however the kết thúc result is regulation of sodium channels, the cystic fibrosis transmembrane conductance regulator (CFTR), and sodium potassium ATPase.10 PKA phosphorylates scaffolding proteins và sodium channels, increasing the number of sodium channels on the apical side of alveolar cells and increasing active transport of sodium ions into cells.10 A91neg.comnism of beta-2 adrenergic receptors can also increase chloride ion transport across CFTR.10 Together, these actions lead khổng lồ passive transport of water out of the alveoli, & the clearance of alveolar fluid.10

TargetActionsOrganism
ABeta-1 adrenergic receptor
Humans
Absorption

Data regarding absorption kinetics of isoprenaline are not readily available.8,7

Volume of distribution

In pediatric patients, the volume of distribution was 216 ± 57 mL/kg.7

Protein binding

Isoprenaline is 68.8 ± 1.2% protein bound in plasma, mainly to lớn serum albumin.9

Metabolism

Isoprenaline is predominantly metabolized khổng lồ glucuronide conjugates.6 Isoprenaline can also be O-methylated by catechol O-methyltransferase to lớn the metabolite 3-O-methylisoprenaline, which can also be further glucuronidated.6

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IsoprenalineRoute of elimination

Isoprenaline is 12.2-27.0% recovered in the feces & 59.1-106.8% recovered in the urine after 48 hours.6 The majority of the recovered dose in the urine is conjugated isoprenaline, with 6.5-16.2% không tính tiền isoprenaline, and 2.6-11.4% 3-O-methylisoprenaline và conjugates.6

Half-life

The half life of intravenous isoprenaline is 2.5-5 minutes.1 Oral isoprenaline has a half life of 40 minutes.6

Clearance

In pediatric patients, the clearance of isoprenaline was 42.5 ± 5.0 mL/kg/min.7

Adverse Effects
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Toxicity

Patients experiencing an overdose may present with tachycardia, arrhythmias, palpitations, angina, hypotension, or hypertension.14 Overdose should be treated by reducing or stopping administration of isoprenaline & monitoring blood pressure, pulse, respiration, và ECG.14

In rats, the LD50 is 2221 mg/kg orally, 128 mg/kg intraperitoneally, & 600 mg/kg subcutaneously.15 In mice, the LD50 is 1260 orally & 450 mg/kg intraperitoneally.15

PathwaysPathwayCate91neg.comry
Isoprenaline action PathwayDrug action
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Interactions

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This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
AbaloparatideThe risk or severity of adverse effects can be increased when Isoprenaline is combined with Abaloparatide.AcebutololThe therapeutic efficacy of Isoprenaline can be decreased when used in combination with Acebutolol.AceclofenacThe risk or severity of hypertension can be increased when Isoprenaline is combined with Aceclofenac.AcemetacinThe risk or severity of hypertension can be increased when Isoprenaline is combined with Acemetacin.Acetylsalicylic acidThe risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with Isoprenaline.AclidiniumThe risk or severity of Tachycardia can be increased when Isoprenaline is combined with Aclidinium.AdenosineThe risk or severity of Tachycardia can be increased when Adenosine is combined with Isoprenaline.AlclofenacThe risk or severity of hypertension can be increased when Isoprenaline is combined with Alclofenac.AlfentanilThe risk or severity of hypertension can be increased when Alfentanil is combined with Isoprenaline.

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AlfuzosinThe therapeutic efficacy of Isoprenaline can be decreased when used in combination with Alfuzosin.