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Isoprenaline
Systematic (IUPAC) name
4-[1-hydroxy-2-(isopropylamino)ethyl]benzene-1,2-diol
Identifiers
CAS number 7683-59-2
ATC code C01CA02 R03AB02
PubChem 3779
DrugBank APRD00182
Chemical data
Formula C11H17NO3 
Mol. mass 211.258 g/mol
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes inhaled 80-120μg
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Isoprenaline (INN) or isoproterenol (USAN, trade names Medihaler-Iso and Isuprel) is a sympathomimetic beta adrenergic agonist medication.

It is structurally similar to adrenaline but acts selectively on beta receptors, activating β1 and β2 receptors equally.[1]

Contents

Uses

Its primary use is for bradycardia or heart block. By activating β1-receptors on the heart, it induces positive chronotropic, dromotropic, and inotropic effects.[1]

It can be used as an inhaled aerosol to treat asthma, although this is currently a rare treatment.[1] Although it activates all beta adrenergic receptors, it works in a similar fashion to the more selective β2-adrenergic agonists e.g. salbutamol, by relaxing the airways to increase airflow.

It is also supplied in ampules under the brand name Isuprel for injection and in sublingual pill form for treatment of asthma, chronic bronchitis and emphysema.

Used with caution, it can also be used to treat torsades de pointes by acquired defect, in conjunction with overdrive pacing and magnesium.

Pharmacology

Isoprenaline is a β1- and β2-adrenoceptor agonist which was commonly used to treat asthma before the more widespread use of salbutamol, which has more selective effects on the airways. Its route of administration is either intravenous, oral, intranasal, subcutaneous, or intramuscular, depending on use. The plasma half-life for isoprenaline is approximately two hours.

Isoprenaline's effects on the cardiovascular system relate to its actions on cardiac β1 receptors and β2 receptors on skeletal muscle arterioles. Isoprenaline has positive inotropic and chronotropic effects on the heart. In skeletal muscle arterioles it produces vasodilatation. Its inotropic and chronotropic effects elevate systolic blood pressure, while its vasodilatory effects tend to lower diastolic blood pressure.

The adverse effects of isoprenaline are also related to the drug's cardiovascular effects. Isoprenaline can produce an elevated heart rate (tachycardia), which predisposes patients to cardiac dysrhythmias.

Warnings and contraindications

Isoprenaline should not be administered to patients with myocardial ischaemia.

References

  1. ^ a b c Shen, Howard (2008). Illustrated Pharmacology Memory Cards: PharMnemonics. Minireview. p. 5. ISBN 1-59541-101-1. 







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