Isoprenaline
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Isoprenaline
Systematic (IUPAC) name
4-[1-hydroxy-2-(1-methylethylamino) 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
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	inhaled 80-120μg

Isoprenaline (INN) or isoproterenol (USAN, trade names Medihaler-Iso and Isuprel) is a sympathomimetic beta adrenergic agonist medication.

It is structurally similar to epinephrine (adrenaline) but acts for the most part on beta receptors.

Uses

It is used as an inhaled aerosol to treat asthma. Although it activates all beta adrenergic receptors, it works in a similar fashion to the more selective beta2-adrenergic receptor 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, in conjunction with overdrive pacing and magnesium.

Adipose tissue also has β-receptors that can be activated by isoproterenol. Once activated, adipocytes begin breaking down the fat stored inside them. This has caused isoproterenol to be used off-label in mesotherapy for body contouring and to help decrease fat. Two studies showed that it can cause a decrease in thigh size. ^[1]

Pharmacology

Isoproterenol 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 isoproterenol is approximately two hours.

Isoproterenol's effects on the cardiovascular system relate to its actions on cardiac β₁ receptors and β₂ receptors on skeletal muscle arterioles. Isoproterenol 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 isoproterenol are also related to the drug's cardiovascular effects. Isoproterenol can produce an elevated heart rate (tachycardia), which predisposes patients to cardiac dysrhythmias.

Other side effects include: nervousness, insomnia, restlessness, and headaches.^[1]

Warnings and Contraindications

Isoproterenol should not be administered to patients with myocardial ischaemia.

References

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