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Salbutamol

Molecular structure of salbutamol

Salbutamol

(R,S)-2-(1,1-dimethylethyl)amino-
1-(4-hydroxy-3-hydroxymethylphenyl)ethanol

Empirical formula C13H21N1O3
Molecular weight 239.3
Bioavailability (Oral) "well absorbed"
Metabolism hepatic
Elimination half life (Oral/inhaled) 2.7-5 hours
Excretion renal
Pregnancy category A (Australia)

Salbutamol (INN) or albuterol (USAN) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and COPD. The name Albuterol comes from Salbutamol aerosol.

Salbutamol sulfate is usually given by the inhaled route for direct effect on bronchial smooth muscle. This is usually achieved through a metered-dose inhaler (MDI) or nebuliser; but other delivery devices marketed for salbutamol sulfate include the Rotahaler, Easyhaler, Diskhaler, and Autohaler. Salbutamol can also be given orally (Volmax®) or intravenously.

Salbutamol became available in the United Kingdom in 1969 and in the United States in 1980 under the brand name Ventolin.

Contents

Clinical use

Salbutamol is specifically indicated in the following conditions:

  • acute asthma
  • symptom relief during maintenance therapy of asthma and other conditions with reversible airways obstruction (including COPD)
  • protection against exercise-induced asthma
  • certain conditions involving hyperkalemia

As a β2-agonist, salbutamol also finds use in obstetrics. Intravenous salbutamol can be used as a tocolytic to relax the uterine smooth muscle to delay premature labour. Whilst preferred over agents such as atosiban and ritodrine, its role has largely been replaced by the calcium-channel blocker nifedipine which is more effective, better tolerated and orally administered. (Rossi, 2004)

Mode of action

As with other β2-adrenergic receptor agonists, salbutamol binds to β2-adrenergic receptors with a higher affinity than β1-receptors. In the airways, activation of β2-receptors results in relaxation of bronchial smooth muscle. resulting in a widening of the airway (bronchodilation). Inhaled salbutamol sulfate has a rapid onset of action, providing relief within 5-15 minutes of administration.

In tocolysis, the activation of β2-receptors results in relaxation of uterine smooth muscle, thus delaying labour.

Adverse effects

Whilst salbutamol is well-tolerated, particularly when compared with previous therapies such as theophylline, like all medications there exists the potential for adverse drug reactions to occur - especially when in high doses, or when taken orally or intravenously.

Common adverse effects include: tremor, palpitations and headache. (Rossi, 2004)

Infrequent adverse effects include: tachycardia, muscle cramps, agitation, hypokalemia, hyperactivity in children, and insomnia. (Rossi, 2004)

Precautions, Specific Considerations & Advice

Pregnancy: Safe to use
Breastfeeding: Safe to use

Salbutamol is most commonly advised to be used in acute attacks only. If a patient uses it regularly to control their bronchospasm, please consult your personal health professional for advice.

Other brand names

Salbutamol is sold under the brand names Airomir, Asmol, Buventol, Proventil, Sultanol, Ventolin and Volmax.

References


The content of this page is retrieved from http://en.wikipedia.org/wiki/Salbutamol under GFDL