What I Have Learned About Salbutamol

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Salbutamol (also known as albuterol in USA) is one of the most famous short-acting β2 agonists. It has become first line treatment for asthma due to its effectiveness. I met this drug in a dispensing session in the first term and I think is a good example of what we have learnt so far. In this essay I will tell you what I know about this drug. Salbutamol is sold in its sulphate form and is marketed as a racemic product. According pharmaceutical chemistry this means that in it, it has 50% of the R enantiomer and 50% of the S enantiomer. However, only the R enantiomer is active at the β receptors. It is thought that the S enantiomer is inactive or causes adverse effects. Because of this, the pure R enantiomer was marketed – levalbuterol. β receptor agonists are used in the treatment of asthma and COPD (chronic obstructive pulmonary disease) to relax the muscles in the air passages in the lungs. Salbutamol is a selective β2 adrenergic agonist, although this selectivity is relative and dose-dependent. This means that the selectivity is lost at high concentration and thus causing side-effects. Albuterol has affinity to β 2 receptors and binds to them, causing a relaxation effect. β2 receptors are members of the adrenergic family of receptors and therefore its effects are caused by an interaction with G proteins. β

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