Latest research on Salbutamol

Salbutamol is a short-acting, selective beta2-adrenergic receptor agonist used in the treatment of asthma and COPD. It is 29 times more selective for beta2 receptors than beta1 receptors giving it higher specificity for pulmonary beta receptors versus beta1-adrenergic receptors located in the heart. Salbutamol is formulated as a racemic mixture of the R- and S-isomers. The R-isomer has 150 times greater affinity for the beta2-receptor than the S-isomer and the S-isomer has been associated with toxicity. This lead to the development of levalbuterol, the single R-isomer of salbutamol. However, the high cost of levalbuterol compared to salbutamol has deterred wide-spread use of this enantiomerically pure version of the drug. Salbutamol is generally used for acute episodes of bronchospasm caused by bronchial asthma, chronic bronchitis and other chronic bronchopulmonary disorders such as chronic obstructive pulmonary disorder (COPD). It is also used prophylactically for exercise-induced asthma.

Salbutamol side effects

The inclusion criteria, with reference to asthma diagnosis criterions of Global Initiative for Asthma including a history of variable respiratory symptoms and confirmed variable expiratory airflow limitation21 were: (1) age 10–12 years; (2) a diagnosis of asthma; (3) use of asthma medication (β2-agonists, corticosteroids, leukotriene antagonists, and/or combination formulation of long acting β2-agonists and corticosteroids) during the past month; (4) dyspnoea, chest tightness and/or wheezing during the past month; and (5) reversible airflow limitation measured during the past year as measured by a 10% increase in forced expiratory volume in 1 s (FEV1) 15 min after inhalation of 0.2 mg Salbutamol per 10 kg body mass (maximum 0.8 mg). [source, 2016]
FORM causes a fast bronchodilation that arises within a few minutes after inhalation, is dose-dependent and not significantly different from that caused by Salbutamol. [source, 2016]
However, in a recent randomized placebo-controlled trial, the effects of the β2-adrenergic receptor agonist, Albuterol, in acute lung injury did not increase ventilator-free days or reduce the rate of death before hospital discharge [19]. [source, 2016]
In Italy, however, the possibility of increased risks of maternal and neonatal transitory hypoglycaemia, maternal and fetal tachycardia, acute heart failure, pulmonary oedema and maternal death were listed in relation to Salbutamol and the guidelines stated that the manufacture advised to avoid during pregnancy unless the potential benefit outweighs the risk. [source, 2016]
As expected, β2-receptor agonist Salbutamol increased intracellular cAMP levels in J774 macrophages (Table 1). [source, 2016]
MKP-1 mRNA expression was increased by LPS and, interestingly, it was further enhanced by Salbutamol and by a cAMP analog 8-Br-cAMP (Fig 1). [source, 2016]
Salbutamol and another β2-receptor agonist terbutaline increased MKP-1 expression alone and in combination with LPS in J774 macrophages in a dose-dependent manner (Fig 2). [source, 2016]
As Salbutamol increased MKP-1 expression, we wanted to investigate whether MKP-1 could mediate the anti-inflammatory effects of Salbutamol, therefore we tested the effect of Salbutamol on the severity of carrageenan-induced paw inflammation in wild-type and MKP-1(-/-) mice. [source, 2016]
We found that Salbutamol increased MKP-1 expression, inhibited the phosphorylation of p38 MAPK and suppressed the production of TNF. [source, 2016]
We found that Salbutamol enhanced cAMP level in macrophages, and that cAMP analog 8-Br-cAMP enhanced MKP-1 expression as did β2-receptor agonists. cAMP has been reported to increase the expression of MKP-1 by activating protein kinase A-CREB pathway [15,42–45]. [source, 2016]