Salmeterol: An inhaled /β2-agonist with prolonged duration of action

Abstract

Salmeterol (Serevent) is an inhaled beta 2-receptor agonist with more than twelve hours' effect duration compared with 4-6 hours for the more short-acting substances bitolterol, fenoterol, salbutamol, and terbutaline. Salmeterol has been studied in several large-scale double-blind multicenter studies with up to one year's duration. More than 6,000 asthmatics have been treated with salmeterol during these controlled studies. All studies show salmeterol to have a significantly better and well-maintained bronchodilating effect with better asthma control, fewer asthma exacerbations, and a decreased need for rescue albuterol inhalations used on demand compared to the treatments in the control groups (200-400 micrograms albuterol q.i.d., inhaled albuterol given only p.r.n., terbutaline given regularly, or individually titrated slow-release theophylline). Salmeterol should be given b.i.d. and in combination with inhaled corticosteroids. Salmeterol seems especially effective in patients with nocturnal symptoms, exercise induced asthma, and in patients sensitive to inhaled irritants such as cold air. The patients should always have short-acting inhaled beta 2-agonists available for break-through attacks. Inhaled salmeterol in combination with inhaled steroids seems to give the best maintenance asthma control available by inhalation today.

Inhibitory effect of salmeterol on the respiratory burst of adherent human neutrophils

“…Although isoproterenol has been shown to inhibit the neutrophil respiratory burst [12,13], the widely used 2 -agonist salbutamol appears to be ineffective, at least using macrophages [14]. Moreover, the recently developed long-acting 2 -agonist salmeterol [15], possibly endowed with potential anti-inflammatory properties [16], was found to be incapable of inhibiting the respiratory burst in guinea pig eosinophils [17]. Therefore, we planned the present work to study the effects of salbutamol and salmeterol on the neutrophil respiratory burst and on the aforementioned PGE 2 -and PDE-IV-mediated regulation of this neutrophil response.…”

Inhaled dry-powder formoterol and salmeterol in asthmatic patients: onset of action, duration of effect and potency

“…Therefore, long-acting β 2 -agonists for inhalation, such as formoterol and salmeterol, have been developed. Both these drugs have been shown to cause bronchodilation for at least 12 h after single dose administration [1][2][3][4]. Twice daily treatment with inhaled formoterol or salmeterol has been shown to reduce diurnal airway calibre fluctuations and asthma symptoms [5][6][7], and inhaled long-acting β 2 -agonists are therefore important components in the therapy of patients with chronic asthma, who are not fully controlled with inhaled anti-inflammatory therapy [8].…”

Salmeterol versus formoterol in patients with moderately severe asthma: onset and duration of action

“…Both compounds, when administered as an aerosol by a metered-dose inhaler (MDI) or when inhaled as a powder, have the property of retaining a bronchodilatory effect for up to 12 h, which accounts for their use in patients with nocturnal asthma. Moreover, the long duration of action allows for a twice daily treatment frequency, for example, on arising in the morning and on going to bed at night, which could be helpful in promoting patient compliance [1][2][3][4][5][6].In vitro work and noncomparative studies on formoterol and salmeterol have shown evidence that there are small differences between the two inhaled drugs with regard to the speed of onset of a bronchodilatory effect, duration of action and dose-dependency of the duration of effect [6][7][8][9][10][11][12][13]. At the present time, a few comparative studies in patients with chronic obstructive pulmonary disease (COPD) have been published [14,15], however, a direct comparison of the profile of the bronchodilatory effect in asthma is still lacking.…”

“…In vitro work and noncomparative studies on formoterol and salmeterol have shown evidence that there are small differences between the two inhaled drugs with regard to the speed of onset of a bronchodilatory effect, duration of action and dose-dependency of the duration of effect [6][7][8][9][10][11][12][13]. At the present time, a few comparative studies in patients with chronic obstructive pulmonary disease (COPD) have been published [14,15], however, a direct comparison of the profile of the bronchodilatory effect in asthma is still lacking.…”