Mechanism of action Like all β adrenoreceptor agonists,<unk>  mimics the effect of epinephrine at β2 receptors in the lung, which causes the bronchi to relax and reduces their resistance to airflow.<unk>  is a nearly full β2 agonist, having 88% intrinsic activity compared to the gold standard isoprenaline/isoproterenol). Its half maximal effective concentration (EC50) is 0.1 nM. It has a higher in vitro selectivity for β2 receptors than the related drugs formoterol and salmeterol: 241-fold versus β1 and 2299-fold versus β3 adrenergic receptors. The high β2/β1 selectivity may account for the apparent lack of tachycardia in clinical trials, which is mediated by β1 receptors on the heart. Pharmacokinetics<unk>  is substantially metabolized by glucuronidation (UGT2B7, UGT1A1, UGT1A9) and O-demethylation (CYP2C8, CYP2C9). Pharmadynamics Once bound to a β2 receptor, an<unk>  molecule stays there for hours — its dissociation half-life is 17.8 hours —, which allows for once-a-day application of the drug like with indacaterol. Other related compounds generally have a shorter duration of action and have to be applied twice daily (e.g. formoterol, salmeterol). Still others (e. g. salbutamol/аlbuterol, fenoterol) have to be applied three or four times a day for continuous action, which can also be an advantage for patients who need to apply β2 agonists only occasionally, for example in an asthma attack.
Olodaterol
Indacaterol
Tenatoprazole
Lorcaserin
Azeloprazole
Lansoprazole
Tegaserod
Abiraterone acetate