ReviewEffects of S-salbutamol on Human Isolated Bronchus
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Salmeterol undergoes enantioselective bronchopulmonary distribution with receptor localisation a likely determinant of duration of action
2018, Journal of Pharmaceutical and Biomedical AnalysisCitation Excerpt :Rare but serious, and as yet unexplained, paradoxical asthma exacerbations have been associated with LABAs, and chronic use is associated with increased bronchial hyperresponsiveness (BHR) and loss of bronchoprotection [4]. While little is known about the adverse pharmacodynamics of (S)-salmeterol, there are convincing in vitro studies showing that (S)- enantiomers of short acting beta2-agonists are associated with a range of adverse airways effects including enhanced contraction of isolated human bronchial tissue [5] and increased airway responsiveness [6]. Rac-salmeterol does appear to be enantioselective in terms of pharmacodynamics, but interestingly not to the same extent as other beta2-agonists [7].
The influence of propofol, remifentanil and lidocaine on the tone of human bronchial smooth muscle
2013, Pulmonary Pharmacology and TherapeuticsCitation Excerpt :In further experiments, the isolated bronchi were pre-treated for 45 min with the selective inhibitor of inducible nitric oxide (NO) synthase (iNOS), aminoguanidine (100 μmol) and then treated with propofol [23]. Moreover, the EFS responsiveness in the presence of remifentanil was tested in desensitized tissues [15,16]. The analysis of the potential synergism/antagonism between propofol, lidocaine and remifentanil was measured by applying the Bliss Independence (BI) theory.
Levalbuterol versus albuterol for acute asthma: A systematic review and meta-analysis
2013, Pulmonary Pharmacology and TherapeuticsCitation Excerpt :Levalbuterol has approximately 100 times greater affinity for the beta2-adrenergic receptor than (S)-albuterol [13]. Till recently, the (S)-albuterol was considered inert part of racemic albuterol but now in vitro and in vivo experimental models have shown that (S)-albuterol results in immune cell proliferation, cytokine production and increases intracellular calcium in airway smooth muscle cells leading to bronchoconstriction [14–17]. Further, (S)-albuterol persists longer in plasma and lung tissue of patients because of its slower metabolism and elimination as compared to levalbuterol [18,19].
Long-term safety study of levalbuterol administered via metered-dose inhaler in patients with asthma
2007, Annals of Allergy, Asthma and ImmunologyEffects of (R,R)- and (R,R/S,S)-Formoterol on Airway Relaxation and Contraction in an Experimental Rat Model
2007, Current Therapeutic Research - Clinical and Experimental16 Drugs acting on the respiratory tract
2007, Side Effects of Drugs AnnualCitation Excerpt :Since the most effective dose of racemic salbutamol was not given, the equipotent dose ratio (racemic salbutamol/levosalbutamol) might be higher than has previously been estimated. S salbutamol plasma concentrations correlated negatively with FEV1, which may be ascribed to opposite actions of the two isomers, as has been suggested in preclinical studies (51E–53E). In contrast, the change in peak expiratory flow after the administration of home inhaled or nebulized levosalbutamol versus racemic salbutamol before admission to the emergency department was not different in 298 patients with acute bronchospastic or obstructive pulmonary conditions in another prospective, open study (54c).
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