Pharmacodynamic and pharmacokinetic assessment of fluticasone furoate plus vilanterol for the treatment of asthma

被引:7
作者
Calzetta, Luigino [1 ]
Rinaldi, Barbara [2 ]
Cazzola, Mario [1 ]
Matera, Maria Gabriella [2 ]
机构
[1] Univ Roma Tor Vergata, Dept Syst Med, Unit Resp Clin Pharmacol, Rome, Italy
[2] Univ Naples 2, Ctr Excellence Cardiovasc Dis, Dept Expt Med, Sect Pharmacol L Donatelli, Naples, Italy
关键词
Asthma; fluticasone furoate; pharmacodynamics; pharmacokinetics; vilanterol trifenatate; ACTING BETA(2)-ADRENOCEPTOR AGONIST; INHALED CORTICOSTEROIDS; PERSISTENT ASTHMA; BETA-AGONIST; FUROATE/VILANTEROL COMBINATION; INTRANASAL CORTICOSTEROIDS; CLINICAL-PHARMACOLOGY; SEVERE EXACERBATIONS; DOUBLE-BLIND; IN-VITRO;
D O I
10.1080/17425255.2016.1192125
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Introduction. The pharmacokinetic (PK) and pharmacodynamic (PD) effects of long-acting beta(2)-agonists and mostly inhaled corticosteroids (ICSs) shape the efficacy and safety of these agents in the treatment of asthma. In fact, the PK and PD characteristics of the drug largely determine the degree of pulmonary targeting Areas covered. In this review, we summarize the PK and PD properties of inhaled fluticasone furoate (FF) and vilanterol trifenatate (VI) and their fixed-dose combination (FDC) for the treatment of asthma Expert opinion. It is difficult to interpret the data that we have described because the preclinical and clinical development of FF/VI FDC was not really based on solid information on quantitative PK/PD approach. Unfortunately, for both FF and VI we only know concentrations in systemic blood, a compartment that is downstream of both target and non-target respiratory tissue. This lack of information does not allow us to understand the temporal relationship between the delivered dose and the drug concentration at the sites of action within the lungs. In addition, all studies performed with FF and VI did not address the fundamental issue that asthma can significantly alter lung deposition, absorption and also clearance of inhaled medicines.
引用
收藏
页码:813 / 822
页数:10
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