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Bioavailability of inhaled compounds
Published in Anthony J. Hickey, Heidi M. Mansour, Inhalation Aerosols, 2019
The forced expiratory volume in one second (FEV1) is the maximal amount of air that a person can forcefully exhale in one second, and it is normally expressed as a percentage of normal (131). In asthmatic patients, FEV1 is measured frequently to evaluate the degree of obstruction caused by the asthma (132); thus, it has been used to evaluate the bioavailability of compounds such as revefenacin and ipratropium bromide. On the other hand, a few studies have correlated the concentration of salbutamol in urine with the inhaled dose (133,134). Furthermore, it has been shown that the amount of salbutamol determined in the urine collected cumulatively for 24 h after inhalation of salbutamol correlates with the total dose that the patient has inhaled (125).
Evaluating revefenacin as a therapeutic option for chronic obstructive pulmonary disease
Published in Expert Opinion on Pharmacotherapy, 2020
Sabina Antonela Antoniu, Ruxandra Rajnoveanu, Ruxandra Ulmeanu, Florin Mihaltan, Mihaela Grigore
The inhibitory potential of revefenacin was also tested ex vivo in human airways in two sets of experiments: static tissue bath and perfusion washout studies. In the former set, concentrations of revefenacin ranging from 1 to 1000 nmol/L inhibited carbachol-induced contraction of the smooth muscle cells in a dose-dependent manner (9–70%). Concentrations of revefenacin 30 nmol/L, ipratropium 10 nmol/L, and tiotropium 10 nmol/L were considered equivalent in their miorelaxing effect. In the second set of experiments, the sustained inhibitory effect of revefenacin was demonstrated with the persistence of at least 50% inhibitory effect (t1/2, inhibition half-life) on carbachol-induced contraction of smooth muscle cells of >10 h after revefenacin 10 nmol/L was added to the human tissues. Tiotropium produced a comparable inhibitory effect at a concentration of 10 nmol/L, whereas a similar concentration of ipratropium was associated with a t1/2 of 2.9 h [9].
Emerging muscarinic receptor antagonists for the treatment of asthma
Published in Expert Opinion on Emerging Drugs, 2020
Maria Gabriella Matera, Carmela Belardo, Michele Rinaldi, Barbara Rinaldi, Mario Cazzola
There is a considerable amount of research investigating the development of mAChR antagonists [6]. Revefenacin (TD-4208) is an interesting LAMA under investigation as a nebulized solution. It exhibits selective antagonism with high affinity at mAChRs and kinetic functional selectivity for M3 over M2 mAChRs [52]. Its pharmacokinetic profile is consistent with low systemic exposure. Revefenacin has been studied in patients with COPD, in which it induced a rapid and 24-hour lasting bronchodilation after once daily administration [53]. The effect of this LAMA administered using a standard jet nebulizer on bronchodilation was confirmed in Phase III studies in patients with moderate to severe COPD [54,55]. The FDA has approved revefenacin as maintenance treatment for COPD [56]. Currently, there are no ongoing trials identified for revefenacin in asthma although, as in COPD, it could be useful when patients have difficulty mastering inhaler techniques or present low baseline FEV1 that makes it difficult to generate flow with an inhaler [57].
Revefenacin for the treatment of chronic obstructive pulmonary disease
Published in Expert Review of Respiratory Medicine, 2020
Collin M Clark, David M Jacobs, Sanjay Sethi
Revefenacin is the first once-daily bronchodilator available for COPD patients who may require or prefer nebulized therapy. The three commonly prescribed inhalation devices for drug delivery in COPD – pMDIs, DPIs, and nebulizers have been shown to have similar efficacy in patients with COPD in systematic studies [33,34]. However, patients in research trials are in a highly regulated environment; therefore, errors in inhaler handling are minimized within these trials. This differs from clinical practice where real-word inhaler device handling errors impact close to 50% of COPD patients, is a major factor for ineffective management, and is linked to worse clinical outcomes and increases costs [35–38]. Therefore, it is of paramount importance for healthcare professionals to ensure proper device use in addition to choosing the appropriate prescribed medication. For instance, up to 68% of patients with respiratory diseases (including COPD) are not using their devices appropriately, and misuse is associated with a lack of device instruction by health-care professionals [39,40]. Differences between devices can be substantial and changing to an easier-to-use device may be necessary to improve medication adherence. Matching the device with patient-specific needs and education may be just as important as choosing the correct medication regimen in order to ultimately improve disease control and patient outcomes. This may be particularly important in the post-acute/long-term care setting, where underuse of long-acting bronchodilator therapy, including individualization of device selection, has been identified as an unmet need for COPD patients [41].