Pharmacokinetic and Pharmacodynamic Interaction of Carmoterol and Budesonide in Asthmatic Patients.

Poli, Gianluigi; Devolder, A.; Backer, W. De; Acerbi, Daniela; Nandeuil, A; Decker, M.; Ramael, Steven

doi:10.1164/ajrccm-conference.2009.179.1_meetingabstracts.a2789

Cited by 2 publications

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“…The finding suggests that carmoterol/budesonide, by optimizing each other's beneficial pharmacological potential, may represent a new fixed combination in asthma. In effect, in mild or moderate asthmatic patients, the systemic exposure to carmoterol 2 µg and budesonide 400 µg was not increased with the combination in comparison with each component administered alone (Poli et al ., 2009). Moreover, a prolonged bronchodilatation was observed with carmoterol/budesonide combination (Poli et al ., 2009).…”

Section: Future Directionmentioning

confidence: 99%

“…In effect, in mild or moderate asthmatic patients, the systemic exposure to carmoterol 2 µg and budesonide 400 µg was not increased with the combination in comparison with each component administered alone (Poli et al ., 2009). Moreover, a prolonged bronchodilatation was observed with carmoterol/budesonide combination (Poli et al ., 2009). The fixed combination carmoterol/budesonide formulated as HFA 134a pMDI (Chiesi Modulite™ HFA technology) administered once a day in asthmatic patients maintained the bronchodilator effect over 24 h and was as effective as formoterol/budesonide Turbuhaler twice a day in patients with moderate or severe persistent asthma (Woodcock et al ., 2009).…”

Section: Future Directionmentioning

confidence: 99%

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β₂‐adrenoceptor agonists: current and future direction

Cazzola

Calzetta

Matera

2011

British J Pharmacology

150

118

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Despite the passionate debate over the use of b2-adrenoceptor agonists in the treatment of airway disorders, these agents are still central in the symptomatic management of asthma and COPD. A variety of b2-adrenoceptor agonists with long half-lives, also called ultra long-acting b2-adrenoceptor agonists (ultra-LABAs; indacaterol, olodaterol, vilanterol, carmoterol, LAS100977 and PF-610355) are currently under development with the hopes of achieving once-daily dosing. It is likely that the oncedaily dosing of a bronchodilator would be a significant convenience and probably a compliance-enhancing advantage, leading to improved overall clinical outcomes. As combination therapy with an inhaled corticosteroid (ICS) and a LABA is important for treating patients suffering from asthma, and a combination with an inhaled long-acting antimuscarinic agent (LAMA) is important for treating COPD patients whose conditions are not sufficiently controlled by monotherapy with a b2-adrenoceptor agonist, some novel once-daily combinations of LABAs and ICSs or LAMAs are under development. LINKED ARTICLESThis article is part of a themed issue on Respiratory Pharmacology. To view the other articles in this issue visit http://dx.doi.org/10.1111/bph.2011.163.issue-1 AbbreviationsACh, acetylcholine; cAMP, cyclic adenosine monophosphate; COPD, chronic obstructive pulmonary disease; EC50, median effective concentration required to induce a 50% effect; ECG, electrocardiogram; EFS, electric field stimulation; Emax, the maximum possible effect for the agonist; FDA, Food and Drug Administration; FEV1, Forced Expiratory Volume in One Second; HFA, hydrofluoroalkane; ICS, inhaled corticosteroid; IFN, interferon; IL, interleukin; LABA, long-acting b2-adrenoceptor agonist; LAMA, long-acting antimuscarinic agent; mL, milliliter; pEC50, negative logarithm of EC50; PK, pharmacokinetics; QTc, corrected QT interval Current directionb2-adrenoceptor agonists, mainly long-acting b2-adrenoceptor agonists (LABAs) such as formoterol and salmeterol, are an important pharmacological approach to induce bronchodilation in patients suffering from chronic obstructive pulmonary disease (COPD) (Celli and MacNee, 2004;Rabe et al., 2007) and asthma (National Asthma Education and Prevention Program, 2007;Bateman et al., 2008a), although controversy has reigned over their regular use prescribed as monotherapy, at least in the treatment of asthma (Wijesinghe et al., 2008). In effect, with chronic or high-dose exposure, b2-adrenoceptor agonists demonstrate proinflammatory effects. In vitro, they can enhance the Th2 inflammatory pathway by inhibiting interleukin (IL)-12 and interferon (IFN)-g (Panina-Bordignon et al., 1997;Agarwal and Marshall, 2000). In vivo, pretreatment with b2-adrenoceptor agonists increases the severity of the late asthmatic reaction (Lai et al., 1989), continuous treatment is associated with an increase in sputum eosinophils, notably when the patient is not taking concomitant inhaled corticosteroids (ICSs) (Aldridge et al., 2000;Lazarus et al., 2001)...

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Section: Future Directionmentioning

confidence: 99%

Section: Future Directionmentioning

confidence: 99%

β₂‐adrenoceptor agonists: current and future direction

Cazzola

Calzetta

Matera

2011

British J Pharmacology

150

118

View full text Add to dashboard Cite

show abstract

“…Intriguingly, carmoterol/budesonide was 2-fold more effective than the formoterol/budesonide combination, which suggests that carmoterol/budesonide, by optimizing each other's beneficial pharmacological potential, may represent a new fixed combination in asthma. In effect, in patients with mild or moderate asthma, the systemic exposure to 2 g of carmoterol and 400 g of budesonide was not increased with the combination compared with each component administered alone (Poli et al, 2009). However, a prolonged bronchodilation was observed with carmoterol/budesonide combination (Poli et al, 2009).…”

Section: Novel Combinations Of Long-acting ␤ 2 -Adrenergic Receptor Amentioning

confidence: 95%

“…In effect, in patients with mild or moderate asthma, the systemic exposure to 2 g of carmoterol and 400 g of budesonide was not increased with the combination compared with each component administered alone (Poli et al, 2009). However, a prolonged bronchodilation was observed with carmoterol/budesonide combination (Poli et al, 2009). The fixed combination carmoterol/budesonide formulated as HFA 134a pressurized MDI (Chiesi Modulite HFA technology) administered once a day to patients with moderate or severe persistent asthma maintained the bronchodilator effect over 24 h and was as effective as twice-daily formoterol/budesonide Turbuhaler (Woodcock et al, 2009).…”

Section: Novel Combinations Of Long-acting ␤ 2 -Adrenergic Receptor Amentioning

confidence: 95%