TY - JOUR
T1 - Bronchodilating drugs for chronic obstructive pulmonary disease: current status and future trends
AU - Montuschi, Paolo
AU - Ciabattoni, Giovanni
PY - 2015
Y1 - 2015
N2 - Inhaled bronchodilators, including long-acting muscarinic receptor antagonists (LAMA) and long-acting β2-adrenoreceptor agonists (LABA), are the mainstay of pharmacological treatment of stable chronic obstructive pulmonary disease (COPD). Among approved LAMA, tiotropium bromide, glycopyrronium bromide, and umeclidinium bromide are administered once daily, whereas aclidinium bromide is administered every 12 h. New LAMA are under development for COPD. Among the approved LABA, indacaterol has a 24 h duration of action, whereas salmeterol and formoterol require twice-daily administration. New once-daily LABA, including vilanterol, olodaterol, milveterol, carmoterol, and abediterol, are in development. LAMA/LABA fixed dose combinations (FDCs) provide the convenience of two bronchodilators with different mechanism of action in a single inhaler. Indacaterol/glycopyrronium, umeclidinium/vilanterol, and olodaterol/tiotropium FDCs have been approved or are under approval and are likely to become a standard pharmacological strategy for COPD. Inhaled dual-pharmacology compounds, combining muscarinic antagonism and β2-agonism (MABA) in a single molecule, potentially provide additive or synergistic bronchodilation over either inhaled antimuscarinic or β2-agonist monotherapy
AB - Inhaled bronchodilators, including long-acting muscarinic receptor antagonists (LAMA) and long-acting β2-adrenoreceptor agonists (LABA), are the mainstay of pharmacological treatment of stable chronic obstructive pulmonary disease (COPD). Among approved LAMA, tiotropium bromide, glycopyrronium bromide, and umeclidinium bromide are administered once daily, whereas aclidinium bromide is administered every 12 h. New LAMA are under development for COPD. Among the approved LABA, indacaterol has a 24 h duration of action, whereas salmeterol and formoterol require twice-daily administration. New once-daily LABA, including vilanterol, olodaterol, milveterol, carmoterol, and abediterol, are in development. LAMA/LABA fixed dose combinations (FDCs) provide the convenience of two bronchodilators with different mechanism of action in a single inhaler. Indacaterol/glycopyrronium, umeclidinium/vilanterol, and olodaterol/tiotropium FDCs have been approved or are under approval and are likely to become a standard pharmacological strategy for COPD. Inhaled dual-pharmacology compounds, combining muscarinic antagonism and β2-agonism (MABA) in a single molecule, potentially provide additive or synergistic bronchodilation over either inhaled antimuscarinic or β2-agonist monotherapy
KW - Antagonisti recettoriali muscarinici inalatori a lunga durata di azione
KW - Beta2-agonisti inalatori a lunga durata di azione
KW - Bronchodilating drugs
KW - Broncopneumopatia cronica ostruttiva
KW - Chronic obstructive pulmonary disease
KW - Farmaci broncodilatatori
KW - Inhaled long-acting beta2 agpnists
KW - Inhaled long-acting muscarinic receptor antagonists
KW - Antagonisti recettoriali muscarinici inalatori a lunga durata di azione
KW - Beta2-agonisti inalatori a lunga durata di azione
KW - Bronchodilating drugs
KW - Broncopneumopatia cronica ostruttiva
KW - Chronic obstructive pulmonary disease
KW - Farmaci broncodilatatori
KW - Inhaled long-acting beta2 agpnists
KW - Inhaled long-acting muscarinic receptor antagonists
UR - http://hdl.handle.net/10807/67055
U2 - 10.1021/jm5013227
DO - 10.1021/jm5013227
M3 - Article
SN - 0022-2623
VL - 58
SP - 4131
EP - 4164
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
ER -