Roflumilast for the treatment of chronic obstructive pulmonary disease.
Chronic obstructive pulmonary disease (COPD) is a progressive disease of the airways that is triggered primarily by smoking. It manifests clinically with dyspnea, cough and sputum production, all of which become aggravated with disease progression. The only intervention that can halt the decline in lung function in COPD is smoking cessation--other interventions and therapeutic treatments can only slow down the progression of the disease. Pharmacologic treatment of stable COPD consists primarily of bronchodilators, which are used for relieving symptoms and reducing lung function decline, and corticosteroids, which are used for minimizing the associated inflammation. Methylxanthines are non-selective phosphodiesterase (PDE) inhibitors with bronchodilatory and anti-inflammatory effects; however, their use in COPD and other respiratory conditions is limited by their narrow therapeutic index and poor safety profile. Cilomilast and roflumilast are selective PDE4 inhibitors that are currently in pre-registration and phase III clinical trials, respectively, for the treatment of COPD (cilomilast and roflumilast) and asthma (roflumilast).
Antoniu
Sabina A
SA
Clinic of Pulmonary Disease, 30 Dr I Cihac Street, 700115 Iasi, Romania. sabinaantoniu@excite.com
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors / Q000378:metabolism; D000280:Administration, Inhalation; D000305:Adrenal Cortex Hormones / Q000008:administration & dosage / Q000627:therapeutic use; D000318:Adrenergic beta-Agonists / Q000008:administration & dosage / Q000627:therapeutic use; D000631:Aminopyridines / Q000008:administration & dosage / Q000627:therapeutic use*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D001549:Benzamides / Q000008:administration & dosage / Q000627:therapeutic use*; D001993:Bronchodilator Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D003521:Cyclopropanes / Q000008:administration & dosage / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical; D004359:Drug Therapy, Combination; D006801:Humans; D010726:Phosphodiesterase Inhibitors / Q000008:administration & dosage / Q000627:therapeutic use*; D029424:Pulmonary Disease, Chronic Obstructive / Q000188:drug therapy* / Q000378:metabolism; D016032:Randomized Controlled Trials as Topic
D000305:Adrenal Cortex Hormones; D000318:Adrenergic beta-Agonists; D000631:Aminopyridines; D000893:Anti-Inflammatory Agents; D001549:Benzamides; D001993:Bronchodilator Agents; D003521:Cyclopropanes; D010726:Phosphodiesterase Inhibitors; C424423:Roflumilast; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4