Tiotropium: an inhaled anticholinergic for chronic obstructive pulmonary disease.
OBJECTIVE
The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, dosage and administration, and formulary considerations of tiotropium are discussed.


CONCLUSIONS
Tiotropium, a long-acting inhaled anticholinergic, recently received approval from the Food and Drug Administration for the management of chronic obstructive pulmonary disease (COPD). In patients with COPD, increased parasympathetic nervous system activity leads to bronchoconstriction and mucus secretion. Tiotropium induces relaxation of the airway smooth muscle, as does ipratropium, but differs in receptor association and dissociation rates, allowing for once-daily administration. After inhalation, tiotropium reaches maximal plasma concentrations within five minutes, but clinical improvements in forced expiratory volume in one second (FEV(1)) are maintained over 24 hours. Clinical trials of tiotropium with placebo, ipratropium, and salmeterol have demonstrated the efficacy of tiotropium in improving FEV(1) and forced vital capacity values and health-related quality of life. The most commonly observed adverse effect is dry mouth. No increase in adverse effects was observed when tiotropium was administered concomitantly with other drugs for COPD, including sympathomimetic bronchodilators and oral and inhaled corticosteroids. The combination of tiotropium and other anticholinergics has not been studied and is not recommended. The recommended dosage of tiotropium is the inhalation of an 18-mug capsule with a HandiHaler breath-actuated inhalation device once daily.


CONCLUSIONS
Tiotropium appears to be at least as effective as currently available alternatives in the treatment of patients with COPD who require daily bronchodilator treatment. Its simplified dosing and tolerable adverse-effect profile can potentially lead to enhanced patient compliance.
Olin
Jacqueline L
JL
Ernest Mario School of Pharmacy, Department of Pharmacy Practice and Administration, Rutgers University, Piscataway, NJ, USA. jlolin@rci.rutgers.edu
D000280:Administration, Inhalation; D018680:Cholinergic Antagonists / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use; D006801:Humans; D029424:Pulmonary Disease, Chronic Obstructive / Q000188:drug therapy* / Q000453:epidemiology / Q000503:physiopathology; D012602:Scopolamine Derivatives / Q000191:economics / Q000494:pharmacology / Q000627:therapeutic use*; D000069447:Tiotropium Bromide
D018680:Cholinergic Antagonists; D003692:Delayed-Action Preparations; D012602:Scopolamine Derivatives; D000069447:Tiotropium Bromide