OBJECTIVETo observe the therapeutic effect of tiotropium bromide powder inhalation on stable bronchiectasis.

METHODSTwenty-two patients with stable bronchiectasis received inhalation of totropium bromide powder at the daily dose of 18 microg, and on days 1 and 28, the patients were examined for forced expiratory volume in one second (FEVl), predicted value [FEVl(%)], forced expiratory volume (FEV), and FEVl/FVC. The symptom score and BODE index were also recorded.

RESULTSAfter 1 month of inhalation therapy, the FEV1% of the patients showed a moderate increase but the increment was not statistically significant (t=-1.875, P>0.05); the symptom score and BODE index decreased significantly after the therapy (t=7.091, P<0.001; t=2.982, P<0.05).

CONCLUSIONLong-term inhalation of tiotropium bromide powder can improve the clinical symptoms and BODE index and enhance the exercise tolerance and quality of life of the patients with bronchiectasis.

Administration, Inhalation ; Adult ; Aged ; Bronchiectasis ; drug therapy ; Female ; Forced Expiratory Volume ; Humans ; Male ; Middle Aged ; Powders ; Receptor, Muscarinic M3 ; antagonists & inhibitors ; Scopolamine Derivatives ; administration & dosage ; Tiotropium Bromide

AIMTo identify anisodine and its metabolites in rat plasma after ingestion of anisodine by combining liquid chromatography and tandem mass spectrometry (LC-MS(n)).

METHODSPlasma samples from rats after a single orally administration of 20 mg anisodine were added with methanol to precipitate protein. Then, it was analyzed by LC-MS(n). Identification and structural elucidation of the metabolites were performed by comparing their changes in molecular masses, retention-times and full scan MS(n) spectra with those of the parent drug and blank plasma.

RESULTSThe results revealed that the parent drug and its four metabolites (norscopine, scopine, hydroxyanisodine, N-oxide anisodine) existed in rat plasma.

CONCLUSIONThis method is sensitive, rapid, simple, and it is suitable for the rapid identification of drug and its metabolits.

Administration, Oral ; Animals ; Chromatography, Liquid ; methods ; Plants, Medicinal ; chemistry ; Rats ; Rats, Wistar ; Scopolamine Derivatives ; isolation & purification ; metabolism ; Sensitivity and Specificity ; Solanaceae ; chemistry ; Tandem Mass Spectrometry ; methods

Because additive effects of inhaled corticosteroids and long-acting anticholinergics are unclear, we undertook this study to compare the efficacy of tiotropium alone and tiotropium plus budesonide in patients with chronic obstructive pulmonary disease. The study subjects were randomized to receive either tiotropium 18 microgram once daily with or without budesonide 200 microgram twice daily for 6 weeks. The efficacy variables were changes in trough forced expiratory volume in one second (FEV1), St. George's Respiratory Questionnaire (SGRQ), 6-minute walk distance (6MWD), and use of rescue medication. One hundred patients were randomized and 81 completed the study. The mean age was 64.0 yr, and the mean FEV1 was 39.7% predicted. Compared with tiotropium alone (N=40), the tiotropium/budesonide combination (N=41) was related to an improvement in the SGRQ total score (tiotropium -2.8 units and tiotropium/budesonide -5.6 units, p=0.003). 6MWD was improved by 13.5 m in the tiotropium group and by 22.5 m in the tiotropium/budesonide group (p=0.031). Changes in trough FEV1 and the use of rescue medication were similar between two groups. In conclusion, compared with tiotropium alone, the tiotropium/ budesonide combination was related to an improved health-related quality of life. These data support that low-dose budesonide may enhance the efficacy of tiotropium.
Aged ; Bronchodilator Agents/*administration & dosage ; Budesonide/*administration & dosage ; Exercise ; Female ; Humans ; Male ; Middle Aged ; Models, Statistical ; Pulmonary Disease, Chronic Obstructive/*drug therapy ; Quality of Life ; Questionnaires ; Scopolamine Derivatives/*administration & dosage ; Spirometry/methods ; Treatment Outcome

BACKGROUNDA pharmacokinetic study in an Asian population showed that tiotropium 5 µg via Respimat leads to the same plasma levels compared to 18 µg via HandiHaler. The objective of the trial was to compare the efficacy and safety of longterm treatment (1 year) with tiotropium bromide (5 µg) via Respimat® with placebo in patients with chronic obstructive pulmonary disease (COPD).

METHODSA total of 3991 patients were randomized in this double-blind, placebo controlled, parallel group study, while in China 338 patients (309 males, 29 females) received either tiotropium bromide (n = 167) or placebo (n = 171). Tiotropium bromide solution or matching placebo was delivered via Respimat® at a dosage of 5 µg (2×2.5 µg/puff) once daily for 48 weeks. Co-primary endpoints were trough forced expiratory volume in one second (FEV1) and the time to first exacerbation.

RESULTSStatistically significant improvements in trough FEV1 and trough forced vital capacity (FVC) in the tiotropium group were achieved at weeks 4, 24, and 48 compared with those in the placebo group. A statistically significant difference (P = 0.0027) in favour of tiotropium was also observed for the time to first exacerbation. The total numbers of exacerbations during treatment were 90 and 128 in the tiotropium and placebo groups, respectively, with a rate ratio of 0.69 (P = 0.0164). The difference between the treatment groups in the adjusted mean changes from baseline of St. George Respiratory Questionnaire (SGRQ) total score was -3.9 (95% CI: -7.5, -0.2) and was of statistical significance (P = 0.0367). The incidences of serious adverse events (SAEs) in the tiotropium and placebo groups were 16.2% and 17.0%, respectively. Seven deaths occurred whilst patients were on treatment, four in the tiotropium group and three in the placebo group, all of which were assessed as non-related study drugs by the investigators.

CONCLUSIONSTiotropium significantly improved lung function and quality of life, delayed the time to first exacerbation, reduced the number of exacerbations. Overall, tiotropium was well tolerated.

Administration, Inhalation ; Aged ; Bronchodilator Agents ; adverse effects ; therapeutic use ; Cholinergic Antagonists ; adverse effects ; therapeutic use ; Double-Blind Method ; Female ; Forced Expiratory Volume ; Humans ; Male ; Middle Aged ; Pulmonary Disease, Chronic Obstructive ; drug therapy ; physiopathology ; Scopolamine Derivatives ; adverse effects ; therapeutic use ; Tiotropium Bromide