BACKGROUND: Salmeterol, a new beta2-adrenergic receptor agonist is a long-acting bronchodilator and benefits patients -with asthma who have nocturnal symptoms. We wished to assess the efficacy of inhaled salmeterol (50 microgram bid) compared to inhaled salbutamol (200 microgram qid) for the treatment of bronchial asthma, particular. ly nocturnal asthma. METHOD: We randomly assigned 35 patents (25 female and 0 male patients, 15 to 50 years old) to one of two treatment groups one group received 50 microgram of salmeterol twice daily and another did 200 microgram salbutamol four times per day. And this study was performed as an open-label and the 6 weeks inhalation period. RESULTS: Analysis of symptom scare; Day and night time symptom score showed significant difference between salmeterol and salbutamol Group (p<0.05). Number of days for additional bronchodilator requirements The number of days and puffs for additional bronchodilator were lower in the salbutamol group in either day and night time (p<0.05). Pulmonary function test; FEV1 showed significant increase in salbutamol group compared to salbutamol group after 2 and 4 weeks inhalation period. Adverse effects, We found no evidence of tolerance to the bronchodilating effects of salmeterol, and adverse reactions to all the treatments were infrequent and mild. CONCLUSION: For the management of bronchial asthma, salmeterol given twice daily is superior to salbutamol given four times daily.
Albuterol* ; Asthma* ; Female ; Humans ; Inhalation* ; Male ; Respiratory Function Tests ; Salmeterol Xinafoate

Salmeterol is a long acting, highly selective, beta2-adrenergic agonist. It prevents asthma symptoms in patients with mild or moderate disease and improves nocturnal asthma and sleep quality. We evaluated the bronchodilator and bronchoprotective effect and duration of action of inhaled salmeterol in patients wlth asthma. We compared the bronchodilator and bronchoprotective effects of salmeterol with salbutamol in 34 patients with asthma. Diagnosis of asthma was confirmed with methacholine challenge test or airway reversibility test. We performed the symptom index questionnaire, peak expiratory flow rate, pulmonary function test and methacholine challenge test. Symptom scores were more improved with salmeterol treatment than salbutamol treatment. After salmeterol inhalation, mean FEV1 increased from 1.95L(pre-treatment) to 2.04L(early stage in the treatment), 2.06L(late stage), 2.03L(follow up). There was no difference in FEV1 between early stage and late stage after salmeterol treatment. With salmeterol, there was a significant increases in PC30 on methacholine challenge test ( PC20 4.96 : 16.42). Salmeterol is a potent, long-acting bronchodilator, with a slower onset and longer duration of bronchodilation than salbutamol. It also has bronchoprotective effect and shows low incidence of adverse effects.
Albuterol ; Asthma ; Diagnosis ; Humans ; Incidence ; Inhalation ; Methacholine Chloride ; Peak Expiratory Flow Rate ; Respiratory Function Tests ; Salmeterol Xinafoate ; Surveys and Questionnaires

PURPOSE: Asthma affects approximately 30 million patients in China; however, tiotropium data for Chinese patients is limited. This study aimed to assess the efficacy and safety of tiotropium in Chinese patients with moderate symptomatic asthma. METHODS: A post hoc subgroup analysis was conducted on 430 Chinese patients pooled from two 24-week, replicate phase 3 trials (NCT01172808 and NCT01172821), in which they received once-daily tiotropium 2.5 µg (Tio R2.5) or 5 µg (Tio R5) (n = 106 or 109, respectively), twice-daily salmeterol 50 µg (Sal 50) (n = 110), or placebo (n = 105), while maintaining inhaled corticosteroids (ICS). The co-primary endpoints assessed in week 24 were forced expiratory volume in 1 second (FEV1) peak0–3h response, trough FEV1 response, and responder rate as assessed using the Asthma Control Questionnaire (ACQ). RESULTS: For both FEV1 peak0–3h responses and trough FEV1 responses, the mean treatment differences were greater for Tio R2.5, Tio R5, and Sal 50 compared with placebo at 0.249 L, 0.234 L, and 0.284 L, and 0.172 L, 0.180 L, and 0.164 L, respectively (P< 0.001). The ACQ responder rate in placebo, Tio R2.5, Tio R5, and Sal 50 was 58.7%, 62.3%, 59.3%, and 69.1%, respectively. Furthermore, 11 (2.6%) of 430 patients had serious adverse events (Tio R5, n = 4; Tio R2.5, n = 1; Sal 50, n = 1; and placebo, n = 5). CONCLUSIONS: Once-daily tiotropium, as add-on to medium-dose ICS, was effective and well tolerated for Chinese patients with moderate symptomatic asthma, consistent with the main analysis.
Adrenal Cortex Hormones ; Adult ; Asian Continental Ancestry Group ; Asthma ; China ; Forced Expiratory Volume ; Humans ; Salmeterol Xinafoate ; Tiotropium Bromide

Chronic obstructive pulmonary disease (COPD) is a type of progressive, obstructive lung disease characterized by long-term poor airflow. The symptoms of COPD may be relieved and its progression delayed by fluticasone (FTS), salmeterol (SM), and tiotropium (TTP). The aim of this study is to investigate pharmacokinetic (PK) characteristics of inhaled FTS, SM, and TTP after co-administration. An open-label, single-arm, three-period, simple ascending dose study was conducted in 10 healthy male subjects. A single dose of FTS/SM (250/50 µg) and TTP (18 µg) were concomitantly inhaled in period 1, and the dose of each drug was escalated to two- and three-fold in periods 2 and 3, respectively, with a 2-week washout between periods. Activated charcoal was co-administered before and after inhalation to block gastrointestinal absorption. Blood samples for PK analysis were collected up to 24 hours. PK parameters were obtained by non-compartmental analysis. FTS, SM, and TTP rapidly reached maximum plasma concentration after inhalation (0.08–3.00 h, 0.03–0.10 h and 0.03–0.10 h, respectively) and were eliminated with mean half-lives of 9.29–10.44 h, 6.09–12.39 h and 0.25–47.42 h, respectively. PK assessment of the lowest dose of TTP was limited due to relatively low systemic exposure compared to the lower limit of quantification. In conclusion, PK characteristics of FTS, SM, and TTP by pulmonary absorption were evaluated after concurrent inhalation. FTS and SM showed dose-proportional PK profiles between 250–750 µg and 50–150 µg, respectively, while TTP presented dose-proportionality in the early phase exposure between 18-54 µg.
Charcoal ; Fluticasone* ; Gastrointestinal Absorption ; Humans ; Inhalation* ; Lung Diseases, Obstructive ; Male ; Pharmacokinetics ; Plasma ; Pulmonary Disease, Chronic Obstructive ; Respiratory Tract Absorption ; Salmeterol Xinafoate* ; Tiotropium Bromide*

beta -Blockers can cause bronchospasm in asthma. beta 2-agonists prolong the QT interval and alter the clinical course of long QT syndrome (LQTS). We report a case of asthma exacerbation treated cautiously with beta 2-agonists in a patient with LQTS, while LQTS was controlled with low-dose beta 1-antagonists. A 31-year-old woman with LQTS visited the emergency room for asthma exacerbation. FEV1 was 0.5 L (18%) and QTc interval was 520 ms. Low doses of salbutamol or salmeterol were used and gradually increased, while monitoring the QT interval. Simultaneously, a low dose of atenolol was maintained. FEV1 was increased to 2.2 L (83%) without further QT prolongation or cardiac events. The case suggests that lower doses of beta 1-antagonists can be tried for cardiac diseases, even in the presence of asthma exacerbations. beta 2-Agonists may be initiated at lower doses and, if tolerated, the dose can be increased in asthmatic patients with a risk for QT prolongation.
Adrenergic beta-Agonists ; Adrenergic beta-Antagonists ; Adult ; Albuterol ; Asthma ; Atenolol ; Bronchial Spasm ; Emergencies ; Female ; Heart Diseases ; Humans ; Long QT Syndrome ; Salmeterol Xinafoate

Churg-Strauss syndrome (CSS) is an eosinophil associated disease, characterized by vaculitis and granulomatosis on small vessel, asthma and eosinophil tissue infiltration. Several cases of CSS have been reported in patients treated with cysteinyl leukotriene receptor antagonist and weaned-off systemic or inhaled corticosteroids. A 39-year-old man with a history of childhood allergic rhinitis was diagnosed with bronchial asthma and his symptoms were well controlled with fluticasone propinate, salmeterol and zafirlukast. However four months later, he was admitted again with prominent skin lesions, tingling sensation on both extremities and fever. We diagnosed CSS with a history of sinusitis and bronchial asthma, marked peripheral eosinophilia, vasculitis and neuropathy. His symptoms and laboratory findings promptly improved after ten days of intravenous corticosteroid and cessation of zafirlukast without recurrence for six months during the follow-up period. We conclude that zafirlukast may cause CSS and attention should be taken when using zafirlukast.
Adrenal Cortex Hormones ; Adult ; Asthma ; Churg-Strauss Syndrome* ; Eosinophilia ; Eosinophils ; Extremities ; Fever ; Follow-Up Studies ; Fluticasone ; Humans ; Receptors, Leukotriene ; Recurrence ; Rhinitis ; Salmeterol Xinafoate ; Sensation ; Sinusitis ; Skin ; Vasculitis

AIMThe liposome/water partition coefficients of salmeterol and budesonide between aqueous phase and liposomes were determined and the factors that influence their partition coefficients were studied, the mechanism of interaction between the two drugs and phospholipid bilayer was elucidated.

METHODSThe liposome/water partition coefficients of the two drugs were determined by equilibrium dialysis technique. The change of the partition coefficients of the two drugs along with liposome composition and medium was also studied.

RESULTSThe partition coefficients of the two drugs decreased with the increase of cholesterol content and saturation of phospholipid used. The liposome/water partition coefficient of salmeterol increased with the increase of liposome surface negative charge, medium pH and ionic strength, while the liposome surface charge, medium pH and ionic strength had no distinct effect on the liposome/water partition coefficient of budesonide.

CONCLUSIONThe liposome/water partition coefficient of drug was affected by the type, saturation of phospholipid used in liposome preparation, the cholesterol content and surface charge of liposome, as well as the pH and ionic strength of medium also have effect on the liposome/water partition coefficient of drug. Accordingly, in order to reflect the actual partition of drug in biological membrane, the determination condition including liposome composition and medium should be similar to the biological membrane.

Albuterol ; analogs & derivatives ; chemistry ; Budesonide ; chemistry ; Cholesterol ; chemistry ; Drug Carriers ; Hydrogen-Ion Concentration ; Ions ; Liposomes ; Membranes, Artificial ; Phospholipids ; classification ; Salmeterol Xinafoate ; Water ; analysis

BACKGROUND: A combination of salmeterol and fluticasone propionate (SFC) and tiotropium bromide (TIO) is commonly prescribed for COPD patients but there is little data on their effectiveness, particularly in COPD patients with bronchial hyperresponsiveness. This study compared the spirometric improvement based on the change in FEV1, FEV1/FVC, and IC as well as the clinical outcomes of the therapeutic strategies with SFC and TIO versus the individual components in patients with severe COPD and bronchial hyperresponsiveness. METHODS: This study examined the spirometric data and clinical outcomes of 214 patients with COPD and hyperresponsiveness, who were divided into three groups according to the therapeutic regimen (TIO only, SFC only, and a triple therapy regimen). RESULTS: All regimen groups showed early improvement in the FEV1 and IC (at 3- and 6 months after treatment). However, long-term beneficial effects were observed only in the SFC group (at 24 months after treatment). However, these beneficial effects decreased after a 36-month follow up. In all spirometric results, the 12-, 24-, and 36-months data showed a similar degree of improvement in the three groups. The triple therapy group showed higher St. George's Respiratory Questionnaire scores and lower acute exacerbations and hospitalization. CONCLUSION: SFC can be a more important component in the pharmacological treatment of severe COPD patients with hyperresponsiveness than TIO, particularly in the spirometric and clinical outcomes.
Albuterol ; Androstadienes ; Diethylpropion ; Drug Therapy, Combination ; Follow-Up Studies ; Hospitalization ; Humans ; Pulmonary Disease, Chronic Obstructive ; Surveys and Questionnaires ; Scopolamine Derivatives ; Treatment Outcome ; Fluticasone ; Tiotropium Bromide ; Salmeterol Xinafoate

Adolescent ; Adrenergic beta-Agonists ; therapeutic use ; Albuterol ; analogs & derivatives ; therapeutic use ; Asthma ; drug therapy ; physiopathology ; Child ; Child, Preschool ; Female ; Forced Expiratory Volume ; drug effects ; Humans ; Male ; Salmeterol Xinafoate

To systematically review the efficacy and safety of Liujunzi Decoction combined with Western medicine in the treatment of stable chronic obstructive pulmonary disease(COPD). Three English databases and four Chinese databases were systematically searched from the database establishment to April 1, 2020. We screened randomized controlled trial(RCT) according to the pre-determined inclusion and exclusion criteria, then extracted data. Methodological quality of included studies was assessed with Cochrane bias risk evaluation tool. Data were analyzed by using RevMan 5.3. A total of 401 articles were retrieved and finally 17 RCTs were included in this study, involving 1 447 patients, and the overall quality of the included studies was not high. Meta-analysis showed that, in reducing traditional Chinese medicine symptom score, Liujunzi Decoction combined with conventional Western medicine or Salmeterol Xinafoate and Fluticasone Propionate Powder for Inhalation was superior to conventional Western medicine or Salmeterol Xinafoate and Fluticasone Propionate Powder for Inhalation alone. In reducing the grade of modified medical research council(mMRC), Liujunzi Decoction combined with Salmeterol Xinafoate and Fluticasone Propionate Powder for Inhalation was superior to Salmeterol Xinafoate and Fluticasone Propionate Powder for Inhalation alone. In reducing COPD assessment test(CAT) score, Liujunzi Decoction combined with conventional Western medicine was superior to conventional Western medicine alone. In delaying the decline of forced expiratory volume in one second(FEV_1) or % in the expected value, Liujunzi Decoction combined with conventional Western medicine or Salmeterol Xinafoate and Fluticasone Propionate Powder for Inhalation was superior to conventional Western medicine or Salmeterol Xinafoate and Fluticasone Propionate Powder for Inhalation alone. In delaying the decline of ratio of FEV_1 to forced vital capacity(FEV_1/FVC), Liujunzi Decoction combined with conventional Western medicine was superior to conventional Western medicine alone, but there was no statistical difference between Liujunzi Decoction combined with Salmeterol Xinafoate and Fluticasone Propionate Powder for Inhalation and Salmeterol Xinafoate and Fluticasone Propionate Powder for Inhalation alone. In reducing acute exacerbation rate, there was no statistical difference between Liujunzi Decoction combined with Salmeterol Xinafoate and Fluticasone Propionate Powder for Inhalation and Salmeterol Xinafoate and Fluticasone Propionate Powder for Inhalation alone. On the other outcome measures of Liujunzi Decoction combined with other Western medicine, Meta-analysis could not be conducted and conclusions due to the inclusion of only one study. In terms of the occurrence of adverse reactions, some studies did not mention, so the safety of Liujunzi Decoction combined with Wes-tern medicine could not be determined in this paper. Due to the limitations of the quality and quantity of inclu-ded studies, the efficacy of Liujunzi Decoction combined with Western medicine for COPD still needs more high-quality studies for confirmation, and its safety needs to be further verified.
Administration, Inhalation ; Bronchodilator Agents/therapeutic use* ; Drug Combinations ; Drugs, Chinese Herbal ; Humans ; Medicine ; Pulmonary Disease, Chronic Obstructive/drug therapy* ; Salmeterol Xinafoate/therapeutic use*