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对囊性纤维化患者口服沙丁胺醇后的血浆浓度及效果

Plasma concentrations and effects of salbutamol administered orally to patients with cystic fibrosis.

作者信息

Demnati R, Michoud M C, Jeanneret-Grosjean A, Ong H, Du Souich P

机构信息

Département de pharmacologie, Université de Montréal, Québec, Canada.

出版信息

Br J Clin Pharmacol. 1995 Oct;40(4):319-24. doi: 10.1111/j.1365-2125.1995.tb04553.x.

Abstract
  1. To test whether cystic fibrosis (CF) altered the kinetics and dynamics of oral salbutamol, 11 patients with CF (19-33 years old; five females; FEV1: 37 +/- 12% of predicted value) and 10 healthy volunteers (20-41 years old; five females; FEV1: 99 +/- 14% of predicted value) received orally 4 mg salbutamol. 2. The estimated pharmacokinetic parameters of salbutamol in patients with CF were identical to those in healthy subjects. For instance, peak plasma concentrations of salbutamol were 10.5 +/- 2.6 (mean +/- s.d.) and 10.2 +/- 2.9 ng ml-1 (NS), and the area under salbutamol plasma concentrations as a function of time (AUC (0, 7 h)) was 43.0 +/- 9.3 ng ml-1 h and 43.3 +/- 12.7 ng ml-1 h (NS) in CF patients and in healthy subjects, respectively. Since on a mg kg-1 dose basis, CF patients received a dose 28% greater than healthy subjects, this lack of differences implies a decrease in the amount of salbutamol absorbed, or alternatively, an increase in both clearance and volume of distribution of salbutamol. 3. Salbutamol did not elicit bronchodilation in CF patients, but increased heart rate from 77 +/- 2 to 103 +/- 3 beats min-1 (P < 0.05). 4. Salbutamol decreased plasma potassium concentrations from 4.5 +/- 0.1 to 3.8 +/- 0.1 mmol l-1 in the CF group (P < 0.05) and from 4.1 +/- 0.2 to 3.4 +/- 0.1 mmol l-1 in the controls (P < 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)
摘要
  1. 为了测试囊性纤维化(CF)是否改变口服沙丁胺醇的动力学和动态变化,11例CF患者(年龄19 - 33岁;5名女性;第一秒用力呼气容积(FEV1):预测值的37±12%)和10名健康志愿者(年龄20 - 41岁;5名女性;FEV1:预测值的99±14%)口服了4毫克沙丁胺醇。2. CF患者中沙丁胺醇的药代动力学参数估计值与健康受试者相同。例如,沙丁胺醇的血浆峰值浓度分别为10.5±2.6(均值±标准差)和10.2±2.9纳克/毫升(无显著差异),CF患者和健康受试者中沙丁胺醇血浆浓度随时间变化的曲线下面积(AUC(0, 7 h))分别为43.0±9.3纳克/毫升·小时和43.3±12.7纳克/毫升·小时(无显著差异)。由于按每千克体重剂量计算,CF患者接受的剂量比健康受试者大28%,这种无差异意味着沙丁胺醇吸收量减少,或者说,沙丁胺醇的清除率和分布容积均增加。3. 沙丁胺醇在CF患者中未引起支气管扩张,但使心率从77±2次/分钟增加到103±3次/分钟(P<0.05)。4. CF组中沙丁胺醇使血浆钾浓度从4.5±0.1毫摩尔/升降至3.8±0.1毫摩尔/升(P<0.05),对照组中从4.1±0.2毫摩尔/升降至3.4±0.1毫摩尔/升(P<0.05)。(摘要截选至250词)

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