环丙沙星对严重肺心病患者茶碱动力学的影响及两药合用后茶碱…

本文应用萤光偏振免疫法分别测定了六名严重肺心病患者单独静滴茶碱达稳态及达稳态后合用环丙沙星２ｄ后茶碱的血药浓度，对药一时数据以ＰＤＰＫ程序按静滴一室模型进行处理，并对结果进行统计分析，结果发现环丙沙星能抑制茶碱的正常代谢，明显延长了茶碱的半衰期（Ｐ〈０．０１），使茶碱稳态血药浓度明显升高（Ｐ〈０．０１），而对分布容积及消除率均无明显影响（Ｐ〉０．０５）。根据实验结果我们对本院临床上几十例合用环丙沙     

稳态时甲磺酸帕珠沙星对兔体内多索茶碱药物动力学的影响

目的:探讨稳态时甲磺酸帕珠沙星对家兔体内多索茶碱药物动力学的影响.方法:8只家兔随机分为2组,单用组多索茶碱给药4 d,合用组甲磺酸帕珠沙星和多索茶碱联合用药4 d.采用高效液相色谱法平行监测给药后多索茶碱的血药浓度,并计算药物动力学参数.结果:与单用组相比,合用组家兔体内多索茶碱的AUCSS、Cmax和Cmin升高,CL/F下降(t=3.371、2.559、3.502和3.952,P<0.05),其余参数在2组间差异无统计学意义(P>0.05).结论:甲磺酸帕珠沙星能延缓多索茶碱的消除,2药长期合用时应对多索茶碱进行血药浓度监测.     

磷霉素钠对肺心病人体内茶碱药物动力学的影响

目的 研究磷霉素钠对肺心病人体内茶碱药物动力学的影响。方法 采用紫外分光光度法分别测定了８例肺心病患者单用氨茶碱及合用霉素稳态血药浓度。结果 磷霉素钠对茶碱的药物动力学无影响（Ｐ〈０．０５）。结论 磷霉素钠不影响茶碱的体内代谢过程,两药合用时无需调整剂量。     

阿奇霉素对长效茶碱药代动力学的影响

目的观察慢性阻塞性肺病患者（ＣＯＰＤ）用阿奇霉素后对长效茶碱类药物舒弗美的药代动力学影响。方法测定患者使用阿奇霉素及加用舒弗美后血清中茶碱的浓度。结果两药合用后血清中茶碱稳态峰浓度、稳态谷浓度、药时曲线下面积及浓度波动系数与单纯长效茶碱组相比差异无显著性（Ｐ＞０．０５），达峰时间略短于对照组，但差异无显著意义。结论阿奇霉素对茶碱药代动力学影响不大，两药合用安全     

环丙沙星对慢性阻塞性肺疾病患者氨茶碱药物动力学的影响

目的量化地研究环丙沙星对慢性阻塞性肺疾病患者氨茶碱药物动力学的影响。方法8例慢性阻塞性肺疾病患者口服氨茶碱(100mg,8h1次)后加服环丙沙星(500mg,12g1次),用紫外分光光度计平行监测合用前后茶碱的经时血药浓度,拟合茶碱药物动力学参数并做统计学比较。结果与合用前相比,患者血清中茶碱浓度显著增高(P<0.05),消除半衰期非常显著地延长(P<0.01),消除率下降(P<0.05)。结论合用环丙沙星对氨茶碱的消除动力学有显著性抑制,临床合用时应注意茶碱的血浓度监测,防止氨茶碱因代谢减慢而引起蓄积中毒。     

氟罗沙星对茶碱在家兔体内药物代谢动力学的影响

目的观察氟罗沙星对茶碱在家兔体内药物代谢动力学的影响.方法动物分为2组,第1组静脉注射茶碱12mg@kg-1;第2组静脉注射氟罗沙星20mg@kg-1,0.5h后静脉注射茶碱12mg@kg-1.测定茶碱的血药浓度,计算药物动力学的参数.结果茶碱的药时曲线符合二室模型.合用氟罗沙星组茶碱的药时曲线消除相血药浓度明显高于单用茶碱组,茶碱的消除半衰期(T1/2β)和曲线下面积(AUC)明显增大,机体清除率(CL)明显降低.结论氟罗沙星能延缓茶碱在家兔体内的消除,合并用药时应对茶碱的用法作适量调整或对茶碱进行临床给药监测.     

茶碱(氨茶碱)(三)

环丙沙星 环丙沙星可以通过细胞色素P450酶系统抑制茶碱的肝代谢,使茶碱血药浓度和毒性上升,合用应监测茶碱血药浓度,茶碱的剂量可能需要减少,或停用环丙沙星.环丙沙星和其他由肝脏代谢的茶碱衍生物之间也存在着类似的相互作用,与二羟丙茶碱则没有相互作用.萘啶酸、氟罗沙星、氧氟沙星、西诺沙星与茶碱之间也未表现出相互作用.     

茶碱不同给药方案与其血药浓度关系的研究

目的探讨茶碱不同给药方案与其血药浓度的关系,为临床合理应用茶碱提供理论依据.方法利用荧光偏振免疫法测定茶碱血药浓度,246例患者茶碱给药方案为：口服组（两个剂量组）,静滴组,口服＋静滴组.结果采用口服＂茶碱缓释片0.2gBid＂组以及口服＂茶碱缓释片0.1gBid＂＋静滴＂氨茶碱针0.25gQd＂组给药方案的患者,超过70%的患者血药浓度值在有效范围5.00～15.00μg/mL,并且平均茶碱血药浓度大于口服＂茶碱缓释片0.1gBid＂与静滴＂氨茶碱针0.25gQd＂组.茶碱血药浓度与不良反应的发生有显著关系,采用口服＂茶碱缓释片0.2gBid＂组的患者,不良反应发生率最高.结论口服＂茶碱缓释片0.1gBid＂＋静滴＂氨茶碱针0.25gQd＂为较好的给药方案.     

阿奇霉素对长效茶碱药代动力学的影响

观察慢性阻塞性肺病患者用阿奇霉素后对长效茶碱类药物舒弗美的药代动力学影响。方法 测定患者使用阿奇霉素及加用舒弗美后血清中茶碱的浓度。两药合用后血清中茶碱稳态峰浓度，稳态谷浓度，药时曲线下面积及浓度波动系数与单纯长效茶碱组相比差异无显著性，达峰时间加短于对照组，但差异无显著意义。     

茶碱血药浓度监测病例分析

目的：了解影响茶碱血药浓度的因素以指导临床用药。方法：对茶碱维持量疗法的820例患者的茶碱血药浓度监测结果进行了回顾性分析。结果：35．1％的病例茶碱血药浓度在有效血药浓度范围内（10-20μg/ml,27．1％的病例茶碱血药浓度高于20μg/ml,环丙沙星,氟罗沙星,沙丁胺醇提高茶碱血药浓度,易使茶碱血药浓度偏高,特布他林,利福平,速尿降低茶碱血药浓度,易使茶碱血药浓度偏低,肝功能不正常,肺心病提高茶碱血药浓度,易使茶碱血药浓度偏高,嗜烟降低茶碱血药浓度,易使茶碱血药浓度偏低。结论：茶碱血药浓度个体差异大,药物因素,疾病因素,嗜好等影响茶碱血药浓度,茶碱血药浓度监测对提高其使用的安全性和有效性具有重要的意义。     

高血浓度茶碱致心律失常的临床观察

目的：观察高血浓度茶碱对心律失常的影响,探索安全合理使用茶碱方法。方法：收集１９４例住院治疗的病例,测定其血液茶碱浓度及作心电图检查,并按血浓度分为高浓度组（Ａ组）和治疗浓度组（Ｂ组）,同时选择５６例未使用氨茶碱作对照组（Ｃ组）。结果：Ａ组及Ｂ组引起窦性心动过速发生率分别为５７．７％、３９．８５％,房纤及房扑发生率分别是４４．４％、２．１５％,房性早搏发生率分别为４４．４％、４．３０％,室性早搏     

血清茶碱测定及其药代动力学

目的判断静注氨茶碱在体内的隔室模型,计算其药代动力学参数。方法用双波长紫外分光光度法测定家兔静注氨茶碱后的血清茶碱浓度,根据相关药代动力学理论研究其药动学。结果静注氨茶碱在体内符合两室模型,药动学方程为c=7.7e-2.58t 20.893e-0.1733。结论可以用紫外分光光度法测定茶碱血药浓度,在体内代谢符合两室模型,并可计算出其药动学方程。     

探讨两种茶碱类药物对高龄支气管哮喘急性发作患者肺部症状、通气功能及不良反应的影响

目的：探讨氨茶碱和多索茶碱对高龄支气管哮喘急性发作患者肺部症状、通气功能及不良反应的影响。方法研究对象方便选取该院2011年1月—2015年12月收治高龄支气管哮喘急性发作患者共100例,以随机区组法分为氨茶碱组(50例)和多索茶碱组(50例),分别采用氨茶碱和多索茶碱静脉滴注治疗;比较两组患者临床疗效,症状体征改善时间,治疗前后肺通气功能指标水平及不良反应发生率等。结果氨茶碱组和多索茶碱组患者治疗总有效率分别为76.00%,94.00%;氨茶碱组患者治疗后FEV1、PEF及FEV1/FVC水平分别为(3.09±1.02)L,(5.14±1.17)L/s,(63.10±14.97)%;多索碱组患者治疗后FEV1、PEF及FEV1/FVC水平分别为(3.74±1.15)L,(5.97±1.42)L/s,(74.55±17.74)%;多索茶碱组患者临床疗效、症状体征改善时间及治疗后肺部通气功能指标水平均显著优于氨茶碱组(P<0.05);同时氨茶碱组和多索茶碱组患者不良反应发生率分别为22.00%,6.00%;多索茶碱组患者不良反应发生率显著低于氨茶碱组(P<0.05)。结论多索茶碱治疗高龄支气管哮喘急性发作临床疗效及安全性均优于氨茶碱,具有临床应用价值。     

Relationship among dosages of aminophylline, plasma levels of theophylline and variation of pulmonary arterial pressure]

The relationship among the dosages of aminophylline, plasma levels of theophylline and variations of mean pulmonary arterial pressure (mPAP) in 72 patients with COPD was investigated. The results showed that after a different loading dosage of aminophylline (6 mg/kg, 5 mg/kg and 4 mg/kg) was administered by intravenous injection, mPAP in the 6 mg/kg group was decreased more significantly (P less than 0.01) than that in the 4 mg/kg group. In the 6 mg/kg group, the decreased mPAP period sustained for 120 min, which was longer than that in the other 2 groups. The plasma levels of theophylline in the 6 mg/kg group of patients 30 to 120 min after loading dose injected were 115.54-79.04 mumol/L, which were higher than that in the others. Within the 120 min period of observation after the drug was administered no patients in any of these groups showed severe untoward effects. According to the results of this experiment, we suggest that the 6 mg/kg as a loading dose should be advised for the treatment of pulmonary hypertension in COPD. The optimum time to give the maintenance dosage should be set within 2 h after the loading dose. It is necessary to monitor the plasma levels of theophylline while aminophylline is administered, so that optimal therapeutic effects could be achieved without side effects.     

四种氟喹诺酮药物对氨茶碱药物动力学的影响

本实验采取自身对照，用双波长分光光度法测定，观察氟哌酸、氟嗪酸、氟啶酸和丙氟哌酸对家兔体内氨茶碱代谢动力学的影响，并计算其药物动力学参数。结果显示氟哌酸、氟嗪酸和氟啶酸分别缩短氨茶碱的血浆半衰期２２．２％、３７．７％和１４．４％，而丙氟哌酸则延长其１５．６％。说明氟哌酸、氟嗪酸和氟啶酸可能诱导肝药酶，丙氟哌酸则抑制其活性。     

Accidental coadministration of intravenous aminophylline and theophylline by mouth: a hazardous practice

Eight patients who inadvertently received theophylline by mouth and aminophylline by the intravenous route together were reviewed by the Clinical Pharmacology Service of the Royal Adelaide Hospital because their serum theophylline levels were in excess of the stated therapeutic range. Six of these patients were severely compromised by their high theophylline level, and two of them, who had advanced obstructive lung disease and respiratory failure, died shortly after the drug levels were detected. Oversights of this nature can arise during the early stages of a patient's hospital admission and when medical staff changes occur. All patients who receive aminophylline by the intravenous route must be kept under close surveillance to ensure that theophylline formulations are not given by mouth concurrently.     

Theophylline blood levels in Sri Lankan asthmatics: comparison of two methods of assay

OBJECTIVES: To assay theophylline blood levels in a sample of Sri Lankan chronic asthmatics taking oral theophylline, and to evaluate a simple and cost effective ultraviolet spectrophotometric assay for theophylline levels in blood. SETTING: Chronic asthmatics taking oral theophylline attending medical clinics at the National Hospital of Sri Lanka (NHSL) were recruited for the study. Blood samples were collected from recruited patients on their subsequent clinic visit. DESIGN AND METHODS: A cross-sectional study of theophylline blood levels. Blood samples were assayed for trough theophylline levels using two methods: an automated homogeneous enzyme immunoassay (EMIT), and a low cost ultraviolet spectrophotometric method. RESULTS: Only 2 patients of the 24 had theophylline blood levels in the accepted therapeutic range (10 to 20 micrograms/ml) (3.4); 19 patients had levels under 5 micrograms/ml. A correlation coefficient of 0.99 was obtained in the statistical comparison of the two methods, indicating that the spectrophotometric method has similar accuracy as the reference EMIT assay. CONCLUSIONS: The results signal a need for monitoring of theophylline in asthmatics when accepted clinical indications are present. The ultraviolet spectrophotometric method is ideal to initiate therapeutic drug monitoring (TDM) in the country because of its low cost (about Rs. 55 per assay), requiring only a UV recording spectrophotometer.     

The pharmacokinetics of lysine theophylline, a new soluble theophylline, in human volunteers

A comparative study of the pharmacokinetics of lysine theophylline and aminophylline in normal subjects reveals no significant difference. If lysine theophylline is shown to have the same clinical efficacy as aminophylline, the hypersensitivity reactions associated with the latter could be avoided.     

茶碱唾液浓度测定及药代动力学

本文用紫外分光光度法,对氨茶碱控释片在病人唾液中的茶碱浓度进行了测定,计算了其茶碱动力学参数。结果显示,氨茶碱控释片的唾液浓度比较稳定,但茶碱动力学参数的个体差异很大,临床很有必要监测茶碱血药浓度。