枸橼酸咖啡因与氨茶碱对早产儿神经行为发育影响分析

目的 比较枸橼酸咖啡因和氨茶碱对早产儿神经行为发育的影响,为早产儿早期合理干预提供临床依据。方法 选择2014年6月-2018年6月在中国西电集团医院新生儿科住院接受枸橼酸咖啡因治疗的原发性呼吸暂停(AOP)早产儿62例作为研究组;2011 年 12 月-2014年5月同在中国西电集团医院新生儿科住院采用氨茶碱治疗的AOP患儿69例作为对照组。出生3~8 d及矫正胎龄40周时分别行头颅MRI检查,评估脑白质损伤(WMD)并进行两组比较;6个月及12个月时应用Gesell婴幼儿发育量表测试比较两组神经行为发育水平。结果 两组患儿在性别、出生胎龄及体重、产前孕母糖皮质激素应用及分娩方式、5 min Apgar评分、辅助通气和表面活性物质的应用等方面差异均无统计学意义(P>0.05)。首次头颅MRI显示两组患儿WMD差异无统计学意义(P>0.05)。矫正胎龄40周时头颅MRI显示,咖啡因组WMD较氨茶碱组明显改善,差异有统计学意义(P<0.05);且6个月及12个月时Gessell婴幼儿发育量表测试,随访至校正6月龄时,咖啡因组患儿的大运动、精细运动及个人-社交评分均高于氨茶碱组(P<0.05);随访至校正12月龄时,咖啡因组患儿的大运动、精细运动、语言、适应性评分均高于氨茶碱组(P<0.05)。结论 枸橼酸咖啡可明显改善AOP患儿6个月及12个月时的神经行为发育。     

西咪替丁对血浆氨茶碱浓度的影响

在１６例呼吸系疾病患者观察了西咪替丁对氨茶碱血浆浓度的影响。结果表明加服西咪替丁４００ｍｇ，３次／日，３天后血浆氨茶碱谷浓度和峰浓度均明显增高（ｐ＜０．０１），其中谷浓度升高４３．０±５１．１％，峰浓度升高２７．０±２９．０％。提示二者合用时，应适当减少氨茶碱用量，以避免氢茶碱中毒的发生。     

硝苯啶治疗慢性阻塞性肺气肿20例

对慢性阻塞性肺气肿(简称慢阻肺)患者20例(男13例,女7例;年龄53±7a)采用硝苯啶10-15mg,tid,po×2wk,后改为5mg,tid,维持用药,总有效率95％,副作用轻微。另设24例慢阻肺患者(男17例,女7例,年龄52±6a)采用氨茶碱0.1-0.2g,tid,po,×2wk,总有效率71％,其中4例因副作用而停药。2组疗效比较无显著差别。     

甲磺酸帕珠沙星对氨茶碱在兔体内药动学影响的研究

 目的研究甲磺酸帕珠沙星对兔体内氨茶碱药动学的影响。方法采用自身对照法,以HPLC测定兔单用氨茶碱及与甲磺酸帕珠沙星合用后的茶碱血清浓度,计算药动学参数。结果经BAPP2.3药动程序拟合,甲磺酸帕珠沙星使兔血清中茶碱的曲线下面积AUC由152.0mg·h·L^-1增加到361.4mg·h·L^-1;半衰期t_1/2由2.292h延长至6.823h;MRT由4.944h延长到9.383h,均有非常显著性差异(P<0.01)。结论家兔体内合用甲磺酸帕珠沙星对氨茶碱的消除药动学有显著抑制作用。     

Influence of aminophylline and strychnine on the protective activity of excitatory amino acid antagonists against maximal electroshock-induced convulsions in mice

Summary Aminophylline reversed the protective action of both, D-3-(2-carboxypiperazine-4-yl)-1-propenyl-1-phosphonic acid (D-CPP-ene — a competitive NMDA antagonist) and valproate (used as a conventional antiepileptic drug for comparative purposes) against maximal electroshock-induced seizures. The respective ED₅₀ values of aminophylline were 55.7 and 98.4mg/kg i.p. However, aminophylline (up to 100mg/kg i.p.) did not influence the protective efficacy of 1-(4-aminophenyl)-4-methyl-7,8-methyl-enedioxy-5H-2, 3-benzodiazepine (GYKI 52466 — a non-NMDA antagonist). Strychnine affected the protection provided by D-CPP-ene, GYKI 52466, and valproate against maximal electroshock — the ED₅₀ values of strychnine for the reversal of the anticonvulsive effects of D-CPP-ene, GYKI 52466 or valproate were 0.082, 0.35 and 0.28mg/kg s.c., respectively.An involvement of strychnine sensitive glycinergic receptor-mediated events in the mechanism of the anticonvulsive activity of excitatory amino acid antagonists and valproate may be postulated. The ineffectiveness of aminophylline to reduce the anticonvulsive effects of GYKI 52466 may distinguish a new class of antiepileptic drugs offering an advantage over conventional antiepileptics in patients with epilepsy, requiring aminophylline for pulmonary reasons.     

Disposition and clinical pharmacokinetics of microcrystalline theophylline

Summary Variation in the systemic disposition of theophylline after ingestion of a new microcrystalline product (Theolair®) has been investigated in 7 hospitalized patients with generalized obstructive lung disease. Disposition (absolute bioavailability) was determined by comparing in the same patients the areas under the serum concentration-time curves after a single oral dose of microcrystalline theophylline and after an intravenous infusion of aminophylline. Oral absorption appeared to be fast. The half-life of absorption was 19±9 min (mean±SD). Maximal serum concentrations reached after 100±30 min were found to be in a rather narrow range: 9.8±2.5 mg · 1^–1. The absolute bioavailability of the microcrystalline preparation was high and it showed only small variation: 102.7±10.2% of the dose. Relevant pharmacokinetic parameters (half-life of elimination, volume of distribution and total body clearance) were determined after both routes of administration. Individual dosage regimens required to obtain a therapeutic serum concentration were calculated for each individual patient on the basis of the observed pharmacokinetic parameters.     

头孢噻肟在输液中与6种注射剂配伍的稳定性研究

 目的:研究头抱噻肟( cefotaxime, CTX)在50g·L^-1蔺萄糖输液中与维生素B_{6<\sub>等6种注射剂配伍的稳定性，为临床合理用药提供科学依据。方法:选择25.37℃在5h内观察配伍液的外观、pH及CTX紫外光谱的变化，用紫外分光光度法测定CTX的含量。结果:其稳定性与温度和pH有关。结论:在25℃，与6种注射剂配伍5h内都稳定可用;在37℃，与维生素C、氛茶碱注射剂配伍，则最好在3h内用完。}     

参麦注射液与氨茶碱对膈肌细胞Ca2+浓度的影响

目的 :探讨参麦注射液与氨茶碱对膈肌细胞内游离Ca2 浓度的影响。方法 :体外培养大鼠膈肌细胞 ,荧光光度法测定参麦注射液与氨茶碱处理前后细胞内Ca2 浓度的变化。结果 :氨茶碱可使膈肌细胞内的Ca2 浓度明显升高(P<0.01) ,维拉帕米或预先去除培养液中Ca2 可消除该作用。参麦注射液对膈肌细胞内Ca2 浓度无明显影响(P>0.05)。缺氧24h即可致膈肌细胞内Ca2 浓度明显升高(P<0.01) ,参麦注射液对缺氧24h所致的膈肌细胞内Ca2 浓度升高有抑制作用。结论 :细胞外Ca2 是氨茶碱导致细胞内Ca2 升高的关键因素 ,氨茶碱可通过促进细胞外Ca2 内流导致细胞内Ca2 升高。参麦注射液可抑制缺氧所致的膈肌细胞内Ca2 超载 ,对细胞有一定的保护作用。以上作用分别参与了二者抗膈肌疲劳的机制     

氨茶碱对体外循环患者肺功能的影响

目的 研究氨茶碱在体外循环中对肺功能的保护的作用.方法 36例体外循环患儿,随机分两组,在麻醉诱导后分别静脉注射氨茶碱和生理盐水.记录CPB时间,主动脉阻断时间,术后呼吸机辅助时间,24 h尿量.分别测量麻醉诱导后,体外循环结束后1、6、8、24h氧合指数,二氧化碳分压;体外循环前,鱼精蛋白后1、2、5min,体外循环后60min气道峰压.结果 氨茶碱组术后24h尿量,氧合指数明显高于对照组,而对照组气道峰压高于氨茶碱组.结论 氨茶碱有良好的肺功能保护作用.     

HPLC测定复方氨肽素片中氨茶碱与马来酸氯苯那敏的含量及含量均匀度

目的 建立HPLC测定复方氨肽素片中氨茶碱与马来酸氯苯那敏的含量及含量均匀度。方法 色谱柱为YMC Hydrosphere C₁₈(4.6 mm×250 mm,5 μm),流动相为乙腈-0.5%磷酸溶液(用三乙胺调pH值至2.2)(10∶90),流速为1.0 mL·min^-1,柱温为30 ℃,检测波长为262 nm。结果 茶碱和马来酸氯苯那敏分别在0.06~0.58 mg·mL^-1和2.2~20.0 μg·mL^-1内线性关系良好,回收率分别为100.4%和101.2%,RSD分别为0.74%和1.40%(n=9)。结论 方法快速准确,重复性好,结果可靠,可同时测定氨茶碱及马来酸氯苯那敏,为产品质量标准提高提供基础。