小诺米星在新生儿的药物动力学

本报告２０例患儿（男性１２例，女性８例；日龄１５±ｓ８ｄ）应用小诺 米星，Ａ组１０例以４ｍｇ／（ｋｇ．ｄ），Ｂ组１０例以５ｍｇ／（ｋｇ．ｄ），均ｂｉｄ，静脉滴注，观察其药物动力学与肾毒发性。单剂０．５ｈ滴毕。结果：血药峰值分别为４．５怀４．７μ／ｍＬ（Ｐ＞０．０５）。２组药物动力学参数（Ｖｄ，Ｃｌ，ＡＵＣ）与肾毒性参数（β２－ＭＧ，ＢＵＮ）差别均无显意义（Ｐ＞０．０５）。提示该药用于新生儿，且     

儿童小诺米星药物动力学研究及其临床意义

用反相高效液相色谱柱前化学衍生法，测定儿童体内小诺米星（ＭＣＲ）血药浓度，并对其代谢动力学进行了研究。结果表明：药一时曲线符合二室开放式模型。主要药动学参数：消除半衰期（Ｔ_（１／２β））为８±５．２ｈ，清除率（Ｃｌ）为０．１２±０．０３（μｇ／ｍｌ），曲线下面积（ＡＵＣ）为１８．９２±５．０８（ｈ·μｇ／ｍｌ，平均血药峰浓度（Ｃ_（ｍａｘ））为３．３２±１．６０μｇ／ｍｌ。与成人肌注ＭＣＲ后药动学参数比较发现，儿童Ｃ_（ｍａｘ）和Ｃｌ较成人低，Ｔ_（１／２β）较成人长。并且８例儿童动力学参数个体间差异显著，这种对药物代谢能力的差异可能是导致少数患儿发生药物中毒的原因。     

小诺米星致新生儿急性肾功能衰竭1例

小诺米星致新生儿急性肾功能衰竭１例谭耀明（广东省韶关市妇幼保健院，韶关５１２０００）关键词小诺米星；新生婴儿；急性肾功能衰竭；过量小诺米星属氨基糖甙类抗生素，能抑制细菌蛋白质合成，破坏细菌细胞膜，从而对革兰阴性杆菌、革兰阳性细菌起强大抗菌作用，该药１...     

小诺米星

小诺米星抗菌谱广,杀菌力强,不为绿脓杆菌、沙雷菌等的乙酰化酶钝化,且血药浓度高,易分布至各脏器,主要经肾脏随尿排出。经日本、意大利等国临床研究疗效满意,副作用轻微。其耳毒性在氨基糖甙类抗生素中仅大于核糖霉素。     

新生儿小诺米星的血液浓度测定及药动学研究

测定小诺米星(MCR)在新生儿体内的血药浓度及药动学参数。8名新生儿静滴MCR后,用荧光光度法测定不同时间内血药浓度,用3P87计算机程序计算药物动力学参数。结果荧光光度法平均回收率95%,RSD为0.3%～1.5%,在1.0～16mg/L范围内,其荧光强度与浓度线性关系良好。MCR在新生儿体内呈二室开放式模型,主要药动学参数平均血药峰浓度(Cmax)为(3.86±1.2)mg/L,消除半衰期(T1/2β)(5.32±1.8)h,清除率(CL)为(0.08±0.03)mg/L,曲线下面积(AUC)为(29.7±10.47)mg*h/L。用药后10h血药浓度为(1.02±0.418)mg/L。结论荧光光度测定法稳定性好,准确可靠。药动学参数与成人比较有显著性差异。小诺米星在新生儿血液和组织中作用较持久。     

硫酸小诺米星注射液的比色测定法

硫酸小诺米星(Ⅰ)为氨基糖甙类抗生素,其原料药及注射液均采用微生物法测定含量。该法虽然可靠,但费时、繁琐,更不适于注射液半成品含量的快速分析。本文根据氨基糖甙类抗生素在碱性条件下可与二价铜离子形成稳定的复合物,在560nm 波长处有最大吸收的原理,采用比色法测定Ⅰ注     

小诺米星致过敏性休克2例

小诺米星(小诺霉素micronomicin)是近几年推广使用的氨基糖成类抗生素,其疗效高,毒性低。出现过敏性休克罕见,现将2例报告如下。     

均匀设计在小诺米星发酵中的应用

均匀设计在小诺米星发酵中的应用孙克俭（哈尔滨制药厂，哈尔滨１５００８４）谢凤龙，赵敏（江苏省微生物研究所，无锡２１４０６３）Ｈｏｍｏｇｅｎｅｏｕｓａｎａｌｙｓｉｓｍｅｔｈｏｄｕｓｅｄｉｎｏｐｔｉｍｉｚａｔｉｏｎｏｆｍｉｃｒｏｎｏｍｉｃｉｎｆｅｒｍｅｎ...     

抗真菌药物在新生儿和婴儿体内的药动学

目前大多数抗真菌药物的药动学数据来自成人,尚未建立不同年龄组儿童给药剂量的标准,且并非所有抗真菌药物都被批准用于新生儿和婴儿真菌感染的预防和治疗。然而新生儿和婴儿药动学特点与成人不同,且药动学参数随生长发育而变化。常用抗真菌药物(多烯大环内酯类、氟化嘧啶类、唑类和棘白菌素类)在新生儿和婴儿体内的吸收、分布、代谢和排泄过程具有较大的个体差异,也不同于其他年龄段儿童。目前抗真菌药物在新生儿和婴儿体内的药动学研究大多限于案例报道,应进一步开展抗真菌药物在新生儿和婴儿体内的药动学和药效学研究。     

Pharmacokinetics of dexamethasone in premature neonates

Objective: Dexamethasone is frequently used in premature neonates with bronchopulmonary dysplasia, however little is known about its disposition in this population. Methods: We evaluated the pharmacokinetics of dexamethasone in 9 premature neonates with a mean gestational age of 27.3 weeks and a postnatal age of 21.8 days. Results: There was a strong relationship between clearance (4.96 ml·min^–1·kg^–1) and gestational age (r=0.884). Pharmacokinetic parameters were grouped based on a gestational age of less than 27 weeks (Group I) and greater than 27 weeks (Group II). Mean clearance in group I and group II was 1.69 and 7.57 ml·min^–1·kg^–1, respectively. Mean distribution volume in group I and II was 1.26 and 2.19 l·kg^–1, respectively. No significant relationships were noted between the disposition of dexamethasone and ventilator requirements or adverse effects. Conclusion: The pharmacokinetics of dexamethasone in premature neonates was related to gestational age.     

高效液相色谱法测定小诺霉素的血药浓度及药动学研究

本文报道了用高效液相色谱(HPLC)测定小诺霉素血药浓度的方法及小诺霉素在12例中国健康志愿者中的药代动力学研究,并分别研究了老年人和青年人以及男性和女性对小诺霉素在体内处置的差异,为进一步正确合理应用小诺霉素提供了重要的数据。本法使用紫外检测器,C_(18)柱,检测限0.2ng,最小检测血药浓度达0.1μg/ml,线性范围1～20μg/ml,小诺霉素和内标氯氮平的保留时间分别为6.8min和8.3min。本法准确、灵敏、快速,适用于小诺霉素药代动力学研究和血药浓度常规监测,12例志愿者单剂量肌注小诺霉素90mg后,药时曲线经计算机自动拟合,符合二室开放模型。主要药动学参数为:T1/2β老年人5.9±2.2h;青年人4.9±2.2h;男性4.2±1.7h;女性6.6±2.5h。CL(ml/min·kg)老年人0.79±0.11;青年人1.06±0.27;男性0.92±0.17;女性0.9±0.3。     

氨苄西林在新生儿的药物动力学

本文报告19例患儿应用氨苄西林以输液泵控恒速静滴与墨菲管滴入2种给药方法的药物动力学与药效学。按体重25-27mg/kg bid计算给药量,单剂(250mg)1h滴毕,12h给药1次。血药峰值分别为117μg/ml和224μg/ml(P<0.05)。药物动力学参数(V_d,Cl,AUC)有非常显著性差异(P<0.01)。恒速静滴药时曲线方程为y=112.61e~(-0.3186t);墨菲管摘入为y=211.36e~(-0.3310t);2组参数均用一室模型模拟,相关系数(r)均为0.9999。不良反应有皮疹等.     

染料比色法测定硫酸小诺霉素的含量

本文采用染料溴麝香草酚蓝与硫酸小诺霉素反应，生成易溶于氯仿的络合物，该络合物在４２１ｎｍ处有最大吸收，线性范围为２４．０～４８．０μｇ·ｍｌ－１，平均回收率为１００．０％，ＲＳＤ＝０．３４％（ｎ＝４）。此方法简便、灵敏，结果可靠。     

小诺霉素与复方氨基比林注射液的配伍实验

本文观察了硫酸小诺霉素与复方氨基比林注射液的配伍稳定性，结果表明两药混合后，在１ｈ内肌注是可行的。     

硫酸小诺霉素注射液在两种甲硝唑输液中的稳定性探讨

硫酸小诺霉素注射液在两种甲硝唑输液中的稳定性探讨郭清峰（河北省沧州市药品检验所０６１００１）ＳｔａｂｉｌｉｔｙｏｆｍｉｃｒｏｎｏｍｉｃｉｎｉｎｔｗｏｔｒａｎｓｆｕｓｉｏｎｓｏｌｕｔｉｏｎｓｏｆｍｅｔｒｏｎｉｄａｚｏｌｅＧｕｏＱｉｎｇ－ｆｅｎｇ（Ｃａｎ...     

Pharmacokinetics of gentamicin in malnourrished infants

Summary The pharmacokinetics of gentamicin was investigated in normal and malnourished infants aged 4–10 months. Neither mean elimination nor distribution half life show any difference, but the volume of distribution was higher in malnourished babies, probably due to their larger total body water.     

Clomipramine concentration and withdrawal symptoms in 10 neonates

AIM

After in utero exposure to tricyclic antidepressants, neonatal withdrawal symptoms have been reported with an estimated incidence between 20 and 50%; however, few data are available for clomipramine. This could also be the case for neonatal pharmacokinetic clomipramine parameters and so this study was set up.

METHODS

Babies exposed to clomipramine in utero were included in an observational study, approved by the local ethics committee, after written informed consent. Withdrawal symptoms were scored at 12, 24 and 48 h after birth using the Finnegan score. Plasma concentrations were determined using an in-house-developed, validated liquid chromatography with mass detection (LC-MSMS) method at 0, 12, 24 and 48 h after birth.

RESULTS

We found that three of 11 pregnancies were complicated with pre-eclampsia. Ten neonates were observed for clomipramine withdrawal symptoms. The observed withdrawal symptoms were too short a period of sleep after feeding (6), poor feeding (3), mild to severe tremors (6), hyperactive Moro reflex (3) and respiratory rate >60 breaths min⁻¹. Serious withdrawal reactions, such as tachycardia and cyanosis, were seen. We calculated a half-life value of 42 ± 16 h for clomipramine in neonates. Only a weak correlation was found between withdrawal reactions and clomipramine plasma concentration or desmethylclomipramine plasma concentration.

CONCLUSIONS

In neonates, clomipramine is eliminated with a half-life value of 42 h, compared with 20 h in adults. In two of 10 neonates, tachycardia and cyanosis were seen as serious withdrawal symptoms after maternal use of clomipramine.