头孢地尼片对呼吸道感染疗效初步观察

目的:探讨头孢地尼片对呼吸道感染的效果。方法:收集某院2007年3月～2010年3月间收治的轻中度呼吸道急性感染或慢性感染的急性发作病例17例,采用头孢地尼片,每次1～2片,每片100mg,1日3次,一般5～7天为一疗程,进行呼吸道感染的治疗,治疗后进行临床疗效及安全性评价并进行统计分析。结果:17例患者在口服头孢地尼片后,均取得了良好的疗效。在观察期间均无不良反应发生,和各项实验室检查指标也均在正常范围之内。结论:头孢地尼片可适合于由敏感菌株所致的社区获得性呼吸系感染以及慢性阻塞性肺病的急性加重期,值得临床上进一步验证观察。     

集中带量采购中选与原研头孢地尼口服常释制剂疗效和安全性比较

目的比较国家组织集中带量采购(集采)头孢地尼分散片(达力先)与原研头孢地尼胶囊(全泽复)的临床疗效和安全性。方法通过医院信息系统收集2020年1月1日至2021年12月31日首都医科大学宣武医院门诊单次使用头孢地尼患者的性别、年龄、医保类型、感染类型、头孢地尼用药情况、是否合并使用其他抗菌药物, 头孢地尼用药前后血常规、C反应蛋白和肝肾功能等实验室检查结果, 以及头孢地尼不良反应报告资料等信息。对集采中选头孢地尼组(集采组)和原研头孢地尼组(原研组)患者年龄、性别、医保类型、感染类型及是否合并使用其他抗菌药物等进行倾向性评分匹配后, 比较2组患者药物临床应用情况, 间接评价2种药物的疗效。通过比较2组患者用药前后白细胞计数、中性粒细胞百分比及C反应蛋白检测值, 不良反应报告上报情况, 用药前后肝肾功能, 对2药疗效和安全性进行评价。结果共纳入符合入选标准的患者9 514例, 集采组7 037例, 原研组2 477例;经倾向性评分匹配后, 2组患者均为1 268例, 其性别、年龄、感染类型、合并其他抗菌药物等情况比较差异均无统计学意义(均P>0.05)。集采组头孢地尼日剂量、疗程及...     

盆腔炎患者采用头孢地尼联合奥硝唑治疗的临床疗效分析

目的:分析对盆腔炎患者给予头孢地尼、奥硝唑联合治疗的临床疗效。方法:对本院2015年5月-2017年5月收治的48例盆腔炎患者进行观察,将其中采用头孢地尼单独治疗的24例患者设为参照组,将采用头孢地尼、奥硝唑联合治疗的24例患者设为实验组,观察并记录两组治疗效果。结果:实验组总有效率(91.67%)优于参照组(P0.05);实验组IL-1、CPR指标明显改善,低于参照组(P0.05)。结论:头孢地尼、奥硝唑联合治疗能迅速控制患者临床症状,减轻炎症反应,不良反应少,安全性高,值得推广应用。     

改进HPLC法考察试制头孢地尼缓释微丸的稳定性

目的:通过HPLC法监控试制的头孢地尼缓释微丸的含量及有关物质变化趋势.方法:对<中国药典>2010版头孢地尼各论所载HPLC方法加以改进,用以测定头孢地尼缓释微丸的含量及有关物质,考察试样的稳定性.结果:经过改进的HPLC方法能有效检测头孢地尼,辅料及自身降解产物对测定无干扰.结论:本色谱系统能真实反映头孢地尼缓释微丸制剂质量优劣,制剂稳定性良好.     

头孢地尼用于治疗下吸道感染的临床疗效分析

头孢地尼为第三代口服头孢菌素,我科2006年7月～2007年1月应用头孢地尼(商品名:世扶尼)治疗下呼吸道感染44例,取得较好疗效,现报道如下。     

分子排阻色谱法测定头孢地尼胶囊中的高分子杂质

目的:建立测定头孢地尼胶囊中高分子杂质的方法。方法:采用分子排阻色谱法。色谱柱为依利特SephadexG-10,以0.025mol·L-1磷酸盐缓冲液(pH7.0)为流动相A(供试品测定),以水为流动相B(对照品测定),流速为1.5mL·min-1,检测波长为254nm。结果:头孢地尼与高分子杂质分离度良好,头孢地尼检测浓度线性范围为3.95～11.85μg·mL-1(r=0.9995),精密度试验RSD=1.67%,检测限为9.9ng。结论:该方法简单、快速、准确、重复性好,可用于头孢地尼胶囊中高分子杂质的检测。     

头孢地尼颗粒剂治疗儿童急性细菌性扁桃体炎的疗效和安全性

目的:评价头孢地尼颗粒剂治疗儿童急性细菌性扁桃体炎的疗效和安全性。方法:30例患儿口服头孢地尼颗粒剂5 mg·kg-1·次-1,tid,疗程5 d。结果:48 h内退热率83．33％,不良反应发生率3．33％,痊愈率90．00％,总有效率96．67％,细菌清除率100％,药物敏感率100％。结论:头孢地尼颗粒剂治疗儿童急性细菌性扁桃体炎安全有效。     

药品行政保护品种介绍:抗感染药物(一)(待续)

头孢克肟通用名:头孢克肟(cefixime).化学名:(6R,7R)-7-[(Z)-2(2-氨基-4-噻唑基)-2-(羧甲氧基亚胺)-乙酰胺基]-3-乙烯基-8-氧-5-硫杂-1-氮杂二环[4,2,0]-2-辛烯-2-羧酸.申请日:1993年7月9日,申请人:日本藤泽药品工业株式会社.授权日:1994年1月18日.授权号:B-JP 94011801.法定行政保护期:从授权之日起7.5 a,至2001年7月18日.     

头孢地尼与头孢克罗治疗社区获得性肺炎51例疗效比较

目的:评价头孢地尼治疗社区获得性肺炎的有效性和安全性。方法:采用随机对照方法,29例接受头孢地尼9～18mg/(kg·d),2次/d;22例接受头孢克罗20～40mg/(kg·d),3次/d,疗程5～7d。结果:头孢地尼治疗组总有效率100%,头孢克罗治疗组总有效率91%。结果显示两组均有效,经统计学检验差异无显著性(χ2=1.343,P>0.05)。结论:头孢地尼治疗社区获得性肺炎安全有效。     

头孢地尼与奥硝唑联用对慢性盆腔炎患者的疗效评价

目的:评价头孢地尼与奥硝唑联用对慢性盆腔炎患者的临床疗效。方法:选取2015年1—10月间收治的慢性盆腔炎患者134例,将其分为观察组和对照组,每组67例;对照组患者均给予奥硝唑片治疗,观察组患者在对照组基础上加用头孢地尼胶囊治疗,用药1周后比较两组患者的临床疗效。结果:观察组患者治疗后的总有效率为94.03%高于对照组为79.10%(P<0.05)。结论:采用头孢地尼与奥硝唑治疗慢性盆腔炎患者的疗效优于单用奥硝唑的疗效,可减少患者白带的量、下腹不适及月经不调等症状。     

Allosteric interaction of zinc with recombinant alpha(1)beta(2)gamma(2) and alpha(1)beta(2) GABA(A) receptors

In a recent study we have provided evidence that inhibition of native GABA(A) receptors by zinc depends primarily on the allosteric modulation of receptor gating. Both the kinetics and the sensitivity of the GABA(A) receptor to zinc depend on subunit composition, especially on the presence of the gamma(2) subunit. To analyze the mechanism of action of zinc its effects have been tested on recombinant alpha(1)beta(2)gamma(2) and alpha(1)beta(2) receptors expressed in HEK 293 cells. The currents produced by ultrafast application of GABA have been measured to assess the impact of zinc ions on GABA(A) receptor gating with resolution corresponding to the time scale of synaptic currents. While, as expected, zinc markedly reduced the peak amplitude of alpha(1)beta(2)-mediated currents, its effect on kinetics was significantly different from that observed for alpha(1)beta(2)gamma(2). In particular, unlike alpha(1)beta(2)gamma(2), zinc did not affect the onset of alpha(1)beta(2)-mediated responses. Moreover, zinc increased the extent of desensitisation of alpha(1)beta(2)gamma(2) receptors and reduced desensitisation of alpha(1)beta(2) ones. Quantitative analysis suggests that zinc exerts an allosteric modulation on both alpha(1)beta(2)gamma(2) and alpha(1)beta(2) receptors. Zinc effects on alpha(1)beta(2)gamma(2) were qualitatively similar to those reported for native receptors.     

(S)-(-)-氨磺必利-D-(-)-酒石酸盐的合成

目的研究（S）-（-）-氨磺必利-D-（-）-酒石酸盐的制备方法。方法以4-氨基-2-甲氧基-5-巯基苯甲酸为原料,经乙基化、氧化得4-氨基-2-甲氧基-5-乙基磺酰基苯甲酸（4）,另由1-乙基-2-氨甲基吡咯烷经D-（-）-酒石酸拆分得S-（-）-1-乙基-2-氨甲基吡咯烷（6）,4与6缩合制得S-（-）-氨磺必利（7）,再与D-（-）-酒石酸成盐制得目标物S-（-）-氨磺必利-D-（-）-酒石酸盐（1）。总收率达25%（以4-氨基-2-甲氧基-5-巯基苯甲酸计算）。结果所得产物经元素分析,红外光谱、核磁共振谱及质谱确证了结构。结论本方法原料易得,反应条件温和,产品质量易控制。     

alpha-glucosidase (CHO) (Genzyme)

Genzyme General is developing recombinant human alpha-glucosidase, produced in mammalian cell culture, as a potential treatment for Pompe disease. By July 2004, enrollment was completed in two clinical trials and an observational study in adults. Genzyme was planning to file for regulatory approval in Europe during 2004, followed by filings in the US and Japan in mid-2005.     

(S)-oxybutynin (Sepracor)

Sepracor is developing (S)-oxybutynin, a single-isomer version of Alza's Ditropan (racemic oxybutynin), a muscarinic acetylcholine receptor antagonist, as a potential treatment for urinary incontinence.     

Developmental toxicity of di-(C(7)-C(9) alkyl) phthalate and di-(C(9)-C(11) alkyl) phthalate in the rat

Two phthalate esters, di-(C(7)-C(9) alkyl) phthalate (D79P) and di-(C(9)-C(11) alkyl) phthalate (D911P), have been assessed for their potential to cause developmental toxicity in the rat. Groups of 22 timed-mated Sprague-Dawley rats were administered 250, 500, or 1000 mg/kg D79P or D911P daily by oral gavage (5 ml/kg) between gestation days (GD) 1 and 19. Control animals received the vehicle (olive oil) alone. On GD20, the animals were sacrificed and the fetuses examined. Treatment resulted in no signs of maternal toxicity, as assessed by adjusted maternal bodyweight gain throughout gestation and clinical examinations, and no effects upon litter size, fetal survival or bodyweight. Pups of the high dose D79P and intermediate and high dose D911P groups showed increased incidences of supernumerary lumbar ribs. There was a significant increase in dilated renal pelves in pups of the low dose D79P and high dose D911P groups, but only for D911P was there a significant trend. Consequently, the no observed adverse effect level (NOAEL) for maternal toxicity for both D79P and D911P is 1000 mg/kg/day. The NOAEL values for developmental toxicity are 500 mg/kg/day D79P and 250 mg/kg/day D911P.     

Psychopharmacological profile of 1-(m-(trifluoromethyl) phenyl) piperazine (TFMPP)

The effect of TFMPP, an agonist of the 5-HT1b receptors, was studied in mice on several psychopharmacological parameters. In contrast to imipramine-like drugs, TFMPP neither antagonized reserpine-induced hypothermia nor increased yohimbine-induced toxicity. Similarly to imipramine-like drugs, TFMPP antagonized oxotremorine-induced hypothermia and was active in the behavioural despair test. In addition, TFMPP normalized a social behavioural deficit induced by isolation. The effects of TFMPP on oxotremorine-induced hypothermia in the behavioural despair test and in the isolation-induced social behavioural deficit are all antagonized by d-1 propranolol. It is concluded that TFMPP seems to possess psychotropic activity resembling only in part that of imipramine-like drugs and that these actions may be mediated through 5-HT1b receptors.     

Inhibition of Poly(ADP-Ribose)Polymerase (PARP)

Recently, studies of B-cell physiology have continued to provide new and surprising insights into the nature of autoimmunity, highlighting novel potential immunointervention strategies. The meeting on ‘B cells and autoimmunity: new concepts and therapeutic perspectives’ brought together basic scientists and clinicians with research interests in a range of autoimmune diseases. Recent advances in different facets of B-cell biology were discussed in the prospect of understanding autoimmunity, and significant advances in our understanding of the mechanisms that regulate the autoimmune response at the B cell-level were described. Even though no single message emerged, it is clear that the B lymphocyte is truly destined to become a therapeutic target for the treatment of autoimmune disease.     

Two-generation reproduction toxicity studies of di-(C(7)-C(9) alkyl) phthalate and di-(C(9)-C(11) alkyl) phthalate in the rat

Di-(C(7)-C(9) alkyl) phthalate (D79P) and di-(C(9)-C(11) alkyl) phthalate (D911P), based on high-normality linear oxo-alcohols, have been assessed for their impact upon reproductive performance in Sprague-Dawley rats. Rats were continuously exposed to either D79P or D911P at dietary levels of 0%, 0.1%, 0.5%, or 1.0% over two generations. Selected F(0) offspring (F(1) generation) were exposed to the same dietary concentration of D79P or D911P as the respective F(0) animals, and were mated to produce F(1) offspring. Both D79P and D911P markedly reduced body weight gain in F(0) and F(1) adult males at the highest dose, but females were affected to a lesser extent. There was no impairment of fertility, fecundity, or development in either generation, but body weights of offspring in the 1.0% D79P and 1.0% D911P groups were slightly and transiently reduced over the weaning period. Although decreases in the weight of several organs were accounted for by depressed body weight, ovary weights were reduced in both generations exposed to 1.0% D79P, and epididymidal weights were slightly reduced in adults of both generations exposed to 1.0% D911P. However, ovarian function-assessed by the oestrus cycle and mating behaviour-and epididymidal sperm concentration, motility, and morphology were unaffected by either substance. Treatment resulted in liver changes, particularly in males, characterised by increased liver weight in young animals, histopathologic changes and reduced organ weight in mature animals, and an increase in palmitoyl CoA oxidase activity. In conclusion, neither D79P nor D911P impaired reproductive function in rats when administered in the diet at levels that induce systemic toxicity, and the NOAEL for effects on reproduction in the rat is 0.5% for both D79P and D911P.     

Mechanisms of anabolic androgenic steroid modulation of alpha(1)beta(3)gamma(2L) GABA(A) receptors

Modulation of GABA(A) receptors induced by both anabolic androgenic steroids (AAS) and the benzodiazepine (BZ) site agonist, zolpidem, show equivalent dependence upon gamma subunit composition suggesting that both compounds may be acting at a shared allosteric site. Here we have characterized modulation induced by the AAS, 17alpha-methyltestosterone (17alpha-MeT), for responses elicited from alpha(1)beta(3)gamma(2L) GABA(A) receptors and compared it to modulation induced by the BZ site agonists, zolpidem and diazepam. For responses elicited by brief pulses of 20 microM GABA, both the AAS and the BZ site compounds significantly increased the peak current amplitudes and total charge transfer, although 17alpha-MeT was an appreciably weaker agonist than either diazepam or zolpidem at alpha(1)beta(3)gamma(2L) receptors. Neither class of modulator enhanced peak current amplitudes for responses elicited by mM concentrations of GABA. BZ site compounds altered time constants of deactivation, desensitization, and recovery from desensitization, however 17alpha-MeT had no overall effect on these parameters. Experiments in which 17alpha-MeT and BZ site ligands were applied concomitantly indicated that potentiation elicited by 17alpha-MeT and zolpidem were additive and that potentiation by 17alpha-MeT could be elicited in the presence of concentrations of flumazenil that blocked BZ potentiation. Finally, kinetic modeling suggests that while effects of 17alpha-MeT can be simulated by altering receptor affinity, the data for these alpha(1)beta(3)gamma(2L) receptors were best fitted by simulations in which 17alpha-MeT increases transitions into the singly liganded open state. Taken together, our results suggest that 17alpha-MeT does not act at the high-affinity BZ site, but may elicit some of its effects at the low affinity BZ site or at a novel site.