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1.
头孢唑林对阿米卡星在兔体内的药动学影响 总被引:3,自引:1,他引:2
采用微量微生物法对阿米卡星(AMK)单用及与头孢唑林(CEZ)合用后兔体内AMK血药浓度进行测定,药时数据用MCPKP软件经IBM 计算机处理,并对两组药动学参数进行了统计学处理,结果表明CEZ对AMK的药动学有显著的影响。 相似文献
2.
氨苄青霉素对丁胺卡那霉素药动学的影响 总被引:2,自引:1,他引:1
本文采用微量微生物法对AMK单用及AMK与AMP合用后,兔体内AMK血、尿药浓度进行测定;药时数据用MCPKP软件经IBM计算机处理,并对两组药动学参数进行了统计学处理。结果表明AMP对AMK的药动学有显著的影响。 相似文献
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BM13505是新合成的血栓烷受体拮抗剂,BM135050.45和0.23mg/kgiv延长大鼠颈动脉血管阻塞时间(p<0.001和p<0.01).BM135052mg/kgiv有效地防止AA4mg/kg所致的大鼠脑血栓形成(p<0.01)。BM1350510mg/kgip可防止AA诱导的小鼠肺部栓塞(p<0.01)。该药可延长小鼠尾出血时间。BM13505显著抑制AA诱导的兔血小板聚集,半数抑制浓度IC_(50)为0.17Vmol/L,对ADP和胶原诱导的血小板聚集无影响。BM13505降低兔血小板及小鼠血浆中TXB_2水平,对血小板cAMP水平无影响。在不远的将来,BM13505可能会发展成一种理想的抗血小板药及抗血栓药。 相似文献
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双氯灭痛在正常人体内的药物动力学研究 总被引:9,自引:3,他引:6
采用反相高效液相色谱法测定了10例健康人单剂量口服75mg双氯灭痛片剂后血浆药浓度,研究了该药物在中国人体内药物动力学。经用PKBP-N_1程序包在计算机上拟合计算表明,双氯灭痛口服给药多数人表现为二房室模型。其主要药动学参数分别为:T_(α1/2)=0.40±0.11h,T_(β1/2)=1.77±0.5h,T_(max)=1.78±0.32h,C_(max)=1.87±0.9μg/ml,AUC=3.81±1.7μg/(ml·h)。结果表明,中国人体内的药动学参数与所报道的外国人体内相似。 相似文献
5.
应用Bayesian反馈法预测阿替洛尔药物动力学参数及血药浓度 总被引:5,自引:2,他引:3
应用Bayesian反馈法预测21例高血压病人,口服阿替洛尔的个体药动学参数及稳态血药浓度(Cpss)并与经典药动学方法估算结果作比较,结果表明本法的T1/2为6.0±1.7h,Vd为1.43±0.13L/kg,CL为172±34ml/(h·kg);经典法的T1/2为6.8±2.4h,Vd为1.45±0.56L/kg,CL为164±85ml/(h·kg)。两者无显著性差异(P>0.05)。两法所测得Cpss有较好相关性(r=0.993)。 相似文献
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血肌酐值法预测地高辛个体化给药方案 总被引:1,自引:0,他引:1
在地高辛常规监测中,用血肌酐值法预测个体化药动学参数和给药方案。结果表明,84例病人的地高辛药物动力学参数预测值为,CL76±21ml/(kg·h),Vd7.05±1.20L/kg,T1/266±7h。预测的个体化剂量为3.1±0.9μg/(kg·d),预测的稳态血药浓度(C_(ss))为1.24±0.38μg/L,与实测C_(ss)1.2±0.4μg/L比较,差异无显著性(P>0.05)。 相似文献
8.
高糖增强兔血管平滑肌细胞对内皮素-1的增殖反应性(英文) 总被引:2,自引:0,他引:2
观察高糖对内皮素-1(ET-1)促兔主动脉血管平滑肌细胞(VSMC)增殖的影响.方法: VSMC分别培养于含正常葡萄糖、高糖或高渗(5.5,25,葡萄糖 5.5+甘露醇 19.5 mmol·L-1)的培养基中[3H]胸腺嘧啶掺入法检测DNA合成速率,蛋白质印迹法检测磷酸化 p44/42 MAPK的表达.结果:在 10至 10-8mol·L-1浓度范围内, ET-1以浓度依赖方式增加 VSMC的[3H]胸腺嘧啶掺入及磷酸化p44/42 MAPK的表达,从 10-11到 10-8mol·L-1,培养于高糖的 VSMC对相同浓度 ET-1的增殖反应性高于正常糖或高渗培养条件下的VSMC(P< 0.05,或 P< 0.01),而在后两种条件下,VSMC对ET-1的增殖反应无显著差别.同样,在高糖条件下,ET-1诱导的VSMC磷酸化p44/42MAPK的表达较正常糖和高渗VSMC增加 60%-65%结论:高糖增强VSMC对ET-1的增殖反应性,可能与磷酸化的 p44/42 MAPK高表达有关 相似文献
9.
目的探讨钙调神经磷酸酶(CaN)依赖的信号通路在血管紧张素Ⅱ(AngⅡ)刺激的乳鼠心肌成纤维细胞(FBs)增殖中的作用。方法以培养的FBs为模型,用AngⅡ刺激FBs外Ca2+入流,环抱素A(CsA)阻断CaN信号通路,维拉帕米(Ver)阻断FBs钙通道,检测FBs CaN、丝裂素活化蛋白激酶(MAPK)、蛋白激酶 C(PKC)活性,用[3H]-亮氨酸及[3H]-胸腺嘧啶参入量作为反应 FBs增殖的指标。结果Aug Ⅱ刺激组FBs蛋白核酸合成速率明显增高,与对照组相比差异有显著性(P<0.01);CsA及Ver能明显抑制Ang Ⅱ介导的FBs蛋白核酸合成速率增高,与AngⅡ血刺激组相比差异有显著性( P< 0. 01)。同时发现 Ang Ⅱ刺激组 CaN、PKC活性与对照 FBs相比差异有显著性( P< 0. 05或 P<0.01)。 CsA和Ver抑制AngⅡ介导的 FBs CaN活性增高,Ver抑制Ang Ⅱ介导的FBsPKC活性的增高。结论 CaN信号通路在AngⅡ刺激的FBs增殖中起重要作用,但CaN信号通路不是AngⅡ介导FBs的增殖的唯一信号通路,以MAPK为核心的信号通路亦参与了AngⅡ刺激的FBs增殖。 相似文献
10.
粉防己碱对自发性高血压大鼠血管平滑肌细胞增殖及对PDGF-B,bFGF和相关癌基因表达的影响 总被引:12,自引:0,他引:12
用[3H]胸腺嘧啶核苷([3H]TdR)参入法,电镜,免疫组化,原位杂交方法,在自发性高血压大鼠(SHR)观察了粉防己碱(Tet,0.03μmol·kg-1·d-1×8周ig)对血管平滑肌细胞(VSMC)增殖的作用及对生长因子PDGF-B,bFGF的抗原表达及其相关癌基因c-sis,c-mycmRNA表达的影响.结果发现:Tet在降低SHR血压(P<0.01)同时,能减少VSMC的线粒体,粗面内质网和[3H]TdR参入量(P<0.01),并能逆转VSMC增殖时PDGF-B,bFGF抗原(P<0.05)及c-sis,c-mycmRNA的表达增强.提示:Tet抑制SHR的VSMC增殖与生长因子及癌基因调控的分子生物学机制有关 相似文献
12.
Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.
Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.相似文献
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Petrikovics I McGuinn WD Sylvester D Yuzapavik P Jiang J Way JL Papahadjopoulos D Hong K Yin R Cheng TC DeFrank JJ 《Drug delivery》2000,7(2):83-89
This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine. 相似文献
16.
《Critical reviews in toxicology》2013,43(5-6):327-369
AbstractThe uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors. 相似文献
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《Expert opinion on investigational drugs》2013,22(1):79-86
Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation. 相似文献
18.
Chang Min Kim Kun Ho Son Sung Hwan Kim Hyun Pyo Kim 《Archives of pharmacal research》1991,14(4):305-310
In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins
from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins. 相似文献
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