头孢替唑钠、盐酸头孢甲肟在5%转化糖注射液中的配伍稳定性考察

目的考察注射用头孢替唑钠、注射用盐酸头孢甲肟分别与5%转化糖注射液配伍的稳定性,为临床合理用药提供依据。方法在室温(25±1)℃下,将两种注射用抗生素分别与5%转化糖注射液配伍,在8 h内,观察各配伍溶液的pH和外观变化,并采用HPLC法测定各配伍溶液中主药成分的相对含量。结果 8 h内,盐酸头孢甲肟、头孢替唑钠与5%转化糖注射液配伍后,头孢替唑钠的pH、外观和相对含量无明显变化;而盐酸头孢甲肟的pH及含量变化较大,配伍溶液颜色逐渐加深。结论在室温(25±1)℃条件下、8 h内,注射用头孢替唑钠与5%转化糖注射液的配伍液稳定;从医疗安全的角度考虑不提倡盐酸头孢甲肟与5%转化糖注射液配伍使用。     

莪术油葡萄糖注射液与17种药物配伍的稳定性

综述国内有关莪术油葡萄糖注射液与17种药物配伍的稳定性,通过检索文献资料,发现莪术油葡萄糖注射液与氨苄西林钠、阿洛西林钠、哌拉西林钠、头孢唑啉钠、头孢唑肟钠、头孢呋肟钠、头孢噻肟钠、奈替米星、克林霉素、氧氟沙星、利巴韦林、阿昔洛韦、Vit.C加地塞米松磷酸钠等配伍后,外观无变化,pH值变化不大,两药浓度均在初始浓度的90%以上,可以配伍;与头孢哌酮钠、头孢曲松钠、头孢拉定等配伍后,颜色变化明显,含量下降较多,不能配伍.     

注射用头孢噻吩钠与两种常用输液的配伍稳定性考察

目的：考察注射用头孢噻吩钠与0.9%氯化钠注射液、5%葡萄糖注射液的配伍稳定性。方法：分别测定0、0.5、1、2、3、4、5和6h各配伍溶液的pH值,观察配伍液外观,并用高效液相色谱法比较配伍液中头孢噻酚钠的含量变化。结论：在实验条件下,两种输液与头孢噻酚钠配伍基本稳定,可以作为头孢噻酚钠的溶煤。     

转化糖、转化糖电解质与常用抗菌药物配伍稳定性的文献分析

目的：研究转化糖、转化糖电解质作为溶媒与常用抗菌药物配伍的稳定性。方法检索中国期刊全文数据库1998年1月～2013年6月有关转化糖、转化糖电解质与常用抗菌药物配伍稳定性的报道。结果与转化糖配伍：①宜现配现用：美洛西林;②宜2h内用完：头孢硫脒;③宜4h内用完：阿洛西林、氨曲南;④配伍稳定：头孢唑林、头孢他啶、头孢哌酮钠、头孢替唑;⑤不宜配伍：头孢西丁、头孢甲肟。与转化糖电解质配伍：①宜4h内用完：头孢米诺、头孢曲松、头孢哌酮钠／舒巴坦钠阿奇霉素;②配伍稳定：哌拉西林他唑巴坦、洛美沙星;③不宜配伍：阿莫西林／舒巴坦与转化糖电解质最好不要配伍,如果要配伍宜在2h内用完,而头孢地嗪、头孢唑肟不宜与转化糖电解质配伍。结论转化糖与美洛西林、头孢硫脒、阿洛西林、氨曲南、头孢唑林、头孢他啶、头孢哌酮钠、头孢替唑,转化糖电解质与头孢米诺、头孢曲松、头孢哌酮钠／舒巴坦钠、阿奇霉素、哌拉西林他唑巴坦、洛美沙星、阿莫西林／舒巴坦配伍宜在规定的时间内用完;转化糖与头孢西丁、头孢甲肟不宜配伍;转化糖电解质与头孢地嗪、头孢唑肟不宜配伍。     

头孢哌酮钠与常用输液配伍的稳定性观察

本实验采用紫外分光光度法测定注射用头孢哌酮钠的含量及其与常用输液配伍的稳定性,结果表明:注射用头孢哌酮钠与生理盐水、注射用水、5%葡萄糖及10%葡萄糖溶液在室温下(25～30℃)配伍稳定,24小时内含量变化不大.本实验还提示此药物在弱酸条件下较为稳定,其实验结果可供临床配伍使用参考.     

注射用头孢噻酚钠与3种输液的配伍稳定性

摘要目的考察注射用头孢噻酚钠与果糖注射液、转化糖电解质注射液和木糖醇注射液配伍的稳定性。方法模拟临床用药浓度,在室温（20±1）℃下放置6 h,观察配伍液外观、pH变化,并用高效液相色谱法测定配伍液中头孢噻酚的含量变化。结果头孢噻酚钠与木糖醇注射液的配伍液0～6 h内含量、外观均无显著变化,6 h时pH下降0.5;头孢噻酚钠与转化糖电解质注射液的配伍液0～6 h内pH、外观、含量均无明显变化;头孢噻酚钠与果糖注射液的配伍液,0～6 h内pH、外观均无明显变化,2 h含量＞98%,6 h含量下降至95.71%。结论在实验条件下,3种输液与头孢噻酚钠配伍基本稳定,可以作为头孢噻酚钠的溶媒,头孢噻酚钠与果糖注射液配伍时宜在2 h内完成输注。     

莪术油葡萄糖注射液与7种抗菌药物的配伍稳定性

目的 观察莪术油葡萄糖注射液与7种常用抗菌药物配伍后的稳定性。方法 用紫外分光光度法测定莪术油葡萄糖注射液中主成分莪术醇6h内含量的变化，同时观察配伍溶液的外观并测定其pH值、微粒数以及细菌内毒素。结果 莪术油葡萄糖注射液与7种抗菌药物配伍后，样品液均无气体或沉淀产生；pH值、微粒数、色泽在6h内均无明显改变，室温下放置的配伍液6h时细菌内毒素检查也符合规定。与左氧氟沙星、哌拉西林钠、头孢唑啉钠、克林霉素、阿昔洛韦、氨苄西林钠配伍后6h内相对百分含量均＞90％；与头孢哌酮钠配伍含量下降最大，样品液由浅黄色变成深黄色；结论 莪术油葡萄糖注射液与左氧氟沙星、哌拉西林钠、克林霉素、阿昔洛韦、头孢唑啉钠、氨苄西林钠可配伍使用，不宜与头孢哌酮钠配伍。     

RP-HPLC法考察硫酸头孢噻利与奥美拉唑钠的配伍稳定性

目的观察硫酸头孢噻利(第4代头孢菌素类抗生素)与奥美拉唑钠(抗溃疡药)的配伍稳定性。方法用反相高效液相色谱法测定硫酸头孢噻利与奥美拉唑钠配伍后在不同温度下8 h内的相对百分含量,并考察其外观与pH值。结果硫酸头孢噻利与奥美拉唑钠配伍后,在4℃放置8 h、25℃放置3 h、37℃放置1 h,配伍溶液的外观、pH值及两者相对百分含量基本无变化。37℃放置2 h后,奥美拉唑钠相对百分含量变化约5%,配伍液不能使用。结论硫酸头孢噻利与奥美拉唑钠的配伍液在高温环境中1 h内稳定,2 h后稳定性差。     

注射用盐酸头孢甲肟与注射用阿昔洛韦的配伍稳定性考察

目的:考察注射用盐酸头孢甲肟与注射用阿昔洛韦在0.9%氯化钠注射液和5%葡萄糖注射液中的配伍稳定性。方法:在室温下观察盐酸头孢甲肟与注射用阿昔洛韦配伍后的外观及p H值变化,并采用高效液相色谱法测定两药的含量变化。结果:两药配伍后在6 h内外观及p H值均无明显变化,阿昔洛韦含量均大于97%,但头孢甲肟含量下降至79.41%。结论:注射用盐酸头孢甲肟不能与注射用阿昔洛韦在0.9%氯化钠注射液和5%葡萄糖中配伍使用。     

莪术油葡萄糖注射液与7种药物的配伍稳定性

目的观察莪术油葡萄糖注射液与7种常用药物配伍后的稳定性。方法用紫外分光光度法测定莪术油葡萄糖注射液中主成分莪术醇6h内含量的变化,同时观察配伍溶液的外观并测定其pH值。结果莪术油葡萄糖注射液与7种药物配伍后,样品液均无气体或沉淀产生;pH值随加入药物的不同而不同,但在6h内均无明显改变。与左氧氟沙星、哌拉西林钠配伍后6h内相对百分含量均>90%,与克林霉素、阿昔洛韦、氨苄西林钠、头孢唑啉钠配伍后6h内相对百分含量均>94%;与头孢哌酮钠配伍后莪术醇的含量下降最大,样品液为棕色。结论莪术油葡萄糖注射液与左氧氟沙星、哌拉西林钠、克林霉素、阿昔洛韦、氨苄西林钠、头孢唑啉钠配伍安全有效,但不宜与头孢哌酮钠配伍。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

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.

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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.

     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The 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.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

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.     

2-(Acetoxyphenyl)-(Z)-styryl sulfides as cyclooxygenase inhibitors

2-(Acetoxyphenyl)-(Z)-styryl sulfides are described as selective cyclooxygenase-2 (COX-2) inhibitors, useful for treating inflammation and COX-2-mediated disorders including neoplasia. 2-(Acetoxyphenyl)-(Z)-styryl sulfide is claimed to be the most potent COX inhibitor in the series with a COX-2 selectivity ratio of 33. This compound is also claimed to be superior to celecoxib (Celebrex^®, Pfizer) in inhibiting cell growth of colorectal carcinoma cells. In this evaluation, the COX inhibitory activity of this compound is compared to that previously disclosed for diarylheterocycles and 2-(acetoxyphenyl)alkyl sulfides. The validity of the DLD-1 cell line in the growth inhibition studies is questioned based on recent literature reports indicating the lack of COX-2 expression in this cell line.     

Sleep-disordered breathing with chronic opioid use

Chronic opioid use for pain relief or as substitution therapy for illicit drug abuse is prevalent in our societies. In the US, retail distribution of methadone and oxycodone has increased by 824 and 660%, respectively, between 1997 and 2003. μ-Opioids depress respiration and deaths related to illicit and non illicit chronic opioid use are not uncommon. Since 2001 there has been an emerging literature that suggests that chronic opioid use is related to central sleep apnoea of both periodic and non-periodic breathing types, and occurs in ～ 30% of these subjects. The clinical significance of these sleep-related abnormalities are unknown. This review addresses the present knowledge of control of ventilation mechanisms during wakefulness and sleep, the effects of opioids on ventilatory control mechanisms, the sleep-disordered breathing found with chronic opioid use and a discussion regarding the future research directions in this area.     

Drug targets for cognitive enhancement in neuropsychiatric disorders

The investigation of novel drug targets for treating cognitive impairments associated with neurological and psychiatric disorders remains a primary focus of study in central nervous system (CNS) research. Many promising new therapies are progressing through preclinical and clinical development, and offer the potential of improved treatment options for neurodegenerative diseases such as Alzheimer's disease (AD) as well as other disorders that have not been particularly well treated to date like the cognitive impairments associated with schizophrenia (CIAS). Among targets under investigation, cholinergic receptors have received much attention with several nicotinic agonists (α7 and α4β2) actively in clinical trials for the treatment of AD, CIAS and attention deficit hyperactivity disorder (ADHD). Both glutamatergic and serotonergic (5-HT) agonists and antagonists have profound effects on neurotransmission and improve cognitive function in preclinical experiments with animals; some of these compounds are now in proof-of-concept studies in humans. Several histamine H3 receptor antagonists are in clinical development not only for cognitive enhancement, but also for the treatment of narcolepsy and cognitive deficits due to sleep deprivation because of their expression in brain sleep centers. Compounds that dampen inhibitory tone (e.g., GABA_A α5 inverse agonists) or elevate excitatory tone (e.g., glycine transporter inhibitors) offer novel approaches for treating diseases such as schizophrenia, AD and Down syndrome. In addition to cell surface receptors, intracellular drug targets such as the phosphodiesterases (PDEs) are known to impact signaling pathways that affect long-term memory formation and working memory. Overall, there is a genuine need to treat cognitive deficits associated with many neuropsychiatric conditions as well as an increasingly aging population.