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Benzodiazepines medazepam and midazolam are activators of pregnane X receptor and weak inducers of CYP3A4: Investigation in primary cultures of human hepatocytes and hepatocarcinoma cell lines.

Friday, May 21st, 2010

In conclusion, Alprazolam, Bromazepam, Chlordiazepoxide, Clonazepam, Di azepam, Lorazepam, Nitrazepam, Oxazepam, Tetrazepam and Triazolam can be considered as safe drugs in term of their inability to induce PXR- and AhR-dependent cytochrome P450 enzymes CYP1A2 and CYP3A4. Medazepam and Midazolam slightly activated pregnane X receptor and displayed weak potency to induce CYP3A4 mRNA in human hepatocytes.
PMID: 20080160 [PubMed – as supplied (more…)

Erratum to: Validating a human model for anxiety using startle potentiated by cue and context: the effects of alprazolam, pregabalin, and diphenhydramine

Monday, April 26th, 2010

Content Type Journal ArticleCategory ErratumDOI 10.1007/s00213-010-1837-4Authors
J. M. P. Baas, Utrecht University Department of Experimental Psychology, Faculty of Social S ciences Van Unnik Building, Heidelberglaan 2 3584 CS Utrecht The NetherlandsN. Mol, Utrecht University Department of Experimental Psychology, Faculty of Social Sciences Van Unnik Building, Heidelberglaan 2 3584 CS Utrecht The NetherlandsJ. L. Kenemans, Utrecht University (more…)

Experimental design for optimization of microwave-assisted extraction of benzodiazepines in human plasma.

Monday, March 8th, 2010

Authors: Fernández P, Vázquez C, Lorenzo RA, Carro AM, Alvarez I, Cabarcos P
A simple and fast microwave-assisted-extraction (MAE) method has been evaluated as an alternative to solid-phase e xtraction (SPE) for the determination of six benzodiazepines widely prescribed in European countries (alprazolam, bromazepam, diazepam, lorazepam, lormetazepam and tetrazepam) in human plasma. For MAE optimization a Doehlert experimental design (more…)

Discovery That Viagra Enhances Fetal Growth In Female Sheep May Have Human Implications

Thursday, March 4th, 2010

A joke among two Texas AgriLife Research scientists later turned into a fully-funded study. Viagra can aid fetal development in female sheep. Female sheep (ewes) are an agriculturally important species, which can serve as an excellent animal model for studying the physiology of human pregnancy, the researchers said… (Source: Biology / Biochemistry News From Medical N ews Today)

Benzodiazepines medazepam and midazolam are activators of pregnane X receptor and weak inducers of CYP3A4: Investigation in primary cultures of human hepatocytes and hepatocarcinoma cell lines.

Monday, March 1st, 2010

In conclusion, Alprazolam, Bromazepam, Chlordiazepoxide, Clonazepam, Diazepam, Lorazepam, Nitrazepam, Oxazepam, Tetrazepam and Triazolam can be considered as safe drugs in term of their inability to induce PXR- and AhR-dependent cytochrome P450 enzymes CYP1A2 and CYP3A4. Medazepam and Midazolam slightly activated pregnane X receptor and displayed weak potency to induce CYP3A4 mRNA in human hepatocytes.
PMI D: 20080160 [PubMed – as supplied (more…)

Validating a human model for anxiety using startle potentiated by cue and context: the effects of alprazolam, pregabalin, and diphenhydramine

Wednesday, February 17th, 2010

Conclusion  Even though fear-potentiated startle may be used to translate preclinical evidence to human populations, methodological issues
still hamper the application of this model to early screening of putative anxiolytic drugs.

Content Type Journal ArticleCategory Original InvestigationDOI 10.1007/s00213-009-1516-5Authors
J. M. P. Baas, Utrecht University Department of Experimental Psychology, Faculty of Social Sciences (more…)

A comparison of the effects of a subtype selective and non-selective benzodiazepine receptor agonist in two CO2 models of experimental human anxiety

Tuesday, February 16th, 2010

In conclusion, our results show that zolpidem shows some anxiolytic efficacy in the 7.5% CO2 model, similar to alprazolam, and this is the first report of such an effect of zolpidem in a model of anxiety. These and other studies of benzodiazepines in clinical and volunteer studies suggest a definite role of the GABA-A rec eptor in CO2-induced anxiety, and it would be of interest to examine other GABA-A receptor subtype selective drugs, which (more…)

Validated LC-MS/MS assay for the quantitative determination of vardenafil in human plasma and its application to a pharmacokinetic study.

Tuesday, February 16th, 2010

Authors: Lake ST, Altman PM, Vaisman J, Addison RS
A sensitive high-performance liquid chromatography-tandem mass spectrometric (HPLC-MS/MS) assay has been developed for the quantitative analysis of vardenafil in hum an plasma. Vardenafil and the internal standard, alprazolam, were extracted from 0.2 mL aliquots of alkalinized plasma by a single solvent extraction into hexane : dichloromethane. Reversed-phase chromatographic separation was (more…)

Modulation of human risky decision making by flunitrazepam

Monday, February 15th, 2010

C onclusions  At sufficiently high do ses, flunitrazepam can engender increases in risky decision making. Globally, these changes appear
similar to previous effects we have observed after acute administration of alcohol and alprazolam. As suggested by the EVM
outcomes, the mechanisms underlying the changes in risky decision making are more similar to alprazolam than alcohol.

Content Type Journal ArticleCategory Original InvestigationDOI (more…)

Limitations to animal data on sildenafil citrate (Viagra) in the human risk assessment

Thursday, February 11th, 2010

To the Editor: The article titled Sildenafil citrate (Viagra) impairs fertilization and early embryo development in mice by Glenn et al. was of great interest. However, the presented data should be clarified from a teratological point of view, as it is insufficient for any further toxicological evaluation, in particular the human risk assessment. Without recording the initial number of females selected to each examined group, it is impossible (more…)

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