No description available.

No description available.

No description available.

ABSTRACT Background: The Peripheral Benzodiazepine Receptor (PBR) can be classified as a distinct receptor from the central benzodiazepine receptor. The PBR gene has been located to chromosome 22q13.31 in humans and has been found to consist of four exons, with the first and half of the fourth exon being untranslated to form the PBR protein. PBR is involved in numerous biological conditions including the regulation of cellular proliferation and apoptosis, steroidogenesis, heme biosynthesis, anion and porphyrin transport and mitochondrial functions such as oxidative phosphorylation and translocation of cholesterol from the outer to the inner mitochondrial membrane. Recent studies showed that the expression of PBR correlated with tumour malignancy and patient survival. Aim: The objectives of this research were to determine the expression pattern and level of PBR mRNA in various types of human normal and cancer tissues and to isolate the PBR protein.

Insomnia, the experience of poor quality or quantity of sleep, is a very common complaint. In the community estimates for the current prevalence of insomnia range from 15 to 28%. Pharmacological treatment of insomia is faster and more effective than other treatments, including psychotherapy, hypnosis, and so on. In pharmacological treatment, benzodiazepines (BZDs) and non-benzodiazepines, including zolpidem, are very common prescribing hypnotic usages because of more effectiveness and safer side-effect profiles. Our retrospective, current observational study is a chart review of 3,152 psychiatric outpatients, attempted to review adverse effects, specifically somnambulism and antegrade amnesia after these medications, to see whether or not, this is an infrequent occurrence in Taiwan population. Of a total 406 long-/intermitted-half-life BZD hypnotics users, 0.25% (1 of 406) reported incidence of somnambulism and anterograde amnesia. However, 5.1% (13 of 255) reported incidence of zolpidem-induced somnambulism and anterograde amnesia. It serves as a reminder for clinicians to inquire of spouses (bed parters) of the patients about any unusual behavior of parasomnia activities when prescribing zolpidem, specifically in Taiwan population.

Yes

No description available.

Abstract Non-benzodiazepine drugs such as zopiclone and zolpidem are alternatives to treatment of insomnia, but are recommended only for short-term treatment. The objectives of the study were to evaluate the prescribing patterns and usage of these drugs. Method: Data was collected from Clicks Rosebank Pharmacy. One hundred (100) patients presenting with prescriptions for either zolpidem or zopiclone were followed over a period of seven months and data was collected regarding: demographic characteristics of patients; drug and dose distribution; ICD10 codes; prescriber characteristics; period of use; and whether use was continuous or as needed (uninterrupted or interrupted). All data was collected from the Unisolv computer system. Over a period of one year, total prescriptions received for all drugs were compared to the total number of zopiclone/zolpidem prescriptions received to gauge whether there was any seasonal variation in hypnotic use. Results: In each age group, excluding 20 years and below, the number of females was greater than males. The mean age of all patients between the ages of 21 and 80 years was 53.1 years. Out of 100 patients, 85 (85%), used either zolpidem 10mg or zopiclone 7.5mg, which are the standard doses. The most common ICD 10 code observed was G47.0, Disorders of initiating and maintaining sleep [insomnias], occurring in 52 (52%) of 100 prescriptions. Of the 100 initial prescriptions, 68 (68%) were prescribed by General Practitioners, while 32 (32%) were prescribed by Specialists. Thirty of the 100 patients (30%) used one of the drugs for the full seven months; twenty two patients (22%) used one of the drugs for a period of one month or less; and the remaining 48 patients (48%) used a hypnotic for a total of two to six months. The number of patients who used a hypnotic in an interrupted manner, with each period of use of one month or less duration, was 34 (34%). The number of patients who used a hypnotic for at least one uninterrupted period of more than 1 month s duration was 66 (66%). Over a period of 12 months, prescriptions for either zolpidem or zopiclone represented 3.17% of total prescriptions. There was no significant seasonal fluctuation in hypnotic use. Conclusion: The majority of patients used one of the two hypnotics in an uninterrupted manner, and over a long term as well. Despite numerous cautions in the literature, these medications are still being prescribed and used in a manner contrary to existing guidelines.

Thesis (M.S.) in Nursing--University of Maine, 2004. / Includes vita. Includes bibliographical references (leaves 59-79).

The self-regeneration of stereocenters via stereolabile axially-chiral intermediates (SRSvSACI) is a synthetic strategy in which the configuration of a starting material, possessing only a single stereocenter, directs the formation of a chiral axis in an intermediate. The reaction proceeds stereospecifically, although the original stereocenter is destroyed through trigonalization. This is due to the stereochemical information encoded in the chiral axis, which is transformed into the configuration of a stereocenter in the product. In this research, we investigate the generation of axially chiral intermediates arising from both (S)-methyl lactate derivatives and 1,4-benzodiazepin-2,5-dione derivatives. For the deprotonation/alkylation of O-Bn and O-TBS substituted (S)-methyl lactate derivatives containing achiral oxazolidinones, we hypothesized that a twisted amide enolate featuring a chiral C(O-)-N axis could sufficiently impart stereochemical information and control the selectivity of the reaction. Previous work completed by Kobayashi showed in related compounds (E)- vs (Z)-enolate formation could be controlled through the identity of the 2'-oxygen substituent with –Bn affording the (E)-enolate and –TBS affording the (Z)-enolate. We investigated the utilization of achiral oxazolidinone moieties to selectively generate axial chiral intermediates that could then control the facial selectivity of sequential alkylations. Unfortunately, unforeseen synthetic difficulties prevented successful accomplishment of our project goals. We also utilized axially chiral intermediates in the generation of 3,3-disubstituted quinolone-2,4-diones. The target compounds serve as potentially useful drug scaffolds, yet synthetic access to them has remained limited due to the lack of commercial availability of the corresponding enantiopure quaternary substituted amino acids. Prior work in the Carlier group demonstrated the preferential (M)-conformer deprotonation demonstrated by 1,4-benzodiazepin-2,5-diones, and through the installation of an N4-tert-butyloxycarbonyl protecting group, we were able to take advantage of this preferential (M)-conformer deprotonation and generate 3,3-disubstituted quinolone-2,5-diones through an acyl-amino variant of the Chan rearrangement. In general, these reactions were highly enantioselective proceeding with little to no loss of enantiomeric excess. Finally, we collaborated with Professor Bloomquist to test the topical toxicity of selected ring-contracted products against adult Anopheles gambiae, the African vector of malaria. / Ph. D.