Safety and Antihypertensive Effect of Selara® (Eplerenone): Results from a Postmarketing Surveillance in Japan.

Prospective postmarketing surveillance of Selara (eplerenone), a selective mineralocorticoid receptor antagonist, was performed to confirm its safety and efficacy for hypertension treatment in Japan. The change in blood pressure after initiation of eplerenone treatment was also examined. Patients with essential hypertension who were eplerenone-naïve were recruited regardless of the use of other antihypertensive drugs. For examination of changes in blood pressure, patients were excluded if eplerenone was contraindicated or used off-label. Patients received 50-100 mg of eplerenone once daily and were observed for 12 weeks. No treatments including antihypertensive drugs were restricted during the surveillance period. Across Japan, 3,166 patients were included for safety analysis. The incidence of adverse drug reactions was 2.4%. The major adverse drug reactions observed were hyperkalemia (0.6%), dizziness, renal impairment, and increased serum potassium (0.2% each). The mean systolic blood pressure decreased from 152.1 ± 19.0 mmHg to 134.8 ± 15.2 mmHg at week 12, and the mean diastolic blood pressure decreased from 85.8 ± 13.7 mmHg to 77.7 ± 11.4 mmHg. There were no significant new findings regarding the type or incidence of adverse reactions, and eplerenone had a clinically significant antihypertensive effect, leading to favorable blood pressure control.

[The early rehabilitation in children with Down. Paying special attention to shuffling and comorbidities of developmental disorder].

OBJECTIVE: There have been many reports on the effects of early rehabilitation in children with Down syndrome, which have demon- strated that early intervention improves motor skill acquisition and prevents a shuffling gait in these children. With regard to the mental development and mental health of these children, they are known to be friendly and social but some experience difficulties with nursing. Recently there have been a few reports on comorbidities of developmental disorders in Down syndrome. In the present research we studied both the motor and mental developments in children with Down syndrome, paying special attention to the shuffling gait and the comorbidi- ties of developmental disorder. METHODS: Clinical records of 121 children with Down syndrome (age, 1-11 years; mean age, 3.8 years), who visited the Yokohama rehabilitation center, were investigated. RESULTS: Despite early intervention, we found that 14 patients (11.9%) exhib- ited a shuffling gait. Concerning the comorbidities of the psychiatric developmental disorder, 21 patients (17.4%) had autism spectrum disorder (ASD)-like characteristic. The children with a shuffling gait appeared slow with regard to motor developmental milestones. They also had ASD-like characteristics. CONCLUSIONS: Children with Down syndrome needed early rehabilitation not only for its motor skill effects but also for mental support. In spite of early intervention, those with a shuffling gait needed special care owing to the comorbidities such as ASD-like characteristics. More research is needed to establish the prognosis of Down syndrome.

Enzymatic synthesis of a DNA triblock copolymer that is composed of natural and unnatural nucleotides.

DNA molecules have come under the spotlight as potential templates for the fabrication of nanoscale products, such as molecular-scale electronic or photonic devices. Herein, we report an enhanced approach for the synthesis of oligoblock copolymer-type DNA by using the Klenow fragment exonuclease minus of E. coli DNA polymerase I (KF(-) ) in a multi-step reaction with natural and unnatural nucleotides. First, we confirmed the applicability of unnatural nucleotides with 7-deaza-nucleosides-which was expected because they were non-metalized nucleotides-on the unique polymerization process known as the "strand-slippage model". Because the length of the DNA sequence could be controlled by tuning the reaction time, analogous to a living polymerization reaction on this process, stepwise polymerization provided DNA block copolymers with natural and unnatural bases. AFM images showed that this DNA block copolymer could be metalized sequence-selectively. This approach could expand the utility of DNA as a template.

Internal radiation exposure of Ground Self-Defense Force members involved in the management of the Fukushima Nuclear Power Plant disaster.

When the Great East Japan Earthquake occurred on March 11, 2011, the Ground Self-Defense Force (GSDF) was dispatched nationally to Northeast area in Japan. The highly trained GSDF members were simultaneously assigned to various missions for the Fukushima Nuclear Power Plants disaster. The missions of GSDF terminated on August 31, 2011. Special medical examinations were conducted for the members as they returned to each military unit. GSDF members who were assigned to the nuclear power plant were at risk of radiation exposure; therefore, pocket dosimeters were used to assess external radiation exposure. A few months after the mission was terminated, measurements of internal radiation exposure were performed. This is the first report of the internal exposure of GSDF members who worked in the restricted radiation contamination area. Here, we report the amounts of internal and external exposure of and the equipment used by the GSDF members.

Preparation of L-vancosamine-related glycosyl donors.

An improved practical synthesis of L-vancosamine-related glycosyl donors is described. The key steps include (1) stereoselective addition of methylcerium reagent to oximino ether and (2) stereoselective hydrogenation of exocyclic unsaturated glycoside in the presence of Wilkinson catalyst with C(5) inversion to give L-vancosamine derivatives. Three glycosyl donors were prepared, and their reactivities in the aryl C-glycoside formation were compared. Conversion of primary amine and azide to the corresponding N,N-dimethyl derivative is also described.