薬理と治療
Volume 40, Issue 2, 2012
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扉・目次
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DRUG PROFILE SERIES
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新たな切り札 選択的 β3アドレナリン受容体作動性過活動膀胱治療薬ミラベグロン(ベタニス錠 25 mg・50 mg)の基礎と臨床
40巻2号(2012);View Description Hide Description
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REVIEW
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ORIGINAL ARTICLES
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強力かつ持続的な新規アンジオテンシンAT1受容体ブロッカー Azilsartan の薬効薬理作用
40巻2号(2012);View Description Hide DescriptionObjective To clarify pharmacological properties of a novel angiotensinⅡ type 1 receptor blocker(ARB), azilsartan, we conducted several in vivo experiments using normal rats,hypertensive rats and dogs and type 2 diabetic rats exhibiting overt albuminuria.Methods We first evaluated in vivo antagonistic activities of orally administered azilsartan and launched ARBs, olmesartan medoxomil(O. M.)and candesartan cilexetil(C. C.)in normotensive rats. Second, we clarified antihypertensive effects of single or repeated administrations of these ARBs in spontaneously hypertensive rats (SHR), a model of essential hypertension. We also confirmed the antihypertensive effect of azilsartan in renal hypertensive dogs. In addition, we studied the insulin-sensitizing effect and the anti-albuminuria effect of azilsartan using SHR and Zucker diabetic fatty(ZDF)rats which exhibiting overt albuminuria,respectively. We also compared the effects of azilsartan with those of O. M. or C. C. Results Azilsartan inhibited angiotensinⅡ -induced pressor responses in normotensive rats, and its inhibitory effect is longer-lasting than those of O. M. and C. C. In SHRs, azilsartan reduced blood pressure more potently than O. M. and more persistently than O. M. and C.C. In renal hypertensive dogs, single oral administration of azilsartan at 0.3-3 mg/kg reduced BP, and it reduced even 24 hours after administration at 3 mg/kg. In a 2-week repeat dosing study in SHRs, azilsartan showed a more stable antihypertensive effect than O. M., and it more potently improved the glucose infusion rate, an indicator of insulin sensitivity, than O. M. Azilsartan also exerted more potent antiproteinuric effects than C. C. in ZDF rats.Conclusion These results suggest that azilsartan is a potent ARB that has a favourable profile as an antihypertensive agent. -
Enterococcus faecalis EC-12 含有乳性飲料によるスギ花粉症緩和効果―花粉曝露施設における試験―
40巻2号(2012);View Description Hide DescriptionBackground The incidence of seasonal allergic rhinoconjunctivitis triggered by cedar pollen (herewith referred to as cedar pollinosis)continues to increase in Japan, affecting 26.5% of the Japanese population. We evaluated a soft drink containing Enterococcus faecalis EC-12 with respect to its antiallergic effect on patients with cedar pollinosis. This study was performed using an environmental exposure unit(EEU), which assists in the development of effective therapeutic and preventive measures. Methods We recruited 20 patients with cedar pollinosis over a period of 2 years. We administered 200 mL of a drink containing EC-12 daily, for 8 weeks during the offseason for cedar pollen dispersion. The patients were exposed to pollen before and after the intake of the EC-12 drink to examine the subjective symptoms in the pollen exposure room and those during 5 days after the exposure. Results In the EEU,(a)nasal discharge and(b)itchy eyes decreased significantly after the intake of the EC-12 drink(a;p=0.041 at 90 min, b;p=0.034 at 120 min, p=0.038 at 150 min). Nasal obstruction and scratchy throat seemed to improve, and the amount of tears produced seemed to decrease. During 5 days after the exposure, the patients showed a significant difference in the following parameters:(c)disturbance in daily living activities,(d) itchiness of the eyes,(e)the amount of tears produced, and(f)drowsiness(c;p=0.037 on the night of the exposure, d;p=0.031 at Day 1, e;p=0.039 on the night of the exposure,f;p=0.048 on the night of the exposure, p=0.044 at Day 4). Sneezing fits and nasal obstruction seemed to improve. The mucous membrane swelling of the inferior concha on pollen exposure significantly improved after the intake of the drink(p=0.0007). Conclusions These results imply that continuing the intake of the EC-12 drink may alleviate symptoms and improve the quality of life in patients with cedar pollinosis.
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CASE REPORT
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Beneficial Effect of Etanercept in a Patient with Rheumatoid Arthritis and Diabetes Mellitus
40巻2号(2012);View Description Hide DescriptionA 70-year-old woman with both rheumatoid arthritis and type 2 diabetes had initiated etanercept 25 mg twice a week since May 2005. Following improvements in rheumatoid arthritis, etanercept was tapered to 25 mg/week by 6 month, and terminated one more year later. Initially she required 12 U/day of insulin to maintain HbA1c around 7.0% under prednisolone 6 mg/day. During the course, the doses of prednisolone and insulin were tapered, and terminated in May 2007. In October 2011, the both diseases were well controlled:CRP 0.02 mg/dL, ESR 7 mm/hr, CH50 37 U/mL, MMP-3 36.9 ng/mL, and HbA1c 5.9%. Anti-TNF-α agents such as etanercept appeared beneficial for patients having both rheumatoid arthritis and diabetes.
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