Post Graduate Department of Pharmacology and Research Centre, H. S. K. College of Pharmacy, Bagalkot, Karnataka 587101, India.
Mol Cell Biochem. 2011 Aug;354(1-2):135-40. doi: 10.1007/s11010-011-0812-7. Epub 2011 Apr 12.
Gastrointestinal symptoms are fairly common in diabetes mellitus. Glimepride, is a latest second generation sulfonylurea used for the treatment of type II diabetes mellitus, is a insulin secrectagogue; indirectly, it also increases insulin secretion and its specific effect on pancreatic ATP-dependent K(+) channel inhibition. Esomeprazole, the (S)-isomer of omeprazole, is the first proton pump inhibitors developed as a single isomer for the treatment of acid-peptic diseases by specific inhibition of H(+)/K(+)-ATPase in gastric parietal cell. Since there is possibility for drug interaction leading to decreased activity of glimepride, the present study was conducted to evaluate the effect of the combination. Studies in normal and alloxan induced diabetic rats were conducted with oral doses of 135 μg/kg bd.wt. of glimepride, 3.6 mg/kg bd.wt. of esomeprazole, and their combination with adequate washout periods in between treatments. Studies in normal rabbits were conducted with doses 70 μg/1.5 kg bd. wt. of glimepride, 1.8 mg/1.5 kg bd. wt. of esomeprazole, and their combination given orally. The blood samples were collected at 0, 1, 2, 4, 8, 12, 18, 24 h and analyzed for glucose levels by GOD/POD method and insulin in diabetic rats by radioimmunoassay methods. Glimepride produced hypoglycaemic/antidiabetic activity in normal and diabetic rats activity with peak activity maximum at 4 h and hypoglycemic activity in normal rabbits maximum at 4 h and esomeprazole increases the insulin levels in diabetic rats. The study also suggests the necessity to readjust the dose of glimepride, when used concomitantly with esomeprazole.
胃肠道症状在糖尿病中相当常见。格列美脲是一种最新的第二代磺酰脲类药物,用于治疗 2 型糖尿病,是一种胰岛素分泌促进剂;它还间接增加胰岛素的分泌,并对胰腺 ATP 依赖性钾 (K+) 通道有特异性抑制作用。埃索美拉唑是奥美拉唑的 (S)-异构体,是第一个质子泵抑制剂,作为单一异构体开发,通过胃壁细胞中 H(+)/K(+)-ATP 酶的特异性抑制来治疗酸相关疾病。由于存在导致格列美脲活性降低的药物相互作用的可能性,因此进行了本研究以评估联合用药的效果。在正常和四氧嘧啶诱导的糖尿病大鼠中进行了研究,给予格列美脲 135 μg/kg 体重、埃索美拉唑 3.6 mg/kg 体重的口服剂量,在治疗之间有足够的洗脱期。在正常兔中进行了研究,给予格列美脲 70 μg/1.5 kg 体重、埃索美拉唑 1.8 mg/1.5 kg 体重的口服剂量。在 0、1、2、4、8、12、18、24 h 时采集血样,通过 GOD/POD 法测定葡萄糖水平,通过放射免疫分析法测定糖尿病大鼠的胰岛素水平。格列美脲在正常和糖尿病大鼠中产生降血糖/抗糖尿病活性,最大活性在 4 h 时达到峰值,在正常兔中最大活性在 4 h 时达到峰值,埃索美拉唑增加糖尿病大鼠的胰岛素水平。该研究还表明,当与埃索美拉唑同时使用时,有必要调整格列美脲的剂量。