Harvard Medical School, Joslin Diabetes Center, One Joslin Place, Boston, MA 02115, USA.
Horm Metab Res. 2010 Jan;42(1):23-30. doi: 10.1055/s-0029-1241195. Epub 2009 Oct 27.
The bile acid sequestrant, colesevelam hydrochloride, is approved for glycemic control in adults with type 2 diabetes. In three double-masked, placebo-controlled studies, colesevelam hydrochloride 3.75 g/day demonstrated its glycemic-lowering properties when added to existing metformin-, insulin-, or sulfonylurea-based therapy in adults with inadequately controlled type 2 diabetes. This was a 52-week open-label extension study conducted at 63 sites in the United States and one site in Mexico to further evaluate the safety and tolerability of colesevelam hydrochloride in subjects with type 2 diabetes. All subjects who completed the three double-masked, placebo-controlled studies were eligible to enroll in this open-label extension. In total, 509 subjects enrolled and received open-label colesevelam hydrochloride 3.75 g/day for 52 weeks. Safety and tolerability of colesevelam hydrochloride was evaluated by the incidence and severity of adverse events. In total, 360 subjects (70.7%) completed the extension. Of the safety population, 361 subjects (70.9%) experienced an adverse event, most (88.1%) being mild or moderate in severity. Fifty-six adverse events (11.0%) were drug-related; the most frequent drug-related adverse events were constipation and dyspepsia. Thirty-five subjects (6.9%) discontinued due to an adverse event. Fifty-four subjects (10.6%) experienced a serious adverse event; only one was considered drug-related (diverticulitis). Seventeen subjects (3.3%) experienced hypoglycemia; most episodes were mild or moderate in severity. Glycemic improvements with colesevelam hydrochloride were seen without change in weight over 52 weeks (0.2 kg mean reduction from baseline). Colesevelam hydrochloride was safe and well-tolerated as long-term therapy for patients with type 2 diabetes.
胆酸螯合剂考来维仑盐酸盐被批准用于 2 型糖尿病成人患者的血糖控制。在三项双盲、安慰剂对照研究中，当考来维仑盐酸盐 3.75g/天添加到二甲双胍、胰岛素或磺酰脲类药物治疗的血糖控制不佳的 2 型糖尿病成人患者中时，显示出其降低血糖的特性。这是一项在美国 63 个地点和墨西哥的一个地点进行的为期 52 周的开放性标签扩展研究，旨在进一步评估考来维仑盐酸盐在 2 型糖尿病患者中的安全性和耐受性。所有完成三项双盲、安慰剂对照研究的受试者均有资格参加这项开放性标签扩展研究。共有 509 名受试者入组，并接受考来维仑盐酸盐 3.75g/天的开放性标签治疗 52 周。通过不良反应的发生率和严重程度评估考来维仑盐酸盐的安全性和耐受性。共有 360 名受试者（70.7%）完成了扩展研究。在安全性人群中，361 名受试者（70.9%）发生了不良反应，大多数（88.1%）为轻度或中度严重程度。56 例（11.0%）不良反应与药物相关；最常见的药物相关不良反应为便秘和消化不良。因不良反应而停药的有 35 例（6.9%）。54 例（10.6%）发生严重不良事件；只有 1 例被认为与药物相关（憩室炎）。17 例（3.3%）发生低血糖；大多数事件为轻度或中度严重程度。考来维仑盐酸盐治疗 2 型糖尿病患者的长期安全性和耐受性良好，血糖改善而体重无变化（与基线相比平均减少 0.2kg）。
