Mikhail Nasser
Endocrinology Division, OliveView-UCLA Medical Center, 14445 Olive View Dr, Sylmar, CA 91342, Clinical Professor of Medicine, David-Geffen Medical School, CA, USA.
Curr Drug Saf. 2014;9(2):127-32. doi: 10.2174/1574886309666140120100255.
Canagliflozin is a newly approved drug for the treatment of type 2 diabetes. This agent lowers blood glucose mainly by increasing urinary glucose excretion through inhibition of sodium glucose co-transporter 2 (SGLT2) in the kidneys. Data derived from randomized clinical trials lasting up to 52 weeks suggest that canagliflozin is generally well tolerated. The most common adverse effects are genital mycotic infections occurring in 11-15% of women exposed to canagliflozin versus 2-4% of those randomized to glimepiride or sitagliptin. In men, corresponding proportions are 8-9% versus 0.5-1%. Urinary tract infections (UTI) are slightly increased (5-7%) with the use of canagliflozin compared with placebo (4%). The risk of hypoglycemia associated with canagliflozin is marginally higher than placebo, but markedly increases when the drug is used in conjunction of insulin or sulfonylureas (SU), in patients with chronic kidney disease (CKD), and in the elderly. Worsening renal function and hyperkalemia may occur in patients using canagliflozin, particularly in patients with underlying CKD. Mild weight loss (mean 2-4 kg) and lowering of blood pressure represent 2 advantages of canagliflozin owing to its osmotic diuretic effect. However, the latter action may lead to postural hypotension and dizziness in susceptible subjects. Another concerning adverse effect of canagliflozin is an average 8% increase in plasma levels of low-density lipoprotein cholesterol (LDL-C) compared with placebo. Overall, canagliflozin is a useful addition for treatment of type 2 diabetes, but its safety needs to be established in long-term clinical trials.
卡格列净是一种新批准用于治疗2型糖尿病的药物。该药物主要通过抑制肾脏中的钠-葡萄糖协同转运蛋白2（SGLT2）增加尿糖排泄来降低血糖。长达52周的随机临床试验数据表明，卡格列净总体耐受性良好。最常见的不良反应是生殖器真菌感染，在接受卡格列净治疗的女性中发生率为11%-15%，而随机接受格列美脲或西格列汀治疗的女性中发生率为2%-4%。在男性中，相应比例分别为8%-9%和0.5%-1%。与安慰剂组（4%）相比，使用卡格列净会使尿路感染（UTI）略有增加（5%-7%）。与卡格列净相关的低血糖风险略高于安慰剂，但在与胰岛素或磺脲类药物（SU）联合使用时、在慢性肾脏病（CKD）患者以及老年患者中，低血糖风险会显著增加。使用卡格列净的患者可能会出现肾功能恶化和高钾血症，尤其是在有CKD基础疾病的患者中。由于其渗透性利尿作用，轻度体重减轻（平均2-4kg）和血压降低是卡格列净的两个优点。然而，后一种作用可能会导致易感人群出现体位性低血压和头晕。卡格列净另一个令人担忧的不良反应是与安慰剂相比，血浆低密度脂蛋白胆固醇（LDL-C）水平平均升高8%。总体而言，卡格列净是治疗2型糖尿病的一种有用药物，但需要通过长期临床试验来确定其安全性。
