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Essay / Treating diabetes with metformin - 1229
Canagliflozin (Invokana®)Canagliflozin (Invokana®) is a new antihyperglycemic agent approved in March 2013 for the treatment of type 2 diabetes. Canagliflozin was the first inhibitor of sodium-glucose cotransporter 2 (SGLT2) to be approved by the FDA.1 According to the 2014 ADA guidelines, metformin is the preferred initial treatment (if tolerated and not contraindicated), and insulin therapy with or without other These agents should be considered in newly diagnosed patients with markedly symptomatic and/or elevated blood glucose or HbA1C levels. If non-insulin monotherapy at the maximum tolerated dose does not achieve or maintain the A1C goal for 3 months, a second oral agent (sulfonylurea, TZD and DPP-4), a GLP-1 receptor agonist or insulin should be added.2 Pharmacology:2 By inhibiting SGLT2, canagliflozin reduces the renal glucose threshold and increases urinary glucose excretion by interfering with glucose reabsorption in the proximal renal tubules. Pharmacokinetics:2 Oral bioavailability of canagliflozin is approximately 65. Reaches Tmax after 1-2 hours, reaches steady state in 4-5 hours. Canagliflozin is 99% protein bound. Eliminated by renal route 33% (mainly metabolites) and fecal route (41.5%). Dose: 2 The starting dose of canagliflozin is 100 mg PO once daily before the first meal of the day. If the patient tolerates 100 mg per day and has an eGFR of 60 mL/min/1.73 m2 or greater, the dose can be increased to 300 mg per day. Dose adjustment (renal impairment): In patients with an eGFR of 45 to 60 mL/min/1.73 m2, the dose of canagliflozin is limited to 100 mg once daily, canagliflozin should not be used in patients with an eGFR less than 45 mL/min/1.73 m2. Contraindications: 2 hypersensitivity to canagliflozin. Severe kidney failure, (...... middle of article......5. Stenlöf, K., Cefalu, WT, Kim, KA, Alba, M., Usiskin, K., Tong, C ., ... & Meininger, G. (2013). Efficacy and safety of canagliflozin monotherapy in subjects with type 2 diabetes mellitus insufficiently controlled by diet and exercise.6. ., Niskanen, L., Xie, J., ... & Meininger, G. (2013) Efficacy and safety of canagliflozin compared to glimepiride in patients with type 2 diabetes insufficiently controlled by metformin (CANTATA). -SU): 52-week results from a randomized, double-blind, phase 3 non-inferiority trial, The Lancet, 382(9896), 941-950.7, Schernthaner G, Gross JL, Rosenstock J, et al. with type 2 diabetes who do not have adequate glycemic control with metformin and a sulfonylurea. doi.