Canagliflozin (Invokana®)Canagliflozin (Invokana®) is a new antihyperglycemic agent approved in March 2013 for the treatment of type 2 diabetes. Canagliflozin was the first co-transporter inhibitor sodium glucose 2 (SGLT2) to be approved by the FDA.1 Per the 2014 ADA guidelines, metformin is the preferred initial therapy (if tolerated and not contraindicated) and insulin therapy with or without others should be considered in newly diagnosed patients with markedly symptomatic and/or elevated blood glucose or A1C levels. If noninsulin monotherapy at the maximum tolerated dose does not achieve or maintain target A1C over 3 months, a second oral agent (sulfonylurea, TZD, and DPP-4), a GLP-1 receptor agonist, or insulin.2 Pharmacology:2 Through SGLT2 inhibition, canagliflozin reduces the renal glucose threshold and increases urinary glucose excretion by interfering with glucose reabsorption through the proximal renal tubules. Pharmacokinetics:2 the oral bioavailability of canagliflozin is approximately 65. It reaches Tmax after 1-2 hours, reaches steady state in 4-5 hours. Canagliflozin is 99% protein bound. Eliminated renally in 33% (mainly metabolites) and fecally (41.5%). Dose: 2 The starting dose of canagliflozin is 100 mg orally once daily before the first meal of the day. If the patient tolerates 100 mg daily and has an eGFR of 60 ml/min/1.73 m2 or greater, the dose may be increased to 300 mg daily. Dose adjustment (renal impairment): In patients with an eGFR between 45 and 60 ml/min/1.73 m2, the canagliflozin dose is limited to 100 mg once daily, Canagliflozin should not be used in patients with eGFR less than 45 ml/min/1.73 m2. Contraindications: 2 hypersensitivity to canagliflozin. Severe renal failure, (...... half of the paper ...... 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 inadequately controlled with diet and exercise.6. P., Niskanen, L., Xie, J., ... & Meininger, G. (2013 Efficacy and safety of canagliflozin versus glimepiride in patients with type 2 diabetes adequately controlled with metformin (CANTATA-SU). : 52-week results of a randomized, double-blind, phase 3 non-inferiority trial, The Lancet 382(9896), 941-950.7. Schernthaner G, Gross JL, Rosenstock J, et al patients with type 2 diabetes who do not have adequate glycemic control with metformin plus a sulfonylurea doi
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