Sitazuca MH

Adults w/ type 2 DM as adjunct to diet & exercise to improve glycaemic control in patients inadequately controlled on max tolerated dose of metformin alone, metformin & sulphonylurea, metformin & PPARγ agonist, or those already being treated w/ combination of sitagliptin & metformin; as triple combination therapy w/ sulphonylurea or PPARγ agonist (ie, thiazolidinedione). Add-on to insulin (ie, triple combination therapy) as adjunct to diet & exercise to improve glycaemic control in patients when stable dose of insulin & metformin alone do not provide adequate glycaemic control.

Individualized dose. Adult w/ normal renal function (GFR ≥90 mL/min): Patient inadequately controlled on metformin alone, dual combination therapy w/ or w/o insulin Usual starting dose: Sitagliptin 50 mg bid (100 mg total daily dose) + metformin dose already being taken. Patient switching from co-administration of sitagliptin & metformin Initiate at dose of sitagliptin & metformin already being taken. Renal impairment Max daily dose of metformin: Divided into 2-3 daily doses. GFR 60-89 mL/min Max daily dose: Sitagliptin 100 mg & metformin 3,000 mg, 45-59 mL/min Max daily dose: Sitagliptin 100 mg & metformin 2,000 mg. Starting dose is ½ of max dose of metformin, 30-44 mL/min Max daily dose: Sitagliptin 50 mg & metformin 1,000 mg. Starting dose is ½ of max dose of metformin.

Should be taken with food.

Hypersensitivity. Any type of acute metabolic acidosis (eg, lactic acidosis, diabetic ketoacidosis); diabetic pre-coma; acute conditions w/ potential to alter renal function eg, dehydration, severe infection, shock; acute or chronic disease which may cause tissue hypoxia eg, cardiac or resp failure, recent MI. Acute alcohol intoxication, alcoholism. Intravascular administration of iodinated contrast agents. Severe renal failure (GFR <30 mL/min). Hepatic impairment. Breast-feeding.

Serious hypersensitivity reactions including anaphylaxis, angioedema & exfoliative skin conditions including SJS. Not to be used in patients w/ type I diabetes & for treatment of diabetic ketoacidosis; severe infection, or serious accident. Discontinue treatment if pancreatitis; hypersensitivity reaction; bullous pemphigoid is suspected; at the time of surgery under general, spinal or epidural anaesth; prior to or at the time of imaging procedure & not restarted until at least 48 hr after, provided that renal function has been re-evaluated & found to be stable; acute pancreatitis is confirmed. Discontinue immediately if acidosis of either form occurs. Temporarily discontinue treatment in case of dehydration (severe vomiting, diarrhoea, fever or reduced fluid intake); during conditions w/ potential to alter renal function. Discontinue metformin if lactic acidosis symptoms are suspected. Excessive alcohol intake, hepatic insufficiency, inadequately controlled diabetes, ketosis, prolonged fasting & any conditions associated w/ hypoxia. Risk for hypoglycaemia. May increase risk of severe joint pain. Patients w/ history of pancreatitis. Assess GFR before treatment initiation & regularly thereafter (at least annually). Evaluate promptly for evidence of ketoacidosis or lactic acidosis including serum electrolytes & ketones, blood glucose & pH, lactate, pyruvate, & metformin levels. Concomitant use w/ medicinal products that can acutely impair renal function (eg, anti-hypertensives, diuretics, NSAIDs); may cause lactic acidosis. Not to be used concomitantly w/ alcohol. Take into account dizziness & somnolence when driving or using machines. Not to be used in hepatic impairment. Not to be used during pregnancy & lactation. Not to be used in childn & adolescents 10-17 yr. Ped patients <10 yr. Elderly (assess renal function more frequently eg, every 3-6 mth).

Hypoglycaemia; nausea, flatulence, vomiting. Exfoliative skin conditions including SJS.

Increased risk of lactic acidosis w/ alcohol; NSAIDs including selective COX II inhibitors, ACE inhibitors, AIIAs & diuretics especially loop diuretics. Concomitant use w/ iodinated contrast agents. Increase systemic exposure of drugs that interfere w/ common renal tubular transport systems involved in renal elimination of metformin eg, organic cationic transporter-2/multidrug & toxin extrusion inhibitors (eg, ranolazine, vandetanib, dolutegravir, cimetidine). Concomitant use w/ glucocorticoids, β2 agonists & diuretics. Decreased blood glucose level w/ ACE inhibitors. Sitagliptin: Possible alteration of pharmacokinetics w/ potent CYP3A4 inhibitors (ie, ketoconazole, itraconazole, ritonavir, clarithromycin) in patients w/ severe renal impairment or ESRD. Inhibition of organic anion transporter-3 mediated transport w/ probenecid in vitro. Increased plasma AUC & C_max of digoxin.

Antidiabetic Agents

A10BD07 - metformin and sitagliptin ; Belongs to the class of combinations of oral blood glucose lowering drugs. Used in the treatment of diabetes.

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