Glucovance

250 mg/1.25 mg 1st-line therapy for type 2 diabetes in adults, when diet & exercise alone do not result in adequate glycemic control. 500 mg/2.5 mg & 500 mg/5 mg Treatment of type 2 diabetes in adults as 2nd-line therapy, when diet, exercise & initial treatment w/ metformin or glibenclamide (or another sulfonylurea) do not result in adequate glycemic control, & as replacement for previous treatment w/ metformin & glibenclamide in patients whose glycemia is stable & well controlled.

Adult Initial treatment: 1st-line therapy Initially 1 tab of 250 mg/1.25 mg once daily (may be used bid if HbA1c >9% or FPG >2 g/L). May increase dose in increments of 1 tab of 250 mg/1.25 mg daily every 2 wk or longer according to glycemia results. 2nd-line therapy Initially 1 tab of 500 mg/2.5 mg or 500 mg/5 mg once daily. Initial dose must not exceed the daily doses of glibenclamide (or equiv dose of another sulfonylurea) or metformin already being taken. May increase dose in increments of no more than 500 mg/5 mg daily every 2 wk or longer according to the glycemia results up to minimum effective dose to achieve adequate control of blood glucose. Replacement for previous combination therapy w/ metformin & sulfonylurea Initial dose must not exceed the daily dose of glibenclamide (or equiv dose of another sulfonylurea) & metformin already being taken. May increase dose in increments of no more than 500 mg/5 mg daily every 2 wk or longer according to the glycemia results up to minimum effective dose to achieve adequate control of blood glucose. Max: Metformin HCl 2,000 mg/glibenclamide 20 mg daily. Elderly ≥65 yr Start w/ lowest available dose & increased gradually if necessary. Renal impairment CrCl 30-59 mL/min or eGFR 45-59 mL/min/1.73 m² Max: Metformin 1,000 mg daily. Renal function should be closely monitored every 3-6 mth, CrCl 30-59 mL/min or eGFR 30-44 mL/min/1.73 m² Not recommended to initiate but can be maintained in patient already treated, provided that max daily dose: Not >1,000 mg metformin. Renal function should be closely monitored every 3 mth.

Should be taken with food.

Hypersensitivity to metformin HCl, glibenclamide or other sulfonylureas & sulfonamides. Any type of metabolic acidosis (eg, lactic acidosis, diabetic ketoacidosis). Diabetic pre-coma. Acute conditions w/ potential to alter renal function eg, dehydration, severe infection, CV collapse (shock). Disease (especially acute disease or worsening of chronic diseases) which may cause tissue hypoxia eg, unstable CHF, resp failure, recent MI, CV collapse or shock. Porphyria. Severe renal failure (CrCl <30 mL/min or eGFR <30 mL/min/1.73 m²). Hepatic insufficiency, acute alcohol intoxication, alcoholism. Concomitant use w/ miconazole even for local use. Discontinue 48 hr before or from the time of intravascular administration of iodinated contrast media & not reinstituted until 48 hr afterwards & only after renal function has been re-evaluated & found to be normal. Discontinue 48 hr before an elective major surgery & may not be reinstituted until 48 hr afterwards & only after kidney function has been re-evaluated & found to be normal. Lactation.

Risk of lactic acidosis, hypoglycemia, blood sugar imbalance. Patients suffering from any infectious illnesses eg, flu, infection of the air passages or UTI. Patients should continue their diet, w/ regular distribution of carbohydrate intake during the day & should get some regular exercise. Overwt patients should continue their energy-restricted diet. Perform regularly the usual lab tests for diabetes monitoring. Periodic monitoring Vit B₁₂ serum levels. Renal function; determine CrCl or eGFR before initiating treatment & regularly thereafter. Risk of hypoxia & renal insufficiency in patients w/ heart failure. Regular monitoring of cardiac & renal function in patients w/ stable chronic heart failure. Caution in patients w/ G6PD deficiency. Patients w/ congenital galactosemia, glucose & galactose malabsorption syndrome or lactase deficiency. Discontinue immediately if CrCl or eGFR fall <30 mL/min or <30 mL/min/1.73 m². Caution when driving or using machines. Must not be used for treatment of diabetes during pregnancy. Contraindicated in breastfeeding. Elderly ≥65 yr. Neither safety nor efficacy has been established in childn.

GI disorders eg, nausea, vomiting, diarrhea, abdominal pain & loss of appetite. Taste disturbance; vit B₁₂ decrease/deficiency.

Glibenclamide: Increase in hypoglycemic effect w/ possible onset of hypoglycemic manifestations or even coma w/ miconazole (systemic route, oromucosal gel). Increased risk of hepatotoxicity & reduced hypoglycemic effect w/ bosentan. Masked hypoglycemic symptoms w/ β-blockers, clonidine, reserpine, guanethidine or sympathomimetics. Increase t_½ w/ possible onset of hypoglycemic manifestations w/ fluconazole. Reduction in antidiuretic effect of desmopressin. Reduced plasma conc & may lead to reduced hypoglycemic effect w/ colesevelam. Decreased blood glucose levels w/ ACE inhibitors (eg, captopril, enalapril). Metformin: May lead to renal failure w/ iodinated contrast materials. Increase in risk of lactic acidosis during alcohol intoxication. Lactic acidosis w/ diuretics particularly loop diuretics. May reduce efficacy w/ OCT1 substrate/inhibitor (eg, verapamil). May increase GI absorption & efficacy w/ OCT1 inducers (eg, rifampicin). May decrease renal elimination w/ OCT2 substrates/inhibitors (eg, cimetidine, dolutegravir, crizotinib, olaparib, daclatasvir, vandetanib). Sulfonylureas: May increase hypoglycemic action w/ alcohol, phenylbutazone (systemic route). All antidiabetic agents: Medicinal products w/ intrinsic hyperglycemic activity eg, glucocorticoids & tetracosactides (systemic & local routes), β₂ agonists, danazol & chlorpromazine (high dosages of 100 mg/day), diuretics.

Antidiabetic Agents

A10BD02 - metformin and sulfonylureas ; Belongs to the class of combinations of oral blood glucose lowering drugs. Used in the treatment of diabetes.

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