Aptin M 50/500 tablet: Each coated tablet contains Vildagliptin INN 50 mg & Metformin Hydrochloride BP 500 mg.
Aptin M 50/850 tablet: Each coated tablet contains Vildagliptin INN 50 mg & Metformin Hydrochloride BP 850 mg.
Aptin M is a preparation of vildagliptin which is a dipeptidyl peptidase-4 (DPP-4) inhibitor and metformin hydrochloride, a member of the biguanide class. Vildagliptin exerts its actions in patients with type 2 diabetes by slowing the inactivation of incretin hormones. Incretin hormones, including glucagon-like peptide-I (GLP-I) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-I and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP. GLP-I also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. By increasing and prolonging active incretin levels, vildagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose dependent manner. Metformin decreases the glucose level by reducing hepatic glucose production, increases peripheral glucose uptake and utilization by increasing insulin sensitivity of muscle, decreases intestinal absorption of glucose and stimulates intracellular glycogen synthesis by acting on glycogen synthase.
Adults The recommended dose of vildagliptin plus metformin hydrochloride combination is either 50 mg/500 mg or 50 mg/850 mg 1 tab twice daily. Maximum dose of vildagliptin is 100 mg and metformin hydrochloride is 2000 mg per day. Taking combination of vildagliptin plus metformin hydrochloride with or just after food may reduce gastrointestinal symptoms associated with metformin hydrochloride. There is no clinical experience of vildagliptin plus metformin hydrochloride in triple combination with other antidiabetic agents.
Pediatric use Combination of vildagliptin plus metformin hydrochloride is not recommended in patients below 18 years of age.
Patients with hepatic impairment Combination of vildagliptin plus metformin hydrochloride is not recommended in patients with clinical or laboratory evidence of hepatic impairment.
Patients with renal impairment Combination of vildagliptin plus metformin hydrochloride should not be used in patients with renal failure or renal dysfunction (serum creatinine levels =1.5 mg/dl in males and =1.4 mg/dl in females).
Iodinated contrast agents increase risk of lactic acidosis (withhold metformin before procedure); alcohol potentiates metformin-associated lactic acidosis; cationic drugs (cimetidine, ranitidine, digoxin) compete for renal tubular transport; sulfonylureas increase hypoglycemic risk.
The combination of vildagliptin plus metformin hydrochloride is contraindicated in patients with known hypersensitivity to vildagliptin or metformin hydrochloride or to any of the excipients. It is also contraindicated in patients with renal disease or renal dysfunction, congestive heart failure, diabetic ketoacidosis, acute myocardial infarction and septicaemia. It should be temporarily discontinued in patients undergoing radiologic studies involving intravascular administration of iodinated contrast materials.
Common: Tremor, headache, dizziness, nausea, hypoglycemia, fatigue. Rare: Lactic acidosis, hepatic dysfunction.
Overdose
Vildagliptin Information regarding overdose with vildagliptin is limited. Doses up to 200 mg were well tolerated. In the event of an overdose, supportive management is recommended. Mefformin hydrochloride If overdosage is suspected, hemodialysis may be useful for removal of accumulated drug from patients. Metformin hydrochloride is dialyzable with a clearance of up to 170 mL/min under good hemodynamic conditions.
Category C. Not recommended during pregnancy; insulin is preferred for glycemic control. Lactation: Excretion in human milk unknown; contraindicated during breastfeeding.
Store below 25°C in a cool, dry place. Protect from light and moisture. Keep out of the reach of children.