Forbetes Plus 500/5 Mechanism of Action

Pharmacology: Pharmacodynamics: Metformin is a biguanide with anti-hyperglycaemic effects, lowering both basal and postprandial plasma glucose. It does not stimulate Insulin secretion and therefore does not produce hypoglycaemia.
Metformin may act via 3 mechanisms: By reducing hepatic glucose production by inhibiting gluconeogenesis and glycogenolysis.
In muscle, by increasing Insulin sensitivity, improving peripheral glucose uptake and utilisation.
And by delaying intestinal glucose absorption.
Metformin stimulates intracellular glycogen synthesis by acting on glycogen synthase. Metformin increases the transport capacity of all types of membrane glucose transporters (GLUT).
In humans, independently of its action on glycaemia, Metformin has favourable effects on lipid metabolism. This has been shown at therapeutic doses in controlled and report: Metformin reduces total cholesterol, LDL-cholesterol and triglyceride levels. In report conducted so far with combination therapy with Metformin and Glibenclamide, these favourable effects on lipid metabolism have not been shown.
Glibenclamide is a second generation Sulfonylurea with a medium half-life: it causes acute lowering of blood glucose by stimulating the release of Insulin by the pancreas, this effect being dependent on the presence of functioning beta cells in the islets of Langerhans.
The stimulation of Insulin secretion by Glibenclamide in response to a meal is of major importance.
The administration of Glibenclamide to diabetics induces an increase in the postprandial Insulin-stimulating response.
The increased postprandial responses in Insulin and C-peptide secretion persist after at least 6 months of treatment.
Metformin and Glibenclamide have different mechanisms and sites of action, but their action is complementary.
Glibenclamide stimulates the pancreas to secrete Insulin, while Metformin reduces cell resistance to Insulin by acting on peripheral (skeletal muscle) and hepatic sensitivity to Insulin.
In the treatment of type 2 diabetes inadequately controlled by monotherapy with Metformin or Glibenclamide combined with diet and exercise, have demonstrated that the combination had an additive effect on glucose regulation.
Pediatric Patients: Pediatric patients aged 9 to 16 years with type 2 diabetes not adequately controlled with diet and exercise, with or without an oral anti-diabetic treatment, a fixed combination of Metformin Hydrochloride 250 mg and Glibenclamide 1.25 mg was not shown more effective to either Metformin Hydrochloride or Glibenclamide in reducing HbA1c from baseline. Therefore, this product should not be used in pediatric patients.
Pharmacokinetics: Related to the Combination: The bioavailability of Metformin and Glibenclamide in the combination is similar to that noted when one caplet of Metformin and one caplet of Glibenclamide are taken simultaneously. The bioavailability of Metformin in the combination is unaffected by the ingestion of food. The bioavailability of Glibenclamide in the combination is unaffected by the ingestion of food, but the absorption speed of Glibenclamide is increased by eating.