Indications
Linaglip Plus is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both Linagliptin and Metformin is appropriate.
Combination of Linagliptin and Metformin is not recommended for treatment of type 1 diabetes or diabetic ketoacidosis and has not been studied in patients with a history of pancreatitis.
Combination of Linagliptin and Metformin is not recommended for treatment of type 1 diabetes or diabetic ketoacidosis and has not been studied in patients with a history of pancreatitis.
Pharmacology
Linaglip Plus combines 2 antihyperglycemic agents (combination of Linagliptin, a DPP-4 inhibitor & Metformin, a member of the biguanide class) with complementary mechanisms of action to improve glycemic control in patients with type 2 diabetes mellitus.
Linagliptin: Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, Linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation. Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake. GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. Furthermore, GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output.
Metformin: Metformin lowers both basal and postprandial plasma glucose. It does not stimulate insulin secretion and therefore does not produce hypoglyceamia or increased weight gain. Metformin may exert its glucose-lowering effect via four mechanisms:
– by reduction of hepatic glucose production through inhibition of gluconeogenesis and glycogenolysis;
– in muscle, by modestly increasing insulin sensitivity, improving peripheral glucose uptake and utilization;
– by delaying intestinal glucose absorption;
– stimulate intracellular glycogen synthesis by acting on glycogen synthase and increase the transport capacity of glucose transporters (GLUT-1 & GLUT-4)
Linagliptin: Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, Linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation. Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake. GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. Furthermore, GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output.
Metformin: Metformin lowers both basal and postprandial plasma glucose. It does not stimulate insulin secretion and therefore does not produce hypoglyceamia or increased weight gain. Metformin may exert its glucose-lowering effect via four mechanisms:
– by reduction of hepatic glucose production through inhibition of gluconeogenesis and glycogenolysis;
– in muscle, by modestly increasing insulin sensitivity, improving peripheral glucose uptake and utilization;
– by delaying intestinal glucose absorption;
– stimulate intracellular glycogen synthesis by acting on glycogen synthase and increase the transport capacity of glucose transporters (GLUT-1 & GLUT-4)
Dosage & Administration
Recommended starting dose:
Patients not currently treated with Metformin: Initiate treatment with Linaglip Plus 500 tablet twice daily.
Patients already treated with Metformin: If patient is taking Metformin 500 mg tablet twice daily, then give him/her Linaglip Plus 500 tablet twice daily. If patient is taking Metformin 850 mg tablet twice daily, then give him/her Linaglip Plus 850 tablet twice daily.
Patients already treated with Linagliptin and Metformin individual components: May be switched to Linaglip Plus containing the same doses of each component
Maximum recommended dose: 2.5 mg Linagliptin/1000 mg Metformin tablet twice daily.
Patients not currently treated with Metformin: Initiate treatment with Linaglip Plus 500 tablet twice daily.
Patients already treated with Metformin: If patient is taking Metformin 500 mg tablet twice daily, then give him/her Linaglip Plus 500 tablet twice daily. If patient is taking Metformin 850 mg tablet twice daily, then give him/her Linaglip Plus 850 tablet twice daily.
Patients already treated with Linagliptin and Metformin individual components: May be switched to Linaglip Plus containing the same doses of each component
Maximum recommended dose: 2.5 mg Linagliptin/1000 mg Metformin tablet twice daily.
Contraindications
This combination of Linagliptin & Metformin is contraindicated in patients with renal impairment (e.g., serum creatinine >=1.5 mg/dL for men, >=1.4 mg/dL for women, or abnormal creatinine clearance), which may also result from conditions such as cardiovascular collapse (shock), acute myocardial infarction, and septicemia. This combination is also contraindicated in case of acute or chronic metabolic acidosis, including diabetic ketoacidosis. Diabetic ketoacidosis should be treated with insulin. In case of a history of hypersensitivity reaction to Linagliptin, such as anaphylaxis, angioedema, exfoliative skin conditions, urticaria, or bronchial hyperreactivity it is also contraindicated.Contraindicated in case of hypersensitivity to Metformin.
Side Effects
Most common side effects are nasopharyngitis and diarrhea. Hypoglycemia is more common in patients treated with this combination and sulfonylureas.
Pregnancy & Lactation
Pregnancy category B. There are no adequate and well-controlled studies in pregnant women with this combination or its individual component; so it should be used during pregnancy only if clearly needed. Caution should also be excercised when it is administered to a lactating mother.
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