TrajentaTM
TrajentaTM (linagliptin) is an inhibitor of the enzyme DPP-4 (dipeptidyl peptidase-4) which is involved in the inactivation of the incretin hormones GLP-1 and GIP (glucagon-like peptide-1, glucose-dependent insulinotropic polypeptide). Linagliptin glucose-dependently increases insulin secretion and lowers glucagon secretion thus resulting in an overall improvement in the glucose homoeostasis.
Linagliptin is a prescription medicine that is used along with diet and exercise to lower blood glucose in adults with Type 2 Diabetes.2,3 Linagliptin is not for people with Type 1 Diabetes or for people with diabetic ketoacidosis (increased ketones in the blood or urine).1,2
Linagliptin is an original research product of Boehringer Ingelheim. Its an oral once-daily single dose tablet in the treatment of Type 2 diabetes in adults and doesn’t require any dosage adjustment in Renal and Hepatic comorbidities. It is approved in the United States, the European Union and Japan, among other countries, including India. Linagliptin approval is supported by a clinical trial program that involved approximately 6,000 adults with type 2 diabetes, including patients from India.
In India, Trajenta has been launched in - June 2012 and is available on prescription.
Trajenta DUOTM
TRAJENTA DUOTM combines 2 antihyperglycemic agents with complementary mechanisms of action to improve glycemic control in patients with type 2 diabetes mellitus:
Linagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, and metformin, a member of the biguanide class.
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 is an antihyperglycemic agent which improves glucose tolerance in patients with type 2 diabetes mellitus, lowering both basal and postprandial plasma glucose. Its pharmacologic mechanisms of action are different from other classes of oral antihyperglycemic agents. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. Unlike SUs, metformin does not produce hypoglycemia in either patients with type 2 diabetes mellitus or normal subjects (except in special circumstances) [see Warnings and Precautions (5.5)] and does not cause hyperinsulinemia. With metformin therapy, insulin secretion remains unchanged while fasting insulin levels and day-long plasma insulin response may actually decrease.
TRAJENTA DUOTM tablets are 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
TRAJENTA DUOTM tablets are available in the following dosage forms and strengths: 2.5 mg linagliptin/500 mg metformin hydrochloride tablets are light yellow, oval, biconvex tablets debossed with “D2/500” on one side and the Boehringer Ingelheim logo on the other side. 2.5 mg linagliptin/850 mg metformin hydrochloride tablets are light orange, oval, biconvex tablets debossed with “D2/850” on one side and the Boehringer Ingelheim logo on the other side. 2.5 mg linagliptin/1000 mg metformin hydrochloride tablets are light pink, oval, biconvex tablets debossed with “D2/1000” on one side and the Boehringer Ingelheim logo on the other side.
In India Trajenta DuoTM has been Launched in April 2014 and is available on prescription.
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EMPA REG OUTCOME Factsheet
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Introduction to SGLT2 inhibition