Lijenta-M Tablet 2.5 mg+500 mg
Lijenta-M Tablet 2.5 mg+500 mg Uses, Dosage, Side Effects, Food Interaction and all others data.
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). By inhibiting DPP-4 Linagliptin increases the concentrations of active incretin hormones and stimulates the release of Insulin in a glucose dependent manner and decreases the level of Glucagon in the circulation and thus regulates the 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 elevated blood glucose levels. Furthermore, GLP-1 also reduces Glucagon secretion from pancreatic alpha-cells, resulting in a reduction in hepatic glucose output.
A 5mg oral dose of linagliptin results in >80% inhibition of dipeptidyl peptidase 4 (DPP-4) for ≥24 hours. Inhibition of DPP-4 increases the concentration of glucagon-like peptide 1 (GLP-1), leading to decreased glycosylated hemoglobin and fasting plasma glucose.
| Trade Name | Lijenta-M Tablet 2.5 mg+500 mg |
| Generic | Linagliptin + Metformin Hydrochloride |
| Weight | 2.5 mg+500 mg |
| Type | Tablet |
| Therapeutic Class | |
| Manufacturer | NIPRO JMI Pharma Ltd. |
| Available Country | Bangladesh |
| Last Updated: | October 19, 2023 at 6:27 am |
Uses
Linagliptin is used for an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Linagliptin may be used as monotherapy or in combination with other common antidiabetic medications including Metformin, Sulfonylurea, Pioglitazone, or Insulin. As a replacement therapy it is suitable when Metformin therapy is not appropriate due to intolerance or do not provide adequate glycemic control as monotherapy or other antidiabetic drugs are to be discontinued due to renal or hepatic impairment.
Lijenta-M Tablet 2.5 mg+500 mg is also used to associated treatment for these conditions: Type 2 Diabetes Mellitus
How Lijenta-M Tablet 2.5 mg+500 mg works
Linagliptin is a competitive, reversible DPP-4 inhibitor. Inhibition of this enzyme slows the breakdown of GLP-1 and glucose-dependant insulinotropic polypeptide (GIP). GLP-1 and GIP stimulate the release of insulin from beta cells in the pancreas while inhibiting release of glucagon from pancreatic beta cells. These effects together reduce the breakdown of glycogen in the liver and increase insulin release in response to glucose.
Dosage
Lijenta-M Tablet 2.5 mg+500 mg dosage
The recommended dose of Linagliptin is 5 mg once daily and can be taken with or without food. If added with Metformin, the dose of Metformin should be maintained and Linagliptin administered concomitantly. When used in combination with Sulfonylurea, a lower dose of Sulfonylurea may be considered to reduce the risk of hypoglycemia.
Pediatric patients: Safety and effectiveness of Linagliptin in patients below the age of 18 have not been established.
Renal or hepatic impairment: No dose adjustment required.
Side Effects
Treatment with Linagliptin is well tolerated; some of the less common side effects are nasopharyngitis and hypoglycemia.
Toxicity
No dosage adjustment is necessary based on race, age, weight, sex, renal impairment, or hepatic impairment.
Studies of efficacy and safety in pediatric populations were not included in the original drug approval but recent clinical trials show linagliptin to be well tolerated in patients 10 to 18 years old.
Animal studies showed an increased risk of lymphoma in female rats at over 200 times the clinical dose. Aside from this effect, linagliptin was not shown to be mutagenic, clastogenic, or have an effect on fertility.
Precaution
When used with an Insulin secretagogue (e.g., sulfonylurea) or Insulin, consider lowering the dose of the Insulin secretagogue or Insulin to reduce the risk of hypoglycemia. If pancreatitis is suspected, Linagliptin should be discontinued. There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with Linagliptin or any other antidiabetic drug.
Interaction
Linagliptin doesn't interact with Metformin, Glyburide, Simvastatin, Warfarin, Digoxin or oral contraceptives. Linagliptin is a weak competitive and a weak to moderate mechanism-based inhibitor of CYP isozyme CYP3A4, but does not inhibit other CYP isozymes. Again it doesn't act as an inducer of CYP isozymes.
Volume of Distribution
A single intravenous dose of 5mg results in a volume of distribution of 1110L. However an intravenous infusion of 0.5-10mg results in a volume of distribution of 380-1540L.
Elimination Route
Oral bioavailability of linagliptin is 30%.
Half Life
The terminal half life of linagliptin is 155 hours.
Clearance
Total clearance of linagliptin is 374mL/min.
Elimination Route
84.7% of linagliptin is eliminated in the feces and 5.4% is eliminated in the urine.
Pregnancy & Breastfeeding use
Pregnancy: There are no adequate and well-controlled studies in pregnant women. Linagliptin tablets should be used during pregnancy only if the potential benefit of mother justifies the potential risk of the fetus.
Nursing mothers: Caution should be exercised when Linagliptin is administered to a nursing woman.
Contraindication
Linagliptin is contraindicated to patients hypersensitive to Linagliptin or any of the excipients.
Storage Condition
Store in a cool dry place protected from light. Keep out of reach of children.
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