Generic: Linagliptin + metformin hydrochloride
Type: Tablet
Pack Size: 28S
Generic Name: Linagliptin 5mg + Metformin Hydrochloride 1000mg
Company Name: Aristopharma Ltd.
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Indications
When treatment with both Linagliptin and Metformin is appropriate, Linaglip-M is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Linagliptin and Metformin are not recommended for the treatment of type 1 diabetes or diabetic ketoacidosis and have not been studied in patients with a history of pancreatitis.
Pharmacology
Linaglip-M combines two antihyperglycemic agents with complementary mechanisms of action (Linagliptin, a DPP-4 inhibitor, and Metformin, a member of the biguanide class) to improve glycemic control in patients with type 2 diabetes mellitus.
Linagliptin is a DPP-4 inhibitor, which degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). As a result, Linagliptin raises the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner while decreasing glucagon levels in the blood. Both incretin hormones play a role in the physiological control of glucose homeostasis. Throughout the day, incretin hormones are secreted at a low basal level, and levels rise immediately after meals. In the presence of normal and elevated blood glucose levels, GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells. Furthermore, GLP-1 inhibits glucagon secretion from pancreatic alpha cells, lowering hepatic glucose output.
Metformin reduces both basal and postprandial plasma glucose levels. It does not stimulate insulin secretion and thus does not cause hypoglycemia or weight gain. Metformin may lower blood glucose levels through four different mechanisms:
- by lowering hepatic glucose production by inhibiting gluconeogenesis and glycogenolysis;
- in muscle, by improving peripheral glucose uptake and utilization by modestly increasing insulin sensitivity;
- by delaying intestinal glucose absorption;
- by increasing the transport capacity of glucose transporters and stimulating intracellular glycogen synthesis by acting on glycogen synthase (GLUT-1 & GLUT-4)
Dosage and Administration
Starting dose for 2.5/500 & 2.5/850 mg tablets:
The following is the recommended starting dose for a 5/1000 mg ER tablet:
Interaction
Drug Interactions with Metformin
Drug Interactions with Linagliptin
Insulin Secretagogues or Insulin
Drugs Affecting Glycemic Control
Contraindications
This combination of Linagliptin and Metformin is not recommended for patients who have a renal impairment (e.g., serum creatinine >1.5 mg/dL for men, >1.4 mg/dL for women, or abnormal creatinine clearance), which can be caused by conditions such as cardiovascular collapse (shock), acute myocardial infarction, and septicemia. This combination is also not recommended if you have acute or chronic metabolic acidosis, such as diabetic ketoacidosis. Insulin should be used to treat diabetic ketoacidosis in the event of a previous history of hypersensitivities to Linagliptin, such as anaphylaxis, angioedema, exfoliative skin conditions, urticaria, or bronchial hyperreactivity. It is also not recommended if you are allergic to Metformin.
Side effects
The most common side effects of this combination of Linagliptin & Metformin are weakness or tiredness, unusual muscle pain, breathing in trouble, nausea, vomiting, diarrhea, dizziness. Adverse reactions reported in >5% of patients treated with Linagliptin & Metformin combination and more commonly than in patients treated with placebo are nasopharyngitis and diarrhea. Hypoglycemia was more commonly reported in patients treated with the combination of Linagliptin & Metformin and SU compared with those treated with the combination of SU and Metformin.
Pregnancy & Lactation
Pregnancy: Linagliptin & Metformin combination is pregnancy Category B. Linagliptin & Metformin combination tablets should be used during pregnancy only if clearly needed. But the limited data on the combination of Linagliptin & Metformin combination extended-release tablet use in pregnant women are not sufficient to inform a Linagliptin & Metformin extended-release combination - associated or Linagliptin-associated risk for major birth defects and miscarriage.
Nursing mothers: There is no information regarding the presence of both Linagliptin & Metformin combination and Linagliptin & Metformin combination extended-release tablet or Linagliptin in human milk, the effects on the breastfed infant, or the effects on milk production.
Precautions & Warnings
Storage Conditions
Store at 25°C and dry place, protect from light. Keep out of the reach of children.