Indications

When treatment with both Linagliptin and Metformin Hydrochloride is appropriate, this is advised as an addition to diet and exercise to enhance glycemic control in persons with type 2 diabetes mellitus.

Pharmacology

Linagliptin is used to help people with type 2 diabetes control their blood sugar levels. DPP-4 (dipeptidyl peptidase-4) is an enzyme that degrades the incretin hormones GLP-1 (glucagon-like peptide-1) and GIP (glucagon-like peptide-1). Linagliptin is an inhibitor of DPP-4 (dipeptidyl peptidase-4) (glucose-dependent insulinotropic polypeptide). Linagliptin stimulates the release of insulin from pancreatic beta () cells in a glucose-dependent manner while lowering the production of glucagon from pancreatic alpha () cells in the blood, increasing the concentrations of active incretin hormones. Metformin Hydrochloride is an antihyperglycemic medication of the biguanide class that is used to treat type 2 diabetes. Both baseline and postprandial plasma glucose levels are reduced. It has a different mode of action than sulfonylureas and does not cause hypoglycemia. Metformin Hydrochloride reduces hepatic glucose synthesis, intestinal glucose absorption, and insulin sensitivity by increasing peripheral glucose uptake and utilization.

Dosage & Administration

Linagliptin & Metformin immediate-release tablet: Linagliptin & Metformin dosage should be tailored based on efficacy and tolerability. 2.5 mg of Linagliptin and 1000 mg of Metformin Hydrochloride twice daily with meals is the maximum suggested dose. To decrease the gastrointestinal (GI) adverse effects associated with Metformin Hydrochloride use, dose escalation should be gradual.ls

In individuals who have not previously been treated with Metformin Hydrochloride, start with 2.5 mg Linagliptin and 500 mg Metformin Hydrochloride twice daily.

Start with 2.5 mg Linagliptin plus the current dose of Metformin Hydrochloride twice daily in patients who are already taking Metformin Hydrochloride.

Individual components of Linagliptin and Metformin Hydrochloride may be swapped to this combination, which contains the same doses of each component.

Linagliptin and Metformin extended-release tablet dosage should be tailored based on efficacy and tolerability, while not exceeding the maximum recommended total daily dose of Linagliptin 5 mg and Metformin Hydrochloride 2000 mg. This mixture should be taken with a meal once a day.

Start this combo treatment with 5 mg Linagliptin/1000 mg Metformin Hydrochloride extended-release once daily with a meal in individuals who are not currently taking metformin.

Start this combination with 5 mg of Linagliptin total daily dose and a similar total daily dose of Metformin once daily with a meal in patients who are already taking Metformin.

Switch to an extended-release tablet containing 5 mg of Linagliptin total daily dose and a similar total daily dose of Metformin once daily with a meal in patients already using Linagliptin & Metformin immediate-release tablets.

A single extended-release tablet containing 5 mg of Linagliptin and 1000 mg of Metformin Hydrochloride should be taken once a day. Patients using 2.5 mg Linagliptin and 1000 mg Metformin extended-release tablets once a day should take two tablets simultaneously.

Interaction

Amiloride, digoxin, morphine, ranitidine, trimethoprim, and other cationic medicines may impair metformin elimination.

P-glycoprotein/CYP3A4 inducer (i.e. rifampin): When used together, the efficacy of this medicine may be diminished.

 Contraindications

Metformin Hydrochloride is known to be considerably eliminated by the kidney, notwithstanding Linagliptin’s limited renal excretion. With the severity of renal impairment, the risk of Metformin Hydrochloride buildup and lactic acidosis increases. As a result, people with renal impairment should avoid this combination. Acute or chronic metabolic acidosis (diabetic ketoacidosis) and hypersensitivity to Linagliptin or Metformin Hydrochloride are other contraindications.

Side Effects

Nasopharyngitis and diarrhea are the most common adverse effects. Patients taking this combination plus sulfonylureas are more likely to have hypoglycemia.

Pregnancy & Lactation

Because there are no good and well-controlled trials in pregnant women with this combination or its individual components, it should only be taken if clearly needed during pregnancy. When given to a breastfeeding woman, extreme caution should be exercised.

Precautions & Warnings

Metformin should be stopped immediately in patients with lactic acidosis who are taking it, and supportive care should be started every once. Acute pancreatitis has been reported after the drug’s release. If pancreatitis is detected, stop taking Linagliptin and Metformin very away. In patients having radiologic investigations with an intravascular infusion of iodinated contrast materials or any surgical procedures requiring restricted food and fluid intake, temporarily stop taking Linagliptin and Metformin. Because metformin can lower Vitamin B12 levels, hematologic markers should be checked at least once a year.

Therapeutic Class

Oral hypoglycemic medications in combination.

Storage Conditions

Keep away from light and moisture in a cool, dry location (below 30°C). Keep out of children’s reach.

Pharmaceutical Name

Popular Pharmaceuticals Ltd.