Generic

Linagliptin + Metformin Hydrochloride

Indications

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

Pharmacology

Linagliptin is used to help people with type 2 diabetes regulate 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 reducing 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 instant release tablet: Linagliptin & Metformin dose should be customized based on efficacy and tolerability. 2.5 mg Linagliptin and 1000 mg Metformin Hydrochloride twice day with meals is the maximum suggested dosage. To decrease the gastrointestinal (GI) adverse effects associated with Metformin Hydrochloride usage, dose escalation should be done gradually.

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

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 has the same dosages of each component.

Linagliptin and Metformin extended-release tablet dosage should be customized 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 therapy with 5 mg Linagliptin/1000 mg Metformin Hydrochloride extended-release once day with a meal in individuals who are not presently taking metformin.

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

In patients already treated with Linagliptin & Metformin immediate release tablet, switch to extend release tablet containing 5 mg of Linagliptin total daily dose and a similar total daily dose of Metformin once daily with a meal.

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

Interaction

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

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

Contraindications

Metformin Hydrochloride is known to be extensively eliminated by the kidney, notwithstanding Linagliptin’s low renal excretion. With the severity of renal impairment, the risk of Metformin Hydrochloride buildup and lactic acidosis rises. As a result, people with renal impairment should avoid this combination.

Side Effect

Nasopharyngitis and diarrhea are the most prevalent adverse effects. Patients using this combination with sulfonylureas are more likely to have hypoglycemia.

Pregnancy & Lactation

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

Precautions & Warnings

Metformin should be stopped immediately in patients with lactic acidosis who are taking it, and supportive treatment should be started very 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 tests with intravascular injection of iodinated contrast materials or any surgical procedures requiring restricted food and fluid intake, temporarily stop taking Linagliptin and Metformin. Because metformin can reduce Vitamin B12 levels, hematologic markers should be checked at least once a year.

Therapeutic Class

Combination Oral hypoglycemic preparations

Storage Conditions

Store in a cool and dry place, below 30°C and away from light.

Pharmaceutical Name

General Pharmaceuticals Ltd.