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 immediate release tablet: The dosage of Linagliptin & Metformin should be individualized on the basis of both effectiveness and tolerability. Maximum recommended dose of 2.5 mg Linagliptin and 1000 mg Metformin Hydrochloride twice daily with meals. Dose escalation should be gradual to reduce the gastrointestinal (GI) side effects associated with Metformin Hydrochloride use.

Recommended starting dose: In patients currently not treated with Metformin Hydrochloride, initiate treatment with 2.5 mg Linagliptin and 500 mg Metformin Hydrochloride twice daily.

In patients already treated with Metformin Hydrochloride, start with 2.5 mg Linagliptin and the current dose of Metformin Hydrochloride twice daily.

Patients already treated with Linagliptin and Metformin Hydrochloride, individual components may be switched to this combination containing the same doses of each component.


Linagliptin & Metformin extend release tablet: The dosage of this combination should be individualized on the basis of both effectiveness and tolerability, while not exceeding the maximum recommended total daily dose of Linagliptin 5 mg and Metformin Hydrochloride 2000 mg. this combination should be given once daily with a meal.

Recommended starting dose: In patients currently not treated with metformin, initiate this combination treatment with 5 mg Linagliptin/1000 mg Metformin Hydrochloride extended-release once daily with a meal.

In patients already treated with 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 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.

5 mg Linagliptin & 1000 mg Metformin Hydrochloride extended-release tablet should be taken as a single tablet once daily. Patients using 2.5 mg Linagliptin & 1000 mg Metformin extended release tablets should take two tablets together once daily.

Interaction

Cationic drugs (amiloride, digoxin, morphine, ranitidine, trimethoprim etc.): May reduce metformin elimination.

P-glycoprotien/CYP3A4 inducer (i.e. rifampin): The efficacy of this medicine may be reduced when administered in combination.

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. Acute or chronic metabolic acidosis (diabetic ketoacidosis) and hypersensitivity to Linagliptin or Metformin Hydrochloride are additional contraindications.

Side Effects

Most common side effects are nasopharyngitis and diarrhea. Hypoglycemia is more common in patients treated with this combination and sulfonylureas.

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

Keep away from light and heat in a dry area. Keep out of children's reach.