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 improve blood sugar control in patients with type 2 diabetes. Linagliptin is a DPP4 (dipeptidyl peptidase 4) inhibitor, which breaks down the incretin hormones GLP1 (glucagon-like peptide 1) and GIP (promoter polypeptide glucose-dependent insulin). Thus, linagliptin increases the concentration of active glucagon, stimulates pancreatic β (β) cells to release insulin in a glucose-dependent manner, and reduces glucagon secretion from circulating pancreatic α (α) cells.

Metformin hydrochloride is a biguanide oral hypoglycemic agent used to treat type 2 diabetes. It lowers basal and postprandial blood sugar. Its mechanism of action is different from that of sulfonylureas and it does not produce hypoglycemia. Metformin hydrochloride reduces glucose production in the liver, reduces intestinal glucose absorption, and improves 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.

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

Contraindications

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.

Side Effects

The 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 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

Combination of Oral hypoglycemic preparations

Storage Conditions

Keep in a cool & dry place (below 30°C), protected from light & moisture. Keep out of the reach of children.

Pharmaceutical Name

Popular Pharmaceuticals Ltd.