Generic

Linagliptin + Metformin Hydrochloride

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: 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

Although Linagliptin undergoes minimal renal excretion, Metformin Hydrochloride is known to be substantially excreted by the kidney. The risk of Metformin Hydrochloride accumulation and lactic acidosis increases with the degree of renal impairment. Therefore, this combination is contraindicated in patients with renal impairment. It is also contraindicated in acute or chronic metabolic acidosis (diabetic ketoacidosis) and in hypersensitivity to Linagliptin or Metformin Hydrochloride.

Side Effects

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

Pregnancy & Lactation

There are no adequate and well-controlled studies in pregnant women with this combination or its individual component; so it should be used during pregnancy only if clearly needed. Caution should also be excercised when it is administered to a lactating mother.

Precautions & Warnings

In a patient with lactic acidosis who is taking Metformin, the drug should be discontinued immediately and supportive therapy promptly instituted. There have been postmarketing reports of acute pancreatitis. If pancreatitis is suspected, promptly discontinue Linagliptin & Metformin. Temporarily discontinue Linagliptin & Metformin in patients undergoing radiologic studies with intravascular administration of iodinated contrast materials or any surgical procedures necessitating restricted intake of food and fluids. Metformin may lower Vitamin B12 levels; so hematologic parameters shoud be monitored annually.

Therapeutic Class

Combination 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

Beximco Pharma Ltd