Indications of Linax Plus 2.5/850

Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus

Pharmaceutical Name

Ibn Sina Pharmaceuticals Ltd

Pharmacology

Linagliptin is used to enhance glycemic control in people with type 2 diabetes. Linagliptin is a DPP-4 (dipeptidyl peptidase-4) inhibitor, which is an enzyme that destroys the incretin hormones GLP-1 (glucagon like peptide-1) and GIP (glucose dependent insulinotropic polypeptide). Thus, linagliptin raises the concentrations of active incretin hormones in the blood, increasing the release of insulin from pancreatic beta cells in a glucose-dependent manner while reducing glucagon production from pancreatic alpha cells.

Metformin Hydrochloride is an oral antihyperglycemic medication of the biguanide class that is used to treat type 2 diabetes. It reduces both basal and postprandial plasma glucose levels. It has a different mode of action than sulfonylureas and does not cause hypoglycemia. Metformin Hydrochloride reduces hepatic glucose synthesis, lowers intestinal glucose absorption, and increases insulin sensitivity by increasing peripheral glucose uptake and utilization.

Dosage & Administration of Linax Plus 2.5/850

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 of Linax Plus 2.5/850

Cationic medicines (amiloride, digoxin, morphine, ranitidine, trimethoprim, and others): These medications may decrease metformin elimination.

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

Contraindications

Linagliptin is contraindicated in patients with a history of severe renal impairment, acute or chronic metabolic acidosis, including diabetic ketoacidosis and a hypersensitivity reaction to linagliptin and metformin.

Side Effects of Linax Plus 2.5/850

Linagliptin-The most common side effects of linagliptin are stuffy or runny nose and sore throat. Hypoglycemia may occur when linagliptin is combined with insulin or a sulfonylurea-type drug. Allergic reactions and muscle pain also may occur. Pancreatitis also has been reported. Metformin-The most common adverse reactions due to initiation of metformin are diarrhea, nausea/vomiting, flatulence, asthenia, indigestion, abdominal discomfort, and headache.

Pregnancy & Lactation

Pregnancy: Pregnancy Category C.
Nursing mothers: Caution should be exercised when Linagliptin is administered to a nursing woman.
Pediatric patients: Safety and effectiveness of Linagliptin in patients below the age of 18 have not been established.

Precautions & Warnings

Metformin should be stopped immediately in patients with lactic acidosis who are taking it, and supportive therapy should be started right away. Acute pancreatitis has been reported after the drug’s release. If pancreatitis is suspected, promptly discontinue Linagliptin & Metformin. In patients undergoing radiologic studies with intravascular administration 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 parameters should be checked at least once a year.

Therapeutic Class

Oral hypoglycemic medications in combination

Storage Conditions

Linax should be stored between 15°C to 30° C.

Generic Name of Linax Plus 2.5/850

Linagliptin + Metformin Hydrochloride