Lino 5 mg Tablet-

Lino 5 mg Tablet-

Description

LINO-M combines two antihyperglycemic agents with complementary mechanisms of action to improve glycemic control in patients with type 2 diabetes: Sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, and Metformin hydrochloride, a member of the biguanide class. Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor, which is believed to exert its actions in patients with type 2 diabetes by slowing the inactivation of incretin hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. By increasing and prolonging active incretin levels, Sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucosedependent manner.

The pharmacologic mechanism of action of Metformin is different from other classes of oral antihyperglycemic agents.

Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and increases peripheral glucose uptake and utilization.

Composition

LINO-M 500 Tablet : Each film-coated tablet contains Linagliptin INN 2.5 mg & Metformin HCl BP 500 mg.

LINO-M 850 Tablet : Each film-coated tablet contains Linagliptin INN 2.5 mg & Metformin HCl BP 850mg.

Indication

LINO-M tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both linagliptin and metformin is appropriate

Dosage and Administration

The dosage of LINO-M should be individualized on the basis of both effectiveness and tolerability, while not exceeding the maximum recommended dose of 2.5 mg linagliptin/1000 mg metformin hydrochloride twice daily. LINO-M should be given twice daily with meals. Dose escalation should be gradual to reduce the gastrointestinal (GI) side effects associated with metformin use.

Recommended starting dose:

 In patients currently not treated with metformin, initiate treatment with 2.5 mg linagliptin/500 mg metformin hydrochloride twice daily

 In patients already treated with metformin, start with 2.5 mg linagliptin and the current dose of metformin hydrochloride twice daily

Patients already treated with linagliptin and metformin individual components may be switched to LINO-M containing the same doses of each component.

Side Effects

Most common side effect are nasopharyngitis & diarrhea. Hypoglycemia is more common in patients with this combination & sulfonylureas.

Contraindications

Renal impairment (eg, serum creatinine levels at least 1.5 mg/dL [men] and at least 1.4 mg/dL [women], abnormal CrCl); acute or chronic metabolic acidosis, including diabetic ketoacidosis; hypersensitivity to linagliptin, metformin, or any component of the product.

PRECAUTIONS

LINO-M should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis. caution should be taken in patients with lactic acidosis, pancreatitis, Renal & hepatic impaired patients.

PREGNANCY

Pregnancy Category B. There are no adequate and well-controlled studies in pregnant women with the combination of Metformin/ Linagliptin or its individual components; therefore, the safety of the combination in pregnant women is not known. The combination of Linagliptin & Metformin should be used during pregnancy only if clearly needed. Nursing

Mothers : It is not known whether Linagliptin is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when this combination is administered to a nursing woman.

DRUG INTERACTIONS

Cationic drug (amiloride, digoxin, morphine, ranitidine, trimethoprim etc.): May reduce metformin elimination. P-glycoprotien/CYP3A4 inducer (i.e. rifampin): The efficacy of LINO-M may be reduced when administered in combination.