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Linamet
Linagliptin/Metformin
Linamet

LinametTM 2.5/500: Each film coated tablet contains 2.5 mg Linagliptin INN and 500 mg Metformin Hydrochloride BP.
LinametTM 2.5/850: Each film coated tablet contains 2.5 mg Linagliptin INN and 850 mg Metformin Hydrochloride BP.

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Pharmacology/Description

Linagliptin binds to DPP-4 in a reversible manner and increases the concentrations of incretin hormones. Linagliptin glucose-dependently increases insulin secretion and lowers glucagon secretion, thus resulting in a better regulation of the glucose homeostasis. Linagliptin binds selectively to DPP-4 and selectively inhibits DPP-4, but not DPP-8 or DPP-9 activity in vitro at concentrations approximating therapeutic exposures. Metformin is an antihyperglycemic agent which improves glucose tolerance in patients with type 2 diabetes mellitus, lowering both basal and postprandial plasma glucose. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. Unlike SUs, Metformin does not produce hypoglycemia in either patients with type 2 diabetes mellitus or normal subjects (except in special circumstances) and does not cause hyperinsulinemia. With Metformin therapy, insulin secretion remains unchanged while fasting With Metformin therapy, insulin secretion remains unchanged while fasting.

Indication

Linamet 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

LINAMET should be given twice daily with meals. Dose escalation should be gradual to reduce thegastrointestinal (GI) side effects associated with metformin use. For available dosage forms and strengths.

 

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 taken at each of the two daily meals (e.g., a patient on metformin 1000 mg twice daily would be started on 2.5 mg linagliptin/1000 mg metformin hydrochloride twice daily with meals).

 

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

 

  • No studies have been performed specifically examining the safety and efficacy of LINAMET in patients previously treated with other oral antihyperglycemic agents and switched to LINAMET. Any change in therapy of type 2 diabetes mellitus should be undertaken with care and appropriate monitoring as changes in glycemic control can occur.

 

Concomitant Use with an Insulin Secretagogue (e.g., Sulfonylurea) or with Insulin

When LINAMET is used in combination with an insulin secretagogue (e.g., sulfonylurea) or with insulin, a lower dose of the insulin secretagogue or insulin may be required to reduce the risk of hypoglycemia.

Side Effects

Adverse reaction reported in >5% of patients treated with Linamet and more commonly than in patients treated with placebo are nasopharyngitis and diarrhea. Hypoglycemia was more commonly reported in patients treated with the combination of Linamet and SU compared with those treated with the combination of SU and Metformin.

Contraindications

LINAMET is contraindicated in patients with:

 

  • Renal impairment (e.g., serum creatinine ≥1.5 mg/dL for men, ≥1.4 mg/dL for women, or abnormal creatinine clearance), which may also result from conditions such as cardiovascular collapse (shock), acute myocardial infarction, and septicemia.

 

  • Acute or chronic metabolic acidosis, including diabetic ketoacidosis. Diabetic ketoacidosis should be treated with insulin.

 

  • A history of hypersensitivity reaction to linagliptin, such as anaphylaxis, angioedema, exfoliative skin conditions, urticaria, or bronchial hyperreactivity.

 

  • Hypersensitivity to metformin

Drug Interactions

  • Cationic drugs eliminated by renal tubular secretion: May reduce metformin elimination. Use with caution.

 

  • Strong P-glycoprotein/CYP3A4 inducer: The efficacy of LINAMET may be reduced when administered in combination (e.g., rifampin). Use of alternative treatments is strongly recommended.

Precautions

Lactic acidosis: Warn against excessive alcohol use. LINAMET is not recommended in hepatic impairment or hypoxic states and is contraindicated in renal impairment. Ensure normal renal function before initiating and at least annually thereafter.

                 

  • There have been postmarketing reports of acute pancreatitis, including fatal pancreatitis. If pancreatitis is suspected, promptly discontinue LINAMET.

 

  • Temporarily discontinue LINAMET in patients undergoing radiologic studies with intravascular administration of iodinated contrast materials or any surgical procedures necessitating restricted intake of food and fluids.

 

  • Hypoglycemia: When used with an insulin secretagogue (e.g.sulfonylurea (SU)) or insulin, consider lowering the dose of the insulin secretagogue or insulin to reduce the risk of hypoglycemia.

 

  • There have been postmarketing reports of serious hypersensitivity reactions in patients treated with linagliptin (one of the components of LINAMET) including anaphylaxis, angioedema, and exfoliative skin conditions. In such cases, promptly discontinue LINAMET, assess for other potential causes, institute appropriate monitoring and treatment, and initiate alternative treatment for diabetes.

 

  • Vitamin B12 deficiency: Metformin may lower vitamin B12 levels. Monitor hematologic parameters annually.

 

  • Arthralgia: Severe and disabling arthralgia has been reported in patients taking DPP-4 inhibitors. Consider as a possible cause for severe joint npain and discontinue drug if appropriate.

 

  • Macrovascular outcomes: No conclusive evidence of macrovascular risk reduction with LINAMET or any other antidiabetic drug.

Over Dosage

In the event of an overdose with LINAMET, contact the Poison Control Center. Employ the usual supportive measures (e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring, and institute supportive treatment) as dictated by the patient’s clinical status. Removal of linagliptin by hemodialysis or peritoneal dialysis is unlikely. However, metformin is dialyzable with a clearance of up to 170 mL/min under good hemodynamic conditions. Therefore, hemodialysis may be useful partly for removal of accumulated metformin from patients in whom LINAMET overdosage is suspected.

 

Linagliptin

During controlled clinical trials in healthy subjects, with single doses of up to 600 mg of linagliptin (equivalent to 120 times the recommended daily dose), there were

no dose-related clinical adverse drug reactions. There is no experience with doses above 600 mg in humans.

 

Metformin

Overdose of metformin has occurred, including ingestion of amounts greater than 50 grams. Hypoglycemia was reported in approximately 10% of cases, but no causal association with metformin has been established. Lactic acidosis has been reported in approximately 32% of metformin overdose cases.

Pharmaceutical Precautions

Protect from exposure to high humidity. Store in a safe place out of reach of children.

Commercial Pack

LinametTM 2.5/500: Each box contains 2 x 10’s Tablets in Alu-Alu blister pack.

 

LinametTM 2.5/850: Each box contains 2 x 10’s Tablets in Alu-Alu blister pack.