Indications

Coport L tablet is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Pharmacology

Linagliptin inhibits DPP-4 enzyme which declines the incretin hormones glucagon-like peptide-1(GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Linagliptin increases the
concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon. Both incretin hormones are involved in the
physiological regulation of glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake. GLP-1 and GIP increase insulin
biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. Furthermore, GLP-1 also reduces glucagon secretion from pancreatic alpha cells,
resulting in a reduction in hepatic glucose output.

Empagliflozin is an inhibitor of Sodium-glucose co-transporter 2 (SGLT2). SGLT2 is the predominant transporter responsible for reabsorption of glucose from kidney back into the circulation. By
inhibiting SGLT2, Empagliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion.

Dosage & Administration

Recommended dose: 10 mg Empagliflozin and 5 mg Linagliptin once daily, taken in the morning, with or without food.

Increased dose: Dose may be increased to 25 mg Empagliflozin and 5 mg Linagliptin once daily.

Renal impaired patients: Assess renal function before initiating this tablet. Do not initiate this tablet if eGFR is below 45 mL/min/1.73 m2- Discontinue taking this tablet if eGFR falls below 45
ml/min/1.73 m2

Interaction

Diuretics: Coadministration of Empagliflozin with diuretics resulted in increased urine volume and frequency of voids, which might enhance the potential for volume depletion.

Insulin or Insulin Secretagogues: Coadministration of Empagliflozin with Insulin or Insulin secretagogues increases the risk for hypoglycemia.

Inducers of P-glycoprotein or CYP3A4 Enzymes: Rifampin decreased Linagliptin exposure, suggesting that the efficacy of Linagliptin may be reduced when administered in combination with a strong
P-gp or CYP3A4 inducer.

Positive Urine Glucose Test: SGLT2 inhibitors increase urinary glucose excretion and will lead to positive urine glucose tests.

Interference with 1,5-anhydroglucitol (1,5-AG) Assay: Measurements of 1,5-AG are unreliable in assessing glycemic control in patients taking SGLT2 inhibitors.

Inducers of P-glycoprotein or CYP3A4 Enzymes: Rifampin decreased linagliptin exposure, suggesting that the efficacy of linagliptin may be reduced when administered in combination with a strong
P-gp or CYP3A4 inducer.

Contraindications

· Severe renal impairment, end-stage renal disease, or dialysis
. History of hypersensitivity reaction to Linagliptin, such as anaphylaxis, angioedema, exfoliative skin conditions, urticaria, or bronchial hyperreactivity
. History of serious hypersensitivity reaction to Empagliflozin