Gliptinestad 50

Rx

Indication

For adult patients with type 2 diabetes mellitus, Gliptinestad 50 is indicated to improve glycaemic control:

• As monotherapy:
  In patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance.
• As dual oral therapy in combination with:
  + Metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control.
  + A sulphonylurea when diet and exercise plus maximal tolerated dose of a sulphonylurea alone do not provide adequate glycaemic control and when metformin is inappropriate due to contraindications or intolerance.
  + A peroxisome proliferator-activated receptor gamma (PPARy) agonist (i.e. a thiazolidinedione) when use of a PPARy agonist is appropriate and when diet and exercise plus the PPARy agonist alone do not provide adequate glycaemic control.
• As triple oral therapy in combination with:
  + A sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.
  + A PPARy agonist and metformin when use of a PPARy agonist is appropriate and when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.
• Gliptinestad 50 is also indicated as add-on to insulin (with or without metformin) when diet and exercise plus stable dose of insulin do not provide adequate glycaemic control.

Dosage

The dose is 100 mg sitagliptin once daily. When used in combination with metformin and/or a PPARy agonist, the dose of metformin and/or PPARy agonist should be maintained, and Gliptinestad 50 administered concomitantly.

When Gliptinestad 50 is used in combination with a sulphonylurea or with insulin, a lower dose of the sulphonylurea or insulin may be considered to reduce the risk of hypoglycaemia.

If a dose of Gliptinestad 50 is missed, it should be taken as soon as the patient remembers. A double dose should not be taken on the same day.

Special populations

• Renal impairment
  When considering the use of sitagliptin in combination with another anti-diabetic medicinal product, its conditions for use in patients with renal impairment should be checked.
  For patients with mild renal impairment (glomerular filtration rate [GFR] ≥ 60 to < 90 ml/min), no dose adjustment is required.
  For patients with moderate renal impairment (GFR ≥ 45 to < 60 ml/min), no dosage adjustment is required.
  For patients with moderate renal impairment (GFR ≥ 30 to < 45 ml/min), the dose of sitagliptin is 50 mg once daily.
  For patients with severe renal impairment (GFR ≥ 15 to < 30 ml/min) or with end-stage renal disease (ESRD) (GFR < 15 ml/min), including those requiring haemodialysis or peritoneal dialysis, the dose of sitagliptin is 25 mg once daily. Gliptinestad may be administered without regard to the timing of dialysis.
  Because there is a dosage adjustment based upon renal function, assessment of renal function is recommended prior to initiation of Gliptinestad 50 and periodically thereafter.
• Hepatic impairment
  No dose adjustment is necessary for patients with mild to moderate hepatic impairment.
• Elderly
  No dose adjustment is necessary based on age.
• Paediatric population
  Children and adolescents 10 to 17 years of age should not be indicated sitagliptin because of insufficient efficacy.
  Sitagliptin has not been studied in paediatric patients under 10 years of age.

Usage

Gliptinestad 50 can be taken with or without food.

Hypersensitivity to sitagliptin or to any of the excipients.

Common

• Hypoglycaemia,
• Headache.

Uncommon

• Dizziness,
• Constipation,
• Pruritus.

• General
  Gliptinestad 50 should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.
• Acute pancreatitis
  Use of DPP-4 inhibitors has been associated with a risk of developing acute pancreatitis. If pancreatitis is suspected, Gliptinestad 50 and other potentially suspect medicinal products should be discontinued; if acute pancreatitis is confirmed, Gliptinestad 50 should not be restarted. Caution should be exercised in patients with a history of pancreatitis.
  Hypoglycaemia when used in combination with other anti-hyperglycaemic medicinal products.
  In clinical trials of sitagliptin as monotherapy and as part of combination therapy with medicinal products not known to cause hypoglycaemia (i.e. metformin and/or a PPARy agonist).
• Renal impairment
  Sitagliptin is renally excreted. To achieve plasma concentrations of sitagliptin similar to those in patients with normal renal function, lower dosages are recommended in patients with GFR < 45 ml/min, as well as in ESRD patients requiring haemodialysis or peritoneal dialysis.
  When considering the use of sitagliptin in combination with another anti-diabetic medicinal product, its conditions for use in patients with renal impairment should be checked.
• Hypersensitivity reactions
  Post-marketing reports of serious hypersensitivity reactions in patients treated with sitagliptin have been reported. These reactions include anaphylaxis, angioedema, and exfoliative skin conditions including Stevens-Johnson syndrome.
• Bullous pemphigoid
  There have been post-marketing reports of bullous pemphigoid in patients taking DPP-4 inhibitors including sitagliptin. If bullous pemphigoid is suspected, Gliptinestad 50 should be discontinued.
• Due to lack of human data, Gliptinestad 50 should not be used during pregnancy and lactation.
• Gliptinestad 50 has no or negligible inlfuence on the ability to drive and use machines.
• Patients should be altered to the risk of hypoglycaemia when Gliptinestad 50 is used in combination with a sulphonylurea or with insulin.