Gliptinestad 100

Rx

Indications

For adult patients with type 2 diabetes mellitus, Gliptinestad 100 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 (PPARγ) agonist (i.e. a thiazolidinedione): When use of a PPARγ agonist is appropriate and when diet and exercise plus the PPARγ 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 PPARγ agonist and metformin: When use of a PPARγ agonist is appropriate and when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.
• Gliptinestad 100 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 PPARγ agonist, the dose of metformin and/or PPARγ agonist should be maintained, and sitagliptin administered concomitantly.
• When sitagliptin 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 100 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. Sitagliptin 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 sitagliptin and periodically thereafter.
• Hepatic impairment
  No dose adjustment is necessary for patients with mild to moderate hepatic impairment. Sitagliptin has not been studied in patients with severe hepatic impairment and care should be exercised. However, because sitagliptin is primarily renally eliminated, severe hepatic impairment is not expected to affect the pharmacokinetics of sitagliptin.
• No dose adjustment is necessary based on age.
• Sitagliptin should not be used in children and adolescents 10 to 17 years of age because of insufficient efficacy.

Usage

• Gliptinestad 100 can be taken with or without food.

Hypersensitivity to sitagliptin or to any of the excipients.

Common

• Hypoglycaemia,
• Headache.

Uncommon

• Dizziness,
• Constipation,
• Pruritus.

• Gliptinestad 100 should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.
• If acute pancreatitis is confirmed, Gliptinestad 100 should not be restarted. Caution should be exercised in patients with a history of pancreatitis.
• Hypoglycaemia has been observed when sitagliptin was used in combination with insulin or a sulphonylurea. Therefore, to reduce the risk of hypoglycaemia, a lower dose of sulphonylurea or insulin may be considered.
• 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.
• 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. Onset of these reactions occurred within the first 3 months after initiation of treatment, with some reports occurring after the first dose. If a hypersensitivity reaction is suspected,
• Gliptinestad 100 should be discontinued. Other potential causes for the event should be assessed, and alternative treatment for diabetes initiated.
• There have been post-marketing reports of bullous pemphigoid in patients taking sitagliptin. If bullous pemphigoid is suspected, Gliptinestad 100 should be discontinued.
• Gliptinestad 100 should not be used during pregnancy and breast-feeding.
• Gliptinestad 100 has no or negligible influence on the ability to drive and use machines. However, it should be taken into account that dizziness and somnolence have been reported. In addition, there is also the risk of hypoglycaemia when Gliptinestad 100 is used in combination with a sulphonylurea or with insulin.