Pharmacy Diabetes

Formulations-Sitagliptin Phosphate Monohydrate

Sitagliptin phosphate monohydrate

  • Januvia is available for oral use as film coated tablets containing sitagliptin phosphate monohydrate equivalent to 25, 50 or 100 mg of free base.

  • Treatment of type 2 diabetes in adults where physical activity and dietary management has not resulted in adequate glycaemic targets.
  • Monotherapy when metformin is considered inappropriate due to intolerance; or
  • in combination with other anti-hyperglycaemic agents, including insulin.

For the most up to date PBS therapeutic indications for sitagliptin, please see
https://www.pbs.gov.au/medicine/item/9180E-9181F-9182G

  • The recommended dose of Januvia is 100 mg once daily, with or without food.
  • Renal impairment:
    eGFR≥ 30 mL/min/1.73 m to < 45 mL/min/1.73 m , the dose of Januvia is 50 mg once daily. eGFR≥ 15 mL/min/1.73 m to < 30 mL/min/1.73 m or with ESRD(eGFR< 15 mL/min/1.73 m ), including those requiring haemodialysis or peritoneal dialysis, the dose of Januvia is 25 mg once daily. Januvia maybe administered without regard to the timing of dialysis.

  • No dosage adjustment is required in this age population.

  • Type 1 diabetes - Januvia should not be used to treat type 1 diabetes or diabetic ketoacidosis.
  • Pancreatitis - There have been reports of acute pancreatitis with all DPP4 inhibitors. If pancreatitis is suspected, Januvia should be discontinued.
  • Renal impairment - Januvia is renally excreted. To achieve plasma concentrations similar to those in those with normal renal function, lower dosages are recommended in patients with eGFR< 45 mL/min/1.73 m, as well those requiring haemodialysis or peritoneal dialysis.

  • Gastrointestinal disorders: Constipation.
  • Infections and infestations: Pharyngitis.
  • Vascular disorders: Hypertension. Gastrointestinal disorders: Acute pancreatitis, including fatal and nonfatal haemorrhagic and necrotising pancreatitis, constipation; vomiting.
  • Musculoskeletal and connective tissue disorders: Arthralgia; myalgia; pain in extremity; back pain

  • Hypersensitivity to sitagliptin or any of the excipients

The absolute bioavailability of sitagliptin is approximately 87%.

  • Sitagliptin is primarily eliminated unchanged in urine, and metabolism is a minor pathway. Approximately 79%of sitagliptin is excreted unchanged in the urine.

The mean volume of distribution at steady state following a single 100 mg intravenous dose of sitagliptin is approximately 198 litres.
The fraction of sitagliptin reversibly bound to plasma proteins is low (38%).