Saxagliptin

1. Introduction

Saxagliptin is an oral anti-diabetic medication belonging to the dipeptidyl peptidase-4 (DPP-4) inhibitor class. It is used in the management of type 2 diabetes mellitus (T2DM) to improve glycaemic control. Saxagliptin works by enhancing the action of incretin hormones, which increases insulin secretion and reduces glucagon secretion, leading to better blood glucose regulation.

2. Indications

  • Type 2 Diabetes Mellitus:
    • As monotherapy or in combination with other anti-diabetic agents (e.g., metformin, sulfonylureas, or insulin) to improve glycaemic control.
  • Prevention of Diabetes Complications:
    • Reducing hyperglycaemia-associated risks of cardiovascular complications in T2DM.

3. Dosage

Adults:

  • Standard Dose: 2.5 mg or 5 mg orally once daily, with or without food.

Patients with Renal Impairment:

  • Moderate renal impairment (eGFR ≥30 to <45 mL/min/1.73m²): 2.5 mg once daily.
  • Severe renal impairment (eGFR <30 mL/min/1.73m²): 2.5 mg once daily.
  • Dialysis patients: 2.5 mg once daily after dialysis.

Elderly:

  • Same as adult dosing, but monitor renal function closely.

Children:

  • Safety and efficacy have not been established in patients <18 years.

4. Administration

  • Take once daily, at the same time each day.
  • Can be taken with or without food.

5. Forms Available

  • Tablets: 2.5 mg, 5 mg

6. Side Effects

6.1 Common Side Effects:

  • Upper respiratory tract infections
  • Nasopharyngitis
  • Headache

6.2 Less Common Side Effects:

  • Hypoglycaemia (especially when combined with sulfonylureas or insulin)
  • Abdominal pain
  • Fatigue

6.3 Rare but Serious Side Effects:

  • Pancreatitis (severe abdominal pain, nausea)
  • Joint pain (arthralgia)
  • Heart failure (in patients with a history of cardiovascular disease)
  • Severe allergic reactions (e.g., angioedema, rash)

7. Warnings

  • Heart Failure Risk: Use cautiously in patients with a history of heart failure, as saxagliptin may increase the risk of hospitalisation due to heart failure.
  • Pancreatitis: Monitor for signs of acute pancreatitis and discontinue if suspected.
  • Severe Hypersensitivity Reactions: Discontinue if severe allergic reactions occur.
  • Renal Function: Regular monitoring is required, particularly in patients with renal impairment.

8. Precautions

  • Use cautiously in elderly patients due to the higher likelihood of renal impairment.
  • Avoid use in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.
  • Adjust dose in patients with renal impairment to prevent drug accumulation.

9. Interactions

  • Sulfonylureas or Insulin: Increased risk of hypoglycaemia; dose adjustments may be needed.
  • CYP3A4 inhibitors (e.g., ketoconazole, itraconazole): May increase saxagliptin levels; consider dose adjustment.
  • CYP3A4 inducers (e.g., rifampin, phenytoin): May reduce the efficacy of saxagliptin.
  • Other Antidiabetic Agents: Monitor closely for hypoglycaemia when combined.

10. Monitoring Parameters

  • Glycaemic control (HbA1c, fasting blood glucose) at baseline and periodically during treatment.
  • Renal function (eGFR) before initiation and periodically during therapy.
  • Monitor for signs of pancreatitis (persistent severe abdominal pain).
  • Monitor for signs of heart failure, especially in high-risk patients.

11. Use in Children

  • Not approved for use in children under 18 years due to insufficient safety and efficacy data.

12. Use in Pregnancy

  • Category B: Use only if the potential benefit justifies the risk to the foetus. Limited human data is available; animal studies have not shown direct harm.

13. Use in Elderly

  • Safe for use in elderly patients, but renal function should be monitored closely to avoid drug accumulation and side effects.

14. Use in Kidney Disease

  • Dose adjustments are necessary in moderate to severe renal impairment (eGFR <45 mL/min/1.73m²).
  • Avoid use in patients with end-stage renal disease not on dialysis.

15. Use in Liver Disease

  • No dose adjustment is required for mild to moderate hepatic impairment. Limited data is available for severe hepatic impairment.

16. Patient Counselling Points

  • Take saxagliptin as prescribed, once daily at the same time each day.
  • Report symptoms such as severe abdominal pain or persistent fatigue to your doctor immediately.
  • Inform your doctor if you experience unexplained swelling, shortness of breath, or rapid weight gain (possible signs of heart failure).
  • Maintain a healthy diet and exercise routine for optimal diabetes control.
  • Do not skip doses, and check your blood glucose levels regularly as instructed.

17. Table of Brand Names, Manufacturer, and Prices in USD

Brand NameManufacturerStrength/Dosage FormPrice (USD)
OnglyzaAstraZeneca5 mg Tablet$450 (30 tablets)
Generic SaxagliptinVarious5 mg Tablet$200 (30 tablets)

18. 15 FAQs (Frequently Asked Questions)

1. What is Saxagliptin used for?
Saxagliptin is used to manage type 2 diabetes and improve blood sugar levels.

2. How does Saxagliptin work?
It inhibits DPP-4, which increases incretin hormone levels, enhancing insulin secretion and reducing glucagon levels.

3. Can Saxagliptin be taken with metformin?
Yes, it is commonly combined with metformin for better glycaemic control.

4. Is Saxagliptin safe in kidney disease?
Yes, but dose adjustments are required in moderate to severe renal impairment.

5. Can Saxagliptin cause hypoglycaemia?
Rarely when used alone, but the risk increases when combined with insulin or sulfonylureas.

6. Can Saxagliptin cause pancreatitis?
Yes, though rare, pancreatitis is a potential side effect. Report severe abdominal pain immediately.

7. Can Saxagliptin cause weight gain?
No, saxagliptin is weight-neutral, meaning it does not typically cause weight gain.

8. Can Saxagliptin be used in type 1 diabetes?
No, it is only approved for type 2 diabetes.

9. Is Saxagliptin safe during pregnancy?
It is not commonly used during pregnancy; consult your doctor for alternative therapies.

10. Can Saxagliptin be taken with food?
Yes, it can be taken with or without food.

11. What should I do if I miss a dose of Saxagliptin?
Take the missed dose as soon as you remember, but skip it if it is close to the next scheduled dose.

12. Does Saxagliptin require routine blood monitoring?
Yes, monitor HbA1c, fasting glucose, and kidney function regularly.

13. Can Saxagliptin cause joint pain?
Yes, severe joint pain has been reported as a rare side effect.

14. How long does Saxagliptin take to work?
It may take several weeks to see improvements in blood sugar levels.

15. Can Saxagliptin be used in combination with insulin?
Yes, but close monitoring is required to avoid hypoglycaemia.