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T2D Medicine DPP-4 Inhibitor (Januvia)

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By Thiruvelan, 23 June, 2010
T2D Medicine DPP-4 Inhibitor (Januvia)

Januvia (DPP-4 inhibitor) lowers blood-glucose by helping body to make more insulin when needed. In addition, it stops the liver from putting glucose into the blood.

DPP-4 inhibitor or gliptin works by increasing the amount of insulin released by your body and decreasing the amount of sugar made by your body.  Dipeptidyl-peptidase 4 inhibitors preferentially target postprandial glucose excursions; however, it also shows to reduce fasting plasma glucose levels.

Dipeptidyl-Peptidase 4 Inhibitors mechanism of action

DPP-4 inhibitors work by increasing incretin levels (GLP-1 and GIP) this inhibits glucagon release, which increases insulin secretion, delay gastric emptying, and decreases blood-glucose levels.

Dipeptidyl-Peptidase 4 Inhibitors diabetes medications

  • Generic Name: Linagliptin (Brand Name: Tradjenta)
  • Generic Name: Saxagliptin (Brand Name: Onglyza)
  • Generic Name: Sitagliptin (Brand Name: Januvia)
  • Generic Name: Alogliptin (Brand Name: Nesina)

DPP-4 inhibitor’s dosage

The recommended dose is 5 mg once daily, can be taken with or without food.

Side effects of DPP-4 inhibitors

Long-term side effects of DPP-4 inhibitors on mortality and morbidity are so far inconclusive.

Although adverse effects include:

nasopharyngitis (the common cold),

headache, nausea,

hypersensitivity, and

skin reactions have observed in clinical studies.

What can you expect for DPP-4 inhibitors?

DPP-4 inhibitors can lower your A1C by 0.5 to 1.0%, fasting plasma glucose level by 11 to 22 mg/dL or 0.611 to 1.222 mmol/l, postprandial glucose level by 24 to 35 mg/dL or 1.333 to 1.944 mmol/l. There is no change in lipid, no hypoglycemia, no weight gain. A greater reduction in blood glucose levels is in the case of higher baseline A1C level (i.e., A1C ≥ 9.0%). However, the history of previous, glucose-lowering treatment generally results in a smaller reduction in blood glucose levels.

Who can benefit from DPP-4 inhibitors?

While they do not lower glucose as much compared to existing therapies, they offer many potential advantages.  It can achieve sustainable reductions in HbA1c with a low risk of hypoglycemia and no weight gain. It can administer as a once-daily oral dose.

Who should avoid using DPP-4 inhibitors?

Avoid Januvia, if you are pregnant or breast-feeding, having kidney disease, or type 1 with diabetic ketoacidosis.

When compared to sulfonylurea, DPP4 inhibitor is safer with lesser hypoglycemic episodes. However, in combination with other drugs, it has a somewhat higher rate of hypoglycemia. DPP-4 has an association with the immune system; it thought to inhibit it and might impair the immune system. Thus, increase the risk of upper respiratory infection (6.3%) and nasopharyngitis (inflammation of the nose and pharynx in 5.2%).

Primarily, the kidneys break it down and in a small extent by the liver; so the potential for it to interact with other drugs is relatively low.  Thus, DPP-4 inhibitors (only in reduced doses) are safe for treating patients with moderate and severe renal failure.

The most worrying side effects are:

allergic reaction causing anaphylaxis,

low blood pressure, and

angioedema, swelling of the tongue, face, and throat.

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