Sitagliptin

Sitagliptin is a diabetes medication with the brand name Januvia. It belongs to the class of diabetes drugs known as Dipeptidyl Peptidase-4 (DDp-4) Inhibitor. This diabetes medicine was approved by the FDA in 2006 for the treatment of type 2 diabetes.

The use of this type 2 diabetic medicine shows reduction in the patient’s hemoglobin A1C levels, fasting blood glucose and after meal blood sugar. This drug does not seem to affect the patient’s body weight.

Inactive components of Januvia, according to MERK are: microcrystalline cellulose, anhydrous dibasic calcium phosphate, croscarmellose sodium, magnesium stearate, and sodium stearyl fumarate


How Januvia works

In normal individuals, some hormones, called incretin hormones rise after a meal and cause insulin release. These incretin hormones are eventually destroyed by the enzymes called DDP-4, so that insulin is significantly reduced when the glucose from food is used up and blood glucose is at fasting levels.

Januvia works by slowing the action of this DDP-4, so that it does not destroy the incretin hormones quickly. What now happens is that the incretin hormones stay longer in the blood after meals and cause the after-meal release of insulin to be increased and prolonged.

It works by stopping the destruction of the hormones that trigger insulin release after a meal, thereby raising the blood insulin after a meal. It also increases the body’s positive response to insulin and decreases the amount of glucagon in the blood. Glucagon is the hormone that tells the body to increase the blood glucose.

This action is desirable because it releases more insulin only after meals and that reduces the adverse reaction of hypoglycemia. It has an advantage over some diabetic medicines, like sulfonylurea, which causes the pancreas to release insulin, whether or not there is food available to provide glucose. When there is no glucose in the blood, the sulfonylurea then causes hypoglycemia.

Most of Januvia is removed through the kidney mostly as unchanged drug. Small portion of the drug is metabolized and removed in feces.

How Januvia is supplied

This diabetic drug comes in three dosage strength tablets:

  • 100mg tablet
  • 50mg tablets
  • 25mg tablets


How to Use Januvia

  • It is to be used in combination with diabetic diet and exercise in the control of diabetes.
  • Only a doctor can prescribe Januvia. The usual dose is 100mg once daily. It is not necessary to take with food. The dose should be adjusted to 50mg daily for people with moderate kidney disease and 25mg for those with end-stage kidney disease, including those on dialysis. The doctor usually checks the kidney function before starting a patient on this medication, and periodically during the cause of treatment.
  • Take with or without food.
  • Swallow the pill whole.
  • Take once a day because it works for 24 hours.
  • During stress, illness, trauma, infection or surgery, patients’ blood glucose may change, so it is necessary to contact your physician. In some cases, insulin may be introduced temporarily until the situation resolves.
  • Stop taking this medication and contact your doctor if you develop abdominal pain that radiates to the back, as this may be a sign of pancreatitis.
  • Check your hemoglobin A1c as recommended by your doctor, to check the continued effects of the drug.


Adverse reactions with Januvia

  • Hypoglycemia can occur, especially when used in combination with sulfonylurea and/or insulin. The dose of insulin and sulfonylurea should be lowered for patients on this drug. Though hypoglycemia can occur with this diabetic medication, it does so at a significantly lower rate than sulfonylureas. This is because the extra insulin secretion by Januvia occurs mostly after a meal in response to the increase in the blood glucose.
  • Allergic reactions, like Body swelling or angioedema, anaphylaxis and Stevens-Johnson syndrome. Other allergic reactions are itch, rash, redness and peeling of the skin. Stop the use of this medication immediately if allergic reaction occurs.
  • Kidney problems, including acute kidney failures that have required dialysis have been reported.
  • Headache
  • Upper respiratory infections
  • Nasopharyngitis.

The adverse reactions and drug interactions noted in clinical trials it was used appropriately were minimal. This is attributed to the fact that Januvia does not bind very much to blood plasma proteins.


Drug interactions with Januvia

Hypoglycemia when used in combination with sulfonylurea or other insulin secretagogues and/or insulin. The dosage of the sulfonylurea and/or insulin may need to be lowered in this instance.

Insulin secretagogues are the diabetic medicines that cause the pancreas to secret insulin.

Sitagliptin may increase digoxin levels in the blood. While this has not been proved to pose a risk for digoxin toxicity, the doctor should pay close attention to the digoxin levels of patients who are taking digoxin and sitagliptin simultaneously.


Who Should Not Take Januvia

  • Patients with type 1 diabetes
  • Children, eighteen years and under as safety of this drug has not been proven in this population.
  • Patients in diabetic ketoacidosis or diabetic non-ketotic coma.
  • Patients who are allergic to sitagliptin or any of the inactive components of the drug.
  • Patients with history of pancreatitis. If you develop pancreatitis while on sitagliptin, you should stop taking sitagliptin immediately.


Do Not

Do not crush, split or chew Januvia tablets.

Do not take sitagliptin if you are allergic to this sitagliptin or any of its inactive ingredients.


Special Considerations

Use with caution in pregnant women.

Use cautiously in patients with history angioedema reactions to any DDP-4 inhibitor, kidney problems and pancreatitis. There may be a possibility that these populations are more prone to these reactions.

Caution should be taken when used in breast-feeding women. It was found to be secreted in milk of rat.

Januvia is not to be used in children 18 years or lower because it has not been determined to work or be safe for this population.

Use sitagliptin in the elderly patients with caution, because it is mostly cleared by the kidney. Elderly patients with good kidney function may be able to use this medication safely.


Januvia Overdose

Small changes in heart rhythm (QTc changes of 8 milliseconds) were noted

when patients were given 800mg of sitagliptin. The level of the drug in their blood was up about 11 times higher than the regular blood level when patients take the 100mg daily dose. All sitagliptin overdose should be reported to the doctor. High overdoses need to be treated in the hospital with immediate removal of the medication from the stomach and bowels, hemodialysis and close heart monitoring. Unfortunately, about 4 hours of hemodialysis can only remove about 13.5% of the drug. The good news is that it may take many milligrams above the usual dose to get into such overdose.

Treat hypoglycemia as usual if that occurs.

Combination Medicines Containing Sitagliptin

Januvia and metformin are combined in the brand name drug Janumet.

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