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.
works by stopping the destruction of
the hormones that trigger insulin release after a meal, thereby raising
blood insulin after a meal. It also increases the body’s positive
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:
How to Use Januvia
Adverse reactions with Januvia
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
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.
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.
Small changes in heart rhythm (QTc changes of 8 milliseconds) were notedwhen 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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