XELEVIA ® - Sitagliptin

XELEVIA ® a Sitagliptin-based drug

THERAPEUTIC GROUP: Oral hypoglycemic agents - DPP-4 inhibitors

Indications XELEVIA ® - Sitagliptin

XELEVIA ® is indicated in the treatment of type II diabetes mellitus when non-pharmacological measures or single therapy with metformin, sulfonylureas and PPAR gamma agonists do not produce the expected results.
The combined therapy between Sitagliptin and the aforementioned active ingredients therefore guarantees better glycemic control than monotherapies.

Mechanism of action XELEVIA ® - Sitagliptin

Sitagliptin, active ingredient contained in XELEVIA ® belongs to DPP-4 inhibitors, a new pharmacological family characterized by the hypoglycemic effect.
Taken orally, in fact, this is absorbed in the intestine, reaching the maximum plasma concentration within the first 4 hours of intake with an absolute bioavailability of 87%.
Reversibly bound to plasma proteins for about 40%, it carries out its therapeutic action by inhibiting the enzyme DPP-4 (Dipepetidil Peptidase 4), responsible for the irreversible hydrolysis of hormones known as incretins.
The latter, namely GLP1 (Glucagon-like peptide 1) and GIP (Glucose-dependent insulinotropic peptide), can act at the pancreatic level, through intracellular pathways, enhancing the production and secretion of insulin and inhibiting that of glucagon.
This important action results in an evident metabolic implication, that is in a hypoglycemic effect supported both by the greater availability of insulin and by the reduced synthesis of endogenous glucose.
At the end of its action sitagliptin is eliminated unchanged mainly by the kidney, while only a small part of the dose taken undergoes hepatic metabolism.

Studies carried out and clinical efficacy


Endocr J. 2011 Jan 30; 58: 69-73. Epub 2010 Dec 28.

Sitagliptin reduces albuminuria in patients with type 2 diabetes.

Hattori S.

Interesting study that has shown how the administration of sitagliptin in diabetic patients of the second type, can reduce albuminuria, not by acting on the glomerular filtration rate, but by improving that series of related metabolic aspects such as hyperglycemia, blood pressure and level of inflammation, particularly evident in these patients.


Diabetes Metab Syndr Obes. 2010 Mar 29; 3: 31-41.

Use of DPP-4 inhibitors in type 2 diabetes: focus on sitagliptin.

Ahrén B.

The clinical trial of sitagliptin in recent years has shown a particular efficacy of the drug in improving the glycemic profile, supporting the functionality of pancreatic beta cells, with a high safety profile capable of minimizing the risk of hypoglycemia, weight gain. and gastrointestinal disorders


Wien Klin Wochenschr. 2011 Mar 31.

Efficacy and Tolerability of Sitagliptin in Type 2 Diabetic Patients Inadequately Controlled with Metformin. A Prospective Observational Study in Austrian Primary Care.

Ludvik B, Daniela L.

Clinical trial conducted on about 2300 diabetic patients, previously treated with maximum doses of metformin without achieving adequate glycemic control, in which the concomitant intake of sitagliptin allowed a marked improvement in the glycemic profile, with a reduction of "glycosylated hemoglobin and fasting glycemia. and postprandial.

Method of use and dosage

XELEVIA ® sitagliptin 25 mg tablets: in normal clinical practice the most used dosage of XELEVIA ® is that of 100 mg taken in a single daily administration.
However, it is of fundamental importance that the correct dosage and the relative modalities of assumption are established by one's doctor based on the possible presence of other therapies in progress, the physio-pathological conditions of the patient and his metabolic condition.

XELEVIA ® Warnings - Sitagliptin

It should be remembered that the management of second type diabetic disease should include among its therapeutic tools not only pharmacological measures but also daily actions such as a healthy diet and a correct lifestyle.
During therapy with XELEVIA ® it is necessary to periodically monitor the glycemic levels, especially when in combination with sulfonylureas, to avoid the risk of hypoglycemia and to compensate in the way to improve any metabolic decompensation.
The risk of hypoglycemia could in fact reduce the patient's perceptive abilities, making the use of machinery and driving cars dangerous.


XELEVIA ® is contraindicated during pregnancy and lactation, given the absence of clinical data on the safety profile of this drug on fetal health, and given the availability on the market of antidiabetic drugs whose activity is better characterized.


The possible interactions between sitagliptin and other active ingredients are particularly rare, given the low hepatic metabolism to which the drug undergoes.
In general, the intake of cyclosporine and digoxin concomitantly with that of sitagliptin, could determine the appearance of side effects following the change in the pharmacokinetic profile.
Studies have shown that for patients with impaired renal function, it is possible to describe interactions, often clinically insignificant, between potent inhibitors of CYP3A4 and sitagliptin.
However, given the use of sitagliptin in combination therapy with other oral hypoglycemic agents, possible interactions and dose adjustments should be considered.

Contraindications XELEVIA ® - Sitagliptin

XELEVIA ® contraindicated in case of hypersensitivity to the active substance or to one of its excipients, in patients with reduced renal function, type I diabetes and diabetic ketoacidosis, and during pregnancy and lactation.

Undesirable Effects - Side Effects

The clinical trial, which today represents the main source of data on the safety profile of sitagliptin, has shown that the administration of XELEVIA ® is well tolerated and in some cases (combined therapy) can reduce the incidence of side effects observed later. high-dose monotherapy.
In general, the most described side effects were gastrointestinal reactions such as nausea, vomiting, diarrhea and flatulence, headache and dizziness and peripheral edema.
Clinically more significant adverse reactions and hypersensitivity reactions were instead observed rarely and mainly concerned cardiac and bone function as well as the haematological profile.


XELEVIA ® can only be sold under strict medical prescription.

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