Xelevia - Instructions For The Use Of Tablets, Price, Reviews, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Xelevia

Xelevia: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Xelevia

ATX code: A10BH01

Active ingredient: sitagliptin (Sitagliptin)

Producer: Berlin-Pharma, JSC (Russia)

Description and photo update: 2019-24-07

Prices in pharmacies: from 999 rubles.

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Xelevia is a hypoglycemic drug, an inhibitor of dipeptidyl peptidase-4 (DPP-4).

Release form and composition

Dosage form of Kselevia - film-coated tablets: beige, biconvex, round, smooth on one side, engraved on the other “277” (in a cardboard box 2 blisters containing 14 tablets each) and instructions for use of Kselevia.

Composition of 1 tablet:

• active substance: sitagliptin phosphate monohydrate - 128.5 mg (corresponds to the content of sitagliptin - 100 mg);
• auxiliary components: sodium stearyl fumarate - 12 mg; magnesium stearate - 4 mg; croscarmellose sodium - 8 mg; unmilled calcium hydrogen phosphate - 123.8 mg; microcrystalline cellulose - 123.8 mg;
• film sheath: Opadray II beige 85F17438 [iron oxide red (E 172) - 0.37%; iron oxide yellow (E 172) - 3.07%; talc - 14.8%; polyethylene glycol (macrogol 3350) - 20.2%; titanium dioxide (E 171) - 21.56%; polyvinyl alcohol - 40%] - 16 mg.

Pharmacological properties

Pharmacodynamics

Xelevia is a highly selective inhibitor of the DPP-4 enzyme, which is active when taken orally and is intended for the treatment of type 2 diabetes mellitus.

The active substance of Xelevia (sitagliptin) differs from analogs of glucagon-like peptide-1 (GLP-1) and amylin, α-glucosidase inhibitors, γ-receptor agonists that are activated by the peroxisome proliferator (PPAR-γ), insulin, sulfonylurea derivatives and biguanides differs in both chemical structure and pharmacological action. By inhibiting DPP-4, sitagliptin increases the concentration of two hormones of the incretin family - GLP-1 and glucose-dependent insulinotropic polypeptide (GIP).

Hormones of this family are secreted in the intestine for 24 hours, in response to food intake, their concentration increases. Incretins are part of the internal physiological system of glucose homeostasis regulation. Against the background of normal or elevated blood glucose, hormones of the incretin family promote an increase in insulin synthesis and its secretion by pancreatic β-cells through signaling intracellular mechanisms associated with cyclic adenosine monophosphate (AMP).

Also, GLP-1 leads to the suppression of increased secretion of glucagon by α-cells of the pancreas. A decrease in glucagon concentration with an increase in insulin leads to a decrease in the production of glucose by the liver, which ultimately leads to a decrease in glycemia. This mechanism of action differs from that of sulfonylurea derivatives, which stimulate the release of insulin even at low blood glucose levels. This contributes to the appearance of sulfone-induced hypoglycemia not only in patients with type 2 diabetes mellitus, but also in healthy individuals.

At low blood glucose concentrations, the listed effects of incretins on decreasing glucagon secretion and insulin release are not observed. GIP and GLP-1 have no effect on glucagon release in response to hypoglycemia. The activity of incretins under physiological conditions is limited by the DPP-4 enzyme, which rapidly hydrolyzes them with the formation of inactive products. Sitagliptin prevents this process, due to which the plasma concentrations of the active forms of GIP and GLP-1 increase.

By increasing the content of incretins, Xelevia increases the glucose-dependent release of insulin and helps to reduce the secretion of glucagon. In patients with type 2 diabetes mellitus with hyperglycemia, such changes in the secretion of glucagon and insulin serve to decrease the concentration of glycosylated hemoglobin HbA _1C and decrease the glucose content in blood plasma, determined on an empty stomach and after an exercise test.

Taking a single dose of Xelevia in type 2 diabetes mellitus leads to inhibition of the DPP-4 enzyme activity for 24 hours, which serves to reduce fasting glycemia, as well as after glucose or food load, decrease the concentration of glucagon in the blood plasma, increase the plasma concentration of insulin and C- peptide, increasing the concentration of circulating incretins GLP-1 and GIP by 2 or 3 times.

Pharmacokinetics

After oral administration of sitagliptin at a dose of 100 mg in healthy individuals, its rapid absorption is noted and the maximum concentration (C _max) is reached after 1–4 hours after administration. The area under the concentration-time curve (AUC) increases proportionally to the dose and is 8.52 μmol per 1 liter per hour (when taking 100 mg), C _max - 950 nmol per 1 liter. The plasma AUC of sitagliptin increases by approximately 14% after the next dose of 100 mg of Xelevia, after reaching an equilibrium state after taking the first dose. Coefficients of variation in AUC (inter- and intra-subject) are negligible.

The absolute bioavailability of sitagliptin is approximately 87%. Due to the fact that the combined intake of Kselevia with fatty foods does not affect its pharmacokinetics, it can be taken regardless of food.

In the equilibrium state, the average volume of distribution after taking a single dose of 100 mg in healthy individuals is approximately 198 liters. The plasma protein-binding fraction of sitagliptin is relatively low at 38%.

Almost 79% of sitagliptin is excreted unchanged through the kidneys. Only a small part of the drug that has entered the body is subject to metabolism.

Approximately 16% of sitagliptin radioactive (¹⁴ P-labeled sitagliptin) after oral administration in the form of metabolites excreted. Traces of six of its metabolites were found, presumably not having the ability to inhibit DPP-4. Ongoing in vitro studies have established that CYP2C8 and CYP3A4 are the primary isoenzymes involved in limited drug metabolism.

For 7 days after the oral administration of ¹⁴ C-labeled sitagliptin, almost 100% of the administered substance is excreted in healthy individuals: by the kidneys - 87%, through the intestines - 13%. On average, its half-life when taken orally at a dose of 100 mg is approximately 12.4 hours, and renal clearance is 330 ml per minute.

Excretion of Xelevia occurs primarily through excretion by the kidneys through the mechanism of active tubular secretion. Sitagliptin for the third type of human organic anion transporter (hOAT-3) is a substrate that can be involved in the process of excretion of the substance by the kidneys. Clinical studies of the involvement of hOAT-3 in sitagliptin transport have not been conducted. Xelevia is a substrate of P-glycoprotein, which can also take part in the process of its excretion through the kidneys (however, cyclosporin, an inhibitor of P-glycoprotein, did not decrease the renal clearance of the drug).

Renal failure

To study the pharmacokinetics at varying degrees of severity of chronic renal failure, an open study of sitagliptin in a daily dose of 50 mg was conducted. The volunteers included in the study were divided into the following groups:

• patients with mild renal failure: creatinine clearance (CC) 50–80 ml per minute;
• patients with an average degree of renal failure: CC 30-50 ml in 1 min;
• patients with severe renal failure: CC <30 ml in 1 min;
• patients with end-stage chronic renal failure requiring dialysis.

There were no clinically significant changes in the concentration of sitagliptin in plasma in mild renal failure in comparison with the control group of healthy individuals.

Compared to the control group, the AUC of the drug in moderate renal failure increased almost 2 times, and in severe renal failure and in patients with end-stage chronic renal failure - almost 4 times.

With the help of dialysis, the drug was removed weakly (within 3-4 hours of dialysis session, only 13.5% of its dose was removed).

Given these data, the dose adjustment of Xelevia in order to achieve its therapeutic plasma concentration, similar to that in the normal functioning of the kidneys, should be carried out in case of moderate and severe renal failure.

Liver failure

Against the background of moderate hepatic impairment (on the Child-Pugh scale from 7 to 9 points), with a single dose of 100 mg of sitagliptin, the average C _max and AUC increase approximately by 13 and 21%, respectively. In this regard, correction of the dosage regimen in patients with mild / moderate hepatic impairment is not performed.

There are no clinical data on the use of the drug in severe hepatic impairment (Child-Pugh scale> 9 points). However, given that the substance is primarily excreted by the kidneys, one should not expect a significant change in its pharmacokinetics in such cases.

Elderly age

The age of the patients did not have a clinically significant effect on the pharmacokinetic parameters of the drug. Compared to young patients, the concentration of sitagliptin in the elderly (aged 65 to 80 years) is approximately 19% higher. Depending on age, correction of the dosage regimen of Xelevia is not carried out.

Indications for use

Xelevia is prescribed to improve glycemic control in type 2 diabetes:

• monotherapy: in addition to diet and exercise;
• combination treatment: in cases where adherence to diet, exercise and monotherapy with metformin, sulfonylurea derivatives, PPAR-γ agonists or insulin does not lead to adequate glycemic control - in combination with metformin (drugs are also used for starting therapy), or with sulfonylurea derivatives, or PPAR-γ agonists; in cases where adherence to diet, exercise and therapy with the above two drugs does not provide adequate glycemic control - in combination with metformin and sulfonylurea derivatives, or with metformin and PPAR-γ agonists, or with insulin (without or with metformin).

Contraindications

Absolute:

• moderate and severe renal failure (for sitagliptin at this dosage);
• type 1 diabetes mellitus;
• diabetic ketoacidosis;
• pregnancy and the period of breastfeeding;
• age under 18;
• individual intolerance to the components of the drug.

With caution, under medical supervision, Xelevia is prescribed to patients with pancreatitis.

Xelevia, instructions for use: method and dosage

The tablets are taken orally, regardless of food. The recommended dose of the drug is 1 tablet (100 mg) once a day. Xelevia is used in monotherapy, either simultaneously with metformin / sulfonylurea derivatives / PPAR-γ agonists, or with metformin and sulfonylurea derivatives / metformin and PPAR-γ agonists / insulin (without or with metformin).

The dosage regimen of drugs used simultaneously with Kselevia is selected based on the recommended doses for these drugs.

Against the background of combined treatment with Xelevia with insulin or sulfonylurea derivatives, it is advisable to reduce the traditionally recommended doses of insulin and sulfonylureas to reduce the likelihood of insulin-induced or sulfone-induced hypoglycemia.

If you miss a pill, it is recommended to take them as soon as possible after the patient remembers the missed dose. It should be borne in mind that the use of a double dose of the drug on the same day is unacceptable.

Correction of the dosage regimen in case of mild renal failure (CC ≥ 50 ml in 1 min, approximately corresponding to the concentration of serum creatinine ≤ 1.5 mg per 1 for women and ≤ 1.7 mg per 1 for men) is not required.

In patients with moderate to severe renal failure, dose adjustment of sitagliptin is required. Since there is no separation risk on Xelevia tablets and they are not produced in a dosage of 25 or 50 mg (but only in a dosage of 100 mg), it is not possible to provide the required dosage regimen in such patients. In this regard, the drug for this category of patients is not prescribed.

The use of sitagliptin against the background of renal failure requires an assessment of renal function before starting therapy and periodically during the period of its use.

With mild to moderate liver failure, as well as in elderly patients, the dose of the drug is not adjusted. The use of Xelevia against the background of severe hepatic failure has not been studied.

Side effects

In general, the use of sitagliptin is well tolerated both in monotherapy and in combination with other hypoglycemic agents. The overall incidence of adverse events in clinical trials, as well as the number of cases of drug withdrawal due to the development of side effects, are similar to those for placebo.

Four placebo-controlled studies of sitagliptin at a dose of 100-200 mg per day (monotherapy or in combination with pioglitazone / metformin) over a period of 18 to 24 weeks did not reveal adverse drug-related effects, the frequency of which would exceed 1% in a group of people receiving the drug. The safety profile of the 200 mg / day dose was comparable to that of the 100 mg / day dose.

Analysis of the data obtained in the course of these studies showed that the incidence of hypoglycemia, as well as side effects from the gastrointestinal tract (the exception is the more frequent development of nausea with a daily dose of 200 mg) when taking 100 mg of the drug / 200 mg of the drug / placebo are similar, namely:

• hypoglycemia: 1.2 / 0.9 / 0.9%;
• gastrointestinal tract: abdominal pain - 2.3 / 1.3 / 2.1%; diarrhea - 3 / 2.6 / 2.3%; vomiting - 0.8 / 0.7 / 0.9%; nausea - 1.4 / 2.9 / 0.6%.

Hypoglycemia in all studies was recorded based on all reports of its clinically expressed manifestations. No parallel blood glucose measurement was required.

Starting combination therapy with metformin

A 24-week, placebo-controlled factorial study was conducted on initial combination therapy with sitagliptin at a daily dose of 100 mg and metformin at a daily dose of 1000 or 2000 mg (50 mg sitagliptin + 500 or 1000 mg metformin twice a day). According to the data obtained, adverse events associated with taking the drug were observed more often (with a frequency of ≥ 1%) in the group receiving sitagliptin + metformin than in the group receiving metformin alone. The incidence of side effects in the sitagliptin + metformin and metformin monotherapy groups was (respectively):

• diarrhea - 3.5 and 3.3%;
• vomiting - 1.1 and 0.3%;
• headache - 1.3 and 1.1%;
• dyspepsia - 1.3 and 1.1%;
• hypoglycemia - 1.1 and 0.5%;
• flatulence - 1.3 and 0.5%.

Concomitant use with sulfonylurea derivatives or sulfonylurea derivatives and metformin

In a 24-week placebo-controlled study of the combined use of 100 mg sitagliptin per day with glimepiride or glimepiride and metformin in the group receiving the drug, there was a more frequent (with a frequency of ≥ 1%) development of hypoglycemia compared to the group receiving placebo with glimepiride or glimepiride and metformin. The frequency of its development was 9.5 / 0.9%, respectively.

Starting combination therapy with PPAR-γ agonists

In a 24-week study of starting combination treatment with sitagliptin at a daily dose of 100 mg and pioglitazone at a daily dose of 30 mg in the group receiving sitagliptin in combination, side effects were observed more often (with a frequency of ≥ 1%) than in the group receiving pioglitazone as monotherapy … The incidence of adverse events in the sitagliptin + pioglitazone and pioglitazone monotherapy groups was (respectively):

• symptomatic hypoglycemia: 0.4 and 0.8%;
• asymptomatic decrease in blood glucose concentration: 1.1 and 0%.

Combination therapy with metformin and PPAR-y agonists

A placebo-controlled study of the use of 100 mg sitagliptin per day simultaneously with rosiglitazone and metformin was conducted in two groups - patients receiving a combination with the investigational drug and those receiving a combination with a placebo. According to the obtained data, adverse reactions were observed more often (with a frequency of ≥ 1%) in the group receiving sitagliptin than in the group receiving placebo.

At 18 weeks of observation in these groups, side effects were noted with the following frequency:

• vomiting - 1.2 and 0%;
• headache - 2.4 and 0%;
• hypoglycemia - 1.2 and 0%;
• nausea - 1.2 and 1.1%;
• diarrhea - 1.8 and 1.1%.

At 54 weeks of observation, these groups showed the development of a greater number of side effects with the following frequency:

• peripheral edema - 1.2 and 0%;
• headache - 2.4 and 0%;
• nausea - 1.2 and 1.1%;
• fungal skin infection - 1.2 and 0%;
• cough - 1.2 and 0%;
• hypoglycemia - 2.4 and 0%;
• upper respiratory tract infections - 1.8 and 0%;
• vomiting - 1.2 and 0%.

Combination therapy with insulin

In a 24-week placebo-controlled study of the combined use of 100 mg sitagliptin per day and a constant dose of insulin (without or with metformin), side effects were observed more often (with a frequency of ≥ 1%) in the group receiving sitagliptin in combination with insulin (without or with metformin)) than in the group receiving placebo with insulin (without or with metformin). The incidence of adverse events was (respectively):

• headache - 1.2 / 0%;
• flu - 1.2 / 0.3%;
• hypoglycemia - 9.6 / 5.3%.

Another 24-week study in which sitagliptin was used as an adjunct to insulin therapy (with or with metformin) found no drug-related adverse reactions.

Pancreatitis

A pooled analysis of 19 double-blind, randomized clinical trials using sitagliptin at a daily dose of 100 mg or an appropriate control drug (active or placebo) showed that the incidence of unconfirmed acute pancreatitis was 0.1 cases per 100 patient-years of therapy in each group.

Clinically significant deviations of vital signs or electrocardiogram, including the duration of the QTc interval, were not observed when taking sitagliptin.

Study to evaluate the cardiovascular safety of sitagliptin (TECOS)

TECOS enrolled 7332 patients who received 100 mg sitagliptin per day (or 50 mg per day if the baseline estimated glomerular filtration rate was ≥ 30 and <50 ml per minute per 1.73 m ²), and 7339 patients, receiving placebo, in the general population of individuals who were prescribed therapy.

The drug or placebo was added to standard treatment in accordance with existing national standards for the selection of the target HbA _1C level and the control of cardiovascular risk factors. In total, 2004 patients aged 75 years and older were included in the observation, of whom 970 received sitagliptin, and 1034 - placebo. The overall incidence of serious side effects was similar in both groups. Evaluation of complications associated with diabetes mellitus, which were previously designated for monitoring, revealed a comparable incidence of adverse effects between groups when taking sitagliptin / placebo, including impaired renal function (1.4 / 1.5%) and infection (18, 4 / 17.7%). The profile of side effects in patients aged 75 years and older was generally similar to that for the general population.

The incidence of episodes of severe hypoglycemia in the population of patients who were prescribed therapy ("intention-to-treat") and who initially received sulfonylureas and / or insulin therapy when taking sitagliptin / placebo was 2.7 / 2.5%, respectively. At the same time, in patients who initially did not take sulfonylureas and / or insulin preparations, this frequency was 1 / 0.7%, respectively. During the examination, the incidence of confirmed cases of pancreatitis when taking the drug / placebo was 0.3 / 0.2%, and malignant neoplasms - 3.7 / 4%, respectively.

Post-registration observations

Post-marketing monitoring of sitagliptin use in monotherapy and / or in combination with other hypoglycemic drugs revealed additional side effects. Since these data were obtained voluntarily from a population of uncertain size, the frequency and causal relationship with the treatment of these phenomena cannot be established.

These include:

• angioneurotic edema;
• hypersensitivity reactions, including anaphylaxis;
• pruritus / rash, urticaria, pemphigoid, cutaneous vasculitis, exfoliative skin pathologies, including Stevens-Johnson syndrome;
• acute pancreatitis, including hemorrhagic and necrotic forms with / without lethal outcome;
• deterioration of kidney function, including acute renal failure (dialysis is required in some cases);
• upper respiratory tract infections;
• nasopharyngitis;
• vomiting, constipation;
• headache;
• arthralgia, myalgia;
• pain in the limbs, back.

Changes in laboratory parameters

In most clinical studies, there was a slight increase in the leukocyte count in patients receiving sitagliptin (100 mg per day) compared with the placebo group (an average of 200 μl; at the beginning of therapy, the indicator was 6600 μl), which is due to an increase in the number of neutrophils.

There was a slight increase in uric acid (0.2 mg per dl) with 100 and 200 mg sitagliptin per day compared with placebo. Before the start of therapy, the value of the indicator averaged 5–5.5 mg per 1 dl. No cases of gout have been reported.

There was also a slight decrease in the content of total alkaline phosphatase in the group receiving the drug, compared with the placebo group (by almost 5 IU per 1 L; on average, before the start of therapy, the concentration was from 56 to 62 IU per 1 L), which was associated with a small a decrease in the bone function of the enzyme.

These changes in laboratory parameters are not considered clinically significant.

Overdose

When conducting clinical trials of the drug on healthy volunteers, a single dose of sitagliptin of 800 mg was generally well tolerated. In one study, when taking this dose, a minimal change in the QTc interval was detected, which is not considered clinically significant. The use of more than 800 mg of the drug per day in humans has not been studied.

During phase I of clinical observations of repeated use of sitagliptin, there were no side effects associated with its intake (up to 400 mg per day for 4 weeks).

Therapy: with the development of an overdose, standard supportive measures are carried out - the removal of the unabsorbed drug from the gastrointestinal tract, monitoring of vital signs, including an ECG (electrocardiogram), and, if necessary, carrying out supportive treatment.

The drug is poorly dialyzed. Only 13.5% of its dose in clinical trials was removed by dialysis within 3-4 hours. If necessary, prolonged dialysis can be prescribed. There are no data on the effectiveness of peritoneal dialysis of the drug.

special instructions

Hypoglycemia

According to clinical observations, the incidence of hypoglycemia during monotherapy with sitagliptin or its simultaneous treatment with drugs that do not cause this pathological condition (pioglitazone, metformin) was similar to that in the placebo group. As with the use of other hypoglycemic drugs, hypoglycemia occurred when Xelevia was prescribed in combination with sulfonylurea derivatives or insulin. To reduce the likelihood of sulfone-induced hypoglycemia, the dosage of the sulfonylurea derivative is reduced.

Therapy in elderly patients

The safety and efficacy of using Xelevia in clinical trials in elderly patients (409 patients) over 65 years old were comparable to those in a group of volunteers under the age of 65 years. In this regard, it is not required to adjust the dosage regimen depending on the patient's age. It should be borne in mind that older patients are more likely to develop renal failure. Therefore, in the presence of severe renal failure in this age group, like in any other, the dosage of sitagliptin is adjusted.

TECOS

In the TECOS study, volunteers received sitagliptin at a daily dose of 100 mg (or 50 mg per day with a baseline value of the estimated glomerular filtration rate ≥ 30 and <50 ml per minute per 1.73 m ²) or placebo. They were added to standard treatment in accordance with existing national standards for determining target levels of HbA _1Cand control of cardiovascular risk factors. At the end of the median study period (3 years) in people with type 2 diabetes mellitus, taking a drug in addition to standard therapy did not increase the likelihood of hospitalization for heart failure (hazard ratio - 1; 95% confidence interval - 0.83 to 1.2; p = 0.98 for the difference in the frequency of risks) or the risk of serious side effects from the cardiovascular system (hazard ratio - 0.98; 95% confidence interval - 0.89 to 1.08; p < 0.001 to prove lack of superiority).

Influence on the ability to drive vehicles and complex mechanisms

Studies on the effect of Xelevia on the ability to drive vehicles and work with complex mechanisms, as well as engage in activities requiring a high speed of psychomotor reactions and increased attention, have not been conducted.

Application during pregnancy and lactation

Xelevia is not prescribed during pregnancy, since no controlled studies have been conducted to confirm the safety and effectiveness of its use in such cases. Like other oral hypoglycemic agents, the drug is not recommended for use during this period.

There are no data confirming the penetration of sitagliptin into breast milk. In this regard, the drug is not used during breastfeeding.

Pediatric use

For patients under 18 years of age, the drug is not prescribed.

With impaired renal function

In case of moderate and severe renal failure, Xelevia is contraindicated (this is due to the fact that the drug is not released in a dosage of 25 or 50 mg, and there is no separating risk on tablets with a dosage of 100 mg, and therefore it is not possible to provide the required dosage regimen in such patients) …

For violations of liver function

With mild to moderate hepatic impairment, the dose of the drug is not adjusted.

The use of Xelevia against the background of severe hepatic failure has not been studied.

Use in the elderly

Correction of the dosage regimen for elderly patients is not carried out.

Drug interactions

In ongoing studies on the interaction of sitagliptin with other drugs, it did not have clinically significant effects on the pharmacokinetics of oral contraceptives, warfarin, simvastatin, glibenclamide, rosiglitazone and metformin. Based on this, the drug does not inhibit isoenzymes such as CYP2C8, CYP2C9 and CYP3A4. According to in vitro data, it also does not inhibit the isoenzymes CYP1A2, CYP2B6, CYP2C19 and CYP2D6 and does not induce the isoenzyme CYP3A4.

With repeated combined use of metformin with sitagliptin, there were no significant changes in the pharmacokinetic parameters of the second in patients with type 2 diabetes mellitus.

The obtained data of the population pharmacokinetic analysis of patients with type 2 diabetes mellitus showed that concomitant treatment has no clinically significant effect on the pharmacokinetics of the drug. This study evaluated the drugs most commonly prescribed for type 2 diabetes, including the following:

• β-blockers;
• hypolipidemic agents (such as ezetimibe, fibrates, statins);
• antidepressants (such as sertraline, fluoxetine, bupropion);
• antiplatelet agents (eg clopidogrel);
• antihistamines (such as cetirizine);
• medicines for the treatment of erectile dysfunction (eg, sildenafil);
• non-steroidal anti-inflammatory drugs (such as celecoxib, diclofenac, naproxen);
• proton pump inhibitors (such as lansoprazole, omeprazole);
• antihypertensive drugs (such as hydrochlorothiazide, slow calcium channel blockers, angiotensin II receptor antagonists, angiotensin-converting enzyme inhibitors).

A slight increase in AUC and _{Cm ax of} digoxin (by 11 and 18%, respectively) was observed when it was combined with sitagliptin. This increase is not considered clinically significant. With joint therapy, changing the dose of drugs is not recommended.

Increased AUC and C _{m ax} sitagliptin (at 29 and 68%, respectively) noted when it is used at a dose of 100 mg is combined with a single dose of cyclosporin (a potent inhibitor of P-glycoprotein) in the oral dose of 600 mg. The observed changes in the pharmacokinetic characteristics of the drug are not considered clinically significant. When using in combination with cyclosporine or another inhibitor of P-glycoprotein (for example, ketoconazole), it is not recommended to change the dose of Xelevia.

According to the population pharmacokinetic analysis of patients and healthy volunteers (N = 858) for a wide range of concomitant drugs (N = 83, almost half of which are excreted through the kidneys), these substances do not have any clinically significant effects on sitagliptin pharmacokinetics.

Analogs

Analogs of Kselevia are Yasitara, Sitagliptin phosphate monohydrate, Januvia.

Terms and conditions of storage

Store in a place protected from light and moisture at temperatures up to 25 ° C. Keep out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Xelevia

Since the drug is rarely found in pharmacies, there are few reviews of Xelevia, confirming the safety and effectiveness of its use in type 2 diabetes.

Price for Xelevia in pharmacies

The approximate price for Xelevia (28 tablets per pack) is 1,476 rubles.

Xelevia: prices in online pharmacies

Drug name Price Pharmacy

Xelevia 100 mg film-coated tablets 28 pcs. 999 RUB Buy

Xelevia tablets p.p. 100mg 28 pcs. 1389 RUB Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!