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

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

Januvia

Januvia: 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. Instructions for use of Januvia: method 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 of Januvia
19. 19. Price for Januvia in pharmacies

Latin name: Januvia

ATX code: A10BH01

Active ingredient: sitagliptin (sitagliptin)

Producer: Merck Sharp & Dohme BV (Netherlands), Merck Sharp & Dohme SpA (Italy), Akrihin, JSC (Russia)

Description and photo update: 2018-24-10

Januvia is a hypoglycemic drug; dipeptidyl peptidase-4 inhibitor.

Release form and composition

Dosage form Januvia - film-coated tablets: biconvex, round; at a dosage of 25 mg - light pink with a slight beige tint and engraving "221"; at a dosage of 50 mg - light beige, engraved with "112"; in a dosage of 100 mg - beige, engraved with "277" (14 pcs. in blisters, in a cardboard box 1, 2, 4, 6 or 7 blisters).

Composition for 1 tablet:

• active substance: sitagliptin phosphate hydrate - 32.13 / 64.25 / 128.5 mg (which is equivalent to sitagliptin content - 25/50/100 mg);
• auxiliary components: microcrystalline cellulose, unmilled calcium hydrogen phosphate, croscarmellose sodium, magnesium stearate, sodium stearyl fumarate;
• film coating: at a dosage of 25 mg - Opadray II Pink 85 F 97191; at a dosage of 50 mg - Opadray II Light beige 85 F 17498; at a dosage of 100 mg - Opadray II Beige 85 F 17438 (polyvinyl alcohol, titanium dioxide, polyethylene glycol 3350, talc, iron oxide yellow, iron oxide red).

Pharmacological properties

Pharmacodynamics

Januvia's active ingredient, sitagliptin, is a highly selective inhibitor of the DPP-4 (dipeptidylpeptidase-4) enzyme, intended for the treatment of type 2 diabetes mellitus. In terms of chemical structure, as well as pharmacological action, sitagliptin differs from analogues of GLP-1 (glucagon-like peptide-1), sulfonylurea derivatives, insulin, biguanides, γ-receptor agonists (activated by a peroxisome proliferator - PPAR-γ), α-glycosidase inhibitors, analogs amylin. Sitagliptin, inhibiting DPP-4, thereby increases the concentration of GLP-1 and GIP (glucose-dependent insulinotropic peptide), two known hormones belonging to the incretin family, which are secreted in the intestine for 24 hours, and the level of which increases in response to food intake. Incretins are part of the internal physiological biosystem of glucose homeostasis regulation,they promote the synthesis of insulin and its secretion by β-cells of the pancreas due to signaling intracellular mechanisms associated with cyclic AMP (adenosine monophosphate) at normal or increased blood glucose levels.

GLP-1 inhibits the increased secretion of glucagon by α-cells of the pancreas. A decrease in glucagon levels against the background of an increase in insulin concentration helps to inhibit the production of glucose by the liver, which as a result leads to a decrease in glycemia.

In the case of low blood glucose, the influence of incretins on insulin synthesis and glucagon secretion is not observed; they do not affect the release of glucagon in response to hypoglycemia. Under natural conditions, the DPP-4 enzyme limits the activity of incretins, rapidly subjecting them to hydrolysis and decomposition into inactive components.

Sitagliptin, inhibiting the effectiveness of DPP-4, thus prevents the hydrolysis of incretins, increasing the growth of plasma concentrations of the active forms of GLP-1 and GIP, which increases the glucose-dependent release of insulin and helps to reduce the secretion of glucagon. In type 2 diabetes mellitus with hyperglycemia, such a correction of insulin and glucagon secretion leads to a decrease in the concentration of HbA1c (glycosylated hemoglobin) and a decrease in glucose levels, determined both on an empty stomach and after an exercise test.

Taking one dose of Januvia in type 2 diabetes mellitus leads to inhibition of the DPP-4 enzyme for 24 hours, as a result of which the level of circulating incretins GLP-1 and GIP increases 2-3 times, the plasma concentration of insulin and C-peptide increases, and decreases plasma glucagon concentration, fasting blood glucose levels decrease and after food load or glucose load.

Pharmacokinetics

The kinetic patterns of chemical and biological processes occurring with sitagliptin in the body of healthy individuals and patients with type 2 diabetes mellitus have been comprehensively studied. Characteristics for healthy volunteers after oral administration of 100 mg sitagliptin: absorption - fast, TC _max value (time to reach maximum concentration) - 1-4 hours from the moment of administration; AUC (area under the concentration-time curve) - 8.52 μmol / hour, this indicator is proportional to the dose taken; C _max - 950 nmol / l; T _1/2 (mean half-life) - 12.4 hours. AUC of sitagliptin after the next dose of 100 mg of the drug, upon reaching an equilibrium state after taking the first dose, increased by ~ 14%. Intra- and intersubjective variability of the substance AUC is negligible.

Pharmacokinetic characteristics of Januvia:

• absorption: the absolute bioavailability of sitagliptin is ~ 87%; joint administration of the drug with fatty foods does not affect its pharmacokinetics;
• distribution: after a single dose of the drug at a dose of 100 mg, the average volume of distribution of sitagliptin in the equilibrium state in healthy subjects was ~ 198 L. Plasma protein-binding fraction is relatively low (~ 38%);
• metabolism: up to 79% of sitagliptin is eliminated by the kidneys unchanged, only a small part of the substance entering the body is metabolized; after oral administration of ¹⁴ C-labeled sitagliptin, ~ 16% of the radioactive preparation was excreted in the form of metabolites; 6 sitagliptin metabolites were found in trace amounts, most likely not having DPP-4-inhibitory effect;
• Excretion: after oral administration of ¹⁴ C-labeled sitagliptin to healthy subjects, up to 100% of the drug was excreted within one week from the moment of administration as follows: through the intestines - 13%, kidneys - 87%. T _1/2 when taken orally at a dose of 100 mg ~ 12.4 h, renal clearance ~ 350 ml / min.

Indications for use

• monotherapy: patients on a special diet and exercise are prescribed as a drug that improves glycemic control in type 2 diabetes;
• combination therapy: in combination with metformin or PPARγ receptor agonists (thiazolidinediones) is prescribed to patients with type 2 diabetes mellitus to improve glycemic control in case of ineffective diet and exercise in combination with monotherapy.

Contraindications

Absolute:

• type 1 diabetes mellitus;
• diabetic ketoacidosis;
• the period of pregnancy and lactation (lactation);
• children and adolescents up to 18 years old;
• hypersensitivity to any component of the drug.

Relative contraindications: Januvia should be taken with caution in renal failure. Patients with moderate to severe renal failure and end-stage renal disease requiring hemodialysis require dose adjustment of sitagliptin.

Instructions for use of Januvia: method and dosage

Januvia tablets are taken orally, regardless of the meal.

The recommended dosage for monotherapy, as well as in combination with metformin or a PPARγ agonist (thiazolidinediones) is 100 mg once a day.

If the patient has forgotten to take another pill, it should be taken as soon as possible, immediately after he remembers to miss the appointment, but not allowing a double dose.

Side effects

Januvia as monotherapy and in combination with other hypoglycemic drugs is generally well tolerated. The overall incidence of adverse adverse reactions, as well as the incidence of discontinuation of sitagliptin due to undesirable effects, according to clinical studies, were similar to those recorded after taking placebo.

Side effects without an identified connection with sitagliptin intake at a daily dose of 100 and 200 mg, but occurring more often than in patients receiving placebo (≥ 3% of cases): upper respiratory tract infection, nasopharyngitis, headache, diarrhea, arthralgia.

Other side reactions of Januvia:

• Gastrointestinal tract (gastrointestinal tract): abdominal pain, nausea, vomiting, diarrhea;
• laboratory data (not considered clinically significant): a slight increase in uric acid (cases of gout development were not recorded); a slight decrease in the concentration of total alkaline phosphatase, in part due to a small decrease in the bone fraction of alkaline phosphatase; a weak increase in the content of leukocytes due to an increase in the number of neutrophils (the phenomenon was noted in most studies, but not in all cases);
• cardiovascular system: there were no clinically significant changes in vital signs and electrocardiogram (ECG), including the QTc interval.

Overdose

Clinical studies in healthy volunteers have shown that sitagliptin at a single dose of 800 mg is generally well tolerated. In a single case, there was a minimal clinically insignificant change in the QTc interval. The intake of daily doses over 800 mg in humans has not been studied.

In case of an overdose, it is recommended to carry out standard supportive measures: removing unabsorbed drug residues from the gastrointestinal tract, constant monitoring of vital signs, including ECG, as well as prescribing symptomatic treatment if necessary.

The drug is poorly dialyzed (for a 3-4 hour hemodialysis session, according to clinical observations, only 13.5% of the dose is excreted from the body). With proven clinical necessity, prolonged dialysis may be prescribed. There are currently no data on the effectiveness of excretion of sitagliptin during peritoneal dialysis.

special instructions

According to clinical studies, after taking Januvia as a monotherapy drug or as part of a complex treatment with metformin / pioglitazone, hypoglycemia developed in patients with a frequency similar to that when using placebo.

The joint use of the drug in combination with drugs that can cause hypoglycemia, for example, insulin or sulfonylurea derivatives, has not been studied.

Influence on the ability to drive vehicles and complex mechanisms

Studies to study the effect of Januvia on the speed of psychomotor reactions and the ability to concentrate have not been conducted, however, a negative effect of the drug on these indicators is not expected.

Application during pregnancy and lactation

Due to the lack of data from controlled studies on the safety and efficacy of the drug in pregnant women, Januvia, like other hypoglycemic agents for oral administration, is not recommended for use during pregnancy.

There are no data on the release of sitagliptin during lactation, so the drug is not prescribed during breastfeeding.

Pediatric use

According to the instructions, Januvia is not used in pediatric practice.

With impaired renal function

Patients with renal insufficiency need a dose adjustment of Januvia, for which it is recommended to assess renal function before starting the course and then periodically repeat it during therapy.

Dosage adjustment depending on the degree of renal failure and creatinine clearance (CC):

• mild renal failure, CC> 50 ml / min (serum creatinine concentration: in men - less than 1.7 mg / dL; in women - less than 1.5 mg / dL): dose adjustment is not required;
• moderate renal failure, CC from 30 to 50 ml / min (serum creatinine concentration: in men - 1.7-3 mg / dl; in women - 1.5-2.5 mg / dl): daily dose - 50 mg per dose;
• severe renal failure, CC <30 ml / min (serum creatinine concentration: in men - more than 3 mg / dL; in women - more than 2.5 mg / dL); terminal stage of chronic renal failure with the need for hemodialysis or peritoneal dialysis: daily dose - 25 mg per dose; the tablets can be taken regardless of the dialysis schedule.

For violations of liver function

Patients with mild to moderate liver dysfunction do not need dose adjustment for Januvia. In severe hepatic impairment, the effect of the drug has not been studied.

Use in the elderly

The age of patients does not have a clinically significant effect on the pharmacokinetics of sitagliptin, the concentration of the substance in elderly people aged 65–80 is ~ 19% higher than in young patients. Such changes do not require correction of the Januvia dosage regimen.

Drug interactions

• metformin, rosiglitazone, glibenclamide, simvastatin, warfarin, oral contraceptives: sitagliptin has no clinically significant effect on their pharmacokinetics;
• digoxin: sitagliptin increases its AUC by 11%, and the average C _max - by 18%; such an increase is not considered clinically significant, no change in doses of digoxin and Januvia is required;
• cyclosporine - a potent inhibitor of P-glycoprotein (when taken orally in a dose of 600 mg simultaneously with oral administration of Januvia in a single dose of 100 mg): there was an increase in AUC and C _{max of} Januvia, respectively, by 29% and 68%; such an increase is not considered clinically significant; changes in the doses of Januvia and cyclosporine, like other inhibitors of P-glycoprotein (for example, ketoconazole), do not require.

When conducting a population pharmacokinetic analysis with the participation of sick and healthy volunteers on the use of a wide range of concomitant drugs, about half of which are eliminated by the kidneys, no clinically significant reactions of these drugs to sitagliptin pharmacokinetics were detected.

Analogs

The analogues of Januvia are: Galvus, Nesin, Komboglyza XR, Ongliza, Trajenta, etc.

Terms and conditions of storage

Store at 30 ° C. Keep out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Januvia

Used, as a rule, in newly diagnosed diabetes mellitus, Januvia, according to reviews, is effective for the treatment of patients with non-insulin dependent diabetes, both in monotherapy and in combination.

In the reviews of Januvia, among its shortcomings, it is mainly indicated the high cost of the drug.

Price for Januvia in pharmacies

The estimated price for Januvia (tablets in a dosage of 100 mg, 28 pcs in a package) is 1,450 rubles.

Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, 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!