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Januvia 100mg MSD

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Januvia 100mg (Sitagliptin) is an oral hypoglycemic  medicine which belongs to the group of medicines called selective inhibitors of dipeptidyl peptidase-4.

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Generic name: Sitagliptin

Januvia 100mg (Sitagliptin) is an oral hypoglycemic medicine which belongs to the group of medicines called selective inhibitors of dipeptidyl peptidase-4.

Januvia increases the concentration of glucagon-like peptide-1 and glucose-dependent insulinotropic peptide in blood plasma. Thus, increases insulin secretion, reduces glucagon secretion and glycosylated hemoglobin levels in patients with diabetes mellitus type II. The level of glycemia is decreased as well.

Is used to treat non-insulin dependent diabetes mellitus (II type).

Pharmacological properties

Januvia 100mg (Sitagliptin) is an oral hypoglycemic medicine, a selective inhibitor of dipeptidyl peptidase-4. It works by increasing the concentration of glucagon-like peptide-1 and glucose-dependent insulinotropic peptide in blood plasma. It helps increase insulin secretion, causes reduction of glucagon secretion, glycosylated hemoglobin levels and blood glucose levels in patients with diabetes mellitus type II. Januvia is a highly selective inhibitor of dipeptidyl peptidase-4 (DPP-4).

Sitagliptin is different in structure and action mechanism from insulin, sulfonylureas and biguanide derivatives, analogues of glucagon-like peptide-1 agonists, PPAR-gamma (gamma receptor, peroxisome proliferator-activated) inhibitors of alpha-glycosidase, amylin analogues.

Inhibition of dipeptidyl peptidase-4 leads to increased concentrations of two known incretins: glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). These incretins are secreted into the intestine and their concentration is increased in response to food intake. They are part of the internal physiological regulation of glucose homeostasis. At normal or elevated blood glucose levels these incretins contribute to increase of insulin synthesis and secretion of its beta-cells of the pancreas by cAMP-associated signaling intracellular mechanisms.

Glucagon-like peptide-1 also contributes to the suppression of increased glucagon secretion by alpha-cells in the pancreas. Reducing the concentration of glucagon, accompanied by increased levels of insulin helps reduce hepatic glucose production, resulting in a decrease of glycemia levels.

At low concentrations of glucose in the blood the acti listed above effects of incretins on the release of insulin and glucagon secretion are not observed.

Glucagon-like peptide-1 and glucose-dependent insulinotropic peptide do not affect the release of glucagon in response to hypoglycemia. Under physiological conditions, the activity of incretins is limited to dipeptidyl peptidase-4, which rapidly hydrolyzes incretins in inactive products.

Januvia prevents hydrolysis of the active forms of incretin GPP-1 and GIP by the enzyme dipeptidyl peptidase-4, increasing their plasma concentrations, increases insulin release and glucose-dependent secretion of glucagon.

In patients with type II diabetes with hyperglycemia, these changes in insulin secretion and glucagon levels lead to lower glycated hemoglobin (NbA1s) and a decrease in plasma glucose concentration.

In patients with diabetes mellitus type II, after receiving a standard therapeutic dose of Januvia, the inhibition of dipeptidyl peptidase-4 is observed for 24 hours.

Clinical indications

Januvia (Sitagliptin) is used to treat type II diabetes (insulin-dependent diabetes):

Monotherapy: in combination with diet and exercise to improve glycemic control;

Combination therapy: to improve glycemic control in combination with metformin or a PPAR-gamma agonists (eg, pioglitazone or rosiglitazone) when diet and exercise in combination with monotherapy do not provide the desired results.

Mode of administration

Januvia tablets containing Sitagliptin 100ng are taken orally independently on food intake. The dose of the medication is indicated individually by a health care provider and is based on severity of the disease, patients age, other medical conditions treated. Usually the standard recommended dosage of Januvia is 100m once daily as monotherapy or in combination with other anti-diabetic medicines.


  • Hypersensitivity to Sitagliptin or other ingredients of the medication
  • Diabetes mellitus type I (insulin-dependent);
  • Diabetic ketoacidosis;
  • Pregnancy and breastfeeding;
  • Children and teenagers under 18 years

Januvia 100mg (Sitagliptin) should be used with caution in:

Renal failure (in patients with moderate to severe renal impairment the dose adjustment is required).

Pregnancy and lactation

Application of Januvia during pregnancy is contraindicated. Controlled studies of Januvia in pregnant women have not been carried out.

It is not known whether sitagliptin passes through the breast milk . Try to avoid breastfeeding while taking Januvia 100mg.

Side effects

Januvia is generally well tolerated.

In clinical studies, the overall incidence of side effects, as well as the frequency of Januvia withdrawal because of side effects were similar to those on placebo.

CNS: headache, dizziness, drowsiness,

Gastrointestinal tract: diarrhea, abdominal pain, nausea, vomiting.

Respiratory system: respiratory tract infections, nasopharyngitis.

Endocrine system: hypoglycemia.

Musculoskeletal system: arthralgia

Laboratory parameters: increase of uric acid concentration, the overall decrease in the concentration of alkaline phosphatase, an increase of leukocytes blood levels. These changes are not considered clinically significant.


The incidence of hypoglycemia in the application of Januvia as monotherapy or in combination with metformin or pioglitazone/rosiglitazone was similar to the frequency of hypoglycemia with placebo.

In mild hepatic insufficiency (creatinine clearance 50 ml / min) the dose adjustment is required

In patients with severe renal insufficiency dosage adjustment is necessary as well.

Januvia interactions

Sitagliptin does not inhibit CYP3A4, probably, CYP2S8, CYP2C9, CYP2D6, CYP1A2, CYP2C19, CYP2V6 and does not induce CYP3A4.

Sitagliptin had no clinically significant effect on the pharmacokinetics of metformin, rosiglitazone, glyburide, simvastatin, warfarin, oral contraceptives.

It was noted a slight increase in AUC (11%) and C max (18%) of digoxin This increase is not considered to be clinically significant. Januvia should be stored at dry and protected from light place at a room temperature out of reach of children.

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