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2019 Price of Januvia

$449.3330 tablets/100 mg
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Sitagliptin volume of distribution

NameDosageStrengthRouteLabeller
JanuviaTablet, film coated50 mg/1OralCardinal Health
RistabenTablet, film coated50 mgOralMerck Sharp & Dohme Limited
TesavelTablet, film coated100 mgOralMerck Sharp & Dohme Limited
XeleviaTablet, film coated25 mgOralMerck Sharp & Dohme Limited
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2018 Statistics

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Clients Benefit 29%

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Total savings $4,735,080

What is Sitagliptin

Sitagliptin is a new oral hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. This enzyme-inhibiting drug is to be used either alone or in combination with metformin or a thiazolidinedione for control of type 2 diabetes mellitus. The drug works to competitively inhibit a protein/enzyme, dipeptidyl peptidase 4 (DPP-4), that results in an increased amount of active incretins (GLP-1 and GIP), reduced amount of release of glucagon (diminishes its release) and increased release of insulin.

Sitagliptin mechanism of action

Sitagliptin is a highly selective DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes by slowing the inactivation of incretin hormones, thereby increasing the concentration and prolonging the action of these hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. These changes lead to a decrease in hemoglobin A1c (HbA1c)levels, as well as a lower fasting and postprandial glucose concentration. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses.

Dosage forms of Sitagliptin

DrugDosageQuantityPrice
Januvia25mg84 Tablet$114.75
Januvia50mg84 Tablet$75.10
Januvia100mg84 Tablet$234.00
Janumet50/500mg90 Tablet$126.00
Janumet50/850mg56 Tablet$133.00
Janumet50/1000mg90 Tablet$130.00
Janumet XR50/1000mg56 Extended Release Tablet$180.00
Janumet XR100/1000mg28 Extended Release Tablet$239.00

Prescription Generics

Januvia

International Brands

Janumet

Synonyms

Januvia, Ristaben, Tesavel, Xelevia

Manufacturers

AS Medication Solutions, Cardinal Health, Lake Erie Medical&Surgical Supply, Merck Ltd, Merck Sharp & Dohme Limited, Physicians Total Care, Remedy Repack

CAS number

486460-32-6

UNII

QFP0P1DV7Z

State

solid

Affected organisms

Humans and other mammals

Indication of Sitagliptin

For use as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus. Also for use in patients with type 2 diabetes mellitus to improve glycemic control in combination with metformin or a PPAR. agonist (e.g., thiazolidinediones) when the single agent alone, with diet and exercise, does not provide adequate glycemic control.

Toxicity of Sitagliptin

The toxicity potential of sitagliptin was evaluated in a series of repeated dose toxicity studies of up to 53 weeks in dogs and up to 27 weeks in rats. In dogs administered sitagliptin orally at dosages of 2, 10 and 50 mg/kg/day, the no-observed effect level was 10 mg/kg/day (up to 6 times the human exposure based on the recommended daily adult human dose of 100 mg/day). Treatment-related physical signs observed in the 50-mg/kg/day group included open-mouth breathing, salivation, white foamy emesis, ataxia, trembling, decreased activity, and/or hunched posture. These signs were transient, slight in degree, and occurred with decreased incidence during the course of the study. In addition, very slight to slight skeletal muscle degeneration was observed histologically in the 14- and 27-week toxicity studies at the 50-mg/kg/day dose.

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What is Januvia?

Synthetic hypoglycemic drug belongs to the group of incretinomimetic, inhibiting DPP-4. Regular use of Januvia increases the production of incretins, stimulates their activity. Endogenous insulin production increases, glucagon synthesis in the liver is suppressed.

Oral inhibition inhibits the breakdown of glucagon-like GLP-1 peptide, which plays a fantastic role in the implementation of glucose-dependent insulin, and restores its physiological concentrations. Such a set of measures contributes to the normalization of glycemia.

Sitagliptin helps to reduce the performance of glycated hemoglobin, lean glucose, body weight. From the gastrointestinal tract the medicament is absorbed into the bloodstream within 1-4 hours. The intake time and caloric content of food does not affect the pharmacokinetics of the inhibitor.

The drug is suitable for admission at any convenient time: before, after and during meals. Up to 80% of the active component removes the kidneys. The drug can be used both in monotherapy and in complex treatment of type 2 diabetes, especially with increased frequency of hypoglycemic attacks.

What is a Janumet?

Janumet contains a combination of metformin and sitagliptin. Metformin and sitagliptin are drugs for the treatment of diabetes that help control blood sugar levels. Metformin works by reducing the production of glucose (sugar) in the liver and reducing the absorption of glucose in the intestine. Sitagliptin works by regulating the levels of insulin that your body produces after a meal.

Janumet is used along with diet and exercise to improve blood sugar control in adults with type 2 diabetes. Janumet is not intended to treat type 1 diabetes. You should not use Janumet if you have severe kidney disease or diabetic ketoacidosis (see your doctor for insulin).

Janumet can cause a serious condition called lactic acidosis. Get emergency medical care if you have even mild symptoms, such as muscle pain or weakness, numbness or coldness in your arms and legs, trouble breathing, stomach pain, nausea with vomiting, slow or irregular heart rate , dizziness or feeling very weak Or tired.