The information on this site is intended for healthcare professionals in the United States and is not intended for the general public.

i am a healthcare professional i am not a healthcare professional
Head-to-Head vs Sulfonylurea

JANUVIA targets 2 core defects of diabetes in a glucose-dependent manner

JANUVIA + metformin targets 3 core defects of diabetes

Januvia® (sitagliptin) tablets: mechanism of action

Metformin: Increases insulin sensitivity
  • Metformin increases glucose uptake and
  •    utilization (greater in the liver than in muscle
  •    and fat)1,2

JANUVIA: Increases insulin synthesis
and release
  • JANUVIA works in a glucose-dependent manner
  •    to enhance active incretin levels, which stimulate
  •    the synthesis and release of insulin from beta
  •    cells
Metformin and JANUVIA: Decrease hepatic glucose overproduction
  • Metformin reduces glucose production in the liver (gluconeogenesis) and diminishes the
  •    breakdown of glycogen into glucose (glycogenolysis)2,3
  • JANUVIA improves the ability of alpha cells to suppress glucagon secretion (by
  •    enhancing active incretin levels), which results in reduced glycogen breakdown and glucose synthesis
  • JANUVIA increases insulin synthesis and release from pancreatic beta cells, which
  •    helps reduce hepatic glucose overproduction

Glucose-dependent mechanism: targets insufficient insulin release and hepatic glucose overproduction

dpp-4 inhibition
incretin pathway
View a printable mechanism of action card

[PDF: 324 KB, 2 pages]

Selected Important Risk Information
When JANUVIA was used in combination with a sulfonylurea or insulin, medications known to cause hypoglycemia, the incidence of hypoglycemia was increased over that of placebo. Therefore, a lower dose of sulfonylurea or insulin may be required to reduce the risk of hypoglycemia.

The incidence (and rate) of hypoglycemia based on all reports of symptomatic hypoglycemia were: 12.2% (0.59 episodes/patient–year) for JANUVIA 100 mg in combination with glimepiride (with or without metformin), 1.8% (0.24 episodes/patient–year) for placebo in combination with glimepiride (with or without metformin), 15.5% (1.06 episodes/patient-year) for JANUVIA 100 mg in combination with insulin (with or without metformin), and 7.8% (0.51 episodes/patient-year) for placebo in combination with insulin (with or without metformin).

View Additional Selected Important Risk Information

Important Information

JANUVIA® (sitagliptin) tablets is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

JANUVIA should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.

JANUVIA has not been studied in patients with a history of pancreatitis. It is unknown whether patients with a history of pancreatitis are at increased risk of developing pancreatitis while taking JANUVIA.

Before prescribing JANUVIA® (sitagliptin) tablets, please read the Prescribing Information. The Medication Guide also is available.

References: 1. Bailey CJ, Turner RC. Metformin. N Engl J Med. 1996;334(9):574–579. 2. Kirpichnikov D, McFarlane SI, Sowers JR. Metformin: an update. Ann Intern Med. 2002;137(1):25–33. 3. Krentz AJ, Bailey CJ. Oral antidiabetic agents: current role in type 2 diabetes mellitus. Drugs. 2005;65(3):385–411.

This site is intended for health care professionals of the United States, its territories, and Puerto Rico.

Copyright © 2013 Merck Sharp & Dohme Corp., a subsidiary of  Merck & Co., Inc. All rights reserved.

DIAB-1050515-0002 12/12