sitagliptin phosphate

sitagliptin phosphate


Pharmacologic class: Dipeptidyl peptidase 4 (DPP-4) inhibitor

Therapeutic class: Hypoglycemic

Pregnancy risk category B


Inhibits DPP-4 and slows inactivation of incretin hormones, helping to regulate glucose homeostasis through increased insulin release and decreased glucagon levels


Tablets: 25 mg, 50 mg, 100 mg

Indications and dosages

Adjunct to diet and exercise to improve glycemic control in type 2 diabetes mellitus

Adults: 100 mg P.O. once daily

Dosage adjustment

• Moderate to severe renal insufficiency or end-stage renal disease


• History of serious hypersensitivity to drug (such as anaphylaxis or angioedema)


Use cautiously in:

• concurrent administration of drugs that cause hypoglycemia (such as sulfonylureas or insulin)

• renal impairment, history of pancreatitis

• pregnant or breastfeeding patients

• children younger than age 18 (safety and efficacy not established).


• Assess renal function before starting therapy.

Before starting drug, ask patient about possible risk factors for pancreatitis, such as history of pancreatitis, alcoholism, gallstones, or hypertriglyceridemia. However, it's unknown if these conditions make it more likely that pancreatitis will occur.

• Give with or without food.

• Be aware that drug shouldn't be used to treat type 1 diabetes mellitus or diabetic ketoacidosis.

• Know that when drug is used with a sulfonylurea, a lower dose of sulfonylurea may be required, to reduce risk of hypoglycemia.

Adverse reactions

CNS: headache

EENT: nasopharyngitis

GI: abdominal pain, nausea, vomiting, diarrhea, pancreatitis

GU: acute renal failure

Respiratory: upper respiratory tract infection

Other: hypersensitivity reactions (including anaphylaxis, angioedema, exfoliative skin conditions such as Stevens-Johnson syndrome)


Drug-drug. Digoxin: minimally increased digoxin effect and blood level

Insulin, sulfonylureas: possible increased hypoglycemia risk

Patient monitoring

• Monitor renal function periodically.

• Measure patient's weight and body mass index periodically during therapy.

• Monitor blood glucose and hemoglobin A1c levels periodically during therapy.

Monitor patient for signs and symptoms of hypersensitivity reactions and immediately stop drug and institute emergency measures if such reactions occur.

• Check for diabetes signs and symptoms and disease progression routinely during therapy.

Be aware of postmarketing reports of acute pancreatitis, including fatal and nonfatal hemorrhagic or necrotizing pancreatitis. If pancreatitis is suspected, promptly discontinue drug.

Patient teaching

• Instruct patient to take drug with or without food.

• Teach patient about signs and symptoms of hypoglycemia (such as blurred vision, confusion, tremor, sweating, excessive hunger, drowsiness, and fast heart rate).

Teach patient about signs and symptoms of hypersensitivity reactions (such as rash, throat swelling, or difficulty breathing) and to immediately contact prescriber if these occur.

Instruct patient to immediately discontinue drug and report if signs and symptoms of pancreatitis occur (persistent severe abdominal pain, sometimes radiating to the back, which may or may not be accompanied by vomiting).

• Instruct patient to routinely monitor blood glucose levels at home.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs mentioned above.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved
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References in periodicals archive ?
Peruru, Stability-indicating rp-hplc method for simultaneous determination of metformin hydrochloride and sitagliptin phosphate in dosage forms, Chromatographia, 76, 1153 (2013).
DM + anemia (n = 16) Demographic Age (years) 72 (64-78) Female (%) 9 (56.3) Female age (years) (range) 69 (38-82) Male age (years) (range) 73 (54-82) Duration (years) 10 (6-14) Biochemistry HbA1C (%) 6.6 (5.9-7.2) WBC (103/[micro]L) 7.81 [+ or -] 2.52 RBC (106/[micro]L) 4.3 (3.8-4.7) HGB (g/dL) 10.9 (10.4-12.2) Ferritin (ng/mL) 39.2 (11.2-96.1) Glucose (mg/dL) 131.9 (105-153) Fe ([micro]g/dL) 49.1 (33.5-60.9) Transferrin (g/L) 2.7 (2.3-3.5) Transferrin-sat (%) 11.6 (8.4-15.8) CRP (median) (mg/L) 1.9 (1.1-8.7) Medications (%) Insulin 4 (25) Glyburide 3 (18.8) Metformin 7 (43.8) Sitagliptin phosphate 1 (6.3) Aspirin 7 (43.8) NSAIDs 1 (6.3) PPI 15 (93.8) Iron 8 (50) Comorbidities (%) Hypertension 14 (87.5) CVD 3 (18.8) H.
has submitted an application for marketing approval for a combination drug consisting of its Januvia (sitagliptin phosphate hydrate) and Astellas Pharma Inc's (TYO: 4503) Suglat (ipragliflozin L-Proline) for the treatment of type-2 diabetes in Japan, the two Japanese drug makers announced on Friday.
These agents include the [alpha]-glucosidase inhibitors acarbose and miglitol, the amylin analog pramlintide, the dipeptidyl peptidase-4 inhibitor sitagliptin phosphate, the glinides nateglinide and repaglinide, the glucagon-like peptide-1 derivative exenatide, and rapid-acting, bipbasic, and inhaled insulins.
These agents in clude the [alpha]-glucosidase inhibitors acarbose and miglitol, the amylin analog pramlintide, the dipeptidyl peptidase-4 inhibitor sitagliptin phosphate, the glinides nateglinide and repaglinide, the glucagon-like peptide-1 derivative exenatide, and rapid-acting, biphasic, and inhaled insulins.
The drug, sitagliptin phosphate (Januvia), has a unique mechanism of action: it increases a hormone that triggers the pancreas to produce more insulin to turn blood sugar (glucose) into energy, at the same time blocking an enzyme that causes the liver to stop producing glucose.
Food and Drug Administration announced October 17 that it had approved sitagliptin phosphate (Januvia), for the treatment of type 2 diabetes.
Januvia (sitagliptin phosphate), a prescription medicine for lowering blood sugar in patients over the age of 18 years who have type 2 diabetes, has been approved by the Food and Drug Administration.
Sitagliptin phosphate, an agent in the new class known as dipeptidyl peptidase-4 inhibitors, has been approved by the Food and Drug Administration for use as monotherapy or in combination with metformin or a thiazolidinedione.
The newly licensed glucose-lowering agent sitagliptin phosphate appears safe and somewhat effective, but how and where it will fit into the armamentarium of treatment for type 2 diabetes is not yet clear.