Contents

Search

sitagliptin (Januvia)

Indications: - diabetes mellitus type 2 a) monotherapy [3] b) has been used effectively in combination with: - metformin, glyburide, pioglitazone [1,2,3] * sitagliptin treatment at the time of hospitalization is associated with reduced mortality in patients with diabetes mellitus type-2 & COVID-19 [15] Dosage: 100 mg PO QD Pharmacokinetics: renally cleared Dosage adjustment in renal failure: creatinine clearance dosage > 50 mL/min 100 mg QD 30-50 mL/min 50 mg QD < 30 mL/min 25 mg QD Adverse effects: 1) not likely to cause weight gain 2) acute pancreatitis [5] - does not increase risk of acute pancreatitis [7] - small increase in acute pancreatitis not statistically significant [13] 3) as safe as other oral hypoglycemic agents [8] - not likely to cause hypoglycemia [14] 4) increased risk for heart failure hospitalization among patients with preexisting heart failure [9] - not associated with increased risk for hospitalization due to heart failure relative to other diabetes medications [12] 5) noninferior to usual care for cardiovascular outcomes - no increase in hospitalization for heart failure [10] 6) noninferior to placebo for cardiovascular death, MI, stroke, or hospitalization for unstable angina [11]* * editor notes that showing a drug is non-inferior to placebo does not support its use Drug interactions: - none reported Mechanism of action: 1) dipeptidyl peptidase-4 inhibitor 2) inhibits incretin catabolism 3) enhances incretin system 4) lowers A1c about 0.3% to 0.8% 5) effects mostly post-prandial glucose

Interactions

drug interactions drug adverse effects (more general classes)

General

gliptin; dipeptidyl peptidase-4 inhibitor; DPP-4 inhibitor

Properties

Database Correlations

PUBCHEM cid=208902

References

  1. Prescriber's Letter 12(9): 2005 Investigational Medicines for Diabetes: Sitagliptan (Januvia) and Vildagliptan (Galvus) Detail-Document#: 220715 (subscription needed) http://www.prescribersletter.com
  2. Prescriber's Letter 13(11): 2006 New Drug: Sitagliptin (Januvia) Detail-Document#: 221102 (subscription needed) http://www.prescribersletter.com
  3. Aschner P, Kipnes MS, Lunceford JK, Sanchez M, Mickel C, Williams-Herman DE; Sitagliptin Study 021 Group. Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care. 2006 Dec;29(12):2632-7. PMID: 17130196 - Charbonnel B, Karasik A, Liu J, Wu M, Meininger G; Sitagliptin Study 020 Group. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes inadequately controlled with metformin alone. Diabetes Care. 2006 Dec;29(12):2638-43. PMID: 17130197
  4. Prescriber's Letter 14(5): 2007 Januvia's Place in Therapy Detail-Document#: 230511 (subscription needed) http://www.prescribersletter.com
  5. FDA MedWatch Sitagliptin (marketed as Januvia and Janumet) - acute pancreatitis http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm183800.htm
  6. Prescriber's Letter 16(11): 2009 COMMENTARY: Januvia (Sitagliptin) and Pancreatitis CHART: Drug-Induced Pancreatitis COMMENTARY: Pancreatitis and Byetta (Exenatide) Detail-Document#: 251025 (subscription needed) http://www.prescribersletter.com
  7. Garg R et al. Acute pancreatitis in type 2 diabetes treated with exenatide or sitagliptin: A retrospective observational pharmacy claims analysis. Diabetes Care 2010 Nov; 33:2349. PMID: 20682680 - Gonzalez-Perez A et al. Acute pancreatitis in association with type 2 diabetes and antidiabetic drugs: A population-based cohort study. Diabetes Care 2010 Dec; 33:2580. PMID: 20833867
  8. Eurich DT et al Comparative safety and effectiveness of sitagliptin in patients with type 2 diabetes: retrospective population based cohort study. BMJ 2013;346:f2267 PMID: 23618722 http://www.bmj.com/content/346/bmj.f2267
  9. Weir DL et al Sitagliptin Use in Patients With Diabetes and Heart Failure. JACC Heart Fail. 2014 Jun 25. pii: S2213-1779(14)00194-2. PMID: 24998080 http://heartfailure.onlinejacc.org/article.aspx?articleID=1886074 - Bhatt DL and Cavender MA Do Dipeptidyl Peptidase-4 Inhibitors Increase the Risk of Heart Failure? JACC Heart Fail. 2014 Jun 25. pii: S2213-1779(14)00195-4. PMID: 24998081 http://heartfailure.onlinejacc.org/article.aspx?articleID=1886075
  10. Merck News Release. April 27, 2015 Merck Announces the Trial Evaluating Cardiovascular Outcomes with Sitagliptin (TECOS) Met Primary Endpoint. http://www.mercknewsroom.com/news-release/prescription-medicine-news/merck-announces-trial-evaluating-cardiovascular-outcomes-sit
  11. Young K, Fairchild DG, Hefner JE Sitagliptin Doesn't Appear to Raise Cardiovascular Risk. Physician's First Watch, June 9, 2015 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org - Green JB et al Effect of Sitagliptin on Cardiovascular Outcomes in Type 2 Diabetes. N Engl J Med. June 8, 2015 PMID: 26052984 http://www.nejm.org/doi/full/10.1056/NEJMoa1501352
  12. Toh S, Hampp C, Reichman ME et al Risk for Hospitalized Heart Failure Among New Users of Saxagliptin, Sitagliptin, and Other Antihyperglycemic Drugs: A Retrospective Cohort Study. Ann Intern Med. Published online 26 April 2016 PMID: 27110660 http://annals.org/article.aspx?articleid=2517404 - Selby JV Complementary Efforts Make for Efficient Research. Ann Intern Med. Published online 26 April 2016 PMID: 27110867 http://annals.org/article.aspx?articleid=2517405
  13. Buse JB, Bethel MA, Green JB et al. Pancreatic safety of sitagliptin in the TECOS study. Diabetes Care 2017 Feb; 40:164 PMID: 27630212 http://care.diabetesjournals.org/content/40/2/164
  14. Geriatric Review Syllabus, 10th edition (GRS10) Harper GM, Lyons WL, Potter JF (eds) American Geriatrics Society, 2019
  15. Solerte SB et al Sitagliptin Treatment at the Time of Hospitalization Was Associated With Reduced Mortality in Patients With Type 2 Diabetes and COVID-19: A Multicenter, Case-Control, Retrospective, Observational Study. Diabetes Care. 2020 Sep 29:dc201521 PMID: 32994187

Component-of

metformin/sitagliptin; januvia/metformin (Janumet) simvastatin/sitagliptin (Juvisync)