sitagliptin (Januvia)
Jump to navigation
Jump to search
Indications
* sitagliptin treatment at the time of hospitalization is associated with reduced mortality in patients with diabetes mellitus type-2 & COVID-19[15]
Dosage
Dosage adjustment in renal failure
Table
| creatinine clearance | dosage |
|---|---|
| > 50 mL/min | 100 mg QD |
| 30-50 mL/min | 50 mg QD |
| < 30 mL/min | 25 mg QD |
Pharmacokinetics
Adverse effects
- not likely to cause weight gain
- acute pancreatitis[5]
- does not increase risk of acute pancreatitis[7]
- small increase in acute pancreatitis not statistically significant[13]
- as safe as other oral hypoglycemic agents[8]
- not likely to cause hypoglycemia[14]
- 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]
- noninferior to usual care for cardiovascular outcomes
- no increase in hospitalization for heart failure[10]
- 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
- drug interaction(s) of gliptins with sulfonylureas
- drug interaction(s) of fluoroquinolones with hypoglycemic agents
Mechanism of action
- dipeptidyl peptidase-4 inhibitor
- inhibits incretin catabolism
- enhances incretin system
- lowers A1c about 0.3% to 0.8%
- effects mostly post-prandial glucose
More general terms
Component of
References
- ↑ 1.0 1.1 Prescriber's Letter 12(9): 2005 Investigational Medicines for Diabetes: Sitagliptan (Januvia) and Vildagliptan (Galvus) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220715&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 2.0 2.1 Prescriber's Letter 13(11): 2006 New Drug: Sitagliptin (Januvia) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=221102&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 3.0 3.1 3.2 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: https://www.ncbi.nlm.nih.gov/pubmed/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: https://www.ncbi.nlm.nih.gov/pubmed/17130197 - ↑ Prescriber's Letter 14(5): 2007 Januvia's Place in Therapy Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230511&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 5.0 5.1 FDA MedWatch Sitagliptin (marketed as Januvia and Janumet) - acute pancreatitis http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm183800.htm
- ↑ Prescriber's Letter 16(11): 2009 COMMENTARY: Januvia (Sitagliptin) and Pancreatitis CHART: Drug-Induced Pancreatitis COMMENTARY: Pancreatitis and Byetta (Exenatide) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=251025&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 7.0 7.1 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: https://www.ncbi.nlm.nih.gov/pubmed/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: https://www.ncbi.nlm.nih.gov/pubmed/20833867 - ↑ 8.0 8.1 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 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/23618722 <Internet> http://www.bmj.com/content/346/bmj.f2267
- ↑ 9.0 9.1 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. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/24998080 <Internet> 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. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/24998081 <Internet> http://heartfailure.onlinejacc.org/article.aspx?articleID=1886075 - ↑ 10.0 10.1 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
- ↑ 11.0 11.1 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 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/26052984 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1501352 - ↑ 12.0 12.1 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 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27110660 <Internet> http://annals.org/article.aspx?articleid=2517404
Selby JV Complementary Efforts Make for Efficient Research. Ann Intern Med. Published online 26 April 2016 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27110867 <Internet> http://annals.org/article.aspx?articleid=2517405 - ↑ 13.0 13.1 Buse JB, Bethel MA, Green JB et al. Pancreatic safety of sitagliptin in the TECOS study. Diabetes Care 2017 Feb; 40:164 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27630212 <Internet> http://care.diabetesjournals.org/content/40/2/164
- ↑ 14.0 14.1 Geriatric Review Syllabus, 10th edition (GRS10) Harper GM, Lyons WL, Potter JF (eds) American Geriatrics Society, 2019
- ↑ 15.0 15.1 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: https://www.ncbi.nlm.nih.gov/pubmed/32994187