Sitagliptin


Concise Prescribing Info
Indications/Uses
Type 2 DM.
Dosage/Direction for Use
Adult : PO 100 mg once daily.
Dosage Details
Oral
Type 2 diabetes mellitus
Adult: 100 mg once daily.
Renal Impairment
CrCl (mL/min) Dosage
<30 or ESRD requiring dialysis 25 mg once daily.
30 to <50 50 mg once daily.
Administration
May be taken with or without food.
Special Precautions
Patient w/ type 1 diabetes, history of angioedema. Not intended for the treatment of diabetic ketoacidosis. Moderate and severe renal impairment. Pregnancy and lactation.
Adverse Reactions
Headache, dizziness, GI disturbances (e.g. constipation, vomiting), peripheral oedema, upper resp tract infection, nasopharyngitis, elevated liver enzyme values, acute renal failure, hypoglycaemia, arthralgia, myalgia, pain in extremity, back pain.
Potentially Fatal: Acute pancreatitis (e.g. haemorrhagic or necrotising pancreatitis); serious hypersensitivity reactions (e.g. anaphylaxis, angioedema, and exfoliative skin conditions including Stevens-Johnson syndrome).
MonitoringParameters
Monitor glycosylated Hb (HbA1c), serum glucose. Assess renal function prior to initiation of therapy and periodically thereafter.
Drug Interactions
Increased risk of hypoglycaemia when used in combination w/ sulfonylureas or insulin.
Action
Description: Sitagliptin inhibits dipeptidyl peptidase IV (DPP-IV) enzyme resulting in prolonged active incretin levels. Incretin hormones, including glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), regulate glucose homeostasis by increasing insulin synthesis and release from pancreatic β-cells and decreasing glucagon secretion from pancreatic α-cells. Reduced glucagon secretion leads in decreased hepatic glucose production. Under normal physiologic circumstances, incretin hormones are released by the intestine throughout the day and levels are increased in response to a meal; incretin hormones are rapidly inactivated by the DPP-IV enzyme.
Onset: Reduction in postprandial plasma glucose excursion: Approx 60 min.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Bioavailability: Approx 87%. Time to peak plasma concentration: Approx 1-4 hr.
Distribution: Volume of distribution: Approx 198 L. Plasma protein binding: 38%.
Metabolism: Undergoes minimal metabolism, mainly by CYP3A4 isoenzyme and to a lesser extent by CYP2C8 isoenzymes to inactive metabolites.
Excretion: Via urine (approx 79% as unchanged drug; 16% as metabolites) and faeces (13%). Terminal half-life: Approx 12 hr.
Chemical Structure

Chemical Structure Image
Sitagliptin

Source: National Center for Biotechnology Information. PubChem Database. Sitagliptin, CID=4369359, https://pubchem.ncbi.nlm.nih.gov/compound/Sitagliptin (accessed on Jan. 22, 2020)

Storage
Store between 20-25°C.
MIMS Class
References
Anon. Sitagliptin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 10/11/2014.

Buckingham R (ed). Sitagliptin Phosphate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/11/2014.

Januvia Tablet, Film coated (Merck Sharp & Dohme Corp.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 10/11/2014.

McEvoy GK, Snow EK, Miller J et al (eds). SITagliptin Phosphate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 10/11/2014.

Disclaimer: This information is independently developed by MIMS based on Sitagliptin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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