Sitagliptin
- Atc Codes:A10BH01
- CAS Codes:654671-77-9#486460-32-6
- PHARMGKB ID:654671-77-9#486460-32-6
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Substrate of
- Inhibits
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Januvia, Tesavel, Xelevia; Belgium: Januvia; Bulgaria: Januvia, Tesavel, Xelevia; Cyprus: Januvia; Czech Republic: Januvia, Tesavel, Xelevia; Denmark: Januvia; Estonia: Januvia, Tesavel, Xelevia; Finland: Januvia; France: Januvia, Xelevia; Germany: Januvia, Tesavel, Xelevia; Greece: Januvia, Xelevia; Hungary: Januvia, Xelevia; Ireland: Januvia, Tesavel, Xelevia; Italy: Januvia, Tesavel, Xelevia; Latvia: Januvia, Tesavel, Xelevia; Lithuania: Januvia, Tesavel, Xelevia; Luxembourg: Januvia, Tesavel, Xelevia; Malta: Januvia, Tesavel, Xelevia; Netherlands: Tesavel, Xelevia; Poland: Januvia, Tesavel, Xelevia; Portugal: Januvia, Tesavel, Xelevia; Romania: Januvia, Tesavel, Xelevia; Slovakia: Januvia, Tesavel, Xelevia; Slovenia: Januvia, Tesavel, Xelevia; Spain: Tesavel, Xelevia; Sweden: Januvia, Tesavel, Xelevia; UK: Januvia.
North America
Canada: Januvia; USA: Januvia.
Latin America
Argentina: Januvia; Mexico: Januvia.
Drug combinations
Sitagliptin and Metformin
Chemistry
Sitagliptin Phosphate: C~16~H~15~F~6~N~5~O H~3~O~4~P H~2~O. Mw: 523.32. (1) 1,2,4-Triazolo[4,3-a]pyrazine, 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-, phosphate (1:1) monohydrate; (2) 7-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazinemonophosphate monohydrate. CAS-654671-77-9; CAS-486460-32-6 (sitagliptin)(2005).
Pharmacologic Category
Antidiabetic Agents; Dipeptidyl Peptidase IV (DPP-4) Inhibitors. (ATC-Code: A10BH01).
Mechanism of action
Sitagliptin inhibits dipeptidyl peptidase IV (DPP-IV) enzyme resulting in prolonged active incretin levels. Incretin hormones (e.g. glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide) regulate glucose homeostasis by increasing insulin synthesis and release from pancreatic β-cells and decreasing glucagon secretion from pancreatic α-cells. Decreased glucagon secretion results in decreased hepatic glucose production. Under normal physiologic circumstances, incretin hormones are released by intestine throughout the day and levels are increased in response to a meal. Incretin hormones are rapidly inactivated by DPP-IV enzyme.
Therapeutic use
Type 2 diabetes mellitus (non-insulin-dependent).
Pregnancy and lactiation implications
Adverse events not observed in animals. There are no adequate studies in pregnant women. Use of oral agents generally not recommended as routine management of gestational diabetes mellitus or type 2 diabetes mellitus during pregnancy. Insulin is drug of choice for control of diabetes mellitus during pregnancy. Excretion in breast milk unknown (use caution).
Unlabeled use
Contraindications
Serious hypersensitivity (e.g. anaphylaxis, angioedema) or any component of the formulation. Type 1 diabetes mellitus (insulin-dependent), diabetic ketoacidosis.
Warnings and precautions
Rare hypersensitivity reactions, including anaphylaxis, angioedema, and/or severe dermatologic reactions such as Stevens-Johnson syndrome, reported. Use with caution in moderate-to-severe renal dysfunction and end-stage renal disease requiring hemodialysis or peritoneal dialysis. Use caution when used in conjunction with sulfonylureas (risk of hypoglycemia).