Saxagliptin
- Atc Codes:A10BH03
- CAS Codes:361442-04-8
- PHARMGKB ID:361442-04-8
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
- Genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Onglyza; Belgium: Onglyza; Bulgaria: Onglyza; Czech Republic: Onglyza; Denmark: Onglyza; Estonia: Onglyza; Finland: Onglyza; France: Onglyza; Germany: Onglyza; Greece: Onglyza; Hungary: Onglyza; Ireland: Onglyza; Italy: Onglyza; Latvia: Onglyza; Luxembourg: Onglyza; Malta: Onglyza; Netherlands: Onglyza; Poland: Onglyza; Portugal: Onglyza; Romania: Onglyza; Slovakia: Onglyza; Slovenia: Onglyza; Spain: Onglyza; Sweden: Onglyza; UK: Onglyza.
North America
Canada: Onglyza; USA: Onglyza.
Latin America
Argentina: Onglyza; Brazil: Onglyza; Mexico: Onglyza.
Drug combinations
Saxagliptin and Metformin
Chemistry
Saxagliptin Monohydrate: C~18~H~25~N~3~O~2~ H~2~O. Mw: 333.43 (1)(1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile, monohydrate; (2)(1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxyadamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrate. CAS-361442-04-8.
Pharmacologic Category
Antidiabetic Agents; Dipeptidyl Peptidase IV (DPP-4) Inhibitors. (ATC-Code: A10BH03).
Mechanism of action
Increased concentrations of the incretin hormones, such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released into the bloodstream from the small intestine in response to meals. These hormones cause insulin release from the pancreatic beta-cells in a glucose-dependent manner, but are inactivated by the dipeptidyl peptidase-4 (DPP4) enzyme within minutes. GLP-1 also lowers glucagon secretion from pancreatic alpha-cells, reducing hepatic glucose production. In patients with type 2 diabetes, concentrations of GLP-1 are reduced but the insulin response to GLP-1 is preserved. Saxagliptin is a competitive DPP4 inhibitor that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in patients with type 2 diabetes mellitus in a glucose-dependent manner.
Therapeutic use
Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Should not be used for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis. Has not been studied in combination with insulin.
Pregnancy and lactiation implications
Should be used during pregnancy only if clearly needed (there are no adequate, well-controlled studies in pregnant women). Not recommended during lactation.
Unlabeled use
Contraindications
None known to date.
Warnings and precautions
When used with an insulin secretagog (e.g. sulfonylurea), a lower dose of the insulin secretagog may be required to reduce the risk of hypoglycemia. There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with saxagliptin or any other antidiabetic drug.