Drug reference

Saxagliptin

DPP-4 Inhibitor · Antidiabetic

Also known as Saxagliptin hydrochloride

DPP-4 InhibitorAntidiabetic

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

2 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 11 →

BexaroteneSevereDatabaseDDInter
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Mechanism

Saxagliptin inhibits dipeptidylpeptidase-4 (DPP-4), an enzyme responsible for the inactivation of incretin hormones like glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4, Saxagliptin increases the circulating levels of active incretins. This leads to glucose-dependent enhancement of insulin secretion from pancreatic beta cells and suppression of glucagon secretion from pancreatic alpha cells, thereby improving glycaemic control.

Indications

Type 2 diabetes mellitus as monotherapy (if metformin inappropriate)Type 2 diabetes mellitus in combination with other antidiabetic drugs (including insulin) if existing treatment fails to achieve adequate glycaemic controlFirst intensification of treatment with metformin if HbA1c is not controlledAlternative initial single therapy if metformin is contra-indicated or not toleratedDual combination therapy (e.g., with pioglitazone or a sulfonylurea) if initial single drug does not control HbA1cTriple therapy regimen with metformin hydrochloride and a sulfonylureaType 2 diabetes mellitus not controlled by metformin and/or a sulfonylurea with either saxagliptin or dapagliflozin (when used as combination with dapagliflozin)Treatment of type 2 diabetestype 2 diabetes mellitus

Dosing

Adult: 5 mg once daily; for further information on use with other antidiabetic drugs—consult product literature. For Saxagliptin with dapagliflozin (Adult 18–74 years): 5/10 mg once daily (expressed as saxagliptin/dapagliﬂozin). Dose of concomitant sulfonylurea or insulin may need to be reduced.
Renal adjustment: Reduce dose by half in moderately severe renal failure
Geriatric: Elderly patients are a caution for Saxagliptin alone. For Saxagliptin with dapagliflozin, initiation is not recommended for adults 75 years and over.

Pharmacokinetics

Duration

24 hours

Half-life

2–4 hours (active metabolite 3–7 hours)

Protein binding

Circulates primarily in unbound form

Metabolism

Hepatic microsomal enzymes

Excretion

Largely unchanged in the urine

Contraindications

Elderly (as a caution)
History of pancreatitis (as a caution, discontinue if symptoms of acute pancreatitis occur)
Moderate to severe heart failure (limited experience, as a caution)
Initiation not recommended for adults 75 years and over (for Saxagliptin with dapagliflozin combination)