Generic
Saxagliptin
4 brands available in the market
At a glance
Saxagliptin is a DPP-4 inhibitor used for the treatment of type 2 diabetes mellitus. It slows the inactivation of incretin hormones, increasing insulin secretion and reducing glucose production.
Description
Saxagliptin is an orally-active DPP-4 enzyme inhibitor. It competitively inhibits DPP4, slowing the inactivation of incretin hormones, increasing their bloodstream concentrations, and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes.
Indications
- Type 2 diabetes mellitus (as an adjunct to diet and exercise)
Therapeutic class
DPP-4 Inhibitor
Pharmacological class
Dipeptidyl Peptidase-4 (DPP-4) Inhibitor
Pharmacology
Saxagliptin competitively inhibits DPP-4 enzyme, slowing the breakdown of incretin hormones (GLP-1 and GIP). This increases glucose-dependent insulin secretion from the pancreas and reduces hepatic glucose production, lowering both fasting and postprandial blood glucose levels.
Mechanism of action
Inhibits DPP-4 enzyme to enhance incretin hormone activity and improve glycemic control.
Dosage
Adult Dose (Oral):
- Recommended: 2.5 mg or 5 mg once daily
- With strong CYP3A4/5 inhibitors: Do not exceed 2.5 mg/day
- Renal impairment (CrCl <50): 2.5 mg/day (post-dialysis)
Administration
- Take orally with or without food
- Take at the same time each day
- Swallow tablet whole; do not chew, crush, or break
Missed dose
If you miss a dose, take it as soon as possible; if almost time for the next dose, skip it; do not double the dose.
Side effects
Common Side Effects (>5%):
- Upper respiratory tract infection
- Urinary tract infection
- Headache
- Hypoglycemia (with sulfonylurea)
- Peripheral edema (with TZD)
Precautions & warnings
- Not effective in type 1 diabetes or diabetic ketoacidosis
- Be aware of hypoglycemia symptoms
- Caution in severe liver disease
- Avoid alcohol consumption
Contraindications
- Known hypersensitivity to saxagliptin (anaphylaxis, angioedema)
Drug interactions
- With sulfonylureas: Increased risk of hypoglycemia; dose reduction may be needed
- Strong CYP3A4/5 inhibitors: Increase saxagliptin levels (limit to 2.5 mg)
- CYP3A4 inducers: May reduce glycemic effect
Food interactions
Alcohol is unsafe with Saxagliptin (increases hypoglycemia risk).
Use in pregnancy
Use in Pregnancy: Generally safe; animal studies show low or no adverse effects; limited human data; consult your doctor.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably safe; limited human data suggests no significant risk; consult your doctor.
Pediatric use
Safety and efficacy not established in children <18 years
Geriatric use
No dosage adjustment needed in elderly patients
Renal / hepatic impairment
Renal Impairment: CrCl >50: no dose adjustment; CrCl <50: 2.5 mg/day; ESRD on dialysis: 2.5 mg/day post-dialysis; consult your doctor.
Hepatic Impairment: Mild-moderate: no dose adjustment; severe: caution needed; consult your doctor.
Overdose effects
Overdose up to 400 mg/day (80 times MRHD) showed no dose-related adverse reactions; 23% removed by hemodialysis; provide symptomatic treatment.
Storage conditions
Store at 20-25°C, protected from light and moisture; keep out of reach of children.
Chemical structure
Saxagliptin