Generic
Sitagliptin
45 brands available in the market
At a glance
Sitagliptin is a DPP-4 inhibitor used for the treatment of type 2 diabetes mellitus. It slows the inactivation of incretin hormones, increasing insulin release and decreasing glucagon levels.
Description
Sitagliptin is a DPP-4 inhibitor that slows the inactivation of incretin hormones (GLP-1 and GIP). Incretin hormones are released by the intestine in response to meals and are rapidly inactivated by DPP-4. Sitagliptin increases active incretin levels, which enhances glucose-dependent insulin release and reduces glucagon secretion, decreasing hepatic glucose production.
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
Sitagliptin inhibits DPP-4 enzyme, slowing the breakdown of incretin hormones (GLP-1 and GIP). Increased active incretin levels enhance insulin release from pancreatic beta cells and reduce glucagon secretion from alpha cells, decreasing hepatic glucose production and improving glycemic control.
Mechanism of action
Inhibits DPP-4 enzyme to enhance incretin hormone activity and improve glycemic control.
Dosage
Adult Dose (Oral):
- Recommended: 100 mg once daily
- Renal Impairment:
- CrCl >50: 100 mg/day
- CrCl 30-50: 50 mg/day
- CrCl <30 or ESRD: 25 mg/day
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:
- Headache
- Upper respiratory tract infection
- Nasopharyngitis
- Hypoglycemia (with sulfonylurea or insulin)
Precautions & warnings
- Not effective in type 1 diabetes or diabetic ketoacidosis
- Caution in history of pancreatitis; discontinue if suspected
- Be aware of hypoglycemia symptoms
- Dose adjustment needed in severe renal impairment
Contraindications
- Serious hypersensitivity reactions to sitagliptin (anaphylaxis, angioedema)
- Type 1 diabetes
- Diabetic ketoacidosis
Drug interactions
- With sulfonylurea or insulin: Increased hypoglycemia risk
- Digoxin: Slight increase in digoxin concentration
Food interactions
Alcohol is unsafe with Sitagliptin (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 data suggests no significant risk; consult your doctor.
Pediatric use
Safety and efficacy not established in children <18 years
Geriatric use
Elderly patients: Assess renal function for dose selection
Renal / hepatic impairment
Renal Impairment: CrCl >50: no dose adjustment; CrCl 30-50: 50 mg/day; CrCl <30 or ESRD: 25 mg/day; consult your doctor.
Hepatic Impairment: Safe in liver disease; dose adjustment may not be needed; consult your doctor.
Overdose effects
Overdose up to 800 mg was tolerated; slight QTc increase (not clinically important); 13.5% removed by hemodialysis; provide symptomatic treatment.
Storage conditions
Store below 25°C in a dry place, protected from light; keep out of reach of children.
Chemical structure
Sitagliptin