Generic
Metformin Hydrochloride + Sitagliptin
52 brands available in the market
At a glance
Metformin Hydrochloride + Sitagliptin is a combination medicine that controls high blood sugar levels in type 2 diabetes mellitus. Metformin reduces glucose production and absorption, and Sitagliptin is a DPP-4 inhibitor that increases incretin hormone activity.
Description
Metformin is a biguanide that decreases hepatic glucose production, intestinal glucose absorption, and improves insulin sensitivity by increasing peripheral glucose uptake. Sitagliptin is a DPP-4 inhibitor that slows the inactivation of incretin hormones (GLP-1 and GIP), increasing insulin release from pancreatic beta cells and decreasing glucagon secretion from alpha cells.
Indications
- Type 2 diabetes mellitus - as an adjunct to diet and exercise to improve glycemic control
Pharmacological class
Biguanide + DPP-4 Inhibitor
Pharmacology
Metformin reduces glucose production and absorption; Sitagliptin inhibits DPP-4 to increase incretin hormone levels, which stimulates glucose-dependent insulin release and reduces glucagon secretion.
Mechanism of action
Controls blood sugar by reducing glucose production and absorption and increasing incretin activity.
Dosage
Immediate Release (Adult):
- Not on metformin: 50/500 mg twice daily
- On metformin: Sitagliptin 50 mg twice daily + current metformin dose
- Maximum: Sitagliptin 100 mg + Metformin 2000 mg/day
Extended Release (Adult):
- Initial: Sitagliptin 50/100 mg + Metformin ER 500/1000 mg once daily (evening)
- Maximum: Sitagliptin 100 mg + Metformin ER 2000 mg/day
Administration
- Swallow tablet whole; do not chew, crush or break
- Take with food (to reduce stomach upset)
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Drug interactions
- Additive effect with sulfonylureas (hypoglycemia risk)
- Thiazide diuretics, corticosteroids, OCs may worsen glycemic control
- ACE inhibitors may reduce fasting blood glucose
- Cimetidine may increase serum levels
- Increased risk of lactic acidosis with iodinated contrast agents (potentially fatal)
Food interactions
Alcohol consumption with Metformin + Sitagliptin is unsafe.
Contraindications
- Renal dysfunction (males Cr >1.5 mg/dL, females >1.4 mg/dL)
- Metabolic acidosis (including diabetic ketoacidosis)
- History of serious hypersensitivity to sitagliptin or metformin
Side effects
Common Side Effects (≥5%):
- Diarrhea
- Upper respiratory tract infection
- Headache
- Hypoglycemia (with sulfonylurea or insulin)
- Nausea, vomiting, upset stomach
Use in pregnancy
Use in Pregnancy: Metformin + Sitagliptin is generally considered safe during pregnancy (Category B); animal studies have shown low or no adverse effects.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Metformin + Sitagliptin is probably safe during breastfeeding; limited human data suggests no significant risk to the baby.
Precautions & warnings
- Inform doctor if symptoms of lactic acidosis occur (deep/rapid breathing, persistent nausea, vomiting, abdominal pain)
- Monitor blood sugar regularly to avoid hypoglycemia
- Avoid alcohol (risk of lactic acidosis)
- Temporarily stop before major surgery or contrast dye procedures
- Caution in history of pancreatitis
Pediatric use
Safety and efficacy not established in children under 18 years.
Geriatric use
Elderly require dose adjustment due to potential decreased renal function; monitor renal function regularly.
Renal / hepatic impairment
Renal Impairment: eGFR <30: contraindicated; eGFR 30-45: not recommended to initiate; discontinue if eGFR falls below 30; monitor renal function regularly.
Hepatic Impairment: Probably safe in liver disease; dose adjustment may not be needed.
Overdose effects
Overdose may cause lactic acidosis; sitagliptin is modestly dialyzable; metformin is dialyzable.
Therapeutic class
Combination Oral Hypoglycemic Preparations
Storage conditions
Store below 25°C in a dry place, away from light; keep out of reach of children.
Chemical structure
Metformin Hydrochloride + Sitagliptin