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
Therapeutic class
Combination Oral Hypoglycemic Preparations
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.
Side effects
Common Side Effects (≥5%):
- Diarrhea
- Upper respiratory tract infection
- Headache
- Hypoglycemia (with sulfonylurea or insulin)
- Nausea, vomiting, upset stomach
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
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
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.
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.
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.
Storage conditions
Store below 25°C in a dry place, away from light; keep out of reach of children.
Chemical structure
Metformin Hydrochloride + Sitagliptin