Metformin + Vildagliptin
DPP-4 Inhibitor · Antidiabetic
Also known as Galvus Met, Zomelis-Met, Jalra-M, Vinglyn-M, Vysov-M
- ONSET
- 1h · Metformin: Glucose-lowering effects typically observed within hours of first dose. Vildagliptin: Rapid onset of DPP-4 inhibition within 1 hour.
- PEAK
- 2.5h · Metformin: Peak plasma concentration reached in 2-3 hours for immediate release. Vildagliptin: Peak plasma concentrations reached within 1-4 hours.
- t½
- 6.5h · Metformin: Plasma elimination half-life is approximately 4-9 hours. Vildagliptin: Terminal elimination half-life is approximately 3 hours, but the pharmacodynamic effect (DPP-4 inhibition) is longer due to tight enzyme binding.
- DURATION
- 13h · Metformin: Sustained glucose lowering effect over 10-16 hours with standard release. Vildagliptin: Inhibition of DPP-4 enzyme lasts approximately 24 hours.
Mechanism
Metformin, a biguanide, primarily reduces hepatic glucose production and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. Vildagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, prevents the breakdown of incretin hormones (GLP-1 and GIP), leading to enhanced glucose-dependent insulin secretion from beta-cells and suppressed glucagon secretion from alpha-cells. Together, these complementary mechanisms address different pathophysiological defects in type 2 diabetes, leading to improved glycemic control. Combination rationale: This fixed-dose combination provides a synergistic approach to managing type 2 diabetes by targeting different pathways of glucose regulation. Metformin reduces glucose production and improves insulin sensitivity, while Vildagliptin enhances incretin effects to stimulate insulin secretion and suppress glucagon. This combination leads to better glycemic control, significant HbA1c reduction, and improved patient adherence compared to individual components taken separately.
Indications
Dosing
- Adult
- Initial dose typically 50 mg vildagliptin/500 mg metformin once daily, titrated to 50 mg vildagliptin/500 mg metformin twice daily. May be increased to 50 mg vildagliptin/850 mg metformin twice daily or 50 mg vildagliptin/1000 mg metformin twice daily. Administer with meals to reduce gastrointestinal side effects.…
- Pediatric
- Safety and efficacy have not been established in patients under 18 years of age. Not recommended for pediatric use.
- Renal adjustment
- eGFR 60-89 mL/min/1.73m²: Max metformin 2000mg/day, max vildagliptin 100mg/day. eGFR 45-59 mL/min/1.73m²: Max metformin 2000mg/day, max vildagliptin 50mg/day. eGFR 30-44 mL/min/1.73m²: Max metformin 1000mg/day, max vildagliptin 50mg/day. eGFR <30 mL/min/1.73m²: Contraindicated.
- Hepatic adjustment
- Contraindicated in patients with severe hepatic impairment. Not recommended in patients with liver dysfunction, including those with pre-treatment ALT or AST >3 times the upper limit of normal.
- Geriatric
- Caution advised due to potential for decreased renal function; monitor renal function more frequently. Start with lower doses and titrate carefully.
- Max dose
- Maximum recommended daily dose is 100 mg vildagliptin and 2000 mg metformin.
Pharmacokinetics
Contraindications
- Renal dysfunction (eGFR <30 mL/min/1.73m²)
- Metabolic acidosis, including diabetic ketoacidosis
- Hypersensitivity to metformin, vildagliptin, or any excipients
- Acute or chronic metabolic acidosis (e.g., lactic acidosis, diabetic ketoacidosis)
- Severe hepatic impairment
- Acute conditions with potential for altered renal function (e.g., dehydration, severe infection, shock)
- Cardiac or respiratory failure
- Acute myocardial infarction
- Alcohol intoxication
- Radiological studies involving intravascular administration of iodinated contrast agents (temporary discontinuation required)
Side effects
- Lactic acidosis (Metformin)
- Pancreatitis (Vildagliptin)
- Hepatotoxicity (elevated liver enzymes, rare hepatic failure)
- Bullous pemphigoid (Vildagliptin)
- Severe and disabling arthralgia
- Hypoglycemia (especially with concomitant sulfonylurea or insulin)
- Angioedema
Pregnancy & lactation
Pregnancy Category C. Limited data on human pregnancy. Not recommended during pregnancy unless clearly indicated and potential benefits outweigh risks. Insulin is generally preferred for glycemic control during pregnancy.
Metformin is excreted into human milk in small amounts; generally considered compatible with breastfeeding with monitoring. Vildagliptin excretion into human milk is unknown. Due to potential for adverse effects, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Related guidelines
Other DPP-4 Inhibitor drugs
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