Vildagliptin and Metformin

Hypoglycaemic excluding Insulin · Biguanide/Dipeptidyl peptidase-4 inhibitor

Indications

Treatment of type II diabetes mellitus in patients inadequately controlled by maximal tolerated dose of metformin alone or who are already treated with the combination of vildagliptin and metformin as separate tab.

Dosage

Adults: Initially, based on current metformin dose, 50 mg/850 mg or 50 mg/1000 mg twice daily (morning and evening) with or just after food. For patients receiving components as separate tab, switch to equivalent dosage. Recommended daily dose, 100 mg/2000 mg. Children: Not recommended.

Adverse Effects

Metformin: GI upset, taste disturbance, rarely lactic acidosis, abnormal liver function tests, hepatitis, skin reactions, reduced B12 absorptions. Vildagliptin: Bullous and exfoliative skin lesions. Monotherapy: Dizziness. With metformin: Tremor, headache, dizziness, nausea, hypoglycaemia. With a sulfonylurea: Tremor, headache, dizziness, asthaenia, hypoglycaemia. With a glitazone: Wt gain, peripheral oedema. With insulin: Headache, hypoglycaemia, chills, GI upset.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Metformin: Diabetic ketoacidosis or pre-coma. Renal or hepatic impairment. Acute conditions predisposing to renal impairment (e.g. dehydration, severe infection, shock). Cardiac or respiratory failure, recent MI. Acute alcohol intoxication, alcoholism. Discontinue for 48 hours before and after surgery. Patients >75 years of age. Vildagliptin: Diabetic ketoacidosis, hepatic impairment, CHF. Precautions: Metformin: Assess risk factors for lactic acidosis; discontinue immediately if metabolic acidosis suspected. Monitor renal function at least annually. Vildagliptin: Measure liver enzymes before treatment, every 3 months during first year then periodically. If transaminase levels increased, monitor frequently until return to normal; withdraw and do not restart if persistent increase…

Interactions

Metformin: Alcohol, iodinated contrast agents, diuretics, corticosteroids, ACE inhibitors, sympathomimetics, NSAIDs, other hypoglycaemics. Inhibitors of OCT2 (e.g., cimetidine, dolutegravir, ranolazine, trimethoprim). Vildagliptin: ACE inhibitors.

Advice to Patient

Take with meals or immediately after meals.

Pharmacokinetics

VILDAGLIPTIN: Absorption: Rapidly absorbed from the GI tract. Metabolism: Renal. Bioavailability: 85%. Half-life elimination: Oral: 3 hrs. IV inj: 2 hrs. Time to peak, plasma: 1.7 hrs. Excretion: Urine (85%). Faeces (15%). METFORMIN: Onset of action: Within days, max effects up to 2 wks. Metabolism: Not metabolized by the liver. Bioavailability: Absolute: Fasting: 50%-60%. Half-life elimination: Plasma: 4-9 hrs. Blood: Approx. 17.6 hrs. Time to peak, serum: Immediate release: 2-3 hrs. Extended release: 7 hrs. (Range: 4-8 hrs). Excretion: Urine.

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.