metformin:
Onset of action: Within days; maximum effects up to 2 weeks
Distribution: Vd: 654 ?? 358 L; partitions into erythrocytes; concentrates in liver, kidney, and GI tract
Protein binding: Negligible
Metabolism: Not metabolized by the liver
Bioavailability: Absolute: Fasting: 50% to 60%
Half-life elimination: Plasma: 4 to 9 hours; Blood ~17.6 hours
Time to peak, serum: Immediate release: 2 to 3 hours; Extended release: 7 hours (range: 4 to 8 hours)
Excretion: Urine (90% as unchanged drug; active secretion)
vildagliptin:
Absorption
Tmax: 1.7 hours
Bioavailability: 85%
Effect of food: no effect on AUC; 19% decrease in Cmax; Tmax increased to 2.5 hours
Distribution
Protein binding: 9.3%
Vd: 71 L
Metabolism
Possible hydrolysis via kidneys and dipeptidyl peptidase-4
Not metabolized via CYP450 enzymes
Excretion
Fecal: 15%
Renal: 85%, 23% unchanged
Renal clearance: 13 L/hr
Dialyzable: No (hemodialysis), 3% removed
Elimination Half Life: 3 hours
禁忌症
Known hypersensitivity to vildagliptin-metformin or any component of the formulation
ESRD,eGFR<30ml/min/1.73m2
acute or chronic metabolic acidosis with or without coma
acute complication: dehydration, severe infection, shock (acute kidney injury)
heptic dysfunction
breast feeding
alcoholism, acute alcohol intoxication
懷孕分類
Drug(Metformin) has been found to cross the placenta in concentrations which may be comparable to those found in the maternal plasma.Available evidence is is inadequate.
哺乳分類
Should not use in breast-feeding women.Available evidence is is inadequate.
副作用
metformin
>10%:
Gastrointestinal: Diarrhea, nausea and vomiting, flatulence (4% to 12%)
Infection: Infection (21%)
Vildagliptin: Dizziness (1% to less than 10% ), Headache (0.1% to 12.9% ),
Nasopharyngitis (3.5% to 13.2% )
劑量和給藥方法
initial dose :1 tablet twice daily
daily maximum dose: metformin3000mg/vildagliptin100mg
The manufacturer recommends avoiding metformin since liver disease is considered a risk factor for the development of lactic acidosis during metformin therapy