Pharmacology
| Drug | Absorption | Bioavailability (%) | IC50 (nM) | Mean volume of distribution (L) | Protein binding (%) | Half-life (hours,100 mg dose) | Metabolism | Excretion |
|---|---|---|---|---|---|---|---|---|
| Sitagliptin | Rapidly absorbed with peak concentration at 1–4 hours | 87 | 18 | 198 | 38 | 12.4 | Small fraction undergoes hepatic metabolism via CYP 450 3A4 and 2C8 | Excreted in an unchanged form in the urine (79%) |
| Vildagliptin | Rapidly absorbed with peak concentration at 1–2 hours | 85 | 3 | 70.5 | 9.3 | 1.68 (once a day) and 2.54 (twice a day) | Hydrolysis resulting in a pharmacologically inactive metabolite. A fraction (22%) is also excreted unchanged by the kidneys | Excretion of the metabolite is carried out through urine (85%) and feces (15%) |
The pharmacokinetic properties of sitagliptin and vildagliptin appear unaffected by age, sex or BMI. Clinical researches have shown that sitagliptin and vildagliptin do not have the side effects that tend to follow type 2 diabetes treatment, e.g. weight gain and hyperglycemia, but however, other side effects have been observed, including upper respiratory tract infections, sore throat and diarrhea.
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