Pharmacokinetics of Gliptins

• Sitagliptin is well absorbed orally, is little metabolized and is largely excreted unchanged in urine with a t½ averaging 12 hours. Dose reduction is needed in renal impairment, but not in liver disease.
• Vildaglitptin: The major route of elimination of vildagliptin is by hepatic metabolism; only 20–25% is excreted unchanged in urine. Dose reduction is needed in moderately severe liver and kidney disease.
• Linagliptin lowers HbA 1c by 0.4–0.6% when added to metformin, sulfonylurea, or pioglitazone. The dosage is 5 mg daily and since it is primarily excreted via the bile, no dosage adjustment is needed in renal failure.
• Saxagliptin is given orally as 2.5–5 mg daily. The drug reaches maximal concentrations within 2 hours (4 hours for its active metabolite). It is minimally protein bound and undergoes hepatic metabolism by CYP3A4/5. The major metabolite is active, and excretion is by both renal and hepatic pathways. The terminal plasma half-life is 2.5 hours for saxagliptin and 3.1 hours for its active metabolite. Dosage adjustment is recommended for individuals with renal impairment

Pathology Revision + GT - Rs. 999/- You will get access to all till NEET - You can enrol to Subscribe here today