Mô tả
Sitagliptin modestly increases digoxin exposure through inhibition of P-glycoprotein-mediated renal tubular secretion, though the effect is unlikely to be clinically significant at therapeutic digoxin doses.
Cơ chế
Sitagliptin is a mild inhibitor of P-glycoprotein; digoxin is a well-characterised P-gp substrate that relies heavily on renal P-gp for elimination. Mild P-gp inhibition increases digoxin AUC by approximately 11% and Cmax by 18%.
Ý nghĩa lâm sàng
FDA-required interaction study showed a statistically significant but small increase in digoxin exposure; clinical significance is low for most patients but potentially relevant in renal impairment.
Xử trí
No routine dose adjustment is required; monitor for digoxin toxicity (nausea, visual changes, arrhythmia) in patients with renal impairment or on high-end therapeutic digoxin doses.