Pharmacology · Antidiabetic Drugs (Oral Hypoglycemics, Insulins)

A patient on metformin for type 2 diabetes develops lactic acidosis after receiving IV contrast for CT angiography. The metformin-contrast interaction causing lactic acidosis is mediated by:

  • A Contrast dye directly inhibits complex I of the mitochondrial ETC, combining with metformin's ETC inhibition
  • B Contrast dye displaces metformin from albumin binding sites, increasing free drug concentration
  • C Contrast-induced nephropathy reduces renal metformin clearance, causing drug accumulation and subsequent lactate accumulation via enhanced anaerobic glycolysis
  • D Iodinated contrast activates hepatic CYP3A4, metabolizing metformin to a toxic lactate-producing metabolite
Correct answer: C. Contrast-induced nephropathy reduces renal metformin clearance, causing drug accumulation and subsequent lactate accumulation via enhanced anaerobic glycolysis

Explanation

Metformin is entirely renally cleared (not metabolized). Its principal mechanism of lactic acidosis involves inhibition of mitochondrial Complex I (NADH dehydrogenase), shifting hepatic metabolism toward anaerobic glycolysis. Iodinated contrast agents can cause contrast-induced nephropathy (AKI), dramatically reducing metformin clearance and causing accumulation. Elevated metformin levels markedly increase Complex I inhibition and lactate production. Current guidelines recommend withholding metformin 48 hours before and after contrast administration if renal function is borderline (eGFR 30–60 mL/min).

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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