First-generation fibrate (PPAR-α agonist) that activates lipoprotein lipase and lowers serum triglycerides + LDL. Largely supplanted by gemfibrozil and fenofibrate due to a 1978 WHO trial showing increased non-cardiovascular mortality. Highly protein-bound (~96-97%) — clinically relevant as a warfarin plasma-binding displacer.
Dosing Guidelines
PO: Typical 1000 (Range: 500–2000)
Target Organ Systems
cardiovascular
digestive
Interactions
Warfarin (major): Bjornsson 1979 (PMID:480183) verbatim: "Clofibrate caused a displacement of warfarin from plasma protein binding sites, with a 13% increase in the free drug fraction in plasma." Δfu/fu_baseline = 0.13. Mechanism: high albumin binding by both compounds (~97% bound) → competition at site I. Clinically: clofibrate potentiates warfarin's anticoagulant effect — INR monitoring required.