Ballicules.com

Gemfibrozil

LOPID

What it isPPAR-alpha agonist reducing triglycerides; severe hypertriglyceridemia.

Why this oneUnlike fenofibrate, it strongly inhibits statin clearance, so it is the fibrate not to pair with a statin.

What limits itRhabdomyolysis can follow statin coadministration; strong CYP2C8 inhibition also raises susceptible drugs.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Hyperlipidemia / hypertriglyceridemiaAdults600 mg BID (1200 mg/day)600 mg BID1200 mg/day

Renal Contraindicated in severe renal dysfunction

Hepatic Contraindicated in hepatic dysfunction (incl. primary biliary cirrhosis)

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Undefined

Lactation Undefined

NO BOXED WARNINGS

Principal riskMyopathy with a statin; a strong CYP2C8 inhibitor

Cost, est. cash$5–$150/month

Generic entry1993

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger1 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityMyopathy/rhabdomyolysis and hepatotoxicity; interaction burden varies by agent.

Mechanism of action: Gemfibrozil ballicule

Gemfibrozil ballicule: receptor binding, kinetics and half-life diagram

Open Gemfibrozil in the interactive console ↗

Memory aids: mascots and interaction avatars

Gemfibrozil LOPID mascot mnemonic cartoon
“Loppy Gym Fiber”
Gemfibrozil CYP2C8 inhibitor avatar
CYP2C8 inhibitor (strong)
Gemfibrozil OATP inhibitor avatar
OATP inhibitor
Gemfibrozil OATP substrate avatar
OATP substrate
Gemfibrozil P-gp inhibitor avatar
P-gp inhibitor (strong)

Open Gemfibrozil in the interactive console ↗