Dyslipidemia Drugs Flashcards
Atorvostatin
Action: HMG-CoA reductase inhibitor (analog)
Usage: Hyperlipidemia, prophylactic for CAD, Acute Coronary Syndrome
Toxicities: myopathy/rhabdo, hepatic dysfunction (elevated ALT). teratogenic!
Other: oral admin= slow onset w/ long duration, most effective at night. Most effective for pts w/ cardiovascular disease
Niacin
Action: Diacyl glycerol acyl-transferase (DGAT) inhibitor. GPCR 109 Agonist
Usage: Primary hyperlipidemias, elevated LDL/VLDL, low HDL
Toxicities: flushing, hyperuricemia, pruritis
Other: Use w/ statin or bile resins.
Gemfibroliz
Action: PPAR-alpha agonist
Usage: Hypertriglyceremia, dysbetalipoproteinemia
Toxicities: myopathy, hepatic dysfunction
Other: Use w/ statins for max efficacy
Mechanism: PPAR-alpha complex inhibits inflammation. Complex also binds Retinoic Acid Receptor and activates PPRE transcription factor–> increases free fatty acid metabolism proteins, peroxisomes etc.
Colestipol
Action: Bile-acid binding anion-exchange resins
Usage: Primary hypercholesteremia, elevated LDL
Toxicities: constipation/diarrhea/bloating/flatulence
Other: Use w/ statins. May decrease bioavailability of other drugs (warfarin, thiazides, digitalis, aspirin and tetracyclins)
Mechanism: inhibits enterohepatic bile circulation. Decreases plasma cholesterol and increases LDLR expression.
Enzetimibe
Action: NPC1L1 (intestinal cholesterol transporter) inhibitor
Usage: Primary hypercholesteremia, elevated LDL
Toxicities: Diarrhea, hepatic dysfunction
Other: combine w/ statin
Mechanism: inhibit cholesterol uptake –> increases LDLR expression
