Cholesterol Lowering Drugs

What is lovastain

HMG-CoA Reductase Inhibitor (Statin)

What does locastatin do?

decrease LDL and TG; increases HDL

what is atorvastatin

HMG-CoA Reductase Inhibitor (Statin)

what does atorvastatin does

decreases LDL and TG; increases HDL

what is niacin

a water-soluble viatmin

what does Niacin do

decreases TG and LDL; increases HDL

what is gemfibrozil

fibric acid derivative

what does gemfibrozil do

decreases TG; increases HDL; variable LDL

what is fenofibrate

fibric acid derivative

what does fenofibrate do

decreases TG; increases HDL; variable LDL

what is colestipol

bile acid binding agent

what does colestipol do

decreases LDL, increases TG and HDL slightly

what is cholestyramine

bile acid binding agent

what does cholestyramine do

decreases LDL, increases TG and HDL slightly

what is ezetimibe

intestinal sterol absorption inhibitor

what does ezetimibe do

decreases LDL; neutral TG/HDL

what is vytorin

combination of Ezetimibe and Simvastatin

what does vytorin do

dramatically decreases LDL; decreases TG; increases HDL

what is lovaza

Omega-3 Acid Ethyl Esters (EPA / DHA)

what does lovaza do

decreases TG; increases LDL and HDL

what is alirocumab

PCSK9 Inhibitor (Monoclonal Antibody)

what does alirocumab do

dramatically decreases LDL

what is inclisiran

Small Interfering RNA (siRNA)

what does inclisiran do

dramatically decreases LDL

what is bempedoic acid

ATP-Citrate Lyase (ACL) inhibitor

what does bempedoic acid do

decreases LDL

mechanism of action for lovastatin

Competitive inhibition of hepatic HMG-CoA reductase, halting the rate-limiting step of cholesterol synthesis (HMG-CoA to mevalonate). Depleted internal cholesterol up-regulates hepatic LDLR expression, accelerating plasma LDL clearance

mechanism of action for niacin

Inhibits lipolysis in adipose tissue (reducing FFA flux to liver); decreases hepatic VLDL synthesis and secretion; stimulates endothelial LPL to increase VLDL clearance; decreases HDL catabolism.

mechanism of action for gemfibrozil

Agonist at PPAR-alpha receptors; upregulates LPL activity to enhance intravascular triglyceride-rich VLDL hydrolysis. Promotes FFA uptake into tissue and decreases hepatic VLDL secretion.

mechanism of action for colestipol

Non-absorbable anion exchange resin that binds negatively charged bile acids in the gut lumen, preventing enterohepatic recirculation and forcing excretion in stool. Hepatocytes convert internal cholesterol into new bile acids, up-regulating LDLRs to extract LDL from blood.

mechanism of action for atorvastatin

High-potency competitive inhibition of hepatic HMG-CoA reductase, triggering strong LDLR up-regulation. Cheaper and most commonly prescribed drug class. Shares the same adverse effect profile as Lovastatin.

mechanism of action for fenofibrate

Activates PPAR-alpha, increasing LPL expression and ApoA-I/ApoA-II synthesis while down-regulating ApoC-III (an LPL inhibitor), accelerating TG catabolism. Preferred over Gemfibrozil when statin co-administration is necessary.

mechanism of action for cholestyramine

Sequesters bile salts in the gut, interrupting enterohepatic circulation. Induces hepatic conversion of cholesterol to bile acids via 7 alpha-hydroxylase up-regulation, which secondarily increases cell-surface LDLR expression. Non-systemic, useful in statin-intolerant patients.

mechanism of action for ezetimibe

Selectively inhibits the Niemann-Pick C1-Like 1 (NPC1L1) transporter at the enterocyte brush border, blocking dietary and biliary cholesterol absorption. Decreased delivery of dietary cholesterol to the liver upregulates LDLR expression. Mild efficacy alone (about 18% LDL reduction).

mechanism of action for vytorin

Dual-mechanism inhibition: Ezetimibe blocks intestinal cholesterol uptake, while Simvastatin inhibits hepatic HMG-CoA reductase. Synergistically counteracts the compensatory increase in hepatic cholesterol synthesis caused by Ezetimibe monotherapy.

what is the mechanism of action for lovaza

Poor substrate for acyl-CoA:diacylglycerol acyltransferase; inhibits hepatic esterification of other fatty acids and enhances mitochondrial beta-oxidation, reducing hepatic TG synthesis and VLDL secretion.

what is the mechanism of action for alirocumab

Fully human IgG1 monoclonal antibody that binds free circulating PCSK9. Prevents PCSK9-mediated lysosomal degradation of hepatic LDLRs. Recycled LDLRs return to the hepatocyte surface to continually clear LDL-C

what is the mechanism of action for inclisiran

Synthetic siRNA conjugated with GalNAc, targeting hepatic Asialoglycoprotein receptors for targeted hepatocyte uptake. Integrates into the RISC complex to cleave PCSK9 mRNA, preventing translation of the PCSK9 protein.

what is the mechanism of action of bempedoic acid

Prodrug activated in the liver that inhibits ATP-Citrate Lyase (ACL)—an enzyme acting two steps upstream of HMG-CoA reductase in the cholesterol biosynthesis pathway. Decreases hepatic cholesterol synthesis and upregulates LDLR.