Pharmacology A: Anti-lipidemic Properties & Statins

This set of vocabulary flashcards covers the pharmacology of anti-lipidemic drugs, focusing on statins, fibrates, ezetimibe, and plant sterols, including their mechanisms of action, metabolism, and side effects.

Lipophilic Statins

A class of statins, including Simvastatin and Atorvastatin, characterized by their high tendency to diffuse into skeletal muscle tissues, leading to a higher incidence of myopathy.

Pravastatin

Identified as the most hydrophilic statin, it exhibits minimal CYP450 metabolism, is excreted through the kidneys, and is highly hepato-selective.

Hepatoselectivity

The property of statins being actively transported to the liver, which is the target organ for endogenous cholesterol synthesis.

CYP3A4

The Cytochrome P450 enzyme responsible for metabolizing Atorvastatin and Simvastatin; its inhibition can lead to toxic drug accumulation.

Furanocoumarin

The specific active compound found in grapefruit that is responsible for inhibiting the CYP3A4 enzyme.

Rosuvastatin

The most potent statin available that achieves maximum LDL lowering at the lowest numerical dose; it is principally metabolized by CYP2C9 and CYP2C19.

PPAR-alpha ($PPAR-\alpha$)

The receptor activated by fibrates that forms a dimer with the Retinoid X Receptor ($RXR$) to alter gene expression, specifically increasing Lipoprotein Lipase (LPL) expression.

Lipoprotein Lipase (LPL)

An enzyme in the muscle that facilitates the breakdown of triglycerides into free fatty acids and glycerol.

Fenofibrate

A fibrate medication that can cause phototoxicity due to a molecular structure it shares with the NSAID Ketoprofen.

Gemfibrozil

A fibrate more likely than Fenofibrate to interact with statins by decreasing statin uptake in the liver and inhibiting the glucuronidation process.

Ezetimibe

A cholesterol absorption inhibitor that binds to the Niemann-Pick C1-Like 1 (NPC1L1) receptor in the intestine's brush borders.

Enterohepatic Recycling

The process by which a drug is absorbed through the intestine, transported to the liver, and then excreted back into the intestine, contributing to a longer duration of action.

Plant Sterols

Compounds with a structure similar to cholesterol that compete for space within micelles, thereby preventing cholesterol absorption in the intestine.

HMG CoA Reductase

The rate-limiting enzyme in cholesterol synthesis that is inhibited by statins to decrease intracellular cholesterol concentration.

Rhabdomyolysis

A severe adverse effect of statins involving muscle breakdown and the release of myoglobin, $K^+$, and creatinine kinase into the blood, potentially leading to organ failure.

Myositis

A muscle-related adverse effect involving inflammation of the muscle tissue.