Related Experiment Video
Updated: Jun 24, 2026
08:45
LDL Cholesterol Uptake Assay Using Live Cell Imaging Analysis with Cell Health Monitoring
Published on: November 17, 2018
Etofibrate enhances 123I-LDL-binding in human liver
Barbara Palumbo1, Anthony Oguogho, Renato Palumbo
1Institute of Nuclear Medicine, University of Perugia, Italy.
Hellenic Journal of Nuclear Medicine
|March 31, 2009
Summary
Etofibrate treatment improved lipid profiles in patients with mixed hyperlipidemia. The drug enhanced low-density lipoprotein (LDL) uptake by the liver, indicating a beneficial effect on LDL receptor activity in vivo.
Area of Science:
- Pharmacology
- Lipid Metabolism
- Cardiovascular Research
Background:
- Etofibrate, a fibric and nicotinic acid combination, treats hyperlipidemia.
- Limited data exists on etofibrate's effect on liver LDL binding and kinetics in patients.
Purpose of the Study:
- To investigate the in vivo effect of etofibrate on autologous low-density lipoprotein (LDL) binding to the liver.
- To assess etofibrate's impact on lipid profiles in patients with mixed hyperlipidemia.
Main Methods:
- 11 patients with mixed hyperlipidemia received 500mg etofibrate twice daily for 6 weeks.
- In vivo liver uptake of autologous (123)I-LDL was measured.
- Serum lipid profiles were analyzed before and after treatment.
Main Results:
- Etofibrate increased in vivo liver uptake of (123)I-LDL by 16.1%.
- Plasma decay of LDL was shortened, and lipid profiles improved significantly.
- Total cholesterol decreased by 14.9%, LDL-cholesterol by 22.2%, and HDL-cholesterol increased by 10.9%.
Conclusions:
- Etofibrate demonstrates a beneficial effect on LDL liver receptor level in vivo.
- The drug effectively improves lipid profiles in patients with mixed hyperlipidemia.
- Findings support etofibrate's role in managing dyslipidemia through enhanced hepatic LDL clearance.
Related Concept Videos
01:20Lipid-Lowering Drugs: Statins and Miscellaneous Agents
Hyperlipidemia, a medical condition often referred to as high cholesterol, is characterized by abnormally elevated levels of lipids in the bloodstream. When present in excess, these lipids, specifically cholesterol and triglycerides, can lead to serious health complications, often involving cardiovascular diseases. Illnesses like atherosclerosis, heart attacks, and pancreatitis have all been linked to untreated hyperlipidemia. This means controlling and regulating cholesterol and triglyceride...
01:26Effect of Hepatic Disease on Pharmacokinetics: Drug Dosing and Hepatic Blood Flow
Chronic liver disease significantly impacts drug metabolism due to alterations in hepatic blood flow and enzyme accessibility. This disruption affects the body's pharmacokinetics—the movement and processing of drugs within the system. Key enzymes crucial for metabolizing medications become less accessible, changing how drugs are processed and utilized. Furthermore, liver disease influences the synthesis of plasma proteins, such as albumin and globulins, which play critical roles in drug binding...
01:29Cholesterol: Significance and Regulation
Although not a source of energy, cholesterol plays a significant role as a foundational structure for bile salts, steroid hormones, and vitamin D, as well as being a crucial component of plasma membranes. Approximately 15% of blood cholesterol is derived from our diet, with the remainder synthesized from acetyl CoA by the liver and intestines. Cholesterol is eliminated from the body through its conversion into bile salts, which are eventually discarded in the feces.
Considering cholesterol and...
Considering cholesterol and...
01:09Hepatic Drug Clearance: Effect of Protein Binding
Hepatic clearance is influenced by protein binding based on the drug's extraction ratio. Drugs with high extraction ratios are considered flow-limited and remain unaffected by protein binding during hepatic clearance. On the other hand, drugs with low extraction ratios may be impacted by plasma protein binding, although the extent of this influence depends on the fraction of the drug bound.
For low-extraction-ratio drugs that are less than 80% protein-bound, minor changes in protein binding...
For low-extraction-ratio drugs that are less than 80% protein-bound, minor changes in protein binding...
01:14Effect of Hepatic Disease on Pharmacokinetics: Active Drug, Metabolite and Fraction of Metabolized Drug
In pharmacotherapy, monitoring drug concentrations is paramount, especially for drugs whose therapeutic effects hinge on both the active compound and its metabolite. Hepatic impairment profoundly influences drug potency by altering liver function. If the drug is more potent than its metabolite, impaired liver function amplifies drug activity due to elevated drug concentration levels. Conversely, if the metabolite holds greater potency, diminished liver function diminishes drug activity by...
01:08Effect of Hepatic Disease on Pharmacokinetics: Dose Adjustments Due to Hepatic Impairment
Hepatic impairment, characterized by decreased liver function, does not uniformly mandate adjustments in drug dosage. Whether dosage modifications are necessary depends on various factors related to the drug's metabolism and elimination pathways. If a drug is primarily excreted via the kidneys and bypasses significant hepatic processing, if it undergoes minimal metabolic transformation in the liver, or if it is volatile and primarily expelled through the lungs, dose adjustments may not be...