What is the mechanism of action of fibrates?
Fibrates stimulate cellular fatty acid uptake, conversion to acyl-CoA derivatives, and catabolism by the beta-oxidation pathways, which, combined with a reduction in fatty acid and triglyceride synthesis, results in a decrease in VLDL production.
What is the mechanism of action of gemfibrozil?
Mechanism of Action: Activation of the nuclear transcription receptor “peroxisome proliferator – activated receptor alpha” (PPAR-α). PPAR-α activation by fibrates results in numerous changes in lipid metabolism that act together to decrease plasma triglyceride levels & increase plasma HDL.
Which drug is considered a fibrate?
Fibrate drugs, such as gemfibrozil (Lopid) and fenofibrate (TriCor), are undoubtedly the best tools to address the condition characterized by high triglycerides, low high-density lipoprotein (HDL), and small dense low-density lipoprotein (LDL) (atherogenic dyslipidemia), but the most recent guidelines from both the …
How do fibrates cause gallstones Usmle?
Fibrates decrease the synthesis of bile acid by down-regulation of cholesterol 7 alpha-hydroxylase and sterol 27-hydroxylase expression, therefore making it easier for cholesterol to precipitate and increasing the risk for gallstones.
What are the side effects of fibrates?
The side effects of fibrates include nausea, stomach upset, and sometimes diarrhea. Fibrates can irritate (inflame) the liver. The liver irritation usually is mild and reversible, but it occasionally can be severe enough to require stopping the drug. Fibrates can cause gallstones when used for several years.
What does fibrates do to your body?
Fibrates are medicines prescribed to help lower high triglyceride levels. Triglycerides are a type of fat in your blood. Fibrates also may help raise your HDL (good) cholesterol. High triglycerides along with low HDL cholesterol increase the risk of heart disease and stroke.
What is the mechanism of action of simvastatin?
Simvastatin is in a class of medications called HMG-CoA reductase inhibitors (statins). It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body.
What is the mechanism of action of ezetimibe?
Mechanism Of Action Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine. In a 2-week clinical study in 18 hypercholesterolemic patients, ZETIA inhibited intestinal cholesterol absorption by 54%, compared with placebo.
Are fibrates safe?
Fibrates are associated with a slightly increased risk (<1.0%) for myopathy, cholelithiasis, and venous thrombosis. In clinical trials, patients without elevated triglycerides and/or low high-density lipoprotein cholesterol (HDL) levels, fibrates are associated with an increase in noncardiovascular mortality.
Do fibrates inhibit CYP450?
9 While neither of the fibrates are inhibitors of any of the CYP450 enzymes used by statins currently on the market, gemfibrozil can inhibit glucuronidation and some of the transporters they do rely upon.
Is fenofibrate bad for kidneys?
Conclusion: Short-term fenofibrate treatment did not alter glomerular filtration rate by more than 20% in subjects with normal kidney function, but a smaller decrease cannot be ruled out. Increased serum creatinine levels may be caused by decreased creatinine clearance.
Who should not take fenofibrate?
chronic kidney disease stage 3B (moderate) chronic kidney disease stage 4 (severe) chronic kidney disease stage 5 (failure) Child-Pugh class A liver impairment.
What is the mechanism of action of fibrate drugs?
Mechanism of action. The main mechanism of fibrate drugs is activation of gene transcription factors known as PPARs, particularly PPAR-α, which regulate the expression of genes that control lipoprotein metabolism.
How are fibrate drugs related to thiazolidinediones?
Mechanism of action. The main mechanism of fibrate drugs is activation of gene transcription factors known as PPARs, particularly PPAR-α, which regulate the expression of genes that control lipoprotein metabolism. Fibrates are related to thiazolidinediones, and their PPAR-mediated actions are described in Chapter 40.
How does PPAR-α mediate the action of fibrates?
The PPAR-α form mediates fibrate action on HDL cholesterol levels via transcriptional induction of synthesis of the major HDL apolipoproteins, apoA-I and apoA-II. Fibrates lower hepatic apoC-III production and increase lipoprotein lipase—mediated lipolysis via PPAR.
How does a fibrate affect HDL cholesterol levels?
Fibrates activate specific transcription factors belonging to the nuclear hormone receptor superfamily, termed peroxisome proliferator-activated receptors (PPARs). The PPAR-α form mediates fibrate action on HDL cholesterol levels via transcriptional induction of synthesis of the major HDL apolipoproteins, apoA-I and apoA-II.
