What are fibrates
What are fibrates
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Fibrates
Fibrates
Fibrates are a class of lipid-lowering medications primarily used to treat hypertriglyceridemia (high levels of triglycerides in the blood) and certain types of dyslipidemia. They are especially useful when triglyceride levels are very high or when HDL (good cholesterol) is low.
Mechanism of Action of fibrates:
Mechanism of Action of fibrates:
1- Fibrates bind to and activate PPAR-α in liver and adipose tissue.
2- Activated PPAR-α increases transcription of lipoprotein lipase (LPL) and apolipoprotein A-I and A-II (apoA-I, apoA-II), enhancing triglyceride breakdown and HDL synthesis.
3- They decrease hepatic production of apolipoprotein C-III, an inhibitor of LPL, further promoting triglyceride hydrolysis.
4- This leads to increased catabolism of triglyceride-rich lipoproteins (VLDL and chylomicrons), lowering plasma triglycerides.
5- Fibrates also stimulate fatty acid uptake and beta-oxidation, reducing triglyceride synthesis and VLDL secretion.
6- Overall effects: ↓ triglycerides (up to 50%), ↑ HDL cholesterol (up to 20%), variable effects on LDL cholesterol.
How do Fibrates work
How do Fibrates work
Examples of Medication Brand Names
Examples of Medication Brand Names
Fenofibrate.
Brand names: Tricor ,Fenogal ,Lipidil
Gemfibrozil.
Brand name: Lopid
Bezafibrate.
Brand name: Bezalip
Indication of fibrates
1- Lowering high triglyceride levels, especially in severe hypertriglyceridemia (triglycerides ≥ 500 mg/dL), to reduce the risk of pancreatitis.
2- Increasing HDL (good) cholesterol levels in patients with low HDL and high triglycerides, which helps reduce cardiovascular risk.
3- Adjunctive treatment of primary hypercholesterolemia and mixed dyslipidemia when statins are not sufficient or not tolerated.
4- Managing atherogenic dyslipidemia characterized by high triglycerides, low HDL, and small dense LDL particles, often seen in metabolic syndrome and type 2 diabetes.
Side effects of fibrates
Nausea.
stomach pain.
diarrhea.
indigestion.
Liver irritation or damage, usually mild and reversible but can be severe.
Blood clots, which can lead to pulmonary embolism or deep vein thrombosis .
Severe allergic reactions including swelling of face/throat.
breathing problems.
hives.
Changes in liver enzymes, homocysteine creatinine levels (monitored by doctors).
Muscle breakdown (rhabdomyolysis), rare but serious, especially if combined with statin.
Blood disturbances and interactions with blood thinners like warfarin.
Precautions for fibrates include:
1- Avoid use in patients with liver disease, kidney disease, gallbladder disease, or severe hepatic impairment, as fibrates may worsen these conditions.
2- Caution in renal impairment: fibrates can increase creatinine levels; dose adjustment may be necessary.
3- Avoid combining gemfibrozil with statins due to increased risk of myopathy; fenofibrate is preferred if combined with statins.
4- Monitor liver and kidney function periodically during treatment; discontinue or adjust dose if significant abnormalities occur.
5- Fibrates can increase effects of blood thinners like warfarin, requiring dose adjustments and close monitoring.
6- Not recommended during pregnancy or breastfeeding.
7- Watch for side effects such as muscle pain, weakness, abdominal pain, jaundice, or allergic reactions; report these promptly to a healthcare provider.
8- Use caution in elderly patients and those with pancreatitis or diabetes
Contraindications of fibrates include:
Contraindications of fibrates include:
1- Severe renal impairment or end-stage renal disease, including patients on dialysis.
1- Severe renal impairment or end-stage renal disease, including patients on dialysis.
2- Active liver disease or severe hepatic impairment, including unexplained persistent liver function abnormalities.
2- Active liver disease or severe hepatic impairment, including unexplained persistent liver function abnormalities.
3- Gallbladder disease or known gallstones, as fibrates increase cholesterol excretion into bile and may promote gallstone formation.
3- Gallbladder disease or known gallstones, as fibrates increase cholesterol excretion into bile and may promote gallstone formation.
4- Hypoalbuminemia and primary biliary cirrhosis.
4- Hypoalbuminemia and primary biliary cirrhosis.
5- Nephrotic syndrome.
5- Nephrotic syndrome.
6- Pregnancy and breastfeeding, due to potential risks and lack of safety data.
6- Pregnancy and breastfeeding, due to potential risks and lack of safety data.
7- Known hypersensitivity to fibrates or any ingredients in the formulation.
7- Known hypersensitivity to fibrates or any ingredients in the formulation.
Monographs
Monographs
3Drug monograph.pdfBezafibrate
Shahenaz Fayez (pharma).pdfCiprofibrate
Gemfibrozil. (5).pdfGemfibrozil
Drug monograph (2).pdfFenofibrate
Drug monograph-End``.pdfClofibrate
References
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