Bezafibrate
Brand and Other Names:
Bezafibrate
Mechanism of Action:
Indications:
Route:
Dose:
Adverse Reactions:
Contraindication:
Warnings and Precautions:
Not FDA approved
GOOGLE OVERVIEW
Bezafibrate is a fibrate drug used primarily to treat hyperlipidemia, a condition characterized by high levels of lipids (fats) in the blood. It is available in various countries, including Canada, but it is not currently approved for clinical use in the United States.
Key actions and uses
- Lipid Lowering: Bezafibrate effectively lowers high levels of triglycerides (up to 50%) and low-density lipoprotein (LDL) cholesterol ("bad" cholesterol) (up to 20%), while simultaneously increasing high-density lipoprotein (HDL) cholesterol("good" cholesterol) (up to 20%).
- Hyperlipidaemia and Hypertriglyceridemia: It's specifically used to treat hyperlipidaemia, particularly when associated with high triglyceride levels. In patients with hypertriglyceridemia and coronary artery disease, bezafibrate has been associated with a significant long-term reduction in mortality.
- PPAR Agonism: Bezafibrate acts as an agonist for peroxisome proliferator-activated receptors (PPARs), particularly PPAR-α. This mechanism involves:
- Reducing the liver's secretion of very low-density lipoprotein (VLDL).
- Increasing the activity of triglyceride lipases, which break down triglyceride-rich lipoproteins.
- Reducing cholesterol biosynthesis and stimulating LDL-receptor mediated lipoprotein catabolism.
Potential side effects
- Gastrointestinal Issues: Common side effects include nausea, stomach pain, gas, and stomach upset. These are often mild and may improve with time.
- Muscle Problems: Muscle aches, pain, cramps, or weakness (myopathy) can occur. In rare instances, this can escalate to a serious condition called rhabdomyolysis, which involves rapid muscle tissue breakdown and potential kidney damage.
- Liver Function: Bezafibrate can affect liver function, potentially causing elevated liver enzymes. Regular monitoring of liver function tests is important.
- Other potential side effects: Allergic reactions (rash, hives, itching, swelling), headaches, dizziness, skin redness, and problems with renal (kidney) function.
Dosage and administration
- Bezafibrate is typically administered as an oral medication.
- Standard dosage often involves 200 mg three times daily, or a sustained-release preparation of 400 mg once daily.
- It should be taken with or after meals.
- The sustained-release tablets should be swallowed whole and not chewed, crushed, or broken.
- Dosage adjustments may be necessary for individuals with impaired renal (kidney) function.
Important interactions and precautions
- Statins: Caution is advised when combining bezafibrate with statins, particularly in patients predisposed to muscle disease, due to an increased risk of muscle-related side effects.
- Warfarin: Bezafibrate may enhance the anticoagulant effect of warfarin, potentially increasing the risk of bleeding.
- Other Medications: Bezafibrate can interact with a variety of other medications, including:
- Medications that increase the risk or severity of myopathy or rhabdomyolysis.
- Medications that affect blood sugar levels (sulfonylureas).
- Certain medications that can decrease bezafibrate's metabolism or excretion.
- Contraindications: Bezafibrate is not recommended for individuals with primary biliary cirrhosis, pre-existing gallbladder disease, or Type I hyperlipoproteinemia. It is also contraindicated in pregnant or breastfeeding women.
Further considerations
- Mitochondrial Function: Bezafibrate has shown promise in preclinical studies and is being investigated for its potential role in improving mitochondrial function in conditions such as mitochondrial myopathy.
- X-Linked Adrenoleukodystrophy (X-ALD): Clinical trials are exploring bezafibrate's ability to reduce very long chain fatty acids (VLCFA) in patients with X-ALD.
- Diabetes and Metabolic Syndrome: Compared to other fibrates, bezafibrate has shown positive effects on glucose metabolism and insulin resistance, potentially reducing the incidence of type 2 diabetes.
Note: This information is intended for general knowledge and should not be considered medical advice. Always consult with a healthcare professional for diagnosis, treatment, and any questions regarding your health or medications
See package insert for full prescribing information.