Fenofibrate

Fenofibrate is an active substance that is used to treat hypercholesterolemia and hyperlipidemia. Hypercholesterolemia is diagnosed on the basis of blood findings when patients have high cholesterol levels. Hyperlipidemia is an excess of lipids (fats) in the blood. This is also colloquially referred to as "blood lipids". Both blood values should not be too high, as otherwise the risk of vascular calcification increases and thus the risk of heart attack and stroke. Fenofibrate belongs to the group of fibrates and is a lipid-lowering agent. It is available as a monopreparation, but also as a combination preparation with simvastatin. It is usually available as a white crystalline powder, is insoluble in water and is a prodrug. A prodrug is an inactive substance that is only converted into its active form in the body, where it is supposed to work. The active form of fenofibrate is fenofibric acid.

Fenofibrate works by binding to the peroxisome proliferator-activated receptors (PPAR). This binding stimulates the lipid metabolism. Among other things, the LDL (low density lipoprotein) cholesterol value, the triglycerides and apolipoprotein B are lowered. At the same time, the HDL (high density lipoprotein) cholesterol value is increased. PPAR belongs to the nuclear receptors. Its activation leads to an increase in lipid, glucose and amino acid homeostasis. The increased lipid metabolism can lead to liver damage.

Fenofibrate is broken down in the liver. The half-life, i.e. the time the body needs to excrete half of the active substance, is around 23 hours. The maximum plasma concentration (Cmax), i.e. the maximum concentration of the active substance in the blood plasma (liquid cell-free part of the blood), is 6-9.5 mg/L and is reached after 4-6 hours.

Always take fenofibrate exactly as described in the package leaflet or as advised by your doctor.

Adults:

The usual recommended dose is 250 mg fenofibrate daily.

The following side effects may occur:

Frequent:

• Abdominal pain
• Nausea
• vomiting
• Diarrhea
• flatulence
• elevated transaminases
• Increased homocysteine level in the blood

Occasionally:

• deep vein thrombosis
• Pulmonary embolism (pulmonary infarction)
• Headaches
• Pancreatitis (inflammation of the pancreas)
• Gallstones
• Hypersensitivity of the skin
• Muscle weakness
• muscle cramps
• Muscle diseases
• Sexual dysfunction
• Increased creatinine levels in the blood

Rarely:

• Decreased hemoglobin level in the blood
• Decreased leukocyte count
• Hypersensitivity
• Inflammation of the liver (hepatitis)
• Hair loss (alopecia)
• photosensitivity of the skin
• Increased blood urea

Frequency unknown:

• Lung diseases
• jaundice
• inflammation of the gallbladder
• inflammation of the bile duct
• biliary colic
• Erythema multiforme
• Stevens-Johnson syndrome
• Toxic epidermal necrolysis
• rhabdomyolysis
• fatigue

Interactions may occur if the following medicines are taken at the same time:

• "Blood thinners" (oral anticoagulants)
• Ciclosporin
• other fibrates or drugs to lower blood lipid levels
• Drugs for the treatment of type 2 diabetes mellitus (glitazones)
• with CYP450 enzymes

Fenofibrate must NOT be taken in the following cases

• in case of hypersensitivity to fenofibrate
• hepatic insufficiency
• gallbladder disease
• severe renal insufficiency
• in case of pancreatitis
• in case of known photoallergic or phototoxic reactions with other fibrates or ketoprofen

Fenofibrate should NOT be used under the age of 18.

Fenofibrate should only be used during pregnancy after a careful risk-benefit assessment by a doctor. No harmful effects have been demonstrated in animal studies. At doses that were already toxic to the mother, toxic effects were also observed in the unborn baby.

Fenofibrate should NOT be used during breastfeeding, as it is not known whether the active substance passes into breast milk.