Medication Description: Clofibrate (Clofibratum)
CLOFIBRAT (Clofibratum) *.
Ethyl- a - (para-chlorophenoxy) -isobutyrate.
Synonyms , Fibramid, Geromid, Hypocerol, Klofibrat, Lipavil, Lipavlon, Lipomid, Liponorm, Lisisterol, Miscleron, Neo-Atromid, Nibratol, Normolipol, Regelan, Sterochol, etc.
Light yellow liquid with a faint aromatic odor. Insoluble in water, soluble in alcohol, ether and other organic solvents.
Clofibrate was the first drug from the group of fibric acid derivatives (fibrates), which have been used as lipid-lowering agents. Currently, a number of fibric acid derivatives are used (see Bezafibrat, Fenofibrate, etc.).
The preparations of this group cause a decrease in the content of cholesterol and triglycerides in plasma, triglycerides in VLDL and cholesterol in LDL. However, they increase cholesterol in HDL (anti-atherogenic).
The decrease in cholesterol is associated with the ability of fibrates to block the hydroxymethylglutar coenzyme A reductase (HMG CoA), which is involved in cholesterol biosynthesis, and to increase cholesterol breakdown.
Fibrates also reduce platelet aggregation and blood viscosity. Reduce the level of uric acid in the blood plasma. In order to prevent these drugs are used for familial hypercholesterolemia, hyperlipidemia and hypertriglyceridemia, idiopathic lowering of LDL.
As therapeutic agents, they are used in complex therapy for sclerosis of coronary and peripheral vessels, brain vessels, diabetic angiopathy and retinopathy, various diseases accompanied by hyperlipidemia, including hyperlipidemia in combination with an increase in plasma uric acid levels.
The preparations of the fibrates group differ in their effectiveness and tolerability. For example, clofibrate is somewhat less effective than new drugs (bezafibrate, fenofibrate) of this group, and more often causes side effects.
Clofibrate is administered orally in capsules containing 0.25 g each. It is taken 0.5 to 0.75 g (2 to 3 capsules) 3 times a day (after meals). Treatment is usually carried out in courses of 20-30 days with the same breaks (4-6 courses).
When using fibrates, gastrointestinal disorders (nausea, vomiting), pruritus, urticaria, muscle pain (such as myositis), muscle weakness (more often in the legs) are possible; increase in body weight due to water retention in the body. After the abolition of drugs, these phenomena usually pass.
With prolonged use of clofibrate and other fibrates, intrahepatic cholestasis may develop, and cholelithiasis may worsen. When using clofibrate, the formation of stones in the gallbladder and biliary tract was observed (and therefore in some countries this drug was no longer used).
Fibrates enhance coumarin anticoagulants, butadion, salicylates, oral antidiabetic drugs. Use them in patients with diabetes should be with caution to avoid hypoglycemia.