Fibrates: Effects, Uses & Risks

Fibrates are carboxylic acids and belong to the organic compounds. Various representatives such as clofibrate, gemfibrozil and etofibrate are known on the market. Fibrates bind to specific receptors in cell organelles, causing a reduction in blood lipid levels. They are therefore used to treat lipid disorders such as high cholesterol or triglyceride levels. Fibrates should … Fibrates: Effects, Uses & Risks

Statins

Products Most statins are commercially available in the form of film-coated tablets, and some are also available as capsules. The first active ingredient to be marketed was lovastatin from Merck in the United States in 1987. In many countries, simvastatin (Zocor) and, shortly thereafter, pravastatin (Selipran) were the first agents to be approved in 1990. … Statins

Ezetimibe

Products Ezetimibe is commercially available in tablet form, as a monopreparation (Ezetrol, generic), and as a fixed combination with simvastatin (Inegy, generic) and with atorvastatin (Atozet). Also released is a combination with rosuvastatin. Ezetimibe was approved in many countries and in the United States in 2002. Generic and auto-generics entered the market in November 2017. … Ezetimibe

Colchicine

Products Medicines containing colchicine are no longer on the market in many countries. Drugs are available abroad that can be imported. It may also be possible to prepare an extemporaneous formulation in a pharmacy (difficulties: toxicity, substance). Stem plant Colchicine is the main alkaloid of the autumn crocus (Colchicaceae), which contains it particularly abundantly in … Colchicine

Lipid-Lowering Agents

Products Lipid-lowering agents are mainly sold as tablets and capsules as monopreparations and combination preparations. Some other dosage forms exist, such as granules and injectables. Statins have established themselves as the most important group at present. Structure and properties The chemical structure of lipid-lowering agents is inconsistent. However, within the class, groups with comparable structures … Lipid-Lowering Agents

Pravastatin

Products Pravastatin is commercially available in tablet form (Selipran, generics). It has been approved in many countries since 1990. Structure and properties Pravastatin (C23H36O7, Mr = 424.5 g/mol) is present in drugs as pravastatin sodium, a white to yellowish-white powder or crystalline powder that is readily soluble in water. It is not a prodrug, unlike … Pravastatin

Gemfibrozil

Products Gemfibrozil is commercially available in the form of film-coated tablets (Gevilon, Gevilon Uno). It has been approved in many countries since 1985. Structure and properties Gemfibrozil (C15H22O3, Mr = 250.3 g/mol) exists as a white powder that is practically insoluble in water. Effects Gemfibrozil (ATC C10AB04) has lipid-lowering properties. It lowers VLDL, triglycerides, total … Gemfibrozil

Glitazare

Effects Glitazars combine the lipid-lowering effects of fibrates (lower triglycerides and LDL, increase HDL) with the antidiabetic effect of glitazones, which increase tissue sensitivity to insulin. Mechanism of action Glitazars have a dual mechanism of action. On the one hand, they activate the nuclear receptor PPAR-alpha, the drug target of fibrates, and on the other … Glitazare

Fibrate

Effects Fibrates (ATC C10AB) have lipid-lowering properties. They primarily lower elevated blood triglyceride levels and have a moderate effect on LDL cholesterol and slightly increase HDL. The effects are due to activation of nuclear receptors PPAR (mainly PPARα). Indications Blood lipid disorders, especially hypertriglyceridemia. Agents Bezafibrate (Cedur retard) Fenofibrate (Lipanthyl) Fenofibric acid (Trilipix) Gemfibrozil (Gevilon) … Fibrate

Fenofibrate

Products Fenofibrate is commercially available in the form of capsules (lipanthyl). It has been approved in many countries since 1977. In 2014, a fixed combination with simvastatin was registered (Cholib); see Fenofibrate Simvastatin. Structure and properties Fenofibrate (C20H21ClO4, Mr = 360.8 g/mol) exists as a white crystalline powder that is practically insoluble in water. It … Fenofibrate

Fenofibric Acid

Products Fenofibric acid was approved in many countries in 2013 in sustained-release capsule form (Trilipix). The capsules are not commercially available. Structure and properties Fenofibric acid (C17H15ClO4, Mr = 318.8 g/mol) is present in the drug as the choline salt (choline fenofibrate), a white to yellow powder that is very soluble in water. Fenofibric acid … Fenofibric Acid