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

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

Repaglinide

Products Repaglinide is commercially available in tablet form (NovoNorm, generic). It was approved in many countries in 1999. Structure and properties Repaglinide (C27H36N2O4, Mr = 452.6 g/mol) is a meglitinide and carbamoylmethylbenzoic acid derivative without sulfonylurea structure. It is a white, odorless powder that is practically insoluble in water due to its lipophilicity. In drugs, … Repaglinide

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

Rosuvastatin

Products Rosuvastatin is commercially available in the form of film-coated tablets (Crestor, generic, auto-generic). It was approved in many countries in 2006 (Netherlands: 2002, EU and US: 2003). The marketing authorization holder is AstraZeneca. The statin was originally developed at Shionogi in Japan. In the USA, generic versions came on the market in 2016. In … Rosuvastatin

Rosiglitazone

Products Rosiglitazone was commercially available in tablet form (Avandia). It had been approved since 1999 and was also commercially available in fixed combination with the biguanide metformin (Avandamet). The combination with the sulfonylurea glimepiride (Avaglim, EU, off-label) was not approved in many countries. A publication in on possible cardiovascular risks led to a controversy about … Rosiglitazone

Cerivastatin

Products Cerivastatin was commercially available in the form of film-coated tablets (Lipobay, Baycol). Because of rare possible adverse effects, it was withdrawn from the market in August 2001 (see below). Structure and properties Cerivastatin (C26H34FNO5, Mr = 459.6 g/mol) is a pyridine derivative and is present in drugs as cerivastatin sodium. Unlike other statins, it … Cerivastatin

Pioglitazone

Products Pioglitazone is commercially available in tablet form (Actos, generics). It is also available as a fixed-dose combination with metformin (Competact). Pioglitazone has been approved in many countries since 2000. Structure and properties Pioglitazone (C19H20N2O3S, Mr = 356.4 g/mol) belongs to the thiazolidinediones. It is present in drugs as a racemate and as pioglitazone hydrochloride, … Pioglitazone

Meulengracht’s Disease

Background The human organism has several mechanisms to metabolize endogenous and foreign substances. One of these mechanisms is glucuronidation, which occurs primarily in the liver. In this process, enzymes from the superfamily of UDP-glucuronosyltransferases (UGT) transfer a molecule of glucuronic acid from UDP-glucuronic acid to the substrate. Using acetaminophen as an example, alcohols, phenols, carboxylic … Meulengracht’s Disease

Simvastatin: Drug Effects, Side Effects, Dosage and Uses

Products Simvastatin is commercially available in the form of film-coated tablets (Zocor, generics). It is also combined fixed with ezetimibe (Inegy, generic). Simvastatin has been approved in many countries since 1990. Structure and properties Simvastatin (C25H38O5, Mr = 418.6 g/mol) exists as a white crystalline powder that is practically insoluble in water. It is a … Simvastatin: Drug Effects, Side Effects, Dosage and Uses

Gemfibrozil: Effects, Uses & Risks

Gemfibrozil is a medical agent that belongs to the so-called fibrates. As such, gemfibrozil is administered to treat diseases as well as disorders of lipid metabolism. It can also be taken for dietary purposes. Through this, weight loss can be achieved. What is gemfibrozil? Gemfibrozil is an orally taken fibrate. The term fibrate covers various … Gemfibrozil: Effects, Uses & Risks