Enterohepatic Circulation

Definition Pharmaceutical agents are excreted primarily in the urine and, via the liver, in the bile in the stool. When excreted via the bile, they re-enter the small intestine, where they may be reabsorbed. They are transported back to the liver via the portal vein. This repetitive process is called the enterohepatic circulation. It prolongs … Enterohepatic Circulation

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

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

Combination Products

Definition Drugs today usually contain a defined active pharmaceutical ingredient. However, numerous drugs with two or more active substances also exist. These are called combination drugs or fixed combinations. For example, Aspirin C contains both acetylsalicylic acid and vitamin C. Many blood pressure medications are combination preparations, for example perindopril + indapamide or candesartan + … Combination Products

Bempedoic Acid

Products Bempedoic acid was approved in the EU, the United States, and many countries in 2020 in the form of film-coated tablets (Nilemdo). The active ingredient is also combined fixed with ezetimibe (Nustendi film-coated tablets). Structure and properties Bempedoic acid (C19H36O5, Mr = 344.5 g/mol) exists as a white crystalline powder that is practically insoluble … Bempedoic Acid

Glucuronidation

Definition Glucuronidation refers to an intracellular metabolic reaction in which an endogenous or exogenous substrate is conjugated to glucuronic acid. The organism thereby makes the substrates more water soluble so that they can be rapidly excreted in the urine. Glucuronidation belongs to phase II metabolism (conjugations). UDP: uridine diphosphate UGT: UDP-glucuronosyltransferase Enzymes involved Glucuronidation is … Glucuronidation

Atorvastatin

Products Atorvastatin is commercially available in the form of film-coated tablets (Sortis, generic, auto-generic). It has been approved in many countries since 1997. Atorvastatin is also available as a fixed combination with ezetimibe; see Atorvastatin and Ezetimibe. Structure and Properties Atorvastatin (C33H35FN2O5, Mr = 558.64 g/mol) is present in drugs as atorvastatin calcium trihydrate, (atorvastatin)2– … Atorvastatin

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