CYP450 Cytochromes P450s are a family of enzymes that are of paramount importance in drug biotransformation. The most important isoenzymes for drug metabolism are: CYP1A1, CYP1A2 CYP2B6 CYP2C9, CYP2C19 CYP2D6 CYP2E1 CYP3A4, CYP3A5 and CYP3A7 The number after the abbreviation CYP stands for the family, the following letter for the subfamily and the last number … Cytochrome P450 (CYP)
Introduction Biotransformation is an endogenous pharmacokinetic process that leads to a change in the chemical structure of active pharmaceutical ingredients. The organism’s general goal in doing so is to make the foreign substances more hydrophilic and to direct them to excretion via the urine or stool. Otherwise, they could be deposited in the body and … Metabolism (Biotransformation)
Definition When two or more drugs are combined, they may affect each other. This is especially true with regard to their pharmacokinetics (ADME) and effects and adverse effects (pharmacodynamics). This phenomenon is called interaction and drug-drug interaction. Interactions are usually undesirable because they can lead to, for example, loss of efficacy, side effects, poisoning, hospitalization, … Interactions
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
Products Topiramate is commercially available in tablet and capsule form (Topamax, generic). It has been approved in many countries and in the United States since 1996. Structure and properties Topiramate (C12H21NO8S, Mr = 339.36 g/mol) lies as a white powder with a bitter taste that is soluble in water. It is a sulfamate-substituted monosaccharide. Effects … Topiramate
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
Products Lamotrigine is commercially available as tablets and dispersible or chewable tablets (Lamictal, generics). It has been approved in many countries since 1994. Vanillin is typically added to the tablets as a flavoring agent and saccharin as a sweetener. Structure and properties Lamotrigine (C9H7Cl2N5, Mr = 256.1 g/mol) is a chlorinated phenyltriazine derivative that was … Lamotrigine (Lamictal)
Products Oxymorphone is commercially available in the United States as tablets and sustained-release tablets and has also been administered parenterally and rectally. It is not registered in many countries. Oxymorphone has been approved in the U.S. since 1959 (brand names: Numorphan, Opana, Opana ER, generics). It is a narcotic drug. Due to the potential for … Oxymorphone
