Pharmacodynamics and pharmacokinetics. When we take a tablet, we are usually interested in its immediate effects. The drug is supposed to relieve a headache or reduce symptoms of a cold. At the same time, we may think about the possible side effects it may trigger. The desired and undesired effects that a drug exerts on … ADME
Elimination at the kidney The kidneys, along with the liver, play a central role in the elimination of pharmaceutical agents. They can be filtered at the glomerulus of the nephron, actively secreted at the proximal tubule, and reabsorbed at various tubular segments. In renal insufficiency, these processes are impaired. This may result in a renally … Dose Adjustment in Renal Insufficiency
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 and properties When active pharmaceutical ingredients enter the bloodstream, they often bind to proteins, especially albumin, to a greater or lesser extent. This phenomenon is called protein binding, and it is reversible: drug + protein ⇌ drug-protein complex Protein binding is important, first, because only the free portion distributes to tissues and induces a … Protein Binding
Products Human albumin is commercially available as an infusion solution for intravenous use. Structure and properties Human albumin is a monomeric protein with a heart-shaped structure that can be extracted from human plasma for the production of drugs. In the body, it is produced by the liver. The mature protein consists of 585 amino acids, … Albumin: Protein in the Blood
Definition Distribution (distribution) is a pharmacokinetic process that begins immediately after absorption of the drug from the intestine. During this process, the drug enters the bloodstream and travels to organs, body fluids, and tissues. Distribution is necessary for the drug to reach its drug target at a sufficient concentration. For example, an antidepressant must be … Distribution
Definition and examples When a drug is administered, for example, a tablet is swallowed or an injection is injected into a vein, the active pharmaceutical ingredients subsequently spread throughout the body. This process is called distribution. Active ingredients distribute throughout the bloodstream, into tissues, and are eliminated through metabolism and excretion. Mathematically, the volume of … Volume of Distribution
Products Raloxifene is commercially available in the form of film-coated tablets (Evista). It has been approved in many countries since 2000. Structure and properties Raloxifene (C28H27NO4S, Mr = 473.6 g/mol) is present in the drug as raloxifene hydrochloride, a benzothiophene and white to yellowish powder that is sparingly soluble in water. Effects Raloxifene (ATC G03XC01) … Raloxifene
