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

Amoxicillin (Amoxil)

Products Amoxicillin is commercially available in the form of tablets, film-coated tablets, dispersible tablets, as powder or granules for the preparation of a suspension, as an infusion and injection preparation, and as a veterinary drug. In addition to the original Clamoxyl, numerous generics are available today. Amoxicillin was launched in 1972 and has been approved … Amoxicillin (Amoxil)

ADME

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

Pharmacokinetic Booster

Definition and mechanisms A pharmacokinetic booster is an agent that improves the pharmacokinetic properties of another agent. It is a desirable drug interaction It can exert its effects at different levels (ADME): Absorption (uptake into the body). Distribution (distribution) Metabolism and first-pass metabolism (metabolization). Elimination (excretion) Pharmacokinetic enhancers can increase absorption, increase distribution to an … Pharmacokinetic Booster

Elimination

Introduction Elimination is a pharmacokinetic process that describes the irreversible removal of active pharmaceutical ingredients from the body. It is composed of biotransformation (metabolism) and excretion (elimination). The most important organs for excretion are the kidney and the liver. However, drugs can also be excreted through the respiratory tract, hair, saliva, milk, tears, and sweat. … Elimination

First-Pass Metabolism

The effect of the first liver passage For a perorally administered pharmaceutical agent to exert its effects at the site of action, it usually must enter the systemic circulation. To do so, it must pass through the intestinal wall, the liver, and part of the circulatory system. Despite complete absorption in the intestine, the bioavailability … First-Pass Metabolism

Metabolism (Biotransformation)

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)

Insulin Aspart

Products Insulin aspart is marketed as an injectable (NovoRapid, USA: NovoLog). It has been approved in many countries since 1999. The fixed combination IDegAsp (insulin aspart + insulin degludec, Ryzodeg) was registered in many countries and in the EU in 2013. In 2017, Fiasp ultra-fast-acting, a very fast-acting insulin aspart, was also approved. With the … Insulin Aspart

Interactions

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

Protein Binding

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

Turmeric

Products Turmeric is commercially available as a spice. Along with other parts of the plant, it is an important ingredient of curry powder. Products available in pharmacies and drugstores include turmeric powder, liquid preparations, capsules and tablets. The powder contains the active ingredient curcumin (see below). The orange-yellow dye is also used as an additive … Turmeric