Phase 1 metabolism involves chemical reactions such as oxidation (most common), reduction and hydrolysis. There are three possible results of phase 1 metabolism. The drug becomes completely inactive. … One or more of the metabolites are pharmacologically active, but less so than the original drug.
What is the difference between Phase 1 and Phase 2 metabolism?
Phase I reactions of drug metabolism involve oxidation, reduction, or hydrolysis of the parent drug, resulting in its conversion to a more polar molecule. Phase II reactions involve conjugation by coupling the drug or its metabolites to another molecule, such as glucuronidation, acylation, sulfate, or glicine.
Where does phase 1 metabolism occur?
Although Phase I drug metabolism occurs in most tissues, the primary and first pass site of metabolism occurs during hepatic circulation. Additional metabolism occurs in gastrointestinal epithelial, renal, skin, and lung tissues.
What are the three phases of metabolism?
The metabolism of xenobiotics is often divided into three phases:- modification, conjugation, and excretion.
What happens in first pass metabolism?
The drug is absorbed from the GI tract and passes via the portal vein into the liver where some drugs are metabolised. Sometimes the result of first pass metabolism means that only a proportion of the drug reaches the circulation.
What are the two phases of drug metabolism?
Drug metabolism reactions comprise of two phases: Phase I (functionalization) reactions such as oxidation, hydrolysis; and Phase II (conjugation) reactions such as glucuronidation, sulphate conjugation. Oxidation reactions are the most common and vital.
Where does Phase 2 of drug metabolism occur?
Glucuronidation, the most common phase II reaction, is the only one that occurs in the liver microsomal enzyme system. Glucuronides are secreted in bile and eliminated in urine. Thus, conjugation makes most drugs more soluble and easily excreted by the kidneys.
Where does Phase 1 and 2 metabolism occur?
The liver is the primary site for metabolism. Liver contains the necessary enzymes for metabolism of drugs and other xenobiotics. These enzymes induce two metabolism pathways: Phase I (functionalization reactions) and Phase II (biosynthetic reactions) metabolism.
Is first pass metabolism the same as Phase 1?
Phase 1 reactions are often oxidations or hydrolysis reactions, although reductions also occur. In terms of first-pass metabolism in the liver – hydrolysis of pharmacologically inactive esters (prodrugs) to active drugs are important phase 1 reactions.
What are the two routes by which drugs can be eliminated into the system?
It is accomplished in two ways, either by excretion of an unmetabolized drug in its intact form or by metabolic biotransformation followed by excretion. While excretion is primarily carried out by the kidneys, other organ systems are involved as well.
What are the three main purpose of metabolism?
The three main purposes of metabolism are the conversion of food/fuel to energy to run cellular processes, the conversion of food/fuel to building blocks for proteins, lipids, nucleic acids, and some carbohydrates, and the elimination of nitrogenous wastes.
What is Glucuronidation metabolism?
Glucuronidation involves the metabolism of parent compound by UDP-glucuronosyltransferases (UGTs) into hydrophilic and negatively charged glucuronides that cannot exit the cell without the aid of efflux transporters.22 мая 2017 г.
What are the steps of metabolism?
In humans, the most important metabolic pathways are: glycolysis – glucose oxidation in order to obtain ATP. citric acid cycle (Krebs’ cycle) – acetyl-CoA oxidation in order to obtain GTP and valuable intermediates. oxidative phosphorylation – disposal of the electrons released by glycolysis and citric acid cycle.
How do I overcome my first pass metabolism?
Bypassing First Pass Metabolism
Two ways to bypass first pass metabolism involve giving the drug by sublingual and buccal routes. The drugs are absorbed by the oral mucosa in both methods. In sublingual administration the drug is put under the tongue where it dissolves in salivary secretions.
What is first pass metabolism of a drug?
The first pass effect is a phenomenon in which a drug gets metabolized at a specific location in the body that results in a reduced concentration of the active drug upon reaching its site of action or the systemic circulation.
Why is first pass metabolism important?
The liver metabolizes many drugs, sometimes to such an extent that only a small amount of active drug emerges from the liver to the rest of the circulatory system. This first pass through the liver thus may greatly reduce the bioavailability of the drug.