Most drugs must pass through the liver, which is the primary site for drug metabolism. Once in the liver, enzymes convert prodrugs to active metabolites or convert active drugs to inactive forms. The liver’s primary mechanism for metabolizing drugs is via a specific group of cytochrome P-450 enzymes.
Where does the majority of drug metabolism occur?
Drug metabolism is the term used to describe the biotransformation of pharmaceutical substances in the body so that they can be eliminated more easily. The majority of metabolic processes that involve drugs occur in the liver, as the enzymes that facilitate the reactions are concentrated there.
Where is the primary site of drug metabolism?
Excretion involves elimination of the drug from the body, for example, in the urine or bile. Most drugs must pass through the liver, which is the primary site for drug metabolism.
How are drugs metabolised in the body?
Drugs can be metabolized by oxidation, reduction, hydrolysis, hydration, conjugation, condensation, or isomerization; whatever the process, the goal is to make the drug easier to excrete. The enzymes involved in metabolism are present in many tissues but generally are more concentrated in the liver.
Where does phase 2 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.
What are the factors that affect drug metabolism?
Many factors affect the rate and pathway of metabolism of drugs, and the major influences can be sub-divided into internal (physiological and pathological) and external (exogenous) factors as indicated below: Internal: species, genetic (strain), sex, age, hormones, pregnancy, disease. External: diet, environment.
What is metabolism activity?
Metabolism is a balancing act involving two kinds of activities that go on at the same time: building up body tissues and energy stores (called anabolism) breaking down body tissues and energy stores to get more fuel for body functions (called catabolism)
What are the 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.
Does exercise speed up drug metabolism?
Exercise reduces the blood flow in the liver and deactivation of drugs with flow-limited (high clearance) hepatic metabolism such as nitrates and lidocaine. Metabolism of capacity-limited (low clearance) drugs, e.g. antipyrine, diazepam and amobarbital, is not influenced by exercise.
What is Phase 2 drug 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.
What organs are involved in drug metabolism?
Most drugs must pass through the liver, which is the primary site for drug metabolism. Once in the liver, enzymes convert prodrugs to active metabolites or convert active drugs to inactive forms.
How does age affect metabolism of a drug?
Thus, age-related changes in drug metabolism should be considered a typical phenotypic characteristic of the aging process. Generally, older age is associated with increased blood concentrations of drugs and altered metabolism, reduced effectiveness, and increased risk of adverse reactions for many medications (2).
What is meant by drug?
A drug is any substance (with the exception of food and water) which, when taken into the body, alters the body’s function either physically and/or psychologically. Drugs may be legal (e.g. alcohol, caffeine and tobacco) or illegal (e.g. cannabis, ecstasy, cocaine and heroin).
Where does Phase 1 and 2 metabolism occur?
Where does metabolism occur in the body? 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.
What are the two phases of metabolism?
Metabolism is often divided into two phases of biochemical reaction – phase 1 and phase 2. Some drugs may undergo just phase 1 or just phase 2 metabolism, but more often, the drug will undergo phase 1 and then phase 2 sequentially.
What is oxidation in metabolism?
Listen to pronunciation. (OK-sih-DAY-tiv meh-TA-buh-lih-zum) A chemical process in which oxygen is used to make energy from carbohydrates (sugars). Also called aerobic metabolism, aerobic respiration, and cell respiration.