Individual drug metabolism rates are influenced by genetic factors, coexisting disorders (particularly chronic liver disorders and advanced heart failure), and drug interactions (especially those involving induction or inhibition of metabolism).
What are three things that can 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 does altering drug metabolism mean?
Drug metabolism is the chemical alteration of a drug by the body. (See also Introduction to Administration and Kinetics of Drugs.) Some drugs are chemically altered by the body (metabolized).
What are the two major goals of drug metabolism?
The purpose of metabolism in the body is usually to change the chemical structure of the substance, to increase the ease with which it can be excreted from the body. Drugs are metabolized through various reactions including: Oxidation. Reduction.
How can I increase my drug metabolism?
The common approaches in drug metabolism to improve PK/PD and safety of drug candidates include blocking a metabolic soft spot to lower total clearance, deuterium replacement to alter metabolism of a lead, prodrug for improved absorption and distribution, minimizing DDI and bioactivation potential, and selection of …
Which factor is most important for drug metabolism?
The cytochrome P450 (CYP) is considered to be the most influential enzyme in the drug metabolism, which led to the development of many models such as QSAR for the prediction of the metabolism of molecules by the CYP enzyme.
How does liver disease affect drug metabolism?
Cirrhosis causes changes in the architecture of the liver leading to changes in blood flow, protein binding, and drug metabolizing enzymes. Drug metabolizing enzymes are primarily decreased due to loss of liver tissue. However, not all enzyme activities are reduced and some are only altered in specific cases.
What are the consequences of drug metabolism?
In general, the metabolism of a drug decreases its therapeutic effect. The majority of drugs are metabolized to increase their water solubility to allow elimination in urine or bile. However some drugs are metabolized into active compounds first before subsequent metabolism to inactive compounds and be excreted.
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.
What is metabolism and what factors affect it?
The amount of kilojoules your body burns at any given time is affected by your metabolism. Your metabolic rate is influenced by many factors – including age, gender, muscle-to-fat ratio, amount of physical activity and hormone function.
What is oxidation in metabolism?
Metabolic energy derives from processes of oxidation and reduction. When energy is consumed in a process, chemical energy is made available for synthesis of ATP as one atom gives up electrons (becomes oxidized) and another atom accepts electrons (becomes reduced).
What are the 2 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 factors can affect drug metabolism in an elderly?
Aging results in a number of significant changes in the human liver including reductions in liver blood flow, size, drug-metabolizing enzyme content, and pseudocapillarization. Drug metabolism is also influenced by comorbid disease, frailty, concomitant medicines, and (epi)genetics.
Which drug increases the metabolism of Bishydroxycoumarin?
Chronic treatment of experimental animals with phenobarbital resulted in accelerated metabolism of a variety of drugs such as bishydroxycoumarin, diphenylhydantoin, and antipyrine.
Why do I metabolize drugs so slow?
Because of their genetic makeup, some people process (metabolize) drugs slowly. As a result, a drug may accumulate in the body, causing toxicity. Other people metabolize drugs so quickly that after they take a usual dose, drug levels in the blood never become high enough for the drug to be effective.
What is Glucuronidation metabolism?
n. a metabolic process by which drugs or other substances are combined with glucuronic acid to form more water-soluble compounds, which are more readily excreted by the kidneys or in bile. Glucuronidation is the most prevalent of the Phase II reactions of drug metabolism. ADVERTISEMENT.