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Toxicokinetics II: Biotransformation of Toxicants

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36 Questions

What is the primary function of biotransformation in an organism?

To enhance the elimination and detoxification of chemicals

What is the result of Phase I metabolism in xenobiotic metabolism?

Increased excretability of metabolites

What is the primary location of biotransformation reactions within the cell?

Cytoplasm

What is the effect of storage on the body's ability to biotransform and eliminate toxicants?

It affects the body's ability to biotransform and eliminate toxicants

What is the term for the 'build-up' process of biochemical reactions in metabolism?

Anabolism

What is the primary purpose of Phase II metabolism in xenobiotic metabolism?

To increase the excretability of metabolites

What is the result of biotransformation on the fate of lipophilic compounds in the body?

They become more hydrophilic

What is the term for the process of converting chemicals to less toxic forms in biotransformation?

Detoxification

What is the primary route of elimination of hydrophilic metabolites in the body?

Kidneys

What is the primary goal of the detoxification process?

To convert toxicants into more water-soluble forms

What is the main site of biotransformation in the body?

Liver

What is the result of Phase I reactions in biotransformation?

Increase in hydrophilicity

What is the purpose of biotransformation in the body?

To terminate the biological activity of chemicals

What is the result of some chemicals being partially converted to more toxic products?

Increased toxicity of the parent substance

What is the role of cytochrome P450 in biotransformation?

To add or unmask reactive side groups

What is the primary mechanism for eliminating toxicants from the body?

Excretion through urine and feces

What is the result of Phase II reactions in biotransformation?

Conjugation of reactive side groups

What is the main organ responsible for the elimination of toxicants through excretion?

Kidney

What is the primary effect of the oxidation reaction in Phase I metabolism?

Addition of oxygen and removal of hydrogen

What is the role of the enzyme alcohol dehydrogenase in Phase I metabolism?

To catalyze oxidation reactions

What is the effect of CYP450 enzyme induction on the metabolism of toxicants?

It increases the bioactivation of toxicants

What is the primary function of the P450 system in Phase I metabolism?

To bioactivate non-toxic compounds

What is the role of glutathione in the metabolism of paracetamol?

To conjugate with the reactive metabolite NAPQI

What is the effect of a paracetamol overdose on the metabolism of NAPQI?

Conjugation with glutathione becomes saturated, leading to increased hepatocyte damage

What is the effect of CYP450 enzyme induction on the composition of P450 enzymes?

It causes a marked increase (>20-fold) in the composition of P450 enzymes

What is the role of esterases in Phase I metabolism?

To catalyze hydrolysis reactions

What is the effect of rifampin on the expression of CYP450 enzymes?

It induces the expression of CYP3A

What is the effect of induction on the therapeutic effect of drugs?

It decreases the therapeutic effect of drugs

What is the role of P450 in biotransformation?

It is a phase I reaction enzyme that can be induced by toxicants

What is the effect of conjugation reactions on molecular size and polarity?

It increases molecular size and polarity

What is the role of CYP2E1 in the metabolism of vinyl chloride?

It converts vinyl chloride to chloroethylene oxide

What is the effect of chronic low-level exposure to aflatoxins?

It increases the risk of liver cancer

How does oltipraz prevent AFB1 toxicity?

It inhibits CYP450 and induces GST

What is the result of biotransformation reactions?

It increases the polarity of compounds and decreases toxicity via metabolism of a toxic parent compound

What is the role of CYP3A4 in the metabolism of aflatoxin B1?

It bioactivates aflatoxin B1 to its epoxide form

What is the effect of induction on tolerance to toxicants?

It increases tolerance to some toxicants while enhancing the toxicity of others

This quiz covers the biotransformation of toxicants in the body, including the processes of anabolism and catabolism, and how storage affects the body's ability to eliminate toxic substances. It also explores how biotransformation has evolved to deal with metabolites and naturally occurring toxicants. Test your knowledge of this important topic in toxicology!

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