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Toxicology > Lecture 03 - Pharmacokinetics and Pharmacodynamics > Flashcards

Lecture 03 - Pharmacokinetics and Pharmacodynamics Flashcards

1
Q

What can drug metabolites do

A

contribute significantly to therapeutic affects or adverse side effects

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2
Q

What are xenobiotics

A

organic compound that are foreign to the body

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3
Q

What are most pharmacologically active molecules

A

lipophilic and remain non-ionized or only partially ionized at physiological pH

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4
Q

What is drug metabolism

A

the means of converting these molecules into substances that are more easily excreted

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5
Q

What is biotransformation

A

the enzymatic transformation of molecules by functionalization reactions and/or conjugation reactions into molecules that are polar and water soluble

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6
Q

What are phase I reactions

A

introduction, exposure or modification of a specific chemical groups via oxidation-reduction reactions

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7
Q

What are phase II reactions

A

conjugation of small endogenous molecules

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8
Q

What do water soluble compounds of Phase I reactions require

A

conjugation

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9
Q

What do we need to dissolve xenobiotics in urine for efficient elimination

A

increased hydrophilicity

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10
Q

How can metabolism backfire

A

metabolites might be toxic

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11
Q

What is an example of a drug with toxic metabolites

A

Acetaminophen and its metabolite NAPQI

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12
Q

What does NAPQI do

A

destroys liver cells

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13
Q

What is used to conjugate NAPQI

A

glutathione

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14
Q

Where are the major enzymes for biotransformation

A

cytosolic or are anchored in the membrane of the endoplasmic reticulum

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15
Q

What is the main enzyme system for oxidation

A

cytochrome P450 (CYP)

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16
Q

What are the properties of benzodiazepines

A

anxiolytic, sedative, and anticonvulsant

17
Q

How do secondary and tertiary amine tricyclics differ

A

their ability to block muscarinic, histaminergic and alpha-adrenergic receptors

18
Q

Why is it important to monitor tricyclic antidepressants

A

their hydroxy metabolites cause cardiotoxicity

19
Q

How do tertiary amines become secondary amines

A

demethylation

20
Q

What do the metabolites of SSRIs do

A

selectively inhibit the reuptake of serotonin (same effect as precursor)

21
Q

What are the CYP enzymes

A

heme-containing proteins that play a role in metabolizing

22
Q

How many known drugs/xenobiotics do the CYP enzymes metabolize

A

over 400

23
Q

What do we look for to indicate a redox reaction

A

Gain or lose elections, gain or lose oxygen, conversion between hydroxides aldehydes and carboxylic acids, movement of H+ between thiol functional groups, changes of the number of oxygens bound to a carbon atom

24
Q

What are the components of the CYP enzyme system

A

hemoprotein, flavoprotein, heat stable lipid component

25
Q

What is hemoprotein

A

iron protoporphyrin IX which contains a heme group

26
Q

What does hemoprotein do

A

serves as a substrate and oxygen binding site of the enzyme system in which the heme iron undergoes cyclic oxidation/reduction

27
Q

What is flavoprotein

A

acts as the electron carrier shuttling electrons from NADPH to the CYP substrate complex, binds the cofactor NADPH

28
Q

What is the heat stable lipid componenet

A

holds everything where its supposed to be positioned in space

29
Q

How many gene families of CYP have been described

A

74

30
Q

How many gene families exist in all mammals

A

18

31
Q

Which families play the greatest role with respect to drug metabolism

A

1, 2, and 3

32
Q

What compounds are CYP enzymes used to metabolise

A

steroids, bile acids, fatty acids, prostaglandins, leukotrienes, biogenic amines, retinoids, lipid hydroperoxides, phytoalexins, drugs, environmental chemicals, pollutants

33
Q

How similar are CYP proteins within a gene family

A

> 40% homologous

34
Q

How similar are CYP proteins within a subfamily

A

> 55% homologous

35
Q

What are the four categories that can effect drug metabolism

A
  1. diet and disease states
  2. genetics
  3. enzyme induction by exposure of CYP enzymes
  4. inhibition of CYP enzymes
36
Q

What do brassica vegetables do

A

increase CYP1A2 activity

37
Q

What do apiaceous vegetables do

A

decrease CYP1A2 activity

38
Q

What does grapefruit juice do

A

inhibits CYP3A4 activity

39
Q

What does aging do

A

associated with a slight decrease in redox reaction catalyzed by CYP enzymes

Toxicology (20 decks)

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