Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Intro to Pharmacology > Pharmacokinetics - Metabolism - Phase 2 > Flashcards

Pharmacokinetics - Metabolism - Phase 2 Flashcards

1
Q

Cytochorme p450:

  • contain a _____ (__) group
  • absorb light at ____ nm
  • _____ CYPs: ________ distribution of ________
A

heme (Fe)
450
many - polymorphic distribution of activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

In phase 2 metabolism, all the parts added to drugs are supplied by ______ and are added to the drugs by _________.

A

co-enzymes

transferases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Glucuronic acid conjugation:

  • Drugs carrying a ______ group or a ________ group (less so)
  • Enzymes called _______ ______ ________
  • co-enzymes called ______
A

hydroxyl, carboxyl (less so)
glucoronic acid transferases
UDPGA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Describe a drug that would go through glucoronic acid conjugation directly.

A

Drugs that come into the body with an exposed Hydroxyl (OH) group can undergo this.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Glucoronic acid transferase is a major enzyme in the _____.

A

liver

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is the purpose of drug metabolism?

A

To make the drug more polar/hydrophilic meaning that when it reaches the kidney, it will filter out and get excreted from the body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Tylenol can directly go through glucoronic acid conjugation. Why?

A

Because it enters the body with an already exposed OH group.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Sulfate conjugation (sulfation)

  • Drugs carrying a _____ group or a _______ group
  • enzymes called _____________
  • co-enzyme called ____
A

hydroxyl, carboxyl
sulfotransferases
PAPS

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Sulfotransferases are the major enzymes for phase 2 metabolism in ______. Describe why.

A

Children.
This is because the liver is not fully developed in kids so, this enzyme is more active than the glucoronic acid transferase.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

PAPS is related to what metabolite?

A

AMP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

When tylenol is given to children, what enzyme of phase 2 does it go through?

A

Sulfotransferases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Glutathione conjugation:

  • drugs carrying _____ reactive group that could form a _______ _______
  • enzymes called _______ _-_______
  • coenzyme called ________
A

highly reactive group that could form a reactive radical

glutathione s-transferase

Glutathione

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

glutathione tends to be a ______ agent.

A

reducing

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Conjugation of glutathione occurs where?

A

at the thiol group

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

After glutathione conjugation, what occurs?

A

Drug gets further hydrolyzed to a mercapturic acid conjugate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Acetylation:

  • Drugs carrying a ______ _____
  • enzymes called ______-__________
  • co-enzyme called _____ ____
A

primary amine
acetyl-transferases
Acetyl-CoA

17
Q

When the acetyl group is added to a primary amine, what is formed?

A

Amide

18
Q

Methylation:

  • drugs carrying a ______ ______, ______ or _______
  • enzymes called _______-__________
  • co-enzyme called _-____________
A
  • primary amine, hydroxyl, thiol
  • methyl-transferases
  • S-adenosylmethionine
19
Q

The coenzyme of methylation is also called?

A

SAM

20
Q

What is an example drug that can directly go through methylation?

A

Epinephrine

21
Q

What is peculiar of methylation?

A

It actually reduces polarity

22
Q

What is tylenol?

A

Acetominophen, an over the counter NSAID

23
Q

Tylenol:

  • toxic dose is _______
  • in adults, single doses above ___ grams or ____ mg/kg have a reasonable likelihood of causing _______
  • in adults, single dose of more than __ grams or ____ mg/kg have a high risk of _______
A

variable

  • 10, 140, toxicity
  • 25, 350, lethality
24
Q

What is the antidote to acetominophen overdose?

A

NAC - N-acetylcysteine

25
Q

Describe NAC

A

NAC is rapidly metabolized to intracellular glutathione which acts as a powerful antioxidant in the body

26
Q

When is NAC most effective regarding tylenol overdose?

A

Most effective when given within 8 hours of ingesting acetominophen - to prevent liver damage

27
Q

Why is NAC given rather than glutathione?

A

If a person takes glutathione, acid will cleave off the peptide bond and will not work as an antioxidant

28
Q

Describe the purpose of drug metabolism.

A

Phase 1 and 2 drug metabolism tend to increase polarity and water solubility of the drug to increase ease of excretion

29
Q

What are the different outcomes of drug metabolism?

A

Deactivation
Trans-activation
Activation
Toxification

30
Q

Describe deactivation

A

Metabolites less active then parental molecules, or inactive

31
Q

Describe trans-activation.

A

metabolites are as active after biotransformation

32
Q

Describe Activation

example?

A

pro-drugs become active metabolites and are responsible for toxicity
ex: morphine

33
Q

Describe toxification

Example?

A

Metabolites become toxic

ex: tylenol

Intro to Pharmacology (23 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions