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Pharmacology I Exam #1 > Metabolism/Biotransformation > Flashcards

Metabolism/Biotransformation Flashcards

1
Q

What molecular weight means a drug will be excreted by the kidneys?

A

<350

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2
Q

What molecular weight means a drug will be excreted by the liver?

A

> 350

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3
Q

Where is Penicillin metabolized in the body?

A

Gastric juices

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4
Q

Where is Epinephrine metabolized in the body?

A

Intestinal wall

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5
Q

What occurs with a Phase I reaction?

A

Drug modification

Lipid-soluble, non-ionized parent compounds are converted to water-soluble, ionized compounds

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6
Q

What occurs with a Phase II reaction?

A

Conjugation

An ionized, charged particle is added to a Phase I metabolite to form an even more water-soluble, ionized compound

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7
Q

What type of CYP metabolizes more than 50% of drugs?

A

CYP3A4

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8
Q

What type of CYP has a high degree of polymorphisms?

A

CYP2D6

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9
Q

What type of CYP impairs Codeine metabolism (poor metabolism to Morphine, its active form)?

A

CYP2D6

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10
Q

What type of CYP is induced by ethanol?

A

CYP2E1

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11
Q

What are three examples of induction by CYP450 enzymes?

A
  • Carcinogens, chargrilled foods
  • Ethanol
  • Barbituates/Phenobarbitals
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12
Q

What are three examples of inhibition by CYP450 enzymes?

A
  • Grapefruit juice

- Fluoxetine (Prozac)

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13
Q

What are carcinogens and chargrilled foods an example of in relation to CYP450 enzymes? What specific enzyme is involved?

A

Induction of CYP450 enzymes

- CYP1A2

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14
Q

What is ethanol an example of in relation to CYP450 enzymes? What specific enzyme is involved?

A

Induction of CYP450 enzymes

- CYP2E1

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15
Q

What are Barbituates/Phenobarbitals an example of in relation to CYP450 enzymes?

A

Induction of CYP450 enzymes

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16
Q

What is grapefruit juice an example of in relation to CYP450 enzymes? What specific enzyme is involved? What does this act like?

A

Inhibition of CYP450 enzymes

  • CYP3A4
  • Acts like a non-competitive antagonist
17
Q

What is Fluoxetine (Prozac) an example of in relation to CYP450 enzymes? What specific enzyme is involved? What does this act like?

A

Inhibition of CYP450 enzymes

  • CYP2D6
  • Acts like a competitive antagonist
18
Q

What is an important characteristics of end products of Phase II reactions?

A

They are readily eliminated

19
Q

What is an exception to the Phase II enzymes being non-inducible (aka it is an inducible enzyme)?

A

UDP Glucuronyl Transferase

20
Q

What is an example of Phase II reaction occurring before Phase I reaction?

A

Isoniazid (INH)

21
Q

What are two examples of Phase I polymorphisms discussed in class?

A
  • CYP2D6: poor metabolism of codeine to morphine
  • Alcohol flush reaction (Asian glow): Aldehyde Dehydrogenase deficiency leads to acetaldehyde accumulation, which is toxic to the body
22
Q

What medication is often associated with a bimodal distribution, and what does this mean?

A

Isoniazid (INH)

- Slow and fast metabolizers

23
Q

What size dose is generally given to slow metabolizers and why?

A

Small dose is given to “slow” metabolizers because too much could be toxic due to slower drug metabolization

24
Q

How do plasma concentration levels appear graphically for a slow metabolizer?

A

Plasma concentrations will be higher because the drug is being metabolized slower

25
Q

How do metabolite concentration levels appear graphically for a slow metabolizer?

A

Metabolite concentration will be lower because the drug is being metabolized slower

26
Q

What happens to half-life of drugs involved with enterohepatic circulation? Why is this?

A

Half-life will increase in drugs with enterohepatic circulation
- This is due to more extensive cycling in the liver

27
Q

What are two factors influencing metabolism in young people?

A
  • Incomplete organ maturation (liver, kidneys)

- Undeveloped BBB

28
Q

What are two factors influencing metabolism in older people?

A
  • Decreased renal function FIRST

- Decreased liver function

29
Q

What step of ADME does kidney dysfunction influence?

A

Excretion/Elimination

30
Q

What step of ADME does liver dysfunction influence?

A

Metabolism

31
Q

What is an example of a medication with slow metabolism by the kidney

A

Diazepam

32
Q

What is an example of a medication with fast metabolism by the kidney

A

Penicillin

33
Q

How does a decreased cardiac output affect drug metabolism? Why is this?

A

Decreased cardiac output = Drug metabolism will decrease because flow to liver is limited

34
Q

How does a decreased cardiac output affect drug metabolism? Why is this?

A

Decreased cardiac output = Drug metabolism will decrease because flow to liver is limited

Pharmacology I Exam #1 (5 decks)

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