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Principles of Disease > Drug Metabolism > Flashcards

Drug Metabolism Flashcards

1
Q

What 3 reactions does phase 1 metabolism involve (HOR)

A
  • Hydrolysis
  • Oxidation
  • Reduction
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2
Q

What 2 things does phase 1 do?

A
  • Increases the polarity

- Provides an active site for phase 2

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3
Q

What enzymes carry out phase 1 metabolism mainly?

A

Cytochrome P450’s

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4
Q

Where is CYP3A4 found in the body?

A

Liver

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5
Q

What 3 drugs does CYP3A4 metabolise?

A
  • Diazepam
  • Methadone
  • Simvastatin
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6
Q

What does CYP2D6 metabolise?

A
  • Antidepressants
  • Antipsychotics
  • Codeine
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7
Q

What does CYP2D6 do to codeine?

A

Converts it to morphine

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8
Q

What percentage of the population don’t express the gene for CYP2D6?

A

5-10%

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9
Q

What can induce the effects of CYP2D6 and CYP1A2?

A

Smoking

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10
Q

What does CYP1A2 metabolise?

A

Theophylline

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11
Q

What process does phase 2 metabolism involve?

A

Conjugation

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12
Q

What does conjugation involve?

A

Attachment of something to the compound

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13
Q

What 4 compounds can be attached during conjugation

A
  • Glucaronic acid
  • Gluthianone
  • Sulphate
  • Acetate
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14
Q

What are the 4 compounds in conjugation (phase 2) attached to?

A

The metabolite from phase 1

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15
Q

What does conjugation do to a drug (referring to activity)

A

Inactivates most drugs, some may stay active

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16
Q

What 7 factors may inhibit or induce drug metabolism?

A
  • Other drugs/substances
  • Genetics
  • Hepatic blood flow
  • Liver disease
  • Age
  • Sex
  • Ethnicity
17
Q

How does enzyme induction affect drug metabolism?

A
  • Drug metabolic enzymes can be induced by other substances

- This decreases the drugs efficacy

18
Q

What common inducers of enzymes are there that will reduce a drugs efficacy?

A
  • Smoking

- Alcohol

19
Q

What common drugs are there that will cause enzyme induction?

A
  • Phenytoin

- Carbamazepine

20
Q

What is a drug that can cause enzyme inhibition?

A
  • Erythromycin
  • Cimetidine
  • Clarithromycin
21
Q

How do genetic mutations result in reduces/induced drug metabolism?

A
  • May alter coding genes which can lead to absences/deficiencies of an enzyme
22
Q

What can genetic mutations in the enzymes gene result in when a drug is taken?

A

Toxicity

23
Q

What is a result of difference in individual gene expression

A

Different forms of metabolising enzymes

24
Q

What can enhanced expression lead to?

A
  • Increased metabolism

- Reduced efficacy

25
Q

Why are premature infants unable to metabolise some drugs?

A
  • They lack the metabolising enzymes

- Renal function deficient which leads to toxicity

26
Q

How can race affect metabolism?

A
  • Many differences between races

- Some have different P450 genes

Principles of Disease (35 decks)

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