Polymorphisms and toxic metabolites Flashcards

1
Q

Which of the CYPS is most represented?

A

CYP2

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2
Q

What three categories define metabolic activity?

A
  • Extensive metaboliser
  • Poor metaboliser
  • Ultra rapid metaboliser
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3
Q

Grape fruit juice is a potent CYP3A4 inhibitor. TRUE OR FALSE?

A

TRUE

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4
Q

Which one of the CYPs is unique?

A

CYP2E1

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5
Q

What do CYP2E1 produce?

A

Reactive oxygen radicals through reduction of oxygen

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6
Q

Ethanol strongly induces the production of reactive oxygen radicals via reduction of oxygen. TRUE OR FALSE?

A

TRUE

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7
Q

Where is CYP2E1 located?

A

Located in the ER

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8
Q

CYP2E1 primarily located in the rows of 5 cells around the central venules of a liver lobule. TRUE OR FALSE?

A

TRUE

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9
Q

Name two substrate that can inhibit and induce?

A

Ethanol and Acetone

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10
Q

Name two substrate that inhibit but does not induce?

A

Paracetamol and carbon tetrachloride

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11
Q

Name an inducer that is not a substrate?

A

Imidazole

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12
Q

CYP2E1 is increased in diabetes, obesity and other nutritional states that produce acetone. TRUE OR FALSE?

A

TRUE

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13
Q

Action of alcohol dehydrogenase and aldehyde dehydrogenase leads to accumulation of NADH. TRUE or FALSE?

A

TRUE

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14
Q

CYP pathway generates free radicals, consumes NADPH and depletes glutathione levels. TRUE OR FALSE?

A

TRUE

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15
Q

NADH does not lead to release of ketone bodies and high levels of actetaldehyde, resulting in liver damage and death. TRUE OR FALSE?

A

FALSE

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16
Q

What toxic metabolite is produced when paracetamol is metabolised?

A

NAPQI

17
Q

During Glutathione conjugation the conjugates are less toxic than the parent compound. TRUE OR FALSE?

A

TRUE

18
Q

The conjugates of glutathione conjugation are excreted in bile or via the kidney. TRUE OR FALSE?

A

TRUE

19
Q

How is paracetamol toxicity metabolised?

A

-Sulfation or glucuronidation

20
Q

NAQPI is an electrophile and will react with nucleophilic centres. TRUE OR FALSE?

A

TRUE

21
Q

Glutathione a sacrificial nucleophile protects cellular SH groups. TRUE OR FALSE?

A

TRUE

22
Q

Ethanol is not a CYP2E1 substrate so does not compete with other substrates before CYP2E1 is induced. TRUE OR FALSE?

A

TRUE

23
Q

CYP2E1 metabolism of paracetamol is reduced when drug is administered alongside ethanol. TRUE OR FALSE?

A

TRUE

24
Q

Name an antidote for paracetamol toxicity?

A

Methionine