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Summer Course II > Pharmacogenetics > Flashcards

Pharmacogenetics Flashcards

1
Q

How many % of drugs prove effective in treatment?

A

25-60%

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2
Q

How can pharmacogenetics impact the treatment efficacy of certain drugs?

A

By influencing the metabolism of these drugs, influencing exposure to these drugs

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3
Q

How many % of all hospitalizations is due to adverse drug reactions?

A

5-7%

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4
Q

Which immune system is the most important in the imaging of drugs? How many % of drugs are metabolized by this system?

A

Cytochrome p450, 80% of drugs

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5
Q

What are the three most important cytochrome p450 enzymes? How many % of drugs to they metabolize?

A
  1. CYP3A4 -> 30-40%
  2. CYP2D6 -> 20%
  3. CYP2C9 -> 16%
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6
Q

Which classes of drugs get metabolized by CYP3A4? (4)

A
  1. Oncology drugs
  2. Psychiatry drugs
  3. Cyclosporin
  4. Tacrolimus
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7
Q

Which classes of drugs get metabolized by CYP2D6? (4)

A
  1. Antidepressants
  2. Antipsychotics
  3. Betablockers
  4. Tamoxifen
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8
Q

Which classes of drugs get metabolized by CYP2C9?

A
  1. Warfarin
  2. Acenocoumarin
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9
Q

What is efavirenz?

A

Anti-HIV drug

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10
Q

Which enzyme metabolizes efavirenz?

A

CYP2B6

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11
Q

What influences the metabolism of efavirenz?

A

Polymorphisms in CYP2B6, especially at position 516

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12
Q

How does drug metabolism influence efavirenz dosing for normal, intermediate & poor metabolizers?

A

Normal: 600 mg/day
Intermediate: 400 mg/dag
Poor: 200-400 mg/day

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13
Q

What are phase I enzymes?

A

Oxygenases, performing the first step in modification of many compounds

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14
Q

Which three groups of phase I enzymes are known?

A
  1. Cytochrome p450
  2. Flavin-containing monooxygenases
  3. Epoxide hydrolases
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15
Q

What are phase II enzymes?

A

Transferases, modifying compounds after modification by phase I enzymes

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16
Q

Which groups of phase II enzymes are known? (5)

A
  1. Sulfotransferases (SULT)
  2. UDP-glucuronosyltransferases (UGT)
  3. Glutathione-S-transferases (GST)
  4. N-acetyltransferases (NAT)
  5. Methyltransferases (MT)
17
Q

What is the mechanism of action of sulfotransferases?

A

Addition of a sulphate group

18
Q

What is the mechanism of action of UDP-glucuronosyltransferases?

A

Addition of glucuronic acid

19
Q

What is the mechanism of action of glutathione-S-transferases?

A

Addition of glutathione

20
Q

What is the mechanism of action of N-acetyltransferases?

A

Addition of an acetyl group

21
Q

What is the mechanism of action of methyltransferases?

A

Addition of a methyl group

22
Q

Which three groups of enzymes are involved in drug metabolism in addition to the classical phase I/phase II enzymes?

A
  1. Alcohol dehydrogenases
  2. Aldehyde dehydrogenases
  3. NADP-quinone oxireductase (NQO)
23
Q

Which phase II enzyme is important for the metabolism of mycophenolate mofetil?

A

UGT1A9

24
Q

What is the range of mycophenolate mofetil concentration that UGT1A9 mutations can cause?

A

13-fold range

25
Q

What is the effect of above-target mycophenolate mofetil concentrations in the body?

A

No severe adverse effects

26
Q

What is the effect of below-target mycophenolate mofetil concentrations in the body?

A

Increased risk of organ rejection
Below-target MMF exposure is a storng predictor or organ rejection

27
Q

What are the steps of mycophenolate mofetil (MMF) metabolism?

A
  1. MMF converted into active form MPA and then into inactive MPAG by UGT1A9
  2. MPAG is excreted via urine and bile
  3. MPAG can be reactivated by colon flora and taken up, increasing concentration
28
Q

Which transporter is important for the excretion of MPAG via the bile?

A

ABCC2

29
Q

What kind of mutations influence UGT1A9 activity and thereby mycophenolate mofetil concentrations? How many % of the population carries such a mutation?

A

Promotor polymorphisms, found in 12% of the population

30
Q

What is abacavir? What is its drawback?

A

Antiretroviral therapy with favourable long-term toxicity profile
4-8% of patients suffer severe hypersensitivity reactions

31
Q

What causes hypersensitivity reactions to abacavir?

A

Presentation of abacavir to the immune system by HLA-B*57:01

32
Q

How can hypersensitivity reactions to abacavir be prevented?

A

Genotyping patients for HLA-B*57:01 before initiating treatment

33
Q

Which HLA-type is associated with toxic epidermal necrolsyis when using carbamazepine?

A

HLA-B*15:02

34
Q

Which HLA-type is associated with toxic reactions to allopurinol?

A

HLA-B*58:01

Summer Course II (4 decks)

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