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Biochemistry III > Biotransformations > Flashcards

Biotransformations Flashcards

1
Q

What gives a substrate a better chance for excretion?

A

the formation of a more polar metabolite

goal is to go from lipid soluble → water soluble

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2
Q

What is the cytochrome P450 system composed of?

A

flavoprotein

lipid (membrane- SER)

hemoprotein

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3
Q

Flavoprotein

A

NADPH - P450 oxidoreductase

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4
Q

Lipid

A

phosphatidyl choline

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5
Q

Hemoprotein

A

cytochrome b5

cytochrome P450

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6
Q

What is the reductase- P450 ratio?

A

1:10 → 1:100

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7
Q

How many cytochrome P450 gene families are there in mammals?

A

8

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8
Q

How many cytochrome P450 gene families are there in drug metabolism? What are they?

A

4

CYP1, CYP2, CYP3, CYP4

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9
Q

Where is the cytochrome P450 gene family expressed?

A

liver, lungs, intestines, skin and kidney

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10
Q

What is the flavoprotein function in the P450 system?

A

to reduce the system with NADPH

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11
Q

What is induction dependent on?

A

ability of intracellular receptors

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12
Q

How many genes are present of CYP 1?

A

2

with 100 fold inducibility

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13
Q

What are the inducers of CYP1?

A
  1. metilcholantrene
  2. dioxin derivatives
    • ​​industrial technologies
    • environmental pollution
  3. Cigarette smoke
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14
Q

What can be a consequence of inducibility of CYP 1 ?

A

incidence of bronchial carcinoma

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15
Q

What are the substrates of CYP 1?

A
  1. Policyclic aromatic hydrocarbons (PAH)
    • benzpyrene, benzanthracene
  2. Medicines
    • teophyllin, caffeine, phacetin
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16
Q

What is TEXB? for CYP 1

A

total effective xenogenic burden

endocrine disrupters

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17
Q

What is the intracellular receptor/transcription factor responsible for induction?

A

Ah

(aryl hydrocarbon receptor)

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18
Q

What are the inducers of CYP2?

A

phenobarbital

ethanol

acetone

diazepam derivatives

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19
Q

What is the intracellular receptor/ transcription factor responsible for induction of CYP 2?

A

CAR

phenobarbital

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20
Q

CYP 2A

A

steroids

testosterone

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21
Q

CYP 2B

A

progesterone

D3 vitamin

antiepileptics

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22
Q

CYP 2C

A

mephenytoin - antiepileptics

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23
Q

CYP 2D

A

antidepressants

beta blockers

antihypertensive agents

24
Q

CYP 2E

A

ethanol, acetone

  • diabetes meelitus, starvation
25
Q

What are the inducers of CYP 3?

A

steroids

  • oral contraceptives
  • PCN- pregnenolon carbonitril
26
Q

What are the substrates of CYP 3?

A

antibiotics

nifedipin

cyclosporin

27
Q

What are the endocrine disrupters for CYP3?

A

total effective xenosestrogenic burden

TEXB

28
Q

What are the inducers of CYP 4?

A

clofibrate -antihyperlipemic agent

29
Q

What are the substrates of CYP 4?

A

fatty acids

eicosanoids

30
Q

What are the substrates of CYP 4?

A

fatty acids

eicosanoids

31
Q

What is the intracellular receptor/ transcription factor responsible for induction of CYP 4 ​?

A

PPAR

32
Q

What are the nuclear receptors in regulation of drug metabolism ?

A

CAR

LXR

PXR

PPARαβγ

33
Q

CAR

A

androstanes

phenobarbital

34
Q

LXR

A

oxysterols

35
Q

PXR

A

pregnanes

36
Q

PPARαβγ

A

fatty acids

eicosanoids

37
Q

What is a “gene battery” ?

A

biotransformation phase I, II enzymes

ABC transporters phase III + metabolic regulations

38
Q

What are the possible processes of conjugation?

A
  1. glucuronidation
  2. sulfation
  3. GSH conjugation
  4. Acetylation
  5. Amino acid conjugation
  6. Methylation
39
Q

What are frequent UGT substrates?

A

I. gene family isoenzymes: fenols,bilirubin

II. gene family isoenzymes: steroids, bile acids

40
Q

What is the activation of the UGT substrates?

A

morphine, steroids, bile acids, retinoids, polycyclic aryl hydrocarbones, heterocycle aryl amines

41
Q

What is the rold of UGT-s in activation of drugs?

A
  • morphin
  • steroids
  • bile acids
  • retinoids

→polycyclic aromatic hydrocarbons

→heterocyclic aromatic amines

42
Q

What are examples of unconjugated hyperbilirubinemias?

A

Gilbert disease

Crigler - Najjar syndrome

43
Q

What is Gilbert disease?

A
  • SNP-s in promoter region of UGT genes
  • Low UGT activity
  • benign, 5-6% of population
44
Q

What is the treatment for Gilberts disease?

A

inducer- phenobarbital

45
Q

What is the problem in Crigler- Najjar Syndrome?

A

early stop codon in UGT genes

bilirubin enecephalopathia, fatal

46
Q

What are the conjugated hyperbilirubinemias?

A

Dubin Johnson syndrome

Rotor Syndrome

47
Q

What are the problems in Dubin Johnson and Rotor Syndrome?

A

transport of conjugates is disturbed

expression of MRP2 is depressed

48
Q

What is the method of conjugation by glucuronidation?

A

UDP glucuronate

Enzyme: UDP glucuronosyl transferase (UGT)

49
Q

What is the method of conjugation by sulfation

A

PAPS

Enzyme: sulfotransferases

50
Q

What is the method of conjugation by GSH ?

A

GSH, acetyl CoA

Enzyme: GSH transferases

51
Q

What is the method of conjugation by acetylation?

A

acetyl CoA

52
Q

What is the method of conjugation by Amino acid conjugation?

A

amino acids

53
Q

What is the method of conjugation by methylation?

A

SAM

54
Q

What are the intracellular cofactors of toxicity? (what lol)

A

NADPH

UDPGA

PAPS

GSH

vitamins

55
Q
A

Biochemistry III (8 decks)

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