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Biochemistry > Biotransformation > Flashcards

Biotransformation Flashcards

1
Q

Name some organs, which express P450 isozymes involved in drug metabolism

A

Liver, kidney, skin, intestine + lungs

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2
Q

What is the electron donor for monooxygenases in drug metabolsim?

A

NADPH

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3
Q

What kind of ROS can be formed during P450 monooxygenation?

A

Superoxide (O2-)

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4
Q

Which pathways of the intermediary metabolism involve biotransformation reaction?

A

Bile acid, Steroid hormones synthesis, cholesterol synthesis, D-vitamin, Catacholamines, Drugs

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5
Q

Which phase of biotransformation is mediated by transports?

A

Phase 3

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6
Q

What is the dominant chemical reaction in 1st phase of biotransformation?

A

Hydrolysis, oxidation, hydration, reduction

E.g. Hydroxylation

Formation of a more water soluble drug

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7
Q

Which enzyme catalyse the majority of the reactions in 1st phase biotransformation?

A

CYP P450 monooxygenase complex families

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8
Q

What kind of solubility change is caused by transformation reaction?

A

A substance is transformed into a more water soluble substance, which can be excreted

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9
Q

What is the first enzyme component of the microsomal respiratory chain and what is the electron donor?

A

Enzyme: Cytochrome P450 reductace
Donor: NADPH

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10
Q

What are the 3 phases of biotransformaition?

A

1: Oxidation
2: Conjugation
3: Transporters

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11
Q

What is the general reaction of CYPs?

A

R-H + 02 + NADPH + H+ -> R-OH + H2O + NADP

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12
Q

How many CYP families do we have in drug metabolism?

A

4 families: 1, 2, 3, and 4

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13
Q

Name 1 very important function of the liver?

HINT: portal circulation

A

First pass effect

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14
Q

CYP1: Is it inducible and what is its substrate?

A

Yes, by dioxin derivatives

Substrate: Policyclic aromatic hydrocarbons (PAH)

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15
Q

CYP2: Is it inducible and what is its substrate?

A

Yes, by ethanol, aceton phenobarbital and diazepam derivaties .

Many different substrates depending on sub-family type.
We have CYP2A, 2B, 2C and 2D

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16
Q

Name some nuclear receptors in drug metabolism

A

CAR: androstanes, phenobarbital
LXR: Oxysterols
RXR: Pregnanes
PPAR alpha, beta, gama: fatty acids, eicosanoids

“gene battery”: For phase 1+2 reactions and ABC transporters for phase 3

17
Q

What is the most common type of conjugation?

A

Glucuronidation (UDP-glucuronate -> by UDP-glucuronosyl transferase (UGT))
Other reactions: Sulfunation, glutathione conjugation, amino acid conjugation, methylation, acetylation.

Sulfunation with PAMS by sulfotransferase
Glutathione conjugation:

18
Q

Which receptor mediates dioxin toxicity?

A

Aryl Hydrocarbon receptor (AhR)

19
Q

Whats the effect of hypertriglycedemia on size and density of LDL?

A

Size: decrease
Density: increase

20
Q

Which phase of biotransformation is mediated by transporters?

A

III. phase

21
Q

Dominant chemical reaction in 1st phase of biotransformation?

A

OXYGENATION

22
Q

What kind of metabolizer phenotypes are known due to SNPs of drug metabolizing enzymes?

A

People having Gilberts disease (unconjugated hyperbilirubinemia) due to SNP’s (single nucleotide polymorphism) in the promoter region of UGT (UDP-­‐ gucuronyltransferase) genes.

Poor metabolizers, extensive metabolizers

23
Q

Co- factor of glucoroniditation?

A

UDP- glucoronic acid

24
Q

Which enzymes catalyzes glucorunidation?

A

UDP- glucoronidate transferases (UGT)

25
Q

Most important ligands of nuclear receptors

A

Hormones, Drugs, Vitamins, Eicasonoids

26
Q

Where are the steroid receptors before ligand binding in the cell?

A

On the PM, cytosol, nucleus (generally intracellular)

27
Q

List at least two types of pattern recognition receptor involved in the pathomecanism of arthrosclerosis

A

SCAVANGER r.s., TLRs, NLRP

28
Q

Which are the most important xenobiotic inducers of CYP1 isoenzymes?

A

Polycyclic Aromatic Hydrocarbons

29
Q

Dominant type of conjugation in case of electrophilic intermediates?

A

Glutathion conjugation

30
Q

First component of microsomal respiratory chain

A

NADPH- p450- oxidoreductase

31
Q

Mutation of which receptor are underling the testicular femination syndrome?

A

Androgenic

32
Q

Conjugated hyperbilrubinemias are caused by? what is the name of the syndromes?

A

Transport of conjugated bilrubin is disturbes. Transport problems.

Dubin-Johnsons syndrome
Rotor syndrome

33
Q

What do we need for sulfuration?

A

PAPS (3’-phosphoadenosine-5’-phosphosulfate)

Biochemistry (4 decks)

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