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Biotransformation Flashcards

(58 cards)

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1
Q

What is Biotransformation?

A

Substance is changed from 1 chemical to another

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2
Q

Biotransformation usually takes xenobiotics to more ____ compounds that are ____ in size

A

More polar

Larger in size

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3
Q

Main location for Biotransformation?

A

Liver

- can also occur in GI, lungs, skin, kidneys

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4
Q

Describe the 1st pass effect

A
  • Oral drugs absorbed in small intestine
  • Transported in hepatic portal system
  • Reach the liver and undergo metabolism
    = LIMITS AVAILABILITY
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5
Q

The 1st pass effect limits?

A

Availability of a drug due to its metabolism in the liver

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6
Q

What is an example of a drug that is given via another route due to the 1st pass effect?

A

Morphine

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7
Q

Main purpose of Phase 1 of Biotransformation?

A

Inactivate drug and break it down

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8
Q

Catabolic phase of Biotransformation

A

Phase 1 (break down)

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9
Q

What methods are usually involved with Phase 1 of Biotransformation?

A

Oxidation
Reduction
Hydrolysis

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10
Q

End product of Phase 1 of Biotransformation?

A

More polar and More reactive

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11
Q

What enzymes carry out Phase 1 of Biotransformation?

A

Mixed function oxidases

ex. CYP450 (CYP3A4)

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12
Q

Where are the enzymes located for Phase 1 of Biotransformation?

A

ER membranes of liver

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13
Q

Main purpose of Phase 2 of Biotransformation?

A

Increase water solubility and molecular weight in order to excrete it

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14
Q

Anabolic phase of Biotransformation

A

Phase 2 (build)

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15
Q

What carries out Phase 2 of Biotransformation?

A

Endogenous substances

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16
Q

Endogenous substances form a ____ of the substrate in Phase 2 of Biotransformation

A

Conjugate

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17
Q

Which Phase in Biotransformation is faster?

A

Phase 2

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18
Q

What is Enzyme Induction?

A

Dissimilar xenobiotics induce P450s by enhancing rate of enzyme synthesis or slowing rate of enzyme degradation

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19
Q

Enzyme Induction ______ substrate metabolism

A

INCREASES

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20
Q

Enzyme Induction _____ substrate effects

A

DECREASES

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21
Q

What is Enzyme Inhibition?

A

Interaction between drug and enzyme that leaves biotransformation enzyme inhibited

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22
Q

Enzyme Inhibition _____ substrate metabolism

A

DECREASES

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23
Q

Enzyme Inhibition ____ substrate effects

A

INCREASES

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24
Q

Can enzyme inhibition be reversible or irreversible?

25
In neonates, why are they susceptible to drug toxicity?
LOW hepatic enzyme activity involved with biotransformation
26
In the elderly, what diseases could make them more susceptible to drug toxicity?
Liver and kidney disease that cause decreased metabolism
27
What processes help convert Acetomenophin into non-toxic substrates?
Glucuronidation and GSH conjugation | Sulfation
28
If the endogenous substances used in glucuronidation and sulfation of Acetomenophin are depleted, what will occur?
Toxic metabolites build up = LIVER CELL DEATH
29
When GSH is depleted faster than it is regenerated, what occurs?
Liver cell death due to toxic metabolites from Acetomenophin
30
Pharmacogenomics
Study of the entire genome to assess drug response
31
Pharmacogenetics
Study of differences in drug response due to allelic variation in genes
32
Allele
Alternative form of a gene
33
Polymorphism
Variation in DNA sequence that is present in more than 1% of the population
34
Single Nucleotide Polymorphism (SNP)
Base pair substitution
35
2 Phase 1 enzymes that contribute to variability in drug response?
CYP2D6 - cannot convert Codeine to Morphine | CYP2C19
36
2 Phase 2 enzymes that contribute to variability in drug response?
UGT1A1 | TPMT
37
Normally, what does G6PD produce?
NADPH that then regenerates reduced Glutathione
38
NADPH regenerates reduced Glutathione. What does that do?
Protects cells against oxidative damage
39
Those with variations in G6PD have what?
Abnormal RBC destruction in presence of oxidants due to decreased NADPH and reduced Glutathione
40
2 genes are known to capable of variations when it comes to therapy with Warfarin. What are those genes?
VKORC1 - increased risk for excessive anticoagulation after warfarin CYP2C9 - increased risk for bleeding due to decreased clearance of S-warfarin
41
4 steps to getting a drug on the market?
In vitro Animal studies Clinical Trials Marketing
42
What is a lead compound?
Starting point in a drug for modifications to improve parameters (in vitro)
43
When do you submit an IND (investigational new drug)?
After animal testing and Before clinical trials
44
Clinical Trials have 4 phases. Describe Phase 1.
20-100 patients | Is it safe?
45
Clinical Trials have 4 phases. Describe Phase 2.
100-200 patients | Does it work?
46
Clinical Trials have 4 phases. Describe Phase 3.
1000 -6000 patients | Does it work double blind?
47
Clinical Trials have 4 phases. Describe Phase 4.
Post-marketing surveillance
48
When do you submit an NDA (New Drug Application)?
After clinical trials and before marketing
49
Purpose of IRB (institutional review board)?
Protects rights, safety and welfare of humans participating in the clinical trials - can approve/disprove or require modifications to research
50
Established therapy against which the new agent can be compared
Control
51
Patients entering the trial have an equal probability of receiving the test or control agent
Randomized
52
Neither the health professionals nor the patient know whether the patient is receiving the experimental or control agent
Double blind
53
The health professionals, but not the patient, know which treatment the patient is getting
Single blind
54
Both health professionals and patients know whether the drug is the experimental or control agent
Open label
55
At least 2 regimens are tested simultaneously, but patients are assigned to only 1 therapy
Parallel trial
56
Patients receive each therapy in sequence and therefore serve as their own controls (i.e. A before B or B before A)
Crossover trial
57
Measured to assess a drug's effect
Endpoint
58
An outcome of therapy that predicts the real goal of therapy without being that goal (i.e. reduction in tumor size as a surrogate for survival)
Surrogate endpoint

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