Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm Week > Biotransformation > Flashcards

Biotransformation Flashcards

1
Q

What is Biotransformation?

A

Substance is changed from 1 chemical to another

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

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

A

More polar

Larger in size

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Main location for Biotransformation?

A

Liver

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

The 1st pass effect limits?

A

Availability of a drug due to its metabolism in the liver

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

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

A

Morphine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Main purpose of Phase 1 of Biotransformation?

A

Inactivate drug and break it down

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Catabolic phase of Biotransformation

A

Phase 1 (break down)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What methods are usually involved with Phase 1 of Biotransformation?

A

Oxidation
Reduction
Hydrolysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

End product of Phase 1 of Biotransformation?

A

More polar and More reactive

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What enzymes carry out Phase 1 of Biotransformation?

A

Mixed function oxidases

ex. CYP450 (CYP3A4)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Where are the enzymes located for Phase 1 of Biotransformation?

A

ER membranes of liver

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Main purpose of Phase 2 of Biotransformation?

A

Increase water solubility and molecular weight in order to excrete it

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Anabolic phase of Biotransformation

A

Phase 2 (build)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What carries out Phase 2 of Biotransformation?

A

Endogenous substances

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

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

A

Conjugate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Which Phase in Biotransformation is faster?

A

Phase 2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What is Enzyme Induction?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Enzyme Induction ______ substrate metabolism

A

INCREASES

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Enzyme Induction _____ substrate effects

A

DECREASES

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What is Enzyme Inhibition?

A

Interaction between drug and enzyme that leaves biotransformation enzyme inhibited

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Enzyme Inhibition _____ substrate metabolism

A

DECREASES

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Enzyme Inhibition ____ substrate effects

A

INCREASES

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Can enzyme inhibition be reversible or irreversible?

A

Both

25
Q

In neonates, why are they susceptible to drug toxicity?

A

LOW hepatic enzyme activity involved with biotransformation

26
Q

In the elderly, what diseases could make them more susceptible to drug toxicity?

A

Liver and kidney disease that cause decreased metabolism

27
Q

What processes help convert Acetomenophin into non-toxic substrates?

A

Glucuronidation and GSH conjugation

Sulfation

28
Q

If the endogenous substances used in glucuronidation and sulfation of Acetomenophin are depleted, what will occur?

A

Toxic metabolites build up = LIVER CELL DEATH

29
Q

When GSH is depleted faster than it is regenerated, what occurs?

A

Liver cell death due to toxic metabolites from Acetomenophin

30
Q

Pharmacogenomics

A

Study of the entire genome to assess drug response

31
Q

Pharmacogenetics

A

Study of differences in drug response due to allelic variation in genes

32
Q

Allele

A

Alternative form of a gene

33
Q

Polymorphism

A

Variation in DNA sequence that is present in more than 1% of the population

34
Q

Single Nucleotide Polymorphism (SNP)

A

Base pair substitution

35
Q

2 Phase 1 enzymes that contribute to variability in drug response?

A

CYP2D6 - cannot convert Codeine to Morphine

CYP2C19

36
Q

2 Phase 2 enzymes that contribute to variability in drug response?

A

UGT1A1

TPMT

37
Q

Normally, what does G6PD produce?

A

NADPH that then regenerates reduced Glutathione

38
Q

NADPH regenerates reduced Glutathione. What does that do?

A

Protects cells against oxidative damage

39
Q

Those with variations in G6PD have what?

A

Abnormal RBC destruction in presence of oxidants due to decreased NADPH and reduced Glutathione

40
Q

2 genes are known to capable of variations when it comes to therapy with Warfarin. What are those genes?

A

VKORC1 - increased risk for excessive anticoagulation after warfarin
CYP2C9 - increased risk for bleeding due to decreased clearance of S-warfarin

41
Q

4 steps to getting a drug on the market?

A

In vitro
Animal studies
Clinical Trials
Marketing

42
Q

What is a lead compound?

A

Starting point in a drug for modifications to improve parameters
(in vitro)

43
Q

When do you submit an IND (investigational new drug)?

A

After animal testing and Before clinical trials

44
Q

Clinical Trials have 4 phases. Describe Phase 1.

A

20-100 patients

Is it safe?

45
Q

Clinical Trials have 4 phases. Describe Phase 2.

A

100-200 patients

Does it work?

46
Q

Clinical Trials have 4 phases. Describe Phase 3.

A

1000 -6000 patients

Does it work double blind?

47
Q

Clinical Trials have 4 phases. Describe Phase 4.

A

Post-marketing surveillance

48
Q

When do you submit an NDA (New Drug Application)?

A

After clinical trials and before marketing

49
Q

Purpose of IRB (institutional review board)?

A

Protects rights, safety and welfare of humans participating in the clinical trials
- can approve/disprove or require modifications to research

50
Q

Established therapy against which the new agent can be compared

A

Control

51
Q

Patients entering the trial have an equal probability of receiving the test or control agent

A

Randomized

52
Q

Neither the health professionals nor the patient know whether the patient is receiving the experimental or control agent

A

Double blind

53
Q

The health professionals, but not the patient, know which treatment the patient is getting

A

Single blind

54
Q

Both health professionals and patients know whether the drug is the experimental or control agent

A

Open label

55
Q

At least 2 regimens are tested simultaneously, but patients are assigned to only 1 therapy

A

Parallel trial

56
Q

Patients receive each therapy in sequence and therefore serve as their own controls (i.e. A before B or B before A)

A

Crossover trial

57
Q

Measured to assess a drug’s effect

A

Endpoint

58
Q

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)

A

Surrogate endpoint

Pharm Week (6 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions