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PHRM2500 > WEEK 8 > Flashcards

WEEK 8 Flashcards

1
Q

Variability in response to a drug can be categorised as being … or … in nature.

A

pharmacokinetic or
pharmacodynamic

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2
Q

During metabolism, a drug
is usually converted into a more …-soluble compound.

A

water-soluble compound.

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3
Q

T or F
People can differ in the
ratio of different metabolites that they produce.

A

T

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4
Q

Frequently, a drug
simultaneously undergoes metabolism by several competing … pathways.

A

Enzyme

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5
Q

T or F
Drug excretion does not vary across people and within an individual over time.

A

F
It does vary.

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6
Q

T or F
Normally only free or unbound drug can interact with drug target sites.

A

T

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7
Q

T or F
A drug’s effect at its site of action can vary across people and within an individual over time.

A

T

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8
Q

T or F
Most drugs work by interacting with receptors, enzymes or other
exogenous proteins within the body.

A

F
Endogenous

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9
Q

In terms of pharmacokinetic processes – variability in drug response may be
due to variability in drug …, …, … or …

A

absorption, distribution, metabolism or excretion.

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10
Q

As a result of pharmacokinetic variability people taking the same dose of a
drug can have different … of drug in their body over time,
leading to different drug responses.

A

concentrations

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11
Q

Variability in drug response can be due to differences in….
across people and within an individual over time.

A

receptor and enzyme expression, receptor or enzyme
affinity for the drug and the post-target transduction
process

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12
Q

As a result of pharmacodynamic variability people with the same drug exposure can have different drug …

A

responses

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13
Q

What is “inter-subject
variability”?

A

Variability in drug response may be between individuals

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14
Q

What is “intra-subject variability”?

A

Variability within a person over time

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15
Q

T or F
Inter-subject variability is generally much smaller than intra-subject variability.

A

F
Intra-subject variability is generally much smaller than inter-subject
variability.

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16
Q

As a result of variability, the dosage regimen of some drugs may need to be individualised to patients’ needs by dose titration based on … or …

A

Dose titration based on a person’s response to the drug
or
Dose titration based on drug concentrations (TDM)

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17
Q

Dose titration based on drug concentrations is called what?

A

TDM

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18
Q

Dose titration based on drug concentrations is used if…

A

If a relationship between drug concentration and effect exists and effect is difficult to measure.

19
Q

The potential need for individualised therapy is greatest for drugs that have a
… therapeutic index.

A

narrow

20
Q

What does it mean when a drug has a narrow therapeutic index?

A

Drugs with a narrow therapeutic index are those where there is little difference between a therapeutic dose of the drug and a dose that causes significant toxicity.

21
Q

What are some examples of drugs with a narrow therapeutic index?

A

Examples of such drugs include digoxin, theophylline, warfarin, lithium carbonate, gentamicin, vancomycin, phenytoin, cyclosporine, tacrolimus and many
anti-cancer drugs.

22
Q

For a drug with a narrow therapeutic index there is little difference between
the drug dose required for … and the drug dose that can lead to significant …

A

efficacy
toxicity

23
Q

Some major sources of pharmacokinetic variability include the following factors…

A

Genetics
Age
Gender
Weight
Hepatic disease
Renal disease
Cardiovascular disease
Drug interactions
Environmental influences

24
Q

T or F
Drug metabolic enzymes, transporters and target proteins can all vary in activity and expression across individuals.

A

T

25
Q

When does polymorphism in biology occur?

A

When two or more clearly different phenotypes exist in the same population of a species.

26
Q

What is a genetic polymorphism?

A

A trait that has genetic variation which results in more than a single population being represented in >1% of the total population.

27
Q

Genetic variability in metabolic enzymes and drug transporters is an expression of … (pharmacokinetic or pharmacodynamic) variability?

A

Pharmacokinetic variability

28
Q

Genetic variability in receptors, ion channels, enzyme targets, neurotransmitters, immune cells, etc. is an expression of … (pharmacokinetic or pharmacodynamic) variability?

A

Pharmacodynamic variability

29
Q

What alleles are needed in order to get a poor metabolizer as a phenotype?

A

Two mutant alleles

30
Q

What alleles are needed in order to get an extensive metabolizer as a phenotype?

A

Two active “normal” alleles

31
Q

What alleles are needed in order to get an intermediate metabolizer as a phenotype?

A

One “normal” and one mutant. Heterozygous.

32
Q

What alleles are needed in order to get an ultrarapid metabolizer as a phenotype?

A

Gene duplication of normal alleles.

33
Q

What is INR a measure of?

A

The clotting tendency of the blood.

34
Q

An INR of less than … is associated with an increased risk of thromboembolism.

A

2

35
Q

An INR of more than … is associated with an increased risk of bleeding.

A

4

36
Q

S-warfarin is principally metabolised by

A

CYP2C9

37
Q

What is Rh factor?

A

Rheumatoid factor is an inherited protein found on the surface of erythrocytes which influences whether you have a positive or negative blood type.

38
Q

How does a higher level of rheumatoid factor in the blood influence the severity of rheumatoid arthritis?

A

Patients with a high Rh factor usually have a poorer prognosis.

39
Q

What is the layman’s term for an erythrocyte?

A

A red blood cell

40
Q

What is an erythrocyte sedimentation rate?

A

EST is the rate at which erythrocytes in anticoagulated whole blood descend in a standardized tube over a period of one hour. It is a non-specific (meaning it can’t provide a diagnosis) test that measures inflammation.

41
Q

Having … and … measures of a therapeutic outcome is an important consideration during a pharmacodynamic investigation.

A

sensitive and specific

42
Q

What does SCAR stand for?

A

severe cutaneous adverse reaction

43
Q

SCAR is a dangerous phenomenon with documented mortality rates of up to …%.

A

35%

44
Q

Screening for SCARs has been advised by several expert groups for high-risk patients including…

A

African Americans, Korean patients with renal impairment, and Chinese and Thai populations.

PHRM2500 (5 decks)

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