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PAR2031 - Pharmacology > Week 4 > Flashcards

Week 4 Flashcards

1
Q

What are the benefits/dangers of increasing drug concentration above 80% max response?

A

Little therapeutic effect

Significantly increases risk of adverse reactions

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2
Q

What is an adverse drug event?

A

‘any response to a drug which is noxious, unintended, and which
occurs at doses normally (and appropriately) used in man for
the prophylaxis, diagnosis, or therapy of a disease

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3
Q

What are the 6 Types/classification of Adverse Drug Reactions?

A 
Type A (augmented)
• Type B (bizarre)
• Type C (continuous)
• Type D (delayed)
• Type E (end of use)
• Type F (failure)
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4
Q

What happens when a drug concentration goes above 80%?

A

Achieves little therapeutic effect but significantly increases the risk of adverse reactions

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5
Q

What are the phases of drug discovery?

A
  • Drug discovery
  • Preclinical development
  • Clinical development
  • > phase 1 - PK tolerability, side effects in volunteers
  • > phase 2 - small scale trials in patients
  • > Phase 3 - large scale clinical trials
  • Regulatory Approval
  • Phase IV - postmarketing surveillance
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6
Q

Define an adverse drug reaction

A

an adverse drug event occurs whilst a person is taking a drug but is not necessarily due to the drug (includes mistakes in administration, etc)

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7
Q

What can cause an adverse drug reaction?

A
  • excess stimulation of one ‘type’ of receptor (with a highly selective drug)

OR

Following interactions with other receptors at higher concentrations

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8
Q

Adverse drug reaction identification process must include what?

A
  • Timing (relationship between the use of the drug and the occurrence of ADR)
  • Pattern recognition (may fit the known pharmacology of one of the suspected drugs or a chemically related compound)
  • Investigations (plasma, biopsies, allergy testing)
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9
Q

Explain Type A classifications

A

Type A = Augmented

  • most common (approx 80% of ADR’s)
  • typically predictable from known pharmacology
  • Usually mild with high morbidity and low mortality
  • able to be repoduced in animal studies
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10
Q

What’s an example of Type A classification ADR’s

A

Hypoglycaemia due to insulin injection

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11
Q

Explain Type B classifications

A

Type B = Bizarre

  • uncommon - 20%
  • unpredictable
  • not related to a known pharmacological action of drug
  • high morbidity low mortality
  • lack of reproducibility in animal studies
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12
Q

Example of type B classified ADR

A

Anaphylaxis due to penicillin

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13
Q

Can repeat exposure lead to an increase in hypersensitivity severity?

A

yes

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14
Q

Explain type C classification in ADR

A

Type C = Chronic

  • uncommon
  • related to cumulative dose
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15
Q

Example of type c classified ADR

A
  • colonic dysfunction due to laxatives
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16
Q

Explain type D classification in ADR

A

Type D - Delayed

  • uncommon
  • usually dose related
  • occurs some time after the use of the drug
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17
Q

Explain type E classification in ADR

A

Type E - end use withdrawl

  • uncommon
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18
Q

Example of type E classified ADR

A

opioid withdrawal

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19
Q

Explain type F classification in ADR

A

Type F - Failure of therapy

  • becoming more common
  • unexpected nil response in the setting of appropriate dose related regime
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20
Q

Example of type F classified ADR

A

resistance to antimicrobials

  • superbug type shit
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21
Q

What are the risk factors for development of ADR?

A
  • age
  • gender
  • concurrent diseases
  • genetic factors
  • history of prior drug reaction
  • chemical characteristics
  • route of administration
  • dose
  • duration and frequency
  • polypharmacy
22
Q

What does risk v benefit mean?

A

acceptable risk must be weighed against its potential therapeutic benefit

23
Q

What are the variables influencing risk v benefit for drugs?

A
  • dose administered
  • patient
  • route of administration
  • time administered
24
Q

what is a drug indication?

A

an illness or disorder for which a drug has a documented specific usefulness

25
Q

What is a drug precaution

A

clinical caution practiced in advance of administering a drug

26
Q

What is a drug contraindication?

A

a factor that makes dangerous or undesirable the administration of a drug or the performance of an act or procedure in the care a specific patient

27
Q

what is a mutagenic drug?

A

a mutagen is a physical or chemical agent that causes genetic material (DNA) to undergo a detectable and heritable structural change

28
Q

What is a carcinogenic drug?

A

a carcinogen is any agent that by either direct or indirect actions causes a normal cell to become a neoplastic cell

29
Q

what are teratogenic drugs?

A

any substance that interferes with normal foetal development causing one or more developmental abnormalities

30
Q

when can you give a drug that will affect the foetus?

A

when the benefit outweighs the risk to keep the mother alive

31
Q

how are pharmacokinetics changed during pregnancy in relation to absorption?

A
  • Absorption may be increased or decreased
  • > absorption from lungs may increase due to ventilation rates

-> absorption from skin may be increased due to skin surface area

32
Q

how are pharmacokinetics changed during pregnancy in relation to distribution?

A
  • Altered body composition (increased proportion of fat stores up to 25%)
  • Altered fluid distribution (30-50% increase in plasma vol)
33
Q

how are pharmacokinetics changed during pregnancy in relation to Metabolism?

A
  • hepatic function can change due to enzyme activity
34
Q

how are pharmacokinetics changed during pregnancy in relation to Excretion?

A

maternal renal blood flow and GFR increase

35
Q

By 12-14 weeks, the foetal liver drug-metabolising enzymes operate at?

A

30% of adult

36
Q

How long does it take for a foetus/child to have full maturation of liver drug metabolising enzymes?

A

1 year

37
Q

What happens if a drug metabolite is produced by the foetus?

A

It is more water soluble, thus can’t cross the placenta, accumulating in the amniotic fluid, resulting in increased exposure

38
Q

What are the categories for prescription medication during pregnancy?

A

Category A

Category B

39
Q

explain category A drugs prescribed to pregnant women

A

no proven increase in frequency of malformations or other direct indirect harmful effects

40
Q

explain category B1 drugs prescribed to pregnant women

A

Studies in animals have not shown evidence of an increased occurrence of foetal damage

41
Q

explain category B2 drugs prescribed to pregnant women

A

studies in animals are inadequate or may be lacking…. but some data showing promise

42
Q

explain category B1 drugs prescribed to pregnant women

A

studies in animals have shown evidence of foetal damage… unknown what is going to happen to humans

43
Q

explain category C drugs prescribed to pregnant women

A

have caused or may be suspected of causing harmful effects

can be reversible

44
Q

explain category D drugs prescribed to pregnant women

A

have caused or are expected to cause malformations or irreversible damage

45
Q

explain category X drugs prescribed to pregnant women

A

high risk of causing permanent damage

46
Q

what kind of drugs are easily transferred into breast milk?

A

highly lipid soluble, low plasma bound

47
Q

what pharmacokinetic issues should be considered for children?

A

liver and drug metabolising enzyme activity increased

48
Q

What is an extrapyramidal reaction

A

reaction to antipsychotic drugs in children

49
Q

what % of ADRs in the elderly are dose related?

A

70-80%

50
Q

what does age to to the therapeutic index?

A

often a narrow index

51
Q

what are the altered pharmacokinetics of elderly in relation to absorption?

A
  • increased gastric ph
  • altered gastric emptying and intestinal blood flow
  • decrease first-pass metabolism
52
Q

what are the altered pharmacokinetics of elderly in relation to distribution?

A
  • altered body composition
  • decrease in total body water
  • decrease is plasma albumin
  • decrease in blood flow and CO

PAR2031 - Pharmacology (13 decks)

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