Pharmacokinetics Flashcards

1
Q

Where are most drugs metabolised?

A

The liver

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2
Q

What is the purpose of metabolism?

A

To increase water solubility and aid excretion

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3
Q

What is the name given to the group of drugs that are activated follow metabolism?

A

Prodrugs

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4
Q

Give 2 examples of prodrugs

A

Codeine

Enalapril

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5
Q

What kind of metabolism can involve hydrolysis, oxidation or reduction?

A

Phase 1

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6
Q

How does phase 1 metabolism provide an active site for phase 2?

A

Increasing the polarity

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7
Q

Name the super family of metabolising enzymes?

A

Cytochrome P-450 enzymes

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8
Q

What does the isoform of the cytochrome P-450 determine?

A

Drug specificity

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9
Q

Name the three families of cytochrome P-450 that are important in oxidative drug metabolism

A

CYP1, CYP2, CYP3

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10
Q

Name the major constitutive enzyme in the human liver

A

CYP3A4

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11
Q

What can induce the enzyme CYP1A2?

A

Smoking

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12
Q

What does increased water solubility mean in phase 2 metabolism?

A

Enhanced excretion of the metabolised compound

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13
Q

What conjugation usually result in?

A

Inactivation

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14
Q

What happens to the drug’s effect when the the drug metabolising enzyme is induced?

A

Decreased drug effect

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15
Q

What are the most common enzyme inducers?

A

Alcohol and smoking

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16
Q

What does increased synthesis lead to in terms of enzymes?

A

Increased activity

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17
Q

What can drugs such as clarithromycin do?

A

Inhibit drug metabolising enzymes

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18
Q

Lack/decreased activity of an enzyme often results in what?

A

Increased drug toxicity

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19
Q

What can deficieny in renal function in young children lead to?

A

Metabolites rapidly building up to toxic levels

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20
Q

By what ages can children metabolise many drugs more rapidly than adults?

A

Two

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21
Q

Name the important process involved in eliminating drugs from the body?

A

Metabolism

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22
Q

What is the therapeutic process?

A

Producing the correct therapeutic effect

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23
Q

Name the four basic factors that determine drug pharmacokinetics?

A

Absorption
Distribution
Metabolism
Elimination

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24
Q

What is Tmax?

A

Time to peak concentration

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25
Q

What is Cmax?

A

The peak concentration

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26
Q

What is the range of when the drug is active?

A

Therapeutic range

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27
Q

What is the therapeutic index a measure of?

A

The range at which a drug is safe and active

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28
Q

What bioavailability does a drug given intravenously have?

A

100%

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29
Q

Most drugs are what kinds of acids?

A

Weak Acids

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30
Q

Small changes in pH will do what to the ionisation of a drug?

A

Will significantly influence it

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31
Q

Why should aspirin be absorbed more easily from the stomach?

A

It is a weak acid

32
Q

What must a drug be to pass across a lipid layer?

A

Must be in solution and be lipid soluble

33
Q

What is the name given to the ability of a drug to diffuse across a lipid barrier

A

Lipid-water partition coefficient

34
Q

Where does the bulk flow of liquid occur?

A

Through inter-cellular pores

35
Q

Why is bulk flow important?

A

It is the major mechanism which drugs cross through capillary walls

36
Q

What must drugs resemble to undergo active transport?

A

Naturally occurring compounds

37
Q

What is first pass metabolism?

A

Metabolism of drug prior to reaching systemic circulation

38
Q

What does subcutaneous route depend on?

A

Blood flow to site

39
Q

Drugs given via rectum bypass what?

A

First pass metabolism

40
Q

What do drugs generally need to reach to reach target tissues?

A

Systemic circulation

41
Q

How are most drugs given?

A

Orally

42
Q

Once a drug has been absorbed, what must it be ready for?

A

Biological action and distribution to tissues

43
Q

What, in theory, should volume of distribution be?

A

40L

44
Q

What does volume of distribution show?

A

Where drugs go

45
Q

How can side effects of a drug be cleared?

A

Metabolism or Renal excretion

46
Q

What is the name given to the theoretical volume of fluid from which a drug is completely removed over a period of time?

A

Clearance

47
Q

What is the name given to the time taken for the drug concentration in the blood to decline to half of the current value?

A

Half-life

48
Q

What does a long half-life indicate?

A

Plasma levels will stay long for higher

49
Q

What will the knowledge of the half-life of a drug help us to work out?

A

How often a drug needs to be administered

50
Q

What will increase the toxicity of a drug in terms of half-life?

A

Prolongation of the half life

51
Q

Why do most drugs need to be given chronically?

A

To have a therapeutic effect

52
Q

How many half-lives does it take to reach stable plasma levels?

A

5-6

53
Q

What are the primary organs for drug excretion?

A

The kidneys

54
Q

What is the main mechanism used for drug excretion?

A

Glomerular filtration

55
Q

If a patient is dehydrated, what happens to the clearance of a drug?

A

It reduces

56
Q

How much bile a day does the liver secrete?

A

1 litre

57
Q

What determines where a drug will reach?

A

Chemical properties of the drug

58
Q

What is the definition of drug interaction?

A

Modification of a drug’s effect by prior or administration of a drug at the same time

59
Q

What does a narrow therapeutic index indicate?

A

A small change in blood levels can induce profound toxicity from a drug

60
Q

What can increase the probability of a drug-drug interaction?

A

Increase of number of medicaments

61
Q

What spectrum of antibiotics can destory normal gut flora?

A

Broad Spectrum

62
Q

Where are most oral medicines absorbed?

A

The small intestine

63
Q

Following absorption, where are drugs distributed to?

A

The site of action

64
Q

Name the main inducer of cytochrome P450 enzymes?

A

Smoking

65
Q

Why can drugs that work on the brain not be taken alongside alcohol?

A

As they can produce a synergistic effect that leads to toxicity

66
Q

Where does elimination of drugs occur?

A

In the kidney

67
Q

What side effect does isionazid produce?

A

Peripheral neuropathy

68
Q

What is the definition of first pass metabolism?

A

When drug is metabolised before reaching systemic circulation

69
Q

What are the examples of sub-acute onset of adverse drug reactions?

A

Rash

Serum Sickness

70
Q

How long does the onset of a latent adverse drug reaction?

A

Over 2 days

71
Q

Which type of adverse drug reaction does not require a change of therapy?

A

Acute

72
Q

What are type A adverse drug reactions linked to>

A

Too high a dose

73
Q

How are type A adverse drug reactions stopped?

A

When drug is reduced or stopped

74
Q

Chronic adverse drug reactions are related to what?

A

Duration of treatment

75
Q

Give an example of an ADR that cannot be avoided

A

Nausea in chemotherapy treatment