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Pharmacology > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

What is pharmacokinetics

A

What the body does to drugs

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2
Q

What are the 2 drug in stages

A

Absorption and metabolism

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3
Q

What are the 2 drug out stages

A

Metabolism and elimination

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4
Q

What are the 2 types of drug administration

A

Enteral and parenteral

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5
Q

Give 3 examples of enteral delivery

A

Oral, sublingual and rectal

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6
Q

Give 3 examples of parenteral administration

A

Intravenous, subcutaneous and intramuscular

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7
Q

Where does the majority of drug absorption occur

A

Small intestine

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8
Q

What is the typical transit time of drugs in the small intestine

A

3-5 hours

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9
Q

What are 3 methods for drug absorption

A

Passive diffusion, facilitated diffusion and active transport

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10
Q

What type of drugs are commonly by passive diffusion

A

Lipophilic drugs. Eg steroids and protonated weak acids/bases

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11
Q

What does the diffusion of weak acids and bases depend on

A

Their pKa

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12
Q

What type of transporters are involved in facilitated diffusion

A

Solute carrier transporters

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13
Q

What are the 2 types of solute carrier transporters

A

Organic anion transporters or organic cation transporters

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14
Q

What do SLCs allow the transport of

A

Charged (deprotonated p) drugs

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15
Q

What are the secondary active transporters used in absorption

A

SLCs

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16
Q

Give 3 physiochemical factors that affect drug absorption

A

GI length, drug lipophilicity and amount of SLCs

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17
Q

Give 3 GI physiological factors that affect drug absorption

A

Blood flow, motility and pH

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18
Q

Briefly explain what the first pass metabolism is

A

Where absorbed drugs travel to the liver via the hepatic portal Vein where the are metabolised before they reach systemic circulation

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19
Q

What 2 enzymes are used in metabolising drugs

A

Phase I and II enzymes

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20
Q

What is the result of first pass metabolism

A

Reduces availability of drugs reaching the systemic circulation

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21
Q

What is bioavailability

A

The fraction of drugs which reaches it wh into a specific body compartment

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22
Q

What calculations measures oral bioavailability

A

Amount reaching systemic circulation / total drug given by IV

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23
Q

How do drugs travel throughout the body

A

Bulk flow then diffusion

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24
Q

What is a barrier to diffusion

A

Capillaries permeability

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25
Q

How does albumin affect drug distribution

A

It can bind to drugs reducing the amount of free drug available

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26
Q

How does drug lipophilicity affect drug distribution

A

Highly lipophilic drugs diffuse better and so can travel further

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27
Q

What is the volume of distribution

A

Represents the degree to which a drug is distributed in the body tissue rather than the plasma

28
Q

What does a higher volume of distribution indicate

A

The drug is highly distributed

29
Q

Is the volume of distribution is equal to the volume of plasma what does this suggest

A

All of the drug remains in the plasma

30
Q

What are the units of volume of distribution

A

Litres/Kg

31
Q

Where does drug metabolism largely take place

A

Liver

32
Q

What overall result do phase I and II enzymes have on drugs

A

Increase ionic charge to enhance renal elimination and conjugate drugs to stop reabsorption

33
Q

What are phase I enzymes known as

A

CYP450

34
Q

What do CYP450 enzymes do

A

Give drugs an increase dioxin charge by catalysing hydroxylation, dealkylation and redox reactions

35
Q

What do phase I drugs do to pro-drugs

A

Activate them

36
Q

Give an example of a pro drug and what it’s activated to

A

Codeine to morphine

37
Q

What reactions do phase II enzymes catalyse

A

Sulphation. N-acetylation and Glutathione conjugation

38
Q

How many superfamilies of CYP are there

A

3

39
Q

Give 3 factor that affect drug metabolism

A

Age, sex and health

40
Q

What happens to the rate of elimination if YP450 enzymes are induced

A

Increases

41
Q

What is CBZ an example of

A

A CYP450 inducer

42
Q

What affect does CBZ have

A

Controls epilepsy

43
Q

What 2 methods are there to inhibit CYP450

A

Competitive and non competitive inhibitors

44
Q

If a CYP450 enzyme is inhibited then what happens to the plasma levels of the drug

A

Increase

45
Q

What is an example of a CYP459 inhibitor

A

Grapefruit juice

46
Q

What consequence does grapefruit juice have

A

Can reduce the blood pressure by too much and cause fainting

47
Q

What genetic factor do CYP enzymes show

A

Genetic polymorphism

48
Q

What is genetic polymorphism of CYP enzymes

A

How some CYP enzymes are expressed more than others in different nationalities

49
Q

What is the main route of drug elimination

A

Through the kidney

50
Q

What are the 3 processes involved in renal excretion

A

Glomerular filtration, active tubular secretion and passive tubular reabsorption

51
Q

What percentage of renal blood goes to the glomerulus

A

20%

52
Q

How much renal blood enters the kidney via the peritubular capillaries

A

80%

53
Q

What type of drug enters the kidney at the bowl as capsule

A

Unbound drug

54
Q

What has a high expression in the proximal tubule

A

OATs and OCTs

55
Q

What types of molecules are transported in the proximal tubule

A

Ionised molecules

56
Q

What happened during proximal tubular secretion to lipophilic drugs

A

Pass back into the blood

57
Q

What is clearance

A

Rate of elimination of a drug from the body

58
Q

What does volume of distribution and clear mice collectively predict

A

How long a drug stays in the body

59
Q

What is the drug half life

A

The amount of time over which the concentration of a drug in plasma decreases to half of its original concentration

60
Q

What is the formalin for working our half life

A

0.7 x Vd /CL

61
Q

What affects clearance

A

Heart, kidneys and liver

62
Q

When does zero kinetics occur

A

When there is a saturation of CYPs or transporters

63
Q

What does polypharmcy lead to

A

Zero kinetics and there’s more competition for active sites

64
Q

What type of graph shows linear kinetics

A

Log graphs of time vs drug concentration in plasma

65
Q

What is the advantage of linear graphs

A

Can determine half lives easier

Pharmacology (12 decks)

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