THERAPEUTICS Flashcards

1
Q

what is pharmacodynamics?

A

what the drug does to the body

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2
Q

what is pharmacokinetics?

A

what the body does to the drug

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3
Q

what is a medicinal product?

A

a substance or combination presented as having properties for treating or preventing disease in human beings eg drugs

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4
Q

what is a medical device?

A

anything as simple as a plaster all the way to an MRI machine (any instrument/ machine/ apparatus)

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5
Q

what are the 2 methods by which drugs enter the system?

A
  • Active transport

- Passive diffusion

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6
Q

what 4 processes does pharmacokinetics involve?

A
  • absorption
  • distribution
  • metabolism
  • excretion
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7
Q

where is the main site of metabolism in pharmacokinetics?

A

liver

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8
Q

where is the main site of excretion in pharmacokinetics?

A

kidneys

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9
Q

what is a formulation?

A

the pharmaceutical form of a drug eg tablet or capsule

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10
Q

what does liberation mean?

A

the release of a drug from its pharmaceutical form

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11
Q

what is drug absorption?

A

drug being moved into systemic circulation after being administered

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12
Q

what is distribution?

A

movement of drug into tissue from systemic circulation

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13
Q

what is drug metabolism?

A

conversion of drug into other chemicals in the body

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14
Q

what is drug excretion?

A

elimination of medicine from the body

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15
Q

what is the formula for calculating the volume of distribution?

A

vol of distribution = dose/ plasma conc

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16
Q

what does lower vol of dist (Vd) mean?

A

drug stays in blood stream

eg warfarin

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17
Q

what does higher vol of distribution mean?

A

drug moves into tissues

eg propranolol

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18
Q

what is therapeutic index?

A

the ratio of the dose that results in an undesired effect to that which results in a desired effect

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19
Q

what does therapeutic drug monitoring involve?

A

clinical practice of measuring specific drugs at designated intervals to maintain a constant concentration in a patients bloodstream, thereby optimising individual dose regimens

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20
Q

name some drugs with a narrow therapeutic index

A
  • aminoglycosides
  • ciclosporin
  • carbamazepine
  • digoxin
  • flecainide
  • lithium
  • pheytoin
  • rifampicin
  • theophylline
  • warfarin
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21
Q

what are some factors affecting drug absorption (5)?

A
  • formulation
  • motility of the gut
  • food in stomach
  • degree of 1st pass metabolism
  • lipid solubility
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22
Q

what are some factors affecting drug distribution (4)?

A
  • lipid solubility
  • degree of ionisation
  • drugs which are highly protein bound
  • pharmacogenetics
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23
Q

what is the only type of drug that can exert an effect?

A

unbound drugs

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24
Q

what is a ‘free drug’?

A

active drug

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25
Q

which fruit acts as an enzyme inhibitor?

A

grapefruit

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26
Q

what is meant by affinity?

A

how actively the drug binds to the receptor

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27
Q

what is meant by efficacy?

A

ability of drug to elicit a response when it binds to the receptor

28
Q

what is meant by potency?

A

a measure of the amount of drug required to produce an effect

29
Q

what is an agonist?

A

drug that activates a receptor

30
Q

what is an antagonist?

A

a drug which blocks a receptor

31
Q

what is a partial agonist?

A

drug that binds to and activates a given receptor, but only has partial efficacy at the receptor (relative to full agonist)

32
Q

describe competitive inhibition

A
  • this blocks an enzyme at its active site

- it is temporary

33
Q

describe non-competitive inhibition

A

this stops an enzyme from working by changing the shape of the active site by combining to the allosteric site (not active site)

34
Q

what is bioavailability?

A

the proportion of the administered drug that reaches the systemic circulation, must first pass the intestinal wall and the portal circulation to the liver

35
Q

what does the area under the bioavailability curve indicate?

A

the extent of the absorption

36
Q

what is the peak concentration of the bioavailability curve?

A

the highest conc of a drug in the plasma after a dose is given

37
Q

what is the median toxic dose?

A

the dose at which toxicity occurs in 50% cases in the population

38
Q

what does a phase 1 metabolic reaction primarily involve?

A

oxidation

39
Q

what does a phase 2 metabolic reaction primarily involve?

A

conjugation

40
Q

describe characteristics of phase 1 metabolic reactions

A
  • involves a biotransformation of a drug to a more polar metabolite
  • involve CYP enzymes
  • these reactions mostly oxidation but can be reduction or hydrolysis
41
Q

what happens to phase 1 product in phase 2 metabolic reaction?

A

phase 1 product is bound to conjugate

-drug is now more hydrophilic

42
Q

what is drug clearance?

A

the volume of fluid cleared of a drug per unit time

43
Q

what is half-life?

A

the time for the plasma concentration to fall by 50% of what it was at equilibrium

44
Q

what is distribution half-life?

A

when plasma levels fall to half what they were due to distribution of the drug to body tissue

45
Q

what is elimination half-life?

A

when plasma levels fall to half of what they were due to the drug being metabolised and eliminated

46
Q

what is 1st order elimination?

A

rate of drug elimination is dependent on plasma conc

47
Q

what is zero order elimination?

A

rate of elimination is constant and independent of plasma conc

48
Q

how does the elimination half-life relate to the time taken for drug to be eliminated from the body ?

A

x5 elimination = time at which the drug is eliminated

49
Q

what are the 5 classes of drugs?

A
  • beta-blockers
  • ACE inhibitors
  • ARBs (angioptensin 2 receptor blockers)
  • cholesterol-lowering drugs
  • calcium channel blockers
50
Q

what do beta-clockers generally end in?

A

-alol or -lol

51
Q

what do beta-blockers do?

A

block the beta-adrenergic receptors—->blocks the sympathetic nervous system to heart and lungs, primarily slows heart rate, reduces BP

52
Q

what are some common side effects of beta-blockers (4)?

A
  • bradycardia
  • hypotension
  • congestive heart failure (if HR too low)
  • bronchospasm
53
Q

what do ACE inhibitors typically end in?

A

-pril

54
Q

what do ACE inhibitors do?

A

inhibit angiotensin converting enzymes in the lungs (ACE) —->lower BP

55
Q

what are some common side effects of ACE inhibitors (3)?

A
  • chronic cough
  • angioedema
  • hypotension
56
Q

what do ARB’s (angiotensin II receptor blockers) typically end in?

A

-sartan

57
Q

what do ARBs do?

A

block angiotensin II-which is vasoconstrictor–>lower BP

58
Q

what do cholesterol-lowering drugs generally end in?

A

-statin

59
Q

what do cholesterol-lowering drugs do?

A

inhibit fat adsorption and inhibit cholesterol production

60
Q

what are some common side effects of cholesterol-lowering drugs (4)?

A
  • steatorrhoea
  • muscle weakness
  • diarrhoea
  • abdominal discomfort
61
Q

what do calcium channel blockers generally end in?

A

-pine

62
Q

what do calcium channel blockers do?

A

block calcium channels

63
Q

what are some common side effects of calcium channel blockers (3)?

A
  • bradycardia
  • hypotension
  • heart failure
64
Q

what is meant by ED50?

A

-dose of medicine that produces desired pharmacological effect in 50% of the studied patient population that takes the medication

65
Q

what is meant by TD50?

A

-median toxic dose of drug/toxin-toxicity occurs in 50% cases

66
Q

What is better a small or large therapeutic index?

A

Large

67
Q

What is an example of a drug with a large therapeutic index?

A

Paracetamol