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303 MEDIMAGE > 1. Introduction to Pharmacology > Flashcards

1. Introduction to Pharmacology Flashcards

1
Q

what are the 4 things that patients should be informed aobut

A

why a contrast agent is used
what the contrast agent is
potential adverse reactions associ. w contrast agent
risk factors for potential complications

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2
Q

what is pharmacology

A

study of drugs in living systems

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3
Q

what is a drug

A

chemical substance that affects physiological function

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4
Q

how do drugs work? does it create new bio functions

A

no, it enhances or blocks existing functions

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5
Q

what are the 3 drug nomenclature and what are they based on

A

chemical name - structure of compound
generic - structure/composition
trade name - brand

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6
Q

what are analgesics, what do they do

A

relieve pain

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7
Q

what are anxiolytics, what do they do

A

drugs supress anxiety and relax muscles

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8
Q

what are 3 examples of analgesics

A

NSAIDS/ibuprofen, paracetamol, tradamol

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9
Q

what are 3 examples of anxiolytics

A

lorazepam, midazolam, diazepam

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10
Q

what are antiarrhythmics, what do they do

A

control irregularities of heartbeat

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11
Q

what are 3 examples of antiarrhythmics

A

adenosine
digoxin
llidocaine

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12
Q

what are antibiotics, what do they do

A

combat bacterial infections

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13
Q

what are 2 examples of antibiotics

A

amoxicilin

penicillin

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14
Q

what are anticoagulants, what do they do

A

prevent blood from clotting

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15
Q

what are 2 examples of anticoagulants

A

warfarin

heparin

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16
Q

what are antidiabetics, what do they do

A

used for diabetes

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17
Q

what are 2 examples of antidiabetics

A

metformin

glipizide

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18
Q

what are anticonvulsants, what do they do

A

prevent epileptic seizures

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19
Q

what are 3 examples of anticonvulsants

A

valproate
phenytoin
gabapentin

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20
Q

what are antiemetics, what do they do

A

treat nausea/vomiting

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21
Q

what are 2 examples of antiemetics

A

metoclopramide

promethazine

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22
Q

what are antihistamines, what do they do

A

counteract effects of histamine (chemical involved in allergic reactions)

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23
Q

what are 3 examples of antihistamines

A

fexofenadine
diphenhydramine
loratadine

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24
Q

what are antihyperlipidemics, what do they do

A

reduces high levels of lipids in blood

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25
Q

what are 2 examples of antihyperlipidemics

A

atrovastatin

sinvastatin

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26
Q

what are antineoplastics, what do they do

A

treats cancer

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27
Q

what are 3 examples of antihyperlipidemics

A

fluorouracil
carboplatin
melphalan

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28
Q

what are antipsychotics, what do they do

A

treat symptoms of psychiatric disorders

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29
Q

what are 2 examples of antipsychotics

A

haloperidol

risperdone

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30
Q

what are betablockers, what do they do

A

treat blood pressure and angina

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31
Q

what are bronchodilators, what do they do

A

eases breathing (asthma)

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32
Q

what are corticosteroids, what do they do

A

reduce inflammation and supress the immune system

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33
Q

what are diuretics, what do they do

A

promote urine production (gets rid of excess fluid)

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34
Q

what are laxatives, what do they do

A

increase ease of bowel movements

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35
Q

what are vasoconstrictors, what do they do

A

help relieve low blood pressure

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36
Q

what are vasodilators, what do they do

A

dilate blood vessels allowing blood to flow more easily

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37
Q

what are 2 examples of betablockers

A

metoprolol

propanolol

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38
Q

what are 2 examples of bronchodilators

A

epinephrine

salbutamol

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39
Q

what are 3 examples of corticosteriods

A

betamethasone
dexamethasone
prednisone

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40
Q

what are 2 examples of diruetics

A

bumetanide

furosemide

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41
Q

what is an example of laxatives

A

bisacodyl

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42
Q

what is an example of vasoconstrictors

A

norepinephrine

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43
Q

what is an example of vasodilators

A

nitroglycerin

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44
Q

what is contrast induced nephropathy

who are most at risk

A

cause of acute renal failure

patients at risk: diabetics, pre-exist renal insufficiency. use of nephrotoxic drugs and dehydration

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45
Q

what is phamacokinetics

A

study of absorption, distribution and elimination of drugs

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46
Q

what is pharmacodynamics

A

study of molecular, biochemical and physiological effects of drugs on cellular/body systems and their mechanisms of action

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47
Q

what is pharamacogenomics

A

study of genetic influences on the effectiveness and fate of drugs

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48
Q

what is toxicology

A

study of adverse/toxic effects of drugs and other chemical agents

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49
Q

what is the relation between the body and drug in pharmacokinetics

A

what the body does to the drug

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50
Q

what is the relation between the body and drug in pharmacodynamics

A

what the drug does to the body

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51
Q

drug concentration relates __ to the ___

what is the relationship trend

A

dose to the effect

usually proportionally related

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52
Q

what is the dose of a drug

A

actual amount of drug administered

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53
Q

what is the concentration of a drug

A

what that dose produces in the body

54
Q

dose = ___ x ___

A

conc x volume

55
Q

what is ADME

A

absorption
distribution
excretion
metabolism

56
Q

what is absorption of drugs

A

drug movement from administration site to the systemic circulation

57
Q

what is distribution of drugs

A

reversible movement of drug to the extravascular compartments

58
Q

what is metabolism of drugs

A

drug elimination due to the biotransformation

59
Q

what is excretion of drugs

A

physical removal of drug from body

60
Q

why is ADME important

A

ADME properties of a drug directly influences the concentration time profile in the body

61
Q

what is the symbol for peak concentration

A

Cmax

62
Q

what is the symbol for time to peak concentration

A

Tmax

63
Q

what is the major organ that is involved with absorption

A

GI tract

64
Q

what is the major organ that is involved with metabolism

A

liver

65
Q

what is the major organ that is involved with excretion

A

kidney

66
Q

what is the major organ that is involved with absorption and excretion of gases

A

lungs

67
Q

what phases of ADME involve movement of drug across biological membranes

A

all 4

68
Q

what are the main membranes that a drug has to cross

A

plasma membranes

69
Q

what are the 2 components of the plasma membrane

A

lipid bilayer

proteins embedded in the membrane

70
Q

what does the plasma membrane do

3 functions

A

Plasma membrane separates exterior enivro from inner contents of cell

Protective barrier around cell

Regulate what materials can pass in or out

71
Q

what are transporters and what are the 2 types

A

proteins that carry substrate in/out of cells

uptake = entry
efflux = export substrate out
72
Q

what are the 3 drug physico-chemical properties

A

molecular size
lipophilicity
ionisation

73
Q

how does a drug’s molecular size affect the movement across the membrane

A

smaller molecule = easier movement across

74
Q

how does a drug’s lipophilicity affect the movement across the membrane

A

lipid soluble drugs cross membranes more easily than hydrophilic drugs

75
Q

how does a drug’s ionisation affect the movement across the membrane

A

drugs are weak acids/bases and exist in both their ionised and non ionised forms in different ratios depending on the pH of the soln

76
Q

what do weak acids do when ionised

what charge do they become

A

give up H+ to become negatively charged

77
Q

what do weak bases do when ionised

what charge do they become

A

accept a H+ to become positively charged

78
Q

as pH increases (more basic) what happens to the ionisation of weak acids

A

become more ionised

79
Q

as pH decreases (more acidic) what happens to the ionisation of weak bases

A

become more ionised

80
Q

weak acids/bases __ ___ in soln

A

partially ionised in soln

81
Q

the ratio between ionised and non ionised weak acids/bases varies with what

A

pH

82
Q

the movement towards the ionised form continues until what

A

when equilibrium is reached between fraction ionised and non ionised

83
Q

are ionised polar

A

yes

84
Q

are non ionised polar

A

no they are non polar

85
Q

what form ionised/nonionised crosses the membrane freely?

A

non ionised form (AH or B)

86
Q

polar molecules like/dislike water

A

likes to remain in water

87
Q

non polar prefers to move into what kind of a environment

A

lipid environment

88
Q

can ionised molecules enter the membrane

why/why not

A

no as low lipid solubility so cant enter unless theres a transporter

89
Q

what is the pka

A

pH at which it exists in 50/50 - equal proportions - of its ionised and non ionised forms

A physico-chemical property that controls ionization state when the drug is in soln

90
Q

what happens when the pH = pka

A

If Pka drug = ph of soln then 50/50 exist as ionised and non-ionised

91
Q

if the drug is more acidic, in a acidic soln will the drug exist more in a ionised or non ionised form and what does this mean for its ability to travel through membranes

A

Amoxicillin acidic so at more acidic soln the drug will exist more in non ionised form so can freely cross membranes

the opposite of this scenario with bases is also true

92
Q

why is pH important in relation to the pka of drugs

A

pH of the tissue and the pka of the drug will determine the equilibrium of ionised and non ionised drug

93
Q

drugs that are weak acids/bases is dependent on what for their ability to cross the membrane

A

pH of absorption site

94
Q

weak acids may accumulate in what types of compartments

A

high pH compartments

95
Q

weak bases may accumulate in what types of compartments

what is this effect known as

A

low pH compartments

pH partition

96
Q

how is the pH partition principle utilised in toxicology and drug overdose

A

increase drug elimination in drug overdose situations

acidic drugs more ionised in alkaline urine so dont diffuse back into kidney tubules so can be excreted quickly - overdose in acidic drug can use alkaline to speed up elimiation

97
Q

what are the 5 types of membrane transport

A 
passive diffusion
active transport
filtration
endocytosis
facilitated diffusion
98
Q

why are membranes hard to cross

A

they are selectively permeable so only allows specific things to pass through as phospholipids are tightly packed and there is a hydrophobic centre

99
Q

what is passive diffusion driven by and does it use energy

A

driven by conc gradient and dont use energy

100
Q

what kind of molecules can pass through lipid bilayer via passive diffusion

A

molecules must be lipophilic, uncharged and small

101
Q

what are the 2 types of passive diffusion

A

transcellular and paracellular

102
Q

what is a conc gradient and how is this related to molecule movment

A

difference in conc of a substance across a given space

molecules move from more conc to less conc until they are equally distributed in that space

103
Q

what is the relationship between the conc gradient and speed of passive diffusion

A

greater conc diff = faster diffusion

104
Q

what is transcellular transport and is it the same across all tissues

A

molecules diffuse across membrane directly

same across all tissues

105
Q

what is transcellular transport and is it the same across all tissues

what is it dependent on

A

diffuse through water filled gaps between adjacent cells

tissue dependent and is not the same for all tissues as it is controlled by intercellular junctions

106
Q

what types of molecule can paracellular transport facilitate movement for

A

small hydrophilic/water soluble molecules

passive diffusion for those kinds of molecules

107
Q

what is an example of why paracellular transport is tissue dependent

A

CNS have tight junctions

liver have larger bigger gaps so easier passage between cells

108
Q

what is facilitated diffusion and what is it driven by and does it need energy

A

passive diffusion of drugs through transmembrane proteins

driven by conc gradient, dont need energy

109
Q

what does facilitated diffusion require

A

recognition by carrier or channel protein

110
Q

what kind of molecules can be faciliated by faciliated diffusion

explain why this kind of molecule cant move across the membrane by itself and how facilitated diffusion helps it to do so

A

Large polar/ionic molecules which are hydrophilic cant cross phospholipid bilayer unaided as charged molecules are repelled by hydrophobic tails in the interior of the phospholipid bilayer

Allow transport of POLAR MOLECULES (endogenous substrate like sugars rather than drugs)

If drug is recognized by channel proteins embedded in membrane can be carried across

Only allow specific molecule to pass so drugs need to resemble endogenous molecules to be recognized

111
Q

what are gated channels

A

Gated channels open/close in response to need to cell

112
Q

what is the difference in the rate of diffusion and saturation ability between passive and facilitated diffusion

A

facilitated diffusion rate is usually faster and can saturate (can also have competing ligands for the same transmembrane transporter that slows down diffusion) vs passive where it will just diffuse continuously until equilibrium is reached

113
Q

what does saturability of transporters mean

A

Saturable as # of substrate molecule per time depends on # of channel/carriers avail per cell

114
Q

facilitated diffusion is important in which 2 organs

what proteins are involved

A

kidneys and GI tract

carrier and channel proteins

115
Q

what doe channel proteins do

A

transport ions across membranes

116
Q

what doe carrier proteins do and how do they function

A

bind to specific molecules and flip between membranes so it is open at different sides of membrane

117
Q

what is active transport, is it driven by gradient and does it use energy

A

not driven by conc gradient, acts against conc gradient

uses cellular energy to move molecules against conc gradient, energy from hydrolysis of ATP

118
Q

what does active transport require in terms of transporters

A

requires recognition by membrane transporters

119
Q

is active transport saturable and can it be inhibited

A

yes it is saturable and can be inhibited by similar structural analogs

120
Q

how do molecules bind in active transport and undergoes what to allow translocation of membrane to other side of membrane

A

binds reversibly at specific site, complex underdoes change in conformation which allows translocation of molecule to other side of membrane

121
Q

active transport allows cell to do what 3 things

A

accumulate compounds essential for growth

remove waste products

be protected against toxins

122
Q

what do uptake and efflux transporters do in active transport

A

uptake transporters allow drug to accumulate

efflux removes drug from cell

123
Q

what is endocytosis

what is it degraded in and how is it released by cell

A

drug is taken up by cell in vesicles

degraded by lysosomes and released by cells via exocytosis

124
Q

is endocytosis energy dependent

A

yes

125
Q

what drugs are facilitated by endocytosis

A

drugs may be quite large >1000Da

126
Q

what are the 3 types of endocytosis and explain them

A

pinocytosis = small material and resulting vesicles

phagocytosis = ingest larger materials

receptor mediated endocytosis = specific molecules need to bind and be recognized by receptor on cell surface

127
Q

what is filtration in transport

A

molecules passing through fenestrations/pores

128
Q

most drugs pass through cells to cross biological barriers except at which 2 places and what does filtration there allow

A

blood capillaries - fenestrations allow rapid exchange between blood and interstitial fluid

glomerular capillaries - extremely porous allowing passage of all plasma constituents except macromolecules

129
Q

what factor of molecules is a limitation for filtration transport

A

size - large molecules are too large to diffuse and will be excluded from interstitial fluid

130
Q

filtration is what kind of a process and relies on what

A

passive process

relies on pressure gradient

131
Q

can drugs be transported by a combo of transport mechanisms

A

yes

132
Q

what must drugs be to travel via carrier mediated transport

A

must closely resemble endogenous substrates

303 MEDIMAGE (14 decks)

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