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PSYC 462 > Ch. 1 Principles of Psychopharmacology > Flashcards

Ch. 1 Principles of Psychopharmacology Flashcards

1
Q

Pharmacology definition

A

study of the actions and effects of drugs on living organisms.

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2
Q

what are we primarily studying in pharmacological studies?

A

binding affinity of drugs to different important functional proteins in the body
‘stickiness’

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3
Q

what subdivisions of pharmocology evolved from the development of synthetic drugs?

A

pharmacist
medicinal chemist
neuropsychopharmacology

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4
Q

pharmacist definition

A

one whoprescribes medicinal drugs and knows the effects, side effects and contraindications

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5
Q

medicinal chemist definition

A

one who creates molecules that bind to targets in the body/brain

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6
Q

neuropsychopharmacology definition

A

one who identifies chemical substances that act on the nervous system to alter behaviour

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7
Q

what are the primary goals of neuropsychopharmacology

A

understand the neural basis of ‘normal behaviour’
identify causes/treatments of behavioural abnormalities in psychiatric illnesses

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8
Q

what are the two subdivisions of neuropsychopharmacology

A

neuropharmacology
psychopharmacology

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9
Q

neuropharmacology definition

A

study of drug-induced changes in nervous system cell functioning
more cellular level vs behavioural

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10
Q

psychopharmacology definition

A

study of drug-induced changes in mood, thinking, and behaviour
more behavioural level vs cellular

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11
Q

drug action definition

A

molecular change produced when drug binds to a receptor/target

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12
Q

drug effect definition

A

alterations in physiological/psychological function induced by drug action

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13
Q

example of the drug action and effect of cocaine

A

action; blocks monoamine transporters
effect; increases self-esteem, reduces apetite, etc.

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14
Q

true or false; drug action and effect occur in the same location

A

false, action could happen in a completely different spot than the effect

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15
Q

true or false; different drugs can have the same effect through different actions

A

true

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16
Q

therapeutic vs side effect

A

desired physical or behavioural effect from the drug vs all the other possible effects

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17
Q

what is the relationship between balances in the body/brain and use of drugs?

A

drugs for therapeutic functions are fixing an existing imbalance, but in turn will cause an imbalance in another area that was fine before

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18
Q

how can we control the side effects of drugs on the body’s homeostatis

A

through proper dosing

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19
Q

specific effects definition

A

physiological/biochemical interaction of drug with target site that always happens

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20
Q

non-specific effect definition

A

effect based on unique characteristics of an individual

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21
Q

what characteristics can influence non-specific effects?

A

drug-taking background
mood
expectations of effect
perceptions

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22
Q

placebo effect definition

A

non-specific effect based on your expectations of the drugs effect

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23
Q

pharmacokinetics definition

A

factors that contribute to bioavailability

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24
Q

bioavailability definition

A

amount of drug free to bind at target sites

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25
Q

what are the 5 main factors of bioavailability

A

route of administration
absoprtion/distribution
binding
inactivation
excretion

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26
Q

what other factors besides bioavailability influence the drug effect?

A

speed of the drug reaching the target
prior drug use

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27
Q

routes of drug administration

A

oral
injection
inhalation

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28
Q

oral administration characteristics

A

most popular method
absorbed in gut circulation
resistant to stomach acid enzymes
slow

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29
Q

what factors affect oral drug administration

A

amount of food in stomach
rate stomach empties
physical activity

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30
Q

first-pass metabolism definition

A

chemicals/molecules in the gut first filtered by the liver before entering the bloodstream

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31
Q

why do we have first-pass metabolism?

A

to break down any potential harmful chemicals before they can cause us harm

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32
Q

what effect does first-pass metabolism have on drugs?

A

render drug inactive by breaking down, need high does to overcome liver
render active through metabolite, must be taken orally

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33
Q

injection administration characteristics

A

delivered directly to bloodstream
fastest method
greater risk of overdose
can also be subcutaneous or intramuscular
know exactly what dose you get

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34
Q

difference between intravenous and subcutaneous/intramuscular

A

slower and more even absorption

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35
Q

inhalation administration characteristics

A

absorbed through lungs
irritates nasal passage/lungs

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36
Q

what physical aspects affects the absorption rate of a drug?

A

route of administration
vehicle used
fluid in individual (size, sex affect this)

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37
Q

what chemical aspect affects the absorption rate of a drug?

A

rate of passage through cell membranes

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38
Q

what molecules pass through cell membranes the best and with what mechanism

A

lipid soluble compounds
passive diffusion

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39
Q

what are lipid soluble compounds?

A

hydrophobic molecules

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40
Q

examples od lipid soluble compounds

A

steroids
diacetylmorphine (heroine)

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41
Q

how long does it take a drug to makes its way through the whole body through the blood stream?

A

1-2 minutes

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42
Q

what is the blood brain barrier?

A

separation of brain capillaries from CSF that surrounds the brain

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43
Q

special characteristics of brain capillaries

A

no clefts/pinocyotic sites
no non-lipid soluble molecules can enter
surrounded by glial feet
surrounded by CSF

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44
Q

another name for glial feet

A

astrocytes

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45
Q

weak areas of the blood brain barrier

A

area prostrema
median eminence
parts of hypothalamus

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46
Q

why is the BBB weak around the area prostrema

A

vomit center, needs to sense noxious molecules in blood

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47
Q

why is the BBB weak around the median eminence

A

needs to release neurohormones into the blood

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48
Q

why is the BBB weak around parts of the hypothalamus?

A

so it can access contents of the blood to look for bad/infectious molecules

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49
Q

what does pharmacodynamics encompass?

A

physiological and biochemical interactions of drug molecules with target receptors

50
Q

what are characteristics of drug clearance

A

metabolites of drugs area excreted through urine
mostly excreted according to first order kinetics
quantified by their half life

51
Q

what are first-order kinetics?

A

the exponential clearing of drugs from the system

52
Q

why is drug clearance exponential

A

enzymes that break down the drug are more abundant than the drug and therefore their removal is concentration dependent

53
Q

what are zero-order kinetics?

A

linear removal rate of a drug because metabolism enzymese are supersaturated with it

54
Q

half-life definition

A

time required to remove 50% of the drug in system

55
Q

what are the different classes of biotransformation for drug clearance?

A

Phase 1
Phase 2

56
Q

phase 1 definition

A

removal of drug through oxidation, reduction, or hydrolysis

57
Q

how does phase 1 biotransformation work?

A

ionizes the drug which makes it less active and therefore more readily excreted
sometimes leads to another active form of the drug

58
Q

example of a drug that is converted to another active form after phase 1 biotransformation

A

Diazepam (valium) becomes Oxazepam

59
Q

phase 2 definition

A

removaal of drug through conjugation (attaching drug to other small molecule)

60
Q

how does phase 2 biotransformation work?

A

additional molecule ionizes the drug and therefore makes it more readily excreted

61
Q

which type of biotraansformation is non-synthetic?

A

phase 1

62
Q

which type of biotraansformation is synthetic?

A

phase 2

63
Q

True of False: drugs must go through phase 1 and 2 biotrnaformtations to be inactive and secreted

A

False; different drugs will need one, the other, or both in either order to be excreted

64
Q

factors that modify biotransformation capacity:

A

induction/inhibition of metabolism enzymes
drug competition
genetic polymorphisms

65
Q

how does induction/inhibition of metablism enzymes affect biotransformations?

A

less or more metabolism enzymes will determine how much drug gets cleared

66
Q

how does drug competition affect biotransformations?

A

drugs that use the same enzymes to metabolise will compete for them if in the body at the same time, therefore prolonging taken dose

67
Q

how do genetic polymorphisms affect biotransformations?

A

genetics determine how well the drug-metabolizing enzymes work

68
Q

receptor definition

A

proteins on/in cells. all drugs bind to some kind

69
Q

ligand definition

A

molecule that binds to a receptor with some selectivity

70
Q

endogenous ligand definition

A

molecule produced by the body that binds to a receptor

71
Q

drug affinity definition

A

concentration of drug needed to achieve a certain amount of binding

72
Q

affinity definition

A

amount of attraction between ligand and receptor

73
Q

what is the relationship between drug affinity and drug concentration

A

drugs with higher affinity will need lower concetrations in the blood stream to achieve maximal binding

74
Q

drug efficacy definition

A

how well the ligand initiates a biological action upon binding to receptor

75
Q

true or false: drug affinity and efficacy have no established relationship and are more or less independent

A

true

76
Q

drug potency definition

A

absolute amount of ligand necessary to produce a specific effect

77
Q

what is ED50

A

measure of drug potency using dose needed to produce 50% of maximal response
can vary depending on effect
may also be point where 50% of population experiences a therapeutic effect

78
Q

what are the two dose-response functions possible?

A

sigmoidal shape (most common)
biphasic shape

79
Q

threshold dose definition

A

smallest dose that produces a measurable effect

80
Q

maximum response definition

A

assumes all receptors are occupied

81
Q

what causes a drug to have biphasic effect?

A

higher concentrations of the drug lose receptor selectivity and therefore use other receptors that counteract effect

82
Q

what does it mean if a drug has a biphasic effect

A

higher dose range of the drug either shows no effect or opposite effect

83
Q

what is TD50

A

dose where 50% of the population experiences toxic effect

84
Q

what is the therapeutic index (TI)

A

TD50/ED50

85
Q

metabotropic receptor

A

ligand binding changes the shape of the receptor causing biological action through secondary messengers

86
Q

ionotropic receptor

A

ligand binding changes configuration to open ion channel

87
Q

which type of receptor has the fastest effects?

A

ionotropic receptors

88
Q

what are the two types of ligand-receptor binding

A

temporary
probabilistic

89
Q

temporary ligand-receptor binding

A

after ligand separates, the receptor is free to bind again
affinity determines how long they’re together

90
Q

probabilistic ligand-receptor binding

A

likelihood of ligand binding is influenced by other factors

91
Q

factors affecting probilistic ligand-receptor binding

A

how many ligands are available
how sticky the ligand is for the receptor
competition with other molecules

92
Q

up-regulation of receptors

A

increase in number/sensitivity of receptors in response to absence of ligands

93
Q

down-regulation of receptors

A

reduces number of receptors/sensitivity after chronic activation

94
Q

drug selectivity

A

degree to which a drug binds to a particular receptor compared to other receptors

95
Q

true or false: some drugs only selective bind to one type of receptor

A

false; no drug is truly selective and selectivity is relative

96
Q

what is the relationship between drug selectivity and dose?

A

higher doses cause loss in selectivity

97
Q

agonist

A

best fit and high efficacy in receptor that produces biological effect

98
Q

partial agonist

A

mediocre fit and intermediate efficacy in receptor causing a less potent effect

99
Q

what can a partial agonist be used for?

A

prevent excessive activation of agonist in situations where an antagonist could have negative effects

100
Q

inverse agonists

A

initiate action opposite to that produced by agonist

101
Q

indirect agonist

A

has same effect as agonist but does not interact with a receptor directly

102
Q

how can an indirect agonist affect the receptor?

A

release more NT
increase binding of NT to receptor (positive allosteric modulator)

103
Q

competitive antagonists

A

fit receptor but produce no cellular effect (low efficacy)
in competition with the agonist/endogenous ligands

104
Q

noncompetitive antagonist

A

reduces agonist effect indirectly
e.g. mess with 2nd messenger, block ion channel, etc

105
Q

how do competitive antagonists shift the dose response curve?

A

shift the curve up or down

106
Q

how do non-competitive antagonists shift the dose response curve?

A

change the shape, usually preventing maximal effect

107
Q

physiological antagonism

A

two drugs counteract each other’s effects through opposite mechanisms

108
Q

additive effects

A

two drugs causing the same effect add together

109
Q

potentiation

A

combination of two drugs produces effects much greater than the sum of their individual effects

110
Q

example of two drugs that cause potentiation

A

benzodiazepine and alcohol in their repiratory effects

111
Q

examples of functional antagonism/potentiation

A

physiological antagonism
additive effects
potentiation

112
Q

drug tolerance definition

A

diminished response to a drug after repeated exposure
body’s response to being brought out of homeostasis

113
Q

cross tolerance

A

tolerance to one drug diminishes the effectiveness of another drug withe similar mechanisms

114
Q

characteristics of drug tolerance

A

reversible
dependent of dose/frequency and environment
can occur rapidly, slowly, or never
spans many different mechanisms

115
Q

acute tolerance

A

tolerance after a single administration

116
Q

metabolic tolerance (drug-dispositional)

A

body becomes more efficient at metabolizing, therefore reducing drug that makes it to target tissue

117
Q

functional tolerance (pharmacodynamics)

A

changes at drugs site of action, usually involving receptor sensitivity to the ligand

118
Q

example of drug with effects that build tolerance at different rates

A

opiods:
tolerance to euphoric effects builds rapidly
tolerance to respiratory supression builds slowly

119
Q

behavioural tolerance

A

pavlovian conditioning makes brain associate the drug effects with the context they occur in

120
Q

conditioned tolerance

A

tolerance is maximal when drug is given in environments similar to those where drug effects previously experienced

PSYC 462 (11 decks)

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