CH1 Flashcards

1
Q

The study of the actions of drugs and their effects on living organisms

A

Pharmacology

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2
Q

Prescribes medicinal drugs, knows therapeutic effects, side effects, contraindications

A

pharmacist

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3
Q

Creates molecules that bind to targets in body/brain

A

medicinal chemist

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4
Q

Identifies chemical substances that act on the nervous system to alter behaviour

A

Neuropsychopharmacology

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5
Q

Neuropsychopharmacology uses ______ agents as _____ to gain an understanding of the neurobiology of behaviour. It ranges from ______ (studies in cells/animals) to _____ (working with human patient populations)

A

chemical, probes, pre-clinical, clinical

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6
Q

Primary goals of neuropsychopharmacology

A
  1. understand the neural/neurochemical basis of normal behaviour, 2. identify the causes / treatments of behaviour abnormalities in psychiatric illnesses
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7
Q

Study of drug induced changes in the nervous system cell functioning

A

neuropharmacology

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8
Q

emphasizes drug-induced changes in mood, thinking and behaviour

A

psychopharmacology

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9
Q

molecular changes produced when a drug binds to a receptor/target

A

drug action

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10
Q

alterations in physiological/psychological functions induced by drug action

A

drug effect

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11
Q

the drug-receptor interaction produces desired physical or behavioural changes

A

therapeutic effects

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12
Q

Physiological/biochemical interactions of drug with target site in living tissue; what the drug does to the body that nothing else can do (e.g. alcohol depressing neural activity)

A

specific effects

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13
Q

based on unique characteristics of individual background, mood, expectation of effect, perceptions (e.g. alcohol can augment pleasant moods or amplify unpleasant ones, placebo effect)

A

nonspecific effects

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14
Q

Factors that contribute to bioavailability

A

pharmacokinetics

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15
Q

the amount of drug free to bind at target sites

A

bioavailability

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16
Q

five main factors contributing to bioavailability

A
  1. route of administration, 2. absorption / distribution, 3. binding, 4. inactivation, 5. excretion
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17
Q

drug effect also depends on how ____ the drug reaches its target, and ____/______ of prior drug use

A

rapidly, frequency, history

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18
Q

Oral administration is the most popular method, because it is ____, ______ and economical. The disadvantages are that it is _____, has variable _____, and _____ levels. Drugs taken orally are absorbed from the ____ into circulation. Some are absorbed from the ____ but most are taken up through the ____ ____. These drugs must be resistant to destruction by ____ ____ and _____.

A

safe, self-administered, slow, absorption, plasma, gut, stomach, small intestine, stomach acid, enzymes

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19
Q

through oral administration, the factors that influence absorption include

A
  1. amount/type of food in the stomach, 2. rate that stomach empties, 3. physical activity
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20
Q

potentially harmful chemicals (taken orally) pass through the liver (via portal vein) where they are chemically altered

A

first pass metabolism

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21
Q

the liver may render some drugs _______, with the need to administer by _____ or in higher doses. Other drugs are metabolized into _______ forms by the liver and need to be taken orally to have an effect

A

inactive, injection, active

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22
Q

Injection routes deliver drugs into the _____, which bypass the _____. The advantages are that it is ______, and has the most accurate blood _______. The disadvantages is that there is the greatest risk of _______.

A

bloodstream, first pass metabolism, fast, concentration, overdose

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23
Q

______ or _____ methods of intake allow absorption through capillaries around skin/muscles which allow for _____ and _____ absorption

A

subcutaneous, intramuscular, slow, even

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24
Q

_______ is when the drug is absorbed rapidly from the lungs, which can provide ______ and _____ to nasal passages and ______

A

inhalation, irritation, damage, lungs

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25
Q

The route of administration alters the rate of ____ and ___ ____ of a drug. The ______ that a drug is dissolved in can impact how long it stays in the system after _______. Other factors affecting absorption are the _____ and ____ of an individual

A

absorption, blood levels, vehicle, injection, size, sex

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26
Q

An intramuscular injection delivered through oil takes _______ to take effect, and drug concentration in the blood declines at a ______ rate. The same method but using ______, results in faster _______ and ______

A

longer, slower, saline, drug concentration, decline

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27
Q

A larger person has more ______ to dilute a drug, thus needing a higher dose. Likewise, women tend to have less, and a different physiology, resulting in a ______ dose required

A

body fluid, lower

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28
Q

A key factor determining plasma brain drug levels is the rate of passage by molecules through _____ ______. These prevent most molecules from passing through unless they are ______ soluble. ______ are completely soluble.

A

cell membranes, lipid, steroids

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29
Q

_______ (heroin), is more lipid soluble than _____, has a more rapid ____ and more potent reinforcing properties

A

diacetylmorphine, morphine, onset

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30
Q

Once the drug is in the bloodstream, it is carried throughout the body within _______ minutes. Capillaries in the body are very _____, allowing drugs to enter tissues regardless of _____ ______. However, in the brain, many substances would have ____ effects on brain function if permitted to cross freely. The ______ reduces the diffusion ______ particles, as brain capillaries have no _____/_________ sites.

A

1-2, porous, lipid solubility, disruptive, blood brain barrier, ionized, clefts, pinocytotic

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31
Q

fills the subarachnoid space around the brain, spinal cord, ventricles, and canals

A

cerebrospinal fluid

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32
Q

separates the brain capillaries and the CSF

A

blood brain barrier

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33
Q

extensions of glial cells that surround brain capillaries restricting movement of non lipid soluble molecules

A

astrocytes

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34
Q

Molecules that the brain needs, such as _____, are carried in via _______ ______ transport

A

glucose, carrier mediated

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35
Q

For a drug to be centrally active, it typically needs to be ________ _____, in both _____ and _____ environments

A

lipid soluble, acidic, basic

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36
Q

Some regions have a weaker blood brain barrier, such as the ____ ______ “vomit center” which senses noxious molecules in the blood, the _____ ___, which release neurohormones in the blood, and parts of the ______

A

area postrema, median eminence, hypothalamus

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37
Q

the elimination of drugs via bio-transformation and metabolites and excretion

A

drug clearance

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38
Q

Drug clearance is usually _______ (first order kinetics), meaning only a small fraction of _____ ____ are occupied, so the rate is __________

A

exponential, clearance sites, concentration dependent

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39
Q

time required to remove 50% of the drug in the system

A

half life

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40
Q

some drugs are eliminated via ______ kinetics, meaning that they are eliminated at a constant rate regardless of concentration. This occurs when drug levels are ____, and routes of metabolism elimination are _______ (aka more ____ than there are clearance sites)

A

zero order, high, supersaturated, molecules

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41
Q

_____ and ____ have relatively long half lives, while _____ ____ and ____ have shorter half lives, requiring frequent administration

A

caffeine, ibuprophen, nicotine, morphine, cocaine

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42
Q

Most biotransformation occurs in the ______. The _______ enzyme family are responsible for oxidizing most psychoactive drugs, making them easier to _____

A

liver, cytochrome P450, clear

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43
Q

modification of a drug by oxidation, reduction, or hydrolysis (non-synthetic); involving adding or removing an ion from the molecule to convert it into a less lipid soluble or less active form

A

phase I

44
Q

sometimes, phase I metabolism can convert the drug molecule to another _____ form, resulting in a _____ ____ effect

A

active, long lasting

45
Q

involves conjugation (synthetic) attachment of the drug to other small molecules (glucuronide, sulfate, or methyl groups), which ionizes them and makes them inactive; synthesizes a new molecule

A

phase II

46
Q

Some drugs are metabolized directly by ___ /____, while others need ____ phase I or III processes

A

I, II, multiple

47
Q

Inactive metabolites are excreted via the ____ or ______.

A

kidneys, bile

48
Q

factors that modify biotransformation capacity (3)

A
  1. induction or inhibition of enzymes involves in metabolism, by other drugs, foods, etc., 2. drug competition (when two drugs require the same enzyme to be metabolized), 3. genetic polymorphisms for drug metabolizing enzymes create individual differences
49
Q

molecule that binds to a receptor with some selectivity

A

ligand

50
Q

amount of attraction between ligand and receptor (concentration needed to achieve a certain amount of firing)

A

affinity

51
Q

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

A

drug efficacy

52
Q

absolute amount of ligand necessary to produce a specific effect, typically measured by ED50

A

drug potency

53
Q

the dose needed to produce 50% of the maximal response

A

ED50

54
Q

one individual ____ of a drug may have a different ______ than another effect of the same drug

A

effect, potency

55
Q

_____ curves describe the extent of the effect produced by a given drug. Most curves are _____ shaped. However, some drugs have _____ effects, with a lower dose having one effect, and a higher dose having ___ effect, or even the _____ effect. This is because the drug starts to lose _____, and other parts of the brain are activated that _____ the main effect

A

dose-response, sigmoidal, biphasic, no, opposite, selective, counteract

56
Q

smallest dose that produces a measurable effect

A

threshold dose

57
Q

when all the receptors for the drug are occupied

A

maximum response

58
Q

the dose causing 50% of the population to experience a toxic effect

A

TD50

59
Q

TD50/ED50; want this to be high to prevent toxic effect at low doses

A

therapeutic index

60
Q

the range from ED50 –> the TD for a specific toxic effect

A

margin of safety

61
Q

Most drugs do not ___ into neurons, but instead act on ___ receptors, such as metabotropic or ionotropic receptors

A

pass, surface

62
Q

receptors that activate second messengers inside the cell, causing multiple effects; is generally slow

A

metabotropic receptor

63
Q

second messenger effects

A
  1. modulates ion channels to affect neural activity, 2. alters protein synthesis, 3. alters metabolism of the cell
64
Q

Receptors that open or close ion channels, allowing ions to flow through and excite or inhibit neurons; generally fast

A

ionotropic receptors

65
Q

ligand receptor interactions are ______, meaning after the ligand separates, the receptor is free to ____ again. It is also ______, meaning the likelihood of the ligand binding to a receptor is influenced by the number of molecules of the ______, the ______ of the ligand, and the presence of _______

A

temporary, bind, probabilistic, ligand, affinity, competitors

66
Q

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

A

up-regulation

67
Q

reduced number of receptors or their sensitivity after chronic activation

A

down-regulation

68
Q

the degree to which a drug binds to a particular receptor compared to other receptors; is relative, and highly dependent on dose

A

drug sensitivity

69
Q

have the best chemical fit and high efficacy, readily attaches to the receptor and produces a biological effect; may even activate or stick to the receptor better than the endogenous ligand

A

receptor agonists

70
Q

binds to the receptor and activates it but is less potent and have intermediate efficacy

A

partial agonists

71
Q

initiates an action opposite to that produced by the agonist; ultimate effect is similar to an antagonist, but pharmacological action is different

A

inverse agonists

72
Q

drugs that can also act like agonists, even though they may not directly interact with a particular receptors e.g. by increase NT synthesis or release, or increasing binding of NT to a receptor

A

indirect agonist

73
Q

fit receptors but produce no cellular effect (low efficacy); reduces the effect of the endogenous ligand; ability to block the effect of the agonist depends on the relative concentrations and affinities of the two drugs

A

competitive antagonists

74
Q

reduces the agonist effect by 1. binding to the receptor at a site other than the agonist binding site (e.g. blocking an ion channel) 2. interfering with second messengers initiated by the agonist, 3. disturbing the cell membrane supporting the receptor (protein shape changed)

A

noncompetitive antagonists

75
Q

competitive agonists essentially reduce the _____ of an agonist, and shift the dose response curve so that a ____ dose of agonist is needed to achieve the maximal effect. Adding enough agonist can ____ the effects of the antagonist. However, noncompetitive agonists change the _____ of the dose response curve, often preventing the agonist from achieving _____ effect, irrespective of how much more agonist is added

A

potency, higher, block, shape, maximal

76
Q

two drugs interacting to reduce the effectiveness of both drugs

A

physiological antagonism

77
Q

When two drugs combine to produce effects that are equal to both drug effectiveness combined

A

additive effects

78
Q

when the combination of 2 drugs produces effects greater than the sum of their individual effects; important for things like sedation

A

potentiation / synergistic interactions

79
Q

diminished response to a drug after repeated exposure; dose of drug must be increased to achieve the same magnitude of effect

A

drug tolerance

80
Q

when tolerance to one drug diminishes effectiveness of another drug, usually ones that work on similar mechanisms

A

cross tolerance

81
Q

4 characteristics of drug tolerance

A
  1. reversible when drug use stops, 2. dependent on dose/frequency of drug use and drug taking environment, 3. may occur rapidly, after long periods of use, or never, 4. multiple forms explained by different mechanisms
82
Q

repeated drug use reduces the amount of the drug available at the target tissue; by more efficient metabolism (more enzymes), so less drug gets to site of action

A

metabolic (drug dispositional) tolerance

83
Q

when changes in cell function compensates for repeated drug exposure; typically occurs at the site in the brain or body where the drug exerts its effects (ex. downregulation)

A

functional (pharmacodynamic) tolerance

84
Q

When the brain makes associations between the drug effects and the context where they occurred; and tolerance is maximal when the drug is given in environments similar to those previously experienced; results in body increasing or decreasing response in advance to prepare for the drug effects

A

behavioural tolerance / conditioned tolerance

85
Q

The placebo effect can result in both ______ evaluation of relief and measurable ____ changes

A

subjective, physiological

86
Q

Increase in anxiety and influence in treatment outcome when having negative expectations

A

nocebo effect

87
Q

movement of drug from the site of administration to the blood circulation

A

absorption

88
Q

____ administration may avoid some first pass metabolism, but has irregular _____.

A

rectal, absorption

89
Q

injection used for lab animals that involves injection into the abdominal wall; has rapid effects but variable absorption

A

intraperitoneal (IP)

90
Q

______ ____ of drugs have local drug effects

A

topical application

91
Q

______ (under the tongue), _______, or _______ administration all by pass the first pass metabolism

A

sublingual, intranasal, transdermal

92
Q

_______ (into CSF), ______, _____ or ______ (into ventricles) are central routes of administration

A

intrathecal, epidural infusion, intracranial, infusion pump

93
Q

Plasma levels of drug gradually fall as it is absorbed into the ____, _____, _____ ___, etc. Drug _______ reduces the drug concentrations in organs again to restore equilibrium and ____ the action of the drug

A

heart, brain, kidneys, liver, redistribution, terminate

94
Q

inactive sites where no measurable biological effect is initiated (e.g. fat and bone)

A

drug depots/silent receptors

95
Q

____ binding reduces the concentration of drug at the sites of ______. It results in prolonged drug time in the body

A

depot, action

96
Q

Drug clearance depends on (3)

A
  1. biotransformation rate, 2. depot binding, 3. storage in fat reservoirs
97
Q

the range of plasma drug levels that are high enough to be effective, but not so high that they cause toxic or intolerable side effects

A

therapeutic window

98
Q

the desired blood concentration of drug achieved when the absorption / distribution phase is equal to the metabolism / excretion phase

A

steady state plasma level

99
Q

enzymes on the smooth ER that lack specificity, like cytochrome P450

A

microsomal enzymes

100
Q

baseline receptor function in the absence of ligand

A

constitutive activity

101
Q

receptor proteins for a given drug or NT have different characteristics in different target tissues

A

receptor subtypes

102
Q

The dose of drug that is lethal to 1% of the population compared with the dose that is lethal therapeutically effective in 99% of the population (LD1/ED99)

A

safety factor index

103
Q

when tolerance develops after a single administration

A

acute tolerance

104
Q

a physiological state in which the body adapts to the chronic presence of a drug and elicits a drug-specific withdrawal syndrome if the drug is abruptly stopped

A

physical dependence

105
Q

tasks learned under the influence of a psychoactive drug may subsequently be performed better in the drugged state than in the nondrugged state and vis versa

A

state dependent learning

106
Q

enhancement of particular drug effects after repeated administration of the same dose of drug

A

sensitization

107
Q

sensitization is ___ dependent, can have ______ effects, and be conditioned; more sensitization in a ____ environment, and persist for long periods of ______

A

dose, cross-sensitization, novel, abstinence