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Addiction > Test 1 > Flashcards

Test 1 Flashcards

1
Q

What are the four basic processes in the branch of pharmacology called pharmacokinetics?

A

Absorption, distribution, metabolism, and elimination

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2
Q

What is bioavailability?

A

How much of the drug that is administered actually reaches its target

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3
Q

What is pharmacokinetics?

A

A description of the time course of a drug’s actions (the time of onset and duration of effects)

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4
Q

What are the two general categories in which drugs can be administered

A

Enteral and Parenteral routes

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5
Q

What is an enteral route?

A

When an administered drug involves the gastrointestinal tract

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6
Q

What is a parenteral route?

A

When an administered drug does not involve the gastrointestinal tract

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7
Q

What are the two types of enteral routes of drug administration?

A

Orally & rectally

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8
Q

What are the four type of parenteral routes of drug administration?

A

Injection, Inhalation, Skin absorption, and mucous membrane absorption

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9
Q

How long does it take for 75% of an orally administered psychoactive drug to be absorbed into the blood stream

A

1-3 hours after administration

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10
Q

What are the three disadvantages to oral administration of drugs

A

Can cause vomiting and stomach distress, hard to measure how much of the drug is being absorbed into the blood stream, stomach acid can destroy some drugs before they are absorbed.

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11
Q

What are two popular explanations for why inhalation is a popular method of drug administration?

A
  1. Lung tissues have a large surface area with lots of blood flow allowing for rapid absorption into the blood stream (within seconds). 2. Drugs administered through inhalation can have a faster onset than drugs administered intravenously.
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12
Q

Which drug administration method allows for slow, continuous absorption of the drug over hours or days

A

Transdermal skin patches

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13
Q

What is an advantage of the slow nature of the transdermal skin patches

A

it can minimize the side effects that are associate with rapid rises and falls in plasma concentrations of drugs.

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14
Q

What are the three ways that injection can be used as a way of drug administration

A

intravenous, intramuscular, subcutaneous

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15
Q

What are two ways that injection drug administration is better than oral drug administration

A

faster and more accurate

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16
Q

What are three disadvantages of drug administration by injection

A
  1. Too fast to respond to an unexpected drug reaction or overdose. 2. requires sterile techniques. 3. Once a drug is administered it can’t be recalled.
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17
Q

Which method of drug administration is the most dangerous of all and why?

A

Intravenous because of too rapid injection, allergic reactions, drugs that are not soluble enough which can cause blood clots

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18
Q

What are two types of intramuscular injections

A
  1. fairly rapid onset and short duration of action or 2. Slow onset and prolonged action
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19
Q

Once a drug is absorbed into the blood stream how quickly is it distributed through the circulatory system?

A

Within 1 minute

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20
Q

What is first pass metabolism

A

Drug metabolizing enzymes break down a drug in the GI tract or liver before the drug enters the blood

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21
Q

What are the four types of membranes that affect drug distribution?

A

Cell membranes, capillary membranes, blood brain barrier, and placental barrier

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22
Q

The cell membrane is important for the passage of drugs from and to which three parts of your body

A

from the stomach and intestines into the bloodstream, from the fluid surrounding tissues cells into the interior of those cells, from the interior of cells back into body water, from kidney into bloodstream

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23
Q

What are two words for the pores in capillaries

A

clefts or fenestra

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24
Q

What are the pores in capillaries for

A

allowing the passage of small molecules between blood and body tissues

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25
Q

What affects the rate that drug molecules enter specific body tissue

A

the rate of blood flow through the tissue and how easily the drug molecules can pass through capillary membranes

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26
Q

What are two factors that determined the speed of a drug entering the brain

A

the size of the drug molecule and its lipid (fat) solubility

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27
Q

What are the four routes that a drug can leave the body

A

kidneys, lung, bile, skin

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28
Q

What are the two main functions of the kidneys

A

it excretes most of our body’s metabolic products and it closely regulates substance levels in our blood

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29
Q

What are nephrons

A

functional units consisting of a knot of capillaries (glomerulus) located on the outside of the kidney

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30
Q

What is a glomerulus

A

a knot of capillaries in your kidneys

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31
Q

What is the Bowman’s capsule?

A

the opening of a nephron that fluid flows and filters out of our capillaries

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32
Q

What does the liver do in terms of drug termination?

A

it enzymatically biotransforms drug into metabolites that are less fat soluble, less capable of being reabsorbed, and then are more capable of being excreted in our urine

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33
Q

What is cross-tolerance

A

When taking one drug increases metabolic enzymes for a different drug making someone more tolerant to the second drug

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34
Q

What are three reasons knowing time course of drug action is important

A

predicting the optimal dosage and dose intervals, maintaining optimal drug levels over periods of time, and determine the time needed to eliminate the drug

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35
Q

How long does it take for a drug to leave your body

A

6 half lives

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36
Q

What is first order elimination

A

it is when the metabolic rate of a drug is constant fraction of the amount of drug that is found in plasma instead of a constant amount of the drug per hour

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37
Q

What is zero order elimination

A

It is a pattern of drug elimination that consists of a constant amount of drug being metabolized every hour

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38
Q

How long does it take to reach steady state and when is it achieved

A

6 half lives. It is achieved when the amount of drug administered is equal to the amount of drug being eliminated

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39
Q

Is steady state dependent on the dose

A

no

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40
Q

What happens in metabolic tolerance

A

more enzyme is available to metabolize a drug as a result of enzyme induction

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41
Q

What is cellular-adaptive to pharmacodynamic tolerance

A

When more of a drug is needed to reach the same effect due to receptors becoming less sensitive to the drug or due to the brain down regulating the amount of available receptors

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42
Q

What is a better word for withdrawal (from bad drugs)

A

abstinence syndrome

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43
Q

What is a better word for withdrawal from drugs like medication where the person isn’t addicted

A

discontinuation syndrome

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44
Q

What causes the “side effects” phenomenon

A

drugs are binding to receptors that aren’t the target

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45
Q

What is an example of an enzyme family found in the Cytochrome P450 class

A

CYP-1, CYP-2, CYP-3

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46
Q

What is hepatic metabolism

A

the rate that the drug starts to consistently metabolize

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47
Q

What is the rapid redistribution phase

A

when you first take a drug and there is too much of a drug entering to be metabolized at the same rate

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48
Q

What is the folding on the outside of the brain called

A

convolution

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49
Q

What are the pre central and post central gyrus

A

Tw big fissures that are separated from the central sulcus

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50
Q

What happens when you damage the temporal lobe

A

changes in perceptions and emotions

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51
Q

What does the parietal lobe deal with

A

our representation of the outside world in our brain (somatosensory representation)

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52
Q

What are the two types of molecules of membranes

A

hydrophilic and hydrophobic

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53
Q

When the hydrophilic heads join together what do they make

A

a phospholipid bilayer.

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54
Q

Explain the gradient of ions inside and outside the cell

A

there is a higher gradient of positively charged sodium ions outside the cells and less positive potassium ions inside the cell

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55
Q

What controls the gradient on membranes

A

the sodium potassium ion pump

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56
Q

What is the space between myelin on the axon

A

nodes of ranvier

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57
Q

What are schwann cells

A

cells that makes up myelin.

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58
Q

What is saltatory connection

A

When a message hops from node of ranvier to node of ranvier instead of down the entire axon.

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59
Q

What is the development of schwann cells

A

cell develop in the embryo, continue through childhood, and peak in adolescence

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60
Q

What is one explanation why adolescence have such fast responses

A

the have a lot of myelin (aka faster messages)

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61
Q

What is the on switch for exocytosis

A

calcium

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62
Q

What is endocytosis

A

when calcium brings neurotransmitters back into presynaptic vesicles

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63
Q

What are the three defining characteristics of neurotransmitters

A
  1. Substance must be present within the presynaptic neutron (in vesicles)
  2. Substance must be released in response to presynaptic depolarization and release must be calcium dependent. 3. Specific receptors for the substance must be present on the post synaptic side
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64
Q

What are three neurotransmitters in the catecholamines class

A

Dopamine, epinephrine, and norepinephrine

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65
Q

What are two neurotransmitters in the biogenic amines class

A

serotonin and histamine

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66
Q

What is a major excitatory neurotransmitter

A

Glutamate

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67
Q

What is a major inhibitory neurotransmitter

A

GABA

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68
Q

What are three types of receptors that Glutamate binds to

A

NMDA, AMPA, and Kainate receptors

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69
Q

What is psychodynamics

A

The study of the biochemical and physiological effect of drugs and the mechanisms of drug action and its relationship with drug concentration and effect

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70
Q

What are two things that can be ligands

A

neurotransmitters and drugs

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71
Q

What is a word for membrane-spanning proteins

A

receptors

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72
Q

What are receptors made up of

A

7 or 12 alpha helical coils

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73
Q

Part of every protein is most attractive to a drug because of what?

A

its charge

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74
Q

What two things are at the end of every protein

A

an n and c terminus

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75
Q

What makes the segment of an ion channel

A

4 coils

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76
Q

Instead of lock and key what is the other way a neurotransmitter can flow in

A

coils move to open ion channels

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77
Q

What are carrier proteins

A

proteins that carry small organic molecules across membranes

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78
Q

What is responsible for picking up left over neurotransmitter and bringing it back into the presynaptic cell

A

carrier proteins

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79
Q

Where are G Protein-Coupled receptors found

A

on the postsynaptic side

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80
Q

Once a G protein-coupled receptor is activated what happens?

A

it induces the release of intracellular g protein

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81
Q

What is the role of a G Protein receptor

A

it controls enzymatic activity on the post synaptic side

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82
Q

What is different between G proteins and other ligands

A

it is slower and activates more receptors. G protein messengers modulate multiple ion channels

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83
Q

What are the two types of receptor effects

A

up-regulation and down-regulation

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84
Q

Where is the enzyme AcH found

A

in the synaptic cleft

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85
Q

where is the enzyme MAO found

A

presynaptic neuron

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86
Q

What is drug receptor specificity?

A

How well the ligand fits in the receptor

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87
Q

What happens when drug receptor specificity is high

A

drug effect is more potent.

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88
Q

What happens when drug receptor specificity is low

A

side effects

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89
Q

What does potency of drug refer to

A

the absolute number of drug molecules required to elicit a response

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90
Q

What does efficacy of drug refer to

A

the maximum effect obtainable

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91
Q

What does variability of drug refer to

A

individual differences in drug response

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92
Q

What does ED50 stand for

A

what the effective dose for 50% of the population is

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93
Q

What does LD50 stand for

A

what the lethal dose for 50% of the population is

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94
Q

What is a therapeutic index and how is it calculated

A

the size of the window between helping people and not killing anyone. It is calculate by the LD50 divided by the ED50

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95
Q

How do placebo effects work in a physiological way

A

the psychological relief lowers the stress response and releases opioids. Opioids have pain killing effects.

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96
Q

What are 4 reasons the placebo effect is increasing and what is the one Terry suggested

A

increase of drug taking, increase in options and efficacy, cultural by in (doctor only gives stuff that works),, and most importantly; our understanding, knowledge, and documentation of diseases increases so we assume our treatment increases too.

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97
Q

Alcohol is the __ most commonly used psychoactive substance in the world?

A

second

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98
Q

What is proof in terms of alcohol

A

An old way of defining level of a drink. It is double what the actual alcohol content is in a given drink

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99
Q

How much alcohol is in 1 drink equivalent

A

1/3 of an ounce of 100% ethanol

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100
Q

How much alcohol can our body break down in 1 hour

A

0.015 g

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101
Q

Where is alcohol absorbed in the body

A

20% in the stomach and 80% in the intestines

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102
Q

Where in the body is alcohol metabolized

A

85% in the liver and 15% by first pass metabolism

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103
Q

How much of alcohol is metabolized by alcohol dehydrogenase

A

95%

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104
Q

Why does alcohol get more absorbed by the body on an empty stomach

A

Because food can absorb the alcohol too

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105
Q

What does alcohol dehydrogenase break ethanol down into

A

Acetaldehyde

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106
Q

What is rate limiting step

A

In terms of alcohol it is how much can be broken down in one hour

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107
Q

What does acetaldehyde get broken into

A

Aldehyde dehydrogenase

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108
Q

After acetaldehyde is broken down what is left of the ethanol

A

Water, carbon dioxide, and energy

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109
Q

What happens when you have to much acetaldehyde in your body

A

You feel really sick

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110
Q

What is disulifram

A

A drug that inhibits aldehyde dehydrogenase thus increasing the amount of acetaldehyde and makes people feel sick when the drink alcohol. It is used in the treatment of addiction

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111
Q

How long does it take to metabolize one drink equivalent

A

1 hour

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112
Q

What four factors do we need to know in order to calculate blood alcohol content

A

How much you consumed, when you consumed it, your BMI, and gender

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113
Q

A blood alcohol content of what is considered intoxicated

A

0.08

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114
Q

For what blood alcohol content are driving incidents pretty lenient

A

0.05-0.08

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115
Q

What are the 7 reasons that alcohol is such a popular drug of abuse and which are the ones terry suggested

A 
Legal,
Accessible,
Supported in culture,
Socially acceptable,
Positive effects,
Terry suggested
The dosage is clear & it’s cheap
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116
Q

What are two reasons that women get more drunk when given the same amount of alcohol as men

A

Men have a higher muscle to fat ratio which creates a vascular compartment (more blood). Women also have less gastric alcohol dehydrogenase in their stomach

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117
Q

What is the unitary hypothesis of action of alcohol? In which ways is it right? In which ways is it wrong?

A

Suggests that alcohol affects every part of the body and is completely non discriminatory. It is right because it affects so many different parts, so it still holds true. It is wrong because it affects different parts of the body differently

118
Q

On a neuronal level which systems do alcohol affect?

A

GABA systems, glutamate systems, intracellular transduction processes

119
Q

Which glutamate receptor does alcohol block

A

NMDA

120
Q

What happens when alcohol binds to an NMDA receptor short term? Long term?

A

It lowers the levels of excitation in the brain. Long term this can lead to an up regulation of NMDA receptors. When someone stops drinking it can lead to hyperexcitability (cause seizures)

121
Q

What is acamprosate

A

It is a drug for alcoholics stopping alcohol that blocks the NMDA receptor in a similar way that alcohol would so there isn’t a hyperexcitability when quitting

122
Q

What does alcohol do to GABA receptors

A

It activates gaba receptors (binds to) leading to a state of inhibition

123
Q

What accounts for the stimulatory effects of alcohol? What accounts for the depressant effects?

A

The psychological component accounts for the stimulatory effects of alcohol where the pharmacological nature of alcohol accounts for the depressant effects

124
Q

What GABA receptor does alcohol bind to and what does this lead to

A

Alcohol binds to the GABA A which leads to a relief of panic and anxiety

125
Q

What accounts for the positive reinforcing effects of alcohol

A

The binding of alcohol on GABA A receptors

126
Q

What is one possible reason why offspring of alcoholics also become alcoholics

A

They have a deficit in opioid release

127
Q

What two neurotransmitters does alcohol promote the release of that are associated with feel good effects (not GABA)

A

Dopamine and opioids

128
Q

What is naltrexone

A

A drug used for alcoholics quitting alcohol to prevent cravings by blocking opioid release

129
Q

What serotonin receptors does alcohol bind to

A

Serotonin 2-3 receptors on dopaminergic neurons in the nucleus accumbens

130
Q

What kind of effect does alcohol have on serotonin receptors

A

Agonistic action

131
Q

What happens when antagonistic drugs block serotonin 2-3 receptors on dopaminergic receptors in the nucleus accumbens

A

It reduces the alcohol intake

132
Q

What happens with chronic binding of cannabinoid receptors with anandamide

A

Down regulation of cannabinoid receptors

133
Q

If someone has a down regulation of cannabinoid receptors and they stop drinking

A

Hyperactive receptor activation (craving)

134
Q

What does it mean to say that alcohol causes depressed respiration

A

Your breathing is shallow and there is more pausing between your breaths

135
Q

Alcohol causes a reduction in circulatory function what does this mean

A

Less blood flow, most of the blood flow goes to your core. This causes dilated blood vessels

136
Q

Why is some alcohol good for you and what alcohol and how often

A

Increase in high density lipoprotein and good cholesterol. This is from dry unsweetened red wine 2-3 drinks 2-3 times a week

137
Q

After what BAC are there behavioural changes

A

0.4

138
Q

How much more likely are you to get into an accident when your BAC reaches above 0.4 or more

A

4x

139
Q

What are two possible reasons that violent crimes happen from alcohol

A

Activation of GABA reduces anxiety, and activation of the dopamine system reduces impulse control and increases aggression

140
Q

What two things happen when we depress the glutamate system

A

Impaired cognitive function and alcohol myopia

141
Q

What are the three types of tolerances or dependence

A

Metabolic tolerance, tissue/functional tolerance, homeostatic tolerance (new normal in environment)

142
Q

What are 4 acute side effects of drinking

A

Drug-induced dementia, cloud sensorium, impair judgement, anterograde amnesia

143
Q

What are three cognitive side effects of chronic alcohol use

A

Delusions, hallucinations, and periods of unconsciousness

144
Q

What are physical side effects of chronic alcohol use

A

Liver damage (cirrhosis), dementia (nerve damage in the brain), digestive problems (pancreatitis, chronic gastritis)

145
Q

Someone with a collection of chronic symptoms of alcohol is said to have

A

Wernicke Korsakoff Syndrome

146
Q

What is the first step of cirrhosis

A

Fatty markers on your liver; this is reversible

147
Q

What is the second step in cirrhosis

A

Liver fibrosis is characterized by scar tissue. Recovery is possible (it stops getting worse) but the scar tissue remains

148
Q

What is the third step of cirrhosis

A

Actual cirrhosis which can kill you unless you get a liver transplant. The growth of connective tissue destroys liver cells

149
Q

How many birth defects are from teratogens

A

10%

150
Q

What are some examples of teratogenic agents (4)

A

Ethyl alcohol, ionizing radiation, lithium, thalidomide

151
Q

What is thalidomide

A

A morning sickness pill for pregnant women that caused them to give birth to babies with stunted limbs

152
Q

What are considered to be critical times during fetal development (times where the mother should especially not drink)

A

During the development of the spinal cord certain brain regions

153
Q

What percent of alcohol women give birth to babies with fetal alcohol syndrome? What is the prevalence?

A

30-50% and 3-5 births per 1000

154
Q

What amount of alcohol is said to increase the likelihood of FAS

A

3 ounces of absolute alcohol (5 drink equivalents) daily

155
Q

What are 5 (non-facial) features of FAS

A
  1. Low IQ
  2. Mental dysfunction (relative)
  3. Smaller body growth
  4. Certain facial features
  5. Must have been exposed to alcohol as a fetus
156
Q

What are the three areas of impairment in those with FAS

A

Neurological (nerve function), functional (how well the brain works as a unit), and structural (brain structure)

157
Q

What are three brain differences in FAS brains versus normal

A

FAS is 30% smaller, more holes and gaps, and less grooves

158
Q

What are 9 facial features of people with FAS

A
  1. Microcephaly
  2. Palperbal fissure
  3. Epicanthal folds
  4. Flat midface
  5. Low nasal bridge
  6. Philtrum
  7. Thin upper lip
  8. Micrognathia
  9. Distinct ears
159
Q

What is microcephaly

A

A small head circumference that those with FAS have

160
Q

What is palperbal fissure

A

Short opening of eye that those with FAS have

161
Q

What is philitrum

A

Indistinct vertical grooves between nose and mouths

162
Q

What is micrognathia

A

Small jaw

163
Q

What is distinct between ears of those with FAS and those without it

A

The curve at the top part of the outer ear is underdeveloped

164
Q

What is ARND

A

Alcohol related nerve development disorder

165
Q

What is alcohol related nerve development disorder

A

Occurs when the mother drinks during critical periods but not that much. Baby looks normal but may experience behavioural issues later on in life

166
Q

What is the prevalence of ARND

A

1 out of 100

167
Q

What are the four characteristics of ARND

A

Lower IQ, aggressive behaviour, hyperactivity, and sensory behaviour

168
Q

When treating alcoholism what are the three things we need to take into account

A

Comorbidity with other psychiatric disorders, withdrawal symptoms, and reverse the acute effects of alcohol

169
Q

What is a benzodiazepine

A

A drug that increases GABA

170
Q

What are the four side effects of benzodiazepines

A

Sedation, can become dependent, interacts with alcohol (affects respiration), and psychomotor deficits

171
Q

Why are antipsychotic drugs used for the treatment of alcoholism what is the problem with using them

A

They reduce delirium and hallucination. The problem is they lower the threshold for seizures

172
Q

What are anticonvulsants

A

Drugs that are used in place of benzos. They are newer agents with fewer side effects. Effective in treating alcoholism, example is topomax.

173
Q

What is a problem with anticonvulsants

A

Can contribute to liver and pancreatic problems and they have other side effects

174
Q

What is antabuse

A

An alcohol sensitizing drug that makes you feel sick

175
Q

What is acamprosate

A

A gaba agonist that inhibits glutamate. It mimics what alcohol does neurologically without the cognitive and behavioural consequences

176
Q

What is naltrexone

A

An opioid antagonist. Reduces the pleasurable effects of alcohol

177
Q

What is the best treatment option for alcoholism

A

Naltrexone and acamprosate

178
Q

What is wellubutrin

A

A dopaminergic drug that activates the dopamine reward pathway. It is helpful in treating alcoholics with depression but can be used for alcoholics without depression

179
Q

What type of serotinergic drugs help with alcoholism

A

SSRIs, 5HT1a agonists like BuSpar, and 5HT3a antagonists like zofran

180
Q

What are the two types of drinkers

A

Type A: Later onset drinkers

Type B: early onset drinkers

181
Q

Who is more responsive to placebo, type A or type B drinkers

A

Type B (early onset)

182
Q

What type of drinker is more responsive to sertraline

A

Type A (late onset)

183
Q

Does drinking making you dumb?

A

Long term chronic exposure is associated with alcohol will decrease your cognitive ability

184
Q

What are four resources schools provide to help control student drinking

A

Preventative campaigns, counselling, campus regulation, enforcement (tickets)

185
Q

What age counts as early exposure to alcohol

A

17-18

186
Q

What is the average age of first exposure to alcohol

A

13.6

187
Q

What is the average age people become regular users of alcohol

A

15-16

188
Q

What does drinking earlier on in life make you more prone to dependence

A

Dopamine receptor sensitivity is high in youth, the adolescent brain is more responsive in the ventral tegemental area

189
Q

What are the four disadvantages of measuring blood alcohol content directly

A

Invasive, painful, data lag, costly

190
Q

How does alcohol get into our breath

A

Alcohol in our blood flows through alveolar sAcs in our lungs. A lot of blood flows though these sAcs

191
Q

What is the ratio of BAC to BrAc

A

0.8:0.2

192
Q

What are three types of machines that are used as breathylzers

A

Breathalyzer, intoxilyzer, and alco sensor

193
Q

What does a breathylizer do

A

Initiates a chemical reaction that will produce a colour change

194
Q

What is an intoxilyzer

A

An infrared spectroscopy

195
Q

What does an alcosensor do

A

Fuels 3 or 4 chemical reactions that will fuel certain cells

196
Q

What detects the change in reaction in a breathylzer

A

The photo cells and a meter

197
Q

What is in the glass vial in a breathylzer

A

A chemical substrate

198
Q

What are the pros and cons to a breathylizer

A

Pros: fast and easy to use. Cons: there is room for interpretation

199
Q

Explain the process of the chemical reaction for breathylizers

A

You drink and sulfuric acid helps with alcohol acquisition (draws the alcohol from your breath), silver nitrate acts as a catalyst (speeds up the reaction without adding anything to it). The reactive agent which is the thing that actually detects change in alcohol is potassium dichromate. Those three things make a reaction that will consist of chromium sulfate that will turn green if there is alcohol

200
Q

What two factors can be a source of error for breathylzer

A

Breathing rate and temperature

201
Q

How does air temperature effect a breathylzer

A

Reaction is faster in warmer weather and slower in colder

202
Q

When will you score higher on the BrAc; running or resting

A

Resting because you’re giving your body more time to let blood flow through you’re alveolar sAcs

203
Q

What are three myths of the breathylzer

A

You can disguise the odour with food, you can use gum to lower BrAC, mouthwash can be used to trick the system

204
Q

What was the first barbiturate and when was it introduced

A

Phenobarbital in 1912

205
Q

How are barbiturates classified?

A

By their chemical structure

206
Q

How many receptor sites will you find on a barbiturate nucleus

A

3

207
Q

What is interesting about the chemical composition of barbiturates

A

If something has the basic structure of a barbiturate classified as a barbiturate but it won’t necessarily act like one

208
Q

How selective is neuronal depression from barbiturates? What does it suppress

A

Non specific and it suppresses post synaptic diffuse brain stem neuronal pathways in the brain stem and the cerebral cortex

209
Q

How do barbiturates work

A

Effects electrical and metabolic activity. Which decreases the whole brain glucose metabolism

210
Q

Are barbiturates increasing inhibition or decreasing excitation

A

Both

211
Q

What are the receptors on a barbiturate nucleus called

A

R1,R2,R3

212
Q

What do barbiturates do with glutamate

A

They are glutamate NMDAR antagonists (decrease the amount of excitation)

213
Q

What is the effect of barbiturates acting on the Glutamate NMDAR receptor

A

amnesia due to the changes in glutamatergic transmission. There is lower blood flow in brain regions that are associated with memory.

214
Q

What do barbiturates do with GABA

A

barbiturates enhance GABA transmission at GABAa receptors. This influx accounts for an increase in chloride (which are negative ions)

215
Q

What effects of barbiturates occur because of the binding on the GABAa receptor

A

the sedative-hypnotic and aesthetic properties.

216
Q

Is there more than one binding site on GABAa receptors

A

Yes

217
Q

What are some of the different molecules that kind bind to GABAa receptors

A

Barbiturates, Benzos, and GABA etc.

218
Q

What is the problem with barbiturates in terms of binding on GABAa receptors

A

When barbiturates bind to GABA receptors they open the ion channel to let chloride in without any form of GABA.

219
Q

What can high doses of barbiturates lead to?

A

Amnesia and a state of demensia

220
Q

To be classified as demented one would have to experience 5 out of 12 symptoms; list 5

A

Sensorium (orientation to time and place), Affect, Mental content (fund of knowledge), Intellectual function (ability to reason), and Insight and judgement.

221
Q

What is the half life of barbiturates?

A

They have a wide range of half lives ranging from 3 minutes to 120 hours.

222
Q

Are barbiturates fast or slow acting in terms of absorption?

A

Fast

223
Q

Why is the effect of barbiturates on sleep interesting

A

They put you to sleep but you don’t sleep well because you don’t get normal amounts of REM sleep.

224
Q

Do barbiturates cross the BBB

A

yes

225
Q

It is very dangerous to mix barbiturates with alcohol. Why?

A

It will affect your respiration and it is very easy to overdose.

226
Q

What are some of the major problems with barbiturates?

A

Lethal overdoses, narrow therapeutic ranges, quick tolerance, lots of dangerous interactions

227
Q

Are barbiturates Teratogens

A

we don’t really know. we do see still birth, low birthweight, and low IQ but we aren’t positive.

228
Q

Are barbiturates like a truth serum

A

Not really. They just calm you down much like alcohol and just make you more likely to open up

229
Q

What are non-barbiturates

A

Drugs that don’t have the same structure of traditional barbiturates but act the same way

230
Q

What are three examples of non-barbiturates

A

Soma, Quaalude, and Paraldehyde

231
Q

What is Quaalude

A

a drug that is a non-barbiturate that was very popular in the 70-80’s as a date rape drug and was a anaphrodisiac

232
Q

How are general anesthetics administered

A

inhalation or intravenous injection

233
Q

What are three examples of general anesthetics

A

nitrous oxide, isoflurane, and halothane

234
Q

How do injectable anesthetics make you feel

A

don’t make you feel good or bad they just numb you

235
Q

What is Gamma Hydroxybutyrate

A

It is a precursor to GABA that is found in us endogenously. It is a strong central nervous depressant.

236
Q

What are some of the things that GHB is used for

A

as an aesthetic, for sleep disorders (narcolepsy), and for alcohol detox.

237
Q

What does synergistic mean

A

It interacts with something and makes the effect of the first substance a lot stronger (almost in an unpredictable way)

238
Q

What does GHB do in terms of neurotransmitters

A

increases the amount of dopamine which then activates the dopamine reward pathway (positive reinforcement)

239
Q

What does it mean to say that GHB is a Schedule I and a III Drug?

A

It is illicit but also used for therapeutic purposes.

240
Q

Is GHB a solid, liquid, or gas

A

liquid

241
Q

How long does it take GHB to reach peak plasma levels

A

30-75 minutes

242
Q

What is the half life of GHB

A

30 Minutes

243
Q

What is the urine detectability of GHB

A

It has low detectability

244
Q

What were anti epileptic drugs originally used for? What else are they used for?

A

Hyper-excitability/Seizures. They are also prescribed for sleep or bipolar disorder

245
Q

What is a better name for anti epileptic drugs

A

neuromodulators.

246
Q

What molecule do neuromodulators chemically mimic

A

barbiturates

247
Q

Are neuromodulators or antiepileptics teratogens

A

Yes.

248
Q

When neuromodulator drug users get pregnant what is generally done?

A

Mother goes on a lower dose that is divided up daily. Or the mother will just go off the medication if the seizures aren’t that bad.

249
Q

What kind of drug is a benzodiapine

A

anti-convulsant, sedative, and anxiolytic

250
Q

What is the most widely used psychotherapeutic drug in the world

A

benzos

251
Q

What are three examples of benzos

A

valium, librium, xanax

252
Q

What does the basic chemical structure of Benzos look like

A

3 hexagons (2 on top one on bottom to the right)

253
Q

What major neurotransmitter do Benzos target

A

GABA

254
Q

What is different about the effect that barbiturates and benzos have on GABA receptors

A

barbiturates surpass the need for GABA. Benzos simply facilitate the binding of GABA

255
Q

What brain region to benzos target

A

limbic system

256
Q

What brain regions are associated with anxiety, panic, and the behavioural response to fear

A

amygdala, orbitofrontal cortex, and the insula

257
Q

What happens when you block GABAergic function in the amygdala

A

a person will be more anxious

258
Q

What makes one benzo different from another

A

the rate of metabolism, active metabolites, and the plasma half lives

259
Q

How long does it usually take to reach a peak benzo blood content

A

1 hour

260
Q

What is interesting about the metabolites of benzos

A

They exert their own effect. They are active substances

261
Q

What is the active metabolite of Valium

A

nordiazepam

262
Q

What is the half life of nordiazepam

A

60 hours

263
Q

Are benzos fast or short acting

A

the can be either or intermediate acting

264
Q

Why do we care about active metabolites (2)

A

they could still be in your body by your second dose and they interact with other things

265
Q

What are the four subgroups of people/drug users

A

adults 16-65, seniors 65+, adolescents, and infants

266
Q

What subgroup of people is really sensitive to benzos

A

the elderly

267
Q

what is the problem with the elderly taking benzos

A

benzos can lead to cognitive dysfunction and most elderly people are already prone to it.

268
Q

How do benzos that are complete agonists act on receptors

A

facilitates GABA binding and moderates anxiolytic effects in the amygdala, orbitiofrontal cortex, and the insult.

269
Q

Why do benzos still have side effects if they only target GABA receptors

A

they are activating GABA receptors that are not in the amygdala, orbitofrontal cortex, or insult.

270
Q

What are 4 effects of taking benzos

A

mental confusion and amnesia, muscle relaxant effect, antiepileptic actions, and behavioural rewarding effects

271
Q

What accounts for the behavioural rewarding effects of benzos

A

the binding at the ventral tegementum and the nucleus accumbens

272
Q

What is a better option for long term treatment of sleep issues or anxiety

A

anti-depressants

273
Q

Why do benzos affect the effectiveness of CBT

A

CBT requires you to think and benzos are cognitive inhibitors.

274
Q

If you were using benzos for surgical procedures which type would you use for a short surgery? a long one?

A

Short= midalozam Long=lorazepam

275
Q

What makes rohypnol a good drug for rape (2)

A

80% is absorbed not immediately and the detectability is lost after 72 hours

276
Q

what are the four advantages of benzos

A

fast, anxiolytic effect, less side effects than barbiturates, and patient acceptance

277
Q

What are the disadvantages of benzos

A

effects psychomotor abilities, impaired learning and cognition, reduce alertness, dependency, paradoxical agitation

278
Q

Are benzos teratogens

A

yes

279
Q

What happens when a mother does benzos in the first trimester? near birth?

A

in first trimester the baby will have fetal abnormalities. Near birth the baby can be dependent on benzos and will have floppy-infant syndrome

280
Q

What is flumazenil

A

A GABAa antagonist that blocks GABA binding by binding with the receptor.

281
Q

What is flumazenil used for

A

benzo overdose

282
Q

Whats another world for 2nd generation anxiolytics

A

nonbenzos

283
Q

What type of non benzo is ambien

A

a partial agonist

284
Q

What is ambien used for

A

insomnia

285
Q

What receptor does ambient bind to

A

GABA1a

286
Q

What function of sleep does Sonata aid with? Ambient?

A

Sonata helps with sleep onset and ambient helps with sleep maintenance

287
Q

Where in the brain would serotingergic anxiolytics have their effect

A

5HT1 receptors in the hippocampus, septum, and the amygdala

288
Q

What is the binding of the 5-HT1a receptor associated with

A

anxiety regulation

289
Q

What is BuSpar

A

An anxiolytic that works by facilitating the binding of serotonin at 5HT1a receptors

290
Q

What are the advantages and disadvantages of BuSpar

A

Advantage: low amnesia, no additive effects with alcohol. Problem is the grapefruit issue

Addiction (2 decks)

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