Test 1 Flashcards

(290 cards)

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
What affects the rate that drug molecules enter specific body tissue
the rate of blood flow through the tissue and how easily the drug molecules can pass through capillary membranes
26
What are two factors that determined the speed of a drug entering the brain
the size of the drug molecule and its lipid (fat) solubility
27
What are the four routes that a drug can leave the body
kidneys, lung, bile, skin
28
What are the two main functions of the kidneys
it excretes most of our body's metabolic products and it closely regulates substance levels in our blood
29
What are nephrons
functional units consisting of a knot of capillaries (glomerulus) located on the outside of the kidney
30
What is a glomerulus
a knot of capillaries in your kidneys
31
What is the Bowman's capsule?
the opening of a nephron that fluid flows and filters out of our capillaries
32
What does the liver do in terms of drug termination?
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
33
What is cross-tolerance
When taking one drug increases metabolic enzymes for a different drug making someone more tolerant to the second drug
34
What are three reasons knowing time course of drug action is important
predicting the optimal dosage and dose intervals, maintaining optimal drug levels over periods of time, and determine the time needed to eliminate the drug
35
How long does it take for a drug to leave your body
6 half lives
36
What is first order elimination
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
37
What is zero order elimination
It is a pattern of drug elimination that consists of a constant amount of drug being metabolized every hour
38
How long does it take to reach steady state and when is it achieved
6 half lives. It is achieved when the amount of drug administered is equal to the amount of drug being eliminated
39
Is steady state dependent on the dose
no
40
What happens in metabolic tolerance
more enzyme is available to metabolize a drug as a result of enzyme induction
41
What is cellular-adaptive to pharmacodynamic tolerance
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
42
What is a better word for withdrawal (from bad drugs)
abstinence syndrome
43
What is a better word for withdrawal from drugs like medication where the person isn't addicted
discontinuation syndrome
44
What causes the "side effects" phenomenon
drugs are binding to receptors that aren't the target
45
What is an example of an enzyme family found in the Cytochrome P450 class
CYP-1, CYP-2, CYP-3
46
What is hepatic metabolism
the rate that the drug starts to consistently metabolize
47
What is the rapid redistribution phase
when you first take a drug and there is too much of a drug entering to be metabolized at the same rate
48
What is the folding on the outside of the brain called
convolution
49
What are the pre central and post central gyrus
Tw big fissures that are separated from the central sulcus
50
What happens when you damage the temporal lobe
changes in perceptions and emotions
51
What does the parietal lobe deal with
our representation of the outside world in our brain (somatosensory representation)
52
What are the two types of molecules of membranes
hydrophilic and hydrophobic
53
When the hydrophilic heads join together what do they make
a phospholipid bilayer.
54
Explain the gradient of ions inside and outside the cell
there is a higher gradient of positively charged sodium ions outside the cells and less positive potassium ions inside the cell
55
What controls the gradient on membranes
the sodium potassium ion pump
56
What is the space between myelin on the axon
nodes of ranvier
57
What are schwann cells
cells that makes up myelin.
58
What is saltatory connection
When a message hops from node of ranvier to node of ranvier instead of down the entire axon.
59
What is the development of schwann cells
cell develop in the embryo, continue through childhood, and peak in adolescence
60
What is one explanation why adolescence have such fast responses
the have a lot of myelin (aka faster messages)
61
What is the on switch for exocytosis
calcium
62
What is endocytosis
when calcium brings neurotransmitters back into presynaptic vesicles
63
What are the three defining characteristics of neurotransmitters
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
64
What are three neurotransmitters in the catecholamines class
Dopamine, epinephrine, and norepinephrine
65
What are two neurotransmitters in the biogenic amines class
serotonin and histamine
66
What is a major excitatory neurotransmitter
Glutamate
67
What is a major inhibitory neurotransmitter
GABA
68
What are three types of receptors that Glutamate binds to
NMDA, AMPA, and Kainate receptors
69
What is psychodynamics
The study of the biochemical and physiological effect of drugs and the mechanisms of drug action and its relationship with drug concentration and effect
70
What are two things that can be ligands
neurotransmitters and drugs
71
What is a word for membrane-spanning proteins
receptors
72
What are receptors made up of
7 or 12 alpha helical coils
73
Part of every protein is most attractive to a drug because of what?
its charge
74
What two things are at the end of every protein
an n and c terminus
75
What makes the segment of an ion channel
4 coils
76
Instead of lock and key what is the other way a neurotransmitter can flow in
coils move to open ion channels
77
What are carrier proteins
proteins that carry small organic molecules across membranes
78
What is responsible for picking up left over neurotransmitter and bringing it back into the presynaptic cell
carrier proteins
79
Where are G Protein-Coupled receptors found
on the postsynaptic side
80
Once a G protein-coupled receptor is activated what happens?
it induces the release of intracellular g protein
81
What is the role of a G Protein receptor
it controls enzymatic activity on the post synaptic side
82
What is different between G proteins and other ligands
it is slower and activates more receptors. G protein messengers modulate multiple ion channels
83
What are the two types of receptor effects
up-regulation and down-regulation
84
Where is the enzyme AcH found
in the synaptic cleft
85
where is the enzyme MAO found
presynaptic neuron
86
What is drug receptor specificity?
How well the ligand fits in the receptor
87
What happens when drug receptor specificity is high
drug effect is more potent.
88
What happens when drug receptor specificity is low
side effects
89
What does potency of drug refer to
the absolute number of drug molecules required to elicit a response
90
What does efficacy of drug refer to
the maximum effect obtainable
91
What does variability of drug refer to
individual differences in drug response
92
What does ED50 stand for
what the effective dose for 50% of the population is
93
What does LD50 stand for
what the lethal dose for 50% of the population is
94
What is a therapeutic index and how is it calculated
the size of the window between helping people and not killing anyone. It is calculate by the LD50 divided by the ED50
95
How do placebo effects work in a physiological way
the psychological relief lowers the stress response and releases opioids. Opioids have pain killing effects.
96
What are 4 reasons the placebo effect is increasing and what is the one Terry suggested
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.
97
Alcohol is the __ most commonly used psychoactive substance in the world?
second
98
What is proof in terms of alcohol
An old way of defining level of a drink. It is double what the actual alcohol content is in a given drink
99
How much alcohol is in 1 drink equivalent
1/3 of an ounce of 100% ethanol
100
How much alcohol can our body break down in 1 hour
0.015 g
101
Where is alcohol absorbed in the body
20% in the stomach and 80% in the intestines
102
Where in the body is alcohol metabolized
85% in the liver and 15% by first pass metabolism
103
How much of alcohol is metabolized by alcohol dehydrogenase
95%
104
Why does alcohol get more absorbed by the body on an empty stomach
Because food can absorb the alcohol too
105
What does alcohol dehydrogenase break ethanol down into
Acetaldehyde
106
What is rate limiting step
In terms of alcohol it is how much can be broken down in one hour
107
What does acetaldehyde get broken into
Aldehyde dehydrogenase
108
After acetaldehyde is broken down what is left of the ethanol
Water, carbon dioxide, and energy
109
What happens when you have to much acetaldehyde in your body
You feel really sick
110
What is disulifram
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
111
How long does it take to metabolize one drink equivalent
1 hour
112
What four factors do we need to know in order to calculate blood alcohol content
How much you consumed, when you consumed it, your BMI, and gender
113
A blood alcohol content of what is considered intoxicated
0.08
114
For what blood alcohol content are driving incidents pretty lenient
0.05-0.08
115
What are the 7 reasons that alcohol is such a popular drug of abuse and which are the ones terry suggested
``` Legal, Accessible, Supported in culture, Socially acceptable, Positive effects, Terry suggested The dosage is clear & it’s cheap ```
116
What are two reasons that women get more drunk when given the same amount of alcohol as men
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
117
What is the unitary hypothesis of action of alcohol? In which ways is it right? In which ways is it wrong?
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
On a neuronal level which systems do alcohol affect?
GABA systems, glutamate systems, intracellular transduction processes
119
Which glutamate receptor does alcohol block
NMDA
120
What happens when alcohol binds to an NMDA receptor short term? Long term?
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
What is acamprosate
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
What does alcohol do to GABA receptors
It activates gaba receptors (binds to) leading to a state of inhibition
123
What accounts for the stimulatory effects of alcohol? What accounts for the depressant effects?
The psychological component accounts for the stimulatory effects of alcohol where the pharmacological nature of alcohol accounts for the depressant effects
124
What GABA receptor does alcohol bind to and what does this lead to
Alcohol binds to the GABA A which leads to a relief of panic and anxiety
125
What accounts for the positive reinforcing effects of alcohol
The binding of alcohol on GABA A receptors
126
What is one possible reason why offspring of alcoholics also become alcoholics
They have a deficit in opioid release
127
What two neurotransmitters does alcohol promote the release of that are associated with feel good effects (not GABA)
Dopamine and opioids
128
What is naltrexone
A drug used for alcoholics quitting alcohol to prevent cravings by blocking opioid release
129
What serotonin receptors does alcohol bind to
Serotonin 2-3 receptors on dopaminergic neurons in the nucleus accumbens
130
What kind of effect does alcohol have on serotonin receptors
Agonistic action
131
What happens when antagonistic drugs block serotonin 2-3 receptors on dopaminergic receptors in the nucleus accumbens
It reduces the alcohol intake
132
What happens with chronic binding of cannabinoid receptors with anandamide
Down regulation of cannabinoid receptors
133
If someone has a down regulation of cannabinoid receptors and they stop drinking
Hyperactive receptor activation (craving)
134
What does it mean to say that alcohol causes depressed respiration
Your breathing is shallow and there is more pausing between your breaths
135
Alcohol causes a reduction in circulatory function what does this mean
Less blood flow, most of the blood flow goes to your core. This causes dilated blood vessels
136
Why is some alcohol good for you and what alcohol and how often
Increase in high density lipoprotein and good cholesterol. This is from dry unsweetened red wine 2-3 drinks 2-3 times a week
137
After what BAC are there behavioural changes
0.4
138
How much more likely are you to get into an accident when your BAC reaches above 0.4 or more
4x
139
What are two possible reasons that violent crimes happen from alcohol
Activation of GABA reduces anxiety, and activation of the dopamine system reduces impulse control and increases aggression
140
What two things happen when we depress the glutamate system
Impaired cognitive function and alcohol myopia
141
What are the three types of tolerances or dependence
Metabolic tolerance, tissue/functional tolerance, homeostatic tolerance (new normal in environment)
142
What are 4 acute side effects of drinking
Drug-induced dementia, cloud sensorium, impair judgement, anterograde amnesia
143
What are three cognitive side effects of chronic alcohol use
Delusions, hallucinations, and periods of unconsciousness
144
What are physical side effects of chronic alcohol use
Liver damage (cirrhosis), dementia (nerve damage in the brain), digestive problems (pancreatitis, chronic gastritis)
145
Someone with a collection of chronic symptoms of alcohol is said to have
Wernicke Korsakoff Syndrome
146
What is the first step of cirrhosis
Fatty markers on your liver; this is reversible
147
What is the second step in cirrhosis
Liver fibrosis is characterized by scar tissue. Recovery is possible (it stops getting worse) but the scar tissue remains
148
What is the third step of cirrhosis
Actual cirrhosis which can kill you unless you get a liver transplant. The growth of connective tissue destroys liver cells
149
How many birth defects are from teratogens
10%
150
What are some examples of teratogenic agents (4)
Ethyl alcohol, ionizing radiation, lithium, thalidomide
151
What is thalidomide
A morning sickness pill for pregnant women that caused them to give birth to babies with stunted limbs
152
What are considered to be critical times during fetal development (times where the mother should especially not drink)
During the development of the spinal cord certain brain regions
153
What percent of alcohol women give birth to babies with fetal alcohol syndrome? What is the prevalence?
30-50% and 3-5 births per 1000
154
What amount of alcohol is said to increase the likelihood of FAS
3 ounces of absolute alcohol (5 drink equivalents) daily
155
What are 5 (non-facial) features of FAS
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
What are the three areas of impairment in those with FAS
Neurological (nerve function), functional (how well the brain works as a unit), and structural (brain structure)
157
What are three brain differences in FAS brains versus normal
FAS is 30% smaller, more holes and gaps, and less grooves
158
What are 9 facial features of people with FAS
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
What is microcephaly
A small head circumference that those with FAS have
160
What is palperbal fissure
Short opening of eye that those with FAS have
161
What is philitrum
Indistinct vertical grooves between nose and mouths
162
What is micrognathia
Small jaw
163
What is distinct between ears of those with FAS and those without it
The curve at the top part of the outer ear is underdeveloped
164
What is ARND
Alcohol related nerve development disorder
165
What is alcohol related nerve development disorder
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
What is the prevalence of ARND
1 out of 100
167
What are the four characteristics of ARND
Lower IQ, aggressive behaviour, hyperactivity, and sensory behaviour
168
When treating alcoholism what are the three things we need to take into account
Comorbidity with other psychiatric disorders, withdrawal symptoms, and reverse the acute effects of alcohol
169
What is a benzodiazepine
A drug that increases GABA
170
What are the four side effects of benzodiazepines
Sedation, can become dependent, interacts with alcohol (affects respiration), and psychomotor deficits
171
Why are antipsychotic drugs used for the treatment of alcoholism what is the problem with using them
They reduce delirium and hallucination. The problem is they lower the threshold for seizures
172
What are anticonvulsants
Drugs that are used in place of benzos. They are newer agents with fewer side effects. Effective in treating alcoholism, example is topomax.
173
What is a problem with anticonvulsants
Can contribute to liver and pancreatic problems and they have other side effects
174
What is antabuse
An alcohol sensitizing drug that makes you feel sick
175
What is acamprosate
A gaba agonist that inhibits glutamate. It mimics what alcohol does neurologically without the cognitive and behavioural consequences
176
What is naltrexone
An opioid antagonist. Reduces the pleasurable effects of alcohol
177
What is the best treatment option for alcoholism
Naltrexone and acamprosate
178
What is wellubutrin
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
What type of serotinergic drugs help with alcoholism
SSRIs, 5HT1a agonists like BuSpar, and 5HT3a antagonists like zofran
180
What are the two types of drinkers
Type A: Later onset drinkers | Type B: early onset drinkers
181
Who is more responsive to placebo, type A or type B drinkers
Type B (early onset)
182
What type of drinker is more responsive to sertraline
Type A (late onset)
183
Does drinking making you dumb?
Long term chronic exposure is associated with alcohol will decrease your cognitive ability
184
What are four resources schools provide to help control student drinking
Preventative campaigns, counselling, campus regulation, enforcement (tickets)
185
What age counts as early exposure to alcohol
17-18
186
What is the average age of first exposure to alcohol
13.6
187
What is the average age people become regular users of alcohol
15-16
188
What does drinking earlier on in life make you more prone to dependence
Dopamine receptor sensitivity is high in youth, the adolescent brain is more responsive in the ventral tegemental area
189
What are the four disadvantages of measuring blood alcohol content directly
Invasive, painful, data lag, costly
190
How does alcohol get into our breath
Alcohol in our blood flows through alveolar sAcs in our lungs. A lot of blood flows though these sAcs
191
What is the ratio of BAC to BrAc
0.8:0.2
192
What are three types of machines that are used as breathylzers
Breathalyzer, intoxilyzer, and alco sensor
193
What does a breathylizer do
Initiates a chemical reaction that will produce a colour change
194
What is an intoxilyzer
An infrared spectroscopy
195
What does an alcosensor do
Fuels 3 or 4 chemical reactions that will fuel certain cells
196
What detects the change in reaction in a breathylzer
The photo cells and a meter
197
What is in the glass vial in a breathylzer
A chemical substrate
198
What are the pros and cons to a breathylizer
Pros: fast and easy to use. Cons: there is room for interpretation
199
Explain the process of the chemical reaction for breathylizers
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
What two factors can be a source of error for breathylzer
Breathing rate and temperature
201
How does air temperature effect a breathylzer
Reaction is faster in warmer weather and slower in colder
202
When will you score higher on the BrAc; running or resting
Resting because you’re giving your body more time to let blood flow through you’re alveolar sAcs
203
What are three myths of the breathylzer
You can disguise the odour with food, you can use gum to lower BrAC, mouthwash can be used to trick the system
204
What was the first barbiturate and when was it introduced
Phenobarbital in 1912
205
How are barbiturates classified?
By their chemical structure
206
How many receptor sites will you find on a barbiturate nucleus
3
207
What is interesting about the chemical composition of barbiturates
If something has the basic structure of a barbiturate classified as a barbiturate but it won’t necessarily act like one
208
How selective is neuronal depression from barbiturates? What does it suppress
Non specific and it suppresses post synaptic diffuse brain stem neuronal pathways in the brain stem and the cerebral cortex
209
How do barbiturates work
Effects electrical and metabolic activity. Which decreases the whole brain glucose metabolism
210
Are barbiturates increasing inhibition or decreasing excitation
Both
211
What are the receptors on a barbiturate nucleus called
R1,R2,R3
212
What do barbiturates do with glutamate
They are glutamate NMDAR antagonists (decrease the amount of excitation)
213
What is the effect of barbiturates acting on the Glutamate NMDAR receptor
amnesia due to the changes in glutamatergic transmission. There is lower blood flow in brain regions that are associated with memory.
214
What do barbiturates do with GABA
barbiturates enhance GABA transmission at GABAa receptors. This influx accounts for an increase in chloride (which are negative ions)
215
What effects of barbiturates occur because of the binding on the GABAa receptor
the sedative-hypnotic and aesthetic properties.
216
Is there more than one binding site on GABAa receptors
Yes
217
What are some of the different molecules that kind bind to GABAa receptors
Barbiturates, Benzos, and GABA etc.
218
What is the problem with barbiturates in terms of binding on GABAa receptors
When barbiturates bind to GABA receptors they open the ion channel to let chloride in without any form of GABA.
219
What can high doses of barbiturates lead to?
Amnesia and a state of demensia
220
To be classified as demented one would have to experience 5 out of 12 symptoms; list 5
Sensorium (orientation to time and place), Affect, Mental content (fund of knowledge), Intellectual function (ability to reason), and Insight and judgement.
221
What is the half life of barbiturates?
They have a wide range of half lives ranging from 3 minutes to 120 hours.
222
Are barbiturates fast or slow acting in terms of absorption?
Fast
223
Why is the effect of barbiturates on sleep interesting
They put you to sleep but you don't sleep well because you don't get normal amounts of REM sleep.
224
Do barbiturates cross the BBB
yes
225
It is very dangerous to mix barbiturates with alcohol. Why?
It will affect your respiration and it is very easy to overdose.
226
What are some of the major problems with barbiturates?
Lethal overdoses, narrow therapeutic ranges, quick tolerance, lots of dangerous interactions
227
Are barbiturates Teratogens
we don't really know. we do see still birth, low birthweight, and low IQ but we aren't positive.
228
Are barbiturates like a truth serum
Not really. They just calm you down much like alcohol and just make you more likely to open up
229
What are non-barbiturates
Drugs that don't have the same structure of traditional barbiturates but act the same way
230
What are three examples of non-barbiturates
Soma, Quaalude, and Paraldehyde
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What is Quaalude
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
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How are general anesthetics administered
inhalation or intravenous injection
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What are three examples of general anesthetics
nitrous oxide, isoflurane, and halothane
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How do injectable anesthetics make you feel
don't make you feel good or bad they just numb you
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What is Gamma Hydroxybutyrate
It is a precursor to GABA that is found in us endogenously. It is a strong central nervous depressant.
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What are some of the things that GHB is used for
as an aesthetic, for sleep disorders (narcolepsy), and for alcohol detox.
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What does synergistic mean
It interacts with something and makes the effect of the first substance a lot stronger (almost in an unpredictable way)
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What does GHB do in terms of neurotransmitters
increases the amount of dopamine which then activates the dopamine reward pathway (positive reinforcement)
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What does it mean to say that GHB is a Schedule I and a III Drug?
It is illicit but also used for therapeutic purposes.
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Is GHB a solid, liquid, or gas
liquid
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How long does it take GHB to reach peak plasma levels
30-75 minutes
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What is the half life of GHB
30 Minutes
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What is the urine detectability of GHB
It has low detectability
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What were anti epileptic drugs originally used for? What else are they used for?
Hyper-excitability/Seizures. They are also prescribed for sleep or bipolar disorder
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What is a better name for anti epileptic drugs
neuromodulators.
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What molecule do neuromodulators chemically mimic
barbiturates
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Are neuromodulators or antiepileptics teratogens
Yes.
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When neuromodulator drug users get pregnant what is generally done?
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.
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What kind of drug is a benzodiapine
anti-convulsant, sedative, and anxiolytic
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What is the most widely used psychotherapeutic drug in the world
benzos
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What are three examples of benzos
valium, librium, xanax
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What does the basic chemical structure of Benzos look like
3 hexagons (2 on top one on bottom to the right)
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What major neurotransmitter do Benzos target
GABA
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What is different about the effect that barbiturates and benzos have on GABA receptors
barbiturates surpass the need for GABA. Benzos simply facilitate the binding of GABA
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What brain region to benzos target
limbic system
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What brain regions are associated with anxiety, panic, and the behavioural response to fear
amygdala, orbitofrontal cortex, and the insula
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What happens when you block GABAergic function in the amygdala
a person will be more anxious
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What makes one benzo different from another
the rate of metabolism, active metabolites, and the plasma half lives
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How long does it usually take to reach a peak benzo blood content
1 hour
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What is interesting about the metabolites of benzos
They exert their own effect. They are active substances
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What is the active metabolite of Valium
nordiazepam
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What is the half life of nordiazepam
60 hours
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Are benzos fast or short acting
the can be either or intermediate acting
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Why do we care about active metabolites (2)
they could still be in your body by your second dose and they interact with other things
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What are the four subgroups of people/drug users
adults 16-65, seniors 65+, adolescents, and infants
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What subgroup of people is really sensitive to benzos
the elderly
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what is the problem with the elderly taking benzos
benzos can lead to cognitive dysfunction and most elderly people are already prone to it.
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How do benzos that are complete agonists act on receptors
facilitates GABA binding and moderates anxiolytic effects in the amygdala, orbitiofrontal cortex, and the insult.
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Why do benzos still have side effects if they only target GABA receptors
they are activating GABA receptors that are not in the amygdala, orbitofrontal cortex, or insult.
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What are 4 effects of taking benzos
mental confusion and amnesia, muscle relaxant effect, antiepileptic actions, and behavioural rewarding effects
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What accounts for the behavioural rewarding effects of benzos
the binding at the ventral tegementum and the nucleus accumbens
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What is a better option for long term treatment of sleep issues or anxiety
anti-depressants
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Why do benzos affect the effectiveness of CBT
CBT requires you to think and benzos are cognitive inhibitors.
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If you were using benzos for surgical procedures which type would you use for a short surgery? a long one?
Short= midalozam Long=lorazepam
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What makes rohypnol a good drug for rape (2)
80% is absorbed not immediately and the detectability is lost after 72 hours
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what are the four advantages of benzos
fast, anxiolytic effect, less side effects than barbiturates, and patient acceptance
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What are the disadvantages of benzos
effects psychomotor abilities, impaired learning and cognition, reduce alertness, dependency, paradoxical agitation
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Are benzos teratogens
yes
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What happens when a mother does benzos in the first trimester? near birth?
in first trimester the baby will have fetal abnormalities. Near birth the baby can be dependent on benzos and will have floppy-infant syndrome
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What is flumazenil
A GABAa antagonist that blocks GABA binding by binding with the receptor.
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What is flumazenil used for
benzo overdose
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Whats another world for 2nd generation anxiolytics
nonbenzos
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What type of non benzo is ambien
a partial agonist
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What is ambien used for
insomnia
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What receptor does ambient bind to
GABA1a
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What function of sleep does Sonata aid with? Ambient?
Sonata helps with sleep onset and ambient helps with sleep maintenance
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Where in the brain would serotingergic anxiolytics have their effect
5HT1 receptors in the hippocampus, septum, and the amygdala
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What is the binding of the 5-HT1a receptor associated with
anxiety regulation
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What is BuSpar
An anxiolytic that works by facilitating the binding of serotonin at 5HT1a receptors
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What are the advantages and disadvantages of BuSpar
Advantage: low amnesia, no additive effects with alcohol. Problem is the grapefruit issue