Test 1 Flashcards
What are the four basic processes in the branch of pharmacology called pharmacokinetics?
Absorption, distribution, metabolism, and elimination
What is bioavailability?
How much of the drug that is administered actually reaches its target
What is pharmacokinetics?
A description of the time course of a drug’s actions (the time of onset and duration of effects)
What are the two general categories in which drugs can be administered
Enteral and Parenteral routes
What is an enteral route?
When an administered drug involves the gastrointestinal tract
What is a parenteral route?
When an administered drug does not involve the gastrointestinal tract
What are the two types of enteral routes of drug administration?
Orally & rectally
What are the four type of parenteral routes of drug administration?
Injection, Inhalation, Skin absorption, and mucous membrane absorption
How long does it take for 75% of an orally administered psychoactive drug to be absorbed into the blood stream
1-3 hours after administration
What are the three disadvantages to oral administration of drugs
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.
What are two popular explanations for why inhalation is a popular method of drug administration?
- 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.
Which drug administration method allows for slow, continuous absorption of the drug over hours or days
Transdermal skin patches
What is an advantage of the slow nature of the transdermal skin patches
it can minimize the side effects that are associate with rapid rises and falls in plasma concentrations of drugs.
What are the three ways that injection can be used as a way of drug administration
intravenous, intramuscular, subcutaneous
What are two ways that injection drug administration is better than oral drug administration
faster and more accurate
What are three disadvantages of drug administration by injection
- 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.
Which method of drug administration is the most dangerous of all and why?
Intravenous because of too rapid injection, allergic reactions, drugs that are not soluble enough which can cause blood clots
What are two types of intramuscular injections
- fairly rapid onset and short duration of action or 2. Slow onset and prolonged action
Once a drug is absorbed into the blood stream how quickly is it distributed through the circulatory system?
Within 1 minute
What is first pass metabolism
Drug metabolizing enzymes break down a drug in the GI tract or liver before the drug enters the blood
What are the four types of membranes that affect drug distribution?
Cell membranes, capillary membranes, blood brain barrier, and placental barrier
The cell membrane is important for the passage of drugs from and to which three parts of your body
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
What are two words for the pores in capillaries
clefts or fenestra
What are the pores in capillaries for
allowing the passage of small molecules between blood and body tissues
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
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
What are the four routes that a drug can leave the body
kidneys, lung, bile, skin
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
What are nephrons
functional units consisting of a knot of capillaries (glomerulus) located on the outside of the kidney
What is a glomerulus
a knot of capillaries in your kidneys
What is the Bowman’s capsule?
the opening of a nephron that fluid flows and filters out of our capillaries
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
What is cross-tolerance
When taking one drug increases metabolic enzymes for a different drug making someone more tolerant to the second drug
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
How long does it take for a drug to leave your body
6 half lives
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
What is zero order elimination
It is a pattern of drug elimination that consists of a constant amount of drug being metabolized every hour
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
Is steady state dependent on the dose
no
What happens in metabolic tolerance
more enzyme is available to metabolize a drug as a result of enzyme induction
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
What is a better word for withdrawal (from bad drugs)
abstinence syndrome
What is a better word for withdrawal from drugs like medication where the person isn’t addicted
discontinuation syndrome
What causes the “side effects” phenomenon
drugs are binding to receptors that aren’t the target
What is an example of an enzyme family found in the Cytochrome P450 class
CYP-1, CYP-2, CYP-3
What is hepatic metabolism
the rate that the drug starts to consistently metabolize
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
What is the folding on the outside of the brain called
convolution
What are the pre central and post central gyrus
Tw big fissures that are separated from the central sulcus
What happens when you damage the temporal lobe
changes in perceptions and emotions
What does the parietal lobe deal with
our representation of the outside world in our brain (somatosensory representation)
What are the two types of molecules of membranes
hydrophilic and hydrophobic
When the hydrophilic heads join together what do they make
a phospholipid bilayer.
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
What controls the gradient on membranes
the sodium potassium ion pump
What is the space between myelin on the axon
nodes of ranvier
What are schwann cells
cells that makes up myelin.
What is saltatory connection
When a message hops from node of ranvier to node of ranvier instead of down the entire axon.
What is the development of schwann cells
cell develop in the embryo, continue through childhood, and peak in adolescence
What is one explanation why adolescence have such fast responses
the have a lot of myelin (aka faster messages)
What is the on switch for exocytosis
calcium
What is endocytosis
when calcium brings neurotransmitters back into presynaptic vesicles
What are the three defining characteristics of neurotransmitters
- Substance must be present within the presynaptic neutron (in vesicles)
- 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
What are three neurotransmitters in the catecholamines class
Dopamine, epinephrine, and norepinephrine
What are two neurotransmitters in the biogenic amines class
serotonin and histamine
What is a major excitatory neurotransmitter
Glutamate
What is a major inhibitory neurotransmitter
GABA
What are three types of receptors that Glutamate binds to
NMDA, AMPA, and Kainate receptors
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
What are two things that can be ligands
neurotransmitters and drugs
What is a word for membrane-spanning proteins
receptors
What are receptors made up of
7 or 12 alpha helical coils
Part of every protein is most attractive to a drug because of what?
its charge
What two things are at the end of every protein
an n and c terminus
What makes the segment of an ion channel
4 coils
Instead of lock and key what is the other way a neurotransmitter can flow in
coils move to open ion channels
What are carrier proteins
proteins that carry small organic molecules across membranes
What is responsible for picking up left over neurotransmitter and bringing it back into the presynaptic cell
carrier proteins
Where are G Protein-Coupled receptors found
on the postsynaptic side
Once a G protein-coupled receptor is activated what happens?
it induces the release of intracellular g protein
What is the role of a G Protein receptor
it controls enzymatic activity on the post synaptic side
What is different between G proteins and other ligands
it is slower and activates more receptors. G protein messengers modulate multiple ion channels
What are the two types of receptor effects
up-regulation and down-regulation
Where is the enzyme AcH found
in the synaptic cleft
where is the enzyme MAO found
presynaptic neuron
What is drug receptor specificity?
How well the ligand fits in the receptor
What happens when drug receptor specificity is high
drug effect is more potent.
What happens when drug receptor specificity is low
side effects
What does potency of drug refer to
the absolute number of drug molecules required to elicit a response
What does efficacy of drug refer to
the maximum effect obtainable
What does variability of drug refer to
individual differences in drug response
What does ED50 stand for
what the effective dose for 50% of the population is
What does LD50 stand for
what the lethal dose for 50% of the population is
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
How do placebo effects work in a physiological way
the psychological relief lowers the stress response and releases opioids. Opioids have pain killing effects.
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.
Alcohol is the __ most commonly used psychoactive substance in the world?
second
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
How much alcohol is in 1 drink equivalent
1/3 of an ounce of 100% ethanol
How much alcohol can our body break down in 1 hour
0.015 g
Where is alcohol absorbed in the body
20% in the stomach and 80% in the intestines
Where in the body is alcohol metabolized
85% in the liver and 15% by first pass metabolism
How much of alcohol is metabolized by alcohol dehydrogenase
95%
Why does alcohol get more absorbed by the body on an empty stomach
Because food can absorb the alcohol too
What does alcohol dehydrogenase break ethanol down into
Acetaldehyde
What is rate limiting step
In terms of alcohol it is how much can be broken down in one hour
What does acetaldehyde get broken into
Aldehyde dehydrogenase
After acetaldehyde is broken down what is left of the ethanol
Water, carbon dioxide, and energy
What happens when you have to much acetaldehyde in your body
You feel really sick
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
How long does it take to metabolize one drink equivalent
1 hour
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
A blood alcohol content of what is considered intoxicated
0.08
For what blood alcohol content are driving incidents pretty lenient
0.05-0.08
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
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
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
On a neuronal level which systems do alcohol affect?
GABA systems, glutamate systems, intracellular transduction processes
Which glutamate receptor does alcohol block
NMDA
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)
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
What does alcohol do to GABA receptors
It activates gaba receptors (binds to) leading to a state of inhibition
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
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
What accounts for the positive reinforcing effects of alcohol
The binding of alcohol on GABA A receptors
What is one possible reason why offspring of alcoholics also become alcoholics
They have a deficit in opioid release
What two neurotransmitters does alcohol promote the release of that are associated with feel good effects (not GABA)
Dopamine and opioids
What is naltrexone
A drug used for alcoholics quitting alcohol to prevent cravings by blocking opioid release
What serotonin receptors does alcohol bind to
Serotonin 2-3 receptors on dopaminergic neurons in the nucleus accumbens
What kind of effect does alcohol have on serotonin receptors
Agonistic action
What happens when antagonistic drugs block serotonin 2-3 receptors on dopaminergic receptors in the nucleus accumbens
It reduces the alcohol intake
What happens with chronic binding of cannabinoid receptors with anandamide
Down regulation of cannabinoid receptors
If someone has a down regulation of cannabinoid receptors and they stop drinking
Hyperactive receptor activation (craving)
What does it mean to say that alcohol causes depressed respiration
Your breathing is shallow and there is more pausing between your breaths
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
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
After what BAC are there behavioural changes
0.4
How much more likely are you to get into an accident when your BAC reaches above 0.4 or more
4x
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
What two things happen when we depress the glutamate system
Impaired cognitive function and alcohol myopia
What are the three types of tolerances or dependence
Metabolic tolerance, tissue/functional tolerance, homeostatic tolerance (new normal in environment)
What are 4 acute side effects of drinking
Drug-induced dementia, cloud sensorium, impair judgement, anterograde amnesia
What are three cognitive side effects of chronic alcohol use
Delusions, hallucinations, and periods of unconsciousness
What are physical side effects of chronic alcohol use
Liver damage (cirrhosis), dementia (nerve damage in the brain), digestive problems (pancreatitis, chronic gastritis)
Someone with a collection of chronic symptoms of alcohol is said to have
Wernicke Korsakoff Syndrome
What is the first step of cirrhosis
Fatty markers on your liver; this is reversible
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
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
How many birth defects are from teratogens
10%
What are some examples of teratogenic agents (4)
Ethyl alcohol, ionizing radiation, lithium, thalidomide
What is thalidomide
A morning sickness pill for pregnant women that caused them to give birth to babies with stunted limbs
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
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
What amount of alcohol is said to increase the likelihood of FAS
3 ounces of absolute alcohol (5 drink equivalents) daily
What are 5 (non-facial) features of FAS
- Low IQ
- Mental dysfunction (relative)
- Smaller body growth
- Certain facial features
- Must have been exposed to alcohol as a fetus
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)
What are three brain differences in FAS brains versus normal
FAS is 30% smaller, more holes and gaps, and less grooves
What are 9 facial features of people with FAS
- Microcephaly
- Palperbal fissure
- Epicanthal folds
- Flat midface
- Low nasal bridge
- Philtrum
- Thin upper lip
- Micrognathia
- Distinct ears
What is microcephaly
A small head circumference that those with FAS have
What is palperbal fissure
Short opening of eye that those with FAS have
What is philitrum
Indistinct vertical grooves between nose and mouths
What is micrognathia
Small jaw
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
What is ARND
Alcohol related nerve development disorder
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
What is the prevalence of ARND
1 out of 100
What are the four characteristics of ARND
Lower IQ, aggressive behaviour, hyperactivity, and sensory behaviour
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
What is a benzodiazepine
A drug that increases GABA
What are the four side effects of benzodiazepines
Sedation, can become dependent, interacts with alcohol (affects respiration), and psychomotor deficits
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
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.
What is a problem with anticonvulsants
Can contribute to liver and pancreatic problems and they have other side effects
What is antabuse
An alcohol sensitizing drug that makes you feel sick
What is acamprosate
A gaba agonist that inhibits glutamate. It mimics what alcohol does neurologically without the cognitive and behavioural consequences
What is naltrexone
An opioid antagonist. Reduces the pleasurable effects of alcohol
What is the best treatment option for alcoholism
Naltrexone and acamprosate
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
What type of serotinergic drugs help with alcoholism
SSRIs, 5HT1a agonists like BuSpar, and 5HT3a antagonists like zofran
What are the two types of drinkers
Type A: Later onset drinkers
Type B: early onset drinkers
Who is more responsive to placebo, type A or type B drinkers
Type B (early onset)
What type of drinker is more responsive to sertraline
Type A (late onset)
Does drinking making you dumb?
Long term chronic exposure is associated with alcohol will decrease your cognitive ability
What are four resources schools provide to help control student drinking
Preventative campaigns, counselling, campus regulation, enforcement (tickets)
What age counts as early exposure to alcohol
17-18
What is the average age of first exposure to alcohol
13.6
What is the average age people become regular users of alcohol
15-16
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
What are the four disadvantages of measuring blood alcohol content directly
Invasive, painful, data lag, costly
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
What is the ratio of BAC to BrAc
0.8:0.2
What are three types of machines that are used as breathylzers
Breathalyzer, intoxilyzer, and alco sensor
What does a breathylizer do
Initiates a chemical reaction that will produce a colour change
What is an intoxilyzer
An infrared spectroscopy
What does an alcosensor do
Fuels 3 or 4 chemical reactions that will fuel certain cells
What detects the change in reaction in a breathylzer
The photo cells and a meter
What is in the glass vial in a breathylzer
A chemical substrate
What are the pros and cons to a breathylizer
Pros: fast and easy to use. Cons: there is room for interpretation
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
What two factors can be a source of error for breathylzer
Breathing rate and temperature
How does air temperature effect a breathylzer
Reaction is faster in warmer weather and slower in colder
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
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
What was the first barbiturate and when was it introduced
Phenobarbital in 1912
How are barbiturates classified?
By their chemical structure
How many receptor sites will you find on a barbiturate nucleus
3
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
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
How do barbiturates work
Effects electrical and metabolic activity. Which decreases the whole brain glucose metabolism
Are barbiturates increasing inhibition or decreasing excitation
Both
What are the receptors on a barbiturate nucleus called
R1,R2,R3
What do barbiturates do with glutamate
They are glutamate NMDAR antagonists (decrease the amount of excitation)
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.
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)
What effects of barbiturates occur because of the binding on the GABAa receptor
the sedative-hypnotic and aesthetic properties.
Is there more than one binding site on GABAa receptors
Yes
What are some of the different molecules that kind bind to GABAa receptors
Barbiturates, Benzos, and GABA etc.
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.
What can high doses of barbiturates lead to?
Amnesia and a state of demensia
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.
What is the half life of barbiturates?
They have a wide range of half lives ranging from 3 minutes to 120 hours.
Are barbiturates fast or slow acting in terms of absorption?
Fast
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.
Do barbiturates cross the BBB
yes
It is very dangerous to mix barbiturates with alcohol. Why?
It will affect your respiration and it is very easy to overdose.
What are some of the major problems with barbiturates?
Lethal overdoses, narrow therapeutic ranges, quick tolerance, lots of dangerous interactions
Are barbiturates Teratogens
we don’t really know. we do see still birth, low birthweight, and low IQ but we aren’t positive.
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
What are non-barbiturates
Drugs that don’t have the same structure of traditional barbiturates but act the same way
What are three examples of non-barbiturates
Soma, Quaalude, and Paraldehyde
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
How are general anesthetics administered
inhalation or intravenous injection
What are three examples of general anesthetics
nitrous oxide, isoflurane, and halothane
How do injectable anesthetics make you feel
don’t make you feel good or bad they just numb you
What is Gamma Hydroxybutyrate
It is a precursor to GABA that is found in us endogenously. It is a strong central nervous depressant.
What are some of the things that GHB is used for
as an aesthetic, for sleep disorders (narcolepsy), and for alcohol detox.
What does synergistic mean
It interacts with something and makes the effect of the first substance a lot stronger (almost in an unpredictable way)
What does GHB do in terms of neurotransmitters
increases the amount of dopamine which then activates the dopamine reward pathway (positive reinforcement)
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.
Is GHB a solid, liquid, or gas
liquid
How long does it take GHB to reach peak plasma levels
30-75 minutes
What is the half life of GHB
30 Minutes
What is the urine detectability of GHB
It has low detectability
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
What is a better name for anti epileptic drugs
neuromodulators.
What molecule do neuromodulators chemically mimic
barbiturates
Are neuromodulators or antiepileptics teratogens
Yes.
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.
What kind of drug is a benzodiapine
anti-convulsant, sedative, and anxiolytic
What is the most widely used psychotherapeutic drug in the world
benzos
What are three examples of benzos
valium, librium, xanax
What does the basic chemical structure of Benzos look like
3 hexagons (2 on top one on bottom to the right)
What major neurotransmitter do Benzos target
GABA
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
What brain region to benzos target
limbic system
What brain regions are associated with anxiety, panic, and the behavioural response to fear
amygdala, orbitofrontal cortex, and the insula
What happens when you block GABAergic function in the amygdala
a person will be more anxious
What makes one benzo different from another
the rate of metabolism, active metabolites, and the plasma half lives
How long does it usually take to reach a peak benzo blood content
1 hour
What is interesting about the metabolites of benzos
They exert their own effect. They are active substances
What is the active metabolite of Valium
nordiazepam
What is the half life of nordiazepam
60 hours
Are benzos fast or short acting
the can be either or intermediate acting
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
What are the four subgroups of people/drug users
adults 16-65, seniors 65+, adolescents, and infants
What subgroup of people is really sensitive to benzos
the elderly
what is the problem with the elderly taking benzos
benzos can lead to cognitive dysfunction and most elderly people are already prone to it.
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.
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.
What are 4 effects of taking benzos
mental confusion and amnesia, muscle relaxant effect, antiepileptic actions, and behavioural rewarding effects
What accounts for the behavioural rewarding effects of benzos
the binding at the ventral tegementum and the nucleus accumbens
What is a better option for long term treatment of sleep issues or anxiety
anti-depressants
Why do benzos affect the effectiveness of CBT
CBT requires you to think and benzos are cognitive inhibitors.
If you were using benzos for surgical procedures which type would you use for a short surgery? a long one?
Short= midalozam Long=lorazepam
What makes rohypnol a good drug for rape (2)
80% is absorbed not immediately and the detectability is lost after 72 hours
what are the four advantages of benzos
fast, anxiolytic effect, less side effects than barbiturates, and patient acceptance
What are the disadvantages of benzos
effects psychomotor abilities, impaired learning and cognition, reduce alertness, dependency, paradoxical agitation
Are benzos teratogens
yes
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
What is flumazenil
A GABAa antagonist that blocks GABA binding by binding with the receptor.
What is flumazenil used for
benzo overdose
Whats another world for 2nd generation anxiolytics
nonbenzos
What type of non benzo is ambien
a partial agonist
What is ambien used for
insomnia
What receptor does ambient bind to
GABA1a
What function of sleep does Sonata aid with? Ambient?
Sonata helps with sleep onset and ambient helps with sleep maintenance
Where in the brain would serotingergic anxiolytics have their effect
5HT1 receptors in the hippocampus, septum, and the amygdala
What is the binding of the 5-HT1a receptor associated with
anxiety regulation
What is BuSpar
An anxiolytic that works by facilitating the binding of serotonin at 5HT1a receptors
What are the advantages and disadvantages of BuSpar
Advantage: low amnesia, no additive effects with alcohol. Problem is the grapefruit issue
