Lecture: Neurotransmitters and Neuropharmacology Flashcards
how many drug overdose deaths occurred in 2019?
70,000
How many drug overdose deaths occurred in the last 12 months?
100,000
What drug caused the majority of drug overdose deaths in the last 12 months?
Opioids
Which neurotoxin binds irreversibly blocks the release of glycine from axon terminals?
Tetanospasmin
what does glycine do?
Relaxes muscles
What does tetanospasmin do?
Blocks the release of glycine
Is tetanospasmin reversible?
no
How does one recover from tetanospasmin/tetanus?
Wait for the production of new receptors that don’t have tetanospasmin attached
What is the term for when every muscle in the body is contracted to the full?
Opisthotonus
What are the two types of neurotransmitter receptors?
Ionotropic
Metabotropic
Did inotropic or metabotropic receptors evolve first?
ioniotropic
Which type of receptor opens directly when bound by a neurotransmitter
Ionotropic
Which type of receptor are ligand-gated ion channels?
Ionotropic
Which type of receptor activates a G-protein after recognizing a neurotransmitter
metabotropic
Are ionotropic or metabotropic receptors faster?
Ionotropic
Are metabotropic receptors direct or indirect?
indirect
Which type of receptor is typically used to treat pain? Why?
Ionotropic because they’re faster
__% of all drugs act via metabotropic receptors
75%
An ____ initiates normal effects of the receptor
Agonist
What happens when an agonist attaches to a receptor?
It opens
What are the two types of agonists?
Agonist
Partial Agonist
When a partial agonist is used, the resulting signal is ___%
<100%
Do agonists work on ionotropic or metabotropic receptors?
Both
What is the difference between agonists and partial agonists?
Partial only partially match the shape of the natural ligand
Which type of drug acts just like the natural ligand?
Agonist
Agonists are often used in _____ systems
Sensory
An ____ prevents a receptor from being activated by other ligands
Antagonist
What are the two types of antagonists?
Competitive Antagonist
Noncompetitive Antagonist
Antagonists (open/close) receptors
Close
What is the result of a competitive antagonist?
No signal
What is the result of a noncompetitive antagonist?
Partial signal
What type of drug binds to an allosteric (non-agonist) site on the receptor to prevent activation of the receptor.
Noncompetitive antagonist
Which type of antagonist fits the ligand site on a receptor?
Competitive antagonist
True or False?
Some people are more prone to concussion than others
True
Does Opisthotonos affect awareness?
No
Where does Alzheimer’s begin?
Hippocampus
What are the key brain regions in the cholinergic pathway?
Basal forebrain
Hippocampus (under the surface)
Cerebellum
Fornix
What class of neurotransmitters is endogenous morphine?
Neuropeptide
Peptides that bind to opioid receptors and relieve pain
Endogenous Opiates
Are endogenous opiates addictive?
Yes
Endorphines are produced in the brain during:
Exercise
Excitement
Pain
Eating spicy food
love
orgasm
Are the activities that produce endorphins addictive?
yes
Endogenous opiates produce _____
analgesia
What feeling is associated with analgesia?
Well-being
_____ indirectly affect neurotransmitter release or receptor response
Neuromodulators
_____ is normally release with catecholamines
Adenosine
Adenosine _____ catecholamine release via presynaptic auto receptors
inhibits
_____ blocks the effect of adenosine
Caffeine
During wakefulness, _____ builds up, making us _____
Adenosine
Sleepy
What is an example of a neuromodulator?
Adenosine
A study if 40,000 individuals found greater than ___% mortality in young men an women who __________
50
Drank more than 4 cups a day of coffee
Moderate coffee intake _____ all-cause mortality
Lowers
What ion do Benzodiazepines use?
Cl- influx
Endogenous benzodiazepines
Allopregnanolone
Diazepam-binding inhibitors
What drug is often referred to as the brains natural valium
Diazepam-binding inhibitor
Why are barbiturates depressing?
They slow down neuron firing
What channel do barbiturates work on?
GABA subscript A
What is phenobarbital used to treat?
Babies with epilepsy
What does it mean for alcohols effects to be biphasic?
They affect different neurotransmitters at different times
What three molecules does alcohol effect, in order?
Dopamine
GABA
NMDA
When is dopamine affected when drinking?
After first beer
_____ receptors are sensitive to alcohol
Dopamine
What happens when GABA is activated while drinking?
People become clumbsy
When is GABA activated when drinking?
3-4 beers
What happens when NMDA receptors are opened while drinking?
Person can die
All three alcohol compounds are _____
Psychoactive
What is the effect of alcohol at GABA receptors?
Sedation
Anxiety reduction
Muscle relaxation
Inhibited cognitive and motor skills
What are the stages between normal and withdrawal for alcoholics?
A. Normal
B. Acute Ethanol
C. Chronic Ethanol
D. Ethanol withdrawal
Why does chronic intoxication shrink the brain?
It slowly kills neurons
Can casual drinking shrink the brain?
No, only chronic intoxication
What can fetal alcohol syndrome present similarly to?
Autism
What is the main neurological cause of fetal alcohol syndrome?
The brain doesn’t make enough neurons
What is the head small in children with fetal alcohol syndrome?
The brain has less neurons than it should
What does the Corpus Callosum do?
Connect hemispheres of the brain
Can some infants with fetal alcohol syndrome lack a corpus callosum?
Yes, but not common
True or false?
Fetal alcohol syndrome can lead to small malformed areas of the brain
True
Did heroin work as a cure for codeine addiction?
Yes
What is Codeine?
An opioid pain reliever used to treat mild to moderately severe pain
What is fentanyl
An opioid
What is used to treat fentanyl overdose?
Naloxone
The brain has cannabinoid receptors that bind _____
Endocannabinoids
What is 2-AG
2 arachidonoyl glycerol
What do lipophilic molecules do since they cannot be stored in vesicles?
Exist as part of the membrane
CB receptors concentrate in brain areas that influence:
Pleasure, memory, concentration, time perception, appetite, pain, coordination
True or false?
Cannabis does not affect short-term memory
False
True or false:
Cannabis alters judgement/decision making
True
What is significant about cannabis inducing anxiety and paranoia in high doses?
It is the opposite of its normal effect
Can cannabis cause schizophrenic symptoms?
Yes
What is the primary psychoactive and addictive drug in tobacco?
Nicotine
What does nicotine activate in the periphery?
Muscles and twitching
What does nicotine generally increase?
Altertness
What does nicotine activate in the ventral tegmental area in the CNS?
Nicotinic ACh receptors
Where does nicotine activate nicotinic ACh receptors in the CNS?
Ventral tegmental area
Can one die of nicotine overdose/poisoning?
Yes
True or False?
Smoking risk is mostly due to other compounds in tobacco, not nicotine
True
__% of each attempt to quite nicotine and heroin are successful.
5%
Nicotine is just as addictive as _____.
Heroin
What is the primary cause of preventable death in the world?
Smoking
How many people does smoking kill per year in the US?
493,000
How many people does smoking kill per year worldwide?
4,000,000
Is the smoking rate in the US rising or falling?
Falling
How many people does heroin kill per year in the US?
4,000
Drug use by teens is (up/down)
Diwb
Why might drug use in teens be down?
Could be transferred to social addictions such as tiktok
Has cocaine become more or less popular?
Less
What has the cocaine trend been replaced by?
Fentanyl
What plant does cocaine come from?
Coca shrub
What do leaves from coca shrub do?
Alleviate hunger
enhance endurance and sense of well-being
Are the leaves of coco shrub addictive?
No
What is the difference between cocaine and leaves from coca shrub?
Cocaine is a purified extract
Why is cocaine addictive and leaves from coca shrub are not?
Cocaine enters the brain more rapidly, higher speed of absorption
What does cocaine do in the synapse?
Blocks the reuptake of monoamine transporters, especially dopamine, so more in the synapse
What is the peptide involved in pleasure sensations from cocaine and appetite suppression?
Cocaine-amphetamine-regulated-transcript (CART)
What does CART stand for?
Cocaine-amphetamine-regulated-transcript
Amphetamine is (more/less) addictive than cocaine
More
_____ and _____ are synthetic stimulants
Amphetamine
Methamphetamine
What do Amphetamine and methamphetamine do in the synapse?
Block reuptake and increase release of catecholamines, especially dopamine
What are the short term effects of amphetamine?
Alertness
Euphoria
Stamina
What are the long term effects of abusing amphetamines?
Sleeplessness
Weight-loss
Schizophrenic symptoms
What is Methamphetamine made from?
P2P
Where is 95% of meth in the US from?
P2P crystal meth made in Mexico
Stimulants for ADHD
Adderall
Ritalin
What is another name for adderall?
Dextroamphetamine
What is another term for ritalin?
Methylphenidate
How do ADHD stimulants work?
Stimulating inhibitory networks
What neurotransmitter does LSD stimulate?
Serotonin
What does LSD activate?
Serotonin
Does LSD activate dopamine?
No
LSD effects are _____
unpredictable
What do LSD effects depend on
Amount taken
User’s personality
Mood
Expectations
Surroundings
What are the physical effects of LSD?
dilated pupils
increased heart rate and blood pressure
Sweating
Sleeplessness
Tremors
What does LSD do to emotions?
User may feel different emotions at once or swing from one to another
What does LSD directly lead to?
Delusions and visual illusions
True or false?
Sensation cross overs occur due to LSD
True
Sensation crossovers:
Users can hear colors and see sounds
What does PCP stand for?
Phencyclidine
What does PCP make people do?
things that are nonsensible
What drug produces depersonalization and detachment from reality?
PCP
What drug produces side effects including combativeness and catatonia?
PCP
What drug is angel dust
PCP
What is PCP at the synaptic level?
Glutamate NMDA receptor antagonist
What drug is MDMA
Exstasy
What does the A in MDMA stand for?
Amohetamine
Amphetamine’s primary effects in the brain are on neurons that use _____
Serotonin
Which drug is being looked into for PTSD treatment?
MDMA
What does MDMA do at the synaptic level?
Blocks the serotonin reuptake transporter (removes serotonin from the synapse)
_____ prolongs serotonin signal excessive release of serotonin
MDMA
_____ causes oxytocin release
MDMA
What is an example of a synthetic opiate?
Carfentanil
Carfentanil is _____ times more potent than morphine
10,000
What is the lethal dose of carfentanil?
20 micrograms
What is a similar size to a lethal dose of carfentinal?
about one grain of salt
There are currently _____ active phase II trails with psychedelics
80
What psychedelics are being looked into with trials?
Psilocybin
MDMA
Ketamine
Ibogaine
What are trials researching psychedelics ability to treat?
Depression
PTSD
Addiction
Anxiety
Is the data for using psychedelics to treat PTSD strong?
No
Is Psilocybin permanent?
Either permanent or long lasting
Psilocybin
psychedelic compound found in certain mushrooms that can cause hallucinations.
Psilocybin _____ the human brain
desynchronizes
_____ reboots the brain’s default functional networks
Psilocybin
Addiction starts as _____, then becomes a _____ _____
Voluntary
Brain disorder
How is addiction voluntary at first?
First time taking it is voluntary
_____ is a chronic brain disorder that relapses despite harmful consequences
Addiction
Are addiction and tolerance the same thing?
No
Decreased sensitivity to a drug as a result of taking it
Tolerance
Increased sensitivity to a drug as a result of taking it
Sensitization
What is the only drug we have learned that causes sensitization
nicotine
Caused by withdrawal symptoms (not the reason people continue to take most drugs)
physical dependence
Compulsive and repetitive use, craving
Psychological dependence
True or False?
Addiction is caused by cravings, not avoiding withdrawals.
No
Addicts are preoccupied with:
Obtaining a certain drug
Addicts participate in compulsive use of the drug despite:
Adverse concequences
Addicts have a high chance of:
relapse after quitting
Withdrawal is:
The opposite effect of the drug
What is the negative reaction when drug use is stopped
Withdrawal
True or False:
Everybody is addicted to something
True, like oxygen
True or false?
All addictions are bad
false
The basis for addiction is _____
reward
Reward is the positive effect _____ _____ has on the user
any agent
_____ _____ _____ is the major reward system
Mesolimbocortical dopamine system
True or False?
Anything that causes dopamine secretion can be addictive
True
Abused drugs increase dopamine in the _____
VTA
Where is dopamine created?
VTA
What does VTA stand for?
Ventral tegmental area
True or False?
Dopamine underlies the addictive effects of:
Drugs
Food
Sex
Gambling
Warm Fuzzies
Reddit upvotes
Tiktok likes
True
Why does drug rehab usually fail?
Craving
True or false?
The changes in the brain caused by addiction are reversible
False
_____ builds up in neurons with each drug exposure
Delta FosB
delta FosB reamins activated for _____ after last drug exposure
years
Delta FosB remodels the _____ ______
nucleus accumbens
What happens when delta FosB remodels the nucleus accumbens?
It perpetuates craving and causes high relapse in treated addicts
More addictive drugs are more _____ potent
Delta FosB
What does delta FosB do in the nucleus
Turns on gene transcription which makes proteins
Treatment strategy that mimics the drugs effect, but milder
Agnostic treatments
What are examples of agnostic treatments?
Buprenorphine for opiate addiction
Nicotine patches
How often do nicotine patches work to quite nicotine?
5%
How do nicotine patches work?
Chantix stimulates nicotine receptors more weakly than icotine does
Are nicotine receptors partial or normal agnosits?
Parial
Why do agnonistic treatments work?
They replace the drug
What are the three strategies for pharmacologic treatments?
Antagonist
Agonist
Aversive
What to antagonistic drug treatments do?
Block drug effects
What is the antagonistic treatment for opiate addiction?
Naltrexone
What is the antagonistic treatment for alcohol addiction?
Baclofen
How does baclofen work?
Interferes with the dopamine pathway to block craving
What does compliance of antagonistic treatments depend on?
Addicts motivation to quit
Why do antagonistic treatments depend on the addicts motivation to quit?
They don’t replace the drug
What do Aversive drug treatments do?
Cause violent reaction if drug is used
What is the aversive treatment for alcohol addiction?
Antabuse
What drug treatment strategy is like a punishment for use?
Aversive
Are aversive drug treatments effective?
No
When are mGluRs used?
when there is a sustained elevation in glutamate conc. at the synapse
What is the antagonist for glycine?
strychnine