Chapter 10 Flashcards
What is psychopharmacology
The study of the effects of exogenous drugs on the nervous system and on behavior
What is an exogenous drug
Something that is administered from outside the body
What is pharmacokinetics
How the drug is used by the body
What must a drug do to have an effect on you (3)
- It must get inside of you
- It must get to the site of action
- It must bind to a receptor
What are the routes of administration of a drug (6)
- Injection
- Oral
- Sublingual
- Rectal
- Inhalation
- Topical
What are the ways drugs can be injected into the body (4)
- Intravenous
- Intraperitoneal
- Intramuscular
- Subcutaneous
What types of drugs are administered topically
Steroids
What types of steroids are most commonly administered topically (2)
- Sex steroids
2. Cortisol like steroids
What are 2 types of routes to administer drugs that are used in animals but not humans
- Intracerebral
2. Intracerebroventricular
What makes a drug more addictive
The faster it gets into circulation the more addictive the drug
What is the order from fastest to slowest route of administration of a drug (4)
- Intravenous
- Smoked
- Intranasal
- Oral
True or False:
Morphine activates your endogenous opioid system
True
What happens if you take too many opiates
You stop breathing
Does a high or low therapeutic index indicate a safer drug
High therapeutic index
True or False: Alcohol has a lower therapeutic index than cocaine therefore it is more dangerous than cocaine
True
What is tolerance
With repeated use of a drug you start to need more of the drug to get the same effect
What is sensitization
With repeated use of a drug you start to see an increased effect of the drug
What is a precursor
A substance from which another substance is formed
What is an agonist
A drug that facilitates postsynaptic effects
What is an antagonist
A drug that blocks postsynaptic effects
What is the therapeutic index determined by
The number of patients that ended up dying from the negative side effects of the drug
What is the margin of safety
The dose of a drug that is considered safe to use for a patient to receive the positive effects of the drug and avoid the more serious negative effects
What is direct agonist/antagonist
Competitive binding
What is indirect agonist/antagonist
Non-competitive binding
What does the term NT refer to
The way the chemical is used by the body
Does the term NT have anything to do with the chemical itself
Not really
True or False:
The same chemical can be a hormone and a NT
True
What are chemicals used for neurocrine mediation called
Neurotransmitters
Neural signaling causes release of what
Neurotransmitters
What is paracrine signaling
Release of chemicals that effects cells nearby
What is endocrine signaling
The release of a hormone into the blood stream that has an effect on cells far from the sight of release
What are the 4 criteria for something to be a NT
- In terminal button
- Ca++ dependent release
- Subject to inactivation
- Receptors exist
What does acetylcholinesterase (AChE) do
Breaks ACH into choline and acetic acid
What are the NTs that are amino acids (4)
- Glutamate
- Aspartate
- Gylcine
- Gamma-aminobutyric acid (GABA)
What are the NTs that are monoamines (4)
- Catecholamines
- Indoleamines
- Histamine
- Acetylcholine
What is a type of indoleamines
5-HT/serotonin
What are the NTs that are neuropeptides (2)
- Substance P
2. Endorphins
What are the catecholamines (3)
- Dopamine (DA)
- Norepinephrine (NE)
- Epinephrine (EP)
True or False:
Amino acid NTs are the work horse of the CNS
True
What is the predominant type of NT
Amino acid neurotransmitters
What % of synapses involve 4 amino acid transmitters
90%
What are the 4 amino acids that make up 90% of synapses
- Glutamate
- Glycine
- GABA
- Aspartate
Can amino acid NTs be excitatory or inhibitory
Yes’m
What are the excitatory amino acid NTs (2)
- Glutamate
2. Aspartate
What are the inhibitory amino acid NTs (2)
- GABA
2. Glycine
What do most of the amino acid NT use for receptors
Iontropic receptors
What do some of the amino acid NT use for receptors
G-protein coupled receptor (GPCR)
What is an ionotropic receptor
Receptor that is an ion channel
True or False:
Usually neurons that release seratonin and dopamine release glutamate and GABA
True
How are amino acid transmitters inactivated (2)
- NT is taken up by astrocyte
2. NT is taken up by the terminal button
What is the major excitatory neurotransmitter that is widely distributed through the CNS
Glutamate
What are the types of glutamate receptor (4)
- AMPA
- Kainate
- NMDA (N-Methyl-D-Aspartate)
- G-Protein coupled glutamate receptors
What are the ionotropic receptors of glutamate (3)
- AMPA
- Kainate
- NMDA (N-Methyl-D-Aspartate)
How many varieties of the G-Protein coupled glutamate receptors are there
At least 8
What are NMDA and AMPA receptors used for (2)
- Learning
2. Memory
True or False:
NMDA is a coincidence receptor
True
What is a coincidence receptor
Detects when 2 things happen simultaneously
What plugs the pore in an NMDA receptor when glutamate is bound causing the channel to open
Mg++
What 2 things that must occur for an NMDA receptor to be active
- Glutamate needs to bind
2. Depolarization of the postsynaptic cell by another channel
What are the 2 important functions of NMDA receptors
- Coincidence receptor
2. Permeable to Ca++
What does NMDA receptors being permeable to Ca++ allow
Ca++ can bind to and activate enzymes through intracellular messenging
True or False:
Glutamate and GABA are produced everywhere in the brain
True
Is GABA a major inhibitory or excitatory NT
Major inhibitory NT
True or False:
GABA is widely distributed through the CNS
True
What must we know for the test about NT (5)
- Where they are produced
- Function
- How they are broken down
- Synthesis pathway
- Where is it released
What synthesize GABA
Glutamate and glutamic acid decarboxylase
What is released during the synthesis of GABA
CO2
What are the IPSPs (2)
- Cl-
2. K+
What are the EPSPs (2)
- Ca++
2. Na+
True or False:
A NT is considered inhibitory if it causes hyperpolarization
True
What are the 2 types of GABA receptors (2)
GABA a and GABA b receptors
What do GABA a receptors allow
Cl- ions into the neuron
What does the Cl- cause in the neuron
Hyperpolarization
What type of receptor is GABA a
Ionotropic receptor
What is diazepam (2)
- Valium
2. Benzodiazapine
What 2 things enhance the inhibitory action of GABA (2)
- Benzodiazepines
2. Barbiturates
What does benzodiazapine do the the effects of GABA
Increases the probability of opening the channel
What is another name for barbituate
Phenobarbital
What does barbituate do to the effects of GABA
Increases the open time of the receptor
How does alcohol effect the release of GABA
It increases the release
What do GABA b receptors connected to
K+ channels which hyperpolarizes the membrane
What was the first isolated NT
Acetylcholine
Who first isolated acetylcholine
Otto Loewi
How is acetylcholine synthesized
Acetyl coenzyme A and choline are combined by choline acetyltransferase
What does choline acetyltransferase make (2)
- Acetylcholine
2. Coenzyme A
How does choline acetyltransferase make acetylcholine
Transfers acetate ion from acetyl-CoA to choline
What breaks down acetylcholine
Acetylcholinesterase
What are the types of acetylcholine receptors (2)
- Nicotinic acetylcholine receptor
2. Muscarinic acetylcholine receptor
What does the 2nd order neuron release in parasympathetic nervous system
Acetylcholine
What does the 2nd order neuron release in the sympathetic nervous system
Norepinephrine
Where are the important areas that cholinergics like ACh are produced in (3)
- Dorsal lateral pons
- Basal forebrain
- Medial septum
What are the 9 CNS functions of ACh
- Memory
- Learning
- Aggression
- Grand Mal seizures
- Sensory perception
- Behavioral arousal
- Energy conservation
- Motor coordination
- REM sleep
What is the precursor to catecholamines
Tyrosine
What is the precursor to indoleamines
Tryptophan
What is the precursor to histamine
Histidine
What is the precursor to acetylcholine
Acetyl CoA + Choline
What are the 3 catecholamines
- Dopamine
- Norepinephrine
- Epinephrine
What is the indolemine
- Serotonin (5-HT)
What do all catecholamines have
Catechol group
How is dopamine made
Tyrosine 5-hydroxylase converts tyrosine into dopa which is then converted to dopamine by aromatic amino acid decarboxylase
What is the rate limiting step for the production of dopamine
Tyrosine 5-hydroxylase
What is Dopa used for
Treatment for Parkinson’s Disease
True or False:
Dopa is able to cross the blood brain barrier while dopamine is not able to cross the blood brain barrier
True
Why is dopa used to treat Parkinson’s Disease
It is able to cross the blood brain barrier so it can get into the brain
What is dopamine a precursor for (2)
- Epinephrine
2. Norepinephrine
How is norepinephrine made
Dopamine b-hydroxylase converts dopamine into norepinephrine
How is epinephrine made
Phenylethanolamine N-methyl transferase (PNMT) converts norepinephrine into epinephrine
What are the 5 subtypes of dopamine receptors
D1. D2, D3, D4, and D5
Are D1 like dopamine excitatory or inhibitory receptors
Excitatory (Gs)
Are D2 like dopamine inhibitory or inhibitory receptors
Inhibitory (Gi)
True or False:
You have to be very specific to the type of dopamine receptor you want
True
Where does the mesolimbic run to and from
Ventral tegmental area to nucleus accumbens and amygdala
What is the function of the mesolimbic tract (3)
- Reinforcement
- Drug addiction
- Schizophrenia
The mesolimbic provides the feeling of what
Wanting something
Where does the mesocortical run to and from
Ventral tegmental area to the prefrontal cortex
What is the function of the mesocortical tract (2)
- Short term memory (STM)
2. Planning
Where does the nigrostriatal run to and from
Substantia nigra to the basal ganglia
What is the function of the nigrostriatal tract (1)
- Movement
What tract is not functioning in people with Parkinson’s Disease
Nigrostriatal tract
What are the 3 spots dopamine goes in the brain to perform it’s functions
- Mesolimbic
- Mesocortical
- Nigrostriatal
Where is dopamine made (2)
- Substantia nigra
2. Ventral tegmental area (VTA)
Where does norepinephrine have a function (2)
- Brain
2. Autonomic nervous system
Where is norepinephrine produced
Locus coeruleus
True or False:
Norepinephrine projects to almost every brain region
True
What are 2 big functions of norepinephrine
- Vigalance
2. Attentiveness
Where is norepinephrine stored and released from
Axonal varicosities
How do axonal varicosities release norepinephrine
Paracrine secretion
What order neurons of the sympathetic nervous system release norepinephrine
2nd order neurons
What receptors effectively bind epinephrine (4)
- Alpha 1
- Alpha 2
- Beta 1
- Beta 2
What receptors effectively bind norepinephrine (3)
- Alpha 1
- Alpha 2
- Beta 1
What effect do alpha 1 receptors have on the body
Vasoconstriction of skin and GI
What effect do alpha 2 receptors have on the body
Neural
What effect do beta 1 receptors have on the body
Increases heart rate
What effect do beta 2 receptors have on the body
Vasodilation of skeletal muscle
What type of receptor are alpha 1 and 2 and beta 1 and 2
Metabotropic G-protein coupled receptors
True or False:
Norepinephrine causes explosive responses
True
How are catecholamines inactivated
They are taken in from the synaptic cleft by catecholamine transporter and is inactivated by monoamine oxidase
How does cocaine enhance the effects of dopamine
Cocaine blocks dopamine transporter
True or False:
Tryptophan is in all meat not just turkey
True
What do all indoleamines have
Indole group
How is serotonin made
Tryptophan 5-hydroxylase converts tryptophan into 5-hydroxytryptophan which is converted into serotonin by aromatic amino acid decarboxylase
How are indoleamines inactivated
They are brought back in from the synaptic cleft by 5-HT transporterand is inactivated by monoamine oxidase
What are the functions of serotonin (6)
- Mood
- Sensory
- Perception,
- Sleep
- Arousal
- Pain
Where is serotonin made
The raphe nucleus
Where is serotonin released in the brain
Everywhere
What effect the inactivation of serotonin (3)
- Antidepressants
- SSRIs (selective serotonin reuptake inhibitors)
- MAOI (monoamine oxidase inhibitor)
True or False:
MAOIs effect dopamine, epinephrine, and norepinephrine as well
True
How are neuropeptides inactivated
Peptidases degrade the bioactive peptides into inactive fragments
True or False:
In general they are a metabotropic receptor deactivated by peptidases
True
What are low density vesicles (LDV)
The are vesicles filled with neuropeptide
What do low density vesicles look like
Big dark black circles
What peptide is colocalized with acetlycholine (1)
Vasoactive intestinal peptide
What peptide is colocalized with norepinephrine (3)
- Somatostatin
- Enkephalin
- Cholecystokinin
What peptide is colocalized with dopamine (2)
- Cholecystokinin
2. Enkphalin
What peptide is colocalized with epinephrine (1)
- Enkephalin
What peptide is colocalized with serotonin (2)
- Substance P
2. Thyrotropin releasing hormone
True or False:
In one terminal button there can be release of multiple chemicals at once
True
What does an agonist do to the postsynaptic cell
Causes an enhanced response
What does an antagonist do to the postsynaptic cell
Causes an inhibited response in postsynaptic cell
What is psychopharmacology
The study of the effects of exogenous drugs on the nervous system and on behavior
What type of activity does stimulating an auto receptor have agonist or antagonist and why
Antagonist because it says there is too much NT in the synapse
What does tetrahydrocannabinoid stimulate
Cannabinoid recptors in the cerebellum, globus pallidus, hippocampus, and substantia nigra
What was the first natural ligand for THC discovered
Anandamide
True or False:
There are very few THC receptors in the brain stem so it has a low toxicity and won’t kill you
True
How does LSD (lysergic acid diethylamine) affect the body
Distortion of visual perception
How does MDMA (ectasy) affect the body
Excitatory and hallucinogenic effects
True or False:
LSD messes with serotonin
True
