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25 Cards in this Set

  • Front
  • Back
know the drugs used to treat CNS disorders.
know the classification and mechanism of action of drugs used to treat CNS disorders.
know the acute and chronic effectiveness, side effects, and addictive potential of drugs used to treat CNS disorders.
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Name eight ways that a drug can affect neurotransmission.
Give a specific example for each of three of the eight ways that a drug can have an effect.
Synthesis of neurotransmitter -e.g. B6 Cofactor
Storage of neurotransmitter -e.g. MDMA (Ecstasy)
Release of neurotransmitter -e.g. Amphetamines
Reaction of Postsynaptic/Presynaptic Receptor to neurotransmitter binding -e.g. Barbiturates
Metabolism of neurotransmitter -e.g. Vigabatrin
Reuptake of neurotransmitter -e.g. Tricyclic antidepressants
Binding of neurotransmitter to receptor -e.g. Naloxone (i.e. receptor antagonists)
Neurotransmitter receptor by acting like the neurotransmitter -e.g. Nicotine (i.e. receptor agonists)
Why is blood-brain barrier important in CNS drug action?
tight junctions around BVs in the brain are critical to the action of CNS drugs
What are some general depressants?
General anesthetics
Ether, NO2 inhalants

Sedative hypnotics
Barbs, alcohol, Dalmane, Seconal


Minor tranquilzers
Meprobamate, valium, librium
What are some general stimulants
convulsants
strychnine, metrazol

amphetamines
benzadrine, dexedrine, ritalin

cocaine

Caffeine
Give exapmple of major tranqulizer
thorazine
What are groups of selective CNS agents
hallucinogens, antidepressants, major tranquilizers, opiates
Name some SSRIs
Fluoxetine (Prozac®) Most widely prescribed antidepressant Sales exceed 1 bill. $ / year

Paroxetine (Paxil®)
Sertraline (Zoloft®)
Clotalopram (Celexa®)
Main side effects of SSRIs
Main side effect: inhibition of sexual climax
Rare, but severe side effect: aggression, violence
How is Hippocampal BDNF affected by stress and antidepressants, respectively?
Stress depresses the BDNF content

Antidepressants elevate the BDNF content
What chemicals are released after cigarette nicotine activates an nAchR?
dopamine
Glutamate
Is the CB1 receptor presynaptic or post?
pre

it inhibits neurotransmitter release
Serotonin:
Termination mainly by reuptake (dopamine transporter - inhibited by Cocaine) and metabolism via ____ and COMT
MAOB
Serotonin:

Two distinct receptor groups exist (coupled to heterotrimeric G proteins):
D1-group (D1,D5: stimulate Adenylate cyclase: CNS, renal arteries) D2-group (D2,D3, D4: inhibit Adenylate cyclase: CNS)
Serotonin:

Three main dopaminergic pathways:
Nigrostriatal (substantia nigra): motor control (Parkinson’s disease)
Mesolimbic/mesocortical: emotion and reward system
Tuberohypophysal: from hypothalamus to pituitary
(Medulla oblongata: Vomiting center: D2 receptors)
Schizophrenia: _______ dopamine levels and D2 receptors
increased
Serotonin:

Seven distinct receptor types exist (7-TM):
5-HT1 group (CNS, blood vessels) (cAMP) 5-HT2 group (CNS, blood vessels) (IP3/DAG) 5-HT3 group (peripheral nervous system) 5-HT4 group (enteric nervous system)
___ = agonist of 5-HT2A receptor
LSD
Varenicline

Partial agonist at the α_ß_ nicotine receptor
Partial agonists have some effects like nicotine but can also act like antagonists
A dual mechanism of action is proposed:
Partial nicotine-like effects
Nicotine blockade from cigarette smoking
Varenicline

Partial agonist at the α4ß2 nicotine receptor
Partial agonists have some effects like nicotine but can also act like antagonists
A dual mechanism of action is proposed:
Partial nicotine-like effects
Nicotine blockade from cigarette smoking
When reading emotion, teens rely on what part of the brain?

(Adults rely on the prefrontal cortex)
amygdala (gut reaction)
Tolerance
Decreased response with repeated administration, or
A higher dose is required to produce the original effect (shift to _____)
right
Sensitization
Increased response with repeated administration, or
A lower dose is required to produce the original effect (shift to ___)
left
dynorphin
quiets dopamine release and depresses the reward circuit, causing user to need higher dose to feel high
Dopamine signaling leads to increased ____ and Ca++
This activates CREB protein which activates genes that make dynorphin
cAMP
Dopamine signaling leads to delta FosB protein which suppresses _______ and stimulates production of CDK5
dynorphin