drugs neurochemistry

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ligand
ligand
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substance that binds to receptor molecules or that binds postsynaptic receptors
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agonist
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activates receptor mimics transmitter
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receptor agonist
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binds and activates receptors
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antagonist
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blocks receptor reduces action of transmitter
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receptor blockers
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bind to receptors and do not activate them but block them
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binding affinity
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how well molecules of a drug bind to receptors
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efficacy
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extent to which a drug activates a response when binding to a receptor
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determines the overall action of a drug
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affinity and efficacy
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high affinity
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binds strongly
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low affinity
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binds weakly
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efficacy of agonists
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high
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efficacy of antagonists
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low or none
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competitive drug
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uses the same binding space as the NT
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noncompetitive drug
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binds on a different spot of the receptor than the NT
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dose-response curve
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graph of a drug’s effects v. dose given
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therapeutic index
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separation of useful doses and dangerous doses you want most drugs to have a WIDE therapeutic index
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potent drugs
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require a lower dose to get the same effect
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blood brain barrier
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protective property of cerebral blood vessels that impede movement of substance from blood stream into the brain
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drug tolerance
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repeated exposure causes individual to become less responsive to a constant dose
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types of tolerance
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metabolic functional
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metabolic tolerance
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BODY repeated exposure causes metabolism to become more efficient at getting rid of the drug
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functional tolerance
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BRAIN repeated exposure causes receptor levels to change
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types of regulation
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up-regulation down-regulation
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down-regulation
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decrease receptors repeated doses of agonists SSRIs
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up-regulation
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increase receptors repeated doses of antagonists
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cross-tolerance
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development of tolerance for one drug causes someone to develop tolerance for another
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drug effects on presynaptic processes
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1. transmitter production 2. transmitter release 3. transmitter clearance
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effects on transmitter production
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inhibition of transmitter synthesis block axonal transport interfere with storage
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effects on transmitter release
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prevent synaptic transmission alter synaptic transmitter release modulate transmitter release by presynaptic receptors
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effects on transmitter clearance
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inactivate reuptake block degradation
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autoreceptors
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receptor for a synaptic transmitter that is located in presynaptic membrane and tells axon terminal how much transmitter has been released
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drug effects on postsynaptic processes
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1. transmitter receptors 2. cellular processes
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effects on transmitter receptors
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block receptors activate receptors
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effects on cellular processes
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alter number of postsynaptic receptors modulate second messengers

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