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28 Cards in this Set

  • Front
  • Back
frontal, parietal, temporal, occipital
entry of drugs into the CNS (4)
-Cerebral and spinal cord vasculature
-peripheral capillaries
-cerebral and spinal cord capillaries
entry route CSF
-diffusion, slow and inefficient
-in the hollow spaces, surrounds brain and spinal cord
-secreted by capillaries
entry route peripheral capillaries
-endothelial cells are gap junctions
-hydrophilic drugs pass through water filled gaps
-lipophilic drugs penetrate by passive diffusion through endothelial cells
entry route: cerebral and spinal cord capillaries
-anatomical- tight junctions
-enzymatic- MAO, COMT, ChE, gabatransaminase
ways to cross bbb
-passive diffusion
crossing bbb: passive diffusion
proportional to lipid solubility and amount non-ionized, mw <500
crossing bbb: carrier-mediated
-active and facilitated
-no lipid solubility needed
-must fit transporter
-for essential substances and some drugs
crossing bbb: pinocytosis
-endocellular inclusion
-no lipid solubility needed
-no need to fit transporter
-rare in CNS
chemoreceptor trigger zone
sense toxity and puke
cellular target of drugs in CNS
main target of drugs in CNS
-pumps and transporters
alternate direct targets of drugs in CNS
-nuclear receptors
-intracellular signal transduction systems
-cell membrane bilayer components
how to modify synaptic function
-inhibit NT release
-facilitate NT release
-decrease NT in cleft
-increase Nt in cleft
-mimic action of NT on post
-block access of NT to receptor on post
-decrease action of NT
-increase action of NT
inhibit NT release
-inhibit uptake of precursor
-inhibit synthesis
-inhibit uptake/storage in vesicle
-inhibit release into cleft
-increase destruction
facilitate NT release
-increase uptake of precursors
-increase synthesis
-increase uptake/storage into vesicles
-increase release
-slow destruction
decrease Nt in cleft
-facilitate uptake into presynaptic or perisynaptic cells
-facilitate destruction in cleft
increase NT in cleft
-block uptake in presynaptic or perisynaptic cells
-decrease destruction in cleft
decrease NT action
-decrease affinity
-decrease response of receptor activation
increase NT action
-increase affinity
-increase response of receptor activation
ionotropic receptors
ligand-gated membrane ion channels
metabotropic receptors
G-protein coupled membrane receptors
presynaptic inhibition
inhibit excitatory synaptic terminal by axo-axonic synapse. This reduces excitatory NT released per nerve impulse
remove inhibition from neuron/groups of neurons to cause excitation
terminal autoreceptors
inhibit NT relase
somatodendritic autoreceptors
decrease neuron firing rate
hierarchial (spatially focused) system
-sensory and motor systems
-convey info from point to point
-limited synaptic distribution from individual neuron
-classical synaptic contacts
-excitatory or inhibitory
diffuse (widely divergent) systems
-individual neurons influence many other cells
-highly collateralized system
-non-directed tansmission
-toning influence
-cholinergic, noradrenergic, dopaminergic, serotonergic