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