Pharmacology 5

  1. What type of drugs pass through the BBB?
    • Non-polar, lipophilic (lipid soluble)
    • Polar, lipophobic usully do not pass
    • Exceptions with carrier mediated transport systems; e.g., glucose (protein tyrosine-kinase)
  2. Acetylcholine
    • Excitatory
    • Abundant in cerebral cortex
    • Originates in pyramidal cells of the motor cortex and basal ganglia (both help with motor activities)
  3. Monoamines
    • Catecholamines: Dopamine (I) and Norepinephrine (I)
    • Serotonin (I)
  4. Dopamine
    • I
    • Helps regulate motor control; influences moods and emotions
  5. Norepinephrine
    • I
    • Has overall excitatory effect d/t disinhibition
    • Secreted by neurons in the locus coeruleus of pons
  6. Serotonin
    • I-Strong
    • Mediates inhibition of painful stimuli
    • Helps control mood and behavior
  7. Glycine
    • I
    • Involved with Renshaw cells
  8. GABA
  9. Glutamate
    • Main Excitatory NT in CNS
    • May be toxic.
    • Aspartate is also a excitatory NT
  10. Substance P
    • A peptide the propagates nociception in SC
    • Involved in peripheral sensitization (hyperalgesia)
  11. Endogenous Opioids
    • Excitatory in nature and inhibit painful sensations
    • Endorphins
    • Dynorphins
    • Enkephalins
    • Neoendorphindes
  12. Metyrosine
    • Demser
    • Inhibits enzyme essential for catecholamine (Dopa,Norepi-) synthesis
  13. Reserpine
    • Impairs the storage of NT in presynaptic vesicles.
    • Antihypertensive drug
  14. Amphetamines
    MOI: Increase release of catecholamines from presynaptic terminal.
  15. Botox
    MOI: Impairs release of ACh from presynaptic terminal during AP
  16. Tricyclic antidepressants
    MOI: Impair reuptake of NT into presynaptic cleft increasing time in the cleft.
  17. Neostigmine
    MOI: Inhibits anticholinesterase Keeps ACh in the synapse.
  18. Block postsynaptic receptor
    • Antagonists
    • E.g. Benzodiazepam Diazepam (Valium)
  19. Presynaptic Autoreceptor activation
    Serves as a negative feedback to control NT release
  20. Presynaptic Membrane Alteration
    Alters the fluidity of membrane to affect release of NT
Card Set
Pharmacology 5
Pharmacology 5