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Pharmacology 5
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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)
Acetylcholine
Excitatory
Abundant in cerebral cortex
Originates in pyramidal cells of the motor cortex and basal ganglia (both help with motor activities)
Monoamines
Catecholamines
: Dopamine (I) and Norepinephrine (I)
Serotonin (I)
Dopamine
I
Helps regulate motor control; influences moods and emotions
Norepinephrine
I
Has overall excitatory effect d/t disinhibition
Secreted by neurons in the locus coeruleus of pons
Serotonin
I-Strong
Mediates inhibition of painful stimuli
Helps control mood and behavior
Glycine
I
Involved with Renshaw cells
GABA
I-Main
Glutamate
Main Excitatory NT in CNS
May be toxic.
Aspartate is also a excitatory NT
Substance P
A peptide the propagates nociception in SC
Involved in peripheral sensitization (hyperalgesia)
Endogenous Opioids
Excitatory in nature and inhibit painful sensations
Endorphins
Dynorphins
Enkephalins
Neoendorphindes
Metyrosine
Demser
Inhibits enzyme essential for catecholamine (Dopa,Norepi-) synthesis
Reserpine
Impairs the storage of NT in presynaptic vesicles.
Antihypertensive drug
Amphetamines
MOI: Increase release of catecholamines from presynaptic terminal.
Botox
MOI: Impairs release of ACh from presynaptic terminal during AP
Tricyclic antidepressants
MOI: Impair reuptake of NT into presynaptic cleft increasing time in the cleft.
Neostigmine
MOI: Inhibits anticholinesterase Keeps ACh in the synapse.
Block postsynaptic receptor
Antagonists
E.g. Benzodiazepam Diazepam (Valium)
Presynaptic Autoreceptor activation
Serves as a negative feedback to control NT release
Presynaptic Membrane Alteration
Alters the fluidity of membrane to affect release of NT
Author
Kalanzo
ID
64971
Card Set
Pharmacology 5
Description
Pharmacology 5
Updated
2011-02-08T22:52:53Z
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