Belonging to the class of CNS stimulants, what is the name of the inactive prodrug that is active only after being converted by the body into dextroamphetamine + L-lysine (essential amino acid)?
LISDEXAMPHETAMINE
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LISDEXAMPHETAMINE is used for ADHD, what does it do to the synaptic availability of noradrenaline, dopamine and to a lesser extent 5-HT?
increases
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where does Dextroamphetamine (and amphetamine) enter to cause the causing release of NA and DA towards the synapse. Inhibiting the enzyme MOA, preventing the breakdown of NA and DA, further enhancing their release
presynaptic monoamine vesicle
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despite LISDEXAMPHETAMINE being a good solution, Methylphenidate is the first line of defence. it Inhibits transporters for both noradrenaline (NA) and dopamine (DA)
Increase in synaptic levels of NA and DA
thought to contribute to its efficacy in ADHD, w
Prefrontal cortex
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why does methylphenidate have less potential for abuse?
not a substrate for these transporters and thus does not enter the nerve terminals to facilitate noradrenaline (NA) and dopamine (DA) release
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what pathway does Atomoxetine (for ADHD) work on?
norepinephrine transporter (NET),
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where does Atomoxetine increases DA levels due to less expression of dopamine transporter (DAT), dopamine reuptake by NET is also inhibited
Prefrontal cortex
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what receptors does Guanfacine work on?
Agonist at post-synaptic α2A adrenoceptors dendritic spines of PFC pyramidal neurons
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Pitolisant is a drug used to treat Narcolepsy with or without cataplexy, working on the brain's histamine system. WHAT is the sole source of histamine in the brain?
The Tuberomammillary Nucleus (TMN)
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TMN neurons are in the hypothalamus and send their axons to a wide range of brain regions
The TMN-histamine system involved in: select incorrect answer
Movement
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Histamine signals via 3 different histamine receptors, two are located postynaptically inducing excitation, and the other presynaptically limiting H release? which is the latter pre
H3
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Pitolisant is a WHAT antagonist/inverse agonist(bind to receptor but have opposite effect to agonist)
H3
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It DOES WHAT TO histamine synthesis and release whilst- Promotes wakefulness WITHOUT PSYCHO-STIMULATION
increases
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used to treat Narcolepsy with or without cataplexy, Sodium oxybate is the sodium salt of what endogenous compound and metabolite of the neurotransmitter GABA
gamma-hydroxybutyrate (GHB)
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Sodium Oxybate increases WHAT, which in turn decreases excessive daytime sleepiness
slow-wave sleep
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what transporter does Modafinil work on?
dopamine transporter
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Modafinil's increase of dopamine is in turn increasing what (promoting wakefulness)?
Histamine
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what drug used to treat excessive sleepiness associated with narcolepsy with or without cataplexy
DAT and NET inhibitor
Inhibits DA and NE reuptake
Leads to an increase in DA and NE activity
Solriamfetol
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caffeine is an ANTAGONIST at what nucleotide that builds up during the day? (caffeine prevents what from binding therefore delays fatigue)
adenosine
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The activation of ARs promotes sleep.
Caffeine-mediated AR antagonism reduces inhibitory GABA neurotransmission to what
tuberomammillary nucleus (TMN).
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Psilocybin is metabolised in the body to psilocin
Psilocin structural similarity to serotonin and is an agonist at WHAT receptors.
5-HT2A
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Other cards in this set
Card 2
Front
LISDEXAMPHETAMINE is used for ADHD, what does it do to the synaptic availability of noradrenaline, dopamine and to a lesser extent 5-HT?
Back
increases
Card 3
Front
where does Dextroamphetamine (and amphetamine) enter to cause the causing release of NA and DA towards the synapse. Inhibiting the enzyme MOA, preventing the breakdown of NA and DA, further enhancing their release
Back
Card 4
Front
despite LISDEXAMPHETAMINE being a good solution, Methylphenidate is the first line of defence. it Inhibits transporters for both noradrenaline (NA) and dopamine (DA)
Increase in synaptic levels of NA and DA
thought to contribute to its efficacy in ADHD, w
Back
Card 5
Front
why does methylphenidate have less potential for abuse?
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