HY pharm Flashcards
Levodopa
dopamine replacement; precursor to DA, able to cross BBB.
tx: parkinson’s
+carbidopa
Entacapone
COMT inhibitor (prevents peripheral conversion of L-Dopa –> Methyldopa)
tx: parkinson’s
+levodopa/carbidopa
LIVER TOXICITY
DISCOLORED URINE
Selegiline
Rasagiline
MAO-B inhibitors (prevent selective degradation of DA)
tx: parkinson’s
pramipexole
ropinirole
D2 receptor agonists, non-ergots
tx: parkinson’s
dizziness and SUDDEN SLEEPINESS
compulsive behaviors
apomorphine
DA agonist, super POTENT
tx: parkinson’s
subQ injection for intermittent episodes
ORTHOSTASIS
benztropine
anticholinergic (anti-muscarinic)
tx: parkinson’s
- Used to rebalance DA:Ach ratio; treats tremors > rigidity
- can also be treating acute dystonic effects
amantadine
anti-viral
tx: parkinson’s (unknown MOA)
may improve rigidity, tremor and drug-related dyskinesia.
Methylphenidate
amphetamine, indirect monoamine agonist
block storage/reuptake of NE/DA
tx: ADHD
atomoxetine
ADHD
Selective inhibitor of NE transport (NSRI)
NONSTIMULANT
Blocks NE REUPTAKE so it is available in synapse for longer in prefrontal cortex.
similar mech to anti-depressants.
Guanfacine, Clonidine
ADHD
MOA: alpha-2 receptor agonists (sympatholytic) –> prevents release of NTs
(recall alpha-2 receptors - when stimulated - suppress release of transmitter)
(MOA for ADHD unclear)
caffeine
MOA: adenosine receptor antagonist (same shape, but does not cause same effect, just blocks site)
- ultimately inhibiting an inhibitor –> inc transmitter release
Adenosine binding to PRESYNAPTIC receptor:
- closes Ca++ channels
- decreased NT release
Adenosine binding to POSTSYNAPTIC receptor:
- open K+ channel
- hyperpolarizes cell
- decreased response to stimuli
If BLOCKED:
- increased NT release
- increased response to stimuli
Modafinil
tx: Sleepiness
Inhibits DA reuptake (dopamine available in synapse longer).
UNCLEAR how it relates to sleep
gammahydroxybutyrate
tx: narcolepsy, cataplexy
-potent enhancer of GABA (powerful sedative bc GABA is primary inhibitor)
-exhibits GABA and dopamine-like effects
^ DA/GABA agonism
date rape drug (conscious sedation)
phentermine
anorexiant
NE transporter inhibition
- NE stays in synapse longer, acts as stimulant
- sympathetic NS activated, parasympathetic suppressed
lorcaserin
anorexiant
5HT(2C) [serotonin] receptor agonist
- more serotonin produced
- change in hypothalamus
- less hungry
-similar receptor being modulated as fen-phen –> possibly future cardiomyopathy issues?