Pharmacology - Parkinson's Flashcards
what is the precursor to dopamine
L-dopa
where does parkinsons start
substantia nigra
AE of D1 agonist activity
impulsivity
*muscarinic antagonist that can be used for PD
what is specific MOA
SE?
benztropine
M1 antagonist. has the typical anticholinergic side effects
**___ and ___ are D2/D3 agonists
which is more D2 and which is more D3
pramipexole and ropinirole
pramipexole is more D3 agonist and ropinirole is more D2 agonist
*AE of pramipexole
sleep attacks, compulsive behaviors, and gambling
*AE ropinirole
hallucination
*general nonselective dopamine agonists
rotigotine (neupro)
apomorphine
*as mentioned,rotigotine and apomorphine are, in general, nonselective dopamine agonists
do either have greater selectivity for certain receptors
rotigotine is 10 fold more selective for D3
apomorphine is more selective for d2
*rotigotine is a D2 agonist where?
in the caudate-putamen
*AE of rotigotine
psychological - sudden sleep onset during normal activities
insomnia, somnolenc
SE apomorphine
profound hypotension - loss of consciousness
QT prolongation
induces nausea - pretreat with antiemetic!
*name 3 COMT inhibitors
entacapone
tolcapone
opicapone
*name 2 MAO-B inhibitors
rasagiline
selegiline
*does entacapone cross the BBB?
NO
*AE of tolcapone
liver toxicitiy
*how often is opicapone administered
QHS
where is the MAO enzyme located
in the mitochondria
selegeline AE
insomnia (metabolized to amphetamine-like)
elevates all amines - risk of hypertensive crisis
*Amantadine MOA
NMDA antagonist
increased dopamine release and blocks its reuptake
*pimavanserin MOA
5HT2A inverse agonist
*how is L-dopa converted to dopamine
by DOPA decarboxyalse
*name 2 things that can be used to inhibit the peripheral conversion of L-dopa to dopamine
why is this good
allows us to decrease the dose of L-dopa we use
carbidopa or benzserazide
most L-dopa is broken down in periphery - these other drugs prevent!
*when dopamine is in the periphery, it has __ and __ effects
GI and CV
*true or false
carbidopa and benzserazide do not cross the BBB
true
in what area of the brain does dopamine work
the basal ganglia
