Neuro: neurodegenerative drugs Flashcards
In parkinson, as dopamine levels _______ ACH levels______
dopamine—-decreases
ACH—-increases
do the parkinson drugs stop or reverse the diseaes
NO just help with s/s
what is levodopa
-can it penetrate BBB
immediate precursor (before) of dopamine and is immediately converted to dopamine once it crosses the BBB
what is carbidopa
dopamine decarboxylase inhibitor
–diminishes metabolism of levodopa in the periphery (reducing s/e)—-increasing the availability of levodopa to the CNS—therefore more levodopa to cross BBB and become DOPAMINE
what happens when we add carbidopa to levodopa
it lowers the amount of levodopa needed by 4-5 fold!
*decreases SE too from peripherally formed dopamine
what happens if we dont add carbidopa to levodopa?
the levodopa is converted to dopamine peripherally—-and less will be available to cross BBB and then the effects of the drug are diminished
Mainstay of TX for PD???
L-C
*reduces severity of s/s for the first few years of tx
Long term use of Levodopa causes?
“wearing off”
flucctations and diskinesias
Peripheral SE from L-C
N/V
cardiac arrythmias
hypoT
Central SE from L-C
visual/auditory hallucintions, dyskineseas, psych S/s
drug-drug interactions of L-C
Vit B6—-pyridoxine diminishes effectiveness
If L-C is given with _______ can cause HTN crisis
MAOI
What happens if L-C given with MAOI
HTN CRISIS
T1/2 of L-C
1-2 hours
where is L-C absopbed
small intestine (if taken w/o food)
MAO Type B
—MOA?
inhibits MAO type B—-enzyme that b/d dopamine
actions of levodopa are potentiated*** letting dose be reduces
Selegiline and Rasagiline
MAO type B
*adjunct tx to L-C
Catechol-O-Methyltransferease Inhibitors (COMT)
MOA–?
which of the drugs is prefered?
ENTACAPONE AND TOLCAPONE
MOA—enzyme COMTresp for b/d of dopamine
*entacapone prefered over Tolcapone
Tolcapone–can cause??
COMT-Inhib
may cause fulminating hepatic necrosis—–need to monitor liver enzymes
Dopamine rec agonists work where in brain
basal ganlia
Which drug causes more movement disturbances and dyskineasias:
-Levodopa OR Dopamine rec agonists?
LEVODPA
Bromocriptine
Pramipexole
Ropinirole
dopamine rec agonists
Which receptors does Bromocriptine stimulate
dopamine
alpha
serotonin
Which patients need to be cautious when using Bromocriptine
Hx of MI or Periph vasc disease due to incr risk of vasospasms
what condition can administrtion of bromocriptine worsen?
psychiatric conditions
Bromocriptine is a _____ derivative
ERGOT–fungus
Amantadine
anti-viral
MOA amantadine
increases presynaptic dopamine release and improves long term levodopa induces dyskineases
- tolerance develops quick
- few SE