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Pharm Parkinsons
KYCOM Block 14
50
Pharmacology
Graduate
02/26/2014

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Cards

Term
symptoms of parkinsons 9
Definition
50-70yo
15% have family history
bradykinesia: slowness of movement
muscle rigidity: tremor, posture instability
shiffling gait
frequent falls
cognitive impairment
death due to immobility (pulmonary embolism, aspiration pneumonia)
Term
cause of parkinsons
Definition
ROS or diminished antioxidants or both damage nigrostrital dopaminergic area

dopamine can undergo auto-odidative reactions forming H2O2

Fe and H2O2 cause hydroxyl radicals and cellular damage through proteins, lipids, and DNA

MPTP is metabolized to MPP radical which is a neurotoxin causing the disease
Term
how is dopamine nroken down
Definition
AMO degrades into DOPAC and HDO@

H2O2 is broken into OH by Fe or into water by glutathione
Term
chages in the CNS in parkinsons disease
Definition
loss of pigmented dopamine neuronsin substantia nigra (midbrain)

lewy bodies: abnormal cytoplasmic inclusions

loss of nitrostriatal dopamine neurons (no stimulation to D1/2 increases GABA input to cerebral cortex)

increased ACh: dopamine can no longer inhibit release, increased GABA transmission occurs as result
Term
what are the two dopamine receptors and their function
Definition
D1 stimulates direct pathway
D2 inhibits indirect pathway

dopamine acting on either receptor causes excitatory input for the cerebral cortex
Term
what are the 6 categories of parkinsons therapy
Definition
increased dopamine
direct dopamine receptor agonist
dopamine storage uptake/reelease
inhibit MAO-B
anti-cholinergics
inhibit COMT
Term
what drugs increase dopamine 1
Definition
levadopa
Term
what drugs are dopamine receptor agonists 4
Definition
bromoctyptine
perfolide
pramipexole
ropinirole
Term
what drugs are dopaine release/uptake drugs
Definition
amantadine
Term
what drug is a MOA-B inhibitor
Definition
selegiline
Term
what drugs are anti-muscarinic agents 2
Definition
truhexylphenidyl
benzotropine
Term
what drugs are COMT inhibitors 2
Definition
tolcapone
entacapone
Term
MOA levodopa
Definition
meabolic precursor of dopamine
Term
distribution of levodopa
Definition
crosses BBB on active carrier (aromatic AA) so can reach brain but little does
Term
where is levodopa metabolized 3, how
Definition
liver, kidney, GI

formulated with peripheral L-aromatic AA decarboxylase inhibitor (carbidopa)
Term
what are the SE of levodopa no matter how long youve been taking it 3
Definition
decarboxylation to dopamine in dopaminergic neurons in striatum causes SE

nausea and vomiting (less when combined with carbidopa)

on-off phenomenon
Term
what are the early SE of levodopa 5
Definition
N/V
orthostatic hypotension
tachycardia
arrhythmia
dark urine
Term
what are the late SE of levodopa 5
Definition
dyskinesias: choreiform movements
hypersentive receptors
mental disturbance: hallucinations, wild dreams, delusions
Term
what is the on-off phenomenon
Definition
when blood levels of levodopa drop there is an immediate reversal of symptoms (esp in sustained release formula)
deelops 2y into therapy
B6 increases peripherial breakdown and levodopa makes this worse
Term
use of levodopa
Definition
DOC and most effective for parkinsons disease
Term
MOA bromocryptine
Definition
D2 agonist
D1 partial antagonise
may save other dopaminergic neurons from oxidative stress
Term
use bromoctyptine
Definition
often used as adjunct to levodopa to lessen on-off phenomenon
Term
SE bromocryptine 7
Definition
dyslinesias
orthostatic hypotension
mental disturbance: hallucinations, wild, dreams, delusions
pleuropulmonary and retroperitoneal fibrosis (ergot like)
Term
MOA pergolide, SE
Definition
no longer on market
causes heart valve fibrosis due to activation of 5HT 2B receptors
agonist of D1 and D2 receptors
more potent than bromocryptine
Term
MOA pramipexole and ropinirole
Definition
non-ergot dopamine agonist at D2/3 receptors
Term
USE pramipexole and ropinirole 3
Definition
first line or adjunct for parkinsons
in pt who have not had levodopa
may delay need for levodopa

restless leg syndrome
fibromyalgia
Term
SE pramipexole and ropinirole
Definition
less hallucinations and orthostatic hypotension (like ergot agonists)

reward seeking behavior: drinking, smoking, gambling
Term
how is pramipexole elimiated by
Definition
renal
Term
contraindications to primipexole
Definition
cimetidine increases t1/2 by 40%
Term
MOA amantadine
Definition
anti-viral drug alters dopamine release of uptake (uless mass effect) anticholinergic effects
litte effect on tremor
good gainst rigidity and bradkyinesia
Term
USE amatadine 2
Definition
influenza
parkinsons
Term
SE amantadine 3
Definition
orthostatic hypotension
dry mouth
hallucinations
Term
MOA selegiline
Definition
MOA-B is prodominate form in striatum and causes most oxidative metabolism of dopamine that causes harm in parkinsons

low doses do not affect MOA-A bu high doeses will causing severe HTN
Term
SE selegiline
Definition
severe HTN in high dose due to MOA-A mass effect
Term
usE selegiline
Definition
enhance levodopa
Term
MOA trihexylphenidyl and benstropine
Definition
blocks cholinergic transmission to augment dopamine
modest anti-parkinson action
Term
use of trihexylphenidyl and benstropine
Definition
adjunct levodopa
Term
SE trihexylphenidyl and benstropine
Definition
same as high dose atropine
Term
MOA tolcapone
Definition
selective inhibitor of COMT (minor enzyme in pathway of levodopa metabolism)

often combined with carbidopa which blocks peripherial decarboxylase and 3-O-methyldopa is formed that competes with levodopa for active transport in the CnS

inhibition of COMT decreases 3-O-methyldopa increasing central levodopa uptake

helps with on-off phenomenon
Term
SE tolcapone 2
Definition
hepatotoxic: measure heptatic enzymes
blood dyscarcies
Term
t1/2 tolcapone
Definition
long acting
Term
MOA entacapone
Definition
same as tolcapone
Term
SE entacaopne
Definition
not hepatotoxic
no blood dyscrasias
Term
t1/2 entacapone
Definition
short acting (administer with ea dose of levodopa/carbidopa)
Term
cause of alzheimers disease
Definition
loss of cortical and subcortical neurons causes dementia

due to b-amyloid causing ROS attack and loss of cholinergic transmission
Term
3 acetylcholinesterase inhibitors, 1 SE
Definition
tacrin: hepatotoxic
donepezil
rivastigmine
Term
what 2 categories of drugs tx alzheimers disease
Definition
acetylcholinesterase inhibitors
n-methyl-d-aspartate receptor antagonist
Term
what drug is a n-methyl-d-aspartate receptor antagonist
Definition
memantine
Term
MOA memantine
Definition
overstimulation of NMDA receptors by glytamate lets Ca flow freely into the cell

sustained over exposure of the cells causes cellular degeneration
Term
what symptomatic tx can be used in alzheimers disease
Definition
depression - SSRI (citalopram, paroxetine, sertaline, fluoxetine, edcitalopran)

psychosis/agitation: atypical anti-psychotics (risperidone, olanzapine, queitapine)
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