Parkinsons Flashcards
Safinamide MOA
- inhibits voltage activated Na channels
- inhibits glutamate release
- is a reversible MAO B inhibitor
- modulation of Ca channels
- It improves motor sx when given with levodopa
Amantidine MOA
- NMDA blocker
- Anticholinergic effects
- enhance DA release/or reuptake inhibtion
- is an antiviral, dizzy, lethargy, nausea, vomiting
parkinson tremor is
rest tremor, goes away with voluntary movement
where are lewy bodies found
intracellulary, they are alpha synuclein aggregates
Levodopa MOA and SE
- it is a dopamine precursor which can cross the BBB
SE: - involuntary choreiform or dystonic movements
- anorexia, nausea
- paranoid ideation
- depression
LONG TERM THERARY RESUTLS IN MOTOR FLUCTUATIONS AND DYSKINESIA
DA receptor agonists examples
ERGOT DA: - bromocriptine - cabergoline - lisuride - pergolide NON ERGOT DA: - pramipexole - ropinorole - piribedil
Whats wrong with using ergot derivatives for parkinsons
they induce nausea and fatigue, valvular disease and you need to increase the dose with time.
ROPINIROLE MOA
- D2, D3, D4 agonist
- metabolised by the liver
PRAMIPEXOLE MOA
- D2, D3 agonist
- excite the direct striatopallidal pathway by D3 stimulation
- inhibit the indirect striatopallidal pathway by D2 stimulation
APOMORPHINE MOA and SE
- is a dopaminergic agonist
- given via subcutaneous injection
- for rescue therapy for acute intermittent off episodes
SE: highly emetogenic, QT prolongation, can be abused, increased dose can lead to hallucinations, dyskinesia, and abnormal behavior
important side effect of dopaminergic therapy
impulse control disorders
inhibitors of dopamine degradation
COMT inhibitors
Selective MAO-B inhibitors
Selective MAO-B inhibitors examples
selegiline
- does not inhibit peripheral metabolism of catecholamines
- does not cause lethal potentiation of catecholamine action
- well toleration
- metabolites include amphetamine nad methamphetamine which can cause anxiety, insomnia
(RASAGILINE does not form the unwanted metabolites)
COMT inhibitors example
- TOLCAPONE
- ENTACAPONE
enta is short acting, tolcapone is long acting - tolcapone causes hepatotoxicity (fulminant hepatic failure) - are used in fluctuating pts who have failed other therapies