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38 Cards in this Set

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Parkinson's: what is the NT change?
1. Decreased dopamine - loss of dopaminergic neurons
2. Increased Ach - excess cholinergic activity
Parkinson's: what are the 4 pharmacologic strategies?
1. Agonism of dopamine receptors
2. Increase dopamine levels
3. Prevent dopamine breakdown
4. Curb excess cholinergic activity
Parkinson's: what is the mnemonic for tx?
BALSA
1. Bromocriptine
2. Amantadine
3. Levodopa
4. Selegiline
5. Antimuscarinics
Parkinson's: name drugs that agonize dopemine receptors (4)
1. Bromocroptine
2. Pergolide
3. Pramipexole
4. Ropinerole
Parkinson's: what is pergolide and what is it's contraindication?
An ergot alkaloid and partial dopamine agonist
It is a vasoconstrictor and so it is contraindicated in CAD
Parkinson's: of the dopamine receptor agonists, which types are preferred?
The non-ergot types
Parkinson's: name the drugs which increase dopamine levels
1. Amantadine
2. levodopa + carbidopa
Parkinson's: what else is amantidine used for?
It may increased dopamine release but it is also used as an antiviral against influenza A and rubella
Parkinson's: what is the toxicity of amantidine?
ataxia
Parkinson's: what does levadopa do
increases the CNS levels of dopamine
Parkinson's: why give levadopa instead of straight up dopamine?
Dopamine cannot cross the BBB, but levadopa can.
Parkinson's: what happens to levadopa before it can be used in the CNS?
Once in the CNS it is converted to usable dopamine by DOPA decarboxylase
Parkinson's: what are the toxicities of levadopa? (3)
1. Arrhythmias caused by peripheral conversion into dopamine
2. Long term use leads to dyskinesias after administration and akinesias inbetween doses (tolerance leads to on-off phenomenon)
Parkinson's: why is carbidopa given with levadopa
To inhibit peripheral DOPA decarboxylase to prevent conversion of levadopa into dopamine which:
1. Increases the amount available to the brain
2. Reduces side effects of peripheral dopamine
Parkinson's: what drug should not be given with levadopa?
MAO-A inhibitors can lead to HTN crises
Parkinson's: what drugs are used to prevent dopamine breakdown?
1. Selegiline
2. Tolcapone
3. Entacapone
Parkinson's: how does selegeline work?
Selective inhibitor of MAO-B
Parkinson's: what is the normal job of of MAO-B
It preferentially breaks down dopamine over NE and 5-HT
Thus inhibition of MAO-B increases levels of endogenous dopamine
Parkinson's: what is unique about selelgiline compared to other MAOI
it is the only one that is used for PD
Parkinson's: what is the role of selegiline in PD therapy
as an adjunct to levadopa
Parkinson's: what are the toxicities of selegeline is PD therapy
may enhance the adverse effects of levadopa
Parkinson's: how do tolcapone and entacopone work?
Inhibits COMT in the periphery which converts levadopa into 3-O-methyldopa thus allowing more levadopa for the CNS
Parkinson's: what drugs are used to curb excess cholinergic activity?
Antimuscarincs - esp. benztropine
Parkinson's: what symptoms do antimuscarinics improve?
They improve tremor and rigidity
Parkinson's: what symptoms do antimuscarinics NOT improve?
Bradykinesia
AZD: what are the 4 drugs?
1. Memantine
2. Donezipil
3. Galantamine
4. Rivastigmine
AZD: what is the mechanism of memantine?
NDMA receptor antagonist which binds more tightly than Mg2+
this therfore inhibits the prolonged influx of Ca2+ ions
this therefore inhibits neuronal excitotoxicity
AZD: what are the toxicities of memantine (3)
1. Dizziness
2. Confusion
3. Hallucinations
AZD: Name the 3 AchEI's that are used for AZD
1. Donezipil
2. Galantamine
3. Rivastigmine
Huntington: what is the NT alteration? (3)
Increased dopamine
Decreased GABA
Decreased Ach
Huntington: what 4 drugs are used to treat
1. Reserpine
2. Tetrabenzine
3. Haloperidol
4. Benzo
Huntington: what is the mechanism of reserpine and tetrabenzine
Inhibits VMAT which leads to decreased dopamine output into the synaptic clefts
Huntington: what is the normal job of VMAT
works in the presynatpic terminal to package monoamines into secretory vesicles for release into the cleft
Huntington: what does haloperidol do?
Dopamine receptor antagonist
Sumatriptan: how does it work? (3)
1. Agonist of 5-HT 1B/1D which leads to vasoconstriction
2. Inhibits trigeminal activate
3. Inhibits vasoactive peptide release
Sumatriptan: what is the 1/2 life
< 2 hours
Sumatriptan: what are the 2 toxiciites?
1. Vasoconstriction
2. Mild tingling
Sumatriptan: in whom is this contraindicated?
1. CAD patients
2. Prinzmetal's angina