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25 Cards in this Set

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Levadopa Mechanism
- immediate precursor of D that must be converted by an aromatic aa decarboxlyase (aaad)
- often given w/ aaad inhibitor that cant cross BBB so its not broken down until it crosses BBB
Levadopa SE's
- if no aaadI, anorexia, Nandv (direct stimulation of chemoreceptor trigger zone in lower brainstem but outside the BBB)
- increased cats cause arrhythmias
- increased D causes dyskinseasea and behavioral effects (can give the 4 atypicals)
- dont give to crazy's, it will make them worse!
carbidopa
an aromatic aa decarboxylase inhibitor that doesn’t cross BBB give w/ L-dopa
chlorpromazine
antiemetic - dont give if nausea from parkinsons! it is a DR antagonist and can exacerbate the dz
Selegiline
- selective blocks MAO B
– alone in PD or for advanced if reduced response to levodopa-carbidopa
- has neuroprotective effect
desmethylselegiline
- metabolite of D (makes this and H202)
- reducing both (via Selegiline an anti oxidant / neuroprotective effect
rasagiline
blocks MAO-B, and is more potent than Selegiline, but not yet approved for PD as adjuvant to L-dopa
entacapone
- COMT-I, levodopa adjunct
- prevents D meth to 3OMD, which is inactive but competes w/ L-dopa for CNS access
- need liver testing
tolcapone
- COMT-I, levodopa adjunct
- prevents D meth to 3OMD, which is inactive but competes w/ L-dopa for CNS access
Direct-acting dopamine agonists
- good alone or w/ L-dopa
– don’t require functional D neurons / decarboxylase so good w/ “wearing-off” and “on-off” phenomena
- SE’s like L-dopa
- dont use it crazy's
Bromocriptine
- ergot alkaloid D2R agonist
- can be used in como w/ l-dopa as disease progresses, but may worsen vasospasm if peripheral vascular disease
pergolide
- ergot alkaloid D1R and D2R agonist
Pramipexole
– non-ergot, D2-R agonist
– can be used in levodopa-naïve and advanced PD
– no vaso-constrictive SE
ropinirole
- non-ergot, D2-R agonist
– can be used in levodopa-naïve and advanced PD
- for RLS now
Amantadine
- antiviral that helps PD
- MAY stimulating release of D ordelay reuptake
– an NMDA-R antagonist, reduces glutamate-mediated excitotoxicity and neuronal death
– loses effectiveness in 6-8 wks, so reserved for short tx intervals
trihexyphenidyl
- for PD - compete w/ ACh for M R’s and to stop stimulating GABAergic output
- improves tremor, but doesnt help bradykinesias
- good for drug induced parkinsonism, b/c other's make crazy people worse
benztropine
- for PD - compete w/ ACh for M R’s and to stop stimulating GABAergic output
- improves tremor, but doesnt help bradykinesias
- good for drug induced parkinsonism, b/c other's make crazy people worse
procyclidine
- for PD - compete w/ ACh for M R’s and to stop stimulating GABAergic output
- improves tremor, but doesnt help bradykinesias
- good for drug induced parkinsonism, b/c other's make crazy people worse
biperiden
- for PD - compete w/ ACh for M R’s and to stop stimulating GABAergic output
- improves tremor, but doesnt help bradykinesias
- good for drug induced parkinsonism, b/c other's make crazy people worse
diphenydramine
antihistamines w/ anticholinergic properties used for PD (esp. drug induced)
Huntingtons etiology
- too much D
- so too little GABA
- so too much movement
Huntingtons drugs
- block post D and help psychosis
- Phenothiazines (fluphenazine, perphenazine), haloperidol, and olanzipine
- reserpine and tetrabenazine deplete cerebral D by preventing intraneuronal storage
- Amantadine and riluzole are NMDA-R antagonists that reduce glutamate-mediated excitotoxicity
– Benzos (diazepam) may help potentiate GABA signaling
Tics and Tourette's drugs
- haloperidol, pimozide, and atypicals (risperidone, olazapine)
– can also try α2-agonist / anti-hypertensive clonidine (and related guanfacine)
– benzodiazepine’s clonazepam and diazepam
– anticonvulsive carbamazepine
Tremor Tx
- Tx physiologic and essential w/ propranolol, a β-blocker
- if you cant use them, try off-label use of the anticonvulsant primidone
RLS tx
- iron tends to make it worse, so take iron, B12, or folate
– levodopa and other D agents
- non-ergot, D2R agonist ropinirole recently approved