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Flashcards in parkinson's Deck (42):
1

l-DOPA (Larodopa; Sinemet)
l-DOPA plus Carbidopa (Sinemet), Parcopa
l-DOPA plus Carbidopa plus Entacapone (Stalevo)

Dopaminergic Agents
precursor, converted to dopamine in dopamine neurons in CNS
(dopamine itself does not cross BBB + has CV effects)

2

Bromocriptine (Parlodel)

Dopaminergic Agent

ergo derivative, act as non-sp DA rec agonists
less effective than l-DOPA but can be used when not tolerated, dec. "on-off" phenomenon, can be used in combo with l-DOPA

SEs: N/V, post hypotns, mental disturbs, endocrine disturbs: inhib prolactin secretion

*used to be used to tx ammenorrhea and galactorrhea assoc. with hyperprolactinemia, caused psych rxns and seizures
use Carbergoline instead

3

Pramipexole (Mirapex)

Dopaminergic Agent

stimulates post-synaptic dopamine receptors
Non ergot
antioxidant and neuroprotecitive effects, may slow disease progression
"restless leg syndrome"

4

Ropinirole (Requip)

Dopaminergic Agent

not effective at symptom control as L-Dopa
FLD and add-ons
similar to Dopa
stimulates post-synaptic dopamine receptors (D2, D3)

5

Amantadine (Symmetrel)

Dopaminergic Agent

causes release of DA
anti-influenza(viral)
stim. rel of DA from nerve endings
L-D>aman>antichol.

SEs: mental disturbs, hyperexcita., ataxia, confusion, convulsions, choreiform movements
excr. in kidney, adjust for pts with imp. renal function

6

Selegiline/Deprenyl (Eldepryl, Zelapar)

MAO-B Inhibitor

inhib. L-dopa brkdwn
used in later stages of park.
dec. "on-off"

SE: like l-DOPA, less sev.: choreiform movements, tremor, dyskinesias, hallucinations, agitation, behavior changes, nausea, wl, "cheese toxicity" at high doses

7

Rasagiline (Azilect)

MAO-B Inhibitor

inhibit L-dopa breakdown
used in early and late stages

SE: like l-DOPA, less sev.:
choreiform movements, tremor, dyskinesias, hallucinations, agitation, behavior changes, nausea, wl, "cheese toxicity" at high doses

8

Entacapone (Comtan)

COMT Inhibitor
inhibits dopamine metabolism

Stalevo: combo product: l-DOPA + carbidopa + entacapone

9

Benztropine (Cogentin)

Antimuscarinic Agent (centrally acting)
("remove weight from ACh side, enhancing DA side")

10

Trihexyphenidyl (Artane)

Antimuscarinic Agent (centrally acting)

11

Diphenhydramine (Benadryl)

Antihistamine (centrally acting)
(blocks muscarinic as well, enhances DA)
used in ER

12

disturbances in Parkinsons

Autonomic Disturbances (sweating, difficulty in swallowing, drooling, etc...)

Apathy, Social Withdrawal, Cognitive Impairment, Dementia

13

classification of parkinsonism

primary/Idiopathic: death of dopaminergic neurons in the nigrostriatial dopamine pathway

Iatrogenic (anti emetics, antipsychotics-block DOPA rec in striatum)

secondary: post traumatic, post encephalitic, or atherosclerotic
damage striatal pathway

14

pathway

substantia nigra-->dopamine containing neurons-->striatum

dopamine: inhibitory
ACh: excitatory

15

balance

between dopamine and acetlycholine

too little DA, parkinsonism
-blockade of DA receptors or degeneration of striatal pathway?

too little ACh, GABA: choreiform moevents

16

drug-induced parkinsonism: resolve?
tx??

yes, some may take a day

tx to alleviate pt w. benadryl: antihistamine, blocks muscarinic rec.

17

parkinsons drug SEs

choreiform type movements (tilted see-saw other way)
(drugs to not cure disease, tx symptoms)

18

MPTP oxidized to ??? in parkinson's via ??

to what effect??

MPP+ via MAO-B

MPP+ is (toxic) destroys nigrostriatal dopamine neurons

19

Parkinson's: genetic?

weak genetic, mostly aging and environmental

20

GABA antagonists not used for Parkonsinism

cause seizures

21

Huntington's chorea
(aut. dom, mid 30s, motor)

DA-antagonist
Cholinesterase inhibitors
benzodiazepines (enhance GABA)

22

L-dopa used in combo with...

Carbidopa:
inhib. L-dopa conversion in periphery, does not enter CNS

L-dopa(via DOPA decarboxylase)-->Dopamine (some may happen in periphery even tho we want in CNS)

23

L-dopa SEs: GI

N/V, triggers CRTZ, tolerance may develop
CRTZ is outside BBB, administering with carbidopa helps

24

L-dopa tx as disease progresses

less pronounced effect
does not halt progression

25

L-dopa SE: CV

hypotensn
tachy
arrythmias
*carbidopa helps dec. freq/sev, but still use caution in pts with existing CV disease

26

L-dopa SE: CNS

depression, psychotic reactions, hallucinations, exacerbation of psychoses, nightmares, euphoria, mood and personality changes
increased libido, release of inhibitions, compulsive behavior
*more common w. combo prep*
take "drug holidays" or lower dose

27

use ?? for managing L-dopa psych SEs

atypical antipsychotic clozapine (Clozaril)
*only one that doesn't cause extrapyrimadal motor problems

28

Clozapine (Clozaril) is associated with...

agranulocytosis -monitor!

29

end of dose phenomenon

decline in blood levels of l-DOPA near the end of the dosage interval
show sudden parkinsonism after good period

30

on-off phenomenon

can occur at any time in the dosage interval and appears to be related to the progression of the disease
v. worrisome
*use sustained release prep or add DA agonist +/- COMT inhibitor to regimen*

31

L-Dopa SE: endocrine

dec. prolactin secretion

(used to be used for women who choose not to breast feed)

32

L-Dopa contraindications

cardiac arrhythmias
psychosis
melanoma
glaucoma
active peptic ulcer disease

33

L-dopa drug interaction

pyridoxine:enhancement of extracerebral metabolism decreases therapeutic effects

antipsychotics (DA antagonists)

MAO inhibitors: HTN crisis (not when MAO-B inhibs used @ approp. dose)

tricyclic antideps. : HTN crisis

34

mild-mod parkinsons tx

L-Dopa most effective

amantadine, dopamine agonist, MAO-B inhibitors or anticholinergics,
pramipexole and ropinirole (becoming pop. FLDs)

35

mod-sev parkinsons tx

L-Dopa and carbidopa +/- entacapone

36

non-responsive pts tx

add a dopamine agonist, seligiline, amantadine or anticholinergics

37

L-dopa and carbidopa tx: early in course?

recommended by some, others recommend DA agonist (pramipexole)

38

Huntington's tx

decreasing dopaminergic activity
(antipsychotics) or enhancing the effects of GABA (benzodiazepines) or acetylcholine (physostigmine, rivastigmine) (BOARDS stuff)

39

seligeline for early use?

not approved, use rasaligine

40

L-dopa misc. effects

glaucoma
gout
hot flashes
taste/smell disturbs
elev. of liver enzymes
+ Coomb's test
blood dyscrasias
exacerbation of malignant melanoma

41

Ropinirole and Pramipexole SEs

choreiform, dyskinetic movements
nausea
dizzness, confusion, sedation, behav. changes, hallucinations

42

iatrogenic park. tx

stop/dec. drug, add anticholinergic for rapid reversal