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102 Cards in this Set

  • Front
  • Back
what are the names of receptor agonist
apomorphine, bromocriphine, promipexole, ropinirole
monoamine oxidase inhibitors
rasagiline, selegiline
what are some catechol o methyl transferase inhibitors
entacapone, tolcapone
when does the intention tremor of parkinsons stop and what makes it worse
it stops when you go to do a voluntary movement and it is made worse by cold, fatigue, and strong emotions
___ is an involuntary, compulsive, rapid, repetitive, movement or vocalization, experienced as irresistable although it can be surpressed for some length of time. it is made worse with stress. may be simple or complex
tics
in what disease do tics happen
gilles de la tourette syndrome
what is dopamines normal role
to inhibit the GABAergic (inhibitory) output from the striatum (caudate and putamen) ..so in PD GABA is no longer inhibited and causes unstoppable inhibition
what can people with PD be treated with
dopaminergic drugs or antimuscarinic agents
what is the immediate metabolic precusor to dopamine
levodopa
how does levodopa enter the cns
LAT
what is the moa of levodopa
binds to d2 as an agonist
what is levodopa coadministered with and why
carbidpoa (dopamine decarboxylase inhibitor) because it reduced the peripheral metabolism , increased plasma levels, increases the half life, which means there is more levodopa available to get into the brain and decreases the daily req
does levodopa stop the PD dz progression
no but it does decrease mortality when initiated early in the dz
what is the wearing off phenomenon of levodopa
from long term tx. its is where each dose effectively improves symptoms for a limited time and by the time the dose wears off the rigidity and akenesia return..so you can try and increase the dose but this is limite by dyskinesias
what are the main SE of Levodopa
GI: if given without a decarboxylase it can cause nausea, vomiting and anorexia, so carbidopa minimizes SE-- vomiting is caused by activation of the chemoreceptor trigger zone
CV:postural hypotensio, hypertension (if take w MOA or symp mimetics)
Dykinesias: choreoanthetosis bw quick and slow movements of the face
behavioral changes: mood, insomnea, confusion--may take antipsychotics for these
what is the on off phenomena of levodopa
in the off period- akinesia alternate over the course of a few hours with on periods of improved mobility but still marked dyskinesia
what drug can provide temp relief for pts with severe off periods
SQ injections of apomorphine
why would you take a drug holiday from levodopa
to increase responsiveness and alleviate some adverse effects, may cause risk of immobility, this is no longer recommended
what drug drug interaction result happens when levodopa and MOA inhibitors
hypertensive crisis
who should not get levodopa
psychos, angle closure glaucoma, melanoma hx, suspicious skin lesions, pt with active peptic ulcer dz may cause GI bleeding
what kind of drug is Bromocriptine
what is a SE
D2 receptor agonist that is an ergot alkaloid derivative
SE: digital vasospasm
what is bromocriptine used for
PD and endoctine disorders, hyperprolactinemia, prolactin secreting adenomas,
-half life 15 hours
-extensive first pass
what does pramipexole bind to
d3 receptors
what is pramipexole used to treat
PD and restless leg syndrome
half life 8 hours
how is pramipexole excreted
unchanged in the urine
what does ropinirole bind to
d2 recpetors
what is ropinirole used for
RLS and PD
how long is the half life of ropinirole and what is it metabolized with and coadministered with
6 hr
coadmin with agents that may also reduce the clearance of ropinirole and are also metabolized by CYP1A2
what are adverse effects of Dopamine receptor agonists
GI: anorexia, nausea, vom- dec symp if take with meal, constipation, dyspepsia, and reflux esopagitis
CV: postural hypotension, peripheral edema and cardiac arrythmias
Dyskinesias
mental probs-confusion, hallucinations, mental probs more severe than with levodopa
what SE is assoc with ergot derivatives that are dopamin receptor agonist
HA, nasal congest, increased arousal, pulm infiltrates, pleural and retroperitoneal fibrosis
what SE is assoc with pramipexole and ropinirole
uncontrollable urge to fall asleep at inappropriate times
who should not get dopamin receptor aagonists
ppl with psychotic dz, recent MI, or active peptic ulceration
who should not get Bromocriptine
ppl with peripheral vasc dz
what does MAO A metab
norep and serotonin
what does MAO B metb
phenylethylamine and benzylamine
what does MAO A and B equally metab
dopamine and tryptamine
what is the MOA of selegiline
irreverible MAO B inhibitor and MAO A at high doses-
- slows the breakdown of dopamine and prolongs the antiparkinsonian effects of levodopa, may reduce mild on off or wearing off phenomena
what is selegiline used for
pt with declining or flucating responses to levodopa
who should not take selegiline
pt taking meperidine, tricyclic antidepressants, or serotonin reuptake inhibitors
what is does Rasagiline inhibit
irreversible inhibitor of MAO-B more potent than selegiline
what is Rasagiline used for
neuroprotective agent and early symptomatic treatment of PD
the combined administration of levodopa and non selective MAO inhibitor must be avoided why?
because it may lead to a hypertensive crisis due to peripheral accum of norep
what is the function of COMT
metabolizes levodopa to 3-O methyldopa which compted with levodopa for transport across the intestinal mucosa and the BBB
what is the role of COMT inhibitors
prolong the activity of levodopa by inhibiting its peripheral metabolism, which decreases clearance and increases bioavail
what are COMT inhibitors used for
ppl getting levodopa that are experiences fluctations in response
what are two COMT inhibitors and what is the diff between them
Tolcapone and entacapone
tolcapone has both central and peripheral effects whereas entacapone has peripheral effects only
what is a side effect of tolcapone
death from increase in liver ensymes- bc it leads to hepatic failure
what are SE of COMT inhibitors
orange urine, diarrhea, abdominal pain and sleep probs
what is the MOA of Apomorphine
dopamine agonist that stim postsynaptic d2 recpetors in the caudate -putamen
what is apomorphine used for
injected sq for pt in off period of dopamine tx- works in ten min
what are side effects of Apomorphine and what can they be treated with
nausea ( can pretreat with trimethobenzamide) dyskinesia, sweating, hypotension,
what is amantadine
antiviral that might potentiate dopaminergic effects used to treat PD
-short half life
what are side effects of amantadine
restlessness, depression, irritabilty, insomnia, agitations,HA, heart failure, urinary retention GI probs
***livido reticularis- purpleish mottled discoloration on skin
who should use amantadine with severe caution
ppl w hx of seizures, or heart failure
what part of PD are antimuscarinics used to treat
the rigidity and tremor but have little effect on bradykenisia
what are the names of the antimuscarinics that can be used to tx pd
benzotropine, biperiden, orphenadrine, procyclidine, trihexyphenidyl
what are tremors that are associated with B1 receptors treated with
metoprolol and propanolol
what antiepileptic drug can be used to treat a symptomatic tremor
primidone- used in a smaller dose
what serotonin receptor agonist has been shown effecting in tremor tx
topirimate
what benxodiazepine has been shown to help tremor
alprazolam
which drugs impair dopaminergic activity and alleviate chorea
resperine, tetrabenazine, olanapine, perphenazine, halpperidol
what is reduced in the BG of peeople w HD
GABA and choline transferase
what is the MOA of resperine and tetrabenazine
block the vesicular monoamine transporter adn deplete cerebral dopamine stores
tetrabenazine- has less peripheral activty and a shorter duration of action
what is the first choice of tx for hd
dopamine antagonist or anxiolytics which reduce involuntary movement
what is the most predictive and effective pharm tx for tics
and what is the backup plan
neuroleptic antipsychotics- ex pimozide
back up for less SE: alpha adrenergic agents ex. clonidine, guanfacine
what is the first line tx for RLS
non ergot dopamine agonist pramipexole and ropinirole
what is the MOA of penicillamine
chelatin agent that forms a stable complex with copper and is readily exctreted by the kidney
what are SE of penicillamine
nephritic syndome, myasthenia, optic neuropathy, blood disorders
what agent reduced the intestinal absorption of copper and can be prescribed with penicillamine
potassium disulfide
what is the MOA of zince acetate and zinc sulfate
increase pooping of copper by decreasing copper absorption
why is levodopa more effective for PD treatment than dopamine
bc it can cross the BBB and dopamin can not
what is the most commonly used drug for PD
levodopa/carbidopa=Sinemet
what are SE of levodopa
nausea, hypotension, and nightmares, psychosis and aggression
what are the two newest and best tolerated dopaminergic drugs where do they bind and what do they do
Pramipaxole and ropinirole
they bind to d2 in striatum
what are the side effects of pramipaxole and ropinirole
hypotension and behavioral changes, psychosis and hallucinations! more than with levodopa(sinemet)
what is the role of amandatine in tx PD
helps release dopamine, also anticholinergic ( antagonizes glutamate)
helps with wearing off of leva
-loses effect after 6 mo
what is an example of an anticholinergic that can be used for PD and what is its fxn
trihexyphenidyl,used to counter the loss of dopamine
what is a SE of trihexyphenidyl
delerium esp in elderly
what are the trade names of two monoamine oxidase inhibitors and which one is neuroprotective
Eldepryl, and Azilect
Azilect is neuroprotective
which COMT inhibitor can be combined with levodopa and is not hepatotoxic
entacapone when combined its called stalveo
what is the best treatment for an essential tremor
propanolol
what other drug is also good for essential tremor but may cause delerium and sedation
primidone
what is used for severe cases of essential tremor
deep brain stim or ablation of C/L thalmus
what is Tourette's treated with
Haloperidol a d2 blocker
___ is sustained abnormal movements, minutes, hr or even days of sustained muscular contractions, with twisting. will cause abnorm posture
dystonia
what is another name for oppenheim dystonia
DYSTONIA MUSCULORUM DEFORMANS
what is the prob in oppenheim dystonia
possibly and atpase prob
what age group gets oppenheim dystonia
second or third decade= aka 13
what are symtpoms of dystonia
bizzarre twisting movement of one leg while running or playing. body may become horridly distorted, trunk and head involved/
what is the time frame of oppenheim dystonia
flexion over 5-10 years an then a plateua
what drugs are used for oppenheim dystonia
levo-dopa, diazepam ( is a benzo), tetrabenazine (anticholinergic)
or botulinum toxin
what is char of adult onset dystonia
they stay focal Blepharospasm of the eyes, writer’s cramp of the forearm, hemifacial spasm, spastic dysphonia of the vocal cords
what is another name for toricollis
cervical dystonia
what is the best treatment for tortilcollis
botulinum toxin- which prevents ach release
what is a blepharospasm
severe contractions of the orbicular oculi, bilateral, interfering with vision; associated with Parkinson’s disease
what all types of dystonias are responsive to botinum toxin
blepharospasm, hemifacial spasm, writers cramp, dystonia of vocal cords
what are choreas treated with
dopamine antagonist ie haloperidol if the known cause can not be treated
what disease is this: chorea, dementia, depression, irritable, impulsive, psychosis, decreased muscle tone and weakness, weight loss, ultimately fatal in all cases
Huntigtons
what age group gets huntingtons
what causes it
30-40. genetics=AD
what is visible on CT or MRI if HD pt
destruction of caudate or putamen and other areas of brain
what are the early signs of HD
irritability, fault-finding, nagging, angry, fidgety, neglect of personal care
then chorea begins- worse in the head and face
what are some drugs that can be tried with HD
haloperidol, Reserpine. tetrabenazine-limits dementia, dimebon (stabilize mito)