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Pharm 28: Movement disorders
pharmacologic management of Parkinsonism and other movement disorders
71
Pharmacology
Professional
02/02/2012

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Term
Levodopa: MOA?
Definition
transported into CNS, converted to dopamine
Term
What are the peripheral dopaminergic effects of levodopa?
Definition
anorexia, nausea, vomiting, cardiac arrhythmias, postural hypotension, hypertension, dyskinesias, changes in mood or personality, mydriasis, etc
Term
why isn't levodopa always used as first drug in Parkinson's disease?
Definition
development of disabling response fluctuations over time
Term
Name the drug: 6-8 effect, tox: GI upset, arrhythmias, dyskinesias, on-off, behavioral disturbances
Definition
levodopa
Term
What drug diminishes the dosage of levodopa required? Which drugs prolong the duration of effect?
Definition
carbidopa, COMT or MAO-B inhibs
Term
Does carbidopa enter the CNS?
Definition
no
Term
What is Sinemet?
Definition
levodopa and carbidopa
Term
What is Stalevo?
Definition
levodopa, carbidopa and entacapone
Term
Which drug is a direct agonist at D3 receptors? Is it an ergot?
Definition
pramipexole, no
Term
Effects of pramiprexole?
Definition
reduces symptoms of park's, smooths out fluctuations in levodopa response
Term
pramipexole: clinical applications?
Definition
park's, initial therapy or for on-off phenomenon
Term
How is pramipexole taken? What is the DOA? Tox?
Definition
orally, 8 hrs, nausea, vomiting, postural hypotension, dyskinesias
Term
Ropinirole is similar to which other drug? What is the MOA? Is it an ergot?
Definition
pramipexole, relatively pure D2 agonist, nonergot
Term
Bromocriptine is a potent agonist at ___ receptors
Definition
D2
Term
Name an ergot derivative that is an agonist at D2
Definition
bromocriptine
Term
How does the toxicity of bromocriptine compare to pramipexole or ropinirole?
Definition
it is more toxic
Term
Is apomorphine an ergot derivative? What is it used for? There is a high incidence of which side effects? what is the MOA?
Definition
no, subcutaneous route useful for rescue treatment in levodopa-induced dyskinesia, nausea and vomiting, it is a potent dopamine agonist
Term
What are pramipexole, ropinirole, bromocriptine and apomorphine?
Definition
dopamine agonists
Term
Name the dopamine agonists
Definition
pramipexole, ropinirole, bromocriptine, apomorphine
Term
What are rasagiline and selegiline?
Definition
MAOIs
Term
name 2 MAOIs used in movement disorders
Definition
rasagiline and selegiline
Term
What is the MOA of rasagiline?
Definition
inhibits MAO-B selectively, higher doses also inhibit MAO-A
Term
Which drug inhibits MAO-B, and at higher doses also inhibits MAO-A?
Definition
rasagiline
Term
What are the effects of rasagiline?
Definition
increases dopamine stores in neurons, may have neuroprotective effects
Term
Clinical applications for rasagiline?
Definition
park's, adjunctive to levodopa, smooths levodopa response
Term
How is rasagiline taken? Toxicity and interactions?
Definition
orally, may cause serotonin syndrome with meperidine, theoretically also with SSRIs and TCAs
Term
Selegiline is like which other drug? May be less potent in what situation?
Definition
rasagiline, MPTP-induced park's
Term
Which drugs used for movement disorders could cause serotonin syndrome with SSRIs, meperidine, or TCAs?
Definition
rasagiline, selegiline
Term
Name 2 COMT inhibitors used in movement disorders
Definition
entacapone, tolcapone
Term
what are entacapone and tolcapone?
Definition
COMT inhibitors
Term
What is the MOA of entacapone?
Definition
inhibits COMT in periphery, does not enter CNS
Term
which drug inhibits COMT in the periphery?
Definition
entacapone
Term
What are the effects of entacapone?
Definition
reduces metabolism of levodopa and prolongs action
Term
Which drug reduces the metabolism of levodopa and and prolongs its action?
Definition
entacapone
Term
clinical applications for entacapone?
Definition
park's
Term
How is entacapone taken? Toxicity?
Definition
orally, increased levodopa toxicity, nausea, dyskinesia, confusion
Term
Tolcapone is like which other drug? Does it enter the CNS? Tox?
Definition
entacapone, YES it enters the CNS, some evidence of hepatotoxicity and elevation of liver enzymes
Term
Which drug enters the CNS to inhibit the metabolism of levodopa?
Definition
tolcapone
Term
Name some antimuscarinic agents used in movement disorders
Definition
benztopine, biperiden, orphenadrine, procyclidine, trihexyphenidyl
Term
What kind of drugs are these: benztopine, biperiden, orphenadrine, procyclidine, trihexyphenidyl
Definition
antimuscarinics
Term
MOA of benztropine?
Definition
antagonist at M receptors in basal ganglia
Term
Which drug is an antagonist at M receptors in basal ganglia?
Definition
benztropine
Term
what are the effects of benztropine?
Definition
reduces tremor and rigidity, little effect on bradykinesia
Term
Which drug reduces tremor and rigidity but has little effect on bradykinesia?
Definition
benztropine
Term
clinical application for benztropine?
Definition
park's
Term
how is benztropine taken? Toxicity?
Definition
orally, antimuscarinic effects: sedation, mydriasis, urinary retention, dry mouth
Term
Name some drugs used in Huntington's disease
Definition
tetrabenazine, reserpine, haloperidol
Term
tetrabenazine, reserpine and haloperidol are used in which situation?
Definition
Huntington's disease
Term
What is the MOA of tetrabenazine and reserpine?
Definition
depletes amine transmitters, especially dopamine, from nerve endings
Term
which drugs deplete amine transmitters, especially dopamine, from nerve endings
Definition
tetrabenazine and reserpine
Term
what are the effects of tetrabenazine and reserpine?
Definition
reduce chorea severity
Term
How are tetrabenazine and reserpine taken? Toxicity? Which is somewhat less toxic?
Definition
orally, hypotension, sedation, depression, diarrhea, tetrabenazine is somewhat less toxic
Term
which drugs can cause hypotension, sedation, depression and diarrhea?
Definition
reserpine and tetrabenazine
Term
Which drugs are used in Tourette's?
Definition
haloperidol, clonidine, phenothiazines, benzodiazepines, carbamazepine
Term
haloperidol, clonidine, phenothiazines, benzodiazepines and carbamazepine are sometimes used for...
Definition
Tourette's
Term
What is the MOA of haloperidol?
Definition
blocks central D2 recepts
Term
which drug blocks central D2 recepts?
Definition
haloperidol
Term
What are the effects of haloperidol in Tourettes?
Definition
reduces vocal and motor tic frequency and severity
Term
How is haloperidol taken? Toxicity?
Definition
orally, parkinsonism, other dyskinesias, sedation
Term
Clonidine is effective in about __% of Tourette's pts
Definition
50%
Term
Which drugs are "sometimes of value" in Tourettes?
Definition
phenothiazines, benzos, carbamazepine
Term
What is the preferred tx for RLS?
Definition
dopaminergic therapy - pramiprexole or ropinirole
Term
adverse effect of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) and is irreversible
Definition
Drug induced Parkinsonism
Term
Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
Definition
levodopa
Term
Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia
Definition
bromocriptine
Term
What is the weird toxic effect of bromocriptine?
Definition
erythromelalgia
Term
Enhances dopaminergic neurotransmission, SE's include CNS excitation, acute toxic psychosis and livedo reticularis
Definition
Amantadine
Term
What does amatadine do? side effects?
Definition
Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis
Term
Agent effective in physiologic and essential tremor
Definition
propranolol
Term
Pimozide is used in...
Definition
tourettes
Term
Chelating agent used in Wilson's disease
Definition
penicillamine
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