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76 Cards in this Set
- Front
- Back
Loss of pigmented cells occurs in what anatomic area in Parkinsons?
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Substantia nigra
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What are the inclusions called in the basal forebraine in Parkinsons?
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Lewy bodies
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What is the neurotransmitter deficit in Parkinsons?
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Dopamine
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What is the ideal pharmacologic treatment of Parkinsons?
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Levodopa/Carbidopa
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Direct pathway facilitates or inhibits movement?
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Direct pathway facilitates movement
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Indirect pathway facilitates or inhibits movement?
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Indirect pathway inhibits movement
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Direct pathway feeds into Gpi or Gpe?
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Gpi
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Direct pathway from Gpi goes to what part of the brain?
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Subthalamic nucleus
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Indirect pathway feeds into Gpi or Gpe?
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Gpe
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From Gpe, the indirect pathway can take two courses:
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1. Subthalamic nucleus
2. Gpi |
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With Parkinsons, which pathway increases and what decreases - direct and indirect?
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Direct pathway increases (increased movement) and indirect pathway decreases (decreased movement pathway)
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D1 receptor is excitatory or inhibitory?
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D1 receptor is excitatory
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D2 receptor is excitatory or inhibitory?
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D2 receptor is inhibitory
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What class of drugs is ideal in EARLY treatment of idiopathic Parkinsons experiencing a prominent tremor?
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Anticholinergics
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What class of drugs is the mechanism of action: to compensate for reduced inhibitory actions of dopaminergic neurons from substantia nigra on the striatum?
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Anticholinergics
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What makes up the striatum?
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Caudate and putamen
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Name two anticholinergics used in Parkinsons?
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1. Trihexylphenidyl
2. Benztropine |
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What class of drug is Trihexylphenidyl?
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Anticholinergic
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What class of drug is benztropine?
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anticholinergic
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What are adverse reactions of anticholinergics? Name 2:
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Dry mouth
Sedation Blurred vision Glaucoma exacerbation Urinary retention Impairment of cognitive function |
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What drug crosses the BBB and taken up into dopaminergic neurons to be converted into dopamine?
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Levodopa
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Where does the conversion and production of dopamine occur?
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In dopaminergic neurons
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What drug is a peripheral dopa-decarboxylase inhibitor?
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Carbidopa
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What is the most effective and rapidly acting treatment form SYMPTOMS of idiopathic Parkinsons?
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Levodopa/Carbidopa
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Dyskinesias and motor fluctuations are adverse effects of what drug?
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Levodopa/Carbidopa
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Does levodopa/carbidopa help balance disorder of Parkinsons?
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No, it does not
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In the past, why was Levodopa weighed out in giant amounts of grams.
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So little of it gets to the BBB.
Rationale for giving with Carbidopa which is a peripheral dopa-decarboxylase inhibitor |
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What enzyme rapidly breaks down levodopa in the periphery?
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Dopa-decarboxylase
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How much of ingested levodopa actually reaches the brain?
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<1%
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vazar
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to leak
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70% of levodopa is metabolized by what enzyme. 10% of levodopa is metabolized by what enzyme?
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70% by dopa-decarboxylase
10% by COM-T |
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What does COM-T stand for?
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Catechol-o-methyltransferase
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What is the half-life of levodopa/carbidopa?
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1-1.5 hours
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What drug is a peripheral inhibitor of COM-T?
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Entacapone
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What drug increases the elmination half-life of levodopa by 50%?
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Entacapone
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What drug metabolite causes the urine to turn orange?
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Entacapone
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Can Entacapone cause dyskinesias and motor fluctuations?
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Yes it can. Adverse effects are similar to those of levodopa
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Dietary amino acids can have a competing effect on LNAA transporter in the GI tract and BBB?
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Yes it can
(LNAA = large neutral amino acid) transporter |
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Levodopa + dopa decarboxylase produces what?
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Dopamine
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Levodopa + COMT produces what?
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3-O-methyldopa (inactive)
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What drug is a helper drug in treating Parkinsons?
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Amantadine
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What drug can cause livedo reticularis (Rsh)
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Amantadine
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What drug promotes dopamine release, inhibits DA reuptake, has anticholinergic actions and acts as a glutamate receptor antagonist?
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Amantadine
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Amantadine is indicated for early/late Parkinsons?
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Early Parkinsons
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Name an ergot derivative
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Bromocriptine
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What class of drugs mimic DA at receptors in the striatum?
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DA agonists
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What drugs are indicated as first-line treatment for symptomatic idiopathic Parkinsons?
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DA agonists
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"Sleep attacks" are a big problem associated with what drug?
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Bromocriptine (Ergot derivative)
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Ergot and non-ergot derivatives belong to what class of drugs?
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DA agonists
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Name two non-ergot derivatives
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Pramipexole
ropinirole |
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Pramipexole is what kind of drug?
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Non-ergot derivative (DA agonist)
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Ropinirole is what kind of drug?
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Non-ergot derivative (DA agonist)
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What drugs are also indicated for restless legs syndrome? (2)
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Non-ergot derivative:
Pramipexole Ropinirole |
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"Sleep attacks" can/cannot also occur with non-ergot derivatives?
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Can also occur
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What is the indication for non-ergot derviatives?
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1st line treatment for symptomatic Parkinsons
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What was the first dopamine agonist shown to be effective in 1951?
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Apomorphine
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Subcutaneous injections of what drug is used as "rescue" treatment?
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Apomorphine
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Severe GI reaction is an adverse reaction of what drug?
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Apomorphine
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MAO-A or MAO-B causes the breakdown of DA?
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MAO-B
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Selegiline belongs to what drug class?
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MAO-B selective inhibitor
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Rasagiline belongs to what drug class?
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MAO-B selective inhibitor
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Which of the two are irreversible MAO-B selective inhibitors - Seligiline or rasagiline?
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Rasagiline
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Which of the two has amphetamine metabolite and has a higher side effect profile? Rasagiline and seligiline
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Selegiline
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Which of the two has less side effects b/c it does not have amphetamine metabolites? Rasagiline vs. seligiline?
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Rasagiline
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Motor fluctuations can/cannot occur with continuous dopaminergic stimulation?
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Yes - switch between dyskinesia and bradykinesia
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Continuous therapy with levodopa plus entacapone stabilizes plasma levodopa levels? (T/F)
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True - reduces motor fluctuations between dyskinesia and bradykinesia
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What drug increases synthesis of dopamine?
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Levodopa
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What drug increases the release of DA?
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Amantadine
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What drug has action at the dopamine receptor?
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DA agonists
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Degradation of DA by MAO-B is inhibited by what drugs?
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Seligiline and rasagiline
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Reuptake of DA is inhibited by what drug?
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Amantadine
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What is the percent of people with essential tremor and autosomal dominant pattern of inheritance?
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50%
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What movement disorder is very common with prevalence near 6%
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Essential tremor
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Propanolol, primidone, gabapentin, alprazolam, and clonazepam can be used to treat what movement disorder?
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Essential tremor
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Trihexylphenidyl, BZD, Baclofen (GABA-B agonist), and Botox are used to treat what movement disorder?
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Dystonia
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What drug is useful for focal dystonia?
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Botox
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