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76 Cards in this Set

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