Flashcards in Neurodegenerative Disease Deck (45)
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Levodopa
Parkinsons
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Levodopa MOA
metabolic precursor to Dopamine. Becomes dopamaine to restore post-synaptic concentration of dopamine. Activates post-synaptic D1 and D2 receptors
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Carbidopa
inhibits dopa decarboxylase to allow levodopa to enter the BBB
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Levodopa contraindications
MAOI use, history of malignant melanoma, narrow angle glaucoma. Monitor LFT
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Levodopa ADR
Dyskinesias, "on-off" effect, Nausea, anorexia, hypotension, confusion, insomnia, nightmares, schizophrenic like syndrome
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Dopamine Agonists
apomorphine, bromocriptine, pergolide, pramipexole, ropinirole, rotigotine
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Dopamine Agonists ADR
N/V, anorexia, hypotension, cardiac arrythmias, HA, confusion, hallucinations, sedation, pulmonary fibrosis
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Ergot Dopamine Agonists
Bromocriptine and Cabergoline. D2 receptor agonists
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NonErgot Dopamine Agonists
Pramipexole, Ropinerole, Rotigotine (patch), Apomorphine
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Pramipexole indications
advanced Parkinsons and restless leg syndrome
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Ropinerole indications
monotherapy in mild parkinsons and restless leg syndrome
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Rotigone ADR
sudden somnolence
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Apomorphine receptor type
D1/D2
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Pramipexole receptor type
D3. some D2/D4
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Ropinerole receptor
D2
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Apomorphine indications
subQ injection for temporary relief of "off" periods
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Apormorphine ADR
dyskinesias, drowsiness, sweating, hypotension
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Selegiline MOA
monoamine oxidase- B inhibitors
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Selegiline indications
effective as monotherapy or in combination with levodopa for parkinsons. enables reduction in levodopa
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Selegiline ADR
blocks MAO-A at high doses, fatal hyperthermia
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Rasagiline MOA
irreversible MAO-B inhibitor
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Rasagiline indications
early treatment of Parkinsons and as adjunct with Levodopa
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Rasagiline metabolism
extensive liver metabolism. metabolized at CYP1A2.
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Rasagiline Drug interactions
meperidine, dextramethorphan, St. Johns Wort, cyclobenzaprine, ciprofloxacin
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Catechol-O-Methyltransferase inhibitors
Tolcapone, entecapone
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COMT inhibitors MOA
inhibits metabolism of dopamine. increase availability of Ldopa
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COMT indications
adjunct treatment for Parkinsons with levodopa
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COMTI ADR
increased plasma concentration of Ldop (dyskinesias, nausea, confusion), Diarrhea, abd pain, orthostatic hypotension, sleep disorders, orange urine discoloration. Tolcapone may be hepatotoxic
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COMT pearls
do not use MAO-A and COMT together. MAO-B may be okay. Entacapone=P450 inhibitor. Taper dosing for discontinuation
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Stalevo
Levodopa + Carbidopa + entacapone
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Amantadine
Antiviral drug with anti-parkinsonian properties
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Amantadine ADR
primarily CNS- restlessess, depression, irritability, insomnia, agitation, excitement, hallucinations, confusion, seizures. HA, edema, postural hypotension, HF, GI
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Anticholinergics MOA
dopamine def augment excitatory cholinergic system. blocks this system
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Anitcholinergics
Trihexyphenidyl and Benztropine
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AA of Neuro guidelines
Selegiline first, Levodopa or dopamine agonist, Alternative- exercise, speech therapy
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Cholinesterase inhibitors Indications
First line in Alzheimers
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Cholinesterase inhibitors
Donezepil, Rivastigmine, Galantamine
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Donezepil ADR
Cholinergic side effects , NVD, insomnia, fatigue, muscle cramps
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Donezepil interactions
metabolized by P450
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Rivastigmine ADR
NVD and weight loss, dyspepsia, sinusitis, dizziness
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Galantamine MOA
dual MOA. Competitive inhibition of acetylcholinesterase and allosteric modulation of presynaptic and postsynaptic nicotinic receptors
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Galantamine ADR
N, weight loss, agitation and diarrhea
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NMDA receptor Antagonists
Memantine
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Memantine
noncompetitive NMDA receptor antagonist. increased glutamate release in CNS produces excitotoxic reactions and cell death, idea is to block this.
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