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22 Cards in this Set
- Front
- Back
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Levodopa (l-dopa)
Mech |
Decarbox to dopamine
activates D2 receptors and adenylyl cyclase on post jxnal striatal neurons and prejxnal axons in sub. nigra |
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Levodopa (l-dopa)
Pharmaco |
rapidly ab. GI; food dec. ab.
95% metab to dopamin in periph, so need high doses can be admin. with periph decarboxylase inhib |
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Carbidopa
(alpha-methyl dopa hydrazine) decarbox inhibitor Features |
with l-dopa
does not cross BBB dec. adverse peripheral effects of l-dopa (N&V&CV) |
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Levodopa (l-dopa)
Therapy Effects |
clinical improvement in weeks
tremor/dementia more resistant to therapy over time, neurons continue to deteriorate |
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Levodopa (l-dopa)
Side E Neuro |
1. dyskinesias - repetitive invol movements of face and limbs
2. motor fluctuations (akinesias) - dec. in vol. movement over min/hr due to wearing off of drug Rapid fluct between effects of l-dopa and no effects, usually in later stages of disease |
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Levodopa (l-dopa)
Side E Behavioral |
anxiety, insomnea
dream alteration visual hall. |
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Levodopa (l-dopa)
Side E GI |
N&V direct dopamine effects on CTZ
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Levodopa (l-dopa)
Side E CV |
post hypotension
uncommon, arrhythmias mydriasis |
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Levodopa (l-dopa)
Contraindications |
psychosis
angle closure glaucoma peptic ulcer disease melanoma |
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Levodopa (l-dopa)
Drug Interactions |
antipsychotics reduce DA effects
tricyclic antiD dec GI absorption natural aromatic AA dec GI absorption no be used with MAOA and MAO B inhib, can caus hypertensive crisis Vit B6 inc. dopa decarboxylas in periph |
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Ropinirole
Pramipexole Mech |
D2 receptor agonist
pramipexole preferres D3 |
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Ropinirole
Pramipexole Bromocriptine Treatment |
given with l-dopa;
not as long lasting b.c of dopamine receptor desensitization |
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Ropinirole
Pramipexole Side E |
similar to l-dopa
behavioral disturbances more severe - loss of impulse control pedal depma sevee hypotension (rare) |
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Amantadine
Mech |
anti-viral petentiates DA action in CNS
excreted unchanged; renal fxn impt |
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Amantadine
Side E |
headache, confusion, hall
reversible discoloration of skin (livedo reticularis) periph. edema, CHF overdose can cause toxic psychosis |
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Selegiline
Rasagiline Mech |
MOA inhibitors
MAO-B at low doses dec. DA metab in CNS |
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Selegiline
Rasagiline Contraindications |
NOT taken with SSRIs or meperidine
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Entacapone
Mech |
peripheral inhib of COMT (inhib metab of catecholamines, l-dopa)
provides smoother response to l-dopa, less fluctuations |
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Entacapone
Side E |
dyskinesias
nausea confsusion hypotension |
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Benztropine
Trihexyphenidyl anticholinergic drugs Mech |
suppress over activity of cholinergic neurons in basal ganglia
used in initial stages, younger patients, etc better effects on tremor and not bradykinesia |
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Benztropine
Trihexyphenidyl Biperiden Procyclidine anticholinergic drugs Effects |
help tremor and rigidity but not bradykinesia and postural reflexes
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Benztropine
Trihexyphenidyl Biperiden Procyclidine anticholinergic drugs Side E Contraindications |
restlessness, sedation, drymouth, mydriasis
NOT used in prostatic hypertrophy, narrow angle glaucoma, or paralytic ileus |
