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16 Cards in this Set
- Front
- Back
Parkinson disease cause |
Death of dopaminergic neurons in the brain, accompanied by misfolding and aggregation of α-synuclein |
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When do symptoms of parkinson appear? |
When neuronal loss is such that itcauses an 80% reduction of dopamine in thestriatum (part of the basal ganglia of the brain) |
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Familial form of Parkinsonism |
Autosomal Dominant pattern of inheritance |
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Other forms of Parkinsonism due to specific entities |
Viral Inflammation Brain Trauma, Stroke, and by poisoning by Manganese Intoxication with MPTP Idiopathic (loss of dopamine neurons with age) |
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Iatrogenic Parkinsonism |
Complication of antipsychotic therapy especially following the use of butyrophenone and phenothiazine drug classes |
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Levodopa |
Dopamine precursor (L-dopa), converted to DA by Dopa-decarboxylase. Crosses BBB On and off phenomena, due the to the decrease in number of dopamine neutrons with time. |
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Levodopa Pharmacokinetics |
Orally Proteins interfere with its absorption Taken 45 minutes before a meal Short half-life (1 to 2 hours) |
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Carbidopa |
does not cross BBB inhibits L-amino acid DOPA-carboxylase in the periphery |
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Levodopa + Carbidopa |
fewer adverse effects in the periphery and GIT |
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Tolcapone |
COMT inhibitor, an enzyme that converts Levodopa to 3OMD, which competes with Levodopa for transport into the CNS
Extend the duration of action of Levodopa Causes acute hepatic failure |
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Levodopa adverse effects |
Emesis Postural Hypotension Mydriasis Fluctuations Dyskinesia (reflects the overactivity of dopamine receptors) Contraindicated in angle-closure glaucoma |
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Ropinirole Pramipoxole Rotigotine Apomorphine |
Dopamine receptor agonists Longer duration of action than levodopa (No fluctuations Pramipexole depends on renal function for its elimination |
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Dopamine Receptor Agonists adverse effects |
Sedation Hallucination Confusion Nausea Hypotension |
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Amantadine |
Enhances DA neurotransmission by increasing synthesis or release of DA orinhibition of reuptake of DA Also antimuscarinic actions lasts only for few weeks |
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Selegiline |
Selective inhibitor of MAO type B enzyme that metabolises dopamine Therefore, increases Dopamine levels in the brain. Metabolised to amphetamine |
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Rasagilin |
Irreversible inhibitor of MAO Type B 5 times more potent than Selegiline Not metabolised to amphetamine |