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39 Cards in this Set
- Front
- Back
What is the biological defect in PD? |
1. Excessive cholinergic activity 2. Deficient dopaminergic activity In the striatum |
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What is the most effective agent to tx PD? |
1. Levodopa |
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What is the MOA of levodopa? |
1. Converted to dopamine in striatal neurons 2. Dopamine responsible for therapeutic effects |
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Why can't you use dopamine to tx PD? |
1. Does not cross BBB |
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What are the adverse effects of levodopa? |
1. Dyskinesia 2. N/V 3. Postural hypotension 4. Psychosis |
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What is the effect of conventional antipsychotics on levodopa? |
1. Decrease efficacy |
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What will MAO inhibitors+levodopa cause? |
1. HTN crisis |
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What is the use of carbidopa? |
1. Used in combo with levodopa |
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What is the MOA of carbidopa? |
1. Inhibits decarboxylating enzymes in intestines and peripheral tissue 2. Increases levodopa levels |
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What is the advantage of using levodopa/carbidopa? |
1. Decrease levdopa dose--- decrease adverse effects |
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What are the disadvantages to levodopa/carbidopa use? |
1. Dyskinesias and psychiatric problems may occur sooner |
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When do levodopa effects tend to peak? When does it wear off? |
1. Peak-- middle of interdose period 2. Wear off--- constant time interval after last dose |
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How can you keep levodopa from "wearing off"? |
1. More frequent dosing 2. Controlled release formulation 3. Prolong levodopa half-life |
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What is the use of Sinemet CR? |
1. Controlled release of levodopa |
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What is the use of COMT inhibitor? |
1. Prolong levodopa half-life |
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What are the dopamine agonists? |
1. Pramipexole 2. Ropinirole |
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What is the use of dopamine agonists in the tx of PD? |
1. Patients with mild or moderate ssx |
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What are the advantages to the use of dopamine agonists? |
1. Don't depend on nigrostriatal neurons to convert levodopa 2. Don't compete with dietary protein 3. Better for long-term use 4. Can be combine with levodopa |
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What are the adverse effects of dopamine agonists? |
1. Hallucinations 2. Daytime sleepiness 3. Postural hypotension |
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What is the MOA of apomorphine? |
1. Dopaminergic agonist 2. High affinity for D4 |
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What is the clinical use of apomorphine? |
1. Rescue tx for intermittent off states 2. Adjunct drug for advanced Parkinson's |
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What are the COMT inhibitors? |
1. Entacapone |
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What is the MOA of entacapone? |
1. Blocks peripheral conversion of levodopa |
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What is the advantage of entacapone use? |
1. Less hepatotoxicity than tolcapone 2. May reduced wearing off of levodopa/carbidopa |
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What are the adverse effects of entacapone use? |
1. Raise plasma levodopa levels--- 2. Dyskinesias 3. Vomiting 4. Diarrhea/constipation 5. Urine discoloration |
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What is Stalevo? |
1. Levodopa/carbidopa/entacapone combo |
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What leads to the "on-off" effect in PD drugs? |
1. Incomplete delivery of DA 2. Variations in levodopa absorption 3. Competition from dietary substrates 4. Progressive loss of DA neurons |
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What are the selective MAO-B inhibitors? |
1. Selegiline 2. Rasagiline |
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What is the advantage of MAO-B inhibitor use? |
1. May be neuroprotective 2. Less amphetamine-like side effects |
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What are the centrally-acting muscarinic antagonists? |
1. Trihexyphenidyl 2. Benztropine |
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What is the use of centrally-acitng muscarinic antagonists? |
1. Reduce tremor and rigidity
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What is the 2o drug for tremors? |
1. Cholinergic antagonists |
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What are the adverse effects of cholinergic antagonists? |
1. Sedation, confusion, delusions, hallucinations 2. Dry mouth, blurred vision, urinary retention |
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What is the MOA of amantadine in the tx of PD? |
1. Inhibit dopamine uptake 2. Stimulate dopamine release 3. Block cholinergic receptors 4. Block glutamate receptors |
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What are the adverse effects of amantadine? |
1. Confusion, light-headedness, anxiety 2. Dry mouth, blurred vision, urinary retention |
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How do you tx restless leg syndrome? |
1. Tx iron deficiency 2. Ropinirole/pramipexole 3. >50 y/o= carbidopa/levodopa |
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What is used to tx essential tremor? |
1. Propranolol 2. Primidone (anticonvulsant) |
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How do you tx chorea in Huntington's? |
1. Tetrabenazine 2. Reserpine 3. Antipsychotics |
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How do you tx ALS? What is its MOA |
1. Riluzol--- antiglutaminergic |