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26 Cards in this Set
- Front
- Back
- 3rd side (hint)
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What is the pathophysiology of PD?
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loss of dopamine in the nigrostriatal pathway that causes the thalamus to become overstimulated with GABA
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What is the first line drug choice in PD?
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levodopa (metabolic precursor of dopamine) - can cross the BBB to get in basal ganglia and be converted to dopamine; extremely short half-life (plasma levels drop and cause on-off phenomenon, person gets sudden tremors, etc)
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What is the disadvantage of levodopa and how is it remedied?
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large doses are required because the drug gets decarboxylated in the periphery to dopamine; remedy situation by using carbidopa (blocks GI and peripheral tissue metabolism of DOPA to dopamine- doesn't get by BBB- doesn't hurt the dopamine in the CNS)
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What receptor and pathway are most involved in Parkinson's?
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D2; D2 activation inhibits the indirect pathway (causes more GABA to be released from the striatum leading to more GABA release at the thalamus (causing a net inhibition at the thalamus)
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How many dopamine receptors are there and what do they each do to cAMP?
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D1,2,3,4,5; D1 and D5 cause in increase in cAMP; D2,3,4 cause a decrease in cAMP
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What Dopamine receptor do the anti-Parkinson's dopamine agonists largely activate?
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D2
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Name the four dopamine agonist used in parkinson's treatment
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bromocriptine -ergoline-D2; also used for hyperprolactinemia), ropinirole (non-ergoline-D2), pramipexole (non-ergoline-D3),pergolide (ergoline D2,D1) (hint: old parkinson's pts BuRPP)
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Name the benefits and limitations to dopamine agonists.
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BENEFITS:directly stimulates the dopa receptor, independent of viable dopamine cells, reduces risk of dyskinesia, not affected by dietary proteins(like levadopa), delays motor complications; LIMITS:have to titrate individual dose, s/e:N/dizzy, halluncinations, illusions, somnolence, edema, compulsions
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Using what drug with l-dopa (levadopa) will prevent what?
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carbidopa + L-dopa will prevent the levadopa from being broken down in the periphery by dopa decarboxylase (carbidopa is an inhibitor of dopa decarboxylase)
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What two enzymes can metabolize levadopa into dopamine in the periphery?
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COMT and DDC (dopa decarboxylase)
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What is the role of MAOb?
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break-down dopamine in the presynaptic channel
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what is the role of COMT?
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break-down dopamine in the periphery
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Name all the major categories of drugs that can treat Parkinsons.
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precursor of dopamine(levadopa); dopamine agonists (4), MAOb inhibitors, COMT inhibitors, anti-viral(amantadine), antimuscarinics (BTB), apomorphine
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Name the 3 anti-muscarinic drugs used in PD treatment.
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BTB - benztropine, trihexyphenidyl, biperiden (decrease in dopamine causes an increase in Ach)
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Name the COMT inhibitors used in treating parkinson's disease.
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entacapone and tolcapone (hepatotoxic) - think of al capone
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None
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Name the MAOb inhibitors.
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selegiline(metabolized to weak amphetamine) and rasagiline(irreversible blocking)
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What would you need to give with apomorphine to prevent a common side-effect?
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anti-emetic - acute emesis 5-HT3 antagonist like Tigan
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Name the anti-PD drug that is a combo levadopa/carbidopa that is orally dissolvable.
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parcopa
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what is an essential tremor?
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a neurological disorder characterized by shaking of (usually) the hands, evoked by intential movements; very common; incidence and prevalence increases with age; 95% upper limbs, 34% head, benign condition
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how do you treat essential tremor?
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pharm - non-selective b-blocker, propanolol and/or anticonvulsant primidone; SURGICAL: DBS(deep brain stimulation), Thalamotomy, gamma knife thalamotomy.
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Name the disorder that is characterized by leg dysthesias that are exacerbated by inactivity, relieved by movement?
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RLS Restless Leg Syndrome
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Name the disorder that is characterized by brief, repetitive jerking of lower limbs while in stage 1 and 2 sleep; causes awakening.
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PLMD - Periodic Limb Movement Disorder
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Who commonly gets RLS Restless Leg Syndrome?
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19% of pregnant women
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Restless leg syndrome and Periodic Limb Movement Disorder is exacerbated by what?
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caffeine, TCAs, SSRIs, anemia, family history
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How do you diagnose Restless leg syndrome and PLMD?
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RLS- clinically; PLMD- sleep study
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What is the FDA approved med for RLS?
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ropinirole (dopamine agonist)
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