Glossary of T2 anti-parkinson's and other motor disorder - pharm
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- What is the pathophysiology of PD?
- loss of dopamine in the nigrostriatal pathway that causes the thalamus to become overstimulated with GABA
- What is the first line drug choice in PD?
- 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)
- What is the disadvantage of levodopa and how is it remedied?
- 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)
- What receptor and pathway are most involved in Parkinson's?
- 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)
- How many dopamine receptors are there and what do they each do to cAMP?
- D1,2,3,4,5; D1 and D5 cause in increase in cAMP; D2,3,4 cause a decrease in cAMP
- What Dopamine receptor do the anti-Parkinson's dopamine agonists largely activate?
- Name the four dopamine agonist used in parkinson's treatment
- 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)
- Name the benefits and limitations to dopamine agonists.
- 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
- Using what drug with l-dopa (levadopa) will prevent what?
- carbidopa + L-dopa will prevent the levadopa from being broken down in the periphery by dopa decarboxylase (carbidopa is an inhibitor of dopa decarboxylase)
- What two enzymes can metabolize levadopa into dopamine in the periphery?
- COMT and DDC (dopa decarboxylase)
- What is the role of MAOb?
- break-down dopamine in the presynaptic channel
- what is the role of COMT?
- break-down dopamine in the periphery
- Name all the major categories of drugs that can treat Parkinsons.
- precursor of dopamine(levadopa); dopamine agonists (4), MAOb inhibitors, COMT inhibitors, anti-viral(amantadine), antimuscarinics (BTB), apomorphine
- Name the 3 anti-muscarinic drugs used in PD treatment.
- BTB - benztropine, trihexyphenidyl, biperiden (decrease in dopamine causes an increase in Ach)
- Name the COMT inhibitors used in treating parkinson's disease.
- entacapone and tolcapone (hepatotoxic) - think of al capone
- Name the MAOb inhibitors.
- selegiline(metabolized to weak amphetamine) and rasagiline(irreversible blocking)
- What would you need to give with apomorphine to prevent a common side-effect?
- anti-emetic - acute emesis 5-HT3 antagonist like Tigan
- Name the anti-PD drug that is a combo levadopa/carbidopa that is orally dissolvable.
- what is an essential tremor?
- 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
- how do you treat essential tremor?
- pharm - non-selective b-blocker, propanolol and/or anticonvulsant primidone; SURGICAL: DBS(deep brain stimulation), Thalamotomy, gamma knife thalamotomy.
- Name the disorder that is characterized by leg dysthesias that are exacerbated by inactivity, relieved by movement?
- RLS Restless Leg Syndrome
- Name the disorder that is characterized by brief, repetitive jerking of lower limbs while in stage 1 and 2 sleep; causes awakening.
- PLMD - Periodic Limb Movement Disorder
- Who commonly gets RLS Restless Leg Syndrome?
- 19% of pregnant women
- Restless leg syndrome and Periodic Limb Movement Disorder is exacerbated by what?
- caffeine, TCAs, SSRIs, anemia, family history
- How do you diagnose Restless leg syndrome and PLMD?
- RLS- clinically; PLMD- sleep study
- What is the FDA approved med for RLS?
- ropinirole (dopamine agonist)
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