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55 Cards in this Set
- Front
- Back
What is another name for parkinsons?
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paralysis agitans
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Signs of parkinsons include?
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rigidity,akinesia, flat facies, tremor
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Pathologically what occurs in Parkinsons?
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decrease dopamine in nigrostriatal tract that inhibit striatal GABAergic neurons
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Most postsynaptic receptors on GABAergic neurons are what?
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D2 which are negatively coupled to adenylyl cyclase
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Which drugs cause parkinsons?
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Antipsychotics
1) butyrophenone 2) phenothiazine Others 1) resperpine |
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What byproduct of synthetic heroine production can cause irreversible parkinsonism?
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MPTP is a meperidine analog that destroys dopaminergic neurons in the nigrostriatal tracts
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Antiparkinson drugs act on what receptor?
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D2
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What is the MOA of carbidopa? Where in body does it work?
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1) given Levodopa
2) can NOT cross blood brain barrier 3) Inhibits DOPA decarboxylase peripherally |
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What are toxicities of levodopa?
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1) anorexia, Nausea, emesis
2) postural hypotension 3) tachycardia, asystole, arrythmias 4) chorea, ballismus, myoclonus, tics, tremor 5) anxiety, agitation, confusion, delusions, hallucinations, depression |
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Who is levodopa contraindicated in?
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people with psychosis
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What is the MOA of bromocriptine and pergolide?
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ergot alkaloids that are partial agonists of D2 receptors in brain
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What are toxic effects of bromocriptine and pergolide?
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1) anorexia, nausea, vomiting
2) postural hypotension, arrythmias 3) dyskinesias 4) confusion, hallucinations, delusions |
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Who is bromocriptine contraindicated in?
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psychotic patients
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Why was pergolide removed from the market?
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it was implicated in cardiac valvular disease
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What are ergot related effects of bromocriptine?
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pulmonary infiltrates and erythromelalgia
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What is the MOA of ropinirole and pramipexole?
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ropinirole: D2 receptor agonist
pramipexole: D2 and D3 receptor agonist and is neuroprotective by scavenging H2O2 |
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What are toxicities of pramipexole and ropinirole?
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1) anorexia, nausea, vomiting
2) dyskinesias, 3) postural hypotension, lassitude |
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What enzyme metabolizes ropinirole? What other drugs does it metabolize?
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1) CYP1A2
2) caffeine and warfarin |
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What is the MOA of apomorphine?
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dopamine receptor agonist providing relief for 1-2 hours
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What are the side effects of apomorphine?
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1) nausea
2) have to take with antiemetic trimethobenzamide 3) dyskinesia 4) hypotension 5) drowsiness 6) sweating |
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What is the MOA of amantadine?
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1) enhances dopaminergic neurotransmission
2) may block muscarinic receptors |
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Taking amantadine can improve what?
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1) bradykinesia
2) rigidity 3) tremor 4) influenza type a |
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What are side effects of amantidine?
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1) restlessness, agitation, insomnia, confusion, hallucinations, acute toxic psychosis
2) LIVEDO RETICULARIS ( mottled reticulated vascular pattern that appears like a lace-like purplish discoloration of the lower extremities) 3) GI problems, urinary retention, postural hypotension and EDEMA |
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What is the MOA of selegiline rasagiline?
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inhibitor of MAO-B which metabolizes dopamine in preference of NE and epinephrine
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What are the toxic effects of selegiline and rasagiline?
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1) insomnia, mood change
2) dyskinesia 3) GI distress 4) hypotension |
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Meperidine in combination with selegiline has resulted in what?
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1) agitation
2) delerium 3) death |
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What anti-parkinson drug has been implicated in serotonin syndrome when patients are also taking an SSRI?
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selegiline
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What is the MOA of entacapone and tolcapone?
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inhibit COMT which converts levodopa to 3-O-methyldopa
Note: 3OMD competes with levodopa for transport into the CNS |
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What are the toxic effects of entacapone and tolcapone?
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1) dyskinesias, GI and postural
2) ORANGE discoloration of urine 3) Tolcapone has caused liver failure |
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Which antimuscarinic drugs are used in parkinsons?
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1) benztropine
2) trihexyphenidyl |
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Which features of parkinsons do antimuscarinic effect? what don't they treat?
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Improve:
1) tremor 2) rigidity 3) reverse extrapyramidal symptoms caused by antipsychotics ***Do NOT help with bradykinesia*** |
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What are toxicities of antimuscarinics?
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1) drowsiness, inattention, confusion, delusions and hallucinations
2) peripherally act like atropine 3) exacerbate tardive dyskinesias from antipsychotic drugs |
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How can tremors be treated?
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1) propanol = beta blocker
2) metoprolol = beta 1 selective blocker 3) antiepileptic drugs including primidone and topiramate |
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Who should propanol be used with caution in?
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CHF, asthma, diabetes or hypoglycemia
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tremor in someone that also has pulmonary disease might benefit from?
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metoprolol
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How is essential tremor treated?
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1) propanol
2) primidone 2) topiramate |
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How is Huntingtons treated?
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1) reserpine and tetrabenazine = amine depleting drugs
2) haloperidol = dopamine receptor antagonist |
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How is tourettes treated?
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1) haloperidol
2) D2 receptor blockers (pimozide) 3) Carbamazepine, clonazepam, clonidine |
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How are acute dystonias treated?
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1) benzotropine
2) diphenhydramine (anti-H1) Note: levodopa and bromocriptine are not helpful because dopamine receptors are blocked by antipsychotics |
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What causes tardive dyskinesias?
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older antipsychotics form a denervation supersensitivity
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How is Wilsons disease treated?
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pencillamine (dimethylcystiene) removes excess copper
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What are the toxic effects of pencillamine?
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1) GI distress
2) MYASTHENIA 3) optic neuropathy 4) BLOOD DYSCRIAS |
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What is restless leg syndrome? who is it common in?
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1) idiopathic unpleasant creeping discomfort of limbs at rest
2) common in pregnant women, uremic and diabetic patients |
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How is restless leg syndrome treated?
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1) dopaminergic therapy and ropinirole
2) can use opioid analgesics and benzos |
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Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia
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Bromocriptine
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Irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog)
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Drug induced Parkinsonism
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This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias)
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Carbidopa
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Clinical response that may fluctuate in tx of Parkinson's dx
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"On-off-phenomenon"
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Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
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Levodopa
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Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia (severe burning, itching and swelling of hands)
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Bromocriptine
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Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis
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Amantadine
livedo reticularis - mottled reticulated vascular pattern that appears like a lace-like purplish discoloration of the lower extremities |
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Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed patients
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Selegiline
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Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects
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Benztropine
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Agent effective in physiologic and essential tremor
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Propranolol
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What is sumatriptan used for? What is its MOA?
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1) acute migraine and cluster HA
2) 5-HT1B/1D agonist |