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55 Cards in this Set

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

livedo reticularis - mottled reticulated vascular pattern that appears like a lace-like purplish discoloration of the lower extremities
Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed patients
Selegiline
Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects
Benztropine
Agent effective in physiologic and essential tremor
Propranolol
What is sumatriptan used for? What is its MOA?
1) acute migraine and cluster HA
2) 5-HT1B/1D agonist