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66 Cards in this Set
- Front
- Back
loss of cholinergic neurons in nucleus basalis of Maynert
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in Alzhemier's disease
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loss of striatal projection neurons
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huntington's disease
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loss of dopaminergic neurons in the substantia nigra
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parkinson's disease
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what four features charac parkinson's disease
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bradykinesia
muscular rigidity resting tremor impairment of postural balance |
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what are the forst symptoms to appear in parkinson's diases
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rolling tremor of the hand and mask like face
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what is the rate limiting step in the dopamine synthesis
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conversion of tyrosine>L-DOPA by tyrosine hydroxylase
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what enzyme is abudant in brain
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DOPA decarboxylase: conv L DOPA to dopamine
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cytoplamic dopamine is degraded by
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MAO
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what receptors are lost in parkinson disease
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D2: found in substantia nigra
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by th time first symptoms appear +______%of neurons are lost
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70
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death___% of neurons are lost
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90
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dopamine action is
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inhibitory
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can dopamine cross BBBB
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nop
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inceased dopamine in the peripheral system causes
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nausea, vommiting, orthostatic hypotension
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what are the drugs that act as dopamine precursors
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levodopa
carbidopa |
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inhibitors of dopamine metabolism is
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selegiline
rasagiline |
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COMT inhibitors
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entacapone
tolcapone |
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dopamine receptor agonists
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bromocriptine
apomorphine pramipexole ropinirole rotigotine |
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nondopamergic
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amantadine
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levodopa (L DOPA)
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readily crosses BBB
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L-Dopa side effcets in peripheral system are
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nausea, vommiting, cardiac arrthymias, hypotension
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what _%L-DOPA reaches CNS
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1-3%
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what is an inhibitor of DOPA decarboxylase
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carbidopa: does not cross BBB
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how is carbidopa benefoicial
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prevents the peripheral side effects as it prevents the conversion of L-DOPA to dopamine in peripheral system
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L-DOPA is always adminstered with
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carbidopa
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brown saliva and urine
hypotension anorexia nausea' vomitting mydriasis |
side effcets of L-DOPA and carbidopa
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visual and
hallunication dyskineasea mood changes, depression, psychosis anxiety |
all CNS side effects LDOPA and carbidopa
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vitamin pyridoxine (b6)
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increases peripheral breakdown of L-DOPA
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can excerbate symptoms in psychotic patients
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L-DOPA and CArbidopa
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can increases intraocular pressure in glaucoma patients
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L-DOPA and CArbidopa
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can cause cardiac arrthymias
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L-DOPA and CArbidopa
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antipsychotic drugs
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can potentially block dopamine R's
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selegiline and rasadiline are
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MAO-B inhibitors not MAO-A
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severe hypertension
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selegiline
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selegiline is metabolized to
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methamphetamine and amphetamine
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not metabolized to amphetamine like substances
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rasagiline
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5X more potent than selegilien
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rasagiline
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irreversible non selective inhibitor of brain MAO-B
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rasagiline
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fluminating hepatic necrosis
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COMT inhibitors(tolcapone only)
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extensively bound to albumin
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COMT inhibitors(tolcapone and entacapone)
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COMT that is not hepatotoxic
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entacapone
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what are the adverse effects of COMT inhibitors(tolcapoen and entacapone)
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diarrhea, postural hypotension, nausea, anorexia, dyskinesias, hallucinations, sleep disorders.
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which COMT inhibitor has greater duration of acti0n
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tolcapone
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which COMT can penetrate BBB
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tolcapone and inhibit COMT in brain
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ergot dopamine agonists
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bromocriptine
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bromocriptine is contraindicated in which gp of people
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history of MI
peripheral vascular disease peptic ulcers psyc illness |
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peptic ulcers so what is CI
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bromocriptine
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what are the non ergot dopamine agonists
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apomorphine
pramipexole ropinirole rotigotine |
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which ones do not compete for BBBB
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non ergot dopamine agonists
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available in trandermal formulations
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rotigotine
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inhibitors of CYP1A2
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ropinirole(non ergot dopamine agonists)
D3R>D2R. |
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depends on good renal function for elimination
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pramipexole
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used for acute management of Off phenomenon
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apomorphine
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powerful emetic drug and is a opiod but do not bind to opiod receptors
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apomorphine
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which one play only adjuvant role in aniparkinson therapy
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antimuscranics
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pyloric stenosis
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CI is antimuscranics
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antimiscranics are CI in
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glaucoma
prostatic hyperplasia pyloric stenosis |
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increases release of dopamine, blocks cholinergic receptors and inhibits NMDA glutamate receptors
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amantadine
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little effect on tremor but more effective than anticholinergics against rigity and bradtkinesia
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amantadine
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what other porposes is amantatide used
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ANTI VITAL AGENT FOR INFLUENZA A
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in high doses cause acute toxic psychosis
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amantadine
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restlessness,
agatation confusion hallucinations orthostatic hypotension urinary retyension peropheral edema dry mouth |
all are the side effects of amantadine
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mood changes
dryness of mouth vision problems pupillary dilation hallucinatins urinary retension sinus tachycardia constipation are all side effects of |
antimuscranics
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has largely repalced tolcapone
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entacapone
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forms of toxic metabolite amphetamine (can lead to insomnia and confusion in elderly)
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selegiline
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treats L-DOPA induced dyskinesias in late stages
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amantadine
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