Term
| ENHANCERS OF DA SYNTHESIS (4) |
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Definition
levodopa
L-DOPA + carbidopa
entacapone
amantadine |
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Term
| DOPAMINE RECEPTOR AGONISTS (4) |
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Definition
apomorphine
bromocriptine
pramipexole
ropinirole |
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Term
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Definition
benztropine
trihexyphenidyl |
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Term
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Definition
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Term
| ACETYLCHOLINESTERASE INHIBITORS (4) |
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Definition
donepezil
galantamine
rivastigmine
tacrine |
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Term
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Definition
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Term
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Definition
NMDA ANTAGONIST
USE: improve daily acivities and cognitive functions in alzheimers
Mechanism: block NMDA receptors and protects neurons from Ca overload that normally elad sot death, denefits are added when given with donezepil
Side effects: dizzy, headache, confusion, agitation, constipation |
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Term
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Definition
ACETYLCHOLINESTERASE INHIBITOR
USE: modest improvement in Alzheimers
Mechanism: block catabolism of AcH and increase its amount in presynaptic terminals
Side Effects: tremors, bradycardia, nausea, vomit, diarrhea, anorexia
Other: good oral bioavailability
- metabolized by liver ezymes
long half life |
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Term
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Definition
ACETYLCHOLINESTERASE INHIBITOR
USE: modest improvement in Alzheimers
Mechanism: block catabolism of AcH and increase its amount in presynaptic terminals
Side Effects: tremors, bradycardia, nausea, vomit, diarrhea, anorexia
Other: good oral bioavailability
- 7 hr half life, metabolize dby liver |
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Term
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Definition
ACETYLCHOLINESTERASE INHIBITOR
USE: modest improvement in Alzheimers
Mechanism: block catabolism of AcH and increase its amount in presynaptic terminals
Side Effects: tremors, bradycardia, nausea, vomit, diarrhea, anorexia
Other: good oral bioavailability
- 1.5 hr half life
metabolized by plasma cholinesterase |
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Term
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Definition
ACETYLCHOLINESTERASE INHIBITOR
USE: modest improvement in Alzheimers
Mechanism: block catabolism of AcH and increase its amount in presynaptic terminals
Side Effects: tremors, bradycardia, nausea, vomit, diarrhea, anorexia
Other: good oral bioavailability
- 3 hr half life and metabolized by liver |
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Term
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Definition
MAOB INHIBITOR
USE: adjunct with Parkinsons and L-DOPA
Mechanism: selective ihibitor of brain MAO-B
Other - not metabolized to amphetamine like substance decreasing side effects |
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Term
| SELEGILINE (l-DEPRENYL OR ELDEPRYL) |
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Definition
MAOB INHIBITOR
USE: adjunct treatment in Parkinsons with L-DOPA
Mechanism: inhibits MAOB and decreases production of byproduce H2O2 and limits ROS, little benefit when taken alone
Other: oral, renal exretion, metabolized to methamphetamine and amphetamines giving side effects like insomnia |
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Term
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Definition
ANTICHOLINERGIC
USE: alleviated tremor and rigidity as monotherapy or with other dugs
Mechanism: loss of nigrostriatla neurons leads to increased firing of striatal cholinergic interneurons and overstimulation of muscarinic receptors so this antagonist blocks this
Side effects: antimuscarinic effects like blurred vision, dry mouth, urinary retention, constipation, aggravating glaucoma, delirium psycosis, memory impairment |
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Term
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Definition
ANTICHOLINERGIC
USE: alleviated tremor and rigidity as monotherapy or with other dugs
Mechanism: loss of nigrostriatla neurons leads to increased firing of striatal cholinergic interneurons and overstimulation of muscarinic receptors so this antagonist blocks this
Side effects: antimuscarinic effects like blurred vision, dry mouth, urinary retention, constipation, aggravating glaucoma, delirium psycosis, memory impairment |
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Term
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Definition
DOPAMINE RECEPTOR AGONIst
USE: monotherapy or adjunct with L-DOPA for parkinsons
Mechanism: D2 and D3 agonist
Other: orally
active, begin with low doses and gradually increase keeping side effets minial
Side effects: cardiac arrythmia, postural hypotension, depression confusion, hallucination, sleepiness, impulsivity, nausea, vomit
Contraindicated with heart or mental problems
usual maintenance = 10-30 mg/day |
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Term
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Definition
DOPAMINE RECEPTOR AGONIST
USE: monotherapy or adjunct with L-DOPA for parkinsons
Mechanism: D2 and D3 agonist
Other: orally active, begin with low doses and gradually increase keeping side effets minial
usual maintenance = 10-30 mg/day
Side effects: cardiac arrythmia, postural hypotension, depression confusion, hallucination, sleepiness, impulsivity, nausea, vomit
Contraindicated with heart or mental problems
usual maintenance = 10-30 mg/day |
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Term
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Definition
DOPAMINE RECEPTOR AGONIST
USE: monotherapy in diseae or adjunct to L_DOPA
Mechanism: D2 agonist and D1 partial agonist
Other: orally active, begin with low doses and gradually increase keeping side effets minial
usual maintenance = 10-30 mg/day
Side effects: cardiac arrythmia, postural hypotension, depression confusion, hallucination, sleepiness, impulsivity, nausea, vomit
Contraindicated with heart or mental problems |
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Term
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Definition
DOPAMINE RECEPTOR AGONIST'
USE: acute treatment with advanced parkins for off periods with bradykinesia and immobility
SUBQ injection (IV can lead to PE)
Side effect: nausea, vomit, arrythmia, postural hypotension, hallucination, sleepiness |
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Term
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Definition
ENAHNCER OF DA SYNTHESIS
USE: alleviate bradykinesia and rigidity with mild to moderate parkinsons before giving L-DOPA
Mechanism: moderately increases DA release and blocks cholinergic M receptors and Glutamine NMDA receptors
SIde effects: hallucinations, confusion, nausea, dizziness, rash of lower extremities,
conrtaindication in some heart disease ang glaucoma
- also an antivirla for influenza |
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Term
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Definition
ENHANCER OF DA SYNTHESIS
USE: can be added to L-DOPA and carbidopa to decrease peripheral metabolism and increase L-DOPA in the brain |
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Term
| L-DOPA + CARBIDOPA (SINEMET) |
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Definition
ENHANCER OF DA SYNTHESIS
Use: med of choice to treat Parkinsons, espcialley at advanced stage
mechanism: carbidopa blocks peripheral metabolism and increases L-DOPA to the brain allowing reduction of L-DOPA dose reducing side effects |
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Term
| LEVODOPA (l-DOPA, DOPAR, LARDOPA) |
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Definition
ENHANCER OF DA SYNTHESIS
Use: decrease rigitity, tremors, and other symptoms of parkinsons
Mechanism: precursor of dopamine that crosses BBB
other: after 305 years there is a wearing off effect, oral rapidly absorbed, only 1-3% reaches brain counteracting ROS, short half life of 1-2 hours
Side effects: nausea, vomit, anorexia, cardiac arrythmia, orthostatic hypotension, visual and auditory hallucinations, abnormal involuntrary movement or dyskinesia, mood change |
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Term
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Definition
| rigid with bradykinesia = parkinsonism |
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Term
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Definition
| choreic and jerky = huntingtons - gentic with only striatal neurons effected |
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Term
| AMYOTROPHIC LATERAL SCLEROSIS (als) |
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Definition
| neurodegenerative disease involving muscle weakness and atrophy due to degeneration of motor neurons in the spinal cord and cerebral cortex |
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Term
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Definition
neurodegeneration charcterized by dementia due to degeneration fo neurons in the hippocampus and cerebral cortex
- impaired short term memory and cognitition, most commone dementia in adults
- memory loss, language deteriorates, impaire mental ability to manipulate visula infor, poor judgement, confusion , mood swings |
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Term
| factors in selective neurodegeneration |
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Definition
1. genetic and environmental
2. excitotoxicity
3. energy metabolism
4. free radicals |
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Term
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Definition
progressive disorder of muscle movement
- bradykinesia, tremors, rigdigity abnormal posture, mask like face and shuffling, impaired speech |
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Term
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Definition
degeneration of nigrostriatal dopamine neurons in the striatum - substantia nigrra
>80% of neurons degenerate before symptoms
presence of lewy bodie sin surviging neurons
a-synuclein misfolds and converts to lewy bodies |
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Term
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Definition
idiopathic
- aging, environment, genetic |
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Term
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Definition
| disorders resembling Parkinsons but has a known cause and different rates of progression such as multiple small strokes, brain injury and antipsychotics |
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Term
| Direct pathway in basal ganglia |
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Definition
controlled by D1 receptors
- dopamin activated GABA and inhibits GABA neurons that go to the thalamus for increased movement |
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Term
| Indirect pathway in the basal ganglia |
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Definition
D1 receptors control it
- Dopamine inhibits pathways and activates GABA, inhibits Glutamate and decreases activity of GABA to the thalamus leadinging to decreased movement |
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Term
| Abnormal function of basal ganglia paths in Parkinsons |
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Definition
| reduce amoutn fo dopamine at D1 and D1, direct path inhibited and indirect path activated, GABA neuraons activated, glutamate inhibtied leading to disinhibition of indirect path and decreaed movement |
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Term
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Definition
Increase DA synthesis = L-DOPA,L-DOPA + carbidopa, entacapone
Decrease DA catabolism = selegiline, rasalgiline
DA receptor agonists = bromocriptine, ropinirole, pramipexole, apomorphine
antagonist of M cholinergics - benzropine, trihyxyphenidyl
other: amantadine - block NMDA |
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Term
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Definition
degenerate base forebrain cholinergic neurons
- preence of amyloid plaqes and neurofibrillary tangles
neuron and synapse loss in cerebral cortex and hippocampus |
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Term
| risk factors in alzheimers |
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Definition
age (1% for 65-70) and 6-8% iover 85
genes - 10% are familial with a mutation in APP, PS1 or PS2 gene |
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Term
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Definition
| Aceytlcholinesterase inhibitors and NMDA receptor inhibitor |
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