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33 Cards in this Set

  • Front
  • Back
Phenylpropionic Derivatives
- type of drug
- mechanism
- adverse effects
- largest group of aspirin alternatives
- inhibit cyclo-oxygenase and prostaglandin synthesis
- cause fewer GI side effects than aspirin so are being used in place of aspirin
Celecoxib
- type of drug
- mechanism
- what do they treat
- adverse effects
- new NSAIDs
- inhibit COX-2
- rheumatoid arthritis and osteoarthritis
- could cause cardiovascular damage
Combination Preparations
- what are the 3 combinations
- aspirin + Acetaminophen
- NSAIDs + caffeine
- NSAIDs + Opioid
what drug is used to treat migraine headaches
Sumatriptan
what happens in the brain that leads to Parkinson's disease
progressive and selective loss of neurons from specific brain regions
what are some other neurodegenerative disorders
ALS
Alzheimer's disease
Huntington' disease
what are the 4 symptoms of Parkinson's disease
muscular rigidity
tremor
bradykinesia
postural instability
Parkinsons is an idiopathic disease that if left untreated will do what
progress to a rigid, akinetic state in which patients can no longer care for themselves
the therapy of Parkinson's is to enhance action of what
dopamine in the CNS
what is the first mechanism to enhance action of dopamine
replacement of CNS dopamine by giving the dopamine precursor L-DOPA
what is the immediate precursor of dopamine
Levodopa
Levodopa
- what does it do
- increases dopamine production within the basal ganglia
usually combined with a peripheral dopa-decarboxylase inhibitor to decrease side effects
the combination of Levodopa combined with peripheral dopa-decarboxylase inhibitor is called what
sinemet
what is the 2nd mechanism to enhance action of dopamine
administration of direct acting dopamine agonists
what are the 2 dopamine receptor agonists
bromocriptine
pramipexole
what do bromocriptine and pramipexole do
directly stimulate CNS post synaptic dopamine receptors
what is the 3rd mechanism to enhance action of dopamine
use of agents that alter dopamine metabolsim or synaptic concentration
what is the MAO-B inhibitor (i have no idea what this means)
selegiline
(oh of course)
what does the MAO-B inhibitor, selegiline do
blocks major pathway in dopamine metabolism thus increasing the duraction of action of dopamine
what is the 4th and final mechanism to enhance the action of dopamine
a depression of unopposed CNS cholinergic systems
what does benztropine do to enhance dopamine
blocks the increased excitatory activity of cholinergic interneurons on outflow pathways from basal ganglia, secondary to the loss of dopamine inhibition of these neurons
a primary therapy for Parkinson's is dopamine replacement via the use of what
levodopa (L-DOPA)
does dopamine cross the blood brain barrier
no
b/c dopamine does not cross the blood brain barrier, what does this mean
large doses of the immediate metabolic precursor which does enter the brain where its converted to dopamine
what % of administered L-DOPA enters the brain with the majority converted to dopamine
1%
so high doses must be given which gives a lot of side effects
b/c of the side effects of large doses, L-DOPA is given with what
carbidopa
- a peripheral DOPA sinemet
carbidopa will greatly reduce the peripheral side effects but will not reduce what
CNS untoward effects
what are the 2 dopamine agonists
Bromocriptine
Pramipexole
Dopamine Agonists
- duration of action
- mechanism
- longer duration of action
- provide direct stimulation of CNS dopamine receptors and do not require enzymatic conversion to dopamine
Bromocriptine
- type of drug
- mechanism
- non-selective dopamine agonist
- stimulates both D1 and D2- like dopamine receptors
Pramipexole
- type of drug
- mechanism
- dopamine agonist
- selective stimulants of D2 dopamine receptor
produce fewer side effects
Selegiline
- type of drug
- mechanism
- monoamine oxidase (MAO) inhibitor
- inhibitor of MAO that increases dopamine levels by reducing its metabolic inactivation
Benztropine
- type of drug
- mechanism
- adverse effects
- muscarinic receptor antagonists
- block cholinergic mechanisms in the striatum that are normally opposed by tonic release of dopamine
- cycloplegia, dry mouth, urinary retention
- with high doses, CNS effects (confusion, hallucinations) may occur
may improve tremor and rigidity