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Neuro Pharmacology Flashcards

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1
Q

How can medications interfere with neuronal regulation?

A

Alter axonal conduction and synaptic transmission

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2
Q

What is a medication agonism?

A

Drug that causes the same effect that naturally occurs (receptor activation)

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3
Q

What is a medication antagonism?

A

Drug reduces or causes opposite effect (receptor deactivation)

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4
Q

What are the steps of synaptic transmission?

A

Neurotransmitter synthesis and storage

Release of neurotransmitter into cleft

Post-synaptic receptor binding

Inactivation of neurotransmitter

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5
Q

Where is the CNS location of acetylcholine?

A

Cerebral cortex, basal ganglia, limbic and thalamic regions, and spinal interneurons

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6
Q

Where is the CNS location of norepinephrine?

A

Neurons originating in brainstem and hypothalamus that project throughout other areas of the brain

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7
Q

Where is the CNS location of dopamine?

A

Basal ganglia and limbic system

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8
Q

Where is the CNS location of serotonin?

A

Neurons originating in brainstem that project upward (to hypothalamus) and downward (to spinal cord)

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9
Q

Where is the CNS location of GABA?

A

Interneurons throughout the spinal cord, cerebellum, basal ganglia, and cerebral cortex

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10
Q

Where is the CNS location of glycine?

A

Interneurons in spinal cord and brainstem

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11
Q

Where is the CNS location of glutamate, aspartate?

A

Interneurons throughout brain and spinal cord

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12
Q

Where is the CNS location of substance P?

A

Pathways in spinal cord

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13
Q

Where is the CNS location of enkephalins?

A

Pain and suppression pathways in brain and spinal cord

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14
Q

What is the effect of acetylcholine?

A

Excitation

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15
Q

What is the effect of norepinephrine?

A

Inhibition

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16
Q

What is the effect of dopamine?

A

Inhibition

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17
Q

What is the effect of serotonin?

A

Inhibition

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18
Q

What is the effect of GABA?

A

Inhibition

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19
Q

What is the effect of glycine?

A

Inhibition

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20
Q

What is the effect of glutamate, aspartate?

A

Excitation

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21
Q

What is the effect of substance P?

A

Excitation

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22
Q

What is the effect of enkephalins?

A

Excitation

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23
Q

What can drugs that affect the CNS do to movement?

A

Limit and cause involuntary movement

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24
Q

What can drugs that affect the CNS do to sleep and arousal?

A

Induce it

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25
What do drugs that affect the CNS treat?
Anxiety, depression
26
What do drugs that affect the CNS increase?
Attention and focus (affect memory)
27
What does the blood brain barrier do?
Protects against foreign substances from entering the brain (prevents entry of damaging and therapeutic substances)
28
How is the BBB achieved?
By structure and function of CNS capillaries
29
What do not pass the BBB easily?
Large molecules and highly charged molecules
30
What do not pass BBB?
Low lipid soluble molecules
31
What can pass the BBB?
Lipid soluble molecules
32
What can cause the BBB to be affected to allow easier entry of molecules?
Birth (not fully formed) Post radiation Infectious agent present Trauma (ischemic and inflammation)
33
What is used to decrease risk of future stroke?
Anti-platelet agents (aspirin)
34
What is the action of aspirin that helps reduce the risk of strokes?
Irreversibly acetylates COX-1 to prevent synthesis of TXA2, key to platelet aggregation
35
What drug is used post stroke thrombolysis?
Tissue plasminogen activators (tPA)
36
What is the action of Tissue plasminogen activators (tPA)?
Clot buster
37
What are side effects of Tissue plasminogen activators (tPA)?
Hemorrhage and mild systemic bleeding (GI or GU)
38
What should you monitor in a patient taking Tissue plasminogen activators (tPA)?
Neuro checks every 15 min for 2 hours, every 30 min for 6 hours then every hour until 24 hours (no other anticoagulants every 24 hours)
39
What is most important to do with an ischemic stroke?
Control BP
40
What are the BP recommendations post ischemic stroke?
< 185/110
41
How can you control BP?
With IV medications Labetalol Hydralazine Metoprolol Sodium nitroprusside Nicardipine drip
42
What is there an imbalance in when it comes to spasticity?
Excitatory and inhibitory input to alpha motor neuron
43
What are the motor unit changes with spasticity?
Collateral sprouting Silent synapse activation Denervation super sensitivity
44
What happens to the mechanical properties of muscle post stroke?
Sarcomere is shorter and stiffer
45
What are the treatment goals with spasticity?
Improvements in positions Mobility Contracture prevention
46
What are managements techniques for spasticity?
Ice Medications Nerve block Surgery Intrathecal meds Marijuana
47
What are the side effects of muscle relaxants?
CNS depression Sedation Anticholinergic side effects (especially in elderly)
48
Where is Botox injected for contractures?
Directly into muscle
49
How long does Botox last?
3-3.5 months
50
How long does Botox take to take effect?
<2 weeks
51
What side effects are often seen with Botox?
Hematoma and muscle weakness near injection site
52
How is intrathecal baclofen administered?
Directly into spinal canal
53
When is the onset of intrathecal baclofen?
1/2-1 hour with peak effect at 4 hours
54
How does intrathecal baclofen work?
A pump that delivers doses when needed and has to be refilled every 3 months
55
What is the mechanism of action of baclofen?
Inhibits transmission of reflexes at spinal cord (anti spasticity agent)
56
What is the mechanism of action of carisoprodol?
Blocks interneuronal activity and depresses poly synaptic neuron transmission
57
What is the mechanism of action of Chlorzoxazone?
Spinal cord and subcortical areas of the brain to inhibit reflex arcs that cause muscle spasms
58
What is the mechanism of action of cyclobenzaprine?
Reduces tonic somatic motor activity
59
What is the mechanism of action of diazepam?
Agonizes benzodiazepine subunit on GABA receptors in CNS
60
What is the mechanism of action of dantrolene?
Interferes with release of calcium ions
61
What is the mechanism of action of metaxalone?
Disrupts pain/spasm cycle through general CNS depression
62
What is the mechanism of action of methocarbamol?
Muscle relaxation via general CNS depression
63
What is the mechanism of action of orphenadrine?
Indirect muscle relaxant through central atrophine-like effects
64
What is the mechanism of action of tizanidine?
Decreases spasticity by increasing Presynaptic inhibition resulting in a reduction in spinal motor neuron conduction
65
What is Parkinson’s disease?
Degenerative and progressive disorder
66
How does Parkinson’s progress?
Unilateral Bilateral Balance issues Restricted to cane or bed
67
What are the non motor effects of Parkinson’s?
Cognitive Behavioral Dementia Disturbance of autonomic nervous system
68
What is the most effective drug for Parkinson’s?
Levodopa
69
What are side effects of levodopa?
GI CV Psych Hypotension Dyskinesia Neuropathy (prolonged use)
70
What happens with prolonged use of levodopa?
Decrease response due to controlled release formulation and adding additional medications
71
What is levodopa delayed by?
High protein meals
72
Where is most levodopa metabolized at?
The periphery (small amounts cross BBB)
73
What does the small amount of levodopa that crosses the BBB cause?
Nausea
74
What is sinemet?
Levodopa combined with carbidopa
75
Where is most of the nausea caused with levodopa?
When levodopa is converted into dopamine in the periphery
76
What prevents conversion of levodopa into dopamine in the periphery?
Adding carbidopa
77
What does carbidopa allow levodopa to do?
Cross the BBB intact with allows the conversion of levodopa into dopamine in the CNS rather than periphery
78
What is end of dose wearing off with sinemet?
Effectiveness wears off before next dose is given and there are more frequent doses given
79
What do COMTs do to levodopa?
Inhibit enzymes that degrade it to increase its availability
80
What do COMTs extend?
Half life of levodopa from 1.5 to 2.5hrs
81
When are COMTs used?
Only in combination with levodopa/carbidopa
82
What do COMTs do?
Decrease wearing off times
83
What are types of COMTs?
Entacapone and tolcapone
84
Why is tolcapone rarely used?
Due to liver toxicity
85
What are the adverse effects of COMTs?
Nausea, vomiting, diarrhea, abdominal pain, and dyskinesias
86
What is used in early stages of Parkinson’s to reduce symptoms?
Dopamine agonisds
87
What do dopamine agonists delay the need for?
Levodopa
88
What is the mechanism of action for dopamine agonists?
Stimulates dopamine receptors in the absence of dopamine
89
What are the side effects of dopamine agonists?
Orthostatic hypotension Dizziness Unsteadiness
90
What line of therapy is a dopamine agonist?
1st line
91
What is apomorphine used for?
When a patient is stuck (advanced disease)
92
What is apomorphine?
Dopamine agonist
93
What is amantadine?
Dopamine agonist (glutamate antagonist)
94
What is amantadine effective for?
Levodopa induced dyskinesia
95
What is selegiline/eldepryls place in therapy?
1st line in patients with mild disease to slow progression and need for levodopa
96
What is the mechanism of action for selegiline/eldepryl?
Decreases breakdown of dopamine
97
What happens at too large of doses of selegiline/eldepryl?
Loses its specificity (can lead to hypertensive crisis if taken with tyramine)
98
What are helpful for 1/3 of Alzheimer’s patients?
Cholinesterase inhibitors
99
What do cholinesterase inhibitors do?
Inhibit AChe breakdown which increases level of duration of ACh
100
What are side effects of cholinesterase inhibitors?
Indigestion, diarrhea, loss of appetite, slowed HR
101
Why are dopamine agonists created?
To reduce side effects of levodopa
102
What may minimize memory loss in Alzheimer’s?
Memantine (block effects of plaque production)
103
What is the effect of glutamate?
Excitatory
104
What is the effect of acetylcholine?
Excitatory
105
What is the effect of GABA?
Inhibitory
106
What is the effect of glycine?
Inhibitory
107
What is the effect of noradrenaline?
Modulatory
108
What is the effect of dopamine?
Slows locomotor pattern
109
What does the BBB play a critical role in?
Controlling influx and effluent of biological substances
110
What are the four purposes of CNS medications?
Minimize secondary damage in the acute stage Increase or decrease neurotransmission Try and slow down disease progression Minimize signs and symptoms secondary to problems that develop with neuro conditions
111
When should TPA be used for a stroke?
If the stroke occurred < 4.5 hours ago
112
What does TPA bind to?
Fibrin in the thrombus
113
What is TNK derived from?
TPA
114
What is the first choice in treatment of ICP due to trauma?
Mannitol
115
What is the mechanism of action of mannitol?
Increases serum osmolality, resulting in creation of osmotic gradient that allows fluid from the cerebral parenchyma to be drawn into the serum (reduces cerebral edema and ICP)
116
What are the side effects of mannitol?
Hypotension and dehydration
117
What are the key points of levodopa?
Treats symptoms most effectively but effects wear off 25-50% within 5 years
118
What are the key points of dopamine agonist?
Used with younger people because it can cause confusion and hallucinations
119
What are the key points of COMT inhibitors?
Can increase ON time and allows reduction of levodopa (can worsen dyskinesias)
120
What are the highly effective medications used for MS?
Methylprednisolone (corticosteroid) Ocrelizumab Ofatumumab Natalizumab
121
What was the first disease-modifying therapy available to treat MS?
Interferon beta
122
What are the adverse effects of interferon beta?
Injection site reaction and flu-like symptoms
123
What are the 2 medications for ALS that slow the progression?
Radicava Riluzole
124
What is the mechanism of action of radicava?
Free-radical scavenger (protects cells from damage inflicted by oxidative stress)
125
What is the mechanism of action of riluzole?
Neuroprotective drug that blocks glutamatergic neurotransmission in the CNS
126
How does baclofen help with spasticity?
It binds to GABA receptors to act as a GABA agonist to inhibit transmission within the spinal cord
127
How is baclofen often administered?
Orally
128
What do you need to watch for if Baclofen is administered intrathecally?
Overdose
129
What are side effects of baclofen?
Drowsiness, confusion, and hallucinations
130
What is baclofen overdose?
Leads to hypotonia and flaccid paralysis (respiratory depression and coma)
131
What is baclofen withdrawal?
Hyperreflexia and increased spasticity
132
What is the mechanism of action of Botox?
Binds to Presynaptic terminal and enters the terminal where it destroys fusion proteins so AcH cannot be released
133
What is the mechanism of action of antiseizure medications?
Inhibit excitation or enhance inhibition
134
What does phenytoin do for seizures?
Primary drug for most seizures and blocks sodium current
135
What does carbamezepine do for seizures?
Blocks sodium current
136
What does phenobarbital do for seizures?
Enhances inhibitory GABA receptors
137
What does valproic acid do for seizures?
Prevents re-uptake of GABA at synapses
138
What does benzodiazepine do for seizures?
Used to treat status epilepticus
139
What is a common side effect of anti seizure medication?
CNS depression
140
Why are Antiepileptics after used for neuropathic pain?
They appear to interfere with overactive transmission of pain signals

Pharmacology (20 decks)

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