CNS drugs - EX 4 Flashcards
1
Q
What are the CNS neurotransmitters?
A
Acetylcholine, Glutamate, Dopamine, and GABA
2
Q
What is acetylcholine used for?
A
memory and learning
3
Q
What is dopamine used for?
A
“Joy” and motor control
4
Q
What is glutamate used for?
A
memory
5
Q
what is GABA used for?
A
memory and movement
6
Q
What is parkinson’s disease?
A
too little dopamine and too much acetylcholine
7
Q
What two types of medications treat parkinsons
A
Dopaminergic agnes (more commonly used) and anticholinergic agents
8
Q
How do dopaminergic agent work to treat parkinsons
A
directly or indirectly activate dopamine receptors
9
Q
how do anticholinergic agents works to treat parkinsons
A
blocks receptors for acetylcholine
10
Q
what is Levodopa?
A
Dopamine replacement
11
Q
what is the MOA of Levodopa
A
increases the amount of available dopamine
12
Q
what does it mean that Levodopa is a prodrug
A
converted into active form after crossing BBB (inactive until reaching brain)
only 2% reaches the brain
13
Q
Important considerations for Levodopa
A
food delays absorption, esp meals high in protein
short T1/2 of 1-2 hrs
“loss of effect” common
14
Q
adverse effects of Levodopa
A
N/V
Dyskinesis (involuntary mvt)
Cardiovascular
Psychosis
Harmless darkening of sweat and urine
15
Q
what are the drug interactions of Levodopa? (bad vs. good)
A
bad: meds that block dopamine receptors
- not given with first class antipsychotics
good: anticholinergics block acetylcholine
-
16
Q
Education considerations for levodopa
A
- take without food
-requires multiple doses in a day - darkens sweat and urine
- report loss of effect
- rise slowly
- report any new tremors, palpitations, hallucinations/paranoia
17
Q
what is Carbidopa/Levodopa
A
Sinemet
18
Q
Carbidopa/Levodopa works how?
A
as a crossing guard
prevent decarboxylase actions
19
Q
Carbidopa/Levodopa allows what?
A
to give a lower dose of levodopa
20
Q
Carbidopa/Levodopa is only available how?
A
in a combo pill
21
Q
What is Entacapone/levodopa/carbidopa
A
stalevo
22
Q
how does Entacapone/levodopa/carbidopa work
A
like a RR crossing arm
inhibits COMT enzyme from breaking down levodopa
23
Q
COMT stands for
A
catechol-o-methyltransferase
24
Q
Entacapone/levodopa/carbidopa action:
A
extends half life of levodopa
25
Entacapone/levodopa/carbidopa only available in what form?
combo pill
26
Pramipexole is what
dopamine receptor agonist
27
what is the MOA of Pramipexole
directly activates dopamine receptors in the brain
28
when is Pramipexole of used?
in first line
alone in early stages
used with levodopa/carbidopa in advanced stages
29
what are the adverse side effects of Pramipexole?
- produced by receptor activation
Pramipexole alone: nausea, dizziness, weakness, sleep changes
Pramipexole + levodopa/carbidopa O-hypotension, dyskinesias, hallucinataions
- * sleep attacks *
- impulse control disorders/ compulsive behaviors
30
education considerations for Pramipexole
- OK to take w/meals
- rise slowly
- report sleep attacks
- report any impulse control concerns
31
For alzheimer's what do pts. have low levels of
acetylcholine
32
what are the two major drug classes to treat alzheimers
cholinesterase inhibitors
NMDA antagonists
33
Donepezil is what
cholinesterase inhibitor
34
MOA of Donepezil
prevents breakdown of acetylcholine
35
benefits of Donepezil
improved QOL, memory, reasoning
36
does Donepezil delay alzheimer's disease progression?
no
37
considerations for Donepezil
highly protein bound = long half life
increase in acetylcholine causes cholinergic effects
38
cholinergic side effects (Donepezil effects)
SLUDGE
Salivation
Lacrimation
Urination
Defecation
Gastric upset
Emesis
39
what is rivastigmine
cholinesterase inhibitor
40
what is the MOA of rivastigmine
prevents breakdown of acetylcholine
41
benefits of rivastigmine
improved QOL, memory, reasoning
42
does rivastigmine delay disease progression?
no
43
considerations of rivastigmine
available as a transdermal patch
44
adverse side effects of rivastigmine
increase acetylcholine causes cholinergic effects (SLUDGE) and CV effects (bradycardia --> fainting, falls)
45
what is memantine
NMDA antagonist
46
what is the memantine MOA
blocks NMDA receptors and prevents excessive calcium accumulation in the neurons
47
benefits of memantine
slow decline, may improve symptoms
48
does memantine modify the underlying disease process
no
49
what are the adverse effects of memantine
minimal
potential effect: donepezil and memantine
50
what is Multiple Sclerosis?
chronic, progressive, inflammatory, autoimmune disorders affecting the myelin sheath of neurons on the spinal cord
51
what type of MS are we focusing on?
relapsing-remitting
52
immunomodulator considerations
- not just for MS
- indicated for all pts. w/relapsing-remitting subtype
- very expensive
53
what is interferon beta
immunomodulator
54
how does interferon beta work
slows inflammation of CNS myelin
55
how is interferon beta administered
parenterally (SQ or IM); dosing interval varies
56
what are the adverse effects of interferon beta
common - flu like symptoms
hepatotoxicity
bone marrow suppression
injection site problems
headache
57
when pts have a headache as a side effect of interferon beta is it okay to take tylenol or ibuprofen?
yes
58
immunosuppressants considerations
- less preferred (stronger immunosuppression and more toxic)
- used in pts who don't respond to immunomodulators
- effective against all subtypes of MS
59
what is mitoxantrone?
immunosuppressant
60
how does mitoxantrone work
suppresses productions of immune cells
61
how is mitoxantrone administered?
IV infusion every 3 months
62
adverse effects of mitoxantrone
hepatotoxicity - monitor LFTs
Bone marrow suppression - infections precautions
Cardiotoxicity - looks like HF
Toxic to frequently dividing cells - teratanogenic
63
how do you treat the MS symptom fatigue?
stimulants, SSRIS
64
how do you treat the MS symptom muscle spasticity
CNS muscle relaxants
65
how do you treat the MS symptom neuropathic pain
antiepileptics, antidepressants
66
how do you treat the MS symptom bladder dysfunction
anticholinergic or alpha adrenergic blocker drugs
67
how do you treat the MS symptom constipation
bulk laxatives, stool softeners
68
how do you treat the MS symptom sexual dysfunction
lubricant for women, sildenafil (viagra) for men
69
what is the treatment for acute MS flares?
high dose IV steroids for 3-5 days
70
what does a high dose of steroids for 3-5 days to treat an MS flare cause
reduces acute inflammation
71
What is the first way Antiepileptic drugs (AEDs) work
suppression of sodium influx in cell membranes = decreases ability of neurons to fire at high frequency
72
what is the second way Antiepileptic drugs (AEDs) work
suppression of calcium influx in axon terminals = blocks channels to suppress transmission
73
what is the third way Antiepileptic drugs (AEDs) work
antagonism of glutamate - NT
74
what is the fourth way Antiepileptic drugs (AEDs) work
potentiation of GABA - NT
75
what is the goal of using AEDs
decrease focal epileptic activity and prevent spread to other areas of the brain
76
AED consideration
adherence is important to meet therapeutic response
77
traditional AED consideration
less expensive
teratogenic
more interactions
more adverse effects
78
new AED considerations
more expensive
safer in pregnancy
less interactions
less adverse effects
79
Traditional AED examples and MOA
Phenytoin - sodium channel suppression
Phenobarbital - potentiates GABA
Valproic acid - sodium channel suppression and GAB potentiation
80
Newer AED example and MOA
Oxcarbazepine - sodium channel suppression
81
Phenytoin considerations
NTI drug - therapeutic levels 1-20 mcg/Ml
first line med and most widely used
long T1/2 life
82
How is Phenytoin metabolized?
liver is easily overwhelmed by this drug = toxic levels
half life is dose dependent (8-60 hrs)
CYp enzyme inducer
83
adverse effects of phenytoin
CNS effects
- headache, drowsiness, irritability,
- levels >20 mcg/mL: Nystagmus, sedation, ataxia, diplopia, cog impairments
Gingival hyperplasia
Rash
Teratogenic
lots of drug interax
84
Valproic acid used for
all major seizure types and bipolar disorder and migraines
85
Valproic acid adverse effects
GI effect common, rare hepatotoxicity, SERIOUS teratogen
86
Phenobarbital consideration
sedation
many adverse side effects
87
oxcarbazepine adverse effects
CNS
Rare- hyponatremia
serious skin rxns
teratogenic
lots of drug interax
88
what is a spasm
involuntary contraction of a muscle or a muscle group
89
what is spasticity
prolonged muscle tightness or contraction
90
what are the s/sx of a spasm
pain and reduced funtion
91
what are causes of spasms
epilepsy, hypocalcemia, chronic pain syndrome, localized muscle injury
92
what are s/sx of spasticity
increased muscle tone, spasms, deacred fine motor control/dexterity,
93
what causes spasticity
multiple sclerosis, cerebral palsy, stroke, traumatic spinal cord lesions
94
What drugs treats spasms
cyclobenzaprine
95
what class is cyclobenzaprine
centrally acting muscle relaxers
96
what drugs treat spasticity?
baclofen, dantrolene, diazepam
97
what is the class of baclofen?
centrally acting muscle relaxer
98
what class is dantrolene
direct acting muscle relaxer
99
what class is diazepam
benzodiazepine
100
what are some treatments for muscle spasms
medications : acetaminophen, ibuprofen, cyclobenzaprine
physical therapy: stretching, flexibility exercises, TENS
local hear: heating pad, whirlpool, or warm baths
101
therapeutic uses of cyclobenzaprine?
relief of pain from acute muscle spasm, to increase ROM
not effective to treat spasticity
102
status epilepticus
extended period of continuous seizure
medical emergency
goal is to intervene in the first 5 minutes
103
treatment of status epilepticus?
secure airway, give IV benzodiazepine, followed by antiepileptics
104
adverse effects of cyclobenzaprine?
CNS effects (drowsiness, dizziness, sedation)
Anticholinergic effects (dry mouth, blurry vision, urinary retention, constipation - can't pee cant see cant spit cant poop-
105
cyclobenzaprine interacts with?
alcohol and other CNS depressants (increased drowsiness)
antidepressants (risk for serotonin syndromes)
- tolerance and dependence can develop
106
Baclofen acts within?
within the spinal cords to suppress hyperactive reflexes
107
main adverse side effect of baclofen and diazepam (valium)
sedation
108
Dantrolene acts directly on?
skeletal muscle
109
Dantrole PO dosing used for?
spasticity
110
Dantrolene IV dosing used for?
malignant hyperthermia
