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Drugs for Neurologic Disorders Flashcards

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1
Q

PARKINSON’S DISEASE

A

Low dopamine
degeneration of dopaminergic neurons in brain

Reason is unknown

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2
Q

PARKINSON’S DISEASE

information

A

Chronic degenerative neurologic disorder of the extrapyramidal motor tract

movement disorder:
resting tremor
rigidity/freezing
bradykinesia
posture changes
shuffling gait
lack of facial expression
pill-rolling motion of fingers
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3
Q

PARKINSON’S DISEASE

TERMS

A

dopaminergic neurons:
release dopamine

Dopamine: inhibitory neurotransmitter in the CNS

ACh: excitatory neurotransmitter in the CNS

extrapyramidal motor tract: originate in the brainstem, carrying motor fibers to the spinal cord; they are responsible for the involuntary (automatic) control of all musculature, such as muscle tone, balance, posture and locomotion

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4
Q

PARKINSONISM TREATMENT

A

Pharmacologic measures
Can not halt the progression of PD

Can improve quality of life,
ability to performs ADLs (symptom mgmt.)

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5
Q

PARKINSONISM TREATMENT

A

Dopaminergic

Delivering dopamine across BBB

Dopamine agonist

Improve dopamine action

Anticholinergic centrally acting

Block cholinergic receptors in CNS

Dystonia: involuntary abnormal posture stiffness, contraction, twisting, distortions, spasms
Dyskinesia: involuntary abnormal movements

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6
Q
  1. DOPAMINERGIC
A

carbidopa-levodopa

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7
Q

carbidopa-levodopa

MOA

A

dopamine replacement

Gradual lower effectiveness after about five years of treatment

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8
Q

carbidopa-levodopa

COMBINATION REASONING

A

When levodopa is used alone, only 1% reaches the brain

99% converts to dopamine while in the PNS

hence mixed with carbidopa

carbidopa inhibits conversion of levodopa to dopamine in the periphery

more levodopa would cross the BBB and reach the brain

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9
Q

carbidopa-levodopa

DURATION

A 
Short duration (4-5 hrs; t1/2 50min) 
=> must take frequent doses

“Wearing off” or “off” episodes may happen at any time lasting minutes to hours (even at high dose)

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10
Q

DOPAMINERGIC SIDE EFFECTS AND NURSING

carbidopa-levodopa

A

Dystonia
involuntary abnormal posture stiffness, contraction, twisting, distortions, spasms

Dyskinesia
involuntary abnormal movements (head bobbing, tics, grimacing)

Akathisia motor restlessness
the compulsive urge to move constantly

Psychosis:
hallucinations, nightmares, paranoia, severe depression, suicidal ideation

avoid:
CNS depressants,
dopamine-blockers
- e.g. antipsychotics haloperidol (Haldol)

Peripheral nervous system effects:
1. Anticholinergic effects (see code phrases)

  1. Do not abruptly discontinue
  2. Warn of harmless brown discoloration of urine & sweat
  3. N/V: may activate vomiting center in the brain, warn, report
  4. Avoid pyridoxine (B6 reduces drug effects)
    - fortified cereals &
    - meat/poultry/fish/soybean (protein foods are high in B6)
  5. Monitor skin for malignant melanoma
  6. Monitor blood cell counts
  7. Leukocytopenia, thrombocytopenia
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11
Q

DOPAMINERGIC SIDE EFFECTS AND NURSING
carbidopa-levodopa

NOTES

A

Dystonia: involuntary abnormal posture stiffness, contraction, twisting, distortions, spasms
Dyskinesia: involuntary abnormal movements
tardive dyskinesia: dyskinesia
Malignant melanoma: skin cancer
Leukocytopenia: low white blood cells (WBC)
Agranulocytosis: sever leukopenia
Thrombocytopenia: low platelets
Dopamine-antagonist (GI effects) => ↑ GI motility: promethazine (Phenergan), metoclopramide (Reglan), prochlorperazine (Compazine)

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12
Q
  1. DOPAMINE AGONISTS
A

amantadine

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13
Q

amantadine

MOA

A

Also antiviral drug for influenza A

improve dopamine action

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14
Q

amantadine

TOLERANCE

A

Drug tolerance develops

only temporary improvement of symptoms

Do not discontinue abruptly

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15
Q

amantadine

SIDE EFFECTS

A

livedo reticularis
- temporary skin discoloration while on amantadine

Anticholinergic effects: (see code phrases)

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16
Q

3- ANTICHOLINERGICS

A

Centrally acting anticholinergic

benztropine

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17
Q

benztropine

MOA

A

inhibit the release of acetylcholine in CNS

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18
Q

benztropine

SIDE EFFECTS

A

may affect PNS =>
anticholinergic side effects (see code phrases)

Dystonia

  • involuntary abnormal posture
  • stiffness,
  • contraction,
  • twisting,
  • distortions,
  • spasms
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19
Q

benztropine

CONTRAINDICATION

A

history of Alzheimer or MG

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20
Q

benztropine

NOTES

A

Antihistamine: diphenhydramine (Benadryl)

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21
Q

ALZHEIMER’S DISEASE

Pathophysiology

A

Chronic,
progressive,
degenerative condition of the cholinergic neurons in the brain

low Acetylcholine

cognitive dysfunction

Incurable dementia illness

compare & contrast:
Low ACh neurotransmitter (CNS) in AD
Low ACh receptor sites (nicotinic receptors) in MG

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22
Q

ALZHEIMER’S DRUGSCHOLINESTERASE INHIBITORS (AChE-I)

A

donepezil

memantine

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23
Q

donepezil
memantine
MOA

A

Prevents the breakdown of ACh => more ACh in neuron synapses
improve cognitive function

done memory

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24
Q

donepezil
memantine
SIDE EFFECTS

A 
Dizziness, 
insomnia, 
HA, 
anorexia, 
muscle cramps
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25
MYASTHENIA GRAVIS (MG)
Acquired chronic autoimmune disorder Destruction of ACh receptor sites by - antibodies Lack of nerve impulses & muscle responses at myoneural junction Chronic fluctuating muscle weakness and fatigue (mostly voluntary muscle) compare & contrast: Low ACh neurotransmitter (CNS) in AD Low ACh receptor sites (nicotinic receptors) in MG
26
CHOLINESTERASE INHIBITORSAChE Inhibitor
edrophonium ultra short-acting for diagnosing myasthenia crisis vs. cholinergic crisis neostigmine short-acting for treatment of acute myasthenic crisis Reversal of nondepolarizing paralytic agents pyridostigmine intermediate-acting for maintenance therapy of MG
27
edrophonium neostigmine pyridostigmine MOA
preventing destruction of ACh => | better transmission of neuromuscular impulses
28
edrophonium neostigmine pyridostigmine SIDE EFFECTS
cholinergic effects on the peripheral autonomic nervous system See code phrases Fasciculation: muscle twitching Lacrimation: tear production
29
edrophonium
ultra short-acting for diagnosing
30
neostigmine
crisis Reversal of nondepolarizing paralytic agentsshort-acting - for treatment of acute myasthenic
31
pyridostigmine
intermediate-acting for maintenance therapy of MG
32
MUSCLE SPASM
localized involuntary muscle contractions (increased tone) with pain When do we need muscle paralysis without the presence of muscle spasm? (see neuromuscular blockers in anesthesia slides)
33
Neuromuscular blockers
succinylcholine vecuronium, pancuronium cyclobenzaprine, carisoprodol
34
vecuronium, pancuronium
Centrally acting muscle relaxants (used as antispasmodic)
35
1. PARALYTIC AGENTS | INDICATIONS
adjunct to general anesthesia short procedures that require flaccidity (such as intubation) during mechanical ventilation during electroconvulsive therapy (ECT)
36
1. PARALYTIC AGENTS | EFFECTS
Do not cross BBB => no CNS effects No unconsciousness, amnesia, analgesia
37
1. PARALYTIC AGENTS | DRUGS
A. depolarizing (succinylcholine) B. non-depolarizing (vecuronium) neostigmine (Prostigmin) short-acting AChE-I, used for treatment of acute myasthenic crisis & reversal for nondepolarizing neuromuscular blockers
38
1. PARALYTIC AGENTS | a. depolarizing
succinylcholine
39
succinylcholine | MOA
ACh agonist, binds to nicotinic receptor at the neuromuscular junction ACh at nicotinic receptors is an stimulant Not metabolized by AChE but metabolized by plasma pseudocholinesterase hence short acting (so with short term airway support and ventilation succinylcholine will be metabolized)
40
succinylcholine | CAUSES
Causes sustained depolarization of the muscle => muscle paralysis!!!
41
succinylcholine | NO REVERSAL AGENT: BUT..
reversal agent: none | intubate/ventilate the patient until the drug is metabolized
42
succinylcholine | CONTRAINDICATION
pregnancy, | MG
43
succinylcholine | SIDE EFFECTS
hyperkalemia (see code phrases)
44
succinylcholine | ADVERSE EFFECTS
respiratory depression, apnea (support airway and ventilation) malignant hyperthermia (muscle rigidity, high temp (109℉)) Stop the drug, dantrolene IVP & gtt, O2, cooling measures (cooling blanket, iced IVF)
45
1. PARALYTIC AGENTSb. nondepolarizing
vecuronium | pancuronium
46
vecuronium pancuronium MOA
Competitive antagonist | binds to ACh receptors without inducing the effect of ACh
47
vecuronium pancuronium EFFECTS
paralysis
48
vecuronium pancuronium SIDE EFFECTS
``` histamine release => rash, hives, angioedema, bronchospasm, low BP, tachycardia ```
49
vecuronium pancuronium NURSING
Prepare antihistamine to treat the side effects Must use reversal agent neostigmine
50
vecuronium pancuronium REVERSAL AGENT
neostigmine ``` Nondepolarizing: act as competitive antagonist (bind to receptor (competing with ACh) but not induce the effect of ACh which is to open Na+ channels (antagonist) AChE inhibitors (used for MG e.g., neostigmine (Prostigmin)) are the reversal agent for nondepolarizing blockers (pancuronium)!!! Do not get confused (-ium) is shared between these drugs and AChE-inhibitors used for MG ```
51
2. SPASMCENTRALLY ACTING MUSCLE RELAXANTS
CNS sedation => depress spasticity of muscles cyclobenzaprine carisoprodol
52
cyclobenzaprine carisoprodol SIDE EFFECTS
Sleepiness, lightheadedness, fatigue, fall Physical dependence: Short term use, taper the dose, avoid stopping abruptly
53
cyclobenzaprine carisoprodol EDUCATION
Educate safety, avoid CNS stimulants/depressants, driving
54
``` MULTIPLE SCLEROSIS (MS) Pathophysiology ```
Neuromuscular autoimmune disorder Progressive loss of myelin sheath of nerve fibers in CNS No cure (mgmt. symptoms, reduce frequency of exacerbations) No specific diagnostic test
55
``` MULTIPLE SCLEROSIS (MS) Characteristics ```
Early onset 20s-40s Slow progression, remissions and exacerbations
56
MULTIPLE SCLEROSIS (MS) CHARACTERISTICS SENSORY
``` diplopia, blurred vision, paresthesia, vertigo, tinnitus ```
57
MULTIPLE SCLEROSIS (MS) CHARACTERISTICS MOTOR
weakness/spasticity/paralysis, | fall
58
MULTIPLE SCLEROSIS (MS) CHARACTERISTICS EMOTIONAL
depression
59
MULTIPLE SCLEROSIS (MS) CHARACTERISTICS CEREBELLAR
nystagmus, ataxia, dysarthria, dysphagia
60
MULTIPLE SCLEROSIS (MS) CHARACTERISTICS NEUROLOGIC
neuropathic pain
61
MS DRUGS
Immunomodulators | reduce the frequency of flare-ups (prevent relapses)
62
MS DRUGS
interferon beta 1a IM/SubQ injection interferon beta 1b SubQ injection
63
interferon beta 1a IM/SubQ injection interferon beta 1b SubQ injection SIDE-EFFECTS
Flu-like symptoms (body-ache, fever/chills, fatigue/malaise) myalgia, arthralgia, muscle spasm depression, suicidal ideation, dizziness, fatigue
64
Mgmt. of MS exacerbation:
Corticosteroids prednisone (Deltasone)
65
MS DRUGS | NOTES
Interferon are a group of glycoproteins produced by the body to: fight viral infections and other foreign matter help control immune system activities inhibit inflammation that can cause MS flare-ups Don’t confuse with interferon alpha (discussed in cancer non-cytotoxic, Biologic Response Modifiers) CP: chest pain

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