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Pharm > Drugs for Neurologic Disorders > Flashcards

Drugs for Neurologic Disorders Flashcards

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
Q

MYASTHENIA GRAVIS (MG)

A

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

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26
Q

CHOLINESTERASE INHIBITORSAChE Inhibitor

A

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

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27
Q

edrophonium
neostigmine
pyridostigmine
MOA

A

preventing destruction of ACh =>

better transmission of neuromuscular impulses

28
Q

edrophonium
neostigmine
pyridostigmine
SIDE EFFECTS

A

cholinergic effects on the peripheral autonomic nervous system
See code phrases

Fasciculation: muscle twitching
Lacrimation: tear production

29
Q

edrophonium

A

ultra short-acting for diagnosing

30
Q

neostigmine

A

crisis

Reversal of nondepolarizing paralytic agentsshort-acting
- for treatment of acute myasthenic

31
Q

pyridostigmine

A

intermediate-acting for maintenance therapy of MG

32
Q

MUSCLE SPASM

A

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
Q

Neuromuscular blockers

A

succinylcholine
vecuronium, pancuronium
cyclobenzaprine, carisoprodol

34
Q

vecuronium, pancuronium

A

Centrally acting muscle relaxants (used as antispasmodic)

35
Q
  1. PARALYTIC AGENTS

INDICATIONS

A

adjunct to general anesthesia

short procedures that require flaccidity (such as intubation)

during mechanical ventilation

during electroconvulsive therapy (ECT)

36
Q
  1. PARALYTIC AGENTS

EFFECTS

A

Do not cross BBB => no CNS effects

No unconsciousness, amnesia, analgesia

37
Q
  1. PARALYTIC AGENTS

DRUGS

A

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
Q
  1. PARALYTIC AGENTS

a. depolarizing

A

succinylcholine

39
Q

succinylcholine

MOA

A

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
Q

succinylcholine

CAUSES

A

Causes sustained depolarization of the muscle => muscle paralysis!!!

41
Q

succinylcholine

NO REVERSAL AGENT: BUT..

A

reversal agent: none

intubate/ventilate the patient until the drug is metabolized

42
Q

succinylcholine

CONTRAINDICATION

A

pregnancy,

MG

43
Q

succinylcholine

SIDE EFFECTS

A

hyperkalemia (see code phrases)

44
Q

succinylcholine

ADVERSE EFFECTS

A

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
Q
  1. PARALYTIC AGENTSb. nondepolarizing
A

vecuronium

pancuronium

46
Q

vecuronium
pancuronium
MOA

A

Competitive antagonist

binds to ACh receptors without inducing the effect of ACh

47
Q

vecuronium
pancuronium
EFFECTS

A

paralysis

48
Q

vecuronium
pancuronium
SIDE EFFECTS

A 
histamine release => 
rash, 
hives, 
angioedema, 
bronchospasm, 
low BP, 
tachycardia
49
Q

vecuronium
pancuronium
NURSING

A

Prepare antihistamine to treat the side effects

Must use reversal agent
neostigmine

50
Q

vecuronium
pancuronium
REVERSAL AGENT

A

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
Q
  1. SPASMCENTRALLY ACTING MUSCLE RELAXANTS
A

CNS sedation => depress spasticity of muscles

cyclobenzaprine
carisoprodol

52
Q

cyclobenzaprine
carisoprodol
SIDE EFFECTS

A

Sleepiness,
lightheadedness,
fatigue,
fall

Physical dependence:
Short term use,
taper the dose,
avoid stopping abruptly

53
Q

cyclobenzaprine
carisoprodol
EDUCATION

A

Educate safety,
avoid CNS stimulants/depressants,
driving

54
Q 
MULTIPLE SCLEROSIS (MS)
Pathophysiology
A

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
Q 
MULTIPLE SCLEROSIS (MS)
Characteristics
A

Early onset 20s-40s

Slow progression,
remissions and exacerbations

56
Q

MULTIPLE SCLEROSIS (MS)
CHARACTERISTICS
SENSORY

A 
diplopia, 
blurred vision, 
paresthesia, 
vertigo, 
tinnitus
57
Q

MULTIPLE SCLEROSIS (MS)
CHARACTERISTICS
MOTOR

A

weakness/spasticity/paralysis,

fall

58
Q

MULTIPLE SCLEROSIS (MS)
CHARACTERISTICS
EMOTIONAL

A

depression

59
Q

MULTIPLE SCLEROSIS (MS)
CHARACTERISTICS
CEREBELLAR

A

nystagmus,
ataxia,
dysarthria,
dysphagia

60
Q

MULTIPLE SCLEROSIS (MS)
CHARACTERISTICS
NEUROLOGIC

A

neuropathic pain

61
Q

MS DRUGS

A

Immunomodulators

reduce the frequency of flare-ups (prevent relapses)

62
Q

MS DRUGS

A

interferon beta 1a
IM/SubQ injection

interferon beta 1b
SubQ injection

63
Q

interferon beta 1a
IM/SubQ injection

interferon beta 1b
SubQ injection

SIDE-EFFECTS

A

Flu-like symptoms (body-ache, fever/chills, fatigue/malaise)
myalgia, arthralgia, muscle spasm
depression, suicidal ideation, dizziness, fatigue

64
Q

Mgmt. of MS exacerbation:

A

Corticosteroids prednisone (Deltasone)

65
Q

MS DRUGS

NOTES

A

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

Pharm (7 decks)

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