Week 15: Neuro Meds Flashcards

1
Q

Prototype Neuro Drugs

A
  1. Vaproic Acid (Depakote, Depakene)
  2. Lamotrigine (Lamictal)
  3. Cabamazepine (Tegretol)
  4. Neostigmine (Prostigmin)
  5. Atropine
  6. Levodopa/Carbidopa (Sinemet) (Parkinsons)
  7. Donepezil (Aricept)
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2
Q

Seizure

A

disturbance in electrical activity of the brain caused by excessive discahrge of neurons

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3
Q

Epilepsy

A

disorder characterized by recurrent seizures

most say “seizure disorder” now

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4
Q

What do seizure medications do

A

they depress abnormal neuronal discharges

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5
Q

What are some considerations one needs to have when choosing an anti seizure medication

A

type of seizure (s)

age and developmental level

cost

personal habits (particularly alcohol intake)

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6
Q

What is the trend for seizure med therapy

A

monotherapy - want to treat seizures with one medicaiton if possible

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7
Q

Most anti seizure drugs do one or more of what 3 things

A
  1. Decrease rate sodium flows into cells
  2. Inhibits calcium flow into the cell
  3. Increases the effect of GABA (Neuroinhibitor)
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8
Q

Most anti seizure medications are also what

A

CNS depressants (no alcohol)

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9
Q

Anti Seizure medications do cause a risk of…

A

teratogenicity (structural abnormalities in a fetus)

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10
Q

Valproic Acid (Depakote, Depakene) Classification

A

Anticonvulsant

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11
Q

Action of valproic acid

A

increases concentration of GABA (inhibitory NT) in the brain

This suppresses neuron abnormal discharges

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12
Q

Route and Absorption of Valproic Acid

A

rapidly absorbed ORALLY - onset in 15-30 minutes

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13
Q

ADRs of Valproic Acid

A
  1. Most Common - GI RELATED - NVD (tends to ease after being on it for a bit)

Other: Drowsiness - mild and transient, HA, tremor, dizziness, weight gain

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14
Q

How should dosages of valproic acid work

A

start low and titrate slowly

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15
Q

When taking valproic acid avoid…

A

concomitant alcohol and other CNS depressants

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16
Q

Are the various formulations of valproic acid interchangeable (Oral, IV, SR)

A

NO

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17
Q

Valproic Acid is the drug of choice for what things

A

Primary Generalized Tonic Clonic Seizures

Migraine Prophylaxis

Mania of Bipolar Disorder

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18
Q

___ lowers serum levels of valproic acid and should not be taken with it

A

Aspiring

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19
Q

Black Box warning of Valproic Acid

A

Never use in children 2 years or younger - can cause fatal hepatotoxicity

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20
Q

Valproic acid should never be abruptly ___

A

stopped

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21
Q

Most anti-convulsants require a patient to have what

A

medic-alert (bracelet, etc)

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22
Q

Lamotrigine (Lamictal) Classification

A

anti convulsant

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23
Q

Action of Lamotrigine

A

exact mechanism unknown

Inhibits flow through Na ion channels and possibly Ca channels too

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24
Q

Absorption and Route of Lamotrigine

A

Readily Absorbed Orally

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25
Q

ADRs of Lamotrigine

A

Generally Well Tolerated !!!

  1. SERIOUS SKIN TOXICITY / SKIN RASHES

OtherL Drowsiness, dizziness, ataxia, somnolence, HA, diplopia, NV, insomnia

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26
Q

What drug is the preferred choice for epilepsy treatment in pregnant women and the elderly

A

lamotrigine (safe)

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27
Q

Lamotrigine must be discontinued when what occurs

A

any sign of a skin rash

this skin rash can cause fatal skin loss

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28
Q

Uses for Lamotrigine

A

many seizures - absent, partial, tonic clonic

bipolar disorder

pregnant epilepsy

elderly

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29
Q

What has fewer cognitive effects: Lamotrigine or Carbamazepine

A

Lamotrigine

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30
Q

What reduces serum levels of lamotrigine and should not be used alongside it

A

oral contraceptives

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31
Q

Avoid ___ while taking lamotrigine

A

alcohol

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32
Q

all anticonvulsants need what when stopping

A

gradual reduction not suddenly stopping

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33
Q

Carbamazepine (Tegretol) Classification

A

anti convulsant

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34
Q

Action of Carbamazepine

A

suppresses high frequency neuronal discharge in and around seizure foci

similar to phenytoin (Dilantin)

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35
Q

Carbamazepine acts similarly to

A

Phenytoin (Dilantin)

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36
Q

What kind of seizure can carbamazepine NOT be used for

A

absent seizures

37
Q

Route and Absorption of Carbemazepine

A

oral - delayed and variable absorption

38
Q

What is important to know about the distribution and half life of carbemazepine?

A

Half life is 25-65 hours but decreases over time to 12-17 hours as people continue to take it because of enzymes produced

it is distributed widely with 75-90% protein bound and peaks at 4-12 hours

39
Q

ADRs of Carbemazepine

A
  1. HEMATOLOGIC: MILD LEUKOPENIA (more worrisome than thrombo), ANEMIA, THROMBOCYTOPENIA

Other: Neurologic (visual disturbances, dizziness, vertigo, confusion, nystagmus), NVD, Abdominal pain, hyponatremia, cardiovascular problems, rash, RARE APLASTIC ANEMIA

40
Q

What lab value needs close watch when taking carbemazepine and why

A

CBC - we need to monitor and grow concerned if WBC falls below 3000

41
Q

While carbemazepine has a little cognitive effect (but more than lamotrigine) what is the concern about the effect?

A

It is still not good for those wiht suppressed cognition and since many children develop seizure disorders early in development it can effect cognitive development over time

42
Q

What does it mean that carbemazepine is an effective inducer of the microsomal system?

A

It will decrease the effectiveness of oral contraceptives and warfarin because it boosts metabolism in the liver

43
Q

Therapeutic Range of Carbemazepine

A

4-12 mcg/mL

44
Q

What inhibits carbemazepine metabolism and cannot be taken with it

A

Grapefruit juice

45
Q

Neostigmine (Prostigmin) Classification

A

Anticholinesterase (Indirect Acting)

46
Q

Action of neostigmine

A

reversibly inhibits acetylcholinesterase - blocking AcH destruction

AcH will accumulate in the synapse to increase muscle strength and duration of action

Indirectly boosts AcH levels

47
Q

Neostigmine is used in the diagnosis and treatment of what

A

Myasthenia Gravis (Muscle Fatigue Disorders) - improves grip strength

Rare - Post Op Abdominal Distension (stim PNS to rest and digest)

48
Q

Neostigmine is the opposite of ____

A

atropine

49
Q

What is the neostigmine antidote

A

atropine

50
Q

Route of Neostigmine

A

IV, SC, IM (Oral poorly absorbed)

51
Q

ADR of Neostigmine

A
  1. CHOLINERGIC CRISIS
  2. PNS OVERACTIVITY - DROP BP, SWEATING, BRONCHOCONSTRICTION, DROOLING

Other: Bradycardia, Cramps

52
Q

Atropine Classification

A

Anticholinergic (Muscarinic Antagonist)

53
Q

Action of Atropine

A

BLOCK AcH at muscular receptors (PARASYMPATHOLYTIC)

Blocks effects of vagus nerve on the heart - enhances conduction thru the AV node

Various Blocking PNS effects

54
Q

What aresome of the effects around the body atropine causes since it blocks the PNS

A

CNS - stimulate medulla/higher cerebral centers

Eye - Dilate pupil and paralyze accomodation

Resp - Inhibits secretions, dry mucous membranes, relax smooth bronchi muscles

CV - moderate to large dose accel HR

Circulation - large dose cause vasodilation of vessels in face and neck (atropine flush)

GI - inhibit salivation, gastric secretion mildly affected, decreases tone and peristalsis in stomach and intestines

Glands - inhibits sweat glands

Other Smooth Muscles: Urinary retention and hesitancy (decreases bladder tone but increase sphincter tone)

55
Q

Atropine can be used to do what things?

A
  1. Dry Secretions
  2. In Acute Cardiac Conditions (Bradycardia)
  3. Treat eye disorders
  4. Diarrhea in things like Lotomil to prevent abuse
56
Q

The main two things to know atropine does is..

A

1, DRYING SECRETIONS

  1. STOPS BRADYCARDIA (speeds HR)

(NON REST AND DIGEST)

57
Q

When is an example of when atropine may be given in reference to surgery

A

prior to surgery to dry secretions

during surgery to prevent slowing of the heart by anesthetcs

58
Q

ADRs of Atropine

A

WIDE MARGIN OF SAFETY (doesnt make the heart super fast just prevents it being Slow.

Other: Drymouth, great thirst, swallowing and talking trouble, constipation, blurred vision, photophobia, cutaneous flush (esp in children)

59
Q

Contraindications of Atropine

A
  1. Glaucoma (can increase intraocular pressure in some types)
  2. BPH (increases voiding difficulties)
60
Q

Potential big syndrome issue with too much atropine

A

ANTICHOLINERGIC OVERDOSE

61
Q

What does “Mad as a hatter, dry as a bone, red as a beet, and blind as a bat” mean?

A

It is referring to Anticholinergic Overdose from something like Atropine

There is a psychotic effect, decreased salivation, peripheral vasodilation, and mydriasis (4 things)

62
Q

Parkinsons Disease

A

a degenerative neurological disorder (movement disorder)

relative lack of dopamine and relative increase of AcH (only a drop in dopamine occurs which is the relaxing effect)

63
Q

S/S of Parkinsons Disease

A

Resting Tremor

Rigidity

Postural Instability

Slow Movements (Bradykinesia) progressing to Akinesia

Major effects on ADLS

64
Q

Cause of Parkinsons Disease

A

Loss of doapminergic neurons in the substantia nigra

65
Q

Onset of Parkinsons

A

Middle age and older (rises with age)

66
Q

How does drug therapy for parkinsons disease work

A

1 of 2 ways - but does not alter course of the disease:

  1. Directly or Indrectly activate dopamine receptors (dopamine agonist)
  2. Block AcH receptors (anticholinergic)
67
Q

Drug of choice for Parkinsons disease? the issue with this drug?

A

Levodopa

Long term effectiveness is an issue as it usually only works for about 5 years

68
Q

Levodopa (L-Dopa / Sinemet (LevodopaCarbidopa)

A

Anti Parkinson: Dopaminergic Drug

69
Q

Is levodopa Dopamine itself

A

no it doesnt cross the BB and has a small half life

It must cross into the CNS and convert to dopamine

70
Q

Action of Levodopa

A

promotes synthesis of dopamine in the striatum (a precursor of dopamine is what it is)

Crosses the BBB with help and converts to dopamine

71
Q

Where is levodopa absorbed

A

the small intestine

72
Q

What is important to know about levodopa distribution

A

less than 2% reaches the brain

73
Q

How does the metabolism of levodopa work

A

the 2% that reaches the brain converts to dopamine by Dopa Decarboxylase

The other 98% metabolise elsewhere

74
Q

ADRs of Levodopa

A
  1. NV
  2. DYSKINESIAS (Involuntary muscle movements: Facial grimace, tic, head nodding, tongue protrusion)
  3. LIGHTHEADEDNESS DUE TO ORTHOSTATIC HYPOTENSION (fall can be worse than it already is)

Other: Anorexia, Cardiac Dysrhythmia (Dopamine stim heart), Mental changes (hallucination, delusion, mood changes)

MAY DARKNE SWEAT OR URINE

MANY DRUG INTERACTIONS

75
Q

What is important to know about levodopa dosage

A

levels increase slowly

it is given multiple times throughout the day

76
Q

What is Parkinsonism

A

Not Parkinsons Disease

its an iatrogenic disease from long term anti psychotic meds - it looks like parkinsons and is tx the same but they are different

77
Q

What must be avoided with Levodopa

A

Vitamin B6 therapy

MAOIs

High Protein Intake

78
Q

Why can you not ahve high protein intake with levodopa

A

because the amino acids will compete with the drug for absorption

79
Q

On-Off Phenomenon

A

People taking levodopa wiht parkinsons disease will freeze up when it wears off

80
Q

Why can we not give levodopa with Vitamin B6 therapy

A

Vitamin B6 is a precursor to the enzyme Dopa Decarboxylase which turns L dopa into Dopamine

If we give Vitamin B6 then there will be more Dopa Decarboxylase out in the periphery converting it to dopamine before it can cross the BBB into the brain

This is why it should be avoided despite the fact it would seem to help otherwise

81
Q

Why is Sinemet (Carbidopa/Levodopa) almost always the version of Levodopa given to patients

A

The carbidopa will inhibit dopa decarboxylase in the periphery allowing for more levodopa to enter the brain and convert to dopamine

basically MORE WILL REACH THE CNS

82
Q

Donepezil (Aricept) Classification

A

Acetylcholinesterase Inhibitor

83
Q

What drug is also in the same class as Donepezil

A

neostigmine - but the difference is their use and effect

84
Q

Action of Donepezil

A

inhibits acetylcholinesterase int eh CNS - increases level of AcH

Improved transmission by the neurons can cause modest cognitive improvement in Alzheimers Disease

85
Q

What is important to know about the absorption of Donepezil

A

FOOD DECREASES ABSORPTION AND CAUSE NV

You can take it at bedtime but this can cause insomnia and fatigue simultaneously

86
Q

What leads to the NV from levodopa

A

dopamine stimulating the CTZ

87
Q

ADRs of Donepezil

A

NVD

HA

Insomnia

Dream Disturbances

Fatigue

88
Q

Is donepezil a cure for Alzheimer’s?

A

No - there is no cure

89
Q

What are some reasons why anticholinesterase drugs like donepezil only give modest reuslts to Alzheimer’s?

A
  1. They are best used early in the condition but the disease begins long before symptoms appear so often its very late
  2. The tech and meds are not there yet to cure or reverse the disease