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Drugs for Parkinson?

Benztropine
Levodopa/Carbidopa

1

What worsens Parkinsons?

meds (antinauseua)
increasing Ach, decreasing Dopamine

2

What is the goal of Parkinson pts?

Increasing Dopamine
Decreasing Ach

3

Parkinson-What is the last resort drug?

Levodopa/Carbidopa
issue b/c if used early on, there is no tx for long term

4

Parkinson - BBB issue?

Dopamine itself does NOT pass the BBB - drugs must pass the BBB and THEN convert to dopamine

5

What drugs for rigidity and akinesia?

Amontadine

6

What drug helps w/ tremors?

Anticholingeric (Benztropine)

7

What does GABA do?

slows neurological movement down

8

Parkinson - What happens to GABA?

There is no dopamine so there is a GREAT increase of Ach --> hypokinesia

9

What is Benztropine doing to GABA?

blocks Ach so it can decrease Ach --> improve movement (tremor and drooling)

10

Is Benztropine better or Levodopa?

Benztropine is not as effective as Levodopa BUT "start low and slow" (Levodopa is NOT first line)

11

Benztropine MOA?

mostly anticholinergic (dec Ach) but may also incr dopamine
helps w/ tremors NOT rigdity and akinesia

12

Benztropine ADR?

DO NOT USE IN ELDERLY (cognitive probs - over 70yo) - use Levodopa instead
orthostasis
delirium
constipation
"mad as a hatter"
"blind as a bat"
"dry as bone"
"red as a beet"

13

Benztropine - how to dec ADRs?

titration is needed "start low and slow"

14

Benztropine - who do you avoid?

Alzheimer's
Dementia
Cognitive issues
Elderly

15

Benztropine - DI?

ADR duplication
anything w/ anticholinergic effect (benadryl)

16

Amantdaine?

-antiviral
-helps promote Dopamine from the synapse and inhibits reuptake
-increasing Dopamine and decreasing Dopamine that is reabsorbed
-neuroprotective benefits
-helps w/ Parkinson sx
-can be used w/ Levodopa (helps w/the fluctuation of the half life)

17

Amantadine ADR?

-pts can build a tolerance --> drug holiday (bursts of the drug)
-MUST taper off (esp during the drug holiday)- do not stop abruptly

18

What is the point of using Benztropine and Amantadine?

to delay the use of Levodopa

19

Monoamine Oxidase inhibitors?

-parkinson
-can increase dopamine levels
-prevent free radicals

20

MAO - B inhibitors ADR?

CNS irritation (sleepiness, depression)
N&V&D
Constipation
syncope

21

Apomorphine, Bromocriptine, cabergoline?

-bind to dopamine receptors
-dopamine agonist
-metabolized differently
-can be used alone or supplemental (use less Levodopa if used together)
-young pts
-helps w/ fluctuations of levodopa

22

Dopamine agonist -ADR?

CNS issues (hallucination, confusion, fainting, syncope)
constipation, diarrhea
peripheral edema (thiazide)
drink w/ water
RLS if removed abruptly

23

Levodopa/Carbidopa?

prodrug (not active until metabolized)
metabolized in GI
given w/ carbidopa

24

How does Levodopa and Carbidopa work together?

Levodopa - 1-3% to the brain
+ Carbidopa - 10% to the brain

25

Levodopa/Carbidopa population?

cognitive impairment
elderly
motor skills are impaired
intitaion of therapy is individualized

26

Levodopa ADR?

GI issues (N&V) - can take w/ food but efficacy goes down
postural hypotension
irreversible dyskinesias
behavioral effects (depression, anxiety)
resistance of the drug

27

Levodopa half life?

90 min
wearing off (efficacy goes away) --> "on and off" motor fluctuations
can give together w/ MAO B inhibitor

28

Levodopa timeline?

honey moon (no sx) - 3 yrs
wearing off - 3-5 yrs
on - off dyskinesia -5-10yrs
*drug holidays does not help-DO NOT DO

29

Levodopa DI?

dopamine agonist can worsen ADR
ADR duplication
MAO I used for depression

30

COMT inhibitors?

increases dopamine in the brain
increases Levodopa to the brain
prevents breakdown of dopamine in the brain
helps fluctuations of Levodopa

31

COMT inhibitors - labs?

watch liver enzymes

32

Tension headache - sx?

upper back and neck
base of head
ears, above ears
jaw
above the eyes

33

What to keep in mind when tx HA and drugs?

episodic HA can turn into chronic headache - d/t meds (rebound)

34

HA -cx?

DRUGS!
can be drug withdrawal headache

35

Acetaminophen ADR?

alcohol
hypersensitivity

36

Migraine tx?

earlier the better
OTC: excedrin extra strength - first line
triptan (sumatriptan, rizatriptan) - "second line" but first line w/ migraine is severe

37

Sumatriptan ADR?

N&V

38

Triptan MOA?

abortive NOT prophylactic
faster the better
selective 5HT 1D and 2B agonist --> interrupts the pain signal through the trigeminal nerve)

39

Sumatriptan MOA?

first triptan, cheapest
not as effective as Rizatriptan

40

Rizatriptan MOA?

more lipophilic than sumatriptan, more effective

41

Sumatriptan and Rizatriptan ADR?

bad taste
GI upset
dizziness
vasoconstrictor: coronary artery spasm, MI, CVA
seizure
blindness
hypersensitivity

42

Sumatriptan and Rizatriptan DI?

ADR duplication

43

Triptan forms?

oral (cheapest)
skip the GI absorption, etc --> sublingual, nasal

44

Ergot alkaloids?

abortive
vasoconstricts - decreased blood flow to extremities and decreases pulsatile headache
like triptan but not as effective
faster, better
add caffeine to increase efficacy

45

Ergot Alkaloids ADR?

rebound HA
toxicity (Nausea, diarrhea, constipation, etc)
do not use in pregnancy

46

Ergo alkaloid forms?


oral

47

Migraine prophylactic management criteria?

migraine is so bad that it disrupts daily activities
more than 2x/mo

48

Migraine prophylactic goal?

GOAL:
reduce 15%

49

Migraine prophylactic management - is it working?

1 mo

50

Migraine prophylactic drugs?

Propranolol
Nortiptyline
SSRI (venlafaxine)
Gabapentin (anticonvulsants)

51

Cluster HA - tx?

abortive - triptans, erogtamines
100% if avail
NO narcotics

52

Prophylactic cluster HA drugs?

Topiramate

53

Prevention of recurrent stroke?

Tx RF: HTN, diabetes, lipids
antiplatelet therapy (ASA)
lifestyle modification
statins

54

Ischemic stroke - tx?

tPA - if able to use

55

TIA - tx?

do not jump to tPA - unless you can prove to be a stroke
ASA! - long term
statin

56

Common cx of bacterial meningitis?

ALL PREVENTABLE
1) Neisseria Meningitidis (places w/ mold and high humidity) - multiply in nasal mucous
2)
3)

57

Population of the bacterial meningitis?

immunosuppressed
young
old

58

Polio - sx?

variable (some people are asymptomatic)
aseptic menigitis
paralytic
CONTAGIOUS

59

Meningococcal vaccination?

two doses are reommended

60

Polio vaccination?

now is inactive vaccine (live vaccine is out)
total of 4 doses

61

Neuropathic pain - cx?

inflammation of infxn
surgery
trauma
genetically

62

Neurological pain?

not like regular pain
can cause damage to nerves

63

Neurological pain - tx?

mitigate the pain, not completely tx (tolerable pain)
start low and slow
ibuprofen, acetaminophen, et do not work
TCAs, SNRIs, topical lidocaine, opioids, NA ch blockers, anticonvulsants - Gabapentin* and Pregabalin*

64

Gabapentin?

neuropathic pain - esp postherpetic neuralgia and polyneuropathies
relieve atypical pain
insomnia (can help w/ comorbidities)

65

Gabapentin and Pregabalin ADR?

peripheral edema
sedating
well tolerated
hypersensitivity rxn

66

Pregabalin?

used for diabetics
fibromyalgia
insomnia and anxiety (helps w/ comorbidities)

67

tPA is good until?

4.5 hrs

68

neuropathetic pain -tx?

NOT NSAID, acetaminophen
YES anticulvansts

69

Low Ach levels?

cognitive impairment

70

Parkinson AND dementia?

parkinson - give anticholinergic (brings down Ach)
BUT dementia too? (you want to increase Ach)
teeter totter - balance!

71

Antiepileptic drugs used for?

prevent epilepsy (unprovoked)

72

1st seizure? Then 2nd one will occur..?

within the next 2 yrs

73

Goal of epilepsy?

tx underlying trigger and avoid

74

Keppra?

well tolerated
well used in peds

75

Most effective anticonvulsants?

Valproic acid but not well tolerated

76

Well tolerated anticonvulsants?

Lamatrigine but not as effective as valproic acid

77

What to keep in mind for pts taking anticonvulsants?

depresses CNS so suicide rate goes up

78

Acute seizure-tx?

diazepam and lorazepam

79

How does anticonvulsant work?

enhancing GABA abilities
opens up Cl channels --> slows down the signaling (inhibitory) --> enhances GABA effects

80

Drug classification foor Diazepam and Lorazepam?

benzodiazepine

81

Does benzodiazepine increase GABA?

no, just enhances the effectiveness of GABA

82

How does benzodiazepine work?

dose based
anxiety - small dose
sedation - little more
loss of consciousness/hypnosis - heavy dose

83

Benzodiazepine - ADR?

CNS depression - sedation, drowsiness
dependence: NOT GOOD FOR LONG TERM; ONLY FOR SHORT TERM
CARDIOPULM pts - respiratory/cardio depression

84

Benzodiazepine - DI?

ETOH
other CNS depressants
CYP 450 - liver

85

Carbamazepine?

anticonvulsant - first gen
inhibits repetitive firing by blocking Na channels

86

Carbamazepine - important labs to check?

check HLA in asians

87

Carbamazepine - what kind of characteristics does it have?

anticholinergic
antidiuretic
antiarrhythmic
muscle relaxant
anti depressant
sedative

88

Carbamezpine - ADR?

GI
rash/itchy
CNS disturbances
bone marrow depression

89

Carbamazepine - DI?

CYP450 and inducer (speeds up metabolism) - CHECK OTHER DRUGS
ADR duplication

90

Phenytoin-drug use?

do not stop abruptly
used for partial seizures

91

Phenytoin- labs?

serum levels - CBCs, LFTs (liver toxicity) HLA

92

Phenytoin - ADR?

GI upset
gingival hyperplasia
CNS irritability

93

Phenytoin - DI

CYP 450 and inducer

94

Valproate (Valporic acid) - drug use?

MHA
seizure
first generation anticonvulsant

95

Valproate - labs?

serum levels - LFT CBC

96

Valproate - ADR?

do not chew meds
GI upset
hepatoxcity
hyperammonemia (encephalopathy can occur)
thrombocytopenia

97

Topiramate?

anticonvulsant second generation
seizures
MHA
prophylactic for cluster HA
Na channel blocker
*glutamiate (opp of GABA - excitatory part of the brain) inhibitor
enhances GABA

98

Topiramate - ADR?

flushing
loss of appetite
epistaxis
metabolic acidosis

99

Topiramate - DI?

CYP 450 inducer

100

Lamotrigine -ADR?

RASH!
aspetic meningitis
DIC
hypersensitivity (esp if they're young and HD)

101

Lamotrigine - DI?

OCP

102

Alzheimer's Dz?

decrease in Ach

103

Alzheimer dz drugs?

acetyl cholinesterease inhibitor

104

Donezepil -drug use?

reversible acetyl cholinesterase inhibitor
dementia
dose dependent

105

Donezepil - when to take? what to monitor?

bedtime
HR and BP

106

Donezepil - ADR?

GI - diarrhea, loss of appetite
HTN --> AV block, seizures, syncope

107

Donezepil - DI?

anticholinergic
CYP450
ADR duplication

108

Memantine?

used for severe Alzheimer
Glutimate inhibitor - blocks the excitatory part of the brain
helps w/ memory fxn

109

MS tx?

methotrexate
baclofen
SSRi
gabapentin

110

MS sx?

balance and coordination
fatigue
bladder probs
bowel probs
pain
sensory
depression

111

Modafinil?

antinarcoleptic stimulant

112

Modafinil?

can be addictive

113

Modafinil -monitor?

BP

114

Modafinil -ADR/

rash
G upset
dizziness
CNS irritation
HTN