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parkinson's Flashcards

1
Q

benztropine MoA

A

anticholinergic –> dec ACh activity –> rebalance ACh with lower DA levels –> dec s/s due to DA deficiency

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2
Q

benztropine CI

A

BEERS –> CI elderly bc anticoholinergic

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3
Q

trihexyphenidyl MoA

A

anticholinergic –> dec ACh –> rebalance with dec DA

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4
Q

trihexyphenidyl CI

A

BEERS –> CI elderly bc anticholinergic

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5
Q

anticholinergic MoA

A

antimuscarinic

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6
Q

anticholingeric AEs

A

*link to cognitive impairment/decline (inc dementia risk — recall from last unit!!)

  • blind as a bat (mydriasis)
  • dry as a bone (mouth, skin, urinary retention, constipation)
  • hot as a hare (fever)
  • mad as a hatter (depressed, agitated)
  • red as a beet (flushed skin)

opposite of SLUDGE cholinergic effects
S: sialorrhea
L: lacrimatin
U: urination
D: defecation
G: GI emesis, diarrea
E: emesis

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7
Q

anticholinergic place in therapy

A

monotherapy or combo therapy

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8
Q

levodopa MoA

A

synthetic precursor to DA
**CROSSES BBB –> DA does NOT!! –> hence why we cannot just give dopamine

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9
Q

levodopa place in therapy

A

gold standard!!

usually combo therapy with dopa decarboxylase inhibitor, can be monotherapy if IN

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10
Q

levodopa PKPD

A
  • transported by large amino acid transporter in GI and BBB –> THEREFORE will dec absorption if take with high protein meal
  • metabolized by LAAD into DA
  • very little reaches CNS without a decarboxylase inhibiot (carbidopa)
  • renal elim

**HAVE TO GIVE WITH CARBIPODA in order to inc the concentrations of levodopa to reach CNS!!

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11
Q

levodopa and food

A

take on empty stomach or do not change how have been taking it
–> taking with high protein meal –> dec absorption bc competiting for the large amino acid transporters in GI and BBB

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12
Q

levodopa CI

A
  • breast feeding
  • closed angle glaucoma
  • melanoma (in Canada)
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13
Q

levodopa AE

A

**dose-dependent!!

  • dyskinesia (twisting/squirming)
  • “on-off” phenomena, dec effectiveness overtime
  • psychiatric disturbances, vivid dreams
  • GI (N)
  • orthostatic hypotension
  • saliva, sweat, urine discoloration (orange)
  • **NMS (neuroleptic malignant syndrome) with abrupt D/C –> fever, AMS, muscle rigidity, autonomic dysfunction
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14
Q

levodopa DDI

A
  • dopamine antgonists (metoclopramide, antipsychotics)
  • NON-SELECTIVE MAO-Is
  • high protein meal
  • iron salts –> separate admin by 2 hours
  • pyridoxine (B6) –> inhibit efficacy
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15
Q

levodopa dose

A

200-300 mg/day –> 100mg BID or TID, inc by no more than 100mg per week –> no max dose

almost always give with dopa-decarboxylase inhibitor

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16
Q

carbidopa MoA

A

noncompetitive dopa decarboxylase inhibitor

L-dopa –dopa decarboxylase–> inactive peripheral L dopa

therefore –> inhibit breakdown of peripheral L-dopa –> inc DA levels in peripheray –> OHHH hency why bradykinesia and tremor start peripherally

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17
Q

carbidopa effects

A

increase absorption of levodopa AND half life of levodopa!! –> gives it enough time to go into CNS and become DA

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18
Q

carbidopa place in therapy

A

NO PHARMACOLOGIC EFFECTS ON OWN —> ALWAYS COMBO THERAPY!!

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19
Q

carbidopa PKPD

A
  • not cross BBB
  • renal elim
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20
Q

carbidopa CI

A
  • pregnancy
  • lactation
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21
Q

Sinemet

A

carbidopa/levodopa

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22
Q

Sinemet dosing

A

NEED to keep carbidopa dose at 70-100 mg/day minimum
- allows for saturation of enzyme to prevent breakdown
- prevents levodopa AE of N/V

EXCEPTIONS:
low doses can be tolerated –> Sinemet 25/100mg BID

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23
Q

Sinemet CR benefits

A
  • dec total off time
  • dec dosing frequency
  • if take at bedtime, can dec morning rigidity
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24
Q

Sinemet CR cons

A
  • decreased bioavalibilty vs IR (25% of IR)
  • delayed onset of effect when taken in morning (peak at 2 hours instead of 30 min)
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25
how to overcome Sinemet CR delayed onset
- supplemental IR Sinemet in morning - set alarm 30-60min early, take dose, go back to bed
26
how to change from IR to CR
recall: CR 25%F vs IR, therefore CR uses higher doses - start 50% reduction in FREQUENCY!! (ex: QID --> BID) - 25% increase in dose per day
27
Duopa
carbidopa/levodopa intestinal gel
28
Duopa administration
- PEG-J tube (into jejunum) through wearable pump **bypasses variable GI absorption of the oral formulations (high protein meal, dec F, ...)
29
Duopa use
usually for advanced parkinsons (significant off time, or significant dyskinesia) --> achieves more consistent L-dopa levels
30
Duopa dose
1 cassette (2000mg) per day, administered over 16 hours
31
how to dose convert to Duopa
CR --> IR --> Duopa ** clinicla trials only figured out dose conversion from IR**
32
Duopa AEs
- normal carbidopa/levodopa AEs (N/V, dyskinesia, NMS, vivid dreams, ...) - PEG-J: infection, bleeding, tube clog/dislodge - tube needs cleaning and care
33
Inbrija
levodopa powder --> ORAL inhalation!!
34
Inbrija indication
intermittent treatment for off episodes, also treated with carb/levo **advanced parkinson's **NOT replacement for PO carb/levo
35
Inbrija dosing
prn for off symptoms up to 5 times a day
36
Inbrija AE
- somnolence - hallucinations - dyskinesia - cough - nausea - URI - sputum discoloration
37
Inbrija CI
non-selective MAOi use within 2 weeks
38
Inbrija not recommended in
- asthma - COPD - chronic underlying lung disease
39
COMT inhibitors
- tolcapone - entacapone - opicapone
40
COMT inhibitor MoA
- reversible, selective inhibition of COMT --> therefore inhibit L-dopa breakdown --> therefore inc L-dopa levels --> inc DA
41
COMT inhibitior place in therapy
NEED L-DOPA --> MUST be in combination with levodopa
42
COMTi DDIs
- drugs metabolized by COMT (APOMORPHINE, bitolterol, dobutamine, dopamine, epinephrine, isoetharine, isoproterenol, methyldopa, norepinephrine) - non-selctive MAOis
43
entacapone MoA
- COMTi --> prevent L-dopa breakdown --> inc L-dopa
44
entacapone PKPD
- acts in periphery - shorter half life than other COMTis
45
entacapone dose
200mg WITH EACH DOSE of carb/levo --> MDD: 8 times/day
46
entacapone AEs
- similar to levodopa (bc inc leovodopa) - brown/orange urine
47
Stalevo
carbidopa/levodopa/entacapone --> always 200mg entacapone in these doses
48
tolcapone MoA
- COMTi --> therefore inhibit L-dopa breakdown --> inc L-dopa
49
tolcapone PKDP
- central and peripheral activity - food dec bioavliability!!
50
tolcapone CI
- hepatic disease --> tolcapone-induced hepatocellular injury!!!)
51
tolcapone AE
- **hepatocellular injury - delayed onset diarrhea - similar to levodopa
52
tolcapone monitoring
LFTs --> watch for inc, must sign consent
53
tolcapone place in therapy
rarely used anymore - older - hepatocellular injury
54
tolcapone dose
100mg TID
55
opicapone MoA
COMTi
56
opicapone PKDP
- DEC ABSORPTION WITH moderate fat/calorie meal --> dec AUC and Cmax (NOT high protein meal, be careful!!)
57
opicapone dosing
ONCE DAILY - 50mg QHS (bedtime) - do not eat one hour before/after
58
opicapone CI
- nonselective MAOI use - catecholamine secreting neoplasm (pheochromocytoma, paraganglioma) - severe hepatic impairment
59
opicapone caution
- mild-mod hepatic impairment
60
opicapone AE
- similar to levodopa - similar to COMTis
61
central and peripheral MAO-B inhibitors
- selegiline - rasagiline - safinamide
62
MAO-B inhibitior MoA
- noncompetitive, selective antagonist of monoamine oxidase type B --> dec breakdown of dopamine (only DA, not others like NE) (selective therefore no tyramine considerations) - decrease free radical production --> delays need for L-dopa by 9 months - inc peak of L-dopa --> dec L-dopa doses by 50% - symptoms control
63
MAO-Bi place in therapy
- monotherapy or adjunctive therapy
64
which MAO-B is potentially disease-modifying?
rasagiline
65
selegiline MoA
MOA-B inhibitor --> prevents dopamine breakdown --> increase endogenous DA
66
selegiline types
- Eldepryl --> po - Zelapar --> transbuccal
67
selegiline indication
labeled: adjunctive ONLY studies: can be mono
68
selegiline PKPD
- high F - *crosses BBB - ***ACTIVE METABOLITES --> methyldeprenyl, amphetmaine, methamphetamine --> linger for weeks, can show (+) amphetamine tox - slow elimination
69
selegiline dosing
Eldepryl (po) --> 5mg qd-bid Zelapar (dissolving tab) --> 1.25mg qd up to 2.5mg qd, **no food/drink 5 minutes before/after
70
selegiline CI (not absolute)
- dementia, severe psychosis - concomitant use of meperidine, tramadol, methadone, propocyphene --> bc amphetamine-like metabolities
71
selegiline AEs
**dopagenergic (makes sense bc dec DA breakdown --> therefore inc DA) - CNS, GI - HTN crisis - serotonin syndrome - *insomnia, jittery, HA Zelapar (ODT) - irritation of buccal mucosa
72
selegiline DDIs
- MAOI (nonspecific) - TCA, SSRI, SNRI, DXM --> serotonin syndrome - tyramine containing foods when doses >10mg (oh??) - sympathomimetics
73
which is preferred between selegiline and rasagiline ?
rasagiline - no amphet like active metabolites - potentially disease modifying
74
rasagiline place in therapy
monotherpay combo therapy
75
rasagiline dose
with levodopa: 0.5mg qd monotherapy: 1mg qd
76
rasagiline AEs
monotherapy - HA - arthralgia - GI - falls with levo: - dyskineia - GI upset - HA - weight loss - arthralgia - orthostasis --> most common during first two months of treatment
77
rasagiline DDIs
- ciprofloaxacin (metabolized by 1A2) - MAOIs non-specific (2 week washout) - TCA, fluoxetine (5 week washout) - tryamine containing foods - sympathomimetics
78
rasagiline CIs
- meperidine, tramadol, methadone, propxyphene, DXM - St. John's wort - mirtazapine - cyclobenzaprine (serotonin syndrome) - vasoconstrictors (HTN crisis)
79
safinamide MoA
MOA-B inhibitor --> dec dopamine breakdown --> inc DA - Na and K channel blocker, dec glutamate --> all inc inhibition (good bc low inhibition from DA)
80
safinamide indication
- adjunctive to levodopa, for off s/s
81
safinamide dosing
50mg po qd -- > 100mg qd
82
safinamide PKPD
- renal elim - *hepatic metabolism
83
safinamide dose reduction
**Hepatic impairment --> 50mg qd max dose!
84
safinamaide CI
- cirrhosis (child-pugh C)
85
safinamide DDI
- sertonergic drugs (opioids, SSRI, SNRI, TCA, amphet, St John's wort) - sympathomimetics (HTN) - DXM (bizarre behavior) - substrates of BCRP
86
safinamide AE
- dyskinesia - hallucination - psychosis - behavior change - nausea - daytime somnolence - retinal ptahology - **NMS if abrupt withdrawal!!!
87
amantadine options
Symmetrel (IR) Gocovri (ER) Osmolex (ER)
88
amantadine MoA
inc DA release (from storage sites), dec DA reuptake, inhibit NMDA (excitatory) receptors *poorly understood
89
amantadine indication
**levodopa-induced dyskinesia!!! --> add on to levo - dec rigidity, tremor, bradykinesia, dyskinesia
90
amantadine PKPD
- good F - renal elim --> DOSE ADJUST RENAL IMPAIRMENT!!
91
amantadine dosing
Symmetrel (IR): 300mg/day divided doses Gocovri (ER): 137mg qd --> 274mg qd Osmolex (ER): 129mg qd --> 322mg qd
92
amantadine CI
- CHF - orthostatic hypotension - peripheral edema **bc inc fluid retention
93
amantadine AE
- orthostatic hypotension/dizzy/**fall - hallucination - sedation - anticholinergic (hence fluid retention) - **livedo reticularis --> reversible mottling of skin with lower extremity edema - NMS with abrupt d/c
94
amantadine DDI
- Flumist (LAIV) --> dec vaccine efficacy - quinine/quinidine, HCTZ, triamterene
95
which drug is for intermittent off symptoms
Inbrija (levodopa orl inhalation)
96
which drug is for for levodopa induced dyskinesia
amantadine
97
which drugs are monotherpay
- Sinemet - Sinemet CR - Duopa - Stalevo - rasagiline **all others need treatment with levodopa too!!!
98
dopamine agonists
byspass endogenous DA system --> activate post-synaptic receptors
99
dopamine agonists
D2: apomorphine D2 and D3: pramipexole, ropinirole D2, D3, D1: rotigotine
100
dopamine agonist use
*monotherapy --> in younger, healthier patients - reduce risk of developing motor complications (wearing off effects) vs levodopa when used an monotherapy!!! *combination therapy --> deterioation in response to levodopa - when levodopa has fluctuations in response, or unable to tolerate inc doses of levodopa --> dec off time, dec dyskinesia
101
dopamine agonist vs levodopa
**more frequent non-motor side effects vs levo --> especially in older/frail patients - impulsive behaviors, psychosis - N/V, vivid dreams, daytime sedation, orthostatic hypotension
102
apomorphine MoA
stimulates postsynaptic D2 receptors
103
apormorphine indication
advanced PD prn for off episodes
104
apomorphine dose
TEST DOSE: 2mg SQ, under medical supervision - MONITOR BP beofre, 20min, 40min, 60min prn for off periods, MDD: 6mg, TID dosing *rotate injection sites
105
apomorphine PKPD
**rapid onset of action --> hence why for breakthrough
106
apomorphone pre-treatment
**antiemetic - 3 days before, then continue for 2 months, then reassess - NOT dopamine antagonist or antidopaminergic ( metocloproamide, prochlorpazine)
107
apomorphine AE
- N/v - dizzy - somnolence - chest pain/pressure - dyskinesia - falls - yawning - rhinorrhea
108
apomorphine DDI
- dopamine antigonists --> inc hypotensive effects - QT prolongation drugs (additive effects) - DA antiaognists (antiphyschotics)
109
pramipexole MoA
D2 and D3 dopamine agonist
110
pramipexole PKPD
- renal elimination --> DOSE REDUCE if CrCl < 60!!
111
pramipexole dose
IR: tid ERL qd
112
pramipexole DDI
- cimetidine -- inhibitor of renal tubular secretion
113
ropinirole MoA
D2 and D3 dopamine agonist
114
ropinirole PKPD
metabolized by 1A2
115
ropinirole dose
IR: tid XL: qd
116
ropinirole CI
- abrupt discontinuation (all of this drug class) - hepatic disease
117
ropinirole DDI
**CYP 1A2 inhibitors --> inc concentration - cimetidine, cipro, clarithro, diltiazem, erythro, fluvoxamine, omeprazole, ritoniavir **CYP 1A2 inducers --> dec concentration - carbamazepine, phenobarb, phenytoin, rifampin, ciagrette*** smoking will dec drug effect!!
118
rotigotine MoA
D1, D2, D3 agonist --> primarily D2
119
rotigotine dose
**transdermal patch!! start 2mg/24 hours --> 4mg minimum effective dose --> 6mg MDD
120
rotigotine precaution
- heat, MRI --> skin burns - sulfite sensitivity --> anaphylaxis
121
rotigotine AE
- CNS - GI - peripheral edema -**application site reaction
122
rotigotine DDI
- dopamine antagonists --> antipsychotics, metoclopramide
123
adensoine A2A receptor funciton
GPCR abundant in basal ganglia --> caffeine is a competitive antagoinst --> functions to regulate glutamate (excitatory) and dopamine (inhibitory) release
124
adenosine A2A receptor function in parkinsons
overactivation of A2A receptor pathway --> inhibition of motor function therefore, we want to inhibit A2A receptor function!
125
istradefylline MoA
adenosine A2A receptor antagonist --> dec overactivation of A2A --> prevent inhibition of motor function (bradykinesia)
126
istradefylline indication
combo therapy, for off episodes --> reduces off time, effective after 4 weeks
127
istradefylline dose
20mg po every morning! max 40mg
128
what to dose adjust istradefylline for
- concamitant smoking --> inc dose - mod hepatic impairment --> dec dose
129
istradefylline AE
- **dyskinesia - insomnia - hallucinations - dizzy
130
istradefylline metabolism
3A4 and 1A1
131
istradefylline DDI
with strong 3A4 inhibitors (inc conc) --> MDD 20mg avoid use with strong 3A4 inducers (dec conc)
132
best non-pharm option
exercise!!
133
how to treat PD psychosis
1. exclude infection, electrolyte imbalance, hypoxemia 2. D/C and dec doses of meds --> anticholinergics, amantadine, selegiline 3. treat with atypical antipsychoitics
134
PD atypical antipsychotics
- quetipine - clozapine - pimavanserin (Nuplazid)
135
quetipine and clozpine MoA
block both serotonin and DA --> blocking DA counteractive to PD treatment, therefore good that also block serotonin
136
pimavanserin MoA
5HT2A/2C inverse gonist --> blocks serotonin --> does NOT block DA --> good bc not counteracting PD meds!!! increases slow-wave sleep
137
pimavanserin indication
**specifically parkinsons --> hallucinations and delusions
138
pimavanserin BBW
inc death in eldery patients with demetia who are treated with antipsychotic drugs
139
pimavanserin AE
- QT prolongation - peripheral edema - nausea - confusion
140

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