Alzheimers, PD Flashcards
class: Levodopa (Dopar®)
Levodopa/carbidopa (Sinemet®)
Levodopa/carbidopa intestinal gel (Duodopa®)
Dopamine precursors
class: Apomorphine (Apokyn®)
Bromocriptine (Parlodel®)
Pramipexole (Mirapex®)
Ropinirole (Requip®)
Rotigotine (Neupro®)
dopamine agonists
class: Benztropine (Cogentin®)
Trihexyphenidyl (Artane®)
Anticholinergic agents (muscarinic receptor antagonists)
class: Selegiline (Eldepryl®)
Rasagiline (Azilect®)
Safinamide (Xadago®)
Monoamine oxidase B inhibitor
class: Tolcapone (Tasmar®)
Entacapone (Comtan®)
Catechol O-methyl transferase (COMT) inhibitor
levodopa response diminished in ___ years
3-5
pt counseling for levodopa
take on empty stomach
carbidopa function
Carbidopa inhibits peripheral dopa decarboxylase
§ Allows more levodopa to enter CNS
§ Carbidopa does not cross BBB, blocks dopa decarboxylase from converting levodopa to
dopamine in the plasma, allowing more levodopa to cross BBB
AEs:
GI: n/v, anorexia, acid production
Cardiovascular – orthostatic hypotension, tachycardia, arrhythmias à increased peripheral
catecholamines
§ Behavioral – agitation, confusion, depression, anxiety, delusion, hallucinations, compulsive
behavior
§ Dyskinesia – choreoathetosis (superimposed on normal involuntary movements of PD)
§ Response fluctuations – “on vs off” phenomenon, end of dose akinesia
Levodopa/carbidopa
Levodopa/carbidopa interactions
MAO-A inhibitors w/in 2 wks, vitamin B6
Levodopa/carbidopa cautions
Psychotic pts
§ CVD/arrhythmia hx
§ Glaucoma
§ Melanoma
§ PUD
Ergot derivative Dopamine Receptor Agonist
Bromocriptine
MOA: D2 receptor agonists
opamine Receptor Agonists
AEs: hypotension, nausea (pre-treat w/ anti-emetic), dyskinesia, somnolence
Apomorphine (Apokyn)
anti emetic for use w/ apomorphine
Trimethobenzamide 300mg PO/IM TID
o Start 3 days before initiating apomorphine, continue 2 months then reassess need
med interactions: apomorphine
AVOID ondansetron à hypotension and LOC
• AVOID dopamine antagonists (promethazine and metoclopramide) à dec effectiveness
AEs:
o GI: N/V, loss of appetite, anorexia
o CV: orthostatic hypotension
o Dyskinesia – similar to levodopa, reduce total dose of dopaminergic drugs
o Behavioral – confusion, hallucinations, somnolence, impulse control disorders
§ Previous tendency or new phenomena
§ Gambling, shopping, etc
dopamine Receptor Agonists
dopamine Receptor Agonists cautions
Cardiac dz, psychosis hx, CNS depressant use
Monoamine Oxidase B Inhibitors for PD: low or high dose?
low
AEs:
o Insomnia à administer early in the day, less likely w/ rasagiline
o Dizziness, orthostatic hypotension
o GI distress
o Dyskinesia
o At therapeutic doses, less likely to cause HTN crisis or serotonin syndrome
Monoamine Oxidase B Inhibitors
MOA: lowers peripheral metabolism of dopamine/levodopa
o Preserves levodopa à decreases clearance, more enters CNS à prolonged effect, less dosage used
o Reduces response fluctuations à increase “on” time, decrease “off” time
Catechol-O-Methyl Transferase Inhibitor
AEs: typically attributed to increase in levodopa exposure
o GI – N/V/D
o CV – orthostatic hypotension
o Compulsive behaviors possible
Catechol-O-Methyl Transferase Inhibitor
Catechol-O-Methyl Transferase Inhibitor cautions
Psychosis, hx of melanoma, CNS depressant use
main effect of anticholinergic agents
improves resting tremor
AEs: constipation, xerostomia, urinary retention, confusion, blurred vision, tachycardia
Anticholinergic Agents
Anticholinergic Agents cautions
Elderly
o CV dz
o Prostatic dz
o Glaucoma
Amantadine (Symmetrel) as monotherapy for PD?
no
MOA: NMDA receptor antagonist
o Blocks glutamate transmission, enhances dopamine release, blocks acetylcholine
o Weak anti-Parkinson’s’ action (bradykinesia, rigidity, tremor) that typically lasts a few weeks
Amantadine (Symmetrel)
pharm targets for alzheimers
Improving cholinergic neurotransmission
o Inhibiting acetylcholinesterase
Inhibition of NMDA receptor-mediated excitotoxicity; limits glutamate
class: Donepezil (Aricept®)
Rivastigmine (Exelon®)
Galantamine (Razadyne®)
Cholinesterase Inhibitors
class: Memantine (Namenda®)
NMDA antagonist
AEs:
o N/V/D à do not give anticholinergic medications for management of symptoms
o SLUDGE = salivation, lacrimation, urination, diarrhea, GI upset, emesis
Cholinesterase Inhibitors
AEs:
§ N/V/D, SLUDGE
§ HA, insomnia, muscle cramps
§ Bradycardia, syncope, dizziness
Donepezil (Aricept)
Donepezil (Aricept) interactions
CYP3A4 substrate metabolism
wait ___ before switching to different cholinesterase inhibitor
3-6 months
Donepezil (Aricept) dose increases
4-6 weeks between 5 and 10mg increment
o 3 months between 10-23mg increment
which cholinesterase inhibitor comes in transdermal patch
Rivastigmine
Rivastigmine dosing
2 weeks for oral dose adjustment, 4 weeks for patch dose adjustment
AEs:
§ n/v/d, SLUDGE (less w/ transdermal patch)
§ Anorexia, dizziness, fatigue
§ Parkinson’s Exacerbation
• b/c if dopamine neurons are lost ACh is imbalanced and we are adding more ACh
o Too much ACh
Rivastigmine
MOA: Nicotinic receptor modulator à releases additional ACh
§ Increases glutamate and serotonin
Galantamine
Galantamine dosing
4 weeks between dose adjustments
indications: Memantine
mod-severe AD
Memantine dose adjustments
1 week between dose adjustments
AEs:
o Dizziness, HA, confusion
o Somnolence
o Weight gain
o Hallucinations
o Aggression
Memantine
tell pt to take MAO-B inhibitors when?
am bc of insomnia
MAO-B inhibitor causing the least insomnia
rasagiline
classes to treat AZ
Cholinesterase Inhibitors
NMDA Antagonist
classes to treat PD and suffixes
Dopamine Precursors (-dopa)
Dopamine Receptor Agonists (ole, tine)
Monoamine Oxidase B Inhibitors (line, amide)
Catechol-O-Methyl Transferase Inhibitor (pone)
Anticholinergic Agents (pine, dyl)
main levodopa SEs
nausea, agitation, confusion, dyskinesia
main dopamine receptor agonist SEs
Behavioral à confusion, hallucinations, somnolence, impulse control disorders
§ Previous tendency or new phenomena
§ Gambling, shopping, etc
