(2026/2027) | Updated Questions |
Study Pack | A+
• Combo Alzheimer Drugs -✓✓Donepezil + Memantine (Namzaric) both given PO
• Pathophysiology of Alzheimers -✓✓Beta-amyloid plaques, neuritic plaques,
neurofibrillary tangles, and neuronal degeneration cause :
Cholinergic pathways are damaged > loss of Ach
Overstimulation of NMDA receptor by glutamate neuronal damage
Inhibitor of nicotinic receptors > impairs cognition
• Cholinergic Effects/ Effects of Acetylcholine -✓✓Ach boosts parasympathetic
response : bradycardia, muscle weakness/pain/cramps, convulsions, breathing
difficulties, increased stomach acid, increased saliva, N/V, blurred vision, low BP
(DUMBELS)
• Cholinesterase -✓✓enzyme that degrades acetylcholine
• Cholinesterase Inhibitors -✓✓selectively inhibit cholinesterase in the CNS, allowing for
Ach to remain in the system
*can slow deterioration of cognitive function (preserves memory, learning, attention)
*does NOT stop underlying degenerative process
• Cholinesterase Inhibitors Adverse Effects -✓✓(too much Ach is left in the system :
cholinergic effects)
All : DUMBELS
Diarrhea
Urinary incontinence
Miosis/Muscle Weakness
Bronchospasm/bradycardia
Emesis
Lacrimation (tears)
Salivation
(+bradycardia, N/Vsyncope, dizziness)
*titrate does slowly!
Donepezil : insomnia
,Rivastigmine : hepatotoxicity
Galantamine : weight gain
• Cholinesterase Inhibitor Drug Interactions -✓✓anticholinergic drugs
Donepezil is a minor substrate of CYP3A4
(enzyme slightly breaks down Donepezil)
• Memantine (Namenda) -✓✓NMDA receptor antagonist (neuroprotective, down-
regulates excitatory effects of glutamate)
can combo w/cholinesterase inhibitors
no CYP 450 interactions
• Memantine AE -✓✓constipation
headache
confusion
dizziness
hallucinations
HTN
• Parkinson's Disease -✓✓Degenerative disease of the basal ganglia > decline in
motor, autonomic, and cognitive function
severe loss of dopaminergic neurons of substantial nigra (80%)
*presence of Lewy bodies (intracellular inclusions)
=imbalance of Ach and dopamine
mortality from immobility > aspiration pneumonia, clotting
• Pharmacologic Targets for Parkinson's Drugs -✓✓Add Dopamine to suport Substantia
Nigra
Block Ach at Corpus Striatum
(GABA is also reduced in Parkinson's)
• Levodopa -✓✓for Parkinson's Disease
synthetic precursor to dopamine
(dopamine itself degrades peripherally and cannot cross BBB)
*metabolized in peripheral tissue by Decarboxylase and Catechol-O-methyl transferase
(COMT)
• Levodopa AE -✓✓Dose related
, N/V (antacid 30-60 min prior)
orthostatic hypotension, sedation
Depression, delirium, paranoia, delusions, hallucinations, long-term CNS effects
motor fluctuations (dose-related)
**ALWAYS give with Carbidopa
• Levodopa Formulations -✓✓Pair with Carbidopa (Sinemet, Sinemet CR, Parcopa -
ODT)
new formulation combined with Carbidopa in one pill = Rytary (Control-release)
*can be opened and sprinkled
minimal reduction in motor fluctuations
conversion from Sinemet required
$$$
may require fewer doses
• Carbidopa -✓✓Decarboxylase Inhibitor (stops breakdown to dopamine peripherally)
makes sure more drug enters brain
decreases GI, CV AE due to less peripheral conversion
titrate slowly to 75mg Carbidopa/day
• Carbidopa Wearing off phenomenon -✓✓loss of efficacy over time or fluctuation in
response to the med > higher doses needed after 2-5+ years
• COMT Inhibitors -✓✓stop peripheral metabolism of Levodopa by COMT to 3-OMD
metabolite
Tolcapone
Entacapone (more common)
• COMT Inhibitors AE -✓✓hepatotoxicity - Tolcapone
orthostatic hypotension
diarrhea
hallucinations
brown-orange urine - Entacapone
• Stalevo -✓✓Entacapone combined w/Levodopa/Carbidopa
• Monoamine Oxidase Inhibitors (MAOIs) -✓✓for Parkinson's Disease
irreversibly inhibit MAO enzyme system