Cholinesterase Inhibitors

Question 1

Donepezil (Aricept), Rivastigmine (Exelon)

MOA

Answer 1

• reversibly and noncompetitively inhibits centrally active acetylcholinesterase (AChE), which results in increased levels of acetylcholine available for synaptic transmission in the CNS
• acetylcholinesterase is an enzyme that catalyzes the breakdown of acetylcholine
• act as indirect cholinergic agonists
• Exelon can come in patch form; replace every 24 hours, reinitiate at lower dose if patch is off for more than 3 days
• Donepezil metabolized by P450 system; check drug-drug interactions

Question 2

Donepezil (Aricept), Rivastigmine (Exelon)

Caution and Contraindications

Answer 2

• avoid in combination with anticholinergic drugs
• caution in renal and hepatic impairment
• caution with seizure disorder
• risk of QT prolongation (Donepezil)

Question 3

Donepezil (Aricept), Rivastigmine (Exelon)

Adverse Drug Effects

Answer 3

• dizziness, headache, agitation, falls, weight loss, n/v, diarrhea, insomnia, tremor
• toxicity: constricted pupils, excessive salivation, diarrhea

Question 4

NMDA Receptor Antagonist
Namenda
MOA

Answer 4

• low to moderate, noncompetitive antagonist at NMDA receptors; persistent stimulation of NMDA receptors by glutamate is thought to possibly contribute to the symptomatology of AD
• often used in combination with Aricept or Exelon when AD becomes moderate to severe
• may work best on those with neuropsychiatric symptoms rather than cognition or function

Question 5

NMDA Receptor Antagonist
Namenda
Caution and Contraindications

Answer 5

• caution in cardiovascular disease
• caution in renal impairment
• caution with seizure disorders

Question 6

NMDA Receptor Antagonist
Namenda
Adverse Drug Effects

Answer 6

• confusion, dizziness, constipation, headache, somnolence, HTN, diarrhea
• hypersensitivity reaction (rare)