Week 12 - Cholinesterase Inhibitors

Question 1

What conditions would cholinesterase inhibitors be used for?

Answer 1

Alzheimer’s disease

Question 2

Cholinesterase inhibitors: examples

Answer 2

Donepezil (Aricept)

Rivastigmine (Exelon)

Question 3

Cholinesterase inhibitors: MOA

Answer 3

Reversibly and noncompetitively inhibits centrally active acetylcholinesterase –> increased levels of acetylcholine available for synaptic transmission in the CNS

Question 4

Cholinesterase inhibitors: ADR

Answer 4

Dizziness, HA, agitiation, falls, weight loss, N/V/D, insomnia, tremor

Question 5

Cholinesterase inhibitors: caution and contraindications

Answer 5

• Avoid in combination w/ anticholinergic drugs
• Caution in renal and hepatic impairment
• Caution w/ seizure disorder
• Risk of QT prolongation (Donepezil)

Question 6

NMDA receptor antagonist: example

Answer 6

Memantine (Namenda)

Not a cholinesterase inhibitor

Question 7

NMDA receptor antagonist: MOA

Answer 7

Noncompetitive antagonist at NMDA receptors

Persistent stimulation of NMDA receptors by glutamate is thought to possibly contribute to the symptomatology of AD

Question 8

NMDA receptor antagonist: ADR

Answer 8

Confusion, dizziness, constipation, HA, somnolence, HTN, diarrhea

Rare: hypersensitivity reaction

Question 9

NMDA receptor antagonist: caution and contraindications

Answer 9

• Caution in CVD
• Caution in renal impairment
• Caution w/ seizure disorder

Question 10

ANS - cholinergic vs. adrenergic functions

Answer 10

Cholinergic

• Constricted pupils
• Increased saliva
• Bronchoconstriction
• Increased GI mucus
• Bladder fundus contraction

Adrenergic

• Dry mouth
• Dilated pupils
• Increased contractility
• Increased HR
• Bronchodilation
• Bladder fundus relaxation, sphincter contraction