Pharma LT: Treatment Of Dementia Flashcards
Cholinesterase inhibitors
Donepezil
Galantamine
Rivastigmine
Cholinergic activity and AD
In AD—> loss of cholinergic activity in nucleus basalis.
Ach—>regulates memory processing
Anti cholinesterase dont reverse the disease, but slow its progression with an increasing dose over several weeks
Donepezil
MOA
Centrally acting selective cholinesterase inhibitor
Donepezil
Effect on pt
Modest improvement in cognitive scores
Donepezil
Therapeutic use
In early, moderate and severe AD
Donepezil
Pharmacokinetics
Oral bioavailability=100%
Readily crosses bbb (centrally acting)
Long t1/2–> 1 dose/day
Donepezil
Side effects
N/V
Diarrhea
Insomnia
Less frequent than tacrine
Galantamine
MOA
- Competitive reversible inhibitor of cholinesterase
2. Modulates nicotinic receptors—> more Ach in the brain
Galantamine
Therapeutic use
Early-moderate AD
Galantamine
Pharmacokinetics
Oral bioavailability= 80-100%
T1/2= 7hrs therefore requires 2 doses/daily
Peak effect: 1 hr
Protein binding: low
Metabolism: in liver
Galantamine
Side effects
N/V
Diarrhea
Weight loss
Still better tolerated than tacrine
Rivastigmine
MOA
Inhibits both
acetylcholinesterase butrylcholinesterase—> non selective enzyme in plasma and many tissues; part of serine hydrolases
Rivastigmine
Therapeutic use
Mild-moderate AD
Rivastigmine
Side effects
N/V
Weight loss
Upset stomach
Still better tolerated than tacrine
Rivastigmine
Administration
Transdermal patch applied once daily and gives less side effects than when administered orally (oral dose given twice daily)
