Acetylcholinesterase Inhibitors Flashcards
For what type of dementia should acetylcholinesterase inhibitors and memantine not be used for?
Do not use acetylcholinesterase inhibitors or memantine for people with frontotemporal dementia.
Describe the short-term effects of acetylcholinesterase inhibitors in Alzheimer dementia.
In the short term, they modestly improve or stabilise cognition, alertness and function.
Describe the variance in efficacy between acetylcholinesterase inhibitors in Alzheimer dementia.
All acetylcholinesterase inhibitors appear to have similar efficacy for Alzheimer dementia.
What is the major consideration when initiating acetylcholinesterase inhibitors for Alzheimer dementia.
Their modest benefits must be weighed against their significant adverse effects
What are 9 significant adverse effects associated with acetylcholinesterase inhibitors.
- Prominent gastrointestinal adverse effects (particularly nausea, vomiting and anorexia)
- Weight loss
- Vivid dreams
- Urinary incontinence
- Tremor
- Cramps
- Bradycardia
- Dizziness
- Drowsiness
Describe the benefit-harm profile of acetylcholinesterase inhibitors.
Due to their adverse effects, the benefit–harm profile of acetylcholinesterase inhibitors varies depending on patient factors.
What are 3 points of monitoring which should be performed before initiating an acetylcholinesterase inhibitor?
Before starting an acetylcholinesterase inhibitor, perform an electrocardiogram (ECG), record the patient’s weight and assess their falls risk.
Are the adverse effects associated with acetylcholinesterase inhibitors dose-related?
Most adverse effects are dose-related
Describe the difference in ease-of-use of the different acetylcholinesterase inhibitors.
Donepezil, galantamine and the rivastigmine transdermal patch are easier to use than oral rivastigmine because they are dosed once daily and the dose can be more easily titrated.
Describe the effectiveness of memantine.
Memantine offers a small, short-term improvement or stabilisation in cognition and function for people with moderate to severe Alzheimer dementia (regardless of whether it is given as monotherapy or in combination with an acetylcholinesterase inhibitor).
If the response to an acetylcholinesterase inhibitor is inadequate in a patient with moderate to severe Alzheimer dementia, what can be done?
Consider adding memantine.
Besides adding memantine, what should be done if the response to an acetylcholinesterase inhibitor is inadequate for a patient with moderate to severe Alzheimer dementia?
Also consider whether the acetylcholinesterase inhibitor should be continued
If memantine is considered appropriate to treat cognitive impairment in a patient with moderate to severe Alzheimer dementia (eg a patient who cannot take an acetylcholinesterase inhibitor), what is the standard dose?
Memantine 5 mg orally, daily for 1 week. Increase the dose by 5 mg each week to a maximum of 20 mg.
Describe the effectiveness of acetylcholinesterase inhibitors in the treatment of dementia with Lewy bodies
The acetylcholinesterase inhibitors, donepezil and rivastigmine, modestly improve or stabilise cognition, alertness and function, and reduce hallucination frequency.
Describe the routine monitoring for adverse effects when starting an acetylcholinesterase inhibitor or memantine for dementia
Assess the patient for adverse drug effects and adjust the dose or treatment accordingly within 1 month of starting treatment, then again within 6 months (usually after 2 to 3 months of therapy at the maximum tolerated dose), and thereafter every 6 months.
How long should drug therapy for dementia be continued?
If the patient tolerates and appears to benefit from an acetylcholinesterase inhibitor or memantine, continue it for as long as quality of life is maintained—that is, until the patient has end-stage dementia (i.e. lost independent mobility, can no longer swallow) and therapy is no longer achieving their goals and preferences.
If a patient is experiencing intolerable adverse effects at lowest possible dosage of an acetylcholinesterase inhibitor which they have been using for less than 12 months, what can be done?
Switch therapy or cease treatment
If a patient is experiencing intolerable adverse effects at lowest possible dosage of an acetylcholinesterase inhibitor which they have been using for over 12 months, what can be done?
Cease treatment
If a patient’s cognition and function has not improved or stabilised after using the maximum tolerated dose of an acetylcholinesterase inhibitor for 6 to 12 months, what can be done?
Switch therapy or cease treatment
If a patient’s cognition and function has not improved or stabilised after using the maximum tolerated dose of an acetylcholinesterase inhibitor for over 12 months, what can be done?
Cease treatment
If, after initial improvement, a patient’s cognition and/or function has significantly worsen while using the maximum tolerated dose of an acetylcholinesterase inhibitor for 6 to 12 months, what can be done?
Switch therapy or cease treatment
If, after initial improvement, a patient’s cognition and/or function has significantly worsen while using the maximum tolerated dose of an acetylcholinesterase inhibitor for over 12 months, what can be done?
Cease treatment
What can be done is a patient cannot tolerate an acetylcholinesterase inhibitor?
If the patient cannot tolerate one acetylcholinesterase inhibitor, they may be able to tolerate another—stop the acetylcholinesterase inhibitor associated with the adverse effect and only start the new one once the adverse effect has resolved.
What can be done is a patient does not respond to an acetylcholinesterase inhibitor?
If the patient does not respond or stops responding to one acetylcholinesterase inhibitor, they may respond to another—perform a direct switch (ie stop the original acetylcholinesterase inhibitor and start the new one the next day).
If criteria for switching from an acetylcholinesterase inhibitor are not met, but switching is still considered, what should be done?
Seek specialist advice (such as a geriatrician, psychiatrist, or neurologist).
If the criteria for stopping an acetylcholinesterase inhibitor or memantine are not met, but deprescribing is still considered what should be done?
Seek specialist advice (such as a geriatrician, psychiatrist, or neurologist).
What 3 points should be covered in the carer’s plan if stopping an acetylcholinesterase inhibitor or memantine?
- Approach to monitoring
- Dosage adjustment
- Indicators for resuming the drug.
What are 3 first line options for the treatment of cognitive impairment in Alzheimer dementia?
- Oral donepezil
- Oral modified release galantamine
- Transdermal rivastigmine
What is the standard dosage of donepezil in Alzheimer dementia?
Donepezil 5 mg orally, at night for 4 weeks, then increase to 10 mg at night, if tolerated
Describe the evidence for drug therapy in dementia with Lewy bodies
Donepezil and rivastigmine appear to have similar efficacy for dementia with Lewy bodies.
What are 2 first line options for the treatment of cognitive impairment in dementia with Lewy bodies?
- Oral donepezil
2. Transdermal rivastigmine
What is the standard dosage of donepezil for dementia with Lewy bodies?
Donepezil 5 mg orally, at night for 4 weeks, then increase to 10 mg at night, if tolerated
What is the standard dosage of galantamine in Alzheimer dementia?
Galantamine modified-release 8 mg orally, in the morning for 4 weeks, then increase to 16 mg in the morning, if tolerated. If the patient initially responded to a 16 mg dose but, after at least 4 weeks, deteriorates, increase to 24 mg daily, if tolerated
Describe the difference in tolerability in oral rivastigmine and transdermal rivastigmine.
The rivastigmine transdermal patch is better tolerated than the oral formulation.
What is the standard dosage of transdermal rivastigmine in Alzheimer dementia?
Rivastigmine 4.6 mg transdermally, replaced daily for 4 weeks, then increase to 9.5 mg, replaced daily, if tolerated. If needed and tolerated, after at least 4 additional weeks, increase to 13.3 mg, replaced daily
What is a second line option of the treatment of cognitive impairment in Alzheimer dementia?
Oral rivastigmine
What is the standard dosage of oral rivastigmine in Alzheimer dementia?
Rivastigmine 1.5 mg orally, twice daily for 2 weeks, then, if tolerated, increase by 1.5 mg twice daily every 2 weeks up to a maximum of 6 mg twice daily.
What 3 strengths are rivastigmine patches available in?
- 4.6 mg/24 hours (9 mg)
- 9.5 mg/24 hours (18 mg)
- 13.3 mg/24 hours (27 mg)
What is the standard dosage of transdermal rivastigmine for dementia with Lewy bodies?
Rivastigmine 4.6 mg transdermally, replaced daily for 4 weeks, then increase to 9.5 mg, replaced daily, if tolerated. If needed and tolerated, after at least 4 additional weeks, increase to 13.3 mg, replaced daily
What is a second line option for the treatment of cognitive impairment in dementia with Lewy bodies?
Oral rivastigmine
What is the standard dosage of oral rivastigmine for dementia with Lewy bodies?
Rivastigmine 1.5 mg orally, twice daily for 2 weeks, then, if tolerated, increase by 1.5 mg twice daily every 2 weeks up to a maximum of 6 mg twice daily.
Describe the role in therapy of memantine in dementia with Lewy bodies
If a patient cannot take donepezil or rivastigmine, consider using the memantine regimen for Alzheimer dementia.
