Acetylcholinesterase Inhibitors, such as donepezil

[image][image][image][image]Wikipedia: Donepezil, marketed under the trade name Aricept by its developer Eisai and partner Pfizer, is a centrally acting reversible acetylcholinesterase inhibitor. →

Acetylcholinesterase ihibitors are used along, or with ______ for more advanced disease.

A higher dose of donepezile (Aricept) was released in 2010 for advanced disease, however the benefit is very mild (2 point improvement on a 100 - point cognition scale). The motivation for the release of this product was the availability of generic donepezil. If a prescriber writes for the higher dose the patient will need o purchase the brand medicaiton.

No. Medications only delay the inevitable. Patients will lose thier minds :-)

Antidepressants (sertraline, citalopram, escitalopram) can be used to treat related depression and anxiety. Antidepressants can be used to treat delusion/anger, but they increase the risk of death in elderly patients (mostly due to an increased risk of stroke) and provide little benefit.

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Vitamine E is sometimes tried for dementia, but doses (> ____IU) carry risk and should be discussed with the physician.

Empirically? No. But many patients still use it.

Peripher anticholinergics (including incontinence & IBS drugs)

Central anticholinergics (benztropin, etc)

Antihistamines & antiemetics

Antipsychotics

Barbiturates

Benzodiazepines

Skeletal muscle relaxants

Other CNS depressants

MOA: inhibits centrally - active acetylcholinesterase, the enzyme responsible for hydrolysis (breakdown) of acetylcholine, which results in increased ACh.

Donepezil

Rivastigmine

Galantamine

Tacrine

1.5 - 6 mg bid

4.6 & 9.5 mg/24 hr patch

blocks NMDA which inhibits glutamate from binding to NMDA receptors and decreases abnormal activation

approved for use alone or in combination with donepezil (Aricept) for moderate to severe AD

Take XR with food or drink, IR with or without food

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5 - 10 mg BID (titrate aprx weekly)

or 28 mg Q daily if XR (start at 7 mg Q daily and titrate not faster than weekly)

XR caps can be opened & sprinkled in applesauce

Acetylcholinesterase:

use caution with concurrent use of drugs that can lower heart rate (i.e. beta blockers &c.) and with drugs that can cause dizziness (antipsychotics, antihypertensives)

Drugs that have anticholinergic effects can decrase the efficacy of acetylcholinesterase inhibitors

Statement. Not a question.

Donepezil is started at ___ mg, at bedtime. It is taken at ___  to help with ___.

Galantamine is started at ___ mg ___ daily, with or without food.

Exelon Patch:

apply to the upper or lower back, upper arm, or chest; rotate applications site. Do not use the same sith within 14 days. Do not apply to an area of the skin that is hairy, oily, irritated, broken, scarred, or calloused. After 24 hours remove the used patch.

Memantine:

Take ths medication by mouth, with or without food. When you first start taking this medication, you will usually take it once daily. Your dose will be gradually increased to lower the risk of side effects. Once your dose increases to more than 5 milligrams per day, take this medication twice daily (5mg twice daily, and then it usually increases to 10 mg twice daily).

Memantine ER (Namenda XR):

(1) If taken once daily with food or drink - if dysphagia can open capsule and sprinkle on applesauce (do not divide dose) but do not crush or chew the capsule.

(2) Start at 7 mg daily. Titrate weekly (as tolerated) to 28 mg Q daily.

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