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Donepezil Drug Class

donepezil drug class

Pharmacological Class:

Reversible acetylcholinesterase inhibitor (piperidine deriv).

What are Cholinesterase inhibitors?

Cholinesterase inhibitors (also called acetylcholinesterase inhibitors) are a group of medicines that block the normal breakdown of acetylcholine. Acetylcholine is the main neurotransmitter found in the body and has functions in both the peripheral nervous system and the central nervous system. For example, acetylcholine is released by motor neurons to activate muscles; acetylcholine also has an important role in arousal, attention, learning, memory and motivation.

Cholinesterase inhibitors block the action of the enzyme cholinesterase, which is responsible for breaking down acetylcholine. This increases levels of acetylcholine in the synaptic cleft (the space between two nerve endings).

The main use of cholinesterase inhibitors is for the treatment of dementia in patients with Alzheimer's disease. People with Alzheimer's disease have reduced levels of acetylcholine in the brain. Cholinesterase inhibitors have been shown to have a modest effect on dementia symptoms such as cognition.

Treatment of Anticholinergic Toxicity.

Over 600 compounds have significant anticholinergic effects, including over-the-counter drugs, prescription drugs & some plants (Su & Goldman, 2013). Physostigmine, which crosses the blood-brain barrier, has been used as antidotal therapy for severe cases of anticholinergic toxicity. However its use is not without risk. Patients should be placed on a cardiac monitor, and both atropine and equipment for resuscitation should be available before it is administered (Su & Goldman, 2013).

PostOp Urinary Retention. Neostigmine can be used to treat urinary retention that results from general anesthesia. Postoperative urine retention is a relatively common problem and is associated with an increased risk of urinary tract infections (rxlist.com).

Open-Angle Glaucoma. Echothiophate eye drops have been used (historically) to enhance the effect of endogenously released acetylcholine in the eye, causing contraction of the ciliary muscle, which facilitates the outflow of aqueous humor from the interior chamber of the eye, resulting in a fall in intraocular pressure. While echothiophate eye drops are still available, beta blockers and prostaglandins, have become drugs of choice for achieving this treatment goal.

side effect:

  • Actions on the parasympathetic nervous system, (the parasympathetic branch of the autonomic nervous system) may cause bradycardia, hypotension, hypersecretion, bronchoconstriction, GI tract hypermotility, and decrease intraocular pressure, increase lower esophageal sphincter (LES) tone
  • Sludge syndrome.
  • Actions on the neuromuscular junction will result in prolonged muscle contraction.
  • The effects of neostigmine on postoperative nausea and vomiting are controversial and there is not a clear linkage in clinical practice, however, there is good evidence to support the reduction in risk when anticholinergic agents are administered.[11]

Administration of reversible cholinoesterase inhibitors is contraindicated with those that have urinary retention due to obstruction.

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