Cholinesterase Inhibitors Side Effects, Uses, and Drug Interactions

  • Pharmacy Author:
    Omudhome Ogbru, PharmD

    Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.

  • Medical and Pharmacy Editor: Charles Patrick Davis, MD, PhD
    Charles Patrick Davis, MD, PhD

    Charles Patrick Davis, MD, PhD

    Dr. Charles "Pat" Davis, MD, PhD, is a board certified Emergency Medicine doctor who currently practices as a consultant and staff member for hospitals. He has a PhD in Microbiology (UT at Austin), and the MD (Univ. Texas Medical Branch, Galveston). He is a Clinical Professor (retired) in the Division of Emergency Medicine, UT Health Science Center at San Antonio, and has been the Chief of Emergency Medicine at UT Medical Branch and at UTHSCSA with over 250 publications.

What are cholinesterase inhibitors (ChEIs)? How do they work?

Cholinesterase inhibitors or acetylcholinesterase inhibitors are medications that prevent the breakdown of acetylcholine in the body. Cholinesterase inhibitors block the action of acetylcholinesterase. Acetylcholinesterase is an enzyme that breaks down acetylcholine to an inactive form. This reduces nerve cell communications in your body that use acetylcholine to help transmit cell to cell messages.

Acetylcholine is one of the chemicals that nerve cells use to communicate with one another in the brain, the central nervous system (CNS), and other areas of the body. Acetycholine affects learning, memory, and other cognitive function(s). Scientists think that reduced levels of acetylcholine in the brain causes some of the symptoms of Alzheimer’s disease. Blocking the enzyme that destroys acetylcholine with a cholinesterase inhibitor (anticholinesterase) increases the concentration of acetylcholine in the brain, and this increase may improve memory and cognitive function.

What are the uses for cholinesterase inhibitors?

Doctors prescribe cholinesterase inhibitors to individuals with dementia caused by Alzheimer’s disease and dementia.

Doctors also prescribe them to individuals to treat Lewy Body dementia, Parkinson's disease, glaucoma, myasthenia gravis, and schizophrenia.

Some cholinesterase inhibitors are used as antidotes. Some can treat mild to moderate Alzheimer's disease, for example, rivastigmine (Exelon, Razadyne), while donepezil (Aricept) is approved to treat all stages, from mild Alzheimer's to severe Alzheimer's disease.

What are the side effects of cholinterase inhibitors?

Some common side effects or adverse events of cholinesterase inhibitors are:

What are the drug interactions for cholinesterase inhibitors?

Drugs that block the action of acetylcholine produce opposite effects to the effects of cholinesterase inhibitors. They may reduce the effect of cholinesterase inhibitors. Examples of such drugs include atropine, benztropine (Cogentin), and trihexyphenidyl (Artane).

Bethanechol (Urecholine) increases the effect of acetylcholine and therefore may add to the effect and side effects of cholinesterase inhibitors.

What are the types of cholinterase inhibitors?

Cholinesterase inhibitors that are used in medicine are reversible cholinesterase inhibitors. Irreversible (also termed Quasi-irreversible) cholinesterase inhibitors are often used as pesticides or chemical weapons, for example, carbamate, metrifonate.

List of examples of brand and generic names of cholinesterase inhibitors

List and examples (brand and generic names) of some FDA-approved cholinesterase inhibitors.

  • donepezil (Aricept, Aricept ODT)
  • tacrine (Cognex) (This medication is discontinued in the US)
  • rivastigmine (Exelon, Exelon Patch)
  • galantamine (Razadyne or formerly Reminyl)
  • memantine/donepezil (Namzaric)
  • ambenonium (Mytelase)
  • neostigmine (Bloxiverz) for non-depolarizing neuromuscular blocking agents

Are cholinesterase inhibitors safe to use if I am pregnant or breastfeeding?

Cholinesterase inhibitors have not been well studied in pregnant women. It is not known whether they are safe to use during pregnancy or while breastfeeding. If you are pregnant, check with your OB/GYN doctor before using any of these drugs.

Summary

Cholinesterase inhibitors (acetylchlinesterase inhibitors) are medications that block the breakdown acetylcholine (a neurotransmitter), and that block the action of acetylchlinesterase in the body. Researchers believe that decreased levels of acetylcholine in the brain causes Alzheimer's disease and dementia symptoms.

Cholinesterase inhibitors are prescribed for the treatment and management of dementia caused by Alzheimer's disease. They also are used for the treatment and management of Parkinson's disease, glaucoma, myasthenia gravis, schizophrenia, and Lewy body dementia.

Common side effects of cholinesterase inhibitors are insomnia, abnormal dreams, weight loss, headache, nausea, vomiting, diarrhea, confusion, and fatigue. More serious side effect include hallucinations, confusion, fainting, high blood pressure, and frequent urination.

Cholinesterase inhibitors interacts with some drugs. These drugs should not be used during pregnancy or breastfeeding.

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Medically Reviewed on 11/21/2017
References
REFERENCE: FDA Prescribing Information.
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