Key Takeaways

Anticholinergic drugs are used to treat respiratory disorders like chronic obstructive pulmonary disease (COPD), Parkinson disease, overactive bladder, gastrointestinal disorders such as irritable bowel syndrome (IBS), insomnia, motion sickness, and postoperative nausea and vomiting.
Anticholinergics should be used with caution and exactly as prescribed. Older adults are at an increased risk for side effects from anticholinergic drugs because it may take longer for medications to be removed from their bodies compared to younger individuals.
Anticholinergics can also worsen dementia symptoms. Notably, many anticholinergic drugs are on the Beers Criteria (also known as the Beers List) for potentially inappropriate medication use in older adults.

Anticholinergic medications are used to treat a wide range of symptoms and diseases. Please continue reading to learn more about the uses and side effects of anticholinergic drugs.

What is an anticholinergic drug?

An anticholinergic is a drug that blocks the activity of a neurotransmitter acetylcholine by binding to cholinergic receptors, specifically nicotinic receptors and muscarinic receptors at the neuromuscular junction. Muscarinic and nicotinic acetylcholine receptors are found throughout the body.

Acetylcholine is a natural chemical that plays a role in various bodily functions, including involuntary muscle movements, body secretion (such as sweat and saliva), memory, learning, attention, and erections.

By blocking the action of acetylcholine, anticholinergic drugs affect the parasympathetic nervous system, which controls involuntary functions in the respiratory system, gastrointestinal tract, urinary tract, and other parts of the body.

The activity of these medications on the cholinergic system has wide-ranging physiologic effects on the body, including effects on alertness, vision, circulation, digestion, and respiration.

What are some examples of drugs with anticholinergic properties?

There are more than 600 medications that have anticholinergic properties.

Keep in mind that certain anticholinergic medications have effects that are considered therapeutic, while others are considered adverse effects. This means that there are many anticholinergic medications that are designed so that their anticholinergic properties are therapeutic to treat certain conditions or symptoms.

On the other hand, the anticholinergic effects of many medications are just adverse effects. For example, certain antipsychotics and antidepressants have anticholinergic effects that are not therapeutic effects.

The anticholinergic properties of these medications are side effects. Some examples include urinary retention, dry mouth, constipation, and dry eyes.

The degree of these anticholinergic side effects varies. Some can be bothersome, while others can be severe enough to cause discontinuation of treatment.

What are the main uses of anticholinergic drugs?

Anticholinergic drugs are used to treat specific conditions such as:

Respiratory disorders

Anticholinergics such as ipratropium (Atrovent) and tiotropium (Spiriva) are bronchodilators, i.e., they help to dilate (relax and widen) the bronchi (airways) and relieve shortness of breath in people with chronic obstructive pulmonary disease (COPD).

Parkinson disease

Anticholinergic agents such as benztropine mesylate (Cogentin) and trihexyphenidyl HCl (Artane) are used to counter low dopamine levels and relieve symptoms such as stiffness, tremors, spasms, and poor muscle control in people with Parkinson’s disease.

Overactive bladder

Anticholinergic medications such as oxybutynin (Ditropan), tolterodine (Detrol), fesoterodine (Toviaz), and darifenacin (Enablex) are used for the treatment of urinary frequency, urinary incontinence, and overactive bladder. Oxybutynin is also used off-label for hyperhidrosis (excessive sweating).

Gastrointestinal disorders

Clidinium is an anticholinergic agent that reduces stomach acid production and decreases bowel spasms. A combination of clidinium and a benzodiazepine called chlordiazepoxide (brand name Librax) may be prescribed by a digestive and kidney diseases specialist to treat peptic ulcers, enterocolitis (inflammation of the bowel), and irritable bowel syndrome (IBS).

Other medications, such as hyoscyamine (Levsinex), are used to treat stomach and bowel problems, including cramps and IBS.

Anticholinergic drugs such as glycopyrrolate are also used to treat peptic ulcer disease. Glycopyrrolate is also used during anesthesia to decrease respiratory tract secretions. It is also sometimes prescribed for chronic, severe drooling in children with cerebral palsy.

Insomnia

Antihistamines such as diphenhydramine (Benadryl) and doxylamine have strong anticholinergic properties, causing sedation, drowsiness, and sleepiness. Therefore, they are used as sleeping aids and nighttime cold and flu medications.

Motion sickness and postoperative nausea and vomiting

An anticholinergic agent called scopolamine (Transderm-Scop, Scopace, Maldemar) is used to prevent motion sickness and treat postoperative nausea and vomiting.

Muscle pain and stiffness

The anticholinergic drug orphenadrine citrate is used to relax muscles and relieve pain and stiffness associated with strains, sprains, and other muscle injuries. Orphenadrine tablets may also be used to treat people with Parkinson’s disease.

Medical and surgical procedures

Anticholinergic drugs such as atropine, cyclopentolate, and homatropine hydrobromide are used to dilate the pupils before eye examinations.

Atropine is used to reduce respiratory tract secretions during surgical procedures, to treat mushroom and insecticide poisoning, and for emergency treatment of slow heartbeat.

Other anticholinergic medications, such as vecuronium and succinylcholine, are given in addition to general anesthesia during intubation and to promote muscle relaxation during mechanical ventilation and surgical procedures.

What are the major side effects of anticholinergic drugs?

Side effects of anticholinergics include both peripheral and central nervous system effects.

Common anticholinergic side effects include headache, memory problems, cognitive impairment, behavioral changes, anxiety, and insomnia.

High doses of anticholinergic medications can result in toxicity and symptoms such as confusion, agitation, delirium, and lethargy.

Potential adverse effects of anticholinergic medications can also include increased body temperature due to decreased sweating, flushing, dry mouth, fast heartbeat, reduced saliva and tear production, headache, constipation, urinary retention, blurred vision, and dilated pupils.

Who should not take anticholinergic medications?

Research information shows that anticholinergics should be used with caution, especially in older adults.

Compared to younger people, older adults have a more permeable blood-brain barrier and are at an increased risk of side effects from anticholinergic drugs.

Also, the overall anticholinergic burden (cumulative use of multiple anticholinergics) is linked to a greater risk of adverse effects and anticholinergic toxicity.

People with certain health conditions, such as dementia, have a relative contraindication to the use of anticholinergics.

The exact cause of dementia remains unknown. However, it is believed that dementia is associated with reduced acetylcholine levels in the brain, and the use of anticholinergics can worsen dementia symptoms due to increased sedation, lethargy, and confusion.

Other health conditions that can be negatively impacted by the use of anticholinergics include glaucoma, tachyarrhythmias (heart rhythm abnormalities), and prostate hypertrophy (enlarged prostate gland).

Some anticholinergic drugs are available over the counter, while others require a doctor’s prescription. It’s important to take anticholinergic medications exactly as prescribed.

Same as prescription drugs, you should always use OTC medications with caution and consume doses that are within the acceptable daily intake stated on the label. Taking medications as prescribed will lower your risk of serious adverse effects.

If you are 65 years and older, you should always talk to your doctor or pharmacist before taking any new medications.

Many OTC products used for sleep aids and cold and flu symptoms are anticholinergic medications listed on the Beers Criteria for potentially inappropriate medication use in older adults.

It’s also important to give your healthcare provider a complete list of your other drugs before starting an anticholinergic medication to avoid drug interactions.

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References:

https://my.clevelandclinic.org/health/articles/24568-acetylcholine-ach
https://www.ncbi.nlm.nih.gov/books/NBK555893/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4857824/#
https://my.clevelandclinic.org/health/drugs/19824-atropine-injection
https://www.mayoclinic.org/drugs-supplements/chlordiazepoxide-and-clidinium-oral-route/description/drg-20074928
https://www.mayoclinic.org/drugs-supplements/orphenadrine-oral-route/description/drg-20065214#

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