Ask the Pharmacist

Q: I am told that anti-cholinergics can be harmful to the elderly. Can you explain what an anti-cholinergic is and why it can be concerning?

A: Let’s first describe what exactly an anti-cholinergic is and what medications you might be taking that fall into this category.

Anti-cholinergics are a class of drugs that block the action of acetylcholine, a chemical messenger in the nervous system. Acetylcholine plays a crucial role in our body functions, such as muscle movement, digestion, salivation, urination, and memory. By blocking acetylcholine, anti-cholinergics can reduce certain kinds of nervous system activity and help manage conditions, such as overactive bladder, allergies, motion sickness, and even depression.

Some commonly used medications with medium/high anti-cholinergic properties include:
 

• Overactive bladder medications: Oxybutynin (Ditropan), tolterodine (Detrol), and solifenacin (Vesicare)
• Allergy medications: Diphenhydramine (Benadryl) and chlorpheniramine (Chlor-Tripolon).
• Anti-depressants: Amitriptyline, nortriptyline, paroxetine among others.
• Motion sickness medications: Dimenhydrinate (Gravol) and scopolamine.
• Muscle relaxants: Cyclobenzaprine, baclofen, methocarbamol and orphenadrine.
• Parkinson Disease medications: Benztropine and trihexyphenidyl.

Please note that the above list includes just a few examples of anti-cholinergic medications. Also, there are many medications with low anti-cholinergic activity that, alone, may not pose an issue but when they are combined with other low-activity or medium/high anti-cholinergics they may lead to problems.

You might be wondering why anti-cholinergics were fine when you were younger but may no longer be the best choice for you or your loved one. As we mature (at least in years and perhaps not in our behaviour), our bodies undergo numerous physiological changes that can affect how medications work and how we respond to them, and anti-cholinergics is one class of medications that requires special attention in the elderly.

As the earth rotates around the sun year-after-year (i.e. we celebrate another birthday and get older and wiser), we need to assess if it is still safe for us to be taking these medications. There are several reasons behind why our body becomes more sensitive to the anti-cholinergics effects of medications:
 

• Decreased metabolism and clearance: The liver and kidneys, responsible for metabolizing and clearing drugs, may function less efficiently, leading to higher drug levels in the body.
• Increased sensitivity: Aging brains are more sensitive to the effects of acetylcholine blockade, increasing the risk of cognitive decline and delirium.
• Polypharmacy: Many older adults take multiple medications, raising the risk of drug interactions and compounding anti-cholinergic effects. This may also be true of people who use one pharmacy but self-medicate with over-the-counter medications along with their prescriptions.

When this happens, our body experiences a cumulative anti-cholinergic activity which can significantly increase the risk of side effects, including:
 

• Confusion and memory impairment
• Drowsiness and dizziness
• Dry mouth
• Dry eyes
• Blurred vision
• Increased heart rate
• High body temperature
• Vomiting
• Constipation
• Difficulty urinating
• Weakened muscle strength
• Increased risk of falls

This does not mean that if you are taking an anti-cholinergic that you should discontinue it and find an alternative. However, if you are experiencing any of the above symptoms that might be attributed to an anti-cholinergic, it is essential to weigh the benefits of symptom control against the potential risks.

For example, medications for overactive bladder can significantly improve quality of life by reducing frequent trips to the bathroom or accidents. However, these benefits must be considered alongside such risks as cognitive decline or falls. Some pros and cons and alternatives to some common medical conditions that are treated with anti-cholinergics are:
 

• Overactive bladder medications

Pros: Can significantly improve quality of life by reducing urinary urgency, frequency, and incontinence.
Cons: May cause dry mouth, constipation, blurred vision, and confusion.
Alternative: Newer medications, such as mirabegron (Myrbetriq), may be a safer alternative as they work through a different mechanism and have minimal anti-cholinergic effects.
 

• Allergy medications

Pros: Effective for treating allergy symptoms, such as runny nose, itching, and hives.
Cons: First-generation anti-histamines, such as diphenhydramine, can cause significant drowsiness, confusion, and fall risk.
Alternative: Second-generation anti-histamines, such as loratadine (Claritin) or cetirizine (Reactine), are safer options with fewer central nervous system effects.
 

• Anti-depressants

Pros: Useful for managing depression, anxiety, or chronic pain.
Cons: Older tricyclic anti-depressants, such as amitriptyline, have high anti-cholinergic activity.
Alternative: Safer alternatives include selective serotonin re-uptake inhibitors (SSRIs), such as sertraline or citalopram.

If you are taking medications with anti-cholinergic properties, or have a loved one who is doing so, it might be time to book an appointment to review your medications.

You may have noticed that anti-cholinergics are available over-the-counter and by prescription. Therefore, it is essential for you to bring a complete list of your medications, including all over-the-counter products and supplements, to your pharmacist or health-care provider for review.

Ask if there are safer options that provide similar benefits with fewer risks. When starting any new medication, use the lowest effective dose and monitor for side effects. Also, try to drink plenty of water to help counteract dry mouth and prevent constipation.

In conclusion, though anti-cholinergics can be helpful for managing various health conditions, their risks increase significantly with age. Knowing and understanding these risks and being aware of the symptoms to look out for, allows you to make informed decisions about your medications and maintain the best possible quality of life.

For more information about this or any other health-related questions, contact the pharmacists at Gordon Pharmasave, Your Health and Wellness Destination. Also check the website at www.gordon-pharmasave.com/ and the Facebook page at www.facebook.com/GordonPharmasave/