Can increased choline intake reduce the effects of anticholinergic (anticholinergic) drugs?

Can Increased Choline Intake Reduce the Effects of Anticholinergic Drug Taking History?

There is insufficient evidence to recommend increased choline intake as a method to reduce the effects of anticholinergic drug history, as no high-quality clinical guidelines support this practice for improving morbidity, mortality, or quality of life outcomes.

Understanding Anticholinergic Medications and Their Effects

Anticholinergic medications are commonly prescribed for various conditions but carry significant side effects, particularly in older adults. These medications work by blocking the neurotransmitter acetylcholine in the central and peripheral nervous system.

Common anticholinergic side effects include:

• Drowsiness (65%)
• Dry mouth (53%)
• Dry eyes (53%)
• Constipation (39%)
• Blurred vision (39%)
• Urinary hesitancy (28%)
• Confusion (21%) 1

Evidence on Choline Supplementation and Anticholinergic Effects

While some basic science research suggests potential interactions between choline and anticholinergic agents, the clinical evidence for using choline supplementation to counteract anticholinergic effects is limited:

• A 1978 laboratory study showed that choline administration before atropine (an anticholinergic) prevented atropine-induced decreases in acetylcholine concentrations in rat brains 2

• Research from 1986 demonstrated that choline supplementation could prevent the depletion of acetylcholine induced by certain pharmacological agents, but did not enhance acetylcholine levels under normal conditions 3

• However, these studies are decades old, conducted in animal models, and have not been translated into clinical practice guidelines for human patients

Clinical Approach to Managing Anticholinergic Burden

Rather than recommending choline supplementation, clinical guidelines focus on:

1. Deprescribing anticholinergic medications when possible:

   • Older antihistamines (e.g., diphenhydramine)
   • Muscle relaxants (e.g., cyclobenzaprine)
   • Overactive bladder medications (e.g., oxybutynin) 4

2. Selecting alternatives with less anticholinergic properties:

   • For example, nortriptyline has fewer anticholinergic properties than amitriptyline and causes fewer cholinergic blockade symptoms 4

3. Monitoring for anticholinergic burden:

   • Multiple anticholinergic drugs can have cumulative effects on cognition and functionality
   • The Drug Burden Index shows that drugs with strong anticholinergic properties are associated with decline in cognition, functional status, and activities of daily living scores in older patients 4

Special Considerations for Specific Patient Populations

Elderly Patients

• Anticholinergic medications should be used with extreme caution in older adults
• Start at lower doses (e.g., TCAs at 10 mg/day instead of standard doses) 4
• Consider screening for fall risk and cognitive status before prescribing anticholinergics 1

Patients on Cholinesterase Inhibitors

• Anticholinergic drugs may antagonize the effects of cholinesterase inhibitors used in Alzheimer's disease
• Despite this pharmacological opposition, studies show that anticholinergic drug use is paradoxically more common among cholinesterase inhibitor users than non-users 5

Conclusion

While laboratory evidence suggests choline might theoretically counteract some anticholinergic effects, there is no clinical guideline evidence supporting choline supplementation as an intervention to reduce the effects of anticholinergic medications. The preferred approach is to reduce anticholinergic burden through careful medication selection and deprescribing when possible.