Loratadine's Anticholinergic Properties
Loratadine does not have significant anticholinergic properties when used at recommended doses. 1
Evidence on Loratadine's Anticholinergic Profile
The 2008 practice parameter on diagnosis and management of rhinitis clearly distinguishes between first-generation and second-generation antihistamines regarding anticholinergic effects:
First-generation antihistamines (like diphenhydramine, hydroxyzine) have significant anticholinergic effects including:
- Dryness of mouth and eyes
- Constipation
- Inhibition of micturition
- Increased risk for narrow angle glaucoma 1
Second-generation antihistamines, including loratadine, have "less or no tendency" for anticholinergic effects 1
The practice parameter specifically states that second-generation antihistamines like loratadine are "generally preferred over first-generation antihistamines" precisely because they lack significant anticholinergic properties 1.
Clinical Studies Supporting Lack of Anticholinergic Effects
Multiple clinical studies have confirmed the absence of anticholinergic effects with loratadine:
In a comparative study with terfenadine, no anticholinergic side effects were observed in patients receiving loratadine, while dry mouth (an anticholinergic effect) was reported in one terfenadine-treated patient 2
Another study specifically noted that "no anti-cholinergic effects occurred" with loratadine use 3
Dosage Considerations
It's important to note that loratadine's safety profile is dose-dependent:
- At recommended doses (typically 10mg daily), loratadine does not cause sedation or significant anticholinergic effects 1
- However, at doses exceeding the recommended amount, loratadine may cause sedation 1
Clinical Implications
The lack of significant anticholinergic properties makes loratadine a safer choice for:
- Elderly patients who are more susceptible to adverse anticholinergic effects 1, 4
- Patients with conditions that could be exacerbated by anticholinergic effects, such as:
Practical Prescribing Considerations
When prescribing antihistamines and concerned about anticholinergic burden:
- Choose second-generation antihistamines like loratadine over first-generation options
- Adhere to recommended dosing (10mg daily for loratadine)
- Be particularly cautious in elderly patients, who are more sensitive to anticholinergic effects
- Consider the patient's total anticholinergic burden from all medications
Pitfalls to Avoid
- Don't confuse loratadine with first-generation antihistamines, which do have significant anticholinergic properties
- Avoid exceeding recommended doses of loratadine, as higher doses may increase risk of side effects
- Be aware that patients with low body mass may experience higher effective doses on a mg/kg basis, potentially increasing risk of side effects 1
- Remember that anticholinergic effects can be cumulative when multiple medications with such properties are used simultaneously 4