Pilocarpine for Dry Eyes in Sjögren's Syndrome

Mechanism and Indications

Pilocarpine is a cholinergic agonist that binds to muscarinic receptors, stimulating secretion of salivary and sweat glands, and appears to improve tear production in patients with Sjögren's syndrome, as recommended by the American Academy of Ophthalmology 1, 2
The FDA approves pilocarpine for treating symptoms of dry mouth in patients with Sjögren's syndrome, but its use for dry eyes is considered off-label, according to the American College of Rheumatology 3, 2

Patients with Sjögren's syndrome treated with pilocarpine at 5 mg orally four times daily experienced significant improvement in their ability to focus during reading and reduced symptoms of blurred vision compared to placebo, with a moderate level of evidence 1, 2
Clinical studies consistently demonstrate greater improvement in dry mouth than dry eye symptoms in patients with Sjögren's syndrome, with a high strength of evidence 3, 4

The European League Against Rheumatism recommends offering a trial of muscarinic agonists, such as pilocarpine, to patients with moderate glandular dysfunction in Sjögren's syndrome, or in those with mild dysfunction who are refractory to other treatments, with a strong recommendation 5
Pilocarpine should be considered for patients with severe dry eye unresponsive to conventional treatments, such as artificial tears and ocular gels/ointments, and for those with confirmed Sjögren's syndrome with both dry eye and dry mouth, according to the American Academy of Ophthalmology 5, 3

The most common side effect of pilocarpine is excessive sweating, occurring in over 40% of patients, with a high level of evidence 1, 2
Approximately 2% of patients discontinue treatment due to side effects, such as headache, nausea, and vomiting, with a moderate level of evidence 1, 2

Pilocarpine should be used with caution in patients with cardiovascular disease, asthma, or other conditions where cholinergic stimulation may be problematic, as recommended by the American Heart Association 2
Patients should be monitored for side effects and efficacy, with consideration of discontinuation if benefits don't outweigh adverse effects, according to the American Academy of Ophthalmology 2