Salagen (pilocarpine) is an oral medication produced by Merus Labs used to treat dryness in the eyes and mouth caused by Sjögren’s syndrome, a condition that frequently develops in scleroderma patients.

How Salagen works

Saliva and tears are produced by glands that are activated by parts of the nervous system known as the parasympathetic nervous system, which controls bodily functions while a person is in the “rest-and-digest”  mode. It slows heart rate, decreases pupil size, dilates blood vessels, and increases gland secretions and intestinal activity. The effects of the parasympathetic system are carried out through chemical messengers called acetylcholine, which works on acetylcholine receptors. There are two types of acetylcholine receptors: muscarinic and nicotinic.

Pilocarpine, the active ingredient of Salagen, is a compound derived from leaves of an American shrub Pilocarpus jaborandi and works by activating muscarinic acetylcholine receptors, stimulating saliva and tear production and relieving dryness in the mouth and eyes. Pilocarpine also is described as a cholinergic agonist, as it enhances the effects of acetylcholine.

Salagen in clinical trials for Sjögren’s syndrome

A study investigated the effect of Salagen in 44 Taiwanese patients with Sjögren’s syndrome. During the study participants received either 5 mg of Salagen tablets or placebo four times a day for three months. The results supported the effectiveness of Salagen compared to placebos to treat mouth dryness. Patients also reported improvements in their abilities to speak and sleep, as well as overall mouth comfort. None of the participants developed severe side effects, although 22 percent experienced excessive sweating. The study was conducted in the National University of Taiwan and the results were published in the Journal of the Formosan Medical Association.

Another study published in the Annals of Rheumatic Diseases showed that a three-month regimen of 5 mg oral Salagen twice a day, in combination with artificial tears, significantly relieved eye dryness in patients with Sjögren’s syndrome, compared with patients using artificial tears alone or in addition to inferior lacrimal puncta occlusion (the blockage of tear ducts with collagen plugs to prevent tears from draining). Common side effects experienced by patients taking Salagen were nausea, vomiting, headache, and sweating.

A similar study compared the effectiveness of either 2.5 mg or 5 mg of oral Salagen taken four times daily to placebo for three months in 373 patients with Sjögren’s syndrome. Not only did the 5 mg dose of Salagen significantly improve symptoms of dry mouth, it also relieved dry eyes and other symptoms of dryness. Sweating was also the most common side effect experienced by patients in this study and no serious side effects were reported. The study was published in JAMA Internal Medicine.

More details

Common side effects of Salagen include nausea, dizziness, headache, increased blood pressure and heart rate, stomach cramps, flushing, increased need to urinate, and excessive sweating. Taking Salagen before meals and with milk or yogurt just before sleeping may help reduce the stomach cramps.

A team of researchers from Japan sought to overcome these disruptive side effects by producing a novel mixture of oral Salagen with sodium alginate. They found that the new formulation was able to significantly stimulate saliva production in patients with Sjögren’s syndrome after just an hour of taking the compound. The new formulation was also well-tolerated, with patients experiencing only sweating and no other major side effects. The team published its results in March 2018 in the Journal of Pharmaceutical Health Care and Science It is not known whether this formulation will be developed further clinically.

Patients who have severe asthma or eye conditions like acute iritis (inflammation of the iris) and narrow-angle glaucoma are advised to avoid using Salagen because the treatment may worsen their condition.

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