What are the drugs that increase saliva production, such as a spray, specifically sialagogues (saliva stimulants)?

From the Guidelines

Drugs that increase spit production, such as pilocarpine and cevimeline, are available and can be used to stimulate saliva production, with pilocarpine being licensed worldwide 1. When considering treatment options, it's essential to weigh the benefits and risks, particularly for patients with moderate glandular dysfunction.

• Pilocarpine and cevimeline are muscarinic agonists that can increase salivary flow rates and improve symptoms of dry mouth.
• These medications have been shown to be effective in patients with Sjögren's syndrome, although the evidence is limited for certain patient populations, such as those with primary Sjögren's syndrome (pSjS-2002) 1.
• Spray options, such as artificial saliva products or Xylitol-containing sprays, can provide immediate but temporary relief and may be used as needed throughout the day without significant side effects.
• The NCCN panel recommends dietary modifications, topical measures, and systemic sialagogues, such as cevimeline or pilocarpine, for patients with moderate or severe dry mouth symptoms 1.
• It's crucial to consider the potential side effects of oral medications, including sweating, urinary frequency, and digestive issues, and to consult with a healthcare provider before using systemic sialogogues, especially for patients with certain cardiovascular conditions, asthma, or glaucoma.
• The most recent guidelines suggest that holding immunotherapy may be recommended for patients with moderate or severe dry mouth, and rechallenge can be considered after symptoms become grade 1 1.

From the FDA Drug Label

Pilocarpine, in appropriate dosage, can increase secretion by the exocrine glands The sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract may be stimulated. In a study of 12 healthy male volunteers there was a dose-related increase in unstimulated salivary flow following single 5 mg and 10 mg oral doses of pilocarpine hydrochloride tablets. Increases from baseline (means 0.072 and 0.112 mL/min, ranges -0.690 to 0.728 and -0.380 to 1. 689) of whole saliva flow for the 5 mg (63%) and 10 mg (90%) tablet, respectively, were seen 1 hour after the first dose of pilocarpine hydrochloride tablets.

Pilocarpine can increase saliva production.

• The effect of pilocarpine on salivary flow was time-related with an onset at 20 minutes and a peak effect at 1 hour with a duration of 3 to 5 hours.
• Increases in unstimulated parotid flow were seen following the first dose.
• The ability of pilocarpine to stimulate saliva production was assessed in two 12 week randomized, double-blind, placebo-controlled studies. 2

From the Research

Drugs that Increase Spit Production

• Cevimeline is an orally administered muscarinic receptor agonist that is indicated for the treatment of symptoms of dry mouth in patients with Sjogren's syndrome, and it significantly improved the salivary flow rate in patients with Sjogren's syndrome 3.
• Pilocarpine and bethanechol have been reported as potentially effective sialogogues for xerostomic patients, and they can increase resting saliva production, but the increase in stimulated saliva production is limited 4.
• Pilocarpine mouthwash can relieve dry mouth symptoms and improve saliva production with minor side effects in elderly patients with xerostomia 5.
• Salagen and Evoxac are FDA approved salivary stimulants that are effective and safe for the treatment of dry mouth in Sjogren's syndrome, given awareness of their indications, contraindications, potential adverse effects, and patient's tolerance 6.

Saliva Substitutes

• Saliva substitutes can provide short-lived relief from dry mouth, but they do not provide the protective roles of saliva, and their duration of effect is short 6, 7.
• Emerging technologies such as self-assembly, emulsion, liposomes, and microgels are being developed as novel saliva substitutes that can provide efficient moistening and lubrication of the oral mucosa 7.

Treatment of Dry Mouth

• Effective treatment of dry mouth requires increasing salivary output, and pharmacological stimulants such as cevimeline, pilocarpine, and bethanechol can provide an alternative effective measure and improve compliance 3, 4, 6.
• Gustatory stimulation of the salivary glands with sugar-free gum and sugar-free candies may be effective in inducing salivary output, but they impose significant inconvenience on the patient which can compromise compliance 6.