Saliva Stimulants

Topical products to stimulant salivary flow include a variety of OTC sugar-free gums, mints, and candies. Patient acceptance is variable and it is essential that patients be instructed to carefully read the product labels to ensure there are no hidden sugars.

Systemic stimulants include the sialagogues pilocarpine hydrochloride (Salagen®) and cevimeline hydrochloride (Evoxac®). Pilocarpine and cevimeline bind to muscarinic receptors, stimulating exocrine gland activity (such as salivary and sweat glands) and increased smooth muscle tone in the gastrointestinal and urinary tracts. Common adverse effects include sweating, headache, GI discomfort, nausea, increased lacrimation, urinary frequency, and palpitations.

Severe adverse reactions are uncommon, but sialagogues should be used with caution in patients with chronic obstructive pulmonary disease, asthma, significant cardiovascular disease, hepatic impairment, nephrolithiasis or cholelithiasis, and in patients taking ß-blockers. Sialagogues are contraindicated in patients with known hypersensitivity to the drug, uncontrolled asthma, and when miosis is undesirable (e.g., in acute iritis and in narrow-angle (angle-closure) glaucoma).

Pilocarpine is approved by the FDA to manage hyposalivation associated with therapeutic head and neck radiation and Sjögren’s syndrome.8 Cevimeline is FDA approved for the management of hyposalivation associated with Sjögren’s syndrome.9 The response to sialagogues is predicated on the number of functional acinar cells within the gland.4 Optimal dosing is determined by titration and it may take up to 6-12 weeks to achieve maximum efficacy.

Dry Mouth: Rx Pilocarpine

Mechanism of action: Binds to muscarinic receptors, causing an increase in secretion of exocrine glands (such as salivary and sweat glands) and increase tone of smooth muscle in gastrointestinal and urinary tracts.

Indications: Treatment of symptoms of xerostomia and/or salivary gland hypofunction caused by radiotherapy for cancer of the head and neck and Sjögren’s syndrome.

Contraindications: Hypersensitivity to pilocarpine or any component of the formulation; uncontrolled asthma, and when miosis is undesirable, e.g., in acute iritis and in narrow-angle (angle closure) glaucoma.

Warnings/Precautions: Use with caution in patients with cardiovascular disease, cholelithiasis, hepatic impairment, nephrolithiasis, respiratory disorders.

Drug interactions: Acetylcholinesterase inhibitors and ß-blockers may enhance the adverse/toxic effect of cholinergic agonists. Pilocarpine might antagonize the anticholinergic effects of drugs used concomitantly.

Administration:
Dosage form – 5 mg or 7.5 mg tablets.
For post-head and neck irradiation - 5 mg taken 3 times a day. Titrate according to therapeutic response and tolerability (not to exceed 30 mg per day or 10 mg per dose).
For Sjögren’s syndrome - 5 mg taken 4 times a day.

Monitor efficacy: Increased salivary flow rate, improved oral comfort.

Monitor toxicity: Hypotension, bradycardia, tremor, diaphoresis, nausea, dizziness, headache, confusion, muscarinic toxicity.

Length of treatment: No limitations.

Cessation of treatment: Does not require tapering.

Instructions to the patient: Use only as instructed.

For additional information see DailyMed

Dry Mouth: Rx Cevimeline

Mechanism of action: Binds to muscarinic receptors, causing an increase in secretion of exocrine glands (such as salivary and sweat glands) and increase tone of smooth muscle in gastrointestinal and urinary tracts.

Indications: Treatment of symptoms of xerostomia and/or salivary gland hypofunction caused by Sjögren’s syndrome.

Contraindications: Hypersensitivity to pilocarpine or any component of the formulation; uncontrolled asthma, when meiosis is undesirable (e.g., acute iritis, narrow-angle (angle closure) glaucoma).

Warnings/Precautions: Use with caution in patients with cardiovascular disease, cholelithiasis, hepatic impairment, nephrolithiasis, respiratory disorders. Cevimeline should be used with caution in individuals known or suspected to be deficient in CYP2D6 due to reduced cevimeline metabolism. Patients should be informed that cevimeline may cause visual disturbances, especially at night, that could impair their ability to drive safely.

Drug interactions: Acetylcholinesterase inhibitors and ß-blockers may enhance the adverse/toxic effect of cholinergic agonists. Cevimeline might antagonize the anticholinergic effects of drugs used concomitantly.

Administration:
Dosage form – 30 mg capsule.
For Sjögren’s syndrome – 30 mg taken 3 times a day.

Monitor efficacy: Increased salivary flow rate, improved oral comfort.

Monitor toxicity: Hypotension, bradycardia, tremor, diaphoresis, nausea, dizziness, headache, confusion, muscarinic toxicity.

Length of treatment: No limit.

Cessation of treatment: Do not require tapering.

Instructions to the patient: Use only as instructed.

For additional information see DailyMed