Pilocarpine is an effective drug for treating xerostomia (dry mouth) from various causes. It is commercially available in a tablet form for oral use but is not available in the form of a lozenge. The only way to obtain the lozenges is by having them custom made by a compounding pharmacy.

Xerostomia

Xerostomia refers to a sensation of dryness in the mouth that is difficult to alleviate. In most cases xerostomia results from a decrease in the volume of saliva – often below 50% of the level of saliva normally produced. It may also occur not because of a decrease in saliva volume but instead a change in the composition of saliva.

Saliva’s role is not just in assisting with eating. It has other important roles in starting digestion, breaking down starches, and restoring calcium and phosphate to tooth enamel. This is why declines in saliva have other effects besides causing dry mouth. Dental health also declines with decreased saliva production and may result in infection.

Medications are a common cause of dry mouth. In these cases, the dry mouth is usually reversible by discontinuation of the medication or a lower dose. For dry mouth caused by a chronic disorder like Sjögren Syndrome or by radiation therapy, other treatments are often required.

Treatments for Dry Mouth

Lifestyle changes are one way that patients are told to decrease the severity of their dry mouth. This may include consuming less caffeine, avoiding mouthwashes that contain alcohol, sipping water regularly, and discontinuing the use of certain OTC medications. Saliva substitutes may provide temporary relief but most patients find them irritating or inconvenient to use. There may be other techniques that are used to manage the associated symptoms of saliva loss like tooth decay – for example fluoride treatments.

The main types of medication used for managing dry mouth are cholinergic agonists. The two most common cholinergic agonists used are cevimeline and pilocarpine. While they have different mechanisms of action, both medications work similarly and studies have shown there is no significant difference in their effectiveness or safety profiles.

Pilocarpine

Pilocarpine is a naturally occurring compound that is made into a medication from harvested wild or cultivated plants. The plant it is derived from is a South American shrub called Pilocarpus jaborandi. The plant alkaloid is a cholinergic parasympathomimetic agonist. This type of drug works by mimicking or modifying the effects of acetylcholine, which is the primary neurotransmitter of the parasympathetic nervous system. Pilocarpine directly binds to and actives muscarinic receptors which stimulates the production of saliva.

In a study of 33 patients with radiation-induced xerostomia, the commercially available Salagen (pilocarpine tablets) was compared to pilocarpine lozenges and placebo. The percentage of the patients who reported an improvement in oral dryness, sore mouth and speaking after having taken 5-mg pilocarpine lozenges was greater than with Salagen tablets. Patients in this study also reported that they preferred the lozenges to the tablets.

Troches/Lozenges vs. Tablets

Why would a doctor prescribe Pilocarpine troches/lozenges instead of an oral tablet? A few benefits of troches include that it is easy to administer, that there is mechanical stimulation of saliva production, there is a longer period of topical contact, and that systemic side effects may be reduced. Note that a troche is the same as a lozenge – troche is often the preferred term in compounding and pharmacy. A troche is meant to dissolve in the mouth and not be swallowed.

Nonpharmacologic Therapies

Various methods are effective for either increasing saliva production or decreasing the sensation of dry mouth that do not require medication. Sipping on water consistently can reduce xerostomia as can sucking on ice chips. This moisturizes the mouth and helps alleviate symptoms without increasing saliva production. Chewing gum can improve the flow of saliva – some that include xylitol specifically are good for reducing dry mouth.

Compounded Pilocarpine Troches

The treatment course for pilocarpine usually should last at least 6-12 weeks because it can take some time for patients to notice an effect. Side effects of the oral form of the drug include excessive sweating, headache, flushing, dizziness, chills, and nausea. Patients may also experience an increase in urinary frequency and gastrointestinal discomfort. For most patients the benefits outweigh the side effects and the side effects will subside when the medication is discontinued.

Even though pilocarpine lozenges are not commercially available, in preliminary studies it has been shown that patients prefer this form of the drug and that it may be more effective than other forms. In a study of 33 patients, the researchers concluded that the “percentage of patients with decreased feeling of oral dryness, sore mouth or speaking difficulties after taking 5-mg pilocarpine lozenge was greater than Salagen or placebo.” Salagen is the commercially available tablet form of the drug (it does not dissolve in the mouth).

Our compounded pilocarpine troche is typically compounded in a 2mg dosage with a prescription. If you have any questions about our formulations or our pharmacy, you can contact us here.

Articles

Efficacy of cevimeline vs. pilocarpine in the secretion of saliva: a pilot study – Special Care in Dentistry

Drug-Induced Dry Mouth – Pharmacy Times

Pilocarpine Tablets for the Treatment of Dry Mouth and Dry Eye Symptoms in Patients With Sjögren SyndromeA Randomized, Placebo-Controlled, Fixed-Dose, Multicenter Trial – JAMA Internal Medicine

Pharmacological interventions for preventing dry mouth and salivary gland dysfunction following radiotherapy – Cochrane Library