General Information

Salagen (pilocarpine HCl) is a cholinergic agonist.

Salagen is specifically indicated for:

the treatment of symptoms of dry mouth from salivary gland hypofunction caused by radiotherapy for cancer of the head and neck

the treatment of symptoms of dry mouth in patients with Sjogren's syndrome

Salagen is suppled as tablets. The recommended dose is as follows:

Head & Neck Cancer Patients:

The recommended initial dose of Salagen Tablets is 5 mg taken three times a day. Dosage should be titrated according to therapeutic response and tolerability. The usual dosage range is 15-30 mg per day. (Not to exceed 10 mg per dose.) Although early improvement may be realized, at least 12 weeks of uninterrupted therapy with Salagen Tablets may be necessary to assess whether a beneficial response will be achieved. The incidence of the most common adverse events increases with dose. The lowest dose that is tolerated and effective should be used for maintenance.

Sjogren's Syndrome Patients:

The recommended dose of Salagen Tablets is one tablet (5 mg) taken four times a day. Efficacy was established by 6 weeks of use.

Mechanism of Action

Pilocarpine is a cholinergic parasympathomimetic agent exerting a broad spectrum of pharmacologic effects with predominant muscarinic action. 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.

Clinical Trial Results

Head & Neck Cancer Patients:

A 12 week randomized, double-blind, placebo controlled study in 207 patients (142 men, 65 women) was conducted in patients whose mean age was 58.5 years with a range of 19 to 77; the racial distribution was Caucasian 95%, Black 4%, and other 1%. In this population, a statistically significant improvement in mouth dryness occurred in the 5 and 10 mg Salagen Tablet treated patients compared to placebo treated patients. The 5 and 10 mg treated patients could not be distinguished.

Another 12 week, double-blind, randomized, placebo-controlled study was conducted in 162 patients whose mean age was 57.8 years with a range of 27 to 80; the racial distribution was Caucasian 88%, Black 10%, and other 2%. The effects of placebo were compared to 2.5 mg three times a day of Salagen Tablets for 4 weeks followed by adjustment to 5 mg three times a day and 10 mg three times a day. Lowering of the dose was necessary because of adverse events in 3 of 67 patients treated with 5 mg of Salagen Tablets and in 7 of 66 patients treated with 10 mg of Salagen Tablets. After 4 weeks of treatment, 2.5 mg of Salagen Tablets three times a day was comparable to placebo in relieving dryness. In patients treated with 5 mg and 10 mg of Salagen Tablets, the greatest improvement in dryness was noted in patients with no measurable salivary flow at baseline. In both studies, some patients noted improvement in the global assessment of their dry mouth, speaking without liquids, and a reduced need for supplemental oral comfort agents.

Sjogren's Syndrome Patients:

Two separate studies were conducted in patients with primary or secondary Sjogren's Syndrome. A 12-week, randomized, double-blind, parallel-group, placebo-controlled study was conducted in 256 patients (14 men, 242 women) whose mean age was 57 years with a range of 24 to 85 years. The racial distribution was as follows: Caucasian 91%, Black 6%, and other 3%. The effects of placebo were compared with those of Salagen tablets 5 mg four times a day (20 mg/day) for 6 weeks. At 6 weeks, the patients’ dosage was increased from 5 mg Salagen Tablets q.i.d. to 7.5 mg q.i.d. The data collected during the first 6 weeks of the trial were evaluated for safety and efficacy, and the data of the second 6 weeks of the trial were used to provide additional evidence of safety. After 6 weeks of treatment, statistically significant global improvement of dry mouth was observed compared to placebo.