Detailed Drug Information:

DRUG CLASS AND MECHANISM: Pilocarpine is a "cholinergic" drug, that is, a drug that mimics the effects of the chemical, acetylcholine which is produced by nerve cells. Acetylcholine serves as a messenger between nerve cells and between nerve cells and the organs they control. For example, acetylcholine is responsible for causing the salivary glands to make saliva and the lacrimal glands to make tears to lubricate the eyes.

In addition to its effects on the salivary and lacrimal glands, acetylcholine controls the production of fluid within the eye, and pilocarpine eye drops have been used to treat glaucoma for many years. In 1994, an oral formulation of pilocarpine was approved by the FDA for the treatment of dry mouth caused by radiation therapy for head and neck cancer, a treatment that damages the salivary glands and reduces their production of saliva. In 1998, the oral preparation was approved for the management of Sjogren's syndrome, an autoimmune disease that damages the salivary and lacrimal glands. Piloca pilocarpine was first isolated from the leaves of Pilocarpus microphyllus (also called jaborandi) in 1875.

PREPARATIONS: Tablets, 5mg; 7.5mg.

STORAGE: Tablets should be stored at room temperature, 15-30°C (59-86°F).

PRESCRIBED FOR: Oral pilocarpine is used to treat dry mouth caused by Sjogren's syndrome and radiation therapy to the head and neck.

DOSING: Oral pilocarpine usually is taken three or four times daily. The maximum effect occurs in approximately one hour but may occur later if it is taken with food. The effects last three to five hours.

DRUG INTERACTIONS: Medications possessing anticholinergic effects or side effects should not be used with pilocarpine since they will counter pilocarpine's cholinergic effects. Such medications include atropine, e.g., Lomotil; some antihistamines, e.g., carbinoxamine (Cardec-DM, Rondec-D), clemastine (Tavist), diphenhydramine (Benadryl), promethazine (Phenergan), trimeprazine (Temaril); some phenothiazines, e.g., mesoridazine(Serentil), promazine (Sparine), thioridazine (Mellaril), triflupromazine (Vesprin)]; clozapine (Clozaril), cyclobenzaprine (Flexeril), disopyramide Norpace); some antidepressants, e.g., amitriptyline (Elavil), amoxapine (Asendin), bupropion (Wellbutrin; Zyban), clomipramine (Anafranil), doxepin (Sinequan), maprotiline (Ludiomil), and protriptyline (Vivactil).

PREGNANCY: The safety of oral pilocarpine during pregnancy has not been evaluated. The physician and patient need to weigh the benefits and the unknown risk to the fetus before using pilocarpine during pregnancy.

NURSING MOTHERS: It is not known if pilocarpine is secreted in human breast milk in amounts large enough to affect the nursing infant.

SIDE EFFECTS: Excessive sweating (diaphoresis) is a frequent side effect of pilocarpine. Other side effects include chills, dizziness, excessive tearing, flushing, voice change, stuffy nose, tremor, increased need to urinate, visual disturbances, diarrhea, difficulty swallowing, abdominal pain, nausea, vomiting, and slow heart rate.