pilocarpine, Salagen

GENERIC NAME: pilocarpine oral


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 reduces the production of fluid within the eye. Pilocarpine eye drops have been used for many years to treat glaucoma, a condition in which pressure within the fluid of the eye is abnormally elevated and ultimately damages the eye and impares vision. 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 Sjögren's syndrome, an autoimmune disease that damages the salivary and lacrimal glands. Pilocarpine was first isolated from the leaves of Pilocarpus microphyllus (also called jaborandi) in 1875.



PREPARATIONS: Tablets: 5 and 7.5 mg.

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

PRESCRIBED FOR: Oral pilocarpine is used to treat dry mouth due to lack of saliva (xerostomia) caused by Sjögren's syndrome and radiation therapy to the head and neck.

DOSING: Oral pilocarpine usually is taken three or four times daily. The recommended dose for radiation induced xerostomia is 5 to 10 mg three times daily.

The dose for xerostomia associated with Sjögren's syndrome is 5 mg 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 that have anticholinergic effects should not be used with pilocarpine since they will counter pilocarpine's cholinergic effects. Such medications include atropine, for example, Lomotil; some antihistamines,for example, diphenhydramine (Benadryl), promethazine (Phenergan)], and trimeprazine (Temaril); some phenothiazines, for example, mesoridazine (Serentil), promazine (Sparine), thioridazine (Mellaril), and triflupromazine (Vesprin); some antidepressants, for example, amitriptyline (Elavil, Endep), amoxapine (Asendin), bupropion (Wellbutrin; Zyban), clomipramine (Anafranil), doxepin (Sinequan), maprotiline (Ludiomil), and protriptyline (Vivactil) as well as clozapine (Clozaril), cyclobenzaprine (Flexeril), and disopyramide (Norpace).

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.

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