Shocking Diseases of the Mouth

What is pilocarpine, and how does it work (mechanism of action)?

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.

What brand names are available for pilocarpine?

Salagen

Is pilocarpine available as a generic drug?

GENERIC AVAILABLE: Yes

Do I need a prescription for pilocarpine?

Yes

What are the side effects of pilocarpine?

Excessive sweating (diaphoresis) is a frequent side effect of pilocarpine. Other side effects include:

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What is the dosage for pilocarpine?

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.

Which drugs or supplements interact with pilocarpine?

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).

Is pilocarpine safe to take if I'm pregnant or breastfeeding?

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.

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

What else should I know about pilocarpine?

What preparations of pilocarpine are available?

Tablets: 5 and 7.5 mg.

How should I keep pilocarpine stored?

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

Reference: FDA Prescribing Information

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Summary

Pilocarpine (Salagen) is a medication prescribed for the treatment of dry mouth caused by Sjogren's syndrome, and radiation to the neck and head. Side effects, drug interactions, and dosing information should be reviewed prior to taking this medication.

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See more info: pilocarpine on RxList
Reviewed on 9/14/2015
References
Reference: FDA Prescribing Information

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