- What is pilocarpine, and how does it work (mechanism of action)?
- What brand names are available for pilocarpine?
- Is pilocarpine available as a generic drug?
- Do I need a prescription for pilocarpine?
- What are the side effects of pilocarpine?
- What is the dosage for pilocarpine?
- Which drugs or supplements interact with pilocarpine?
- Is pilocarpine safe to take if I'm pregnant or breastfeeding?
- What else should I know about pilocarpine?
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 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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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.
Related Disease Conditions
Sjögren's syndrome is an autoimmune disease involving the abnormal production of extra antibodies that attack the glands and...
Glaucoma is a common eye condition in which the fluid pressure inside the eye rises because of slowed fluid drainage from the...
Dry Mouth (Xerostomia)
Dry mouth is a common side effect of many prescription and non-prescription drugs and certain medical conditions. Symptoms of dry...
Retinal detachment is the separation of the retina from its attachments to the underlying eye tissue. Symptoms of retinal...
Head and Neck Cancer
Head and neck cancer is cancer of the oral cavity, salivary glands, paranasal sinuses and nasal cavity, pharynx, larynx, or lymph...
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Drug InteractionsDrug interactions occur frequently. Get facts about the types of drug interactions, what substances or other things that may interact with drugs such as OTC drug and prescription drugs, vitamins, food(s) (grapefruit), and laboratory tests. Find out how to protect yourself from potential drug interactions.
Drugs: What You Should Know About Your DrugsImportant information about your drugs should be reviewed prior to taking any prescription drug. Side effects, drug interactions, warnings and precauctions, dosage, what the drug is used for, what to do if you miss a dose, how the drug is to be stored, and generic vs. brand names.
Dry MouthDry mouth is a common side effect of many prescription and non-prescription drugs and certain medical conditions. Symptoms of dry mouth include a sticky, dry feeling in the mouth, frequent thirst, sores in the mouth; sores or split skin at the corners of the mouth, cracked lips, a dry feeling in the throat, a burning or tingling sensation in the mouth, and a dry, red, raw tongue.
GlaucomaGlaucoma is a common eye condition in which the fluid pressure inside the eye rises because of slowed fluid drainage from the eye. If untreated, glaucoma may damage the optic nerve and other parts of the eye, causing the loss of vision or even blindness.
Head and Neck CancerHead and neck cancer is cancer of the oral cavity, salivary glands, paranasal sinuses and nasal cavity, pharynx, larynx, or lymph nodes in the upper part of the neck. These cancers account for 3% to 5% of cancers in the U.S. Tobacco and alcohol use are important risk factors. Treatment may involve surgery, radiation therapy, and/or chemotherapy.
Radiation TherapyRadiation therapy is a cancer-fighting technique. In radiation therapy, a radiation oncologist uses high-energy rays to kill cancer cells and stop them from growing and dividing. The two types of radiation therapy are external and internal. Potential side effects of radiation therapy include:
- skin redness,
- permanent pigmentation,
- diarrhea, and
- a reduction in white blood cells.
Retinal DetachmentRetinal detachment is the separation of the retina from its attachments to the underlying eye tissue. Symptoms of retinal detachment include flashing lights and floaters. Highly nearsighted young adults and those who've had cataract surgery are at higher risk for retinal detachment.
Sjogren's SyndromeSjögren's syndrome is an autoimmune disease involving the abnormal production of extra antibodies that attack the glands and connective tissue. Sjögren's syndrome with gland inflammation (resulting dry eyes and mouth, etc.) that is not associated with another connective tissue disease is referred to as primary Sjögren's syndrome. Sjögren's syndrome that is also associated with a connective tissue disease, such as rheumatoid arthritis, systemic lupus erythematosus, or scleroderma, is referred to as secondary Sjögren's syndrome. Though there is no cure for Sjögren's syndrome, the symptoms may be treated by using lubricating eye ointments, drinking plenty of water, humidifying the air, and using glycerin swabs. Medications are also available to treat dry eye and dry mouth.