Salagen (Pilocarpine) - Oral

What Is Salagen?

Salagen (pilocarpine) is a prescription drug used to alleviate the symptoms of xerostomia (dry mouth) due to saliva gland damage from radiation for head and neck cancer or dry mouth symptoms from Sjögren’s syndrome. It is used in adults 18 and older.

Pilocarpine is a cholinergic agonist, also called a cholinergic drug. It mimics the action of a chemical called acetylcholine.

Acetylcholine helps control muscle contraction, including muscles in your eye. It also helps regulate blood pressure and heart rate and stimulates secretions by certain glands, including salivary glands–essential in treating dry mouth.

Salagen is a prescription product, so you can’t purchase it over-the-counter (OTC). Instead, you’ll need a prescription for it from your healthcare provider and will buy it from your local pharmacy.

Salagen is available in the form or oral tablets to be taken by mouth.

What Is Salagen Used For?

Salagen is approved by the Food and Drug Administration (FDA) to treat the following:

• Xerostomia, or dry mouth, is caused by radiation used to treat head and neck cancer. Radiation aims to stop the production of cancer cells but can harm healthy cells, such as those in your salivary glands that normally produce saliva, and prevent your mouth from drying out too much.
• Xerostomia is caused by Sjögren's syndrome, an autoimmune condition that causes joint pain, dry eyes, and dry mouth, in addition to other effects on the body.

The key ingredient, pilocarpine, is also available as an ophthalmic solution, or eye drop, under the brand name Vuity. Pilocarpine is also approved to treat the following conditions but would be treated with Vuity, or generic pilocarpine eye drops rather than Salagen tablets:

• Presbyopia, which is farsightedness or a loss of close-up vision
• Raised intraocular pressure, or pressure inside the eye that is too high, is caused by angle-closure or open-angle glaucoma (a group of diseases that cause damage to the optic nerve)
  

How to Take Salagen

You can take Salagen tablets with or without food. The tablets usually have to be taken multiple times a day, often three or four. It can help to set phone reminders at regular intervals throughout your day, so you don’t accidentally miss doses.

Swallow the tablets whole. Do not crush, cut, or chew them.

Storage

Store Salagen at room temperature (between 59-86 degrees F), out of reach of children and pets. Avoid storing it in an area with a lot of heat and moisture, like the bathroom.

If you’re traveling by plane, you’ll want to keep Salagen in your carry-on luggage so that you aren’t separated from it in case your checked luggage goes missing.

If you’re traveling by car, take care not to leave your medicine in especially hot or cold temperatures for long periods of time, like overnight in the car.

Off-Label Uses

Pilocarpine is approved by the FDA to treat dry mouth of different causes as well as certain eye conditions. However, medications are sometimes used in non-approved conditions based on clinical experience and expert knowledge.

Pilocarpine has been shown to prevent mucositis following chemotherapy treatment. Mucositis is when the inside of your mouth feels sore and painful.

What Are the Side Effects of Salagen?

This is not a complete list of side effects, and others may occur. A healthcare provider can advise you on side effects. If you experience other effects, contact your pharmacist or a healthcare provider. You may report side effects to the FDA at fda.gov/medwatch or 1-800-FDA-1088.

Common Side Effects

While most side effects studied in Salagen clinical trials went away within hours of stopping taking Salagen, common side effects associated with the drug include:

• Hyperhidrosis (excessive sweating, due to the way pilocarpine stimulates your sweat glands in addition to salivary glands)
• Headache
• Nausea
• Rhinitis (allergic-like symptoms such as runny or stuffy nose and sneezing)
• Vasodilation (a widening of the blood vessels which may result in flushing, a reddening of the face and neck, and a warm or burning sensation)
• Polyuria (frequent urination)
  

Severe Side Effects

Side effects that were found to be rarer in Salagen clinical trials yet potentially more serious include:

• Heart effects such as hypotension (low blood pressure), hypertension (high blood pressure), bradycardia (slow heart rate), and tachycardia (fast heart rate), especially in people with prior heart conditions
• Dyspepsia or indigestion, as pilocarpine may cause increased stomach acid secretion
• Urinary tract infection (UTI; common infections that happen when bacteria, often from the skin or rectum, enter the urethra and infect the urinary tract)
• Vaginitis (inflammation or infection of the vagina)

Call your healthcare provider right away if you feel like you are experiencing serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency.

Dosage: How Much Salagen Should I Take?

Modifications

Users should be made aware of the following before beginning Salagen:

In pregnancy and breastfeeding: It's uncertain whether Salagen poses a risk in human pregnancy or if pilocarpine hydrochloride (the primary ingredient in Salagen) is excreted (expelled as waste) in human breast milk.

As such, Salagen should only be used during the pregnancy period or during nursing sessions only if the expected benefits outweigh the potential risks to the fetus or infant child. Speak with your healthcare provider about whether the benefits of Salagen are any risk it may pose to your pregnancy.

In pediatrics: The safety and effectiveness of Salagen in children under 18 have not been established. Therefore, this drug is recommended only for those older than 18 who meet all other benchmarks for prescription.

In older adults: Clinical trials for Salagen showed that the rate of pilocarpine absorption into the bloodstream was similar when comparing older adults to younger men.

However, in five healthy, older female volunteers, the mean Cmax (the highest concentration of a drug in the blood) and AUC (area under the curve; meaning the extent of exposure to a drug and its clearance rate from the body) was approximately twice that of older males and young normal male volunteers.

Be sure to discuss with your healthcare provider how your age may impact your ability to tolerate Salagen.

In hepatic impairment: If you have a hepatic impairment, or decreased liver function, you should start taking Salagen at a slightly lower dose and gradually increase your dose as tolerated. Clearing of the drug was seen to be slower in people with mild to moderate liver impairment.

Missed Dose

If you forget to take a dose of Salagen, just wait and take your next dose at the regularly scheduled time. Do not double up your dose or take a second tablet to make up for your missed dose.

Overdose: What Happens If I Take Too Much Salagen?

Cases of overdose have been reported with Salagen, and symptoms were mostly consistent with the known side effects of the drug, such as excessive sweating and gastrointestinal (GI) side effects.

Treatment for moderate overdosage would be generally keeping you well, such as giving intravenous (IV) hydration. If you are experiencing severe overdose symptoms, you may need treatment with atropine, the antidote to pilocarpine.

Precautions

What Are Reasons I Shouldn't Take Salagen?

Salagen is not appropriate for everyone. You should not take this medication if you are allergic to pilocarpine or any of the inactive ingredients in Salagen.

Salagen may be used with caution in some people only if the healthcare provider determines it is safe. Salagen is not or may not be the best choice for you if you:

• Have a known hypersensitivity or allergy to Salagen.
• Have uncontrolled heart disease, as your body may be unable to handle the effects of pilocarpine, such as hypotension, hypertension, bradycardia, and tachycardia.
• Have active peptic ulcer disease since pilocarpine may cause increased acid secretion.
• Have uncontrolled asthma, as cholinergic drugs may cause bronchoconstriction and decreased airflow.
  

What Other Medications May Interact With Salagen?

There are some drugs that can interact with Salagen and should be monitored by your healthcare provider.

Examples of drugs that may potentially interact with Salagen include:

• Anticholinergic drugs (medications that block the action of acetylcholine, a type of neurotransmitter) may counteract their effects with Salagen, a cholinergic drug. Examples of anticholinergic drugs include Bentyl (dicyclomine), Levsin (hyoscyamine), and Lomotil (atropine/diphenoxylate).
• CYP2A6 substrates may build up in your body and have their actions and side effects amplified if taken with Salagen since pilocarpine can block the protein that clears these drugs. Examples may include Tegafur (5-fluorouracil), Femara (letrozole), Atripla (contains efavirenz), Depakote (valproic acid), and caffeine.
  

What Medications Are Similar to Salagen?

Other cholinergic agonist medications used to treat a variety of conditions include:

• Provocholine (methacholine)
• Miostat (carbachol)
• Bethanechol
• Exelon (rivastigmine)
• Aricept (donepezil)
• Galantamine

This is not a list of drugs recommended to take with Salagen. Ask your healthcare provider if you have questions.

How Can I Stay Healthy While Taking Salagen?

Conditions caused by an overactive immune system–autoimmune diseases–are difficult to understand because our immune systems are so complicated. Of course, dealing with a cancer diagnosis and undergoing radiation treatment comes with a huge set of challenges.

Sjögren’s syndrome and radiation treatment both have profound impacts on your everyday life, and can cause symptoms that affect multiple parts of your body. It can be hard to work efficiently or enjoy things you normally do when you’re experiencing joint pain or dryness in areas like your eyes, nose, and mouth.

Sjögren’s syndrome is a very common autoimmune disease, affecting around 4 million Americans, predominantly women over 40. It can be hard to diagnose, given that symptoms may come and go and seem unrelated. Be sure to let your healthcare provider know any symptoms you are experiencing to help them make an accurate diagnosis.

Symptoms like dry mouth and dry eyes are some of the most common ones and can be some of the most uncomfortable parts of Sjögren’s, as well as a couple of examples of the many unpleasant side effects of radiation treatment. Fortunately, mouthwashes, lip balms, saliva substitutes, and gum can help relieve your dry mouth in addition to medicines like Salagen. At-home remedies like a humidifier may also help dryness in your eyes, nose, and mouth.

Working with your healthcare provider to come up with a treatment plan and sticking to it while prioritizing your mental, emotional and physical self-care can help you live as normal a life as possible with Sjögren’s syndrome or while receiving cancer radiation treatment.