Pilocarpine

What is Pilocarpine?

• Pilocarpine (Salagen) is a cholinergic agonist used to treat symptoms of dry mouth in patients with keratoconjunctivitis sicca (Sjögren syndrome).

Pilocarpine

What are the uses of this medicine?

Pilocarpine (Salagen) is used for:

• the treatment of symptoms of dry mouth from salivary gland hypofunction caused by radiotherapy for cancer of the head and neck
• the treatment of symptoms of dry mouth in patients with Sjogren’s Syndrome.

Pilocarpine Structural Formulae

Pilocarpine molecule ball

How does this medicine work?

• Pilocarpine (pye" loe kar' peen) is a cholinergic agonist that stimulates muscarinic receptors, resulting in an increase in parasympathetic activity.
• Engagement of the cholinergic receptors causes increased secretion from exocrine glands, including sweat, salivary, lacrimal, gastric, pancreatic and intestinal glands, as well as increased tone and motility of smooth muscle cells in the eye, respiratory and gastrointestinal tract.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• uncontrolled asthma
• known hypersensitivity to pilocarpine
• when miosis is undesirable, e.g., in acute iritis and in narrow-angle (angle closure) glaucoma.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• ambenonium (Mytelase)
• antihistamines
• atropine (Motofen, in Lomotil, in Lonox)
• beta blockers such as atenolol (Tenormin), labetalol (Normodyne), metoprolol (Lopressor, Toprol XL), nadolol (Corgard), and propranolol (Inderal)
• bethanechol (Urecholine)
• cevimeline (Evoxac)
• donepezil (Aricept)
• galantamine (Razadyne)
• ipratropium (Atrovent, in Combivent, in Duoneb)
• medications for irritable bowel disease, motion sickness, Parkinson's disease, ulcers, or urinary problems
• neostigmine (Prostigmin)
• physostigmine (Mestinon)
• rivastigmine (Exelon)
• tacrine (Cognex)

Is this medicine FDA approved?

• Pilocarpine for oral use was approved for use in the United States in the 1990s.

How should this medicine be used?

Recommended dosage: In Head & Neck Cancer Patients:

• The recommended initial dose of pilocarpine hydrochloride tablets is 5 mg taken three times a day.
• Dosage should be titrated according to therapeutic response and tolerability.
• The usual dosage range is up to 15 mg per day to 30 mg per day.

In Sjogren’s syndrome Patients:

• The recommended dose of pilocarpine hydrochloride tablets is one tablet (5 mg) taken four times a day.
• Efficacy was established by 6 weeks of use.

Administration:

• Pilocarpine comes as a tablet to take by mouth.
• When pilocarpine is used to treat dry mouth caused by radiotherapy in people who have head and neck cancer, it is usually taken three times a day.
• When pilocarpine is used to treat dry mouth in people who have Sjogren's syndrome, it is usually taken four times a day.
• Take pilocarpine at around the same times every day.
• Your doctor may start you on an average dose of pilocarpine and adjust your dose depending on how well your symptoms are controlled and the side effects you experience.
• Pilocarpine will control your symptoms but will not cure your condition.
• Continue to take pilocarpine even if you feel well.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Each 5 mg pilocarpine hydrochloride tablet for oral administration contains 5 mg of pilocarpine hydrochloride.

This medicine is available in fallowing brand namesː

• Salagen

What side effects can this medication cause?

The most common side effects of this medicine include: In Head & Neck Cancer Patients:

• Sweating
• Nausea
• Rhinitis
• Diarrhea
• Chills
• Flushing
• Urinary Frequency
• Dizziness
• Asthenia

In Sjogren's syndrome Patients:

• Sweating
• Urinary Frequency
• Nausea
• Flushing
• Rhinitis
• Diarrhea
• Chills
• Increased Salivation
• Asthenia

What special precautions should I follow?

• Patients should be informed that pilocarpine may cause visual disturbances, especially at night, that could impair their ability to drive safely.
• If a patient sweats excessively while taking pilocarpine hydrochloride and cannot drink enough liquid, the patient should consult a physician. Dehydration may develop. Be sure to drink plenty of water and call your doctor right away if you are having difficulty drinking enough fluid or if you think you may be dehydrated.
• Pilocarpine should be administered with caution to patients with known or suspected cholelithiasis or biliary tract disease.
• It is not known whether this drug is excreted in human milk.
• Pilocarpine toxicity is characterized by an exaggeration of its parasympathomimetic effects. These may include: headache, visual disturbance, lacrimation, sweating, respiratory distress, gastrointestinal spasm, nausea, vomiting, diarrhea, atrioventricular block, tachycardia, bradycardia, hypotension, hypertension, shock, mental confusion, cardiac arrhythmia, and tremors.
• Pilocarpine should be administered with caution in and under close medical supervision of patients with significant cardiovascular disease.
• Pilocarpine has been reported to increase airway resistance, bronchial smooth muscle tone, and bronchial secretions. Pilocarpine hydrochloride should be administered with caution to and under close medical supervision in patients with controlled asthma, chronic bronchitis, or chronic obstructive pulmonary disease.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• headache
• difficulty breathing
• GI spasm
• confusion
• tearing of eyes
• uncontrollable shaking of a part of the body

Management of overdosage:

• Overdosage should be treated with atropine titration (0.5 mg to 1 mg given subcutaneously or intravenously) and supportive measures to maintain respiration and circulation.
• Epinephrine (0.3 mg to 1 mg, subcutaneously or intramuscularly) may also be of value in the presence of severe cardiovascular depression or bronchoconstriction.
• It is not known if pilocarpine is dialyzable.

Can this medicine be used in pregnancy?

• Pregnancy Category C.
• There are no adequate and well-controlled studies in pregnant women.
• Pilocarpine hydrochloride tablets should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredients:

• PILOCARPINE HYDROCHLORIDE

Inactive Ingredients:

• CELLULOSE, MICROCRYSTALLINE
• SILICON DIOXIDE
• STEARIC ACID
• HYPROMELLOSES
• POLYDEXTROSE
• TITANIUM DIOXIDE
• TRIACETIN
• POLYETHYLENE GLYCOL, UNSPECIFIED

Who manufactures and distributes this medicine?

Manufactured by:

• Amneal Pharmaceuticals of NY, LLC
• Brookhaven, NY

Distributed by:

• Amneal Pharmaceuticals LLC
• Bridgewater, NJ

What should I know about storage and disposal of this medication?

• Store at 20° to 25°C (68° to 77°F).
• Dispense in a tightly-closed, light-resistant container (USP).

Sjögren Syndrome Agents

• Cholinergic Agents
  • Cevimeline
  • Pilocarpine

• Dailymed label info on Pilocarpine
• FDA Pilocarpine