Pilocarpine is a medication that belongs to a class of drugs known as cholinergic agonists. It is commonly used in the form of pilocarpine eye drops to treat increased eye pressure in conditions like glaucoma and ocular hypertension. By helping fluid drain from the eye, it reduces intraocular pressure and protects vision.

In addition to eye conditions, pilocarpine tablets are prescribed for dry mouth, particularly in patients who have undergone radiation therapy or have Sjgren s syndrome. The tablets stimulate saliva production and provide relief from dryness.

Whether used as pilocarpine 5 mg oral doses or as eye drops, this medicine is known for its targeted action and reliable results in restoring moisture or reducing eye pressure. When used as directed, it offers significant symptom relief with a well-understood safety profile.

What Is Pilocarpine?

Pilocarpine is a cholinergic medication that mimics the effects of acetylcholine, a chemical messenger in the body. It is used to treat dry mouth caused by radiation therapy for head and neck cancer and Sjgren's syndrome, an autoimmune disease that affects salivary and lacrimal glands.

Pilocarpine Uses

Pilocarpine treats dry mouth symptoms due to:

  • Sjgren's syndrome
  • Radiation therapy for head/neck cancer

Secondary or Off-Label Uses of Pilocarpine

  • Used off-label to improve saliva flow in patients with certain neurological conditions affecting the salivary glands.
  • Sometimes prescribed to manage dry eye symptoms in patients unresponsive to conventional treatments.
  • May be considered in rare cases to reverse drug-induced pupil dilation (mydriasis).
  • Explored for use in night vision enhancement due to its ability to constrict pupils.

It works by stimulating nerves to increase saliva production, making it easier to speak and swallow.

How Does Pilocarpine Work?

Pilocarpine works by mimicking a natural chemical in the body called acetylcholine, which is part of the parasympathetic nervous system. It activates certain receptors (muscarinic receptors) in the body, especially in the eyes and salivary glands.

In the eyes, this action causes the pupil to constrict and helps fluid drain out, reducing intraocular pressure helpful in conditions like glaucoma. When used in the mouth, such as through pilocarpine tablets, it'stimulates the salivary glands to produce more saliva, relieving dry mouth.

Pilocarpine does not interact directly with hormones but acts through the nervous system by enhancing nerve signals that trigger natural body functions like tear or saliva production.

Pilocarpine Dosage

The dosage of pilocarpine depends on the condition being treated and the form of the medication. For dry mouth, pilocarpine 5 mg tablets are commonly prescribed up to four times a day. For glaucoma, pilocarpine eye drops are usually applied to the affected eye(s) up to four times daily, as directed by a doctor.

What Should I Do If I Miss a Dose?

If you miss a dose, take it as soon as you remember. If it's almost time for your next dose, skip the missed one and resume your regular schedule. Do not double the dose to make up for a missed one.

What Happens If There Is an Overdose?

An overdose of pilocarpine may cause symptoms such as sweating, nausea, vomiting, slow heartbeat, difficulty breathing, or low blood pressure. Overuse of eye drops can also lead to excessive pupil constriction and blurred vision. If you suspect an overdose, seek immediate medical attention.

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Pilocarpine Side Effects

Side effects from pilocarpine occur due to its stimulation of parasympathetic nervous system functions. Overactivation can lead to excessive gland secretion (e.g., sweat, saliva, tears) and smooth muscle stimulation, causing symptoms like urination or GI discomfort.

Common Side Effects

Serious Side Effects

  • Change in vision
  • Irregular heartbeat
  • Blurred vision

Most people do not experience serious side effects. Consult your doctor if you experience any of the above serious side effects

Precautions and Warnings

Before taking Pilocarpine, inform your doctor if you have:

  • Allergies to medications
  • Breathing problems
  • Glaucoma
  • Night blindness
  • Acute iritis
  • Heart disease
  • Low or high blood pressure
  • Liver problems
  • Gall bladder disease
  • Kidney stones
  • Stomach problems
  • Pregnancy: The effects of pilocarpine during pregnancy are not well-studied. Discuss potential risks and benefits with your doctor.
  • Diabetes: Pilocarpine can increase blood sugar levels.
  • Breastfeeding: It is unclear if pilocarpine is secreted in significant amounts in breast milk. Consult your doctor before use.

Possible Interactions with Other Medications (Drug Interactions)

Pilocarpine may interact with certain medications, potentially altering their effects or increasing side effects. Common interactions include:

  • Beta-blockers may increase risk of slow heart rate or low blood pressure
  • Cholinergic drugs can amplify side effects like sweating or stomach cramps
  • Anticholinergic drugs may reduce the effectiveness of pilocarpine

Supplements and Herbal Products

There are no widely reported serious interactions with herbal products or supplements, but it's best to consult a doctor before combining pilocarpine with other remedies.

How Should Pilocarpine Be Stored?

  • Store at room temperature, between 15°C to 25°C (59°F to 77°F)
  • Keep the bottle tightly closed and protect from light and moisture
  • Do not freeze or refrigerate unless specifically advised by a pharmacist

What Happens If Pilocarpine Is Not Stored Properly?

Improper storage can reduce the effectiveness of pilocarpine injection amd tablets may cause the medication to degrade. Avoid exposure to extreme temperatures, and keep it out of reach of children.

Pilocarpine vs Atropine

Pilocarpine Atropine
Cholinergic agonist increases saliva production by stimulating nerves Antimuscarinic/anticholinergic, naturally extracted from belladonna
Treats dry mouth due to Sjögren's syndrome or radiation therapy Used before eye examinations and for certain eye conditions
Common Side Effects:
Sweating, nausea, runny nose, diarrhea, chills, frequent urination
Common Side Effects:
Dry mouth, blurred vision, sensitivity to light, lack of sweating, dizziness

Reference

Effect of poloxamer 407 gel on the miotic activity of pilocarpine nitrate in rabbits - ScienceDirect
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Frequently Asked Questions

In order to facilitate aqueous humour outflow, Pilocarpine contracts the ciliary muscle, causing increased tension on the scleral spur and opening the trabecular meshwork spaces.

Pilocarpine is used in people with head and neck cancer to treat dry mouth caused by radiotherapy, and in people with Sjogren's syndrome to treat dry mouth (a condition that affects the immune system and causes dryness of certain parts of the body such as the eyes and mouth).

This medicine can also be used during some eye operations to counteract the effects of medications used to enlarge the pupil (e.g., during an eye exam). Pilocarpine medications work by forcing the pupil of the eye to shrink by reducing the amount of fluid inside the eye.

Pilocarpine is part of a class of medications referred to as cholinergic agonists. Pilocarpine tablet can increase the amount of saliva you produce by stimulating certain nerves, making it easier and more comfortable to speak and swallow.

Paradoxical effects on the cardiovascular system may be present with pilocarpine. Paradoxical is the anticipated effect of a muscarinic agonist, but Pilocarpine administration may produce hypertension after a brief episode of hypotension.

Take your doses directly after a meal and be sure to take the last dose of the day with your evening meal. If you have Sjögren's syndrome, the usual dose if you are taking pilocarpine is one tablet 3-4 times a day.


Disclaimer: The information provided is accurate and up-to-date to the best of our knowledge. However, it should not be considered a substitute for medical advice or consultation. We do not guarantee its completeness or accuracy. The absence of specific warnings does not mean a medicine is safe for all users. We are not responsible for any outcomes based on this information and strongly recommend consulting a doctor for any medical concerns or questions.

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