Pilocarpine 5mg Tablets
It is used to treat dry mouth.
Drug Class
Sialagogue
Pharmacologic Class
Muscarinic Agonist
Pregnancy Category
Category C
FDA Approved
Jan 1994
DEA Schedule
Not Controlled
Overview
What is this medicine?
Pilocarpine is a medication used to help people who have a very dry mouth, often caused by certain medical conditions like Sjogren's syndrome or radiation treatment for cancer. It works by stimulating your body to produce more saliva, which can make eating, speaking, and swallowing easier.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, it's essential to use it exactly as directed by your doctor. Carefully read all the information provided with your medication and follow the instructions closely. Continue taking your medication as prescribed, even if your symptoms improve.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature in a dry place, avoiding bathrooms. Keep all medications in a secure location, out of the reach of children and pets. Properly dispose of unused or expired medications by throwing them away. However, do not flush them down the toilet or pour them down the drain unless specifically instructed to do so. If you're unsure about the best way to dispose of your medication, consult your pharmacist. You may also want to check if there are drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To get the most benefit from your medication, it's essential to use it exactly as directed by your doctor. Carefully read all the information provided with your medication and follow the instructions closely. Continue taking your medication as prescribed, even if your symptoms improve.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature in a dry place, avoiding bathrooms. Keep all medications in a secure location, out of the reach of children and pets. Properly dispose of unused or expired medications by throwing them away. However, do not flush them down the toilet or pour them down the drain unless specifically instructed to do so. If you're unsure about the best way to dispose of your medication, consult your pharmacist. You may also want to check if there are drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Take pilocarpine with a glass of water.
- You can take it with or without food, but taking it with food might help reduce stomach upset.
- Drink plenty of water throughout the day to help with dry mouth and prevent dehydration.
- Maintain good oral hygiene, including regular brushing, flossing, and dental check-ups.
- Avoid sugary foods and drinks that can worsen dry mouth and increase cavity risk.
- Avoid alcohol and caffeine, as they can contribute to dry mouth.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
5 mg three times daily
Dose Range:
5 - 10 mg
Condition-Specific Dosing:
xerostomia_sjogrens:
5 mg three times daily, may titrate up to 10 mg three times daily if needed and tolerated.
xerostomia_radiation:
5 mg three times daily, may titrate up to 10 mg three times daily if needed and tolerated.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended.
Moderate:
No specific adjustment recommended.
Severe:
Use with caution; consider starting at a lower dose (e.g., 5 mg twice daily) and titrate based on response and tolerability.
Dialysis:
Not well studied; use with caution, monitor for adverse effects.
Hepatic Impairment:
Mild:
No specific adjustment recommended.
Moderate:
Use with caution; consider starting at a lower dose (e.g., 5 mg twice daily) and titrate based on response and tolerability.
Severe:
Use with caution; consider starting at a lower dose (e.g., 5 mg twice daily) and titrate based on response and tolerability.
Pharmacology
Mechanism of Action
Pilocarpine is a direct-acting cholinergic parasympathomimetic agent. It acts as a muscarinic receptor agonist, primarily stimulating M3 muscarinic receptors located on exocrine glands (e.g., salivary, sweat, lacrimal, bronchial glands). This stimulation leads to increased secretion of saliva, sweat, tears, and other exocrine fluids.
Pharmacokinetics
Absorption:
Bioavailability:
Not precisely quantified for oral tablets, but well absorbed.
Tmax:
Approximately 0.75-1.25 hours
FoodEffect:
Food may delay Tmax and decrease Cmax, but does not significantly affect AUC.
Distribution:
Vd:
Not available
ProteinBinding:
Less than 10%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 0.75-1.5 hours
Clearance:
Not available
ExcretionRoute:
Renal (primarily as metabolites, some unchanged drug)
Unchanged:
Approximately 35% (renal excretion)
Pharmacodynamics
OnsetOfAction:
Within 20 minutes
PeakEffect:
Approximately 1 hour
DurationOfAction:
3-5 hours
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high or low blood pressure, including:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
Shortness of breath
Swelling
Abnormal heartbeat (fast, slow, or irregular)
Severe stomach upset or vomiting
Changes in eyesight, eye pain, or severe eye irritation
Excessive tearing
Headache
Excessive sweating
Confusion
Shakiness
Stomach pain
Lower back or side pain
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Dizziness
Fatigue or weakness
Flushing
Mild stomach upset
Frequent urination
Runny nose
Diarrhea
Chills
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high or low blood pressure, including:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
Shortness of breath
Swelling
Abnormal heartbeat (fast, slow, or irregular)
Severe stomach upset or vomiting
Changes in eyesight, eye pain, or severe eye irritation
Excessive tearing
Headache
Excessive sweating
Confusion
Shakiness
Stomach pain
Lower back or side pain
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Dizziness
Fatigue or weakness
Flushing
Mild stomach upset
Frequent urination
Runny nose
Diarrhea
Chills
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Excessive sweating (more than usual)
- Nausea or vomiting
- Diarrhea
- Dizziness or lightheadedness
- Blurred vision or eye pain
- Slow heartbeat
- Difficulty breathing or wheezing
- Severe headache
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Asthma
+ Glaucoma
+ Liver disease
+ Swelling in parts of the eye
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.
To ensure your safety, please provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins you are using
* Any health problems you have
It is vital to verify that it is safe to take this medication with all your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Asthma
+ Glaucoma
+ Liver disease
+ Swelling in parts of the eye
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.
To ensure your safety, please provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins you are using
* Any health problems you have
It is vital to verify that it is safe to take this medication with all your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. When taking this drug, exercise caution when driving or performing tasks that require clear vision, especially at night or in low-light environments. Additionally, be mindful of your body's temperature regulation and hydration levels, particularly in hot weather or during physical activity. To avoid dehydration, it is crucial to drink plenty of fluids. If you experience excessive sweating and are unable to consume sufficient fluids, consult your doctor to discuss strategies for preventing dehydration.
Please note that it may take several weeks for the full effects of this medication to become apparent. If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects. It is also important to discuss your pregnancy status or plans with your doctor, as well as any breastfeeding intentions. Your doctor will help you weigh the benefits and risks of this medication to both you and your baby, ensuring you make an informed decision about your treatment.
Please note that it may take several weeks for the full effects of this medication to become apparent. If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects. It is also important to discuss your pregnancy status or plans with your doctor, as well as any breastfeeding intentions. Your doctor will help you weigh the benefits and risks of this medication to both you and your baby, ensuring you make an informed decision about your treatment.
Overdose Information
Overdose Symptoms:
- Headache
- Nausea
- Vomiting
- Diarrhea
- Abdominal cramps
- Salivation
- Lacrimation (tearing)
- Urinary incontinence
- Diaphoresis (sweating)
- Flushing
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Bronchospasm
- Miosis (constricted pupils)
- Tremor
- Fasciculations (muscle twitching)
- Convulsions
What to Do:
Seek immediate medical attention or call a poison control center (1-800-222-1222). Treatment is supportive and may include atropine as an antidote for severe cholinergic symptoms.
Drug Interactions
Major Interactions
- Anticholinergic agents (e.g., atropine, scopolamine, tricyclic antidepressants, antihistamines): May antagonize the effects of pilocarpine.
- Beta-blockers (e.g., propranolol, metoprolol): Increased risk of bradycardia and bronchospasm due to additive parasympathomimetic effects.
Moderate Interactions
- Drugs that prolong the QT interval: Theoretical risk of additive effect, though pilocarpine itself is not known to prolong QT significantly.
- Other cholinergic agonists (e.g., cevimeline): Additive cholinergic effects, increased risk of adverse events.
Monitoring
Baseline Monitoring
Baseline salivary flow assessment (if applicable)
Rationale: To establish a baseline for evaluating treatment efficacy.
Timing: Prior to initiation of therapy.
Ophthalmologic examination (for patients with narrow-angle glaucoma)
Rationale: Pilocarpine can cause acute angle closure glaucoma in patients with narrow angles.
Timing: Prior to initiation of therapy.
Cardiac history and vital signs (heart rate, blood pressure)
Rationale: Pilocarpine can cause bradycardia and hypotension.
Timing: Prior to initiation of therapy.
Pulmonary history (asthma, COPD)
Rationale: Pilocarpine can cause bronchospasm.
Timing: Prior to initiation of therapy.
Routine Monitoring
Assessment of xerostomia symptoms and salivary output
Frequency: Regularly during follow-up visits (e.g., monthly for first few months, then every 3-6 months)
Target: Improved salivary flow and reduced dry mouth symptoms
Action Threshold: Lack of improvement or worsening symptoms may indicate need for dose adjustment or alternative therapy.
Monitoring for cholinergic side effects (e.g., sweating, nausea, flushing, urinary frequency, blurred vision, bradycardia)
Frequency: Regularly, especially during dose titration and initial therapy
Target: Absence or mild, tolerable side effects
Action Threshold: Persistent or severe side effects may require dose reduction or discontinuation.
Blood pressure and heart rate
Frequency: Periodically, especially in patients with cardiovascular comorbidities
Target: Within normal limits or patient's baseline
Action Threshold: Significant bradycardia or hypotension may require dose adjustment or discontinuation.
Symptom Monitoring
- Increased sweating (diaphoresis)
- Nausea
- Flushing
- Urinary frequency
- Blurred vision
- Headache
- Dizziness
- Diarrhea
- Bradycardia
- Bronchospasm (wheezing, shortness of breath)
Special Patient Groups
Pregnancy
Pilocarpine is Pregnancy Category C. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects at high doses.
Trimester-Specific Risks:
First Trimester:
Potential for adverse effects, but human data are limited. Use only if clearly needed.
Second Trimester:
Potential for adverse effects, but human data are limited. Use only if clearly needed.
Third Trimester:
Potential for adverse effects, but human data are limited. Use only if clearly needed.
Lactation
Pilocarpine is excreted in breast milk in animals. It is not known whether pilocarpine is excreted in human milk. Due to the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Lactation Risk Category L3 (Moderate Risk).
Infant Risk:
Potential for cholinergic effects in the infant (e.g., bradycardia, increased secretions, diarrhea).
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Systemic use is generally not recommended.
Geriatric Use
Elderly patients may be more sensitive to the effects of pilocarpine, particularly cholinergic side effects such as sweating, nausea, and cardiovascular effects. Start with lower doses and titrate carefully, monitoring closely for adverse reactions.
Clinical Information
Clinical Pearls
- Pilocarpine is most effective when some residual salivary gland function remains. It may not be effective in patients with completely destroyed salivary glands.
- The most common side effect is sweating (diaphoresis), which can be dose-dependent. Patients should be advised to stay hydrated.
- Patients should be warned about potential blurred vision, especially at night or in dim light, and advised to use caution when driving or operating machinery.
- Administering pilocarpine with food may help reduce gastrointestinal side effects.
- For patients with Sjogren's syndrome, pilocarpine addresses xerostomia but does not treat the underlying autoimmune disease.
Alternative Therapies
- Cevimeline (another muscarinic agonist for xerostomia)
- Artificial saliva substitutes (e.g., Biotene, Oasis)
- Salivary stimulants (e.g., sugar-free candies, chewing gum)
- Oral moisturizers and rinses
Cost & Coverage
Average Cost:
$20 - $60 per 30 tablets (5mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.