Pilocarpine 7.5mg Tablets
It is used to treat dry mouth.
Drug Class
Sialagogue; Cholinergic agonist
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 your body produce more saliva to relieve dry mouth, often caused by certain medical conditions like Sjogren's syndrome or radiation therapy to the head and neck. It works by stimulating your salivary glands.
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. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, consult with your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs 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. Avoid taking two doses at the same time or taking extra doses, as this can increase the risk of adverse effects.
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. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, consult with your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs 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. Avoid taking two doses at the same time or taking extra doses, as this can increase the risk of adverse effects.
Lifestyle & Tips
- Maintain good oral hygiene.
- Drink plenty of water throughout the day.
- Avoid caffeine, alcohol, and sugary drinks.
- Use sugar-free candies or gum to stimulate saliva.
- Consider using over-the-counter saliva substitutes or oral moisturizers as needed.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
5 mg three times daily
Dose Range:
5 - 10 mg
Condition-Specific Dosing:
xerostomia_sjogrens_syndrome:
Initial 5 mg three times daily, titrate up to 10 mg three times daily if needed and tolerated. Maximum 30 mg/day.
xerostomia_radiation_therapy:
Initial 5 mg three times daily, titrate up to 10 mg three times daily if needed and tolerated. Maximum 30 mg/day.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended, but use with caution and monitor for adverse effects.
Moderate:
No specific dose adjustment recommended, but use with caution and monitor for adverse effects.
Severe:
Not available
Dialysis:
Not available
Hepatic Impairment:
Mild:
No specific dose adjustment recommended, but use with caution and monitor for adverse effects.
Moderate:
No specific dose adjustment recommended, but use with caution and monitor for adverse effects.
Severe:
Not available
Pharmacology
Mechanism of Action
Pilocarpine is a cholinergic parasympathomimetic agent that acts as a direct muscarinic receptor agonist. It stimulates muscarinic receptors, primarily M3, located on exocrine glands (e.g., salivary, sweat, lacrimal glands), leading to increased secretion of saliva, sweat, and tears.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 50%
Tmax:
0.8-1.5 hours
FoodEffect:
High-fat meal delays Tmax by 2 hours and reduces Cmax by 30%, but AUC is not significantly affected.
Distribution:
Vd:
2.1 L/kg
ProteinBinding:
<20%
CnssPenetration:
Limited
Elimination:
HalfLife:
0.76 hours
Clearance:
0.92 L/kg/hr
ExcretionRoute:
Renal (urine)
Unchanged:
Approximately 35%
Pharmacodynamics
OnsetOfAction:
20 minutes
PeakEffect:
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
+ 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
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
+ 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
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 that is bothersome or leads to dehydration
- Severe dizziness or lightheadedness
- Blurred vision or eye pain
- Chest pain or shortness of breath
- Severe nausea, vomiting, or diarrhea
- Slow or irregular heartbeat
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 with your doctor.
Additionally, provide your doctor and pharmacist with a comprehensive list of all the medications you are taking, including:
Prescription medications
Over-the-counter (OTC) medications
Natural products
Vitamins
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 with your doctor.
Additionally, provide your doctor and pharmacist with a comprehensive list of all the medications you are taking, including:
Prescription medications
Over-the-counter (OTC) medications
Natural products
Vitamins
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, as it may affect your eyesight. Additionally, be careful when driving at night or engaging in activities in low-light environments. In hot weather or during physical activity, it is crucial to stay hydrated by drinking plenty of fluids to prevent fluid loss. If you experience excessive sweating and are unable to consume sufficient fluids, consult your doctor to avoid dehydration. Please note that it may take several weeks to experience the full effects of this medication. If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects. If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor to discuss the potential benefits and risks to you and your baby.
Overdose Information
Overdose Symptoms:
- Cholinergic crisis symptoms: excessive sweating, salivation, lacrimation (tearing), miosis (pinpoint pupils), nausea, vomiting, diarrhea, abdominal cramps, bradycardia (slow heart rate), hypotension (low blood pressure), bronchospasm (difficulty breathing), muscle tremors, weakness, seizures.
What to Do:
Call 911 or Poison Control (1-800-222-1222) immediately. Treatment is supportive; atropine may be used as an antidote.
Drug Interactions
Major Interactions
- Anticholinergic agents (e.g., atropine, scopolamine, tricyclic antidepressants, antihistamines)
- Beta-blockers
Moderate Interactions
- Other cholinergic agonists (e.g., bethanechol)
Monitoring
Baseline Monitoring
Baseline assessment of xerostomia severity
Rationale: To establish a starting point for evaluating treatment efficacy.
Timing: Prior to initiation of therapy
Vital signs (heart rate, blood pressure)
Rationale: To assess baseline cardiovascular status due to potential cholinergic effects.
Timing: Prior to initiation of therapy
Routine Monitoring
Xerostomia symptom improvement
Frequency: Weekly initially, then monthly or as needed
Target: Patient-reported improvement in dry mouth symptoms
Action Threshold: Lack of improvement or worsening symptoms may require dose adjustment or alternative therapy.
Adverse effects (e.g., sweating, nausea, blurred vision, urinary frequency, dizziness)
Frequency: At each follow-up visit
Target: Tolerable level of side effects
Action Threshold: Intolerable side effects may require dose reduction or discontinuation.
Vital signs (heart rate, blood pressure)
Frequency: Periodically, especially during dose titration
Target: Within normal limits or patient's baseline
Action Threshold: Significant bradycardia, hypotension, or hypertension may require dose adjustment or discontinuation.
Symptom Monitoring
- Excessive sweating
- Nausea
- Vomiting
- Diarrhea
- Abdominal cramps
- Blurred vision
- Increased urinary frequency
- Dizziness
- Headache
- Flushing
- Bradycardia
- Hypotension
Special Patient Groups
Pregnancy
Category C. Use only if the potential benefit justifies the potential risk to the fetus. Animal studies show adverse effects, but human data is limited.
Trimester-Specific Risks:
First Trimester:
Limited human data; animal studies show teratogenicity.
Second Trimester:
Limited human data.
Third Trimester:
Limited human data.
Lactation
Caution advised. Pilocarpine is excreted into breast milk in animals; human data is limited. Potential for cholinergic effects in the infant.
Infant Risk:
Low to moderate risk; monitor infant for signs of cholinergic effects (e.g., bradycardia, diarrhea, increased secretions).
Pediatric Use
Safety and efficacy not established in pediatric patients for xerostomia.
Geriatric Use
Use with caution due to increased sensitivity to cholinergic effects and potential for comorbidities. Start with lower doses and titrate slowly. Monitor closely for adverse effects, especially cardiovascular and central nervous system effects.
Clinical Information
Clinical Pearls
- Take pilocarpine with food to reduce the incidence of nausea and other gastrointestinal side effects.
- The most common side effect is sweating, which is dose-related. If sweating is bothersome, try reducing the dose or taking it with food. Ensure adequate hydration.
- Pilocarpine may cause blurred vision, especially at night or in dim light. Advise patients to exercise caution when driving or operating machinery until they know how the medication affects them.
- Pilocarpine is generally contraindicated in patients with uncontrolled asthma, narrow-angle glaucoma, or acute iritis due to its cholinergic effects.
- Consistent daily dosing is important for optimal efficacy in managing chronic dry mouth.
Alternative Therapies
- Cevimeline (another muscarinic agonist)
- Saliva substitutes (e.g., Biotene, Oasis)
- Oral moisturizers, lozenges, sugar-free gum
- Lifestyle modifications (e.g., increased fluid intake, avoiding irritants)
Cost & Coverage
Average Cost:
Price range varies widely per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3
General Drug Facts
If your symptoms or health issues persist or worsen, it's 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 be sure to check with your pharmacist for more details. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide information about the medication taken, the amount, and the time it happened.