Pilocarpine 4% Ophth Soln 15ml
It is used to treat glaucoma.It is used to lower high eye pressure.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antiglaucoma agent, Miotic
Pharmacologic Class
Direct-acting cholinergic agonist (muscarinic)
Pregnancy Category
C
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Pilocarpine eye drops are used to treat glaucoma, a condition that damages the optic nerve and can lead to vision loss. It works by helping fluid drain better from your eye, which lowers the pressure inside your eye. It also makes your pupil smaller, which can help with some types of glaucoma.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is for eye use only.
1. Preparation: Wash your hands before and after using this medication. Remove your contact lenses before application, and wait at least 10 minutes after use before putting them back in. However, do not replace your contact lenses if your eyes are irritated or infected.
2. Administration: Avoid touching the container tip to your eye, eyelid, or surrounding skin, as this can introduce bacteria and lead to severe eye problems or vision loss. Tilt your head back, and gently drop the medication into your eye.
3. Post-Application: After applying the medication, keep your eyes closed and apply gentle pressure to the inner corner of your eye for 1 to 2 minutes. This helps the medication stay in your eye.
4. Usage Schedule: Use this medication as directed, even if your symptoms improve. If you are using multiple medications in the same eye, administer them at least 5 minutes apart.
Storage and Disposal
Store this medication at room temperature, avoiding freezing.
Keep all medications in a secure location, out of the reach of children and pets.
* Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. Consult your pharmacist for guidance on disposal, and consider participating in local drug take-back programs.
Missed Dose
If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not use two doses at once or take extra doses.
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is for eye use only.
1. Preparation: Wash your hands before and after using this medication. Remove your contact lenses before application, and wait at least 10 minutes after use before putting them back in. However, do not replace your contact lenses if your eyes are irritated or infected.
2. Administration: Avoid touching the container tip to your eye, eyelid, or surrounding skin, as this can introduce bacteria and lead to severe eye problems or vision loss. Tilt your head back, and gently drop the medication into your eye.
3. Post-Application: After applying the medication, keep your eyes closed and apply gentle pressure to the inner corner of your eye for 1 to 2 minutes. This helps the medication stay in your eye.
4. Usage Schedule: Use this medication as directed, even if your symptoms improve. If you are using multiple medications in the same eye, administer them at least 5 minutes apart.
Storage and Disposal
Store this medication at room temperature, avoiding freezing.
Keep all medications in a secure location, out of the reach of children and pets.
* Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. Consult your pharmacist for guidance on disposal, and consider participating in local drug take-back programs.
Missed Dose
If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not use two doses at once or take extra doses.
Lifestyle & Tips
- Pilocarpine can cause temporary blurred vision, especially when starting treatment or changing concentrations. Be cautious when driving or operating machinery, especially at night or in dim light, until you know how the medication affects your vision.
- Wash hands thoroughly before and after use.
- Do not touch the dropper tip to any surface to avoid contamination.
- If using other eye drops, wait at least 5 minutes between applications.
- Remove contact lenses before instilling drops and wait at least 15 minutes before reinserting them.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
1 drop of 1% to 4% solution in the affected eye(s) 2 to 4 times daily, depending on IOP response and tolerance.
Dose Range:
1 - 4 mg
Condition-Specific Dosing:
Glaucoma/Ocular Hypertension:
1 drop of 1% to 4% solution in the affected eye(s) 2 to 4 times daily.
Miosis induction (e.g., before surgery):
1 drop of 1% or 2% solution, single dose.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established (use in pediatric glaucoma is off-label and requires specialist guidance)
Adolescent:
Similar to adult dosing, but generally not first-line for glaucoma.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed (minimal systemic absorption)
Moderate:
No adjustment needed (minimal systemic absorption)
Severe:
No adjustment needed (minimal systemic absorption)
Dialysis:
No specific considerations (minimal systemic absorption)
Hepatic Impairment:
Mild:
No adjustment needed (minimal systemic absorption)
Moderate:
No adjustment needed (minimal systemic absorption)
Severe:
No adjustment needed (minimal systemic absorption)
Pharmacology
Mechanism of Action
Pilocarpine is a direct-acting cholinergic parasympathomimetic agent. It acts on muscarinic receptors (M3) in the eye, primarily causing contraction of the ciliary muscle and the iris sphincter muscle. Contraction of the ciliary muscle opens the trabecular meshwork, facilitating the outflow of aqueous humor and thereby reducing intraocular pressure (IOP). Contraction of the iris sphincter muscle causes miosis (pupil constriction).
Pharmacokinetics
Absorption:
Bioavailability:
Not precisely quantifiable for ophthalmic use due to local action and minimal systemic absorption. Ocular bioavailability is high.
Tmax:
Not applicable for systemic Tmax due to local action; IOP reduction typically begins within 10-30 minutes.
FoodEffect:
Not applicable (ophthalmic administration)
Distribution:
Vd:
Not precisely quantifiable for ophthalmic use; primarily distributed within ocular tissues.
ProteinBinding:
Not precisely quantifiable for ophthalmic use; minimal systemic protein binding.
CnssPenetration:
Limited (minimal systemic absorption from ophthalmic route)
Elimination:
HalfLife:
Systemic half-life is short (approx. 0.76 hours) but ocular effects persist longer.
Clearance:
Rapid hydrolysis by cholinesterases.
ExcretionRoute:
Primarily renal for systemically absorbed drug; minimal systemic absorption from ophthalmic route.
Unchanged:
Not precisely quantifiable for ophthalmic use.
Pharmacodynamics
OnsetOfAction:
Miosis: 10-30 minutes; IOP reduction: 10-30 minutes.
PeakEffect:
Miosis: 30 minutes to 1 hour; IOP reduction: 1-2 hours.
DurationOfAction:
Miosis: 4-8 hours; IOP reduction: 4-8 hours (up to 12 hours for some formulations).
Confidence:
Medium
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
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 immediate medical attention:
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
Changes in eyesight, eye pain, or severe eye irritation
Severe eye problems, including:
+ Retinal tear or detachment (especially in people with pre-existing retinal disease)
+ Sudden symptoms such as:
- Flashing lights
- Floaters
- A curtain-like shadow coming across your eye
- Sudden eyesight loss
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:
Headache
Eye irritation
Blurred eyesight
Eye redness
Temporary dim or dark eyesight
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, 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 immediate medical attention:
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
Changes in eyesight, eye pain, or severe eye irritation
Severe eye problems, including:
+ Retinal tear or detachment (especially in people with pre-existing retinal disease)
+ Sudden symptoms such as:
- Flashing lights
- Floaters
- A curtain-like shadow coming across your eye
- Sudden eyesight loss
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:
Headache
Eye irritation
Blurred eyesight
Eye redness
Temporary dim or dark eyesight
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, 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:
- Severe eye pain
- Sudden vision changes or loss
- Signs of eye infection (redness, swelling, discharge)
- Severe headache
- Nausea or vomiting (rare with ophthalmic use, but possible with systemic absorption)
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 and its symptoms.
If you have a specific eye condition called iritis.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your existing treatments and health conditions.
Remember, do not start, stop, or modify the dosage of any medication without first consulting your doctor to ensure your safety.
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 and its symptoms.
If you have a specific eye condition called iritis.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your existing treatments and health conditions.
Remember, do not start, stop, or modify the dosage of any medication without first consulting your doctor to ensure your safety.
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 particularly careful when driving at night or engaging in activities in low-light environments. Regularly schedule appointments with your doctor to monitor your eye pressure and vision, as advised. If you are pregnant, planning to become pregnant, or breastfeeding, notify your doctor promptly. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Excessive sweating
- Nausea
- Vomiting
- Diarrhea
- Abdominal cramps
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Bronchospasm
- Increased salivation
- Lacrimation (tearing)
- Miosis (pinpoint pupils)
- Headache
- Visual disturbances
What to Do:
If systemic overdose is suspected (rare with ophthalmic use), seek immediate medical attention. Call 911 or Poison Control at 1-800-222-1222. Treatment is supportive and may involve atropine for severe cholinergic symptoms.
Drug Interactions
Moderate Interactions
- Anticholinergic agents (e.g., atropine, scopolamine, cycloplegics): May antagonize the miotic and IOP-lowering effects of pilocarpine.
- Other ophthalmic miotics: Concurrent use may lead to additive effects and increased risk of adverse reactions.
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess efficacy of treatment.
Timing: Before initiating therapy
Visual Acuity
Rationale: To establish baseline and monitor for changes, especially due to miosis or accommodative spasm.
Timing: Before initiating therapy
Funduscopic Examination
Rationale: To assess optic nerve health and rule out other ocular pathologies.
Timing: Before initiating therapy
Routine Monitoring
Intraocular Pressure (IOP)
Frequency: Regularly, as determined by ophthalmologist (e.g., every 3-6 months or as needed)
Target: Individualized target IOP based on glaucoma severity and progression.
Action Threshold: IOP above target range or signs of progression.
Visual Acuity
Frequency: Regularly, as determined by ophthalmologist
Target: Maintain best corrected visual acuity.
Action Threshold: Significant decrease in visual acuity.
Slit-lamp examination
Frequency: Periodically, as determined by ophthalmologist
Target: Normal ocular structures.
Action Threshold: Signs of inflammation, cataract progression, or other adverse effects.
Symptom Monitoring
- Blurred vision (especially at night or in dim light)
- Headache (especially brow ache)
- Eye pain or discomfort
- Difficulty with night vision
- Increased tearing
- Redness of the eye
Special Patient Groups
Pregnancy
Pilocarpine is Pregnancy Category C. Animal studies have shown adverse effects, but there are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus. Systemic absorption from ophthalmic use is minimal.
Trimester-Specific Risks:
First Trimester:
Potential risk, but minimal systemic exposure.
Second Trimester:
Potential risk, but minimal systemic exposure.
Third Trimester:
Potential risk, but minimal systemic exposure.
Lactation
Pilocarpine is excreted in human milk after systemic administration. However, systemic absorption from ophthalmic administration is minimal, making infant exposure unlikely to be significant. Caution should be exercised when administered to a nursing mother. Monitor the infant for signs of cholinergic effects (e.g., diarrhea, bradycardia).
Infant Risk:
Low risk due to minimal systemic absorption, but monitor for cholinergic effects.
Pediatric Use
Safety and efficacy in pediatric patients have not been established. Use in pediatric glaucoma is generally off-label and requires careful consideration by a specialist due to potential for systemic side effects and accommodative spasm.
Geriatric Use
No specific dose adjustments are typically required. However, geriatric patients may be more susceptible to systemic side effects if significant absorption occurs, and may experience more pronounced visual disturbances (e.g., dim vision, difficulty with night vision) due to pre-existing cataracts or other age-related ocular changes.
Clinical Information
Clinical Pearls
- Pilocarpine is a classic miotic, but its use has declined with the advent of prostaglandin analogs and beta-blockers due to its side effect profile (miosis, accommodative spasm, brow ache, dim vision).
- It is still useful in specific situations, such as acute angle-closure glaucoma (to break the attack) or in patients who cannot tolerate or respond to other classes of IOP-lowering medications.
- The 4% concentration is one of the higher strengths and is typically reserved for patients requiring significant IOP reduction or those who have developed tolerance to lower concentrations.
- Patients should be warned about the potential for dim vision, especially at night or in poorly lit environments, due to miosis.
- Brow ache and headache are common side effects, especially at the initiation of therapy, and often subside with continued use.
Alternative Therapies
- Prostaglandin analogs (e.g., latanoprost, travoprost, bimatoprost)
- Beta-blockers (e.g., timolol, betaxolol)
- Alpha-adrenergic agonists (e.g., brimonidine, apraclonidine)
- Carbonic anhydrase inhibitors (e.g., dorzolamide, brinzolamide, acetazolamide)
- Rho kinase inhibitors (e.g., netarsudil)
- Combination products (e.g., timolol/dorzolamide, timolol/brimonidine)
Cost & Coverage
Average Cost:
$30 - $80 per 15ml bottle of 4% solution
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (Generic)
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 information. 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 details about the medication taken, the amount, and the time it happened.