Pilocarpine 1% 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 (parasympathomimetic)
Pregnancy Category
Category C
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Pilocarpine eye drops are used to treat high pressure inside the eye, often caused by glaucoma. It works by helping fluid drain better from your eye, which lowers the pressure. It also makes your pupil smaller, which can sometimes cause blurry vision, especially in dim light.
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 use in the eyes only.
Preparation and Administration
1. Wash your hands before and after using this medication.
2. Remove contact lenses before applying the medication. You can put them back in 10 minutes after use, but avoid doing so if your eyes are irritated or infected.
3. Avoid touching the container tip to your eye, lid, or other skin, as this can introduce bacteria and lead to severe eye problems or vision loss.
4. Tilt your head back and gently drop the medication into your eye.
5. After application, keep your eyes closed and apply pressure to the inside corner of your eye for 1 to 2 minutes to help the medication stay in your eye.
Using Multiple Medications
If you are using more than one medication in the same eye, apply each medication at least 5 minutes apart.
Storage and Disposal
1. Store this medication at room temperature, away from freezing temperatures.
2. Keep all medications in a safe place, out of the reach of children and pets.
3. 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 a drug take-back program in your area.
Missed Dose
If you miss a dose, use it as soon as you remember. However, if it is close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not use two doses at the same time or take extra doses.
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is for use in the eyes only.
Preparation and Administration
1. Wash your hands before and after using this medication.
2. Remove contact lenses before applying the medication. You can put them back in 10 minutes after use, but avoid doing so if your eyes are irritated or infected.
3. Avoid touching the container tip to your eye, lid, or other skin, as this can introduce bacteria and lead to severe eye problems or vision loss.
4. Tilt your head back and gently drop the medication into your eye.
5. After application, keep your eyes closed and apply pressure to the inside corner of your eye for 1 to 2 minutes to help the medication stay in your eye.
Using Multiple Medications
If you are using more than one medication in the same eye, apply each medication at least 5 minutes apart.
Storage and Disposal
1. Store this medication at room temperature, away from freezing temperatures.
2. Keep all medications in a safe place, out of the reach of children and pets.
3. 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 a drug take-back program in your area.
Missed Dose
If you miss a dose, use it as soon as you remember. However, if it is close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not use two doses at the same time or take extra doses.
Lifestyle & Tips
- Do not drive or operate machinery if you experience blurred vision or difficulty with night vision after using these drops.
- Avoid activities requiring sharp vision in dim light, especially at night.
- If you wear contact lenses, remove them before applying the drops and wait at least 15 minutes before reinserting them.
- Wash hands thoroughly before and after use.
- Do not touch the dropper tip to any surface to prevent contamination.
- If using other eye drops, wait at least 5-10 minutes between applications.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
1-2 drops of 1% solution in the affected eye(s) up to 4 times daily, or as directed by physician.
Dose Range:
1 - 4 mg
Condition-Specific Dosing:
openAngleGlaucoma:
1-2 drops of 1% solution in the affected eye(s) up to 4 times daily.
acuteAngleClosureGlaucoma:
1 drop of 1% solution every 5-10 minutes for 3-6 doses, then 1 drop every 1-3 hours until pressure is controlled, then 1 drop 3-4 times daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established, use with caution and under specialist supervision if considered.
Adolescent:
Dosing similar to adults, but generally not recommended for routine use in pediatric glaucoma; alternative treatments often preferred.
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 for ophthalmic use.
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 by stimulating muscarinic receptors in the eye, primarily the M3 receptors. This stimulation causes contraction of the ciliary muscle, leading to tension on the scleral spur and opening of the trabecular meshwork. This action facilitates the outflow of aqueous humor, thereby reducing intraocular pressure (IOP). Additionally, it causes contraction of the iris sphincter muscle, resulting in miosis (pupil constriction).
Pharmacokinetics
Absorption:
Bioavailability:
Not applicable (topical ophthalmic)
Tmax:
Not applicable (topical ophthalmic); IOP reduction typically within 1 hour.
FoodEffect:
Not applicable
Distribution:
Vd:
Not available (minimal systemic distribution)
ProteinBinding:
Not available (minimal systemic distribution)
CnssPenetration:
Limited (minimal systemic absorption from ophthalmic route)
Elimination:
HalfLife:
Approximately 0.76 hours (systemic, if absorbed significantly)
Clearance:
Not available (minimal systemic absorption)
ExcretionRoute:
Primarily renal (systemic, if absorbed)
Unchanged:
Not available
Pharmacodynamics
OnsetOfAction:
Miosis: 10-30 minutes; IOP reduction: 1 hour
PeakEffect:
Miosis: 30 minutes to 1 hour; IOP reduction: 1-2 hours
DurationOfAction:
Miosis: 4-8 hours; IOP reduction: 4-14 hours (depending on concentration and individual response)
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 medical attention immediately:
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 if they bother you or do not go away, contact your doctor:
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 medical attention immediately:
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 if they bother you or do not go away, contact your doctor:
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 or sudden vision changes
- Signs of allergic reaction (e.g., rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing)
- Persistent or worsening brow ache/headache
- Significant increase in eye redness or irritation
- Systemic symptoms like excessive sweating, nausea, vomiting, diarrhea, slow heart rate, or difficulty breathing (though rare with ophthalmic use, seek immediate medical attention if they occur).
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.
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 in conjunction with your other medications 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 you experienced, including any symptoms that occurred.
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 in conjunction with your other medications 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 engaging in activities that require clear vision, such as driving. Additionally, be particularly careful when driving at night or performing tasks in low-light environments, as your vision may be impaired. Regularly schedule appointments with your doctor to monitor your eye pressure and vision, as advised. If you are pregnant, planning to become pregnant, or are 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 (difficulty breathing)
- Increased salivation and lacrimation (tearing)
- Muscle tremors or weakness
What to Do:
If swallowed or excessive systemic absorption occurs, seek immediate medical attention or call a poison control center (e.g., 1-800-222-1222). Treatment is supportive and may involve atropine as an antidote for muscarinic effects.
Drug Interactions
Moderate Interactions
- Anticholinergic agents (e.g., atropine, scopolamine, tricyclic antidepressants, antihistamines): May antagonize the miotic and IOP-lowering effects of pilocarpine.
- Beta-blockers (ophthalmic or systemic): May potentiate bradycardia or bronchospasm if significant systemic absorption occurs, though rare with ophthalmic pilocarpine.
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess efficacy of treatment.
Timing: Before initiating therapy
Visual Acuity
Rationale: To assess baseline vision and monitor for changes.
Timing: Before initiating therapy
Optic Nerve Head and Visual Fields
Rationale: To assess baseline glaucoma damage and monitor progression.
Timing: Before initiating therapy
Routine Monitoring
Intraocular Pressure (IOP)
Frequency: Regularly, as determined by ophthalmologist (e.g., every 3-6 months or more frequently if unstable)
Target: Individualized target IOP set by ophthalmologist
Action Threshold: IOP above target range, or significant fluctuation
Visual Acuity
Frequency: Annually or as clinically indicated
Target: Stable or improved
Action Threshold: Significant decrease in vision
Optic Nerve Head and Visual Fields
Frequency: Annually or as clinically indicated (e.g., every 6-12 months)
Target: Stable or improved
Action Threshold: Progression of glaucoma damage
Ocular discomfort/adverse effects (e.g., brow ache, blurred vision, miosis)
Frequency: At each follow-up visit and patient self-reporting
Target: Minimal to tolerable
Action Threshold: Severe or intolerable side effects impacting quality of life
Symptom Monitoring
- Blurred vision (especially at night or in dim light)
- Brow ache or headache (especially upon initiation)
- Stinging or burning sensation in the eye
- Redness or irritation of the eye
- Increased tearing
- Difficulty with night vision
- Systemic symptoms (rare): sweating, nausea, vomiting, diarrhea, abdominal cramps, muscle tremors, bradycardia, bronchospasm (report immediately if severe)
Special Patient Groups
Pregnancy
Pilocarpine ophthalmic is classified as Pregnancy Category C. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Systemic absorption from ophthalmic administration is generally minimal, but animal studies have shown some adverse effects at high doses.
Trimester-Specific Risks:
First Trimester:
Potential risk cannot be ruled out; use only if clearly needed.
Second Trimester:
Potential risk cannot be ruled out; use only if clearly needed.
Third Trimester:
Potential risk cannot be ruled out; use only if clearly needed.
Lactation
It is not known whether pilocarpine is excreted in human milk. Due to the potential for serious adverse reactions in nursing infants from pilocarpine, 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. Minimal systemic absorption suggests low risk, but caution is advised.
Infant Risk:
L3 (Moderately safe; potential for minor, non-serious adverse effects or for effects that are not dose-related. Use only if the benefit outweighs the risk.)
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use in children is generally not recommended for routine glaucoma management; alternative treatments are often preferred. If used, it should be under strict specialist supervision due to potential for systemic side effects and impact on developing vision.
Geriatric Use
No specific dosage adjustments are typically required for elderly patients. However, elderly patients may be more susceptible to systemic side effects if significant absorption occurs, and they may experience more pronounced visual disturbances (e.g., dim vision, difficulty with night vision) due to age-related changes in the eye. Use with caution and monitor for adverse effects.
Clinical Information
Clinical Pearls
- Pilocarpine is a classic miotic agent, effective for lowering IOP but often associated with visual side effects (miosis, accommodative spasm, brow ache) that can impact patient compliance.
- The 1% concentration is a common starting point, but higher concentrations (e.g., 2%, 4%) are available for greater IOP reduction, though with increased side effects.
- Educate patients about potential blurred vision and difficulty with night vision, especially when starting therapy.
- Brow ache and headache are common initial side effects due to ciliary muscle spasm; they often diminish with continued use.
- Pilocarpine is particularly useful in acute angle-closure glaucoma to break the attack by pulling the iris away from the angle.
- Ensure proper instillation technique to minimize systemic absorption and maximize local effect (e.g., nasolacrimal occlusion).
Alternative Therapies
- Prostaglandin analogs (e.g., latanoprost, travoprost, bimatoprost)
- Beta-blockers (e.g., timolol, betaxolol)
- Alpha-2 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:
Varies, typically $15-$50 per 15ml bottle
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 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.