Pilocarpine 2% Ophth Soln 15ml

Manufacturer SOMERSET Active Ingredient Pilocarpine Eye Drops (Isopto Carpine)(pye loe KAR peen) Pronunciation pye loe KAR peen
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.
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Drug Class
Antiglaucoma agent, Miotic
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Pharmacologic Class
Cholinergic agonist (Muscarinic)
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Pregnancy Category
Category C
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FDA Approved
Jan 1970
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Pilocarpine eye drops are used to lower high pressure inside the eye, which can damage your vision (glaucoma), or to make your pupils smaller. It works by helping fluid drain better from your eye and by making your pupil constrict.
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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.

Preparation and Administration

1. Wash your hands before and after using this medication.
2. Remove contact lenses before administering the medication. You can reinsert your lenses 10 minutes after use, unless your eyes are irritated or infected.
3. Avoid touching the container tip to your eye, lid, or surrounding 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 administration, keep your eyes closed and apply gentle pressure to the inside corner of your eye for 1 to 2 minutes. This helps retain the medication in your eye.

Using Multiple Medications

If you are using more than one medication in the same eye, administer each medication at least 5 minutes apart.

Storage and Disposal

Store this medication at room temperature, away from freezing temperatures. Keep all medications in a safe location, out of 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 or to inquire about drug take-back programs 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 scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not use two doses at the same time or take extra doses.
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Lifestyle & Tips

  • Wash hands thoroughly before and after use.
  • Do not touch the dropper tip to any surface to avoid contamination.
  • Tilt head back, pull down lower eyelid, and look up. Instill the prescribed number of drops into the conjunctival sac. Close eye gently for 1-2 minutes. Apply pressure to the inner corner of the eye (lacrimal punctum) for 1 minute to minimize systemic absorption.
  • If using other eye drops, wait at least 5 minutes between applications.
  • Pilocarpine can cause blurred vision, dim vision, and difficulty seeing in dim light or at night due to pupil constriction. Exercise caution when driving or operating machinery, especially at night or in poorly lit areas.
  • Report any persistent eye pain, headache, or significant vision changes to your doctor.
  • Store at room temperature, away from light and moisture.

Dosing & Administration

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Adult Dosing

Standard Dose: For open-angle glaucoma or ocular hypertension: 1-2 drops of 2% solution in the affected eye(s) 2-4 times daily. For acute angle-closure glaucoma: 1 drop every 5-10 minutes for 3-6 doses, then 1 drop every 1-3 hours until pressure is controlled. For reversal of mydriasis: 1 drop.

Condition-Specific Dosing:

openAngleGlaucoma: 1-2 drops 2% solution 2-4 times daily
acuteAngleClosureGlaucoma: 1 drop 2% solution every 5-10 minutes for 3-6 doses, then 1 drop every 1-3 hours until pressure is controlled
reversalOfMydriasis: 1 drop 2% solution
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Pediatric Dosing

Neonatal: Not established (use with extreme caution, if at all, for specific conditions like congenital glaucoma, dose individualized)
Infant: Not established (use with extreme caution, if at all, for specific conditions like congenital glaucoma, dose individualized)
Child: Not established (use with caution, generally for specific conditions like congenital glaucoma or reversal of mydriasis, dose individualized, typically 1 drop 2% solution 2-4 times daily or as needed)
Adolescent: Similar to adult dosing, 1-2 drops 2% solution 2-4 times daily for glaucoma or ocular hypertension, or as needed for reversal of mydriasis.
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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 due to 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

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Mechanism of Action

Pilocarpine is a direct-acting muscarinic cholinergic agonist. In the eye, it acts on muscarinic receptors in the ciliary body and iris. Contraction of the ciliary muscle pulls on the scleral spur, opening the trabecular meshwork, which facilitates the outflow of aqueous humor and lowers intraocular pressure (IOP). It also causes miosis (pupil constriction) by contracting the iris sphincter muscle.
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Pharmacokinetics

Absorption:

Bioavailability: Not applicable (ophthalmic, minimal systemic absorption)
Tmax: Ocular effects (miosis) within 10-30 minutes; IOP reduction within 1 hour.
FoodEffect: Not applicable (ophthalmic)

Distribution:

Vd: Not applicable (primarily local ocular action)
ProteinBinding: Not applicable (primarily local ocular action)
CnssPenetration: Limited (minimal systemic absorption from ophthalmic route)

Elimination:

HalfLife: Ocular effects last 4-8 hours. Systemic half-life is short (approximately 0.76 hours if administered systemically).
Clearance: Rapid hydrolysis by cholinesterases.
ExcretionRoute: Not applicable (primarily local metabolism, minimal systemic excretion)
Unchanged: Not applicable (primarily local metabolism)
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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: 4-8 hours
Confidence: Medium

Safety & Warnings

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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 if you have a history of 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.
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Seek Immediate Medical Attention If You Experience:

  • Severe or persistent eye pain
  • Sudden changes in vision
  • Increased redness or irritation of the eye
  • Signs of systemic absorption (rare with ophthalmic use but possible if ingested or excessively absorbed): sweating, nausea, vomiting, diarrhea, abdominal cramps, slow heart rate, dizziness, difficulty breathing.
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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 symptoms you experienced.
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 health conditions and other drugs.

Remember, do not start, stop, or adjust the dosage of any medication without first consulting your doctor to ensure your safety.
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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. Regularly check your eye pressure and vision as directed by your doctor to monitor any potential changes. If you are pregnant, planning to become pregnant, or breastfeeding, consult your doctor to discuss the potential benefits and risks of this medication to both you and your baby.
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Overdose Information

Overdose Symptoms:

  • Bradycardia
  • Hypotension
  • Bronchospasm
  • Sweating
  • Salivation
  • Nausea
  • Vomiting
  • Diarrhea
  • Abdominal cramps
  • Headache
  • Visual disturbances

What to Do:

If accidental ingestion or significant systemic overdose occurs, seek immediate medical attention. Call 911 or Poison Control (1-800-222-1222). Treatment is supportive and may include atropine as an antidote for muscarinic effects.

Drug Interactions

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Moderate Interactions

  • Anticholinergic agents (e.g., atropine, scopolamine, cycloplegics): May antagonize the miotic and IOP-lowering effects of pilocarpine.
  • Other miotics: Additive effects on miosis and IOP reduction.

Monitoring

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Baseline Monitoring

Intraocular Pressure (IOP)

Rationale: To establish baseline and assess response to therapy for glaucoma/ocular hypertension.

Timing: Prior to initiation of therapy.

Visual Acuity

Rationale: To establish baseline and monitor for visual side effects.

Timing: Prior to initiation of therapy.

Ophthalmic Examination (e.g., slit lamp, fundus)

Rationale: To assess ocular health and rule out contraindications.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Intraocular Pressure (IOP)

Frequency: Regularly, as determined by ophthalmologist (e.g., 1-4 times per year or as needed based on disease control).

Target: Individualized, typically <21 mmHg or target pressure to prevent progression.

Action Threshold: IOP not adequately controlled, or significant fluctuations.

Visual Acuity

Frequency: Regularly, as determined by ophthalmologist.

Target: Stable or improved.

Action Threshold: Significant decrease in vision or new visual disturbances.

Ocular discomfort/pain

Frequency: At each visit and patient self-monitoring.

Target: Minimal to none.

Action Threshold: Persistent or severe eye pain, brow ache, or headache.

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Symptom Monitoring

  • Blurred vision (especially at night or in dim light)
  • Dim vision
  • Brow ache or headache (especially upon initiation)
  • Eye pain or discomfort
  • Difficulty with night driving
  • Increased tearing
  • Redness of the eye
  • Rare systemic effects (if significant absorption occurs): sweating, nausea, vomiting, diarrhea, abdominal cramps, bradycardia, hypotension, bronchospasm.

Special Patient Groups

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Pregnancy

Pilocarpine is Pregnancy Category C. Animal reproduction studies have shown an adverse effect on the fetus, but there are no adequate and well-controlled studies in humans. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Trimester-Specific Risks:

First Trimester: Potential for fetal harm based on animal data; use only if clearly needed.
Second Trimester: Potential for fetal harm based on animal data; use only if clearly needed.
Third Trimester: Potential for fetal harm based on animal data; use only if clearly needed.
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Lactation

Pilocarpine is rated L3 (Moderately Safe) for lactation. While systemic absorption from ophthalmic use is minimal, it is unknown if pilocarpine is excreted in human milk. Caution should be exercised when administering to a nursing mother. Monitor the infant for signs of cholinergic effects (e.g., diarrhea, bradycardia).

Infant Risk: Low risk of adverse effects due to minimal systemic absorption, but theoretical risk of cholinergic effects. Monitor infant.
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Pediatric Use

Use with caution. Safety and efficacy in pediatric patients have not been fully established. It may be used in specific conditions like congenital glaucoma or for reversal of mydriasis, but dosing must be individualized and closely monitored by an ophthalmologist. Children may be more susceptible to systemic side effects if significant absorption occurs.

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Geriatric Use

No specific dose adjustment is generally required. However, elderly patients may be more susceptible to visual side effects such as dim vision, especially in low light conditions, and may experience more difficulty with night driving. Monitor closely for visual disturbances and ensure patient safety.

Clinical Information

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Clinical Pearls

  • Pilocarpine is a classic miotic agent, often causing brow ache and headache, especially upon initiation. These side effects often diminish with continued use.
  • Patients should be warned about decreased vision, particularly in dim light or at night, due to miosis. This can significantly impact night driving.
  • It is sometimes used diagnostically for Adie's tonic pupil (denervation supersensitivity to dilute pilocarpine).
  • Due to its short duration of action, pilocarpine often requires frequent dosing (2-4 times daily), which can impact patient adherence compared to once-daily agents.
  • Available in various concentrations (e.g., 0.5%, 1%, 2%, 4%, 6%), with 2% being a common starting point for glaucoma.
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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)
  • Rho kinase inhibitors (e.g., netarsudil)
  • Combination products (e.g., dorzolamide/timolol, brimonidine/timolol)
  • Laser trabeculoplasty
  • Surgical procedures (e.g., trabeculectomy, glaucoma drainage devices)
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Cost & Coverage

Average Cost: Varies, typically $15-$40 per 15ml bottle of 2% solution
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (preferred generic)
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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.