Isopto Carpine 4% Ophth Soln 15ml

Manufacturer ALCON 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 Agents; Miotics
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Pharmacologic Class
Cholinergic Agonists (Direct-Acting)
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Pregnancy Category
Category C
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FDA Approved
Jun 1971
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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 your eye, which can help treat glaucoma. They work by making your pupil smaller and helping fluid drain better from your eye.
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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 use in the eyes only.

Administration Instructions

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 surrounding skin, as this can contaminate the medication 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 gentle pressure to the inner corner of your eye for 1 to 2 minutes. This helps the medication stay 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 place, 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. If you have questions about disposal, consult your pharmacist. You may also have access to drug take-back programs in your area.

Missed Dose Instructions

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 once or take extra doses. Continue using the medication as directed, even if your symptoms improve.
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Lifestyle & Tips

  • Be aware that pilocarpine can cause temporary blurred vision, especially in dim light or at night. Exercise caution when driving or operating machinery, particularly in low light conditions.
  • Remove contact lenses before applying drops and wait at least 15 minutes before reinserting them.
  • Wash hands thoroughly before and after applying eye drops.
  • Do not touch the dropper tip to any surface to avoid contamination.

Dosing & Administration

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Adult Dosing

Standard Dose: 1-2 drops of 1% to 4% solution in the affected eye(s) up to 4 times daily
Dose Range: 1 - 4 mg

Condition-Specific Dosing:

open-angle glaucoma: 1-2 drops of 1% to 4% solution in the affected eye(s) up to 4 times daily
acute angle-closure glaucoma: 1 drop of 2% solution every 5-10 minutes for 3-6 doses, then 1 drop every 1-3 hours until pressure is controlled
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Pediatric Dosing

Neonatal: Not established
Infant: Not established, use with caution and specific indications (e.g., congenital glaucoma) under specialist supervision.
Child: Not established, use with caution and specific indications (e.g., congenital glaucoma) under specialist supervision.
Adolescent: Similar to adult dosing for specific indications, but generally not first-line.
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Dose Adjustments

Renal Impairment:

Mild: No adjustment typically required due to minimal systemic absorption.
Moderate: No adjustment typically required due to minimal systemic absorption.
Severe: No adjustment typically required due to minimal systemic absorption.
Dialysis: No specific considerations due to minimal systemic absorption.

Hepatic Impairment:

Mild: No adjustment typically required due to minimal systemic absorption.
Moderate: No adjustment typically required due to minimal systemic absorption.
Severe: No adjustment typically required due to minimal systemic absorption.

Pharmacology

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Mechanism of Action

Pilocarpine is a direct-acting cholinergic parasympathomimetic agent. It acts on muscarinic receptors in the eye, causing contraction of the ciliary muscle and the iris sphincter. Contraction of the ciliary muscle facilitates the outflow of aqueous humor through the trabecular meshwork, thereby lowering intraocular pressure (IOP). Contraction of the iris sphincter causes miosis (pupil constriction).
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Pharmacokinetics

Absorption:

Bioavailability: Minimal systemic absorption from ophthalmic administration.
Tmax: Not applicable for systemic Tmax due to local action; ocular effects typically within minutes.
FoodEffect: Not applicable (ophthalmic).

Distribution:

Vd: Not applicable (localized ocular action).
ProteinBinding: Not applicable (localized ocular action).
CnssPenetration: Limited (minimal systemic absorption).

Elimination:

HalfLife: Ocular half-life is short (minutes to hours); systemic half-life is also short (approximately 0.76 hours).
Clearance: Rapid hydrolysis by cholinesterases.
ExcretionRoute: Primarily local metabolism; minimal systemic excretion via urine.
Unchanged: Not available (minimal systemic absorption).
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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.

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 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 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 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. Your doctor can provide medical advice about side effects and help you determine the best course of action.
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Seek Immediate Medical Attention If You Experience:

  • Severe eye pain or discomfort that worsens
  • Sudden, significant decrease in vision
  • Signs of an allergic reaction (e.g., rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing - seek immediate medical attention)
  • Persistent headache or brow ache
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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 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 with your other medications and health conditions.

Remember, do not start, stop, or change the dosage of any medication without first consulting your doctor.
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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 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 affected. 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.
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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; atropine may be used as an antidote for severe cholinergic symptoms.

Drug Interactions

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Moderate Interactions

  • Anticholinergic agents (e.g., atropine, scopolamine, tricyclic antidepressants, antihistamines): May antagonize the miotic and IOP-lowering effects of pilocarpine.

Monitoring

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Baseline Monitoring

Intraocular Pressure (IOP)

Rationale: To establish baseline and assess treatment efficacy for glaucoma.

Timing: Prior to initiation of therapy.

Visual Acuity

Rationale: To establish baseline and monitor for changes or side effects.

Timing: Prior to initiation of therapy.

Ophthalmic Examination (e.g., fundus, optic nerve head)

Rationale: To assess the overall ocular health and progression of glaucoma.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Intraocular Pressure (IOP)

Frequency: Regularly, as determined by ophthalmologist (e.g., every 3-6 months or as needed).

Target: Individualized target IOP set by ophthalmologist.

Action Threshold: IOP above target range, or signs of glaucoma progression.

Visual Acuity

Frequency: Periodically, as determined by ophthalmologist.

Target: Stable or improved vision.

Action Threshold: Significant decrease in visual acuity.

Patient-reported side effects (e.g., blurred vision, headache, eye pain)

Frequency: At each follow-up visit.

Target: Minimal or tolerable side effects.

Action Threshold: Intolerable side effects impacting quality of life or adherence.

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Symptom Monitoring

  • Blurred vision (especially at night or in dim light)
  • Headache (especially brow ache)
  • Eye pain or discomfort
  • Eye redness or irritation
  • Difficulty with night vision
  • Changes in vision

Special Patient Groups

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Pregnancy

Pilocarpine is Pregnancy Category C. Use only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects, but there are no adequate and well-controlled studies in pregnant women. Systemic absorption from ophthalmic use is minimal.

Trimester-Specific Risks:

First Trimester: Potential for risk, but minimal systemic exposure limits concern.
Second Trimester: Potential for risk, but minimal systemic exposure limits concern.
Third Trimester: Potential for risk, but minimal systemic exposure limits concern.
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Lactation

Pilocarpine is considered to have a low risk during lactation (L3). While it is unknown if pilocarpine is excreted in human milk, systemic absorption from ophthalmic use is minimal, making infant exposure unlikely to be significant. Monitor the infant for signs of cholinergic effects (e.g., diarrhea, bradycardia) if used.

Infant Risk: Low risk.
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Pediatric Use

Safety and efficacy in pediatric patients have not been fully established. Use with caution and only when clearly indicated (e.g., congenital glaucoma) under the supervision of a pediatric ophthalmologist. Dosage should be carefully titrated.

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Geriatric Use

No specific dosage adjustments are typically required for geriatric patients. However, older patients may be more susceptible to systemic side effects if significant absorption occurs, or may experience more pronounced visual disturbances (e.g., dim vision, difficulty with night vision) due to age-related changes in the eye. Monitor closely for side effects.

Clinical Information

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Clinical Pearls

  • Pilocarpine is a classic miotic agent, often used for acute angle-closure glaucoma to break the attack, but less commonly as first-line for chronic open-angle glaucoma due to its side effect profile (miosis, accommodative spasm, brow ache) and frequent dosing.
  • Patients should be warned about potential dimness of vision, especially in poor illumination, and difficulty with night driving due to miosis.
  • Brow ache and headache are common side effects, particularly at the start of therapy, and often diminish with continued use.
  • Proper instillation technique is crucial: pull down the lower eyelid, apply the drop, close the eye gently, and apply nasolacrimal occlusion (press on the inner corner of the eye) for 1-2 minutes to minimize systemic absorption and maximize local effect.
  • If using other ophthalmic medications, wait at least 5-10 minutes between drops.
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Alternative Therapies

  • Prostaglandin analogs (e.g., latanoprost, travoprost, bimatoprost): Often first-line for open-angle glaucoma.
  • Beta-blockers (e.g., timolol, betaxolol): Common for open-angle glaucoma.
  • Alpha-adrenergic agonists (e.g., brimonidine, apraclonidine).
  • Carbonic anhydrase inhibitors (e.g., dorzolamide, brinzolamide, acetazolamide).
  • Rho kinase inhibitors (e.g., netarsudil).
  • Combination ophthalmic products (e.g., timolol/dorzolamide, timolol/brimonidine).
  • Laser procedures (e.g., Selective Laser Trabeculoplasty - SLT, Argon Laser Trabeculoplasty - ALT).
  • Surgical procedures (e.g., trabeculectomy, glaucoma drainage devices).
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Cost & Coverage

Average Cost: Varies widely, typically $20-$50 per 15ml bottle
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (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 this 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, including the amount taken and the time it happened, to ensure you receive the best possible care.