Isopto Carpine 2% 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
Miotic, Antiglaucoma Agent, Cholinergic Agonist
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Pharmacologic Class
Muscarinic Cholinergic Agonist
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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 treat high pressure inside the eye, a condition often associated with glaucoma. It works by making your pupil smaller and helping the fluid drain better from your eye, which lowers the pressure. This helps protect your vision.
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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.

1. Preparation: Wash your hands before and after using this medication. Remove your contact lenses before applying the medication, and wait 10 minutes before putting them back in. However, do not replace your contact lenses if your eyes are irritated or infected.
2. Administration: To avoid contaminating the medication, do not touch the container tip to your eye, lid, or surrounding skin, as this could lead to bacterial infection, severe eye problems, or vision loss. Tilt your head back, and gently drop the medication into your eye.
3. Post-Administration: 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 retain the medication in your eye.
4. Usage Schedule: Continue using the medication as directed, even if your symptoms improve. If you are using multiple medications in the same eye, administer each medication at least 5 minutes apart.

Storage and Disposal

1. Storage: Store this medication at room temperature, avoiding freezing.
2. Safety Precautions: Keep all medications in a secure location, out of the reach of children and pets.
3. Disposal: 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 the best disposal method, 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.
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Lifestyle & Tips

  • Administer drops exactly as prescribed by your doctor. Do not use more or less often than directed.
  • Wash hands thoroughly before and after administering eye drops.
  • Tilt your head back, pull down your lower eyelid to form a pocket, and instill the prescribed number of drops. Close your eye gently for 1-2 minutes, and apply pressure to the inner corner of your eye (near the nose) to minimize systemic absorption.
  • If using other eye drops, wait at least 5-10 minutes between applications.
  • Remove contact lenses before instilling drops and wait at least 15 minutes before reinserting them.
  • Be aware that pilocarpine can cause blurred vision, especially in dim light or at night, and difficulty with night vision due to pupil constriction. Exercise caution when driving or operating machinery in low light conditions.
  • Report any new or worsening eye symptoms or systemic side effects to your doctor.

Dosing & Administration

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Adult Dosing

Standard Dose: 1 to 2 drops in the affected eye(s) 2 to 4 times daily, depending on the patient's response and tolerance.
Dose Range: 1 - 2 mg

Condition-Specific Dosing:

openAngleGlaucoma: 1 to 2 drops 2 to 4 times daily
acuteAngleClosureGlaucoma: 1 drop every 5 to 10 minutes for 3 to 6 doses, then 1 drop every 1 to 3 hours until pressure is controlled and angle is open.
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Pediatric Dosing

Neonatal: Not established, use with extreme caution and specialist supervision for specific conditions (e.g., congenital glaucoma).
Infant: Not established, use with extreme caution and specialist supervision for specific conditions (e.g., congenital glaucoma).
Child: Not established for routine use. May be used off-label for specific conditions like accommodative esotropia (e.g., 1 drop of 0.125% to 0.25% solution nightly or twice daily) under specialist supervision.
Adolescent: Not established for routine use. May be used off-label for specific conditions under specialist supervision.
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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 parasympathomimetic agent that stimulates muscarinic cholinergic receptors. In the eye, it causes contraction of the iris sphincter muscle, leading to miosis (pupil constriction), and contraction of the ciliary muscle. Contraction of the ciliary muscle pulls on the scleral spur, opening the trabecular meshwork and facilitating the outflow of aqueous humor, thereby reducing intraocular pressure (IOP).
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Pharmacokinetics

Absorption:

Bioavailability: Minimal systemic bioavailability following topical ocular administration; primarily local action.
Tmax: Not applicable for systemic peak; ocular effects onset within minutes.
FoodEffect: Not applicable for ophthalmic use.

Distribution:

Vd: Not applicable (primarily local ocular distribution).
ProteinBinding: Not applicable (primarily local ocular distribution).
CnssPenetration: Limited (minimal systemic absorption).

Elimination:

HalfLife: Ocular effects duration 4-8 hours; systemic half-life not clinically relevant for ophthalmic use due to rapid hydrolysis.
Clearance: Rapid hydrolysis by cholinesterases.
ExcretionRoute: Primarily local metabolism; minimal systemic excretion of intact drug.
Unchanged: Not applicable (rapidly metabolized).
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Pharmacodynamics

OnsetOfAction: Miosis: 10-30 minutes; IOP reduction: within 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 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, which may be more likely in people with retinal disease. Be alert for 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, although many people may not experience any or may only have mild symptoms. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical help:

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 about side effects, contact your doctor for medical advice. 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:

  • Sudden, severe eye pain or discomfort
  • Sudden decrease or change in vision
  • Signs of allergic reaction (e.g., rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing)
  • Systemic cholinergic symptoms (rare but serious): excessive sweating, nausea, vomiting, diarrhea, abdominal cramps, slow heart rate, difficulty breathing, muscle weakness.
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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 (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 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 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 monitor your eye pressure and vision as instructed by your doctor to ensure your eyes remain healthy. If you are pregnant, planning to become pregnant, or are 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:

  • Ocular overdose: Exaggerated local effects such as severe miosis, intense accommodative spasm, brow ache, and blurred vision.
  • Systemic overdose (rare with ophthalmic use): Cholinergic crisis symptoms including nausea, vomiting, diarrhea, abdominal cramps, salivation, sweating, bradycardia, hypotension, bronchospasm, muscle tremors, and weakness.

What to Do:

If systemic overdose is suspected, seek immediate medical attention. Call 911 or your local emergency number. For accidental ingestion or significant systemic symptoms, supportive care should be provided. Atropine may be administered as an antidote for severe systemic cholinergic symptoms. For ocular overdose, discontinue use and manage symptoms symptomatically. Call 1-800-222-1222 (Poison Control Center).

Drug Interactions

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Moderate Interactions

  • Ophthalmic anticholinergics (e.g., atropine, cyclopentolate, tropicamide): May antagonize the miotic and IOP-lowering effects of pilocarpine.
  • Ophthalmic beta-blockers (e.g., timolol), alpha-adrenergic agonists (e.g., brimonidine), carbonic anhydrase inhibitors (e.g., dorzolamide): May have additive IOP-lowering effects when used concurrently with pilocarpine.

Monitoring

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Baseline Monitoring

Intraocular Pressure (IOP)

Rationale: To establish baseline IOP before initiating therapy for glaucoma or ocular hypertension.

Timing: Prior to initiation of therapy.

Visual Acuity

Rationale: To assess baseline visual function and monitor for changes.

Timing: Prior to initiation of therapy.

Slit-lamp Examination

Rationale: To assess ocular health, including iris, lens, and anterior chamber angle.

Timing: Prior to initiation of therapy.

Funduscopic Examination (Optic Nerve Head)

Rationale: To assess for glaucomatous optic neuropathy.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Intraocular Pressure (IOP)

Frequency: Regularly, e.g., every 3-6 months or as clinically indicated, to ensure therapeutic efficacy.

Target: Individualized, typically aiming for a target IOP that prevents further optic nerve damage.

Action Threshold: IOP above target range, or evidence of progressive optic nerve damage/visual field loss.

Visual Acuity

Frequency: Periodically, e.g., annually or as clinically indicated.

Target: Stable or improved.

Action Threshold: Significant decrease in visual acuity not attributable to other causes.

Ocular Side Effects (e.g., miosis, accommodative spasm, brow ache, blurred vision)

Frequency: At each follow-up visit and as reported by patient.

Target: Minimal or tolerable.

Action Threshold: Severe or 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 (particularly brow ache)
  • Eye pain or discomfort
  • Eye redness or irritation
  • Difficulty with night vision
  • Systemic cholinergic symptoms (rare with ophthalmic use but possible with excessive absorption): sweating, nausea, vomiting, diarrhea, abdominal cramps, salivation, bradycardia, bronchospasm.

Special Patient Groups

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Pregnancy

Pilocarpine is classified as Pregnancy Category C. Animal reproduction studies have shown an adverse effect on the fetus, but there are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Minimal systemic absorption is expected with ophthalmic use.

Trimester-Specific Risks:

First Trimester: Potential risk based on animal data; minimal systemic absorption may limit risk.
Second Trimester: Potential risk based on animal data; minimal systemic absorption may limit risk.
Third Trimester: Potential risk based on animal data; minimal systemic absorption may limit risk.
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Lactation

It is not known whether pilocarpine is excreted in human milk. However, due to minimal systemic absorption following topical ocular administration, significant infant exposure is unlikely. Use with caution and monitor the infant for any signs of cholinergic effects (e.g., diarrhea, bradycardia).

Infant Risk: Low risk due to minimal systemic absorption.
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Pediatric Use

Safety and efficacy in pediatric patients have not been fully established for routine use in glaucoma. It may be used off-label for specific conditions like accommodative esotropia or congenital glaucoma under the supervision of a pediatric ophthalmologist. Children may be more susceptible to systemic side effects if significant absorption occurs.

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Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and younger patients. However, elderly patients may be more sensitive to the miotic effects and potential for reduced vision in dim light, which can increase the risk of falls. Systemic side effects are rare but may be more pronounced if they occur.

Clinical Information

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Clinical Pearls

  • Pilocarpine is a classic miotic agent, historically a first-line treatment for glaucoma, but its use has decreased due to side effects (miosis, accommodative spasm, brow ache) and the availability of newer, better-tolertolerated glaucoma medications.
  • It remains a crucial medication for acute angle-closure glaucoma to break pupillary block and facilitate aqueous outflow.
  • Patients should be thoroughly counseled on the potential for blurred vision and difficulty with night vision, especially when driving.
  • Proper instillation technique (nasolacrimal occlusion) is important to maximize local effect and minimize systemic absorption and side effects.
  • The 2% concentration is a common strength, but other concentrations (e.g., 1%, 4%) are also available and may be used depending on patient response and tolerance.
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Alternative Therapies

  • Prostaglandin analogs (e.g., latanoprost, travoprost, bimatoprost): Often first-line for open-angle glaucoma.
  • Beta-adrenergic blockers (e.g., timolol, betaxolol): Reduce aqueous humor production.
  • Alpha-adrenergic agonists (e.g., brimonidine, apraclonidine): Reduce aqueous humor production and increase uveoscleral outflow.
  • Carbonic anhydrase inhibitors (e.g., dorzolamide, brinzolamide, acetazolamide): Reduce aqueous humor production.
  • Rho kinase inhibitors (e.g., netarsudil): Increase outflow through the trabecular meshwork.
  • Combination 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, minimally invasive glaucoma surgery - MIGS).
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Cost & Coverage

Average Cost: Typically low cost (generic). Price varies by pharmacy and formulation (solution/gel). per 15ml bottle
Generic Available: Yes
Insurance Coverage: Generally covered by most insurance plans, often as a Tier 1 or Tier 2 medication.
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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 overdose, including the medication taken, the amount, and the time it occurred.