Phospholine Iodide 0.125% Oph Soln

Manufacturer FERA PHARMACEUTICALS Active Ingredient Echothiophate Iodide(ek oh THYE oh fate EYE oh dide) Pronunciation ek-oh-THYE-oh-fate EYE-oh-dide
It is used to lower high eye pressure. It is used to treat an eye problem where one or both eyes turn inward (esotropia).
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Drug Class
Antiglaucoma agent; Miotic
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Pharmacologic Class
Irreversible cholinesterase inhibitor
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Pregnancy Category
C
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FDA Approved
Jul 1959
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Phospholine Iodide is an eye drop that helps lower pressure inside the eye, often used for certain types of glaucoma or for crossed eyes (esotropia) in children. It works by making the pupil smaller and helping fluid drain better from the eye. Because it's a strong medicine, it's usually used when other treatments haven't worked.
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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. For optimal results, use this medication as directed.

Administration Instructions

This medication is for eye use only.
Before and after use, wash your hands thoroughly to prevent contamination.
Avoid touching the container tip to your eye, lid, or surrounding skin, as this can introduce bacteria into the medication, potentially leading to severe eye problems or vision loss.
Tilt your head back and gently drop the medication into your eye.
After administering the medication, 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.
Use a clean tissue or cloth to blot any excess solution from your eyelid.

Continuing Treatment

Continue using this medication as instructed, even if your symptoms improve.

Storage and Disposal

Before mixing, store the medication in the refrigerator.
After mixing, store the medication at room temperature. Do not refrigerate.
Discard any unused portion of the medication after 4 weeks.
Keep all medications in a secure location, out of the reach of children and pets.

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 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

  • Avoid driving or operating machinery, especially at night, until you know how the drops affect your vision (due to miosis and accommodative spasm).
  • Be aware of potential for brow ache or headache, especially when starting treatment.
  • Report any significant vision changes, eye pain, or systemic symptoms (nausea, diarrhea, muscle weakness) to your doctor immediately.
  • Do not touch the dropper tip to any surface to prevent contamination.
  • If you wear contact lenses, remove them before instilling drops and wait at least 15 minutes before reinserting them.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: Glaucoma: 1 drop of 0.03% to 0.125% solution once daily at bedtime. Accommodative Esotropia: 1 drop of 0.06% or 0.125% solution once daily at bedtime for 2-3 weeks, then reduce to 0.03% or 0.06% every other day or twice weekly.
Dose Range: 0.03 - 0.125 mg

Condition-Specific Dosing:

glaucoma: 1 drop of 0.03% to 0.125% solution once daily at bedtime.
accommodativeEsotropia: Initial: 1 drop of 0.06% or 0.125% solution once daily at bedtime for 2-3 weeks. Maintenance: 1 drop of 0.03% or 0.06% every other day or twice weekly.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Accommodative Esotropia: Initial: 1 drop of 0.06% or 0.125% solution once daily at bedtime for 2-3 weeks. Maintenance: 1 drop of 0.03% or 0.06% every other day or twice weekly.
Adolescent: Accommodative Esotropia: Initial: 1 drop of 0.06% or 0.125% solution once daily at bedtime for 2-3 weeks. Maintenance: 1 drop of 0.03% or 0.06% every other day or twice weekly.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment needed for ophthalmic use due to minimal systemic absorption.
Moderate: No specific adjustment needed for ophthalmic use due to minimal systemic absorption.
Severe: No specific adjustment needed for ophthalmic use due to minimal systemic absorption.
Dialysis: Considerations: No specific adjustment needed for ophthalmic use due to minimal systemic absorption. Monitor for systemic cholinergic effects if significant absorption occurs.

Hepatic Impairment:

Mild: No specific adjustment needed for ophthalmic use due to minimal systemic absorption.
Moderate: No specific adjustment needed for ophthalmic use due to minimal systemic absorption.
Severe: No specific adjustment needed for ophthalmic use due to minimal systemic absorption.

Pharmacology

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Mechanism of Action

Echothiophate iodide is an irreversible cholinesterase inhibitor. It inactivates acetylcholinesterase at the parasympathetic neuroeffector junctions, allowing acetylcholine to accumulate. This leads to sustained miosis, ciliary muscle contraction (accommodative spasm), and increased outflow of aqueous humor, thereby lowering intraocular pressure (IOP).
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Pharmacokinetics

Absorption:

Bioavailability: Not available (topical ophthalmic, minimal systemic absorption)
Tmax: Not available (local action)
FoodEffect: Not applicable (topical ophthalmic)

Distribution:

Vd: Not available (local action)
ProteinBinding: Not available (local action)
CnssPenetration: Limited (minimal systemic absorption, but can cross if absorbed)

Elimination:

HalfLife: Not available (local action, systemic half-life of cholinesterase inhibition is prolonged)
Clearance: Not available
ExcretionRoute: Not available (systemic elimination of metabolites)
Unchanged: Not available
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Pharmacodynamics

OnsetOfAction: Miosis: 10-30 minutes; IOP reduction: 4-8 hours
PeakEffect: Miosis: 2-4 hours; IOP reduction: 24 hours
DurationOfAction: Miosis: 1-4 weeks; IOP reduction: 24-48 hours (effects on cholinesterase can last for weeks)

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Attention Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical help right away:

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
Abnormal heartbeat, including fast, slow, or irregular rhythms
Diarrhea
Loss of bladder control
Excessive saliva production
Muscle weakness
Excessive sweating
Shortness of breath

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 symptoms that bother you or persist, contact your doctor for guidance:

Eye irritation
Burning or stinging sensations
Excessive tearing
Eye redness
Blurred vision
Eyelid twitching
Headache

Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult 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:

  • Sudden decrease in vision or vision loss
  • New or worsening eye pain
  • Signs of retinal detachment (flashes of light, new floaters, curtain-like vision loss)
  • Severe brow ache or headache
  • Systemic symptoms such as nausea, vomiting, diarrhea, excessive sweating, muscle weakness, or slow heart rate (bradycardia)
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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 been diagnosed with narrow-angle glaucoma, a condition that affects the eyes.
* If you have swelling in certain parts of the eye, as this may be relevant to your treatment.

This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication in combination with your other medications and health conditions.

Remember, do not start, stop, or change 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 performing tasks that require clear vision, such as driving, exercise caution to ensure your safety. Regularly schedule check-ups with your doctor to monitor your eye pressure and vision, as advised. If you are exposed to certain insecticides and pesticides, you may be more susceptible to side effects. To minimize risks, wear a breathing mask, frequently wash and change your clothes, and consult with your doctor. When administering this medication to children, do so with caution, as they may be more prone to certain side effects. If you are pregnant, planning to become pregnant, or breastfeeding, notify your doctor to discuss the potential benefits and risks to both you and your baby.
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Overdose Information

Overdose Symptoms:

  • Exaggerated cholinergic effects: severe miosis, accommodative spasm, brow ache, headache, nausea, vomiting, diarrhea, abdominal cramps, excessive sweating, salivation, lacrimation, bradycardia, hypotension, muscle weakness, respiratory depression.

What to Do:

Discontinue drug. Systemic cholinergic crisis may require atropine sulfate (systemic) and/or pralidoxime chloride (2-PAM). For ocular symptoms, topical atropine may be used. Call 1-800-222-1222 (Poison Control) or seek immediate medical attention.

Drug Interactions

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Major Interactions

  • Succinylcholine (prolonged neuromuscular blockade due to inhibition of plasma cholinesterase)
  • Other cholinesterase inhibitors (e.g., donepezil, rivastigmine, galantamine - increased risk of systemic cholinergic effects)
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Moderate Interactions

  • Systemic anticholinergic agents (may antagonize effects)
  • Topical ophthalmic anticholinergic agents (may antagonize miotic effect)

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, including potential for accommodative spasm or cataract formation.

Timing: Prior to initiation of therapy.

Slit-lamp examination

Rationale: To assess lens status (for cataracts), iris cysts, and anterior chamber depth.

Timing: Prior to initiation of therapy.

Funduscopic examination

Rationale: To assess optic nerve and retina, especially for retinal detachment risk.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Intraocular Pressure (IOP)

Frequency: Regularly, as determined by ophthalmologist (e.g., every 1-4 weeks initially, then every 3-6 months)

Target: Individualized target IOP based on glaucoma severity.

Action Threshold: If IOP is not adequately controlled or increases, consider dose adjustment or alternative therapy.

Visual Acuity

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

Target: Stable or improved

Action Threshold: Significant decrease in vision, especially if associated with cataract formation.

Slit-lamp examination

Frequency: Every 3-6 months or as clinically indicated

Target: No new cataracts, stable iris cysts

Action Threshold: Development or progression of cataracts, significant iris cysts.

Plasma cholinesterase levels (if systemic toxicity suspected or prior to surgery with succinylcholine)

Frequency: As needed

Target: Normal range

Action Threshold: Significantly depressed levels.

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Symptom Monitoring

  • Blurred vision (especially at night or with accommodative spasm)
  • Brow ache or headache
  • Increased tearing
  • Redness or irritation of the eye
  • Systemic cholinergic symptoms: nausea, vomiting, diarrhea, abdominal cramps, bradycardia, sweating, muscle weakness (rare with ophthalmic use but possible with excessive absorption)

Special Patient Groups

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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 is minimal, but potential for systemic effects on the fetus cannot be entirely ruled out.

Trimester-Specific Risks:

First Trimester: Potential for fetal harm based on animal data; avoid if possible.
Second Trimester: Potential for fetal harm based on animal data; avoid if possible.
Third Trimester: Potential for fetal harm based on animal data; avoid if possible.
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Lactation

L3 (Moderately Safe). It is not known whether echothiophate iodide is excreted in human milk. Due to minimal systemic absorption, excretion into breast milk is likely low. However, caution should be exercised, and the infant should be monitored for cholinergic effects.

Infant Risk: Low to moderate risk. Potential for cholinergic effects in the infant if significant systemic absorption occurs in the mother and drug is excreted in milk. Monitor for diarrhea, bradycardia, or excessive salivation.
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Pediatric Use

Used for accommodative esotropia in children. Close monitoring for side effects such as iris cysts and cataract formation is crucial. Risk of retinal detachment may be higher in myopic children.

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Geriatric Use

Increased risk of cataract formation. Use with caution in elderly patients, especially those with pre-existing lens opacities. Monitor closely for visual changes and cataract progression.

Clinical Information

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Clinical Pearls

  • Echothiophate iodide is a potent, long-acting, irreversible cholinesterase inhibitor, typically reserved for cases of glaucoma or accommodative esotropia unresponsive to other therapies due to its significant side effect profile.
  • The most common and serious ocular side effects include cataract formation (especially in adults), iris cysts (more common in children), and retinal detachment (especially in myopic patients).
  • Systemic absorption, though minimal, can lead to systemic cholinergic effects, particularly if plasma cholinesterase levels are low (e.g., due to genetic deficiency or liver disease).
  • Patients should be warned about potential for dim vision, especially at night, due to profound miosis.
  • Prior to any surgery requiring succinylcholine, patients should inform their anesthesiologist about echothiophate use, as it can prolong neuromuscular blockade.
  • Discontinuation of the drug may be necessary several weeks before surgery if succinylcholine is planned, to allow plasma cholinesterase levels to recover.
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Alternative Therapies

  • For Glaucoma: Prostaglandin analogs (e.g., latanoprost, travoprost), Beta-blockers (e.g., timolol), Alpha-adrenergic agonists (e.g., brimonidine), Carbonic anhydrase inhibitors (e.g., dorzolamide, brinzolamide), Pilocarpine (reversible miotic).
  • For Accommodative Esotropia: Atropine penalization, Bifocal spectacles, Vision therapy, Surgical correction.
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Cost & Coverage

Average Cost: Not readily available (older, less common drug, often compounded or limited availability) per 5 mL bottle
Generic Available: Yes
Insurance Coverage: Tier 3 or Non-preferred (if covered, often requires prior authorization due to specialty nature or availability)
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General Drug Facts

If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea 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 emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.