Apraclonidine 0.5% Opth Sol 5ml
It is used to lower high eye pressure.
Drug Class
Antiglaucoma Agent, Ophthalmic Alpha-Adrenergic Agonist
Pharmacologic Class
Alpha-2 Adrenergic Agonist
Pregnancy Category
Category C
FDA Approved
Oct 1987
DEA Schedule
Not Controlled
Overview
What is this medicine?
Apraclonidine is an eye drop used to lower high pressure inside the eye. It works by reducing the amount of fluid your eye makes. It's often used for a short time to help manage glaucoma or to prevent pressure spikes after certain eye laser surgeries.
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.
Administration Instructions
1. Remove your contact lenses before using this medication. You can put them back in 15 minutes after administration, unless your eyes are irritated or infected.
2. Avoid touching the container tip to your eye, lid, or surrounding skin, as this can introduce bacteria into the medication and potentially cause severe eye problems or vision loss.
3. Tilt your head back and gently drop the medication into your eye.
4. If you are using multiple medications in the same eye, administer each one at least 5 minutes apart.
Storage and Disposal
Store this medication at room temperature, away from light and freezing temperatures. Keep all medications in a secure location, out of the reach of children and pets.
Missed Dose Instructions
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 take two doses at the same time or use extra doses.
To use this medication correctly, follow your doctor's instructions and read all the information provided. This medication is for eye use only.
Administration Instructions
1. Remove your contact lenses before using this medication. You can put them back in 15 minutes after administration, unless your eyes are irritated or infected.
2. Avoid touching the container tip to your eye, lid, or surrounding skin, as this can introduce bacteria into the medication and potentially cause severe eye problems or vision loss.
3. Tilt your head back and gently drop the medication into your eye.
4. If you are using multiple medications in the same eye, administer each one at least 5 minutes apart.
Storage and Disposal
Store this medication at room temperature, away from light and freezing temperatures. Keep all medications in a secure location, out of the reach of children and pets.
Missed Dose Instructions
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 take two doses at the same time or use extra doses.
Lifestyle & Tips
- Wash hands thoroughly before applying eye drops.
- Tilt head back, pull down lower eyelid to form a pocket, and instill one drop into the pocket. Do not touch the dropper tip to the eye or any other surface.
- Close eye gently for 1-2 minutes after instillation to allow the medication to be absorbed and to minimize systemic absorption.
- If using other eye drops, wait at least 5 minutes between applications.
- Remove contact lenses before instilling drops and wait at least 15 minutes before reinserting them.
- Do not discontinue use without consulting your doctor, even if you feel well, as high eye pressure often has no symptoms.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
For short-term adjunctive therapy in patients on maximally tolerated medical therapy for glaucoma: 1 drop in the affected eye(s) 3 times daily. For prevention/treatment of post-surgical intraocular pressure (IOP) spikes after anterior segment laser surgery: 1 drop in the affected eye 1 hour before laser surgery, then 1 drop immediately after surgery.
Condition-Specific Dosing:
glaucoma_adjunctive_therapy:
1 drop in affected eye(s) 3 times daily
post_laser_surgery_iop_spike:
1 drop 1 hour pre-op, 1 drop immediately post-op
Pediatric Dosing
Neonatal:
Contraindicated (risk of serious systemic adverse reactions including bradycardia, hypotension, hypothermia, CNS depression)
Infant:
Contraindicated (risk of serious systemic adverse reactions including bradycardia, hypotension, hypothermia, CNS depression)
Child:
Not established (safety and efficacy not established; generally not recommended due to potential for systemic effects)
Adolescent:
Not established (safety and efficacy not established; use with caution if considered)
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended due to minimal systemic absorption.
Moderate:
No specific adjustment recommended due to minimal systemic absorption.
Severe:
No specific adjustment recommended due to minimal systemic absorption; use with caution if systemic effects are a concern.
Dialysis:
No specific adjustment recommended due to minimal systemic absorption.
Hepatic Impairment:
Mild:
No specific adjustment recommended due to minimal systemic absorption.
Moderate:
No specific adjustment recommended due to minimal systemic absorption.
Severe:
No specific adjustment recommended due to minimal systemic absorption; use with caution if systemic effects are a concern.
Pharmacology
Mechanism of Action
Apraclonidine is a relatively selective alpha-2 adrenergic agonist. When applied topically to the eye, it reduces intraocular pressure (IOP) by decreasing aqueous humor production. It may also slightly increase uveoscleral outflow.
Pharmacokinetics
Absorption:
Bioavailability:
Minimal systemic absorption (less than 1%) after ocular instillation.
Tmax:
Peak plasma concentrations (in pg/mL range) occur within 1 hour after ocular instillation.
FoodEffect:
Not applicable for ophthalmic solution.
Distribution:
Vd:
Not extensively studied due to minimal systemic absorption.
ProteinBinding:
Not extensively studied due to minimal systemic absorption.
CnssPenetration:
Limited (minimal systemic absorption, but can cause CNS depression in infants/young children).
Elimination:
HalfLife:
Approximately 8 hours (for the small amount systemically absorbed).
Clearance:
Not well-defined due to minimal systemic absorption.
ExcretionRoute:
Primarily renal (for the systemically absorbed portion).
Unchanged:
High percentage of absorbed drug excreted unchanged.
Pharmacodynamics
OnsetOfAction:
Within 1 hour (IOP reduction).
PeakEffect:
3-5 hours (IOP reduction).
DurationOfAction:
Up to 12 hours (IOP reduction).
Confidence:
High
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
If you experience any of the following symptoms, call your doctor or seek medical attention immediately, as they may be signs of a severe and potentially life-threatening reaction:
- 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, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat
- Changes in vision, eye pain, or severe eye irritation
- Swelling of the eyelid
- Eye discharge
- A sensation of having something in the eye
Other Possible Side Effects
While many people taking this medication may not experience side effects or may only have mild ones, it's essential to be aware of the following:
- Blurred vision
- Eye irritation
- Dry eyes
- Dry mouth
- Excessive tearing
- Dizziness or drowsiness
If any of these side effects or any others bother you or do not go away, contact your doctor for advice.
Reporting Side Effects
This list does not include all possible side effects. 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.
If you experience any of the following symptoms, call your doctor or seek medical attention immediately, as they may be signs of a severe and potentially life-threatening reaction:
- 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, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat
- Changes in vision, eye pain, or severe eye irritation
- Swelling of the eyelid
- Eye discharge
- A sensation of having something in the eye
Other Possible Side Effects
While many people taking this medication may not experience side effects or may only have mild ones, it's essential to be aware of the following:
- Blurred vision
- Eye irritation
- Dry eyes
- Dry mouth
- Excessive tearing
- Dizziness or drowsiness
If any of these side effects or any others bother you or do not go away, contact your doctor for advice.
Reporting Side Effects
This list does not include all possible side effects. 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.
Seek Immediate Medical Attention If You Experience:
- Severe eye pain or discomfort that worsens.
- Significant changes in vision.
- Signs of an allergic reaction: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
- Persistent or severe dry mouth, fatigue, or dizziness.
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 are currently taking certain medications, such as:
+ Isocarboxazid, phenelzine, or tranylcypromine, which are used to treat depression
+ Selegiline or rasagiline, which are used to treat Parkinson's disease
+ Linezolid or methylene blue, as these may interact with this medication
This list is not exhaustive, and it is crucial to disclose all your medications, including:
+ Prescription and over-the-counter (OTC) drugs
+ Natural products
+ Vitamins
Additionally, inform your doctor about any existing health problems, as these may affect the safety of taking this medication.
To ensure your safety, it is vital to verify that this medication can be taken with all your current medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting 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 are currently taking certain medications, such as:
+ Isocarboxazid, phenelzine, or tranylcypromine, which are used to treat depression
+ Selegiline or rasagiline, which are used to treat Parkinson's disease
+ Linezolid or methylene blue, as these may interact with this medication
This list is not exhaustive, and it is crucial to disclose all your medications, including:
+ Prescription and over-the-counter (OTC) drugs
+ Natural products
+ Vitamins
Additionally, inform your doctor about any existing health problems, as these may affect the safety of taking this medication.
To ensure your safety, it is vital to verify that this medication can be taken with all your current medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Before engaging in activities that require alertness and clear vision, such as driving, wait until you understand how this drug affects you. Do not exceed the prescribed duration of treatment, and adhere to your doctor's instructions. Regularly schedule check-ups with your doctor to monitor your eye pressure and vision, as advised. Prior to consuming alcohol, marijuana, or other forms of cannabis, or taking prescription or over-the-counter (OTC) medications that may impair your reactions, consult with your doctor. If you are pregnant, planning to become pregnant, or breastfeeding, discuss the potential benefits and risks of this medication with your doctor to make an informed decision regarding you and your baby.
Overdose Information
Overdose Symptoms:
- Drowsiness
- Dizziness
- Dry mouth
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Hypothermia (low body temperature)
- Respiratory depression (especially in infants/young children)
What to Do:
If overdose is suspected, seek immediate medical attention or call a Poison Control Center (1-800-222-1222). Management is generally supportive and symptomatic.
Drug Interactions
Major Interactions
- Monoamine Oxidase Inhibitors (MAOIs): Concomitant use with MAOIs is not recommended due to potential for additive systemic effects (e.g., hypertensive crisis), although systemic absorption is minimal.
- Tricyclic Antidepressants (TCAs): May blunt the hypotensive effect of apraclonidine.
Moderate Interactions
- CNS Depressants (e.g., alcohol, barbiturates, opioids, sedatives, anesthetics): Potential for additive CNS depressant effects (drowsiness, dizziness) if systemic absorption occurs.
- Cardiovascular Medications (e.g., beta-blockers, calcium channel blockers, cardiac glycosides, antihypertensives): Potential for additive effects on blood pressure and heart rate, especially in patients with pre-existing cardiovascular disease, though systemic effects are rare with ophthalmic use.
Confidence Interactions
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess efficacy of treatment.
Timing: Before initiating therapy.
Ocular Examination
Rationale: To assess baseline ocular health and identify any pre-existing conditions.
Timing: Before initiating therapy.
Routine Monitoring
Intraocular Pressure (IOP)
Frequency: Regularly, as determined by the treating physician (e.g., at follow-up visits).
Target: Individualized, aiming for target IOP reduction.
Action Threshold: If IOP is not adequately controlled or if there is evidence of disease progression.
Ocular Adverse Effects
Frequency: At each follow-up visit and as reported by patient.
Target: Absence of significant irritation, hyperemia, itching, discomfort.
Action Threshold: Persistent or severe ocular irritation, allergic conjunctivitis, lid edema, or other significant ocular discomfort.
Systemic Adverse Effects
Frequency: At each follow-up visit and as reported by patient.
Target: Absence of significant dry mouth, fatigue, dizziness, headache.
Action Threshold: Persistent or severe systemic symptoms.
Symptom Monitoring
- Ocular discomfort (stinging, burning, itching, foreign body sensation)
- Ocular hyperemia (redness)
- Blurred vision
- Dry mouth
- Fatigue/Drowsiness
- Dizziness
- Headache
- Allergic conjunctivitis (ocular itching, tearing, lid edema, conjunctival hyperemia)
Special Patient Groups
Pregnancy
Pregnancy Category C. Apraclonidine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects at high doses.
Trimester-Specific Risks:
First Trimester:
Potential risk, use only if clearly needed.
Second Trimester:
Potential risk, use only if clearly needed.
Third Trimester:
Potential risk, use only if clearly needed; consider potential for systemic effects in neonate if significant absorption occurs.
Lactation
It is unknown whether apraclonidine is excreted in human milk. Caution should be exercised when apraclonidine is administered to a nursing woman. The decision to discontinue nursing or discontinue the drug should take into account the importance of the drug to the mother.
Infant Risk:
Low risk due to minimal systemic absorption, but potential for systemic effects (e.g., CNS depression, bradycardia) in the infant cannot be entirely ruled out, especially in premature or very young infants. Monitor infant for drowsiness, lethargy, or feeding difficulties.
Pediatric Use
Contraindicated in infants and young children due to the risk of serious systemic adverse reactions (e.g., bradycardia, hypotension, hypothermia, CNS depression). Safety and efficacy have not been established in older pediatric patients.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients. However, use with caution in elderly patients due to the potential for increased sensitivity to systemic effects, especially if they have underlying cardiovascular or cerebrovascular disease.
Clinical Information
Clinical Pearls
- Apraclonidine is primarily used for short-term management of IOP, particularly for preventing or treating acute IOP spikes after laser surgery, or as short-term adjunctive therapy in glaucoma patients.
- Tachyphylaxis (a rapid decrease in response to the drug) can occur with chronic use, limiting its long-term efficacy for glaucoma.
- While systemic absorption is minimal, patients should be advised about potential systemic side effects like dry mouth, fatigue, and dizziness, especially if they are sensitive to alpha-2 agonists or are on other CNS depressants.
- Proper instillation technique is crucial to maximize ocular absorption and minimize systemic absorption.
- Contraindicated in infants and young children due to significant risk of systemic adverse effects.
Alternative Therapies
- Prostaglandin analogs (e.g., latanoprost, travoprost, bimatoprost)
- Beta-blockers (e.g., timolol, betaxolol)
- Carbonic anhydrase inhibitors (e.g., dorzolamide, brinzolamide)
- Alpha-adrenergic agonists (e.g., brimonidine)
- Rho kinase inhibitors (e.g., netarsudil)
- Miotics (e.g., pilocarpine)
- Combination products (e.g., dorzolamide/timolol, brimonidine/timolol)
Cost & Coverage
Average Cost:
$50 - $150 per 5mL bottle
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is 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 it is a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, do not hesitate to discuss them with 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 overdose, including the medication taken, the amount, and the time it occurred.