Apraclonidine 0.5% Ophth Sol 10ml
It is used to lower high eye pressure.
Drug Class
Antiglaucoma Agent
Pharmacologic Class
Alpha-2 Adrenergic Agonist
Pregnancy 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, which can damage your vision. It works by reducing the amount of fluid your eye makes. It's often used for a short time, especially around eye surgery, or as an add-on treatment for glaucoma when other medicines aren't enough.
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, eyelid, 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 safe 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.
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, eyelid, 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 safe 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.
Lifestyle & Tips
- Do not touch the dropper tip to any surface, including your eye, to avoid contamination.
- Wash hands thoroughly before and after using eye drops.
- 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.
- Be aware of potential for drowsiness or dizziness, especially when starting treatment; avoid driving or operating machinery if affected.
- Report any new or worsening eye symptoms, or systemic side effects, to your doctor.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
1 drop in the affected eye(s) three times daily (for long-term IOP control) or 1 drop immediately before and 1 drop 5 minutes after laser surgery (for acute IOP control).
Condition-Specific Dosing:
openAngleGlaucoma_OcularHypertension:
1 drop in the affected eye(s) three times daily. Due to tachyphylaxis, this is typically for short-term adjunctive therapy.
postLaserIOPSpikePrevention:
1 drop in the affected eye(s) one hour prior to laser surgery, followed by 1 drop immediately after surgery. Alternatively, 1 drop immediately before and 1 drop 5 minutes after laser surgery.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established (safety and efficacy not established; use with caution due to potential for systemic side effects like bradycardia, hypotension, somnolence)
Adolescent:
Not established (safety and efficacy not established; use with caution due to potential for systemic side effects)
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended for ophthalmic use due to minimal systemic absorption.
Moderate:
No specific adjustment recommended for ophthalmic use due to minimal systemic absorption.
Severe:
No specific adjustment recommended for ophthalmic use due to minimal systemic absorption.
Dialysis:
No specific adjustment recommended for ophthalmic use due to minimal systemic absorption.
Hepatic Impairment:
Mild:
No specific adjustment recommended for ophthalmic use due to minimal systemic absorption.
Moderate:
No specific adjustment recommended for ophthalmic use due to minimal systemic absorption.
Severe:
No specific adjustment recommended for ophthalmic use due to minimal systemic absorption.
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 have a minor effect on increasing uveoscleral outflow.
Pharmacokinetics
Absorption:
Bioavailability:
Not available (systemic absorption is minimal after topical ocular administration)
Tmax:
Not available (systemic Tmax not clinically relevant for ophthalmic use)
FoodEffect:
Not applicable (ophthalmic administration)
Distribution:
Vd:
Not available (systemic Vd not clinically relevant for ophthalmic use)
ProteinBinding:
Not available (systemic protein binding not clinically relevant for ophthalmic use)
CnssPenetration:
Limited (minimal systemic absorption, but can cause CNS effects if absorbed)
Elimination:
HalfLife:
Approximately 8 hours (systemic, after oral administration; not directly applicable to ophthalmic use where systemic levels are very low)
Clearance:
Not available (systemic clearance not clinically relevant for ophthalmic use)
ExcretionRoute:
Renal (primarily unchanged)
Unchanged:
High percentage (systemically, if absorbed)
Pharmacodynamics
OnsetOfAction:
Within 1 hour (IOP reduction)
PeakEffect:
3-5 hours (IOP reduction)
DurationOfAction:
Up to 12 hours (IOP reduction)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
While rare, some people may experience severe and potentially life-threatening side effects when 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
Eyelid swelling
Eye discharge
Feeling that something is in the eye
Other Possible Side Effects
As with all medications, some people may experience side effects. Although many individuals have no 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 that bother you or persist, contact your doctor for guidance:
Blurred eyesight
Eye irritation
Dry eyes
Dry mouth
Excessive tearing
* Dizziness or drowsiness
Reporting Side Effects
This list is not exhaustive, and you may experience other 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.
While rare, some people may experience severe and potentially life-threatening side effects when 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
Eyelid swelling
Eye discharge
Feeling that something is in the eye
Other Possible Side Effects
As with all medications, some people may experience side effects. Although many individuals have no 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 that bother you or persist, contact your doctor for guidance:
Blurred eyesight
Eye irritation
Dry eyes
Dry mouth
Excessive tearing
* Dizziness or drowsiness
Reporting Side Effects
This list is not exhaustive, and you may experience other 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
- Significant eye redness or irritation that worsens
- Swelling of eyelids or around the eye
- Blurred vision or vision changes
- Signs of allergic reaction (e.g., severe itching, rash, hives, difficulty breathing)
- Excessive drowsiness or dizziness
- Very slow heart rate or feeling faint
Before Using This Medicine
Before taking this medication, it is essential to inform your doctor about the following:
Any allergies you have, including allergies to this drug, its components, or other substances, such as foods or medications. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you are currently taking certain medications for depression, including isocarboxazid, phenelzine, or tranylcypromine, or medications for Parkinson's disease, such as selegiline or rasagiline.
If you are taking linezolid or methylene blue, as these medications may interact with this drug.
Please note that this is not an exhaustive list of all potential drug interactions or health problems that may be relevant to your treatment with this medication. Therefore, it is crucial to inform your doctor and pharmacist about all your medications, including:
Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
Your doctor and pharmacist will help you determine whether it is safe to take this medication with your existing medications and health conditions. Do not initiate, discontinue, or modify the dose of any medication without first consulting your doctor to ensure your safety.
Any allergies you have, including allergies to this drug, its components, or other substances, such as foods or medications. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you are currently taking certain medications for depression, including isocarboxazid, phenelzine, or tranylcypromine, or medications for Parkinson's disease, such as selegiline or rasagiline.
If you are taking linezolid or methylene blue, as these medications may interact with this drug.
Please note that this is not an exhaustive list of all potential drug interactions or health problems that may be relevant to your treatment with this medication. Therefore, it is crucial to inform your doctor and pharmacist about all your medications, including:
Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
Your doctor and pharmacist will help you determine whether it is safe to take this medication with your existing medications and health conditions. Do not initiate, discontinue, or modify the dose of any medication without first consulting your doctor to ensure your safety.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Before operating a vehicle or engaging in any activity that requires alertness and clear vision, wait until you understand how this drug affects you.
Do not exceed the prescribed duration of treatment, and only use this medication for the length of time specified by your doctor.
Regularly schedule check-ups with your doctor to monitor your eye pressure and vision, as advised.
Prior to consuming alcohol, marijuana, or other cannabis products, or taking prescription or over-the-counter medications that may impair your reactions, consult with your doctor.
If you are pregnant, planning to become pregnant, or are breastfeeding, discuss the potential benefits and risks of this medication with your doctor to determine the best course of action for you and your baby.
Before operating a vehicle or engaging in any activity that requires alertness and clear vision, wait until you understand how this drug affects you.
Do not exceed the prescribed duration of treatment, and only use this medication for the length of time specified by your doctor.
Regularly schedule check-ups with your doctor to monitor your eye pressure and vision, as advised.
Prior to consuming alcohol, marijuana, or other cannabis products, or taking prescription or over-the-counter medications that may impair your reactions, consult with your doctor.
If you are pregnant, planning to become pregnant, or are breastfeeding, discuss the potential benefits and risks of this medication with your doctor to determine the best course of action for you and your baby.
Overdose Information
Overdose Symptoms:
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Somnolence (drowsiness)
- Lethargy
- Sedation
- Miosis (constricted pupils)
- Hypothermia
- Respiratory depression
- Apnea (especially in infants/children)
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Treatment is supportive and symptomatic; maintain airway, breathing, and circulation. Atropine may be considered for bradycardia.
Drug Interactions
Major Interactions
- Monoamine Oxidase Inhibitors (MAOIs): Potential for enhanced hypotensive effects and/or CNS depression. Use with extreme caution or avoid.
- Tricyclic Antidepressants (TCAs): May blunt the hypotensive effect of apraclonidine.
Moderate Interactions
- CNS Depressants (e.g., alcohol, barbiturates, opioids, sedatives, anesthetics): Additive or potentiated CNS depressant effects (e.g., somnolence, dizziness).
- Cardiovascular Medications (e.g., beta-blockers, calcium channel blockers, cardiac glycosides, other antihypertensives): Potential for additive hypotensive or bradycardic effects.
- Other Alpha-Adrenergic Agonists (e.g., oral clonidine): Potential for additive systemic effects (e.g., hypotension, bradycardia, sedation).
Monitoring
Baseline Monitoring
Intraocular Pressure (IOP)
Rationale: To establish baseline and assess efficacy of treatment.
Timing: Prior to initiation of therapy.
Ocular examination (e.g., slit lamp, visual acuity)
Rationale: To assess overall ocular health and identify any pre-existing conditions.
Timing: Prior to initiation of therapy.
Routine Monitoring
Intraocular Pressure (IOP)
Frequency: Regularly, as determined by ophthalmologist (e.g., at follow-up visits, after laser surgery).
Target: Individualized target IOP.
Action Threshold: If IOP is not adequately controlled or if there is a significant increase.
Ocular adverse effects (e.g., ocular discomfort, itching, hyperemia, dry mouth)
Frequency: At each follow-up visit and patient self-monitoring.
Target: Absence of severe or intolerable symptoms.
Action Threshold: If symptoms are severe, persistent, or indicate allergic reaction.
Systemic adverse effects (e.g., somnolence, dizziness, dry mouth, fatigue)
Frequency: At each follow-up visit and patient self-monitoring.
Target: Absence of severe or intolerable symptoms.
Action Threshold: If symptoms are severe, persistent, or impact quality of life.
Symptom Monitoring
- Ocular discomfort
- Ocular itching
- Ocular hyperemia (redness)
- Dry mouth
- Somnolence (drowsiness)
- Dizziness
- Fatigue
- Headache
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Allergic conjunctivitis (ocular itching, redness, lid edema)
Special Patient Groups
Pregnancy
Category C. Animal studies have shown adverse effects on the fetus, but there are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential risk based on animal data; human data lacking.
Second Trimester:
Potential risk based on animal data; human data lacking.
Third Trimester:
Potential risk based on animal data; human data lacking. Consider potential for systemic effects in neonate if significant absorption occurs.
Lactation
L3 (Moderately Safe). It is not known whether apraclonidine is excreted in human milk. Due to the potential for serious adverse reactions in nursing infants from alpha-2 adrenergic agonists, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Minimal systemic absorption suggests low risk, but caution is advised.
Infant Risk:
Low to moderate risk. Potential for systemic effects (e.g., bradycardia, hypotension, sedation) in the infant, especially if significant amounts are absorbed by the mother or if the infant is premature/has underlying conditions.
Pediatric Use
Safety and efficacy have not been established in pediatric patients. Use in children, especially infants, is generally not recommended due to the potential for serious systemic adverse effects such as bradycardia, hypotension, and somnolence, which can lead to apnea. If used, extreme caution and close monitoring are required.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients. However, elderly patients may be more susceptible to systemic adverse effects (e.g., dizziness, somnolence, dry mouth) due to potential for increased sensitivity or comorbidities. Use with caution and monitor for systemic effects.
Clinical Information
Clinical Pearls
- Apraclonidine is primarily used for short-term IOP control, especially around laser surgery, or as adjunctive therapy for glaucoma due to the potential for tachyphylaxis (diminished response over time) with long-term use.
- Patients may develop an allergic-like reaction (ocular itching, hyperemia, lid edema) with chronic use, which can necessitate discontinuation.
- Systemic side effects like dry mouth, somnolence, and dizziness are common, even with ophthalmic administration, due to some systemic absorption.
- Caution is advised in patients with severe cardiovascular disease, renal impairment, or cerebrovascular disease due to potential for systemic effects.
- Educate patients on proper instillation technique to minimize systemic absorption and maximize local effect.
Alternative Therapies
- Beta-blockers (e.g., timolol, betaxolol)
- Prostaglandin analogs (e.g., latanoprost, travoprost, bimatoprost)
- Carbonic anhydrase inhibitors (e.g., dorzolamide, brinzolamide)
- Alpha-adrenergic agonists (e.g., brimonidine - another alpha-2 agonist, often preferred for long-term use over apraclonidine due to less tachyphylaxis)
- Rho kinase inhibitors (e.g., netarsudil)
- Cholinergic agonists (e.g., pilocarpine)
- Combination products (e.g., timolol/dorzolamide, timolol/brimonidine)
Cost & Coverage
Average Cost:
Varies, typically $50-$150 per 10ml bottle
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (often preferred generic)
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 details. 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 information about the medication taken, the amount, and the time it happened.