Apraclonidine is a medication primarily used in ophthalmology. It belongs to a class of drugs known as alpha-2 adrenergic agonists. These medications work by decreasing the production of aqueous humor in the eye, thereby reducing intraocular pressure. This makes apraclonidine useful in treating conditions such as glaucoma, where elevated intraocular pressure can lead to optic nerve damage and vision loss if left untreated.

• Similar to clonidine, apraclonidine is a strong alpha-adrenergic agonist.
• It reduces the formation of aqueous humor and penetrates the blood-brain barrier less avidly than clonidine.

It is used to reduce intraocular pressure.

• For individuals who need a temporary further decrease in intraocular pressure, the 0.5% solution is utilised as a supplementary treatment.

Apraclonidine Dose in Adult

Apraclonidine Dose in the treatment of Elevated intraocular pressure:

It's mainly used for open-angle glaucoma.

• You put 1 to 2 drops in the affected eye(s) three times a day.

Off-label usage for angle-closure glaucoma (1% solution):

• You would use the 1% concentration, putting 1 drop into the affected eye.
• If the eye pressure remains high after 30 to 60 minutes, you may repeat the dose.
• This is usually done as part of a four-drug treatment plan.

Note: It's important to note that this use is typically reserved for emergency situations when you can't see an eye specialist for at least an hour.

Prevention and treatment of postsurgical IOP elevation (1% solution):

• You can use apraclonidine 1%.
• Before anterior segment laser surgery, put 1 drop into the eye undergoing surgery one hour before the procedure.
• Then, immediately after the surgery, put another drop into the same eye.
• This helps to control the pressure inside the eye and reduce the risk of complications after surgery.

Apraclonidine Dose in Children

 Not recommended for use in children.

Apraclonidine Risk Category in Pregnancy: Not assigned

• Using eye medications during pregnancy could potentially cause problems for the baby, as shown in studies with animals.
• If you must use eye drops while pregnant, try to use the smallest amount needed.
• Also, consider using a method to block the tear ducts temporarily to reduce how much of the medication gets into your system and possibly affects the baby.

Breastfeeding:

• We're not sure if apraclonidine passes into breast milk.
• The manufacturer suggests being cautious if you're breastfeeding and need to use apraclonidine 0.5%.
• They also recommend stopping breastfeeding on the day you use apraclonidine 1%.
• This is to minimize any potential risk to the baby.

Apraclonidine Dose in Renal Disease:

• The manufacturer doesn't give specific dose adjustments for different situations.
• However, it's essential to keep a close eye on cardiovascular (heart-related) factors when using the medication.
• If a person has chronic kidney failure, use apraclonidine cautiously.
• Always monitor for any changes in their condition.

Apraclonidine Dose in Liver Disease:

• The manufacturer doesn't specify any dosage adjustments for people with liver problems.
• However, it's crucial to closely monitor cardiovascular parameters, especially in such cases.
• Any changes in heart-related factors should be carefully noted and addressed as needed.

Common Side Effects of Apraclonidine Include:

• Ophthalmic:
  • Ocular hyperemia
  • Eye discomfort
  • Eye pruritus
• Gastrointestinal:
  • Xerostomia

Less Common Side Effects of Apraclonidine Include:

• Cardiovascular:
  • Facial edema
  • Peripheral edema
  • Cardiac arrhythmia
  • Chest pain
  • Localized blanching
• Dermatologic:
  • Contact dermatitis
  • Dermatitis
• Central nervous system:
  • Headache
  • Insomnia
  • Dizziness
  • Drowsiness
  • Malaise
  • Nervousness
  • Altered sense of smell
  • Ataxia
  • Depression
  • Paresthesia
• Neuromuscular & skeletal:
  • Myalgia
  • Weakness
• Gastrointestinal:
  • Constipation
  • Dysgeusia
  • Nausea
• Respiratory:
  • Pharyngitis
  • Rhinitis
  • Asthma
  • Dry nose
  • Dyspnea
• Ophthalmic:
  • Eyelid edema
  • Eye discharge
  • Blurred vision
  • Conjunctivitis
  • Dry eye syndrome
  • Foreign body sensation of eye
  • Lacrimation

Contraindication to Apraclonidine Include:

• Apraclonidine should not be used if someone is allergic to apraclonidine, clonidine, or any ingredients in the formulation. It's also not safe to use apraclonidine if someone is taking MAO inhibitors (a type of antidepressant) at the same time.
• In Canada, additional precautions advise against using apraclonidine in children and adolescents under 18 years old.

Warnings and Precautions

CNS effects

• Apraclonidine can cause dizziness and drowsiness, which might make it unsafe to perform tasks that need full mental alertness, like driving or operating machinery.
• Patients should be warned about this and advised to avoid such activities until they know how the medication affects them.

Hypersensitivity reactions

• Using apraclonidine can sometimes cause allergic-like reactions such as redness, itching, discomfort, tearing, feeling like there's something in the eye, and swelling of the eyelid and the thin layer covering the eye.
• If these symptoms happen, stop using the medication and talk to your doctor.

Cardiovascular disease

• Apraclonidine should be used cautiously in individuals with severe uncontrolled cardiovascular diseases like high blood pressure (hypertension), coronary insufficiency (problems with blood flow to the heart), recent heart attacks, cerebrovascular diseases (related to blood vessels in the brain), Raynaud disease (a condition affecting blood flow to the extremities), and thromboangiitis obliterans (a type of blood vessel inflammation).
• It's important to monitor these patients closely while using apraclonidine.

Hepatic impairment

• Patients with hepatic (liver) impairment should be closely monitored for changes in cardiovascular parameters while using apraclonidine.
• Clonidine, which is structurally related to apraclonidine and is administered systemically, undergoes partial metabolism in the liver.
• Therefore, caution is advised, and careful observation is necessary when using apraclonidine in individuals with liver issues.

Vasovagal reactions

• Apraclonidine may increase the risk of vasovagal reactions, which can cause a sudden drop-in heart rate and blood pressure, leading to fainting.
• Therefore, it should be used cautiously in patients with a history of vasovagal reactions.

Renal impairment

• Patients with renal (kidney) impairment should have their cardiovascular parameters closely monitored when using apraclonidine.
• Caution is advised, especially in patients with chronic renal failure.
• While topical apraclonidine specifically hasn't been studied in patients with renal impairment, it's important to note that clonidine, which is structurally similar to apraclonidine and is administered systemically, has a significantly increased half-life in severe renal impairment.
• Therefore, using apraclonidine cautiously and monitoring patients closely is recommended in this population.

Apraclonidine: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitor:

Exaggerated Reductions in Intraocular Pressure:

• Keep a close eye on patients who experience significant drops in eye pressure.

Visual Fields for Glaucoma Patients:

• Periodically check visual fields, especially for glaucoma patients using the 0.5% solution to delay surgery.

Tachyphylaxis:

• Be aware of the potential for reduced effectiveness over time with continued use.

Cardiovascular Parameters in Renal and/or Hepatic Impairment:

• Monitor cardiovascular health carefully, especially in patients with kidney or liver problems.

Depression in Depressed Patients:

• Pay attention to any signs of depression in patients who are already depressed.

Specific Checks for Acute Angle-Closure Glaucoma:

• After using the 1% solution for acute angle-closure glaucoma, check eye pressure 30 to 60 minutes later.

How to administer Apraclonidine?

Usage Instructions for Apraclonidine Eye Drops

For Topical Ophthalmic Use Only:

• Do not inject or swallow.

0.5% Solution:

• Wait 5 minutes between using other eye drops to prevent washing away the previous dose.
• After applying the drops, press gently on the inner corner of the eye to reduce drainage and minimize absorption into the body.

1% Solution:

• Use a fresh container for each drop and throw away after use.
• When treating acute angle-closure glaucoma, wait at least 1 minute between administering other eye medications.

Mechanism of action of Apraclonidine:

• Apraclonidine is a strong alpha-adrenergic agent, much like clonidine.
• It primarily targets alpha-receptors, though it still binds to some beta-receptors.
• This interaction leads to a decrease in the production of aqueous humor in the eye.
• Unlike clonidine, apraclonidine is less likely to cross the blood-brain barrier, meaning its effects are more focused on the peripheral areas rather than the central nervous system.
• This suggests that its actions are mainly at the site of application rather than affecting the entire body.

Onset of Action:

• It typically takes about 1 hour to start working.

Peak Effect:

• The maximum decrease in intraocular pressure occurs around 3 to 5 hours after administration.

Half-life Elimination (Systemic) for 0.5% Solution:

• The time it takes for half of the medication to be eliminated from the body systemically is about 8 hours.

International Brands of Apraclonidine:

• Alfadrops
• Chen Ze
• Instaprine
• Iopidine
• Iopimax

Apraclonidine Brands in Pakistan:

No brands are available in Pakistan.