Apraclonidine (Iopidine) - for the treatment of glaucoma

Apraclonidine is a potent alpha-adrenergic agonist similar to clonidine.
It reduces the formation of aqueous humor and penetrates the blood-brain barrier less avidly than clonidine.

It is used to reduce intraocular pressure.

The 0.5% solution is used for short-term as adjunctive therapy in patients who require an additional reduction in the intraocular pressure.
The 1% solution is used in the prevention and treatment of elevated intraocular pressure after surgery (following argon laser trabeculoplasty, argon laser iridotomy or Nd: YAG posterior capsulotomy or as part of a 4-drug medical management regimen in acute angle-closure glaucoma (when the ophthalmologist consult is delayed by one hour or more).

Apraclonidine Dose in Adults

Dose in the treatment of Elevated intraocular pressure:

Open-angle glaucoma (0.5% solution):
- Instill 1 - 2 drops into the affected eye thrice daily.
Angle-closure glaucoma as off-label use (1% solution):
- Instill a single drop into the affected eye as part of a 4 drug regimen.
- It may be repeated in 30 - 60 minutes if the intraocular pressure remains elevated (>40 mm Hg).

Note: Reserve medical management should be reserved for emergency situations when an assessment by an ophthalmologist will be delayed by 1 hour or more.

Prevention and treatment of postsurgical IOP elevation (1% solution):
- Instill one drop into the operative eye one hour prior to anterior segment laser surgery and a second drop in same eye immediately after the procedure.

Apraclonidine Dose in Childrens

Not recommended for use in children.

Apraclonidine Risk Category in Pregnancy: Not assigned

Animal reproduction studies have shown adverse outcomes for fetuses.
If used in pregnant women, the minimum effective dose should always be used.
This can be combined with other therapies such as punctual occlusion to reduce potential exposure to the foetus.

Breastfeeding:

Apraclonidine is a drug that can be used during pregnancy.
It is unknown if the drug can be absorbed into breast milk.
Manufacturer recommends breastfeeding mothers use apraclonidine 0.5% with caution.
Additionally, breastfeeding should be stopped immediately after apraclonidine 11% is administered.

Apraclonidine Dose in Renal Disease:

Adjustment in the dose has not been provided by the manufacturer, however, patients with cardiovascular status should be monitored closely.
It should be used with caution in patients with renal impairment.

Apraclonidine Dose in LIver Disease:

Adjustment in the dose has not been provided by the manufacturer, however, patients with cardiovascular status should be monitored closely.

Common Side Effects of Apraclonidine Include:

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

Less Common Side Effects of Apraclonidine Include:

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

Contraindication to Apraclonidine Include:

Allergy to clonidine, Apraclonidine or any other component of the formulation
Use MAO inhibitors in conjunction.
Children and adolescents younger than 18 years old.

Warnings and Precautions

CNS effects
- It can cause dizziness and somnolence, which may lead to impairment of mental or physical abilities.
- Patients who use heavy machinery or do tasks such as driving that require mental alertness must be warned about the dangers of this drug.
Hypersensitivity reactions
- It can cause allergic-like reactions such as hyperemia, pruritus and tearing, foreign body sensations, discomfort and edema of conjunctiva and lid. If severe symptoms occur, the treatment can be stopped.
Cardiovascular disease
- Patients with hypertension, heart disease, cerebral insufficiency or recent myocardial injury, Raynaud disease and cerebrovascular disease, Raynaud disease, Raynaud, Raynaud, Raynaud, Raynaud, and other cardiovascular conditions should be cautious about taking the drug.
Hepatic impairment
- In liver disease, which is characterized by partial hepatic metabolism, it is important to monitor your cardiovascular health.
Renal impairment
- For patients with chronic renal impairment, it is important to monitor their cardiovascular condition.
- Although topical administration of renal impairment has not yet been investigated, it should be noted that the half-life of the formulation when applied systemically is significantly higher in renal impairment.
Vasovagal reactions
- Patients with a history vasovagal reactions should not use it. It may cause a vasovagal attack.

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

Risk Factor C (Monitor therapy).
Tricyclic Antidepressants	Alpha2-Agonists (Ophthalmic) may have a less therapeutic effect.
Risk Factor D (Consider therapy modifications)
Mirtazapine	Alpha2-Agonists may have a lower antihypertensive effect. Management: Consider avoiding concurrent use. If you cannot avoid the combination, monitor for reduced effects of alpha2-agonists if mirtazapine dose is increased/initiated, or increased effects if mirtazapine dosage is decreased/reduced.
Risk Factor X (Avoid Combination)
Mianserin	Alpha2-Agonists (Ophthalmic) may have a less therapeutic effect.
Monoamine Oxidase Inhibitors	May increase the toxic/adverse effects of Apraclonidine. Monoamine Oxidase inhibitors may increase Apraclonidine's serum concentration.

Monitor:

Patients should be closely monitored for an exaggerated response (rapid reduction in the intraocular pressure)
Monitor visual fields periodically for glaucoma patients.
Monitor for tachyphylaxis.
Monitor the cardiovascular status in patients with renal and/or hepatic impairment
Observe features of worsening depression in depressed patients.
Monitor the intraocular pressure 30 - 60 minutes after the administration for acute use of 1% solution for acute angle-closure glaucoma.

How to administer Apraclonidine?

Ophthalmic solution:
- It should only be used for topical ophthalmic purposes only.
- It should not be taken orally or administered parenterally.
  - 0.5% solution:
    - To avoid washout of the previous dose, wait for at least 5 minutes between instillation of other ophthalmic agents.
    - To minimize possible systemic absorption and reduce the drainage into the nose after topical instillation, apply pressure with a finger to the lacrimal sac.
  - 1% solution:
    - A separate container should be used for each single drop dose.
    - The container should be discarded after each use.
    - Separate administration of other ophthalmic agents by at least one minute when treating acute angle-closure glaucoma.

Mechanism of action of Apraclonidine:

It is an alpha-adrenergic antagonist similar to Clonidine.
Although it is selective for alpha-2 receptors, it has some affinity for alpha-1 ones.
It decreases the formation and penetration of aqueous humor, as well as the blood-brain barrier more slowly than Clonidine.
This means that it acts via peripheral receptors and not through central effects.

It is a catalyst for actionapproximately one hour and thepeak effectIt is possible to lower intraocular pressure in as little as 3 to 5 hours. It has been used to reduce intraocular pressure.half-life eliminationAfter systemic administration for approximately 8 hours.