Apraclonidine (Monograph)

Brand name: Iopidine
Drug class: EENT Drugs, Miscellaneous
ATC class: S01EA03
VA class: OP900
Molecular formula: C₉H₁₀Cl₂N₄•HCl
CAS number: 73218-79-8

Medically reviewed by Drugs.com on Sep 12, 2023. Written by ASHP.

Introduction

Relatively selective α₂-adrenergic agonist; imidazoline-derivative sympathomimetic amine.

Uses for Apraclonidine

Inhibition of Perioperative IOP Increases

Apraclonidine 1% is used prophylactically to prevent or reduce intraoperative and postoperative increases in intraocular pressure (IOP) before and after ocular laser surgery (e.g., argon laser trabeculoplasty, argon laser iridotomy, neodymium yttrium aluminum garnet [Nd:YAG] laser posterior capsulotomy).

Glaucoma

Apraclonidine 0.5% is used for short-term (<1 month) adjunctive therapy in patients with open-angle glaucoma receiving maximally tolerated drug therapy (i.e., a topical β-adrenergic blocking agent in conjunction with a systemically administered carbonic anhydrase inhibitor and a sympathomimetic and/or a parasympathomimetic agent) who require additional reduction in IOP.

Apraclonidine Dosage and Administration

Administration

For topical ophthalmic use only. Not for injection or oral use.

Ophthalmic Administration

Apply topically to the affected eye(s) as an ophthalmic solution.

Avoid contamination of the solution container.

If more than one topical ophthalmic drug is used, administer the drugs at least 5 minutes apart.

1% solution is for single use only; use a separate container for each single-drop dose of 1% solution and discard each container after use.

Dosage

Available as apraclonidine hydrochloride; dosage expressed in terms of apraclonidine.

Adults

Inhibition of Perioperative IOP Increases

Ophthalmic

Apraclonidine 1% solution: 1 drop in the eye undergoing surgery 1 hour before surgery; instill 1 drop in the same eye immediately upon completion of surgery.

Glaucoma

Ophthalmic

Apraclonidine 0.5% solution: 1 or 2 drops in the affected eye(s) 3 times daily. Benefit of therapy for most patients is <1 month. (See Tachyphylaxis under Cautions.)

Special Populations

No special population dosage recommendations at this time.

Related/similar drugs

acetazolamide, pilocarpine ophthalmic, Diamox, Combigan, mitomycin ophthalmic, carbachol ophthalmic, Nevanac

Cautions for Apraclonidine

Contraindications

Concomitant use with an MAO inhibitor. (See Specific Drugs under Interactions.)

Known hypersensitivity to apraclonidine, clonidine, or to any ingredient in the formulation.

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity Reactions

Topical hypersensitivity reactions (e.g., hyperemia, pruritus, discomfort, tearing, foreign body sensation, eyelid swelling) reported. If hypersensitivity reaction occurs, discontinue apraclonidine.

General Precautions

Systemic Effects

Perioperative use of apraclonidine hydrochloride ophthalmic solution to date has been associated with a low potential for causing adverse systemic effects; however, continuous (e.g., up to 12 weeks) use of apraclonidine ophthalmic solution has been associated with a higher incidence of adverse systemic effects.

Cardiovascular Effects

Possible adverse cardiovascular effects (e.g., bradycardia, chest heaviness or burning, palpitation, reduced systolic and diastolic BP, orthostatic hypotension).

Use with caution in patients with severe uncontrolled cardiac disease (e.g., hypertension), coronary insufficiency, recent MI, cerebrovascular disease, Raynaud’s disease, or thromboangitis obliterans.

Use with caution in patients with a history of vasovagal attacks; possible vasovagal attacks during laser surgery.

Depressive Episodes

Carefully supervise patients with a history of mental depression; may be subject to further depressive episodes.

CNS Effects

Possible dizziness and somnolence; performance of activities requiring mental alertness and physical coordination may be impaired.

Tachyphylaxis

IOP-lowering efficacy may diminish during therapy with 0.5% ophthalmic solution; careful monitoring recommended.

Patient Monitoring

Closely monitor patients who develop excessive IOP reduction.

Periodic visual field tests and frequent follow-up examinations recommended in patients receiving maximally tolerated drug therapy and 0.5% apraclonidine for glaucoma to delay surgery; discontinue therapy if IOP increases substantially.

Ocular Effects

Abnormal vision, pain, keratitis, keratopathy, blepharitis, blepharoconjunctivitis, photophobia, corneal staining, corneal erosion, corneal infiltrate, and irritation reported rarely.

Specific Populations

Pregnancy

Category C.

Lactation

Not known whether apraclonidine is distributed into milk. Caution advised if 0.5% ophthalmic solution is used. Temporarily discontinue nursing during the day that 1% ophthalmic solution is used for inhibition of perioperative IOP increases.

Pediatric Use

Safety and efficacy not established in children <21 years of age.

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults.

Hepatic Impairment

Closely monitor cardiovascular parameters in patients with impaired liver function.

Renal Impairment

Elimination may be decreased; closely monitor cardiovascular parameters in severe renal impairment.

Use with caution in patients with chronic renal impairment.

Common Adverse Effects

0.5% solution: Discomfort, hyperemia, pruritus, tearing, lid edema, dry mouth, foreign body sensation, blanching, blurred vision, conjunctivitis, discharge, dry eye.

1% solution: Ocular injection, upper lid elevation, irregular heart rate, nasal decongestion, ocular inflammation, conjunctival blanching, mydriasis.

Drug Interactions

Specific Drugs

Apraclonidine Pharmacokinetics

Absorption

Bioavailability

Some systemic absorption occurs following topical administration.

Onset

Following topical application of a 1% solution, reduction in IOP usually occurs within 1 hour and reaches a maximum within 3–5 hours.

Duration

Reduction in IOP persists for at least 12 hours.

Distribution

Extent

Distribution into both ocular and systemic human tissues is unknown.

Not known whether apraclonidine crosses the placenta or is distributed into milk.

Elimination

Metabolism

Metabolic fate not fully elucidated.

Elimination Route

Elimination characteristics not fully elucidated.

Half-life

0.5% solution: 8 hours.

Stability

Storage

Ophthalmic

Solution

0.5% solution: Tight, light-resistant container at 2–27°C; do not freeze.

1% solution: Tight, light-resistant container at 2–25°C.

Actions

• Stimulates α₂-receptors; also may stimulate, to a lesser extent, α₁-receptors.

• Inhibits the production of cyclic adenosine monophosphate (AMP) by inhibition of adenylate cyclase.

• Reduces both elevated and normal IOP in patients with or without glaucoma via peripheral (e.g., local) effects.

• Exact mechanism(s) of action not clearly established, but predominant effect appears to be reduced aqueous humor formation. resulting from constriction of afferent ciliary process vessels.

• Produces local vasoconstriction and reduction in blood flow in the eye.

Advice to Patients

• Importance of learning and adhering to proper administration techniques to avoid contamination of the solution container. If more than one topical ophthalmic drug is used, importance of administering at least 5 minutes apart.

• Importance of delaying insertion of soft contact lenses for at least 15 minutes after apraclonidine instillation, since benzalkonium chloride preservative in the solution may be absorbed by soft lenses.

• Risk of dizziness or fatigue; use caution when driving or operating machinery.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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