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(a pra KLOE ni deen)

Index Terms

  • Aplonidine
  • Apraclonidine HCl
  • Apraclonidine Hydrochloride
  • p-Aminoclonidine

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic:

Iopidine: 0.5% (5 mL, 10 mL); 1% (1 ea) [contains benzalkonium chloride]

Generic: 0.5% (5 mL, 10 mL)

Brand Names: U.S.

  • Iopidine

Pharmacologic Category

  • Alpha2 Agonist, Ophthalmic


Apraclonidine is a potent alpha-adrenergic agent similar to clonidine; relatively selective for alpha2-receptors but does retain some binding to alpha1-receptors; appears to result in reduction of aqueous humor formation; its penetration through the blood-brain barrier is more polar than clonidine which reduces its penetration through the blood-brain barrier and suggests that its pharmacological profile is characterized by peripheral rather than central effects.

Onset of Action

1 hour; Peak effect: Decreased intraocular pressure: 3 to 5 hours

Half-Life Elimination

Systemic: 0.5% solution: 8 hours

Use: Labeled Indications

0.5% solution: Short-term, adjunctive therapy in patients who require additional reduction of IOP

1% solution: Prevention and treatment of postsurgical intraocular pressure (IOP) elevation following argon laser trabeculoplasty, argon laser iridotomy or Nd:YAG posterior capsulotomy


Hypersensitivity to apraclonidine, clonidine, or any component of the formulation; use with or within 14 days of MAO inhibitors

Dosing: Adult

Intraocular pressure reduction: Ophthalmic:

0.5%: Instill 1 to 2 drops in the affected eye(s) 3 times daily

1%: Instill 1 drop in operative eye 1 hour prior to anterior segment laser surgery, second drop in same eye immediately upon completion of procedure

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling; monitor cardiovascular parameters closely.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling; monitor cardiovascular parameters closely.



0.5% solution: Wait 5 minutes between instillation of other ophthalmic agents to avoid washout of previous dose. After topical instillation, finger pressure should be applied to lacrimal sac to decrease drainage into the nose and throat and minimize possible systemic absorption.

1% solution: Use a separate container for each single drop dose; discard container after each use.


Store between 2°C to 25°C (36°F to 77°F); protect from freezing. Protect from light.

Drug Interactions

MAO Inhibitors: May enhance the adverse/toxic effect of Apraclonidine. MAO Inhibitors may increase the serum concentration of Apraclonidine. Avoid combination

Mianserin: May diminish the therapeutic effect of Alpha2-Agonists (Ophthalmic). Avoid combination

Mirtazapine: May diminish the antihypertensive effect of Alpha2-Agonists. Management: Consider avoiding concurrent use. If the combination cannot be avoided, monitor for decreased effects of alpha2-agonists if mirtazapine is initiated/dose increased, or increased effects if mirtazapine is discontinued/dose decreased. Consider therapy modification

Tricyclic Antidepressants: May diminish the therapeutic effect of Alpha2-Agonists (Ophthalmic). Monitor therapy

Adverse Reactions

Frequency not always defined.

5% to 15%:

Gastrointestinal: Xerostomia (10%)

Ophthalmic: Eye discomfort, eye pruritus, ocular hyperemia

1% to 5%:

Cardiovascular: Cardiac arrhythmia (<3%), chest pain (<3%), facial edema (<3%), peripheral edema (<3%), localized blanching

Central nervous system: Altered sense of smell (<3%), ataxia (<3%), depression (<3%), dizziness (<3%), drowsiness (<3%), headache (<3%), insomnia (<3%), malaise (<3%), nervousness (<3%), paresthesia (<3%)

Dermatologic: Contact dermatitis (<3%), dermatitis (<3%)

Gastrointestinal: Constipation (<3%), dysgeusia (<3%), nausea (<3%)

Neuromuscular & skeletal: Myalgia (<3%), weakness (<3%)

Ophthalmic: Blurred vision, conjunctivitis, dry eye syndrome, eyelid edema, eye discharge, foreign body sensation of eye, lacrimation

Respiratory: Asthma (<3%), dry nose (<3%), dyspnea (<3%), pharyngitis (<3%), rhinitis (<3%)

<1% (Limited to important or life-threatening): Blepharitis, blepharoconjunctivitis, bradycardia, conjunctival edema, corneal erosion, corneal infiltrates, corneal staining, crusting of eyelid, epithelial keratopathy, erythema of eyelid, eyelid disease, eyelid retraction, eye irritation, eye pain, follicular conjunctivitis, hypersensitivity reaction, keratitis, ocular edema, photophobia, scaling of eyelid, visual disturbance


Concerns related to adverse effects:

• CNS effects: May cause dizziness and somnolence, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

• Hypersensitivity reactions: Use may lead to allergic-like reactions, including hyperemia, pruritus, discomfort, tearing, foreign body sensation, and edema of the lid and conjunctiva; if these symptoms occur, therapy should be discontinued.

Disease-related concerns:

• Cardiovascular disease: In clinical studies of patients with glaucoma, topical apraclonidine had minimal effects on blood pressure and heart rate; however, use with caution in patients with severe uncontrolled cardiovascular disease (eg, hypertension), coronary insufficiency, recent myocardial infarction, cerebrovascular disease, Raynaud disease, and thromboangiitis obliterans.

• Depression: Use with caution in depressed patients and monitor signs/symptoms of depression; therapy is associated infrequently with depression.

• Hepatic impairment: Close monitoring of cardiovascular parameters is recommended if topical apraclonidine is administered to patients with hepatic impairment; clonidine (structurally related to apraclonidine) administered systemically undergoes partial hepatic metabolism.

• Renal impairment: Close monitoring of cardiovascular parameters is recommended if topical apraclonidine is administered to patients with renal impairment. Topical apraclonidine has not been studied in patients with renal impairment; however, the half-life of clonidine (structurally related to apraclonidine) administered systemically is increased significantly in severe renal impairment.

• Vasovagal reactions: Potential for a vasovagal attack to occur during laser surgery; use with caution in patients with history of vasovagal reactions.

Other warnings/precautions:

• Appropriate use: For topical ophthalmic use only; not for injection or oral administration.

• Tachyphylaxis: The IOP-lowering efficacy may decrease over time in some patients; most patients experience a benefit for less than one month; routinely monitor IOP.

Monitoring Parameters

Closely monitor patients who develop exaggerated reductions in intraocular pressure; visual fields (periodically for glaucoma patients on maximally tolerated medical using 0.5% solution to delay surgery)

Pregnancy Risk Factor


Pregnancy Considerations

Adverse events have been observed in animal reproduction studies. If ophthalmic agents are needed during pregnancy, the minimum effective dose should be used in combination with punctual occlusion to decrease potential exposure to the fetus (Samples 1988).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience blurred vision, dry eyes, or dry mouth. Have patient report immediately to prescriber vision changes, eye pain, severe eye irritation, eyelid edema, eye discharge, or foreign body sensation in eye (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.