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Apraclonidine

Medically reviewed by Drugs.com. Last updated on May 13, 2019.

Pronunciation

(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. [DSC] = Discontinued product

Solution, Ophthalmic:

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

Generic: 0.5% (5 mL, 10 mL)

Brand Names: U.S.

  • Iopidine

Pharmacologic Category

  • Alpha2 Agonist, Ophthalmic

Pharmacology

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

Elevated intraocular pressure:

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

1% solution: Prevention and treatment of postsurgical IOP elevation following argon laser trabeculoplasty, argon laser iridotomy or Nd:YAG posterior capsulotomy (manufacturer's labeling) or as part of a 4-drug medical management regimen in acute angle-closure glaucoma when the patient cannot be seen by an ophthalmologist for ≥1 hour (off-label use) (Krawitz 1990; Pokhrel 2007; Weizer 2019).

Contraindications

Hypersensitivity to apraclonidine, clonidine, or any component of the formulation; concomitant use with MAO inhibitors.

Canadian labeling: Additional contraindications (not in US labeling): Children and adolescents <18 years old.

Dosing: Adult

Elevated intraocular pressure: Ophthalmic:

Open-angle glaucoma: 0.5%: Instill 1 to 2 drops into the affected eye(s) 3 times daily.

Angle-closure glaucoma (off-label use): 1%: Instill 1 drop into the affected eye as part of a 4-drug regimen; may repeat in 30 to 60 minutes if intraocular pressure (IOP) remains elevated (eg, >40 mm Hg). Note: Reserve medical management for emergency situations when an assessment by an ophthalmologist will be delayed by ≥1 hour (Krawitz 1990; Pokhrel 2007; Weizer 2019).

Prevention and treatment of postsurgical IOP elevation: 1%: Instill 1 drop into the 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.

Administration

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

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. When treating acute angle-closure glaucoma, separate administration of other ophthalmic agents by ≥1 minute (Pokhrel 2007; Weizer 2019).

Storage

Iopidine 0.5%: Store between 2°C to 27°C (36°F to 80°F); protect from freezing and light.

Iopidine 1%: Store between 2°C to 25°C (36°F to 77°F); protect from light.

Drug Interactions

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

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

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%, postmarketing, and/or case reports: 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

Warnings/Precautions

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, discontinue use.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with severe uncontrolled cardiovascular disease (eg, hypertension), coronary insufficiency, recent myocardial infarction, cerebrovascular disease, Raynaud disease, and thromboangiitis obliterans.

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

• Renal impairment: Close monitoring of cardiovascular parameters is recommended in patients with renal impairment; use with caution in patients with chronic renal failure. 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 impairment.

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

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Contact lens wearers: Some products contain benzalkonium chloride which may be absorbed by soft contact lenses; contact lenses should be removed during instillation; may be reinserted 15 minutes after instillation.

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 therapy using 0.5% solution to delay surgery); tachyphylaxis; cardiovascular parameters in patients with renal and/or hepatic impairment; depression in depressed patients. Check intraocular pressure 30 to 60 minutes after administration for acute use of 1% solution for acute angle-closure glaucoma (Pokhrel 2007; Weizer 2019).

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 punctal 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, increased tears, 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.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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