Apraclonidine

Pronunciation

(a pra KLOE ni deen)

U.S. Brand Names

Iopidine®

Synonyms

Aplonidine; Apraclonidine Hydrochloride; p-Aminoclonidine

Generic Available

Canadian Brand Names

Iopidine®

Use

Prevention and treatment of postsurgical intraocular pressure (IOP) elevation; short-term, adjunctive therapy in patients who require additional reduction of IOP

Pregnancy Risk Factor

Pregnancy Implications

Embryocidal effects were observed in some animal studies. There are no adequate and well-controlled studies in pregnant women.

Lactation

Excretion in breast milk unknown/use caution

Contraindications

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

Warnings/Precautions

IOP-lowering efficacy decreases over time in some patients; most patients will experience decreased benefit from therapy lasting longer than 1 month. Closely monitor patients who develop exaggerated reductions in intraocular pressure; use with caution in patients with cardiovascular disease, coronary insufficiency, recent myocardial infarction, cerebrovascular disease, history of vasovagal reactions, Raynaud's disease, thromboangiitis obliterans, depression, chronic renal failure, or severe renal or hepatic impairment.

Adverse Reactions

Ocular:

5% to 15%: Discomfort, hyperemia, pruritus

1% to 5%: Blanching, blurred vision, conjunctivitis, discharge, dry eye, foreign body sensation, lid edema, tearing

<1%: Abnormal vision, blepharitis, blepharoconjunctivitis, conjunctival edema, conjunctival follicles, corneal erosion, corneal infiltrate, corneal staining, edema, irritation, keratitis, keratopathy, lid disorder, lid erythema, lid margin crusting, lid retraction, lid scales, pain, photophobia

Other body systems:

1% to 10%: Gastrointestinal: Dry mouth (10%)

<3%:

Cardiovascular: Arrhythmia, chest pain, facial edema, peripheral edema

Central nervous system: Depression, dizziness, headache, insomnia, malaise, nervousness, somnolence

Dermatologic: Contact dermatitis, dermatitis

Gastrointestinal: Constipation, nausea, taste perversion

Neuromuscular & skeletal: Abnormal coordination, myalgia, paresthesia, weakness

Respiratory: Asthma, dry nose, dyspnea, parosmia, pharyngitis, rhinitis

Postmarketing and/or case reports: Allergic reactions, bradycardia

Overdosage/Toxicology

Bradycardia, drowsiness, and hypothermia have been reported following ingestion of the ophthalmic solution.

Drug Interactions

Antihypertensive agents: Apraclonidine may reduce pulse and blood pressure, use systemic agents with caution.

Beta-blockers: Ophthalmic agents may have additive effect on IOP; apraclonidine may reduce pulse and blood pressure, use systemic agents with caution.

CNS depressants: May have additive CNS depression.

MAO inhibitors: Concomitant use is contraindicated.

Pilocarpine: Ophthalmic use may have additive effect on IOP.

Stability

Store between 2°C to 27°C (36°F to 80°F); protect from freezing and light

Mechanism of Action

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.

Pharmacodynamics/Kinetics

Onset of action: 1 hour

Peak effect: Decreased intraocular pressure: 3-5 hours

Absorption: Ocular: Systemically absorbed

Half-life elimination, systemic: 8 hours

Dosage

Adults: Ophthalmic:

0.5%: Instill 1-2 drops in the affected eye(s) 3 times/day

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

Dosing adjustment in renal impairment: Although the topical use of apraclonidine has not been studied in renal failure patients, structurally related clonidine undergoes a significant increase in half-life in patients with severe renal impairment; close monitoring of cardiovascular parameters in patients with impaired renal function is advised.

Dosing adjustment in hepatic impairment: Close monitoring of cardiovascular parameters in patients with impaired liver function is advised because the systemic dosage form of clonidine is partially metabolized in the liver

Administration

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

Monitoring Parameters

Closely monitor patients who develop exaggerated reductions in intraocular pressure

Patient Education

For use in eyes only. May sting on instillation, do not touch dropper to eye. Visual acuity may be decreased after administration. Night vision may be decreased. Distance vision may be altered. Read package instructions for insertion. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnancy. Consult prescriber if breast-feeding.

Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause drowsiness

Mental Health: Effects on Psychiatric Treatment

Dry mouth may be exacerbated by concurrent use of psychotropics

Dosage Forms

Solution, ophthalmic, as hydrochloride: 0.5% (5 mL, 10 mL); 1% (0.1 mL) [contains benzalkonium chloride]

International Brand Names

Iopidine® (AR, AT, AU, BE, CA, CH, CL, DE, DK, FI, FR, GB, HU, IE, IL, IT, LU, NL, NO, NZ, PL, RO, SE, SG, TR, ZA); Iopimax® (ES)

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