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Pronunciation
(a pra KLOE ni deen)
Generic Available (U.S.)
No
Index Terms
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Prevention and treatment of postsurgical intraocular pressure (IOP) elevation; short-term, adjunctive therapy in patients who require additional reduction of IOP
Pregnancy Risk Factor
C
Pregnancy Considerations
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 within 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
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.
Storage
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: Other
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
Nursing: Physical Assessment/Monitoring
Assess potential for interactions with other pharmacological agents patient may be taking. Monitor therapeutic response (intraocular pressure) and adverse effects (ocular and other systems). Teach patient proper use, side effects/appropriate interventions, and adverse symptoms to report.
Dosage Forms
Solution, ophthalmic:
Iopidine®: 0.5% (5 mL, 10 mL); 1% (0.1 mL) [contains benzalkonium chloride]
Pricing: U.S. (www.drugstore.com)
Solution (Iopidine)
0.5% (5): $77.83
0.5% (10): $145.05
1% (1): $14.11
International Brand Names
Lexi-Comp.com
Last full review/revision October 2006
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