Apraclonidine

What is Apraclonidine?

DESCRIPTION Apraclonidine ophthalmic solution 0.5% contains apraclonidine hydrochloride, an alpha adrenergic agonist, in a sterile isotonic solution for topical application to the eye. Apraclonidine hydrochloride is a white to off-white powder and is highly soluble in water. Its chemical name is 2-[(4-amino-2,6 dichlorophenyl) imino]imidazolidine monohydrochloride with an empirical formula of C 9 H 11 Cl 3 N 4 and a molecular weight of 281.57 g/mol. The chemical structure of apraclonidine hydrochloride is: Each mL of apraclonidine ophthalmic solution 0.5% contains: Active: apraclonidine hydrochloride 5.75 mg equivalent to apraclonidine base 5 mg. Preservative: benzalkonium chloride 0.01%. Inactives: hydrochloric acid and/or sodium hydroxide (to adjust pH), purified water, sodium acetate, and sodium chloride. image

Uses of Apraclonidine

Established uses

• INDICATIONS AND USAGE Apraclonidine ophthalmic solution 0.5% is indicated for short-term adjunctive therapy, in patients on maximally tolerated medical therapy, who require additional IOP reduction.
• Patients on maximally tolerated medical therapy, who are treated with apraclonidine ophthalmic solution 0.5% to delay surgery, should have frequent follow-up examinations and treatment should be discontinued if the IOP rises significantly.
• The addition of apraclonidine ophthalmic solution 0.5% to patients already using two aqueous suppressing drugs (i.e., beta-blocker plus carbonic anhydrase inhibitor) as part of their maximally tolerated medical therapy may not provide additional benefit.
• This is because apraclonidine ophthalmic solution 0.5% is an aqueous suppressing drug and the addition of a third aqueous suppressant may not significantly reduce IOP.
• The IOP lowering efficacy of apraclonidine ophthalmic solution 0.5% diminishes over time in some patients.
• This loss of effect, or tachyphylaxis, appears to be an individual occurrence with a variable time of onset and should be closely monitored.

How to take Apraclonidine

DOSAGE AND ADMINISTRATION One to two drops of apraclonidine ophthalmic solution 0.5% should be instilled in the affected eye(s) three times daily. Since apraclonidine ophthalmic solution 0.5% will be used with other ocular glaucoma therapies, an approximate 5 minute interval between instillation of each medication should be practiced to prevent washout of the previous dose. NOT FOR INJECTION INTO THE EYE. NOT FOR ORAL INGESTION.

Dosage

Follow the dose prescribed by your doctor or pharmacist. The ranges below are general information, not a personal prescription.

Adults

DOSAGE AND ADMINISTRATION One to two drops of apraclonidine ophthalmic solution 0.5% should be instilled in the affected eye(s) three times daily. Since apraclonidine ophthalmic solution 0.5% will be used with other ocular glaucoma therapies, an approximate 5 minute interval between instillation of each medication should be practiced to prevent washout of the previous dose. NOT FOR INJECTION INTO THE EYE. NOT FOR ORAL INGESTION.

Side effects of Apraclonidine

Common

• ADVERSE REACTIONS In clinical studies the overall discontinuation rate related to apraclonidine ophthalmic solution 0.5% was 15%.
• The most commonly reported events leading to discontinuation included (in decreasing order of frequency) hyperemia, pruritus, tearing, discomfort, lid edema, dry mouth, and foreign body sensation.
• The following adverse reactions (incidences) were reported in clinical studies of apraclonidine ophthalmic solution 0.5% as being possibly, probably, or definitely related to therapy: Ocular The following adverse reactions were reported in 5% to 15% of the patients: discomfort, hyperemia, and pruritus.
• The following adverse reactions were reported in 1% to 5% of the patients: blanching, blurred vision, conjunctivitis, discharge, dry eye, foreign body sensation, lid edema, and tearing.
• The following adverse reactions were reported in less than 1% of the patients: 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, and photophobia.
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Warnings and who should not take it

Who should NOT take Apraclonidine?

• CONTRAINDICATIONS Apraclonidine ophthalmic solution 0.5% is contraindicated in patients with hypersensitivity to apraclonidine or any other component of this medication, as well as systemic clonidine.
• It is also contraindicated in patients receiving monoamine oxidase (MAO) inhibitors.

Warnings and precautions

• WARNINGS Not for injection or oral ingestion.
• FOR EYE USE ONLY.

Overdose

OVERDOSAGE Ingestion of apraclonidine ophthalmic solution 0.5% has been reported to cause bradycardia, drowsiness, and hypothermia. Accidental or intentional ingestion of oral clonidine has been reported to cause apnea, arrhythmias, asthenia, bradycardia, conduction defects, diminished or absent reflexes, dryness of the mouth, hypotension, hypothermia, hypoventilation, irritability, lethargy, miosis, pallor, respiratory depression, sedation or coma, seizure, somnolence, transient hypertension, and vomiting. Treatment of an oral overdose includes supportive and symptomatic therapy; a patent airway should be maintained. Hemodialysis is of limited value since a maximum of 5% of circulating drug is removed.

Safety at a glance

Children and elderly

Interactions

Medicine and medicine

• Drug Interactions Apraclonidine should not be used in patients receiving MAO inhibitors (see CONTRAINDICATIONS).
• Although no specific drug interactions with topical glaucoma drugs or systemic medications were identified in clinical studies of apraclonidine ophthalmic solution 0.5%, the possibility of an additive or potentiating effect with CNS depressants (alcohol, barbiturates, opiates, sedatives, anesthetics) should be considered.
• Tricyclic antidepressants have been reported to blunt the hypotensive effect of systemic clonidine.
• It is not known whether the concurrent use of these agents with apraclonidine can lead to a reduction in IOP lowering effect.
• No data on the level of circulating catecholamines after apraclonidine withdrawal are available.
• Caution, however, is advised in patients taking tricyclic antidepressants which can affect the metabolism and uptake of circulating amines.

Frequently asked questions