Apraclonidine Hcl (apraclonidine HCl)

Although USP currently states that potency of apraclonidine hyrochloride preparations should be expressed both in terms of the salt and the base (''active moiety''), dosage currently is expressed in terms of the base. (See Chemistry and Stability: Chemistry.)

Apraclonidine hydrochloride is applied topically to the eye as an ophthalmic solution. Care should be taken to avoid contamination of the solution container. Apraclonidine hydrochloride ophthalmic solution is not for oral administration. In addition, the ophthalmic solution should not be injected into the eye.

The potential interactions between apraclonidine hydrochloride ophthalmic solution and other ophthalmic drugs have not been fully evaluated. However, the manufacturer states that topical apraclonidine should not be used in patients receiving a monoamine oxidase (MAO) inhibitor. In addition, although no drug interactions have been reported in clinical studies in patients with glaucoma receiving topical apraclonidine concomitantly with topical or systemic drugs, the manufacturer states that the possibility of additive CNS effects should be considered when topical apraclonidine is administered concomitantly with CNS depressants such as barbiturates, opiates, anesthetics, sedatives, or alcohol. Tricyclic antidepressants have blunted the hypotensive effects of systemically administered clonidine, and it is not known if concurrent use of tricyclic antidepressants with topical apraclonidine may decrease the IOP-lowering effect of the drug. No data is available on the circulating plasma concentrations of catecholamines following apraclonidine withdrawal; however, the manufacturer states that caution should be exercised in concomitant use of drugs (e.g., tricyclic antidepressants) that affect the metabolism or tissue uptake of these amines. It should be considered that systemically administered clonidine and antipsychotic drugs appear to have additive hypotensive effects. Also, the manufacturer cautions that systemically administered clonidine may inhibit production of catecholamines in response to insulin-induced hypoglycemia and mask signs and symptoms of hypoglycemia.

Since apraclonidine may decrease heart rate and blood pressure, the drug should be used with caution in patients receiving antihypertensive agents, cardiac glycosides, topically or systemically administered beta-adrenergic blocking agents, or similar pharmacologic agents. The manufacturer states that pulse and blood pressure should be monitored frequently in patients receiving topical apraclonidine concomitantly with cardiac drugs. Limited data indicate that when apraclonidine hydrochloride ophthalmic solution is used in conjunction with a topical beta-adrenergic blocking agent (e.g., timolol) or pilocarpine, the drugs may have an additive IOP-lowering effect.

Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.

Apraclonidine/Maois

SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.

MECHANISM OF ACTION: Apraclonidine is an alpha-2-adrenergic agonist used to decrease intraocular pressure. The use of apraclonidine ophthalmic solution leads to systemic absorption.(1) As apraclonidine does not cross the blood brain barrier, peripheral alpha-2-adrenergic effects could potentially result in vasoconstriction.(1)

CLINICAL EFFECTS: Not described.(1)

PREDISPOSING FACTORS: Unknown.

PATIENT MANAGEMENT: The manufacturer of apraclonidine states that concurrent administration of apraclonidine to patients on monoamine oxidase inhibitors (MAOI's) is contraindicated.(1)

DISCUSSION: There is no clinical documentation to support this interaction. The manufacturer of apraclonidine states that concurrent administration of apraclonidine to patients on MAOI's is contraindicated.(1) Methylene blue, when administered intravenously, has been shown to reach sufficient concentrations to be a potent inhibitor of MAO-A. Metaxalone is a weak inhibitor of MAO.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

There is no enhanced messaging for this drug.

There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

• Hypertension
• Severe cardiopulmonary disease
• Vagal reflex bradycardia

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More Frequent

• Eye tearing
• Ocular itching
• Ocular redness

Rare or Very Rare

• Asthma
• Blepharitis
• Blepharoconjunctivitis
• Blurred vision
• Bradycardia
• Cardiac arrhythmia
• Chemosis
• Chest pain
• Conjunctivitis
• Contact dermatitis
• Corneal erosion
• Depression
• Disorder of cornea
• Dizziness
• Dyskinesia
• Dyspnea
• Eyelid edema
• Eyelid retraction
• Facial edema
• Infiltrate of cornea
• Keratitis
• Ocular discharge
• Orthostatic hypotension
• Paresthesia
• Peripheral edema
• Vagal reflex bradycardia
• Visual changes

More Frequent

• Conjunctival hyperemia
• Ocular discomfort
• Xerostomia

Less Frequent

• Mydriasis
• Ocular inflammation

Rare or Very Rare

• Acute abdominal pain
• Conjunctival blanching
• Constipation
• Corneal staining
• Diarrhea
• Dream disorder
• Drowsy
• Dry eye
• Dry nose
• Dysgeusia
• Dyspepsia
• Eyelid crusting
• Foreign body sensation of eye
• General weakness
• Headache disorder
• Hypersensitivity drug reaction
• Insomnia
• Malaise
• Myalgia
• Nausea
• Nervousness
• Palpitations
• Pharyngitis
• Photophobia
• Rhinitis
• Vomiting

No enhanced messaging available.

No enhanced messaging available.

Although there are no adequate and controlled studies to date in humans, apraclonidine has been shown to have embryocidal effects in rabbits receiving oral dosages of 3 mg/kg (about 60 times the maximum recommended human dose) daily. In rats, apraclonidine caused dose-related maternal toxicity with oral dosages of 0.3 mg/kg daily (about 6 times the maximum recommended human dosage). It is not known whether the drug can cause fetal harm when administered as an ophthalmic solution to pregnant women. Ophthalmic apraclonidine should be used during pregnancy only when the potential benefits justify the possible risks to the fetus.

It is not known whether apraclonidine is distributed into milk. Because many drugs are distributed into milk, apraclonidine 0.5% ophthalmic solution should be used with caution in nursing women. If apraclonidine 1% ophthalmic solution is used for inhibition of perioperative intraocular pressure (IOP) increases, the need to discontinue nursing temporarily during the day that apraclonidine is used should be considered.

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