APRACLONIDINE solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

APRACLONIDINE HYDROCHLORIDE (UNII: D2VW67N38H) (APRACLONIDINE - UNII:843CEN85DI)

Available from:

Sandoz Inc

INN (International Name):

APRACLONIDINE HYDROCHLORIDE

Composition:

APRACLONIDINE 5.75 mg in 1 mL

Administration route:

OPHTHALMIC

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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

Product summary:

Apraclonidine ophthalmic solution 0.5% as base in a sterile, isotonic, aqueous solution containing apraclonidine hydrochloride. Supplied in plastic ophthalmic DROP-TAINER® * dispenser as follows: 5 mL NDC 61314-665-05 10 mL NDC 61314-665-10 Storage: Store between 2° to 27°C (36° to 80°F). Protect from freezing and light. *DROP-TAINER® is a registered trademark of Alcon Research, Ltd.

Authorization status:

New Drug Application Authorized Generic

Summary of Product characteristics

APRACLONIDINE- APRACLONIDINE SOLUTION
SANDOZ INC
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APRACLONIDINE OPHTHALMIC SOLUTION 0.5% AS BASE
RX ONLY
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 H Cl
N 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. INACTIVES: sodium
chloride, sodium acetate, sodium
hydroxide and/or hydrochloric acid (pH 4.4-7.8), purified water and
benzalkonium chloride 0.01%
(preservative).
CLINICAL PHARMACOLOGY
Apraclonidine hydrochloride is a relatively selective
alpha-2-adrenergic agonist. When instilled in the
eye, apraclonidine ophthalmic solution 0.5%, has the action of
reducing elevated, as well as normal,
intraocular pressure (IOP), whether or not accompanied by glaucoma.
Ophthalmic apraclonidine has
minimal effect on cardiovascular parameters. Elevated IOP presents a
major risk factor in glaucomatous
field loss. The higher the level of IOP, the greater the likelihood of
optic nerve damage and visual
field loss. Apraclonidine ophthalmic solution 0.5% has the action of
reducing IOP. The onset of action
of apraclonidine can usually be noted within one hour, and maximum IOP
reduction occurs about three
hours after instillation. Aqueous fluorophotometry studies demonstrate
that apraclonidine's predominant
mechanism of action is reduction of aqueous flow via stimulation of
the alpha-adrenergic system.
Repeated dose-response and comparative studies (0.125% - 1.0%
apraclonidine) demonstrate that 0.5%
apraclonidine is at the top of the dose-response IOP reduction curve.
The clinical utility of