IOPIDINE
IOPIDINE — apraclonidine hydrochloride solution/ drops
Alcon Laboratories, Inc.
DESCRIPTION
IOPIDINE 1% Ophthalmic Solution 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 C9 H11 Cl3 N4 and a molecular weight of 281.6.
The chemical structure of apraclonidine hydrochloride is:
Each mL of IOPIDINE 1% Ophthalmic Solution contains: Actives: apraclonidine hydrochloride 11.5 mg equivalent to apraclonidine base 10 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). Osmolality is 260-320 mOsm.
CLINICAL PHARMACOLOGY
Apraclonidine is a relatively selective, alpha adrenergic agonist and does not have significant membrane stabilizing (local anesthetic) activity. When instilled into the eye, IOPIDINE 1% (apraclonidine hydrochloride ophthalmic solution) has the action of reducing intraocular pressure (IOP). Ophthalmic apraclonidine has minimal effect on cardiovascular parameters.
Optic nerve head damage and visual field loss may result from an acute elevation in IOP that can occur after argon or Nd:YAG laser surgical procedures. Elevated IOP, whether acute or chronic in duration, is a major risk factor in the pathogenesis of visual field loss. The higher the peak or spike of IOP, the greater the likelihood of visual field loss and optic nerve damage especially in patients with previously compromised optic nerves. The onset of action with IOPIDINE 1% Ophthalmic Solution can usually be noted within one hour and the maximum IOP reduction usually occurs three to five hours after application of a single dose. The precise mechanism of the ocular hypotensive action of IOPIDINE 1% Ophthalmic Solution is not completely established at this time. Aqueous fluorophotometry studies in man suggest that its predominant action may be related to a reduction of aqueous formation. Controlled clinical studies of patients requiring argon laser trabeculoplasty, argon laser iridotomy or Nd:YAG posterior capsulotomy showed that IOPIDINE 1% Ophthalmic Solution controlled or prevented the post-surgical IOP rise typically observed in patients after undergoing those procedures. After surgery, the mean IOP was 1.2 to 4 mmHg below the corresponding pre-surgical baseline pressure before IOPIDINE Ophthalmic Solution treatment. With placebo treatment, post-surgical pressures were 2.5 to 8.4 mmHg higher than their corresponding pre-surgical baselines. Overall, only 2% of patients treated with IOPIDINE* 1% Ophthalmic Solution had severe IOP elevations (spike greater than or equal to 10 mmHg) during the first three hours after laser surgery, whereas 23% of placebo-treated patients responded with severe pressure spikes (Table 1). Of the patients that experienced a pressure spike after surgery, the peak IOP was above 30 mmHg in most patients (Table 2) and was above 50 mmHg in seven placebo-treated patients and one IOPIDINE 1% Ophthalmic Solution-treated patient.
Table 1: Incidence of IOP Spikes Greater Than or Equal to 10 mmHg
Treatment | ||||||
---|---|---|---|---|---|---|
Apraclonidine | Placebo | |||||
Study | Laser Procedure | P-Value | a N | (%) | a N | (%) |
1 | Trabeculoplasty | <0.05 | 0/40 | (0%) | 6/35 | (17%) |
2 | Trabeculoplasty | =0.06 | 2/41 | (5%) | 8/42 | (19%) |
| ||||||
1 | Iridotomy | <0.05 | 0/11 | (0%) | 4/10 | (40%) |
2 | Iridotomy | =0.05 | 0/17 | (0%) | 4/19 | (21%) |
| ||||||
1 | Nd:YAG Capsulotomy | <0.05 | 3/80 | (4%) | 19/83 | (23%) |
2 | Nd:YAG Capsulotomy | <0.05 | 0/83 | (0%) | 22/81 | (27%) |
a N = Number Spikes/Number Eyes.
Table 2: Magnitude of Post-surgical IOP in Trabeculoplasty, Iridotomy and Nd:YAG Capsulotomy Patients With Severe Pressure Spikes Greater than or Equal to 10 mmHg
Maximum Postsurgical IOP (mmHg)
Total | |||||
---|---|---|---|---|---|
Treatment | Spikes | 20-29 mmHg | 30-39 mmHg | 40-49 mmHg | > 50 mmHg |
IOPIDINE | 8 | 1 | 4 | 2 | 1 |
Placebo | 78 | 16 | 47 | 8 | 7 |
INDICATIONS AND USAGE
IOPIDINE 1% Ophthalmic Solution is indicated to control or prevent post-surgical elevations in IOP that occur in patients after argon laser trabeculoplasty, argon laser iridotomy or Nd:YAG posterior capsulotomy.
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