Brands, Medical Use, Clinical Data
- Antiglaucomic Agents
- EENT Drugs
Brands / Synonyms
Aplonidine; Apraclonidina [Inn-Spanish]; Apraclonidinum [Inn-Latin]; C Red No 1; Fd &Amp; Iopidine; P-Aminoclonidine Hydrochloride
For short-term adjunctive therapy in patients on maximally tolerated medical therapy who require additional Intra Ocular Pressure (IOP) reduction.
Apraclonidine significantly lowers intraocular pressure with minimal effects on cardiovascular and pulmonary parameters. It lowers intraocular pressure by reducing aqueous humor production and increasing uveoscleral outflow.
Mechanism of Action
Apraclonidine is an alpha adrenergic receptor agonist. It has a peak ocular hypotensive effect occurring at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that Apraclonidine has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow.
Biotrnasformation / Drug Metabolism
IOPIDINE 0.5% Ophthalmic Solution 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 inhibitors (MAO inhibitors).
Apraclonidine should not be used in patients receiving MAO inhibitors.. Although no specific drug
interactions with topical glaucoma drugs or systemic medications were identified in clinical studies of IOPIDINE®
0.5% Ophthalmic Solution, 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.
An additive hypotensive effect has been reported with the combination of systemic clonidine and
neuroleptic therapy. Systemic clonidine may inhibit the production of catecholamines in response to insulin-induced
hypoglycemia and mask the signs and symptoms of hypoglycemia.
Since apraclonidine may reduce pulse and blood pressure, caution in using drugs such as beta-blockers
(ophthalmic and systemic), antihypertensives, and cardiac glycosides is advised. Patients using cardiovascular drugs
concurrently with IOPIDINE 0.5% Ophthalmic Solution should have pulse and blood pressures frequently monitored.
Caution should be exercised with simultaneous use of clonidine and other similar pharmacologic agents.