Aplonidine - General Information
Aplonidine, also known as iopidine, is a sympathomimetic used in glaucoma therapy. It is an alpha2-adrenergic agonist.
Pharmacology of Aplonidine
Aplonidine 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.
Aplonidine for patients
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.
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).
Additional information about Aplonidine
Aplonidine Indication: For short-term adjunctive therapy in patients on maximally tolerated medical therapy who require additional Intra Ocular Pressure (IOP) reduction.
Mechanism Of Action: Aplonidine 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 Aplonidine has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Apraclonidine
Synonyms: Apraclonidina [Inn-Spanish]; Apraclonidinum [Inn-Latin]; P-Aminoclonidine Hydrochloride
Drug Category: Antiglaucomic Agents; Ophthalmics; EENT Drugs
Drug Type: Small Molecule; Approved
Other Brand Names containing Apraclonidine: Aplonidine; Iopidine; Iopidine Eye;
Absorption: Topical use of apraclonidine ophthalmic solution leads to systemic absorption. Studies of apraclonidine (0.5% ophthalmic solution) dosed one drop three times a day in both eyes for 10 days in normal volunteers yielded mean peak and trough concentrations of 0.9 ng/mL and 0.5 ng/mL, respectively.
Toxicity (Overdose): Accidental or intentional ingestion of oral apraclonidine 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.
Protein Binding: 98.7%
Biotransformation: Not Available
Half Life: 8 hours
Dosage Forms of Aplonidine: Liquid Ophthalmic
Solution / drops Ophthalmic
Chemical IUPAC Name: 2,6-dichloro-N-(4,5-dihydro-1H-imidazol-2-yl)benzene-1,4-diamine
Chemical Formula: C9H10Cl2N4
Apraclonidine on Wikipedia: http://en.wikipedia.org/wiki/Apraclonidine
Organisms Affected: Humans and other mammals