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QuickView for Apraclonidine (compound)


PubChem
Name: apraclonidine
PubChem Compound ID: 2216
Molecular formula: C9H10Cl2N4
Molecular weight: 245.108 g/mol
Synonyms:
Apraclonidine; 4-Aminoclonidine; 66711-21-5; 1,4-Benzenediamine, 2,6-dichloro-N'-(4,5-dihydro-1H-imidazol-2-yl)-; NCGC00015033-01; Apraclonidinum [INN-Latin]; Apraclonidina [INN-Spanish]; C07668; Aplonidine; Lopac-A-0779
DrugBank
Identification
Name: apraclonidine
Name (isomeric): DB00964
Drug Type: small molecule
Synonyms:
Apraclonidine Hydrochloride; Apraclonidinum [INN-Latin]; Apraclonidina [INN-Spanish]; P-Aminoclonidine Hydrochloride
Brand: Iopidine Eye, Iopidine, Aplonidine
Category: Adrenergic alpha-Agonists, Antiglaucomic Agents, Ophthalmics, EENT Drugs
CAS number: 66711-21-5
Pharmacology
Indication: For prevention or reduction of intraoperative and postoperative increases in intraocular pressure (IOP) before and after ocular laser surgery when used prophylactically. Also used as a short-term adjunctive therapy in patients with open-angle glaucoma who are on maximally tolerated medical therapy requiring additional IOP reduction.
Pharmacology: 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 a relatively selective alpha2 adrenergic receptor agonist that stimulates alpha1 receptors to a lesser extent. It has a peak ocular hypotensive effect occurring at two hours post-dosing. The exact mechanism of action is unknown, but fluorophotometric studies in animals and humans suggest that Apraclonidine has a dual mechanism of a...
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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.
Protein binding: 98.7%
Half Life: 8 hours
Toxicity: 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.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
TreprostinilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
TranylcypromineThe MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of the alpha2-agonist, Apraclonidine. Concomitant therapy is contraindicated.

Targets