Apraclonidine drug data and news

Apraclonidine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Apraclonidine
Brand Names/Synonyms Aplonidine; Apraclonidina [Inn-Spanish]; Apraclonidine; Apraclonidinum [Inn-Latin]; B002; CHEMBANK2725; Fd &Amp; C Red No 1; Iopidine; P-Aminoclonidine Hydrochloride
Indication For short-term adjunctive therapy in patients on maximally tolerated medical therapy who require additional Intra Ocular Pressure (IOP) reduction.
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Description Not Available
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 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.
Apraclonidine News
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Dosage Forms LIQUID
Drug_Category Antiglaucomic Agents; Ophthalmics; EENT Drugs; ATC:S01EA03
Absorption Not Available
Interactions -->Interactions for Apraclonidine:

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.

 

Toxicity Not Available
Organisms Affected Humans and other mammals
Chemical IUPAC Name 2,6-dichloro-N-(4,5-dihydro-1H-imidazol-2-yl)benzene-1,4-diamine
Chemical Formula C9H10Cl2N4
Molecular Weight 245.108 g/mol
Smiles String C1CN=C(N1)NC2=C(C=C(C=C2Cl)N)Cl
Melting Point Not Available
Water Solubility Not Available
State Solid
LogP/Hphobicity 1.53
Isoelectric Point Not Available
Biotransformation Not Available
Half Life 8 hours
Protein Binding [%] 98.70%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Apraclonidine.html
http://www.rxlist.com/cgi/generic2/apraclonidine.htm
Drug Type Approved Drug
Accession No APRD00012
CAS Registry Number 66711-21-5
KEGG Compound ID C07668
PubChem ID SID:9870
PharmGKB ID PA448468
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2076306

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