Arsenite - General Information
Arsenite is a chemotheraputic agent of idiopathic function used to treat leukemia that is unresponsive to first line agents. It is suspected that arsenic trisulfide induces cancer cells to undergo apoptosis. Due to the toxic nature of arsenic, this drug carries significant health risks. The enzyme thioredoxin reductase has recently been identified as a target for arsenic trioxide.
Pharmacology of Arsenite
Arsenic Trioxide is indicated for induction of remission and consolidation in patients with acute promyelocytic leukemia (APL) who are refractory to, or have relapsed from, retinoid and anthracycline chemotherapy.
Arsenite for patients
No formal assessments of pharmacokinetic drug-drug interactions between TRISENOX® and other agents have been conducted. Caution is advised when TRISENOX® is coadministered with other medications that can prolong the QT interval (e.g. certain antiarrhythmics or thioridazine) or lead to electrolyte abnormalities (such as diuretics or amphotericin B).
TRISENOX® is contraindicated in patients who are hypersensitive to arsenic.
Additional information about Arsenite
Arsenite Indication: For induction of remission and consolidation in patients with acute promyelocytic leukemia (APL), and whose APL is characterized by the presence of the t(15;17) translocation or PML/RAR-alpha gene expression
Mechanism Of Action: The mechanism of action of Arsenic Trioxide is not completely understood. Arsenite causes morphological changes and DNA fragmentation characteristic of apoptosis in NB4 human promyelocytic leukemia cells in vitro. Arsenite also causes damage or degradation of the fusion protein PML/RAR-alpha.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Arsenic trioxide
Synonyms: Arsenic Trioxide [UN1561] [Poison]; Arsenic, White; Arsenic Sesquioxide; Arsenic Oxidearsenous Trioxide; Arsenic Oxide; Arsenic Blanc [French]; Arseni Trioxydum; Anhydride Arsenieux [French]; Acide Arsenieux [French]; Arsenigen Saure [German]; Arsenious Acid; Arsenious Acid Anhydride; Arsenious Oxide; Arsenious Trioxide; Arsenous Acid; Arsenous Acid Anhydride; Arsenous Anhydride; Arsenous Oxide; Arsenous Oxide Anhydride; Arsentrioxide; Di-Arsenic Trioxide; Diarsenic Trioxide; Diarsonic Trioxide; Oxyde Arsenieux [ISO-French]; Poison Flour; White Arsenic; HSDB 419; Crude Arsenic; Arsenicum Album
Drug Category: Antineoplastic Agents; Homeopathic Agents
Drug Type: Small Molecule; Approved; Investigational
Other Brand Names containing Arsenic trioxide: Arsenite; Arsenolite; Arsodent; Claudelite; Claudetite; Trisenox;
Absorption: Not Available
Toxicity (Overdose): Symptoms of overdose include convulsions, muscle weakness and confusion.
Protein Binding: 75% bound
Biotransformation: The metabolism of arsenic trioxide involves reduction of pentavalent arsenic to trivalent arsenic by arsenate reductase and methylation of trivalent arsenic to monomethylarsonic acid and monomethylarsonic acid to dimethylarsinic acid by methyltransferases. The main site of methylation reactions appears to be the liver. Arsenic is stored mainly in liver, kidney, heart, lung, hair and nails.
Half Life: Not Available
Dosage Forms of Arsenite: Tablet Oral
Chemical IUPAC Name: 2,4,5-trioxa-1,3-diarsabicyclo[1.1.1]pentane
Chemical Formula: As2O3
Arsenic trioxide on Wikipedia: http://en.wikipedia.org/wiki/Arsenic_trioxide
Organisms Affected: Humans and other mammals