Sodium arsanilate (atoxyl), was used in the treatment of syphilis and trypanosomiasis, but there have been at least 50 reports in the literaqture on disturbances of vision. By 1932 atoxyl was known to have caused more than 80 cases of blindness and was no longer used .
The dose causing blindness was as small as 0.5 g, but on the average was 7 g. Typically it caused progressive constriction of the visual fields, with the fundus appearing normal at first. Constriction progressed until central vision was involved, and subsequently optic atrophy developed. In some instances there was deafness [2,3]. Atoxyl is highly toxic by ingestion and inhalation .
Inorganic arsenic reduces cellular apoptosis via damage of mitochondrial membranes and down-regulation of BCL2, a pro-survival protein. Arsenic is actively transported into Trypanosomes by a purine transporter resulting in inhibition of trypanothione production and subsequent parasite lysis. Trivalent arsenic (As3+) disrupts oxidative phosphorylation, leading to free radical formation via inhibition of pyruvate dehydrogenase, which subsequently decreases gluconeogenesis due to lack of acetyl-CoA. Pentavalent arsenic may be transformed to arsenic or substitute for inorganic phosphate in glycolysis, leading to uncoupling of oxidative phosphorylation and loss of ATP formation. Chronically, arsenic may cause DNA damage, mutation in the p-53 suppressor gene, and inhibition of DNA repair mechanisms leading to cancer. Organic arsenic has relatively low toxicity when compared to the inorganic trivalent and pentavalent forms.
In cultures of retina in vitro, addition of 5X10-3 M sodium arsanilate has caused degeneration of the rod cells . In guinea pigs, kidney and inner ear structure were studied. Renal tubues were damaged by exposure to atoxyl. Tubular casts, hemorrhages (in the tubules and in renal calices) and tubular epithelial cell necrosis occurred .
LD50 Rat sc 75 mg/kg .
Quantitative analysis of 24 hrs urine after parenteral administration of sodium arsanilate (15 mg As / kg) to rats and guinea pig failed to detect the presence of any As containing material other than unchanged atoxyl .
Absorption, distribution and excretion
Atoxyl (100 mg / kg) subcutaneous administration to guinea pigs was eliminated much more slowly by the cochleae than by blood and muscle. Atoxyl was excreted via kidneys. Blood atoxyl concentration reached a maximum within 0.5 hrs after injection and then decreased rapidly .
Arsanilic acid and its sodium salt are both poorly absorbed from the digestive tract. Sodium arsanilate may be absorbed through intact skin .
CAS number: 127-85-5 EINECS: 204-869-9
COLOR/FORM: White or creamy-white granular powder
TASTE: Faint salty taste
SOLUBILITIES: Soluble 1 in 3 of water and 1 in 150 of alcohol; practically insoluble in chloroform and ether
STORAGE CONDITIONS: Store in airtight containers .
1. Grant, W.M. Toxicology of the Eye. 3rd ed.
Springfield, IL: Charles C. Thomas Publisher, 1986., p. 114
3. Lewis, R.J. Sax's Dangerous Properties of Industrial Materials. 9th ed. Volumes 1-3. New York, NY: Van Nostrand Reinhold, 1996., p. 270.
4. Sax, N.I. and R.J. Lewis, Sr. (eds.). Hawley's Condensed Chemical Dictionary. 11th ed. New York: Van Nostrand Reinhold Co., 1987., p. 1052.
5. Grant, W.M. Toxicology of the Eye. 3rd ed. Springfield, IL: Charles C. Thomas Publisher, 1986., p. 114.
6. ANNIKO M, LJUNGQVIST A; ACTA PATHOL MICROBIOL SCAND SECT A PATHOL 85 (5): 751 (1977.
7. Lewis, R.J. Sax's Dangerous Properties of Industrial Materials. 9th ed. Volumes 1-3. New York, NY: Van Nostrand Reinhold, 1996., p. 270.
8. Lewis, R.J. Sax's Dangerous Properties of Industrial Materials. 9th ed. Volumes 1-3. New York, NY: Van Nostrand Reinhold, 1996., p. 270.
9. CRISTAU B ET AL; ANN PHARM FR 33 (1): 37 (1975).
10. ANNIKO M, PLANTIN LO; ARCH OTO-RHINO-LARYNGOL 215 (1): 81 (1977).
11. Gosselin, R.E., R.P. Smith, H.C. Hodge. Clinical Toxicology of Commercial Products. 5th ed. Baltimore: Williams and Wilkins, 1984., p. II-130.
12. Reynolds, J.E.F., Prasad, A.B. (eds.) Martindale-The Extra Pharmacopoeia. 28th ed. London: The Pharmaceutical Press, 1982., p. 1754.
13. Lewis, R.J., Sr (Ed.). Hawley's Condensed
Chemical Dictionary. 13th ed. New York, NY: John Wiley & Sons, Inc. 1997.,
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