Acetarsol

Slightly soluble

>41.3 [ug/mL] (The mean of the results at pH 7.4)

151.5 Ų [M+H]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]

153.02 Ų [M+K]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]

Danger

H228 (36.1%): Flammable solid [Danger Flammable solids]

P210, P240, P241, P261, P264, P270, P271, P273, P280, P301+P316, P304+P340, P316, P321, P330, P370+P378, P391, P403+P233, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 61 reports by companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Arsenic poisoning can be treated by chelation therapy, using chelating agents such as dimercaprol, EDTA or DMSA. Charcoal tablets may also be used for less severe cases. In addition, maintaining a diet high in sulfur helps eliminate arsenic from the body. (L20)

Arsenic and its metabolites disrupt ATP production through several mechanisms. At the level of the citric acid cycle, arsenic inhibits pyruvate dehydrogenase and by competing with phosphate it uncouples oxidative phosphorylation, thus inhibiting energy-linked reduction of NAD+, mitochondrial respiration, and ATP synthesis. Hydrogen peroxide production is also increased, which might form reactive oxygen species and oxidative stress. Arsenic's carginogenicity is influenced by the arsenical binding of tubulin, which results in aneuploidy, polyploidy and mitotic arrests. The binding of other arsenic protein targets may also cause altered DNA repair enzyme activity, altered DNA methylation patterns and cell proliferation. (T1, A17)

Drug-Induced Liver Injury Severity and Toxicity (DILIst)

ACETARSOL

DILI Positive

Vaginal

DOI:10.1016/j.drudis.2019.09.022

G - Genito urinary system and sex hormones

P - Antiparasitic products, insecticides and repellents

A - Alimentary tract and metabolism

QA - Alimentary tract and metabolism

QG - Genito urinary system and sex hormones

QP - Antiparasitic products, insecticides and repellents

The mechanism of action of acetarsol is not well known but it is thought to bind to protein-containing sulfhydryl groups located in the infective microorganism and to form a lethal As-S bond. The formation of this bond impairs the protein to function and it eventually kills the microorganism.

This pharmacokinetic property was not addressed.

Arsenic is absorbed mainly by inhalation or ingestion, as to a lesser extent, dermal exposure. It is then distributed throughout the body, where it is reduced into arsenite if necessary, then methylated into monomethylarsenic (MMA) and dimethylarsenic acid (DMA) by arsenite methyltransferase. Arsenic and its metabolites are primarily excreted in the urine. Arsenic is known to induce the metal-binding protein metallothionein, which decreases the toxic effects of arsenic and other metals by binding them and making them biologically inactive, as well as acting as an antioxidant. (L20)

The absorption seems to be very minimal but there are reports of allergic reactions after vaginal administration of acetarsol.

The arsenic found in acetarsol is excreted mainly in the urine. The level of arsenic after acetarsol administration almost reaches the toxic range in urine.

This pharmacokinetic property was not addressed.

This pharmacokinetic property was not addressed.