In pig folliculitis, acetasitol (20 mg/kg; po; once daily for 4 days) has anti-infectious action [1].

Animal/Disease Models: 2-month-old E. coli-infected piglets [1]
Doses: 20 mg/kg
Route of Administration: Po; one time/day for 4 days
Experimental Results: 65% of piglets demonstrated clinical recovery, and no animal diarrhea was observed at the end of treatment .

Absorption, Distribution and Excretion
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.

---

Metabolism / Metabolites
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)

---

Biological Half-Life
This pharmacokinetic property was not addressed.

Toxicity Summary
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)

---

Protein Binding
This pharmacokinetic property was not addressed.

[1]. Argyriou K, et al. Acetarsol in the management of mesalazine-refractory ulcerative proctitis: a tertiary-level care experience. Eur J Gastroenterol Hepatol. 2019 Feb;31(2):183-186.
[2]. V.S. Pandey, et al. Successful therapy of balantidiosis of pigs with acetarsol and oxytetracycline. Veterinary parasitology. 1977, 3(2):189-193.

Acetarsol is a member of acetamides and an anilide.
Acetarsol, with the molecular formula N-acetyl-4-hydroxy-m-arsanilic acid, is a pentavalent arsenical compound with antiprotozoal and antihelmintic properties. It was first discovered in 1921 by Ernest Fourneau at the Pasteur Institute. It was developed by Neolab Inc, and approved by Health Canada as an antifungal on December 31, 1964. It has been canceled and withdrawn from the market since August 12, 1997.
Acetarsol is a pentavalent arsenical compound with antiprotozoal and antihelmintic properties. Although its mechanism of action is not fully known, acetarsone may bind to protein-containing sulfhydryl groups located in the parasite, thereby forming lethal As-S bonds. This may prevent their functioning and eventually kill the parasite.
Acetarsol is a chemical compound of arsenic. It is used as an anti-infective. Arsenic is a chemical element that has the symbol As and atomic number 33. It is a poisonous metalloid that has many allotropic forms: yellow (molecular non-metallic) and several black and grey forms (metalloids) are a few that are seen. Three metalloidal forms of arsenic with different crystal structures are found free in nature (the minerals arsenopyrite and the much rarer arsenolamprite and pararsenolamprite), but it is more commonly found as a compound with other elements. (T3, T59)

---

Drug Indication
Acetarsol has been used for the treatment of different diseases such as syphilis, amoebiasis, yaws, trypanosomiasis, and malaria. Acetarsol was used commonly for the treatment of vaginitis due to _Trichomonas vaginalis_ and _Candida albicans_. When orally administered, acetarsol can be used for the treatment of intestinal amoebiasis and in the form of suppositories it has been researched for the treatment of proctitis. Protozoan infections are parasitic diseases characterized to be caused by organisms classified in the kingdom Protozoa which is formed by a great diversity of organisms.

---

Mechanism of Action
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.

---

Pharmacodynamics
Some reports indicate a certain infection remission with the use of acetarsol but this reports also demonstrate the absorption of systemic arsenic which can be physiologically dangerous.

C8H10ASNO5

275.09

274.977

97-44-9

55588-51-7 (unspecified hydrochloride salt);5892-48-8 (mono-hydrochloride salt);64046-96-4 (calcium salt);64046-96-4 (unspecified calcium salt)

1985

White to off-white solid powder

72.17°C

220.5°C

4

5

2

15

289

0

O=C(C)NC1C(O)=CC=C([As](O)(O)=O)C=1

ODFJOVXVLFUVNQ-UHFFFAOYSA-N

InChI=1S/C8H10AsNO5/c1-5(11)10-7-4-6(9(13,14)15)2-3-8(7)12/h2-4,12H,1H3,(H,10,11)(H2,13,14,15)

m-Arsanilic acid, N-acetyl-4-hydroxy-

Amarsan OsarsolAmoebal Vagisept NSC-13160 NSC13160NSC 13160

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~20.83 mg/mL (~75.72 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (7.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

---

Solubility in Formulation 2: ≥ 2.08 mg/mL (7.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

---

 (Please use freshly prepared in vivo formulations for optimal results.)