Acetarsol (or acetarsone) is an anti- infective drug. It was first discovered in 1921 at

Pasteur Institute The Pasteur Institute (, ) is a French non-profit private foundation dedicated to the study of biology, micro-organisms, diseases, and vaccines. It is named after Louis Pasteur, who invented pasteurization and vaccines for anthrax and rabies. Th ...

by Ernest Fourneau, and sold under the brand name Stovarsol. It has been given in the form of

suppositories A suppository is a dosage form used to deliver pharmaceutical drug, medications by insertion into a body orifice (any opening in the body), where it dissolves or melts to exert local or systemic effects. There are three types of suppositories, eac ...

. Acetarsol can be used to make arsthinol. It has been cancelled and withdrawn from the market since August 12th, 1997.

Medical uses

Acetarsol has been used for the treatment of diseases such as

syphilis Syphilis () is a sexually transmitted infection caused by the bacterium ''Treponema pallidum'' subspecies ''pallidum''. The signs and symptoms depend on the stage it presents: primary, secondary, latent syphilis, latent or tertiary. The prim ...

amoebiasis Amoebiasis, or amoebic dysentery, is an infection of the intestines caused by a parasitic amoeba '' Entamoeba histolytica''. Amoebiasis can be present with no, mild, or severe symptoms. Symptoms may include lethargy, loss of weight, colon ...

yaws Yaws is a tropical infection of the skin, bones, and joints caused by the spirochete bacterium ''Treponema pallidum pertenue''. The disease begins with a round, hard swelling of the skin, in diameter. The center may break open and form an ulc ...

, trypanosomiasisiasis and

malaria Malaria is a Mosquito-borne disease, mosquito-borne infectious disease that affects vertebrates and ''Anopheles'' mosquitoes. Human malaria causes Signs and symptoms, symptoms that typically include fever, Fatigue (medical), fatigue, vomitin ...

. Acetarsol was used for the treatment of ''Trichomonas Vaginalis'' and ''Candida Albicans.'' In the oral form, acetarsol can be used for the treatment of intestinal amoebiasis. As a suppository, acetarsol was researched to be used for the treatment of proctitis.

Mechanism of action

Although the mechanism of action is not fully known, acetarsol may bind to protein-containing

sulfhydryl In organic chemistry, a thiol (; ), or thiol derivative, is any organosulfur compound of the form , where R represents an alkyl or other organic substituent. The functional group itself is referred to as either a thiol group or a sulfhydryl grou ...

groups located in the parasite, which then creates lethal As-S bonds, which then kills the parasite.

Chemistry and pharmacokinetics

Acetarsol has the molecular formula ''N''-acetyl-4-hydroxy-''m''-arsinillic acid, and it is a

pentavalent In chemistry, the valence (US spelling) or valency (British spelling) of an atom is a measure of its combining capacity with other atoms when it forms chemical compounds or molecules. Valence is generally understood to be the number of chemica ...

arsenical Arsenicals are chemical compounds that contain arsenic. In a military context, the term arsenical refers to toxic arsenic compounds that are used as chemical warfare agents. This includes blister agents, blood agents and vomiting agents. Historica ...

compound with

antiprotozoal Antiprotozoal agents ( ATC code: ATC P01) is a class of pharmaceuticals used in treatment of protozoan infection. A paraphyletic group, protozoans have little in common with each other. For example, '' Entamoeba histolytica'', a unikont eukary ...

and

anthelmintic Anthelmintics or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them without causing significant damage to the host. They may also ...

properties. The arsenic found in acetarsol is excreted mainly in urine. The level of arsenic after acetarsol administration reaches close to the toxic range in urine. Some reports indicate a remission of arsenic which can be physiologically dangerous.

Toxicity

Some reports indicate that acetarsol can produce effects in the eyes such as optic

neuritis Neuritis (), from the Greek ), is inflammation of a nerve or the general inflammation of the peripheral nervous system. Inflammation, and frequently concomitant demyelination, cause impaired transmission of neural signals and leads to aberrant ne ...

and

optic atrophy Optic neuropathy is damage to the optic nerve from any cause. The optic nerve is a bundle of millions of fibers in the retina that sends visual signals to the brain. Damage and death of these nerve cells, or neurons, leads to characteristic featu ...

References

{{Agents against leishmaniasis and trypanosomiasis Antiprotozoal agents Acetanilides Arsonic acids Phenols