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

Pasteur Institute The Pasteur Institute (french: Institut Pasteur) 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 ...

Ernest Fourneau Ernest Fourneau (4 October 1872 – 5 August 1949) was a French pharmacist graduated in Pharmacy 1898 for the Paris university specialist in medicinal chemical and pharmacology who played a major role in the discovery of synthetic local anesthetic ...

, and sold under the brand name Stovarsol. It has been given in the form of suppositories. 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 It has been cancelled and withdrawn from the market since August 12th, 1997.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,

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, colonic ...

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 ulce ...

, trypanosomiasisiasis and

malaria Malaria is a mosquito-borne infectious disease that affects humans and other animals. Malaria causes symptoms that typically include fever, tiredness, vomiting, and headaches. In severe cases, it can cause jaundice, seizures, coma, or death. S ...

. 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 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 arsenical 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 eukaryot ...

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 and without causing significant damage to the host. They may ...

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 () 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 nerve function. Neuri ...

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

Antiprotozoal agents Acetanilides Arsonic acids Phenols {{Genito-urinary-drug-stub