Мепакрин: Қолданысы, қасиеттері және тарихы

Medication

Mepacrine, also called quinacrine or by the trade names Atabrine or Atebrin (german), is a medication with several uses. It is related to chloroquine and mefloquine. Although formerly available from compounding pharmacies, as of August 2020 it is unavailable in the United States.

The main uses of mepacrine are as an antiprotozoal, antirheumatic, and an intrapleural sclerosing agent. Antiprotozoal use include targeting giardiasis, where mepacrine is indicated as a primary agent for patients with metronidazole resistant giardiasis and patients who should not receive or cannot tolerate metronidazole. Giardiasis that is very resistant may even require a combination of mepacrine and metronidazole. indicated in the treatment of discoid and subcutaneous lupus erythematosus, particularly in patients unable to take chloroquine derivatives.

Its mechanism of action against protozoa is uncertain, but it is thought to act against the protozoan's cell membrane. It is known to act as a histamine N methyltransferase inhibitor. It also inhibits NF κB and activates p53.

Mepacrine was initially approved in the 1930s as an antimalarial drug. It was used extensively during the second World War by Allied forces fighting in North Africa and the Far East to prevent malaria. This antiprotozoal is also approved for the treatment of giardiasis (an intestinal parasite), and has been researched as an inhibitor of phospholipase A2. Scientists at Bayer in Germany first synthesised mepacrine in 1931. The product was one of the first synthetic substitutes for quinine although later superseded by chloroquine.

In addition it has been used for treating tapeworm infections.

The use of mepacrine for non surgical sterilization for women has also been studied. The first report of this method claimed a first year failure rate of 3.1%. However, despite a multitude of clinical studies on the use of mepacrine and female sterilization, no randomized, controlled trials have been reported to date and there is some controversy over its use. mepacrine sterilization (QS) is potentially safer than surgical sterilization. Nevertheless, in 1998 the Supreme Court of India banned the import or use of the drug, allegedly based on reports that it could cause cancer or ectopic pregnancies.

During the Second Sino Japanese War, American Sino American Cooperative Organization operatives yellowed their skin using mepacrine tablets in order to more closely match the skin color of their Chinese peers.