Niclosamide Explained

Niclosamide, sold under the brand name Niclocide among others, is an anthelmintic medication used to treat tapeworm infestations, including diphyllobothriasis, hymenolepiasis, and taeniasis. It is not effective against other worms such as flukes or roundworms.[1] It is taken by mouth.[2]

Side effects include nausea, vomiting, abdominal pain, and itchiness. It may be used during pregnancy.[2] It works by blocking glucose uptake and oxidative phosphorylation by the worm.[3]

Niclosamide was first synthesized in 1958.[4] It is on the World Health Organization's List of Essential Medicines.[5] Niclosamide is not available for human use in the United States.[6]

Side effects

Side effects include nausea, vomiting, abdominal pain, constipation, and itchiness.[2] Rarely, dizziness, skin rash, drowsiness, perianal itching, or an unpleasant taste occur. For some of these reasons, praziquantel is a preferable and equally effective treatment for tapeworm infestation.Important Note: Niclosamide kills the pork tapeworm and results in its digestion. This then may cause a multitude of viable eggs to be released and may result in cysticercosis. Therefore, a purge should be given 1 or two hours after treatment. CNS cysticercosis is a life-threatening condition and may require brain surgery.[7] [8]

Mechanism of action

Niclosamide inhibits glucose uptake, oxidative phosphorylation, and anaerobic metabolism in the tapeworm.[9]

Other applications

Niclosamide's metabolic effects are relevant to a wide ranges of organisms, and accordingly it has been applied as a control measure to organisms other than tapeworms. For example, it is an active ingredient in some formulations such as Bayluscide for killing lamprey larvae,[10] [11] as a molluscide,[12] and as a general purpose piscicide in aquaculture. Niclosamide has a short half-life in water in field conditions; this makes it valuable in ridding commercial fish ponds of unwanted fish; it loses its activity soon enough to permit re-stocking within a few days of eradicating the previous population.[12] Researchers have found that niclosamide is effective in killing invasive zebra mussels in cool waters.[13]

Research

Niclosamide is under investigation for applications against types of cancer,[14] bacterial infections,[15] or viral infections.[16] [17]

In 2018, niclosamide was observed to be a potent activator of PTEN-induced kinase 1 in primary cortical neurons.[18]

Further reading

External links

Notes and References

  1. Web site: Niclosamide Advanced Patient Information - Drugs.com. www.drugs.com. 8 December 2016 . live . https://web.archive.org/web/20161220223834/https://www.drugs.com/cons/niclosamide.html. 20 December 2016.
  2. Book: WHO Model Formulary 2008 . 2009 . 9789241547659 . ((World Health Organization)) . Stuart MC, Kouimtzi M, Hill SR . 10665/44053 . World Health Organization . World Health Organization . free . 81, 87, 591 .
  3. Book: Antinematodal Drugs . Lanusse CE, Alvarez LI, Sallovitz JM, Mottier ML, Sanchez Bruni SF . Riviere JE, Papich MG . Veterinary Pharmacology and Therapeutics . https://books.google.com/books?id=xAPa4WDzAnQC&pg=PA1096 . 13 May 2013 . John Wiley & Sons . 978-1-118-68590-7 . 1096 . live . https://web.archive.org/web/20170910145626/https://books.google.com/books?id=xAPa4WDzAnQC&pg=PA1096 . 10 September 2017.
  4. Book: Mehlhorn H . Encyclopedia of Parasitology: A-M . 2008 . Springer Science & Business Media . 978-3-540-48994-8 . 483 . live . https://web.archive.org/web/20161220080803/https://books.google.ca/books?id=Jpg1ysgVn-AC&pg=PA483 . 2016-12-20 .
  5. Book: ((World Health Organization)) . World Health Organization model list of essential medicines: 21st list 2019 . 2019 . 10665/325771 . World Health Organization . World Health Organization . Geneva . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO . free .
  6. Web site: Dipylidium – Resources for Health Professionals . U.S. Centers for Disease Control and Prevention (CDC) . 21 May 2020 .
  7. Book: Remington JP, Osol A . Remington's Pharmaceutical Sciences . 16th . Mack Pub. Co. . Easton . 1980. 1182 . 925174053.
  8. Book: The Merck Manual of Diagnosis and Therapy . 1982 . Merck Sharp & Dohme Research Laboratories . Rahway . 978-0-911910-03-2 . 14th . 176 .
  9. Weinbach EC, Garbus J . Mechanism of action of reagents that uncouple oxidative phosphorylation . Nature . 221 . 5185 . 1016–1018 . March 1969 . 4180173 . 10.1038/2211016a0 . 4209497 . 1969Natur.221.1016W .
  10. Web site: Michael . Boogaard . Delivery Systems of Piscicides . dead . https://web.archive.org/web/20170601223345/https://www.usbr.gov/lc/phoenix/biology/azfish/pdf/borfinalreport6t7.pdf . 2017-06-01 . 2017-05-30.
  11. Journal of Great Lakes Research . 29 . Supplement 1 . 2003 . 475–492 . Environmental Fate and Effects of the Lampricide Bayluscide: a Review . Verdel K.Dawson . 10.1016/S0380-1330(03)70509-7 . 2003JGLR...29..475D .
  12. Web site: WHO Specifications And Evaluations. For Public Health Pesticides. Niclosamide . 2019-08-07 . https://web.archive.org/web/20170110145622/http://www.who.int/whopes/quality/en/Niclosamide.pdf . 2017-01-10 . dead .
  13. News: Blank L . 30 October 2018 . Researchers find new methods to combat invasive zebra mussels. The Minnesota Daily. 2018-11-19. 2018-11-21. https://web.archive.org/web/20181121072648/http://www.mndaily.com/article/2018/10/n-researchers-find-new-methods-to-combat-invasive-zebra-mussels. dead.
  14. Web site: Clinical Trials Using Niclosamide . NCI . 20 March 2019.
  15. Rajamuthiah R, Fuchs BB, Conery AL, Kim W, Jayamani E, Kwon B, Ausubel FM, Mylonakis E . 6 . Repurposing salicylanilide anthelmintic drugs to combat drug resistant Staphylococcus aureus . PLOS ONE . 10 . 4 . e0124595 . April 2015 . 25897961 . 4405337 . 10.1371/journal.pone.0124595 . Planet PJ . 2015PLoSO..1024595R . free .
  16. Li Y, Li P, He Q, Zhang R, Li Y, Kamar N, Peppelenbosch MP, de Man RA, Wang L, Pan Q . 6 . Niclosamide inhibits hepatitis E virus through suppression of NF-kappaB signalling . Antiviral Research . 197 . 105228 . January 2022 . 34929248 . 10.1016/j.antiviral.2021.105228 . free .
  17. Braga L, Ali H, Secco I, Chiavacci E, Neves G, Goldhill D, Penn R, Jimenez-Guardeño JM, Ortega-Prieto AM, Bussani R, Cannatà A, Rizzari G, Collesi C, Schneider E, Arosio D, Shah AM, Barclay WS, Malim MH, Burrone J, Giacca M . 6 . Drugs that inhibit TMEM16 proteins block SARS-CoV-2 spike-induced syncytia . Nature . 594 . 7861 . 88–93 . June 2021 . 33827113 . 7611055 . 10.1038/s41586-021-03491-6 . 2021Natur.594...88B .
  18. Barini E, Miccoli A, Tinarelli F, Mulholland K, Kadri H, Khanim F, Stojanovski L, Read KD, Burness K, Blow JJ, Mehellou Y, Muqit MM . 6 . The Anthelmintic Drug Niclosamide and Its Analogues Activate the Parkinson's Disease Associated Protein Kinase PINK1 . ChemBioChem . 19 . 5 . 425–429 . March 2018 . 29226533 . 5901409 . 10.1002/cbic.201700500 .

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