Niridazole

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Niridazole

Systematic (IUPAC) name
1-(5-nitro-1,3-thiazol-2-yl)imidazolidin-2-one
Clinical data
MedlinePlus	a682128
Pregnancy cat.	?
Legal status	?
Identifiers
CAS number	61-57-4
ATC code	P02BX02
PubChem	CID 6093
UNII	N116U8Y5QQ^Y
KEGG	D05170^Y
Chemical data
Formula	C₆H₆N₄O₃S
Mol. mass	214.20 g/mol
Y(what is this?) (verify)

Niridazole is a schistosomicide.^[1] It is used to treat schistosomiasis, the helmintic disease caused by certain flatworms (trematodes) from the genus Schistosoma (formerly Bilharzia). It is also known by its trade name Ambilgar. It is usually is given as tablets. Niridazole has central nervous system toxicity and can cause dangerous side effects, such as hallucinations. Also, it may cause allergic reactions in sensitive people. However, it is one of the most effective schistosomicide drugs.

It has recently also been investigated for use in the treatment of periodontitis.^[2]^[3]

Mechanism of action

Niridazole is rapidly concentrated in the parasite and inhibits oogenesis and spermatogenesis. The compound also inhibits the phosphofructokinase enzyme, leading to glycogen depletion and hepatic shift.

References

^ Tracy, JW; Catto, BA; Webster Lt, LT (1983). "Reductive metabolism of niridazole by adult Schistosoma mansoni. Correlation with covalent drug binding to parasite macromolecules". Molecular pharmacology 24 (2): 291–9. PMID 6193406. edit
^ Barat, R.; Srinatha, A.; Pandit, J.; Mittal, N.; Anupurba, S. (2007). "Ethylcellulose inserts of an orphan drug for periodontitis: preparation, in vitro, and clinical studies". Drug delivery 14 (8): 531–538. doi:10.1080/10717540701606517. PMID 18027183. edit
^ Barat, R.; Srinatha, A.; Pandit, J.; Ridhurkar, D.; Balasubramaniam, J.; Mittal, N.; Mishra, D. (2006). "Niridazole biodegradable inserts for local long-term treatment of periodontitis: possible new life for an orphan drug". Drug delivery 13 (5): 365–373. doi:10.1080/10717540500398126. PMID 16877312. edit

Antiparasitics – Anthelmintics (P02)

Antiplatyhelmintic agents

Antitrematodals
(schistosomicides)

Binds tubulin	benzimidazole (Triclabendazole^#)

AI	phosphonic acid (Metrifonate)

Other/unknown	quinoline (Praziquantel^#, Oxamniquine^#) • phenol (Bithionol) • thiazole (Niridazole) • arylsulfonate (Stibophen)

Anticestodals
(taeniacides)

Binds tubulin	benzimidazole (Albendazole^#)

Other/unknown	salicylanilide (Niclosamide)^# • aminoacridine (Quinacrine) • butyrophenone (Desaspidin) • chlorophenol (Dichlorophen)

Antinematodal agents
(including
macrofilaricides)

Binds tubulin	benzimidazole (Mebendazole^#, Albendazole^#, Thiabendazole, Fenbendazole, Ciclobendazole, Flubendazole)

Chloride channel	macrolide (Ivermectin^#)

NMDA	tetrahydropyrimidine (Pyrantel^#, Pyrantel pamoate, Oxantel)

Other/unknown	piperazine (Piperazine • Diethylcarbamazine^#) • thiazole (Levamisole^#) • quinolinium (Pyrvinium) • benzylammonium (Bephenium) • naphthalenesulfonate (Suramin^#) • Tribendimidine

^#WHO-EM. ^‡Withdrawn from market. Clinical trials: ^†Phase III. ^§Never to phase III

M: IFT

helm,arth (acar)

helm, arth (lice), zoon

helm, arth

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