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Stibophen is an anthelmintic classified as antimony compound and used as treatment of schistosomiasis^[1] by intramuscular injection.

Mechanism of action[edit]

Stibophen inhibits the enzyme phosphofructokinase, which the worms need for glycolysis,^[2] at least partly by binding to the sulfhydryl (–SH) group of the enzyme.^[3] Inhibiting glycolysis paralyzes the worms, which lose their hold on the wall of mesenteric veins and undergo hepatic shift, die, and are phagocytosed by liver cells.^{[citation needed]}

References[edit]

^ Miller, M. J.; Lyon, H. P. (1955). "Treatment of vesical schistosomiasis with stibophen". The American journal of tropical medicine and hygiene 4 (6): 1049–1056. PMID 13268811. edit
^ Bueding, E.; Mansour, J. M. (1957). "The relationship between inhibition of phosphofructokinase activity and the mode of action of trivalent organic antimonials on Schistosoma mansoni". British journal of pharmacology and chemotherapy 12 (2): 159–165. PMC 1509678. PMID 13446367. edit
^ Su, J. G.; Mansour, J. M.; Mansour, T. E. (1996). "Purification, kinetics and inhibition by antimonials of recombinant phosphofructokinase from Schistosoma mansoni". Molecular and biochemical parasitology 81 (2): 171–178. PMID 8898332. edit

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English Journal

Purification, kinetics and inhibition by antimonials of recombinant phosphofructokinase from Schistosoma mansoni.

Su JG, Mansour JM, Mansour TE.SourceDepartment of Molecular Pharmacology, Stanford University School of Medicine, CA 94305-5332, USA.
Molecular and biochemical parasitology.Mol Biochem Parasitol.1996 Oct 30;81(2):171-8.
We reported before on the cloning of a cDNA encoding S. mansoni PFK. In the present investigation we established optimal conditions for expression of the enzyme in insect cells with high yield. The recombinant PFK was purified to homogeneity. Kinetic properties of the pure enzyme were studied with r
PMID 8898332

[Hemolytic anemia caused by excessive use of analgesics].

Kachel L, Krawczyk-Kuliś M, Hołowiecki J.SourceKliniki Hematologii Sl. Ak. Med., Katowicach.
Wiadomości lekarskie (Warsaw, Poland : 1960).Wiad Lek.1992 Jan;45(1-2):52-4.
A 40-year-old female patient is reported who gave a history of analgesics abuse (phenacetin) and had haemolytic anaemia. The probable mechanism of the toxic effect of phenacetin on the haemopoietic system through induction of intravascular haemolysis (so called stibophen-type haemolysis) is discusse
PMID 1295239

Cyclic AMP-dependent and independent protein kinases in Ascaridia galli.

Ossikovski E, Walter RD.AbstractThe occurrence of multiple protein kinases, distinguished with respect to molecular weight and preference for acceptor proteins, was demonstrated in Ascaridia galli. The molecular weights of the cyclic AMP-dependent protein kinase and of phosvitin kinase I and II - both independent of cyclic AMP-were determined to be 160000, greater than 200000 and 40000, respectively. The cyclic AMP-dependent protein kinase preferred histones and kemptide as acceptor substrates; stimulation of enzyme activity was up to 4-fold by cyclic AMP. The activities of phosvitin kinase I and II were found to be effectively inhibited by suramin. The inhibition constants were calculated to be 2 microM and 5 microM, respectively. In addition, stibophen turned out to be a potent inhibitor of phosvitin kinase I; the inhibition constant was determined to be 10 microM.
Molecular and biochemical parasitology.Mol Biochem Parasitol.1984 Jul;12(3):299-306.
The occurrence of multiple protein kinases, distinguished with respect to molecular weight and preference for acceptor proteins, was demonstrated in Ascaridia galli. The molecular weights of the cyclic AMP-dependent protein kinase and of phosvitin kinase I and II - both independent of cyclic AMP-wer
PMID 6090901

Japanese Journal

:稀用薬の入手緩和を求めて

田辺清勝,尾辻義人,中林敏夫,大友弘士,田中寛
Japanese Journal of Tropical Medicine and Hygiene 17(3), 229-236, 1989
昭和55 (1980) 年に発足した厚生省「輸入熱帯病の治療薬に関する研究」班では, 寄生虫病の治療に稀用される薬剤の入手緩和を計ることを検討してきた。わが国の薬事で承認されていない寄生虫薬で, 海外においては一部で既に使用されている16種の薬剤, すなわちファンシダール, クロロキン, プリマキン, キニーネ (注射液), ファンシメフの抗マラリア薬とそれ以外のミンテゾール, メベンダゾール, …
NAID 130003795724

Related Pictures

★リンクテーブル★

リンク元	「駆虫薬」「薬剤性自己免疫性溶血性貧血」

「駆虫薬」

Stibophen
Systematic (IUPAC) name
	Pentasodium 2-(2-oxido-3,5-disulfonatophenoxy)-1,3,2-benzodioxastibole-5,7-disulfonate
Clinical data
Legal status	?
Identifiers
CAS number	23940-36-5
ATC code	P02BX03
PubChem	CID 16683091
Chemical data
Formula	C12H4Na5O16S4Sb
Mol. mass	769.12 g/mol
	SMILES C1=C(C=C2C(=C1S(=O)(=O)[O-])O[Sb](O2)OC3=CC(=CC(=C3[O-])S(=O)(=O)[O-])S(=O)(=O)[O-])S(=O)(=O)[O-].[Na+].[Na+].[Na+].[Na+].[Na+];
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　　[★]

英: anthelmintic, anthelmintics
ラ: anthelmintica
関

http://en.wikipedia.org/wiki/Anthelmintic

antiplatyhelmintic agents	Antitrematodals (schistosomicides)	binds tubulin	benzimidazole (Triclabendazole#)
		acetylcholinesterase inhibitor	phosphonic acid (metrifonate)
		Other/unknown	quinoline (praziquantel#, oxamniquine#) · phenol (bithionol) · thiazole ([[niridazole]) · arylsulfonate (stibophen)
	anticestodals (taeniacides)	binds tubulin	benzimidazole (albendazole#)
	anticestodals (taeniacides)	Other/unknown	salicylanilide (niclosamide)# · aminoacridine (quinacrine) · butyrophenone (desaspidin) · chlorophenol (dichlorophen)
antinematodal agents (macrofilaricides)		binds tubulin	benzimidazole (mebendazole#, thiabendazole, albendazole#, 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

「薬剤性自己免疫性溶血性貧血」

　　[★]

英: drug-induced autoimmune hemolytic anemia
関: 自己免疫性溶血性貧血

キニジン quinidine

機序 (WCH.1175)

drug adsorption mechanism: penicillin type
neoantigen mechanism(immunne complex, innocent by stander mechanism): quinidine/stibophen type

薬物と特定の型の赤血球上に存在する抗原が新しい抗原を作り、これを自己抗体が認識する
薬単体や、薬と特定の型を持たない赤血球にたいしては自己抗体を作らない(特定の型の赤血球とはI,Rh)。

autoimmune mechanism: α-methyldopa type
nonimmunologic protein adsorption mechanism
multiple mechanism

[1] Miller, M. J.; Lyon, H. P. (1955). "Treatment of vesical schistosomiasis with stibophen". The American journal of tropical medicine and hygiene 4 (6): 1049–1056. PMID 13268811. edit

[2] Bueding, E.; Mansour, J. M. (1957). "The relationship between inhibition of phosphofructokinase activity and the mode of action of trivalent organic antimonials on Schistosoma mansoni". British journal of pharmacology and chemotherapy 12 (2): 159–165. PMC 1509678. PMID 13446367. edit

[3] Su, J. G.; Mansour, J. M.; Mansour, T. E. (1996). "Purification, kinetics and inhibition by antimonials of recombinant phosphofructokinase from Schistosoma mansoni". Molecular and biochemical parasitology 81 (2): 171–178. PMID 8898332. edit

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案内

stibophen