関: carbazochrome sodium sulfonate

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/09/23 04:34:02」(JST)

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Carbazochrome is an antihemorrhagic, or hemostatic, agent that will cease blood flow by causing the aggregation and adhesion of platelets in the blood to form a platelet plug, ceasing blood flow from an open wound. It is hoped that this drug can be used in the future for preventing excessive blood flow during surgical operations and the treatment of hemorrhoids, but research on its effectiveness and the severity of possible side effects remains to be fairly inconclusive.

With troxerutin, it has been investigated for use in the treatment of hemorrhoids.^[1]^[2]

Indications

Capillary and parenchymal hemorrhage (trauma, tonsillectomy, during surgery), intestinal bleeding, thrombocytopenic purpura.

Mechanism of action

Carbazochrome, the semicarbazone of adrenochrome, that interacts with α-adrenoreceptors on surface of platelets, which are coupled to Gq protein and initiate PLC IP3/DAG pathway to increase intracellular free calcium concentration with these subsequent actions:

Activates PLA2 and induce arachidonic acid pathway to synthese endoperoxides (TxA2, thromboxane A2)
Calcium binds to calmodulin which then binds and activates myosin light-chain kinase, that will enable the myosin crossbridge to bind to the actin filament and allow contraction to begin. This will change platelet’s shape and induce release of serotonin, ADP, vWF (Von Willebrand factor), PAF (Platelet-activating factor) to promote further aggregation and adhesion.

Vector

Because of its poor solubility in water it must be first thoroughly dissolved in alcohol, melted fat (butter), or vegetable oil (to aid in absorption) and then ingested.^[3]

References

^ Basile M, Gidaro S, Pacella M, Biffignandi PM, Gidaro GS (2001). "Parenteral troxerutin and carbazochrome combination in the treatment of post-hemorrhoidectomy status: a randomized, double-blind, placebo-controlled, phase IV study". Curr Med Res Opin. 17 (4): 256–61. PMID 11922398. doi:10.1185/030079901753403144.
^ Squadrito F, Altavilla D, Oliaro Bosso S (2000). "Double-blind, randomized clinical trial of troxerutin-carbazochrome in patients with hemorrhoids". Eur Rev Med Pharmacol Sci. 4 (1-2): 21–4. PMID 11409185.
^ Gottlieb, Adam; Legal Highs: A Concise Encyclopedia of Legal Herbs and Chemicals with Psychoactive Properties (1973) 20th Century Alchemist

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English Journal

Fluorescence quenching method for the determination of carbazochrome sodium sulfonate with aromatic amino acids.

Gan XJ, Liu SP, Liu ZF, Hu XL, Tian J, Xue JX.SourceEducation Ministry Key Laboratory on Luminescence and Real-Time Analysis, School of Chemistry and Chemical Engineering, Southwest University, Chongqing, China.
Luminescence : the journal of biological and chemical luminescence.Luminescence.2013 May-Jun;28(3):265-9. doi: 10.1002/bio.2375. Epub 2012 Apr 30.
In Britton-Robinson (BR) buffer medium (pH 3.3), carbazochrome sodium sulfonate (CSS) can react with some aromatic amino acids such as tryptophan (Trp), tyrosine (Tyr) and phenylalanine (Phe) to form a 1:1 complex by electrostatic attraction, aromatic stacking interaction and Van der Waals' force, r
PMID 22544487

Multiple targeted drugs carrying biodegradable membrane barrier: anti-adhesion, hemostasis, and anti-infection.

Wang H, Li M, Hu J, Wang C, Xu S, Han CC.SourceState Key Laboratory of Polymer Physics and Chemistry, Joint Laboratory of Polymer Science and Materials, Beijing National Laboratory for Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, P. R. China.
Biomacromolecules.Biomacromolecules.2013 Apr 8;14(4):954-61. doi: 10.1021/bm301997e. Epub 2013 Mar 12.
A multiple targeted drug carrying bilayer membrane for preventing an abdominal adhesion is prepared by electrospinning. Two bioactive drugs were successfully incorporated into this bilayer membrane and can be independently released from nanofibrous scaffolds without losing structural integrity and f
PMID 23448620

A case of superficial siderosis treated with intravenous and oral hemostatic drugs.

Nanri Y, Yakushiji Y, Yukitake M, Nakahara Y, Matsushima T, Hara H.SourceDivision of Neurology, Department of Internal Medicine, Faculty of Medicine, Saga University.
Rinshō shinkeigaku = Clinical neurology.Rinsho Shinkeigaku.2013;53(6):470-3.
A 39-year-old man suffering from progressive dysarthria, gait disturbance, and sensorineural deafness for 2 years was admitted to our hospital. He scored 28 points on the mini-mental state examination. He had previously undergone surgery at 24 years and 39 years of age for a cerebellar tumor (pilocy
PMID 23782826

Japanese Journal

間質性膀胱炎に対するカルバゾクロムスルホン酸ナトリウムの効果

西日本泌尿器科 = The Nishinihon journal of urology 77(9), 326-332, 2015-09
NAID 40020595123

ドラフトチューブ付き噴流層スプレーコーターによる超低粘度ヒドロキシプロピルセルロースを用いた微小核粒子への薬物レイヤリング

粉体工学会誌 52(3), 145-149, 2015
NAID 130005062047

最新原著レビュー人工膝関節全置換術におけるトラネキサム酸を用いたドレーンクランプ法による深部静脈血栓症のリスク

整形外科 = Orthopedic surgery 64(6), 589-591, 2013-06
NAID 40019691574

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★リンクテーブル★

リンク元	「カルバゾクロム」
拡張検索	「carbazochrome sodium sulfonate」

「カルバゾクロム」

Carbazochrome
Clinical data
Trade names	Toxivenol
AHFS/Drugs.com	International Drug Names
Routes of; administration	P/O, I/M
ATC code	B02BX02 (WHO);
Identifiers
	IUPAC name [(3-Hydroxy-1-methyl-6-oxo-2,3-dihydroindol-5-ylidene)amino]urea;
CAS Number	69-81-8;
PubChem CID	5360410;
DrugBank	DB09012 ;
ChemSpider	4514501;
UNII	81F061RQS4;
ChEMBL	CHEMBL2051960;
ECHA InfoCard	100.000.652
Chemical and physical data
Formula	C10H12N4O3
Molar mass	236.23 g/mol
3D model (JSmol)	Interactive image;
	SMILES O=C(N)N/N=C1/C=C2\C(=C/C1=O)N(CC2O)C ;
	InChI InChI=1S/C10H12N4O3/c1-14-4-9(16)5-2-6(12-13-10(11)17)8(15)3-7(5)14/h2-3,9,16H,4H2,1H3,(H3,11,13,17)/b12-6- ; Key:XSXCZNVKFKNLPR-SDQBBNPISA-N ;
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