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Carbazochrome

Carbazochrome structure

CAS No:
69-81-8
Formula:
C10H12N4O3
Chemical Name:
Carbazochrome
Synonyms:
Hydrazinecarboxamide,2-(1,2,3,6-tetrahydro-3-hydroxy-1-methyl-6-oxo-5H-indol-5-ylidene)-;Adrenochrome semicarbazone;5,6-Indolinedione,3-hydroxy-1-methyl-,5-semicarbazone;2-(1,2,3,6-Tetrahydro-3-hydroxy-1-methyl-6-oxo-5H-indol-5-ylidene)hydrazinecarboxamide;Adrenoxyl;Carbazochrome;Adrenostazin;Adrokson;Adroxon;Sangostazin;3-Hydroxy-1-methyl-5,6-indolindione 5-semicarbazone;Adchnon;Cromadrenal;Adedolon;Adrezon;Sangostasin;Carbazochrom;Cartabes;Adrenochrome monosemicarbazone;Cromosil;NSC 73742;2-(3-Hydroxy-1-methyl-6-oxo-2,3-dihydro-1H-indol-5(6H)-ylidene)hydrazinecarboxamide;51055-36-8
Categories:
Active Pharmaceutical Ingredients > Blood System Drugs

Description

Carbazochrome is a member of indoles. It derives from a semicarbazide.|Carbazochrome is a hemostatic agent that promotes clotting, preventing blood loss from open wounds. It is an oxidation product of adrenaline which enhances the microcirculatory tone. In the future this may prevent excessive blood flow during surgical operations and the treatment of hemorrhoids, but research on effectiveness and severity of side effects remains inconclusive. It is not FDA-approved but is available as tablets or IM/SC injections in the treatment of hemorrhages in a number of countries. Carbazochrome has been investigated for use in the treatment of non-surgical acute uncomplicated hemorrhoids in a mixture with [DB13124], and this combination therapy demonstrated efficacy and safe tolerability either at a local or systemic level.

Carbazochrome Basic Attributes

Molecular Weight：

236.23

Exact Mass：

236.23

EC Number：

200-717-0

NSC Number：

73742

DSSTox ID：

DTXSID3048310

ATC Code：

B - Blood and blood forming organs

HScode：

2933990090

Characteristics

PSA：

112

XLogP3：

-0.26090

Appearance：

nacarat crystalline powder

Density：

1.6±0.1 g/cm3

Melting Point：

212-213 °C (decomp)

Refractive Index：

1.733

Storage Conditions：

−20°C

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

safety instructions：

24/25

RTECS Number：

NM1925500

Drug Information

Drug Indication：

Indicated for capillary and parenchymal hemorrhage (trauma, tonsillectomy, during surgery), intestinal bleeding, and thrombocytopenic purpura.

Pharmacology：

Carbazochrome is an anti-bleeding agent that increases platelet aggregation and forms a platelet plug by interacting with α-adrenoreceptors on surface of platelets. It is shown to improve the structure of local capillary vessels in haemorrhage caused by fragility of capillaries. Carbazochrome capillary stabilizer that reverses pulmonary vascular hyperpermeability and decreases arterial PaO2 in experimental models.

MeSH：

Agents acting to arrest the flow of blood. Absorbable hemostatics arrest bleeding either by the formation of an artificial clot or by providing a mechanical matrix that facilitates clotting when applied directly to the bleeding surface. These agents function more at the capillary level and are not effective at stemming arterial or venous bleeding under any significant intravascular pressure. (See all compounds classified as Hemostatics.)

Mechanism of Action：

Carbazochrome interacts with platelet surface α-adrenoreceptors which are Gq-coupled receptors that leads to activation of PLC IP3/DAG pathway and increase in intracellular calcium levels. Elevated calcium ions bind to calmodulin and activates Ca2+/calmodulin-dependent myosin light chain kinase, allowing the myosin crossbridge to bind to the actin filament and polymerisation of globular actin (G-actin) to filamentous actin (F-actin). Subsequent contraction of endothelial cells changes the shape of platelets and promotes the release of factors such as serotonin, ADP, Von Willebrand and platelet activating factor by platelets that induce aggregation and platelet adherence. Carbazochrome is reported to inhibit vascular hyperpermeability by inhibiting agonist-induced phosphoinositides hydrolysis caused by various vasoactive agents such as tryptase, thrombin and bradykinin.

MeSH Entry Terms：

AC-17

Carbazochrome Use and Manufacturing

Uses

This product can reduce the permeability of capillaries and promote the retraction of damaged capillaries to stop bleeding. Mainly used for bleeding caused by increased capillary permeability, such as idiopathic purpura, retinal hemorrhage, chronic pulmonary hemorrhage, gastrointestinal bleeding, epistaxis, hemoptysis, hematuria, hemorrhoidal bleeding, uterine bleeding, cerebral hemorrhage, etc. It is less effective for massive bleeding and arterial bleeding. Hemostatic drug, used for persistent Zipan syndrome, hereditary capillary dilation, and prevention of bleeding in the lungs, kidneys, intestines, brain, and uterus.

Use Classification：

Pharmaceuticals -> Animal Drugs -> Approved in Taiwan

Computed Properties

Molecular Weight:236.23
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:1
Exact Mass:236.09094026
Monoisotopic Mass:236.09094026
Topological Polar Surface Area:112
Heavy Atom Count:17
Complexity:336
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Drug Function and Efficacy

It is an oxidized derivative of adrenaline and has no adrenaline-mimetic effect, so it does not affect blood pressure and heart rate, but it can enhance the resistance of capillaries to damage, stabilize the acidic mucopolysaccharides in blood vessels and surrounding tissues, reduce the permeability of capillaries, and enhance the retraction effect of damaged capillary ends, making it difficult for blood clots to fall off the tube wall, thereby shortening the hemostasis time, but it does not affect the coagulation process.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Adrenaline injection
Ingredients	Chemical name: 3-Hydroxy-1-methylindoline-5,6-dione semicarbazone
Indication	The vasodilator effect of antihistamines and anticholinergics may affect the hemostatic effect of this product. If used in combination, the dosage of this product should be increased. Avoid administering it in the same solution with tetracycline drugs.
Specifications	1ml:5mg
Manufacturer	Anhui Changjiang Pharmaceutical Co., Ltd.

Adrenaline injection
Ingredients	Chemical name: 3-Hydroxy-1-methylindoline-5,6-dione semicarbazone
Indication	The vasodilator effect of antihistamines and anticholinergics may affect the hemostatic effect of this product. If used in combination, the dosage of this product should be increased. Avoid administering it in the same solution with tetracycline drugs.
Specifications	1ml:5mg
Manufacturer	Suicheng Pharmaceutical Co., Ltd.

Adrenaline hydrazone tablets
Ingredients	Chemical name: 3-Hydroxy-1-methylindoline-5,6-dione semicarbazone
Indication	The vasodilatory effect of antihistamines and anticholinergics may affect the hemostatic effect of this product. If used in combination, the dosage of this product should be increased.
Specifications	5mg
Manufacturer	Guangzhou Baiyunshan Guanghua Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

China Resources Double-Crane Pharmaceutical Co., Ltd.

China
Active
Wuhan Wuyao Pharmaceutical Co., Ltd.

China
Active
Changzhou Yabang Pharmaceutical Co., Ltd.

China
Active

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