Клофазимин
- английское имяClofazimine
- CAS №2030-63-9
- CBNumberCB6273466
- ФормулаC27H22Cl2N4
- мольный вес473.4
- EINECS217-980-2
- номер MDLMFCD00056793
- файл Mol2030-63-9.mol
химическое свойство
| Температура плавления | 210-212° |
| Температура кипения | 616.26°C (rough estimate) |
| плотность | 1.1342 (rough estimate) |
| показатель преломления | 1.6300 (estimate) |
| температура хранения | 2-8°C |
| растворимость | Practically insoluble in water, soluble in methylene chloride, very slightly soluble in ethanol (96 per cent). It shows polymorphism (5.9). |
| пка | 8.37; also reported as 8.51(at 25℃) |
| форма | Solid |
| цвет | Yellow to Amber to Dark red |
| Растворимость в воде | 10mg/L(temperature not stated) |
| Мерк | 14,2373 |
| BCS Class | 4/3 |
| FDA UNII | D959AE5USF |
| Код УВД | J04BA01 |
| UNSPSC Code | 41116107 |
| NACRES | NA.24 |
| Коды опасности | Xn,Xi | |||||||||
| Заявления о рисках | 22-36/37/38 | |||||||||
| Заявления о безопасности | 36-26 | |||||||||
| WGK Германия | 3 | |||||||||
| RTECS | SG1578000 | |||||||||
| кода HS | 35040000 | |||||||||
| Токсичность | LD50 orally in mice, rats, and guinea pigs: >4 g/kg (Stenger) | |||||||||
| NFPA 704: |
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рисовальное письмо(GHS)
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рисовальное письмо(GHS)
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сигнальный язык
предупреждение
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вредная бумага
H315：При попадании на кожу вызывает раздражение.
H319：При попадании в глаза вызывает выраженное раздражение.
H335：Может вызывать раздражение верхних дыхательных путей.
H413：Может вызвать долгосрочные отрицательные последствия для водных организмов.
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оператор предупредительных мер
P264：После работы тщательно вымыть кожу.
P280：Использовать перчатки/ средства защиты глаз/ лица.
P302+P352：ПРИ ПОПАДАНИИ НА КОЖУ: Промыть большим количеством воды.
P305+P351+P338：ПРИ ПОПАДАНИИ В ГЛАЗА: Осторожно промыть глаза водой в течение нескольких минут. Снять контактные линзы, если Вы ими пользуетесь и если это легко сделать. Продолжить промывание глаз.
P332+P313：При возникновении раздражения кожи: обратиться за медицинской помощью.
Клофазимин химические свойства, назначение, производство
Химические свойства
Red SolidИспользование
antiinflammatory, glucocorticoidОпределение
ChEBI: 3-Isopropylimino-3,5-dihydro-phenazine in which the hydrogen at position 5 is substituted substituted by a 4-chlorophenyl group, and that at position 2 is substituted by a (4-chlorophenyl)amino group. A dark red crystalline solid, clofazimine is an antimyc bacterial and is one of the main drugs used for the treatment of multi-bacillary leprosy. However, it can cause red/brown discolouration of the skin, so other treatments are often preferred in light-skinned patients.Показания
Clofazimine is a weakly bactericidal dye that has some activity against M. leprae. Its precise mechanism of action is unknown but may involve mycobacterial DNA binding. Its oral absorption is quite variable, with 9 to 70% of the drug eliminated in the feces. Clofazimine achieves significant concentrations in tissues, including the phagocytic cells; it has a plasma half-life of 70 days. It is primarily excreted in bile, with less than 1% excretion in urine.Антимикробная активность
The mode of action is not fully understood. It has bacteristatic and weak bactericidal activity against several species of mycobacteria and some species of Actinomyces and Nocardia. In-vitro minimum inhibitory concentrations (MICs) are: M. tuberculosis 0.5 mg/L and M. leprae (assayed in a mouse model) 0.1–1 mg/L, but these MICs have limited clinical relevance as clofazimine shows marked differences in accumulation in various tissues. Activity against M. leprae is demonstrable in humans only after 50 days of therapy. Clofazimine resistance, although reported, appears to be rare.Фармацевтические приложения
One of a number of substituted iminophenazine dyes originally synthesized as potential antituberculosis agents. It is almost insoluble in water. It stimulates various phagocyte functions including release of free oxygen radicals, but it is not clear whether this contributes to its antimicrobial activity. It also has anti-inflammatory properties, attributed to its ability to inhibit certain patterns of intracellular T-cell receptor- mediated signaling, making it a useful drug for treating leprosy reactions and possibly other autoimmune processes.Фармаколо?гия
Clofazimine is a substituted iminophenazine that was first proposed for treating leprosy in 1962; however, it entered into medical practice toward the end of the 1980s. The mechanisms of its action is not definitively known, although there is the assumption that it can inhibit the formation of matrixes with DNA, which leads to a delay in the growth of mycobacteria. Clofazimine exhibits a bactericidal effect between that of dapsone and rifampicin. Synonym of this drug is lamprene.Фармакокине?тика
Clofazimine is well absorbed by the intestine and is taken up by adipose tissue and cells of the macrophage/monocyte series, including those in the intestinal wall. It has a very long half-life (variously estimated as 10–70 days) and is eliminated, mostly unchanged, in the urine and feces.Клиническое использование
Multibacillary leprosy (in combination with other anti-leprosy drugs)Erythema nodosum leprosum (anti-inflammatory activity)
Clofazimine has been suggested as a drug for treatment of MDR tuberculosis, although its efficacy is unproven. It has been used to treat M. ulcerans infection (Buruli ulcer) but with limited responses. Use in disease caused by mycobacteria of the M. avium complex is no longer recommended as more effective and less toxic alternative agents are available.
Побочные эффекты
Clofazimine is usually well tolerated, but some patients develop nausea, abdominal pain and diarrhea, relieved to some extent by taking the drug with a meal or glass of milk. Dose-related, reversible, skin discoloration is very common and is unacceptable to some patients. Discoloration of the hair, cornea, urine, sweat and tears also occurs. Infants born to mothers receiving clofazimine are reversibly pigmented at birth. Edema of the wall of the small intestine leading to subacute obstruction is a rare but serious complication of prolonged high-dose therapy for leprosy reactions. Deposition of clofazimine in lymph nodes may interfere with lymphatic drainage, occasionally manifesting as edema of the feet.Методы очистки
Clofazimine recrystallises from acetone as dark red crystals. Its solubility in CHCl3 and EtOH is 7% and 0.1%, respectively,at room temperature. It is insoluble in H2O. It is antibacterial. [Barry et al. J Chem Soc 859 1958, Beilstein 25 III/IV 3033.]Клофазимин запасные части и сырье
Клофазимин поставщик
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