Clofazimine

Clofazimine 속성

Clofazimine C화학적 특성, 용도, 생산

화학적 성질

Red Solid

용도

antiinflammatory, glucocorticoid

정의

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.

Indications

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.

Antimicrobial activity

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.

Pharmaceutical Applications

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.

Pharmacology

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.

Pharmacokinetics

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.

Clinical Use

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.

부작용

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.

Purification Methods

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.]

Clofazimine 준비 용품 및 원자재

원자재

준비 용품

Clofazimine 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21686	55
Hangzhou FandaChem Co.,Ltd.	008657128800458; +8615858145714	fandachem@gmail.com	China	9338	55
career henan chemical co	+86-0371-86658258 15093356674;	sales@coreychem.com	China	29914	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	967	58
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28180	58
Chongqing Chemdad Co., Ltd	+86-023-6139-8061 +86-86-13650506873	sales@chemdad.com	China	39916	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49391	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
Hefei TNJ Chemical Industry Co.,Ltd.	0551-65418671	sales@tnjchem.com	China	34571	58
Chemsigma International Co., Ltd.	+86-18136843612 +86-19951791336	info@chemsigma.com	China	1229	58

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