Clofazimine: Difference between revisions
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{{drugbox | {{drugbox | ||
| IUPAC_name = ''N'',5-bis(4-chlorophenyl)-3- (1-methylethylimino)-5''H''-phenazin-2-amine | | IUPAC_name = ''N'',5-bis(4-chlorophenyl)-3- (1-methylethylimino)-5''H''-phenazin-2-amine | ||
| image = Clofazimine. | | image = Clofazimine Wiki Str.png | ||
| width = 150 | | width = 150 | ||
| CAS_number = 2030-63-9 | | CAS_number = 2030-63-9 | ||
| Line 20: | Line 20: | ||
}} | }} | ||
__NOTOC__ | __NOTOC__ | ||
{{CMG}} | {{CMG}} | ||
==Overview== | ==Overview== | ||
Clofazimine is a fat-soluble riminophenazine dye used in combination with [[rifampicin]] and [[dapsone]] as multidrug therapy (MDT) for the treatment of [[leprosy]]. It has been used investigationally in combination with other antimycobacterial drugs to treat [[Mycobacterium avium]] infections in [[AIDS]] patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, [[erythema]] nodosum leprosum (ENL).<ref>{{cite book | last = LastName | first = FirstName | title = Drug evaluations annual 1993 | publisher = American Medical Association | location = Chicago, Ill | year = 1992 | isbn = 0899704980 }}</ref> | |||
==Category== | |||
Antimycobacterial | |||
==US Brand Names== | |||
LAMPRENE<sup>®</sup> ('''''DISCONTINUED''''') | |||
== | ==Historical Perspective== | ||
Clofazimine, initially known as B663, was first synthesised in 1954 by a team led by Dr Vincent Barry at [[Trinity College, Dublin]] as an anti-tuberculosis drug. The drug proved ineffective against tuberculosis but in 1959 a researcher named Chang identified its effectiveness against leprosy. After clinical trials in Nigeria and elsewhere during the 1960s, some sponsored by the Swiss pharmaceutical company [[Geigy]] (today member of the [[Novartis]] group of drug producers), the product was launched in 1969 as Lamprene. | Clofazimine, initially known as B663, was first synthesised in 1954 by a team led by Dr Vincent Barry at [[Trinity College, Dublin]] as an anti-tuberculosis drug. The drug proved ineffective against tuberculosis but in 1959 a researcher named Chang identified its effectiveness against leprosy. After clinical trials in Nigeria and elsewhere during the 1960s, some sponsored by the Swiss pharmaceutical company [[Geigy]] (today member of the [[Novartis]] group of drug producers), the product was launched in 1969 as Lamprene. | ||
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==Supply== | ==Supply== | ||
Clofazimine is marketed under the trade name | Clofazimine is marketed under the trade name Lamprene<sup>®</sup> by Novartis. One of the only suppliers of Clofazimine Active Pharmaceutical Ingredient in the world is Sangrose Laboratories, located at Mavelikara in the southern Indian state of Kerala. | ||
==Metabolism== | ==Metabolism== | ||
Clofazimine has a very long half life of about 70 days. Clofazimine produces pink to brownish skin pigmentation in 75-100% of patients within a few weeks. | Clofazimine has a very long half life of about 70 days. Clofazimine produces pink to brownish skin pigmentation in 75-100% of patients within a few weeks. | ||
==Mechanism of Action== | |||
Clofazimine exerts a slow bactericidal effect on ''[[Mycobacterium leprae]]''. It inhibits mycobacterial growth and binds preferentially to mycobacterial DNA. It also exerts anti-inflammatory properties in controlling erythema nodosum leprosum reactions. However, its precise mechanisms of action are unknown. | |||
==External links== | ==External links== | ||
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*[http://www.rxlist.com/cgi/generic3/clofazimine.htm RxList Clofazimine (most information taken from FDA)] | *[http://www.rxlist.com/cgi/generic3/clofazimine.htm RxList Clofazimine (most information taken from FDA)] | ||
[[Category:Drugs]] | |||
[[Category:Antibiotics]] | [[Category:Antibiotics]] | ||
[[Category:Wikinfect]] | [[Category:Wikinfect]] | ||
Latest revision as of 12:26, 9 April 2015
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| Clinical data | |
|---|---|
| ATC code | |
| Pharmacokinetic data | |
| Elimination half-life | 70 days |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| DrugBank | |
| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
| Chemical and physical data | |
| Formula | C27H22Cl2N4 |
| Molar mass | 473.396 g/mol |
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Overview
Clofazimine is a fat-soluble riminophenazine dye used in combination with rifampicin and dapsone as multidrug therapy (MDT) for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum (ENL).[1]
Category
Antimycobacterial
US Brand Names
LAMPRENE® (DISCONTINUED)
Historical Perspective
Clofazimine, initially known as B663, was first synthesised in 1954 by a team led by Dr Vincent Barry at Trinity College, Dublin as an anti-tuberculosis drug. The drug proved ineffective against tuberculosis but in 1959 a researcher named Chang identified its effectiveness against leprosy. After clinical trials in Nigeria and elsewhere during the 1960s, some sponsored by the Swiss pharmaceutical company Geigy (today member of the Novartis group of drug producers), the product was launched in 1969 as Lamprene.
The U.S. government named Clofazimine an orphan drug in June 1986. Geigy gained FDA approval for the drug in December 1986.
Supply
Clofazimine is marketed under the trade name Lamprene® by Novartis. One of the only suppliers of Clofazimine Active Pharmaceutical Ingredient in the world is Sangrose Laboratories, located at Mavelikara in the southern Indian state of Kerala.
Metabolism
Clofazimine has a very long half life of about 70 days. Clofazimine produces pink to brownish skin pigmentation in 75-100% of patients within a few weeks.
Mechanism of Action
Clofazimine exerts a slow bactericidal effect on Mycobacterium leprae. It inhibits mycobacterial growth and binds preferentially to mycobacterial DNA. It also exerts anti-inflammatory properties in controlling erythema nodosum leprosum reactions. However, its precise mechanisms of action are unknown.
External links
- ↑ LastName, FirstName (1992). Drug evaluations annual 1993. Chicago, Ill: American Medical Association. ISBN 0899704980.
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- E number from Wikidata
- ECHA InfoCard ID from Wikidata
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- Wikinfect