Clofazimine
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Clofazimine
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| Systematic (IUPAC) name | |
| N,5-bis(4-chlorophenyl)-3- (1-methylethylimino)-5H-phenazin-2-amine | |
| Identifiers | |
| CAS number | |
| ATC code | J04 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C27H22Cl2N4 |
| Mol. mass | 473.396 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | 70 days |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
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). (From AMA Drug Evaluations Annual, 1993, p1619).
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[edit] History
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.
[edit] 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.
[edit] 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. Cases of icthyosis are also reported due to this drug
[edit] External links
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