From the Guidelines
Clofazimine's mechanism of action is not fully understood, but it is believed to have both antimycobacterial and anti-inflammatory properties, making it effective in treating mycobacterial infections, particularly in multidrug-resistant cases of leprosy and tuberculosis. The exact mechanism of action of clofazimine is not known, but it is thought to be a prodrug that appears to have both antimycobacterial and antiinflammatory properties 1. Some of the key points about clofazimine's mechanism of action include:
- It has been shown to have in vitro and in vivo activity as a sterilizing drug to treat MDR-TB 1
- It is a lipophilic riminophenazine antibiotic, which allows it to accumulate in macrophages where mycobacteria often reside, enhancing its effectiveness against intracellular pathogens 1
- It has been used to treat leprosy and has been shown to be effective in treating MDR-TB in adults in observational studies and in a nonplacebo randomized controlled trial 1
- The main adverse events associated with clofazimine include prolongation of the QTc interval, and reversible skin pigmentation 1
- The WHO has included clofazimine as part of the “other core second-line agents” that can be used to build a treatment regimen of at least four effective drugs 1
- The recommended dose of clofazimine is 100–200 mg once daily (oral) for adults, and 3–5 mg/kg/day (maximum 100 mg/day) for children 1
From the Research
Mechanism of Action of Clofazimine
- The primary mechanism of action of clofazimine is not fully understood, but it is thought to involve the intercalation of clofazimine with bacterial DNA 2.
- Clofazimine has also been shown to increase levels of cellular phospholipase A2, which may contribute to its antibacterial activity 2.
- Clofazimine has anti-inflammatory and immunosuppressive properties, which may also play a role in its effectiveness against leprosy and other diseases 3.
Bactericidal Activity of Clofazimine
- Clofazimine is active in vivo against M. leprae and in vitro against Mycobacterium avium complex (MAC) 3.
- Clofazimine is used as part of multidrug therapy to treat leprosy, and it has been shown to be effective in reducing the incidence and severity of erythema nodosum leprosum reactions 3.
- The bactericidal activity of clofazimine is often used in combination with other drugs, such as dapsone and rifampicin, to treat multibacillary leprosy 4, 5, 6.