Clofazimine is an antimicrobial drug mainly used to treat leprosy (Hansen’s disease) and certain mycobacterial infections, including some types of tuberculosis. It is part of the phenazine dye class and possesses both antibacterial and anti-inflammatory effects. Clofazimine, sold under the brand name Lamprene, received FDA approval in the U.S. in December 1986 for leprosy treatment. However, it was withdrawn from the U.S. market in 2004 and is no longer available for commercial sale in pharmacies.
BRAND NAME:
Lamprene - It is available as oral tablets with drug composition clofazimine 50mg.
MECHANISM OF ACTION:
Clofazimine primarily acts by binding to mycobacterial DNA, disrupting the replication and transcription processes crucial for bacterial survival. This interference inhibits bacterial growth and replication.In addition, clofazimine produces reactive oxygen species (ROS) within the bacteria, which enhances its bactericidal effect by damaging bacterial cellular components.Moreover, clofazimine possesses anti-inflammatory properties that help decrease the immune response and inflammation linked to leprosy.
PHARMACOKINETICS:
Absorption: Clofazimine is absorbed slowly and variably from the gastrointestinal tract after oral administration. Its bioavailability can be influenced by food intake.
Distribution: It is highly lipophilic and extensively distributed in body tissues, especially in fatty tissues, skin, liver, and spleen. Clofazimine accumulates in macrophages and reticuloendothelial tissues, leading to a prolonged half-life.
Metabolism: Clofazimine undergoes minimal metabolism in the body.
Elimination: The drug is primarily eliminated via the bile into the feces, with only a small amount excreted in the urine. Due to tissue accumulation, it has a very long terminal half-life, ranging from several weeks to months.
PHARMACODYNAMICS:
Clofazimine produces its antimicrobial action by binding to mycobacterial DNA, interfering with DNA replication and transcription processes, thereby inhibiting bacterial growth and reproduction. Additionally, it generates reactive oxygen species (ROS) within the bacteria, causing oxidative damage that contributes to its bactericidal activity. Beyond its antimicrobial properties, clofazimine also has anti-inflammatory effects, which help reduce inflammation and immune-mediated tissue damage associated with diseases like leprosy. Its accumulation in macrophages and tissues enhances both its antimicrobial and anti-inflammatory actions, contributing to its prolonged therapeutic effects.
DOSAGE AND ADMINISTRATION:
Typical Adult Dosage:
- Multibacillary Leprosy:
100 mg taken orally once daily, along with a supervised dose of 300 mg once a month. - Paucibacillary Leprosy:
Used in combination with other medications according to established treatment protocols.
Administration:
Clofazimine is given orally and is best taken with food to enhance absorption.
The duration of treatment is generally long-term, often lasting from several months to a few years, depending on the severity and type of infection.
DRUG INTERACTIONS:
Some drugs should be avoid while taking clofazimine as it get interact with other drugs causing adverse effects. Below are the some drugs mentioned that should be avoid while taking clofazimine.
Antibiotics - Azithromycin, Trimethoprim, sulfamethoxazole, trimethoprim
Antacids – Aluminium hydroxide, magnesium hydroxide, simethicone
FOOD INTERACTIONS:
Avoid taking alcohol.
CONTRAINDICATIONS:
Contraindicated in patients with hypersensitivity to clofazimine and severe gastrointestinal disorders.
ADVERSE EFFECTS:
- Loss of appetite
- Nausea
- Discoloration
- Diarrhea
- Change in taste
- Fever
- Headaches
- Hives
- Jaundice
OVERDOSE:
Taking overdose of clofazimine can cause some toxic effects.
- Cardiotoxicity
- Phototoxicity
- Change in skin colour
