The red dye clofazimine is applied as a drug in human medicine to treat a leprosy disease. The active ingredient is suitable for this purpose because of its bactericidal properties. Off-label, i.e., outside the scope of approval, there is also an area of application for the treatment of massive diseases of the skin.
What is clofazimine?
Clofazimine is a red dye. This is used to treat leprosy due to its bacteria-killing effect (bactericidal properties). In addition, there is a field of application for the drug that exceeds the scope of approval. This is because it is used outside the area approved by the regulatory authorities under public law (so-called off-label use) to treat serious skin diseases. According to the defined field of application, clofazimine is to be used together with other leprosy drugs in order to prevent the development of resistance. These include, for example, dapsone or rifampicin. In chemistry and pharmacology, clofazimine is described by the molecular formula C 27 – H 22 – Cl 2 – N 4. This corresponds approximately to a moral mass of 473.39 g/mol. The literature reports that the chemical properties of clofazimine are very similar to those of cationic amphiphilic drugs (CAD).
Pharmacological effects on body and organs
The exact effect of clofazimine on the human body has not yet been fully elucidated. Various approaches have been developed in science to explain the bactericidal effects of the red dye. However, all explanatory models have in common that they understand clofazimine as a functional inhibitor of acid sphingomyelinase (FIASMA). It is thus considered certain that clofazimine causes inhibition of the enzyme acid sphingomyelinase. The red dye is also indisputably considered to be at least slightly bactericidal. Apart from the mechanism of action, clofazimine can be regarded as well researched. The melting point of the substance, which is a brownish powder at room temperature, is about 212 degrees Celsius.
Medical application and use for treatment and prevention.
Clofazimine is still approved within the European Union only in France. Here, the active ingredient is sold under the trade name Lamprene. In the Federal Republic of Germany, this preparation could be imported from abroad by pharmacies until 2005. Since several changes in the law, which led among other things to the loss of approval, clofazimine can now only be obtained from the WHO. In exceptional cases, direct purchase from the manufacturer is also possible. In France and other countries where approval exists, clofazimine is used primarily for the treatment of leprosy. The active ingredient is prescribed for oral administration as a film-coated tablet and is subject to pharmacy and prescription regulations. It can therefore only be obtained from a state-licensed pharmacy following a doctor’s prescription. Clofazimine is also indicated for the treatment of leprosy. In this case, however, the therapy is always carried out together with other drugs such as rifampicin or dapsone. Off-label use is also possible as a drug for the treatment of massive skin diseases. These include granulomatous mycoses and Melkersson-Rosenthal syndrome.
Risks and side effects
Clofazimine may cause unwanted side effects even when taken completely as directed. However, this is also true for other drugs. It is mandatory to refrain from use if there is a known intolerance or allergy to the active ingredient. According to the literature, it has been proven in numerous studies that there is a connection between the intake of clofazimine and the development of skin discoloration. In some subjects, increased formation of red or brown-black spots occurred, especially in light-exposed areas. In addition, discoloration of the stool, urine, sputum or hair may also occur. Discoloration of sweat has also been reported. Furthermore, after taking clofazimine, disorders of keratinization of the skin (in technical terms: ichthyosis) may occur. Other side effects are disorders of the gastrointestinal tract, which primarily manifest themselves as diarrhea, abdominal or stomach pain, vomiting, and loss of appetite. The development of pathogenically increased photosensitivity is also a potential side effect to be considered.
